| 1. |
- Thomas, HS, et al.
(author)
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- 2019
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swepub:Mat__t
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| 2. |
- Abd El-Wahed, Aida A., et al.
(author)
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Cosmetic Applications of Bee Venom
- 2021
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In: Toxins. - : MDPI AG. - 2072-6651. ; 13:11
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Research review (peer-reviewed)abstract
- Bee venom (BV) is a typical toxin secreted by stingers of honeybee workers. BV and BV therapy have long been attractive to different cultures, with extensive studies during recent decades. Nowadays, BV is applied to combat several skin diseases, such as atopic dermatitis, acne vulgaris, alopecia, vitiligo, and psoriasis. BV is used extensively in topical preparations as cosmetics and used as dressing for wound healing, as well as in facemasks. Nevertheless, the safety of BV as a therapeutic choice has always been a concern due to the immune system reaction in some people due to BV use. The documented unfavorable impact is explained by the fact that the skin reactions to BV might expand to excessive immunological responses, including anaphylaxis, that typically resolve over numerous days. This review aims to address bee venom therapeutic uses in skin cosmetics.
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| 3. |
- Arshad, Nasima, et al.
(author)
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Synthesis, X-ray, Hirshfeld surface analysis, exploration of DNA binding, urease enzyme inhibition and anticancer activities of novel adamantane-naphthyl thiourea conjugate
- 2021
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In: Bioorganic chemistry (Print). - : Elsevier. - 0045-2068. ; 109
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Journal article (peer-reviewed)abstract
- 1-(adamantane-1-carbonyl-3-(1-naphthyl)) thiourea (C22H24N2OS (4), was synthesized by the reaction of freshly prepared adamantane-1-carbonyl chloride from corresponding acid (3) with ammonium thiocyanate in 1:1 M ratio in dry acetone to afford the adamantane-1-carbonyl isothiocyanate (2) in situ followed by treatment with 1-naphthyl amine (3). The structure was established by elemental analyses, FTIR, H-1, C-13 NMR and mass spectroscopy. The molecular and crystal structure were determined by single crystal X-ray analysis. It belongs to triclinic system P - 1 space group with a = 6.7832(5) angstrom, b = 11.1810(8) angstrom, c = 13.6660(10) angstrom, alpha = 105.941(6)degrees, beta = 103.730(6)degrees, gamma = 104.562(6)degrees, Z = 2, V = 910.82(11) angstrom(3). The naphthyl group is almost planar. In the crystal structure, intermolecular C-H center dot center dot center dot O hydrogen bonds link the molecules into centrosymmetric dimers, enclosing R-2(2)(14) ring motifs, while the intramolecular N-H center dot center dot center dot O hydrogen bonds enclose S(6) ring motifs, in which they may be effective in the stabilization of the structure. The Hirshfeld surface analysis of the crystal structure indicates that the most important contributions for the crystal packing are from H center dot center dot center dot H (59.3%), H center dot center dot center dot C/C center dot center dot center dot H (19.8%) and H center dot center dot center dot S/S center dot center dot center dot H (10.1%) interactions. Hydrogen bonding and van der Waals interactions are the dominant interactions in the crystal packing. DFT, molecular docking and urease inhibition studies revealed stability and electron withdrawing nature of 4 as compared to DNA base pairs and residues of urease. The DNA binding results from docking, UV-visible spectroscopy, and viscosity studies indicated significant binding of 4 with the DNA via intercalation and groove binding. Further investigation of the compound was done on hepatocellular carcinoma; Huh-7 cell line as well as normal human embryonic kidney; Hek-293 cell line. The compound showed significant cytotoxic activity against Huh-7 cells in comparison to normal Hek-293 cells indicating selective cytotoxicity towards cancer cells.
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| 4. |
- Aziz, Hamid, et al.
(author)
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New polymorphs of 1-benzylidene thiosemicarbazides : crystal structure and hirshfeld surface analysis
- 2023
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In: Journal of the Iranian Chemical Society. - : Springer. - 1735-207X .- 1735-2428. ; 20, s. 1831-1842
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Journal article (peer-reviewed)abstract
- Thiosemicarbazides are sulfur-based nitrogen-rich donor ligands, characterized by p-delocalized electronic charge and flexible molecular chain. The flexible molecular chain and polydentate nature is responsible for their wide biological and synthetic profile to synthesize several classes of heterocycles. In this context, the molecular and crystal structures coupled with Hirshfeld surface (HS) analysis of benzylidene thiosemicarbazides: (E)-2-(4-hydroxybenzylidene) hydrazine-1-carbothioamide, (3a) and (E)-2-(3-nitrobenzylidene) hydrazine-1-carbothioamide, (3b) are reported. Consequently, single crystal x-ray revealed interesting results, and the analyzed compounds were found to be polymorphs of the previously reported structures each having widely different unit cell. Briefly, compound (3a) crystallized with a single molecule in the asymmetric unit whereas its polymorph has six. In contrast, compound (3b) crystallized with Z = 2 having single molecule in asymmetric unit of the polymorph. Subsequently, HS analysis successfully visualized, explored, and quantified weak interactions present in the crystal lattices of the polymorphs. HS analysis revealed oxygen atoms of the nitro group significantly influence HS of molecule (3b).
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| 5. |
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| 6. |
- Channar, Pervaiz Ali, et al.
(author)
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Synthesis of aryl pyrazole via Suzuki coupling reaction, in vitro mushroom tyrosinase enzyme inhibition assay and in silico comparative molecular docking analysis with Kojic acid
- 2018
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In: Bioorganic chemistry (Print). - : ACADEMIC PRESS INC ELSEVIER SCIENCE. - 0045-2068. ; 79, s. 293-300
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Journal article (peer-reviewed)abstract
- Aryl pyrazoles are well recognized class of heterocyclic compounds found in several commercially available drugs. Owing to their significance in medicinal chemistry, in this current account we have synthesized a series of suitably substituted aryl pyrazole by employing Suzuki cross-coupling reaction. All compounds were evaluated for inhibition of mushroom tyrosinase enzyme both in vitro and in silico. Compound 3f (IC50 = 1.568 +/- 0.01 mu M) showed relatively better potential compared to reference kojic acid (IC50 = 16.051 +/- 1.27 mu M). A comparative docking studies showed that compound 3f have maximum binding affinity against mushroom tyrosinase (PDBID: 2Y9X) with binding energy value (-6.90 kcal/mol) as compared to Kojic acid. The 4-methoxy group in compound 3f shows 100% interaction with Cu. Compound 3f displayed hydrogen binding interaction with His61 and His94 at distance of 1.71 and 1.74 angstrom which might be responsible for higher activity compared to Kojic acid.
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| 7. |
- Drake, TM, et al.
(author)
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Surgical site infection after gastrointestinal surgery in children: an international, multicentre, prospective cohort study
- 2020
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In: BMJ global health. - : BMJ. - 2059-7908. ; 5:12
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Journal article (peer-reviewed)abstract
- Surgical site infection (SSI) is one of the most common healthcare-associated infections (HAIs). However, there is a lack of data available about SSI in children worldwide, especially from low-income and middle-income countries. This study aimed to estimate the incidence of SSI in children and associations between SSI and morbidity across human development settings.MethodsA multicentre, international, prospective, validated cohort study of children aged under 16 years undergoing clean-contaminated, contaminated or dirty gastrointestinal surgery. Any hospital in the world providing paediatric surgery was eligible to contribute data between January and July 2016. The primary outcome was the incidence of SSI by 30 days. Relationships between explanatory variables and SSI were examined using multilevel logistic regression. Countries were stratified into high development, middle development and low development groups using the United Nations Human Development Index (HDI).ResultsOf 1159 children across 181 hospitals in 51 countries, 523 (45·1%) children were from high HDI, 397 (34·2%) from middle HDI and 239 (20·6%) from low HDI countries. The 30-day SSI rate was 6.3% (33/523) in high HDI, 12·8% (51/397) in middle HDI and 24·7% (59/239) in low HDI countries. SSI was associated with higher incidence of 30-day mortality, intervention, organ-space infection and other HAIs, with the highest rates seen in low HDI countries. Median length of stay in patients who had an SSI was longer (7.0 days), compared with 3.0 days in patients who did not have an SSI. Use of laparoscopy was associated with significantly lower SSI rates, even after accounting for HDI.ConclusionThe odds of SSI in children is nearly four times greater in low HDI compared with high HDI countries. Policies to reduce SSI should be prioritised as part of the wider global agenda.
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| 8. |
- El-Garawani, Islam M., et al.
(author)
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In Vitro Induction of Apoptosis in Isolated Acute Myeloid Leukemia Cells : The Role of Anastatica hierochuntica Methanolic Extract
- 2022
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In: Metabolites. - : MDPI AG. - 2218-1989 .- 2218-1989. ; 12:9
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Journal article (peer-reviewed)abstract
- Anastatica hierochuntica L. (Cruciferae) has been known in Egyptian folk medicine as a remedy for gastrointestinal disorders, diabetes and heart diseases. Despite the wide usage, A. hierochuntica research provides insufficient data to support its traditional practice. The cytotoxicity of A. hierochuntica methanolic extract was investigated on acute myeloid leukemia blasts (AML) and normal human peripheral leucocytes (NHPL). The phytochemical identification of bioactive compounds using 1H-NMR and LC-ESI-MS was also performed. A. hierochuntica extract caused non-significant cytotoxicity on NHPL, while the cytotoxicity on AML was significant (IC50: 0.38 ± 0.02 μg/mL). The negative expression of p53, upregulation of Caspase-3 and increase in the BAX/BCL-2 ratio were reported at the protein and mRNA levels. The results suggest that A. hierochuntica extract induced AML cell death via the p53-independent mitochondrial intrinsic pathway and further attention should be paid to this plant as a promising natural anticancer agent.
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| 9. |
- El-Seedi, Hesham, et al.
(author)
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A Spotlight on the Egyptian Honeybee (Apis mellifera lamarckii)
- 2022
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In: Animals. - : MDPI AG. - 2076-2615. ; 12:20
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Research review (peer-reviewed)abstract
- Egypt has an ongoing long history with beekeeping, which started with the ancient Egyptians making various reliefs and inscriptions of beekeeping on their tombs and temples. The Egyptian honeybee (Apis mellifera lamarckii) is an authentic Egyptian honeybee subspecies utilized in apiculture. A. m. lamarckii is a distinct honeybee subspecies that has a particular body color, size, and high levels of hygienic behavior. Additionally, it has distinctive characteristics; including the presence of the half-queens, an excessive number of swarm cells, high adaptability to climatic conditions, good resistance to specific bee diseases, including the Varro disorder, and continuous breeding during the whole year despite low productivity, using very little propolis, and tending to abscond readily. This review discusses the history of beekeeping in Egypt and its current situation in addition to its morphology, genetic analysis, and distinctive characters, and the defensive behaviors of native A. m. lamarckii subspecies.
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| 10. |
- El-Seedi, Hesham, et al.
(author)
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Bee Stressors from an Immunological Perspective and Strategies to Improve Bee Health
- 2022
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In: Veterinary Sciences. - : MDPI AG. - 2306-7381. ; 9:5
-
Journal article (peer-reviewed)abstract
- Honeybees are the most prevalent insect pollinator species; they pollinate a wide range of crops. Colony collapse disorder (CCD), which is caused by a variety of biotic and abiotic factors, incurs high economic/ecological loss. Despite extensive research to identify and study the various ecological stressors such as microbial infections, exposure to pesticides, loss of habitat, and improper beekeeping practices that are claimed to cause these declines, the deep understanding of the observed losses of these important insects is still missing. Honeybees have an innate immune system, which includes physical barriers and cellular and humeral responses to defend against pathogens and parasites. Exposure to various stressors may affect this system and the health of individual bees and colonies. This review summarizes and discusses the composition of the honeybee immune system and the consequences of exposure to stressors, individually or in combinations, on honeybee immune competence. In addition, we discuss the relationship between bee nutrition and immunity. Nutrition and phytochemicals were highlighted as the factors with a high impact on honeybee immunity.
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| 11. |
- El-Seedi, Hesham, et al.
(author)
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Chemistry and the Potential Antiviral, Anticancer, and Anti-Inflammatory Activities of Cardiotonic Steroids Derived from Toads
- 2022
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In: Molecules. - : MDPI AG. - 1431-5157 .- 1420-3049. ; 27:19
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Research review (peer-reviewed)abstract
- Cardiotonic steroids (CTS) were first documented by ancient Egyptians more than 3000 years ago. Cardiotonic steroids are a group of steroid hormones that circulate in the blood of amphibians and toads and can also be extracted from natural products such as plants, herbs, and marines. It is well known that cardiotonic steroids reveal effects against congestive heart failure and atrial fibrillation; therefore, the term cardiotonic has been coined. Cardiotonic steroids are divided into two distinct groups: cardenolides (plant-derived) and bufadienolides (mainly of animal origin). Cardenolides have an unsaturated five-membered lactone ring attached to the steroid nucleus at position 17; bufadienolides have a doubly unsaturated six-membered lactone ring. Cancer is a leading cause of mortality in humans all over the world. In 2040, the global cancer load is expected to be 28.4 million cases, which would be a 47% increase from 2020. Moreover, viruses and inflammations also have a very nebative impact on human health and lead to mortality. In the current review, we focus on the chemistry, antiviral and anti-cancer activities of cardiotonic steroids from the naturally derived (toads) venom to combat these chronic devastating health problems. The databases of different research engines (Google Scholar, PubMed, Science Direct, and Sci-Finder) were screened using different combinations of the following terms: cardiotonic steroids, anti-inflammatory, antiviral, anticancer, toad venom, bufadienolides, and poison chemical composition. Various cardiotonic steroids were isolated from diverse toad species and exhibited superior anti-inflammatory, anticancer, and antiviral activities in in vivo and in vitro models such as marinobufagenin, gammabufotalin, resibufogenin, and bufalin. These steroids are especially difficult to identify. However, several compounds and their bioactivities were identified by using different molecular and biotechnological techniques. Biotechnology is a new tool to fully or partially generate upscaled quantities of natural products, which are otherwise only available at trace amounts in organisms.
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| 12. |
- El-Seedi, Hesham, et al.
(author)
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Exploring natural products-based cancer therapeutics derived from egyptian flora
- 2021
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In: Journal of Ethnopharmacology. - : Elsevier BV. - 0378-8741 .- 1872-7573. ; 269
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Research review (peer-reviewed)abstract
- Ethnopharmacological relevance: Egyptian plants are a rich source of natural molecules, representing considerable biodiversity due to climate variations between the Northern, Southern, Eastern and Western regions of the country. Sinai is considered a precious nature reserves preserving flora, fauna, marine organisms, and historical habitats with ancient origins. Here, traditional medicinal approaches have been used for hundreds of years. Healthy lifestyles, low levels of stress and microbial infections, and a dependence on flora and herbal medicine might in combination explain why the burden of cancer is lower in some regions than in others.Aim of the study: The primary aim of this review is to document the plants and natural products that are used as foods and medicines in Egypt, in general, and in Sinai, in particular, with a focus on those with demonstrated anticancer activities. The documented traditional uses of these plants are described, together with their chemical and pharmacological activities and the reported outcomes of clinical trials against cancer.Materials and methods: A literature search was performed to identify texts describing the medicinal plants that are cultivated and grown in Egypt, including information found in textbooks, published articles, the plant list website (http://www.theplantlist.org/), the medicinal plant names services website (http://mpns.kew.org/mpns-portal/), and web databases (PubMed, Science Direct, and Google Scholar).Results and discussion: We collected data for most of the plants cultivated or grown in Egypt that have been previously investigated for anticancer effects and reported their identified bioactive elements. Several plant species, belonging to different families and associated with 67 bioactive compounds, were investigated as potential anticancer agents (in vitro studies). The most potent cytotoxic activities were identified for the families Asteraceae, Lamiaceae, Chenopodiaceae, Apocynaceae, Asclepiadaceae, Euphorbiaceae, Gramineae, and Liliaceae. The anticancer activities of some species, such as Punica granatum L., Nerium oleander L., Olea europea L., Matricaria chamomilla L., Cassia acutifolia L., Nigella sativa L., Capsicum frutescens L., Withania somnifera L., and Zingiber officinale Roscoe, have been examined in clinical trials. Among the various Egyptian plant habitats, we found that most of these plants are grown in the North Sinai, New-Delta, and Giza Governorates.Conclusion: In this review, we highlight the role played by Egyptian flora in current medicinal therapies and the possibility that these plants may be examined in further studies for the development of anticancer drugs. These bioactive plant extracts form the basis for the isolation of phytochemicals with demonstrated anticancer activities. Some active components derived from these plants have been applied to preclinical and clinical settings, including resveratrol, quercetin, isoquercetin, and rutin.
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| 13. |
- El-Seedi, Hesham, et al.
(author)
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Insights into the Role of Natural Products in the Control of the Honey Bee Gut Parasite (Nosema spp.)
- 2022
-
In: Animals. - : MDPI AG. - 2076-2615. ; 12:21
-
Research review (peer-reviewed)abstract
- The honey bee is an important economic insect due to its role in pollinating many agricultural plants. Unfortunately, bees are susceptible to many pathogens, including pests, parasites, bacteria, and viruses, most of which exert a destructive impact on thousands of colonies. The occurrence of resistance to the therapeutic substances used against these organisms is rising, and the residue from these chemicals may accumulate in honey bee products, subsequently affecting the human health. There is current advice to avoid the use of antibiotics, antifungals, antivirals, and other drugs in bees, and therefore, it is necessary to develop alternative strategies for the treatment of bee diseases. In this context, the impact of nosema diseases (nosemosis) on bee health and the negative insults of existing drugs are discussed. Moreover, attempts to combat nosema through the use of alternative compounds, including essential oils, plant extracts, and microbes in vitro and in vivo, are documented.
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| 14. |
- El-Seedi, Hesham, et al.
(author)
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Metal nanoparticles fabricated by green chemistry using natural extracts : biosynthesis, mechanisms, and applications
- 2019
-
In: RSC Advances. - : Royal Society of Chemistry. - 2046-2069. ; 9:42, s. 24539-24559
-
Research review (peer-reviewed)abstract
- Nanoparticles (NPs) are new inspiring clinical targets that have emerged from persistent efforts with unique properties and diverse applications. However, the main methods currently utilized in their production are not environmentally friendly. With the aim of promoting a green approach for the synthesis of NPs, this review describes eco-friendly methods for the preparation of biogenic NPs and the known mechanisms for their biosynthesis. Natural plant extracts contain many different secondary metabolites and biomolecules, including flavonoids, alkaloids, terpenoids, phenolic compounds and enzymes. Secondary metabolites can enable the reduction of metal ions to NPs in eco-friendly one-step synthetic processes. Moreover, the green synthesis of NPs using plant extracts often obviates the need for stabilizing and capping agents and yields biologically active shape- and size-dependent products. Herein, we review the formation of metallic NPs induced by natural extracts and list the plant extracts used in the synthesis of NPs. In addition, the use of bacterial and fungal extracts in the synthesis of NPs is highlighted, and the parameters that influence the rate of particle production, size, and morphology are discussed. Finally, the importance and uniqueness of NP-based products are illustrated, and their commercial applications in various fields are briefly featured.
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| 15. |
- El-Seedi, Hesham R., et al.
(author)
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Essential oils of aromatic Egyptian plants repel nymphs of the tick Ixodes ricinus (Acari : Ixodidae)
- 2017
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In: Experimental & applied acarology. - : Springer. - 0168-8162 .- 1572-9702. ; 73:1, s. 139-157
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Journal article (peer-reviewed)abstract
- Due to the role of Ixodes ricinus (L.) (Acari: Ixodidae) in the transmission of many serious pathogens, personal protection against bites of this tick is essential. In the present study the essential oils from 11 aromatic Egyptian plants were isolated and their repellent activity against I. ricinus nymphs was evaluated Three oils (i.e. Conyza dioscoridis L., Artemisia herba-alba Asso and Calendula officinalis L.) elicited high repellent activity in vitro of 94, 84.2 and 82%, respectively. The most active essential oil (C. dioscoridis) was applied in the field at a concentration of 6.5 A mu g/cm(2) and elicited a significant repellent activity against I. ricinus nymphs by 61.1%. The most repellent plants C. dioscoridis, C. officinalis and A. herba-alba yielded essential oils by 0.17, 0.11 and 0.14%, respectively. These oils were further investigated using gas chromatography-mass spectrometry analysis. alpha-Cadinol (10.7%) and hexadecanoic acid (10.5%) were the major components of C. dioscoridis whereas in C. officinalis, alpha-cadinol (21.2%) and carvone (18.2%) were major components. Artemisia herba-alba contained piperitone (26.5%), ethyl cinnamate (9.5%), camphor (7.7%) and hexadecanoic acid (6.9%). Essential oils of these three plants have a potential to be used for personal protection against tick bites.
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| 16. |
- El-Seedi, Hesham R., et al.
(author)
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Naturally Occurring Xanthones; Biological Activities, Chemical Profiles and In Silico Drug Discovery
- 2024
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In: Current Medicinal Chemistry. - : Bentham Science Publishers Ltd.. - 0929-8673 .- 1875-533X. ; 31:1, s. 62-101
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Research review (peer-reviewed)abstract
- Xanthones are widely distributed polyphenols, present commonly in higher plants; Garcinia, Calophyllum, Hypericum, Platonia, Mangifera, Gentiana and Swertia. Xanthone tricyclic scaffold is able to interact with different biological targets, showing antibacterial and cytotoxic effects, as well as potent effects against osteoarthritis, malaria, and cardiovascular diseases. Thus, in this article we focused on pharmacological effects, applications and preclinical studies with the recent updates of xanthon & PRIME;s isolated compounds from 2017-2020. We found that only a-mangostin, gambogic acid, and mangiferin, have been subjected to preclinical studies with particular emphasis on the development of anticancer, diabetes, antimicrobial and hepatoprotective therapeutics. Molecular docking calculations were performed to predict the binding affinities of xanthone-derived compounds against SARS-CoV-2 M-pro. According to the results, cratoxanthone E and morellic acid demonstrated promising binding affinities towards SARS-CoV-2 M-pro with docking scores of -11.2 and -11.0 kcal/mol, respectively. Binding features manifested the capability of cratoxanthone E and morellic acid to exhibit nine and five hydrogen bonds, respectively, with the key amino acids of the M-pro active site. In conclusion, cratoxanthone E and morellic acid are promising anti-COVID-19 drug candidates that warrant further detailed in vivo experimental estimation and clinical assessment.
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| 17. |
- El-Seedi, Hesham R., et al.
(author)
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Plants mentioned in the Islamic Scriptures (Holy Qur'an and Ahadith) : Traditional uses and medicinal importance in contemporary times
- 2019
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In: Journal of Ethnopharmacology. - : Elsevier. - 0378-8741 .- 1872-7573. ; 243
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Research review (peer-reviewed)abstract
- Ethnopharmacological relevance: Over the past thousand years, Islamic physicians have collected cultural, philosophical, sociological and historical backgrounds for understanding diseases and medications. The Prophet Mohammed (Peace Be Upon Him (PBUH) said: "There is no disease that Allah has created, except that Allah also has created its cure." Therefore, Islamic scholars are encouraged to explore and use both traditional and modern forms of medicine. Aim of the study: (1) To identify some of the medicinal plants mentioned in the Holy Qur'an and Ahadith textbooks of the period 700-1500 AD; (2) to compare them with presently used traditional medicines; (3) to evaluate their value based on modern research; and (4) to investigate the contributions of Islamic scholars to the development of the scientific branches, particularly medicine. Materials and methods: A literature search was performed relating to 12 medicinal plants mentioned in the Holy Qur'an and Ahadith using textbooks, Al-Azhar scholars, published articles, the plant list website (http://www.theplantlist.org/), the medicinal plant names services website (http://mpns.kew.org/mpns-portal/) and web databases (PubMed, Science Direct, and Google Scholar). Results and discussion: The Islamic Golden Age was a step towards modern medicine, with unique insights and multi-disciplinary aspects. Traditional Islamic Medicine has had a significant impact on the development of various medical, scientific and educational activities. Innumerable Muslim and non-Muslim physicians have built on the strong foundation of Traditional Islamic Medicine by translating the described natural remedies and effects. The influences of different ancient cultures on the traditional uses of natural products were also documented in Islamic Scriptures in the last part of the second millennium. The divine teachings of Islam combine natural and practical healing and incorporate inherited science and technology. Conclusion: In this review, we discuss Traditional Islamic Medicine with reference to both medical recommendations mentioned in the Holy Qur'an and Prophetic Traditional Medicine (al-Tibb al-Nabawi). Although the molecular mechanisms and functions of some of the listed medicinal plants and their derivatives have been intensively studied, some traditional remedies have yet to be translated into clinical applications.
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| 18. |
- El-Seedi, Hesham, et al.
(author)
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Saudi Arabian Plants : A Powerful Weapon against a Plethora of Diseases
- 2022
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In: PLANTS. - : MDPI AG. - 2223-7747. ; 11:24
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Research review (peer-reviewed)abstract
- The kingdom of Saudi Arabia (SA) ranks fifth in Asia in terms of area. It features broad biodiversity, including interesting flora, and was the historical origin of Islam. It is endowed with a large variety of plants, including many herbs, shrubs, and trees. Many of these plants have a long history of use in traditional medicine. The aim of this review is to evaluate the present knowledge on the plants growing in SA regarding their pharmacological and biological activities and the identification of their bioactive compounds to determine which plants could be of interest for further studies. A systematic summary of the plants’ history, distribution, various pharmacological activities, bioactive compounds, and clinical trials are presented in this paper to facilitate future exploration of their therapeutic potential. The literature was obtained from several scientific search engines, including Sci-Finder, PubMed, Web of Science, Google Scholar, Scopus, MDPI, Wiley publications, and Springer Link. Plant names and their synonyms were validated by ‘The Plant List’ on 1 October 2021. SA is home to approximately 2247 plant species, including native and introduced plants that belong to 142 families and 837 genera. It shares the flora of three continents, with many unique features due to its extreme climate and geographical and geological conditions. As plants remain the leading supplier of new therapeutic agents to treat various ailments, Saudi Arabian plants may play a significant role in the fight against cancer, inflammation, and antibiotic-resistant bacteria. To date, 102 active compounds have been identified in plants from different sites in SA. Plants from the western and southwestern regions have been evaluated for various biological activities, including antioxidant, anti-cancer, antimicrobial, antimalarial, anti-inflammatory, anti-glycation, and cytotoxic activities. The aerial parts of the plants, especially the leaves, have yielded most of the bioactive compounds. Most bioactivity tests involve in vitro assessments for the inhibition of the growth of tumour cell lines, and several compounds with in vitro antitumour activity have been reported. More in-depth studies to evaluate the mode of action of the compounds are necessary to pave the way for clinical trials. Ecological and taxonomical studies are needed to evaluate the flora of SA, and a plan for the conservation of wild plants should be implemented, including the management of the protection of endemic plants.
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| 19. |
- Khalifa, Shaden A. M., et al.
(author)
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Marine Natural Products : A Source of Novel Anticancer Drugs
- 2019
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In: Marine Drugs. - : MDPI AG. - 1660-3397. ; 17:9
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Journal article (peer-reviewed)abstract
- Cancer remains one of the most lethal diseases worldwide. There is an urgent need for new drugs with novel modes of action and thus considerable research has been conducted for new anticancer drugs from natural sources, especially plants, microbes and marine organisms. Marine populations represent reservoirs of novel bioactive metabolites with diverse groups of chemical structures. This review highlights the impact of marine organisms, with particular emphasis on marine plants, algae, bacteria, actinomycetes, fungi, sponges and soft corals. Anti-cancer effects of marine natural products in in vitro and in vivo studies were first introduced; their activity in the prevention of tumor formation and the related compound-induced apoptosis and cytotoxicities were tackled. The possible molecular mechanisms behind the biological effects are also presented. The review highlights the diversity of marine organisms, novel chemical structures, and chemical property space. Finally, therapeutic strategies and the present use of marine-derived components, its future direction and limitations are discussed.
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| 20. |
- Khalifa, Shaden A. M., et al.
(author)
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Recent insights into chemical and pharmacological studies of bee bread
- 2020
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In: Trends in Food Science & Technology. - : Elsevier BV. - 0924-2244 .- 1879-3053. ; 97, s. 300-316
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Research review (peer-reviewed)abstract
- Background: Bee bread is a product of the fermentation of a mixture of pollen, nectar and bee saliva that is inoculated by a wide range of bacteria and yeasts necessary for fermentation after storage in comb cells. Bee bread is regarded as the chief protein resource that bees can utilize, especially for feeding of larvae and adults. Since ancient times, bee bread has been used in different cultures for several nutritional and therapeutic purposes.Scope and approach: In this review, we attempt to highlight the possible biological activities, chemical components, methods of isolation and structure of bee bread in addition to its food supplement value and/or medical applications.Key findings and conclusions: Bee bread has been shown to exhibit antimicrobial, antioxidant, antiradical, anticancer, and anti-inflammatory activities. The basic chemical components of bee bread include carbohydrates, proteins and vitamins, as well as minerals, fatty acids and other substances such as enzymes, natural antibiotics, antioxidants and hormones. Bee bread is considered to be a beneficial food supplement. In recent years, there has been significant interest in the use of bee bread to treat many illnesses.
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| 21. |
- Khalifa, Shaden A. M., et al.
(author)
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Screening for natural and derived bio-active compounds in preclinical and clinical studies : One of the frontlines of fighting the coronaviruses pandemic
- 2021
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In: Phytomedicine. - : Elsevier BV. - 0944-7113 .- 1618-095X. ; 85
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Research review (peer-reviewed)abstract
- Background: Starting December 2019, mankind faced an unprecedented enemy, the COVID-19 virus. The world convened in international efforts, experiences and technologies in order to fight the emerging pandemic. Isolation, hygiene measure, diagnosis, and treatment are the most efficient ways of prevention and intervention nowadays. The health organizations and global care systems screened the available resources and offered recommendations of approved and proposed medications. However, the search for a specific selective therapy or vaccine against COVID-19 remains a challenge.Methods: A literature search was performed for the screening of natural and derived bio-active compounds which showed potent antiviral activity against coronaviruses using published articles, patents, clinical trials website (https://clinicaltrials.gov/) and web databases (PubMed, SCI Finder, Science Direct, and Google Scholar).Results: Through the screening for natural products with antiviral activities against different types of the human coronavirus, extracts of Lycoris radiata (L'Her.), Gentiana scabra Bunge, Dioscorea batatas Decne., Cassia tora L., Taxillus chinensis (DC.), Cibotium barometz L. and Echinacea purpurea L. showed a promising effect against SARSCoV. Out of the listed compound Lycorine, emetine dihydrochloride hydrate, pristimerin, harmine, conessine, berbamine, 4'-hydroxychalcone, papaverine, mycophenolic acid, mycophenolate mofetil, monensin sodium, cycloheximide, oligomycin and valinomycin show potent activity against human coronaviruses. Additionally, it is worth noting that some compounds have already moved into clinical trials for their activity against COVID-19 including fingolimod, methylprednisolone, chloroquine, tetrandrine and tocilizumab.Conclusion: Natural compounds and their derivatives could be used for developing potent therapeutics with significant activity against SARS-COV-2, providing a promising frontline in the fighting against COVID-19.
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| 22. |
- Khalifa, Shaden A. M., et al.
(author)
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Truffles : From Islamic culture to chemistry, pharmacology, and food trends in recent times
- 2019
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In: Trends in Food Science & Technology. - : Elsevier BV. - 0924-2244 .- 1879-3053. ; 91, s. 193-218
-
Research review (peer-reviewed)abstract
- Background: Many years back, during Islamic civilization, truffle (Kama'ah) was mentioned by Prophet Muhammed (PBUH) to be well recognized as a therapeutic for eye diseases. (In the Sahihain, it is narrated that the Prophet said: The Kama'ah (truffle) is among the manna (which is a food mentioned in the Qura'n, Surah alBagarah), and its water (extract or juice) cures the eye diseases). Truffles represent a large group of soil fungi belonging to Ascomycota, Basidiomycota, and Zygomycota. Because of their exceptionally profitable protein, fat, polysaccharide, carbohydrate, ash, mineral, phenolic and other organic molecule contents, truffles have been appreciated as food, nutritional and therapeutic sources for many years. Scope and approach: The main aim of this review is to highlight a comprehensive compile of truffles traditional uses, mycochemistry, pharmacological properties and nutritional value with special focus on desert truffles. Such review represents a good candidate reference for future truffle research. Key findings and conclusions: In this review, we discuss the traditional aspects of truffles with reference to Prophetic Traditional Medicine (al-Tibb al-Nabawi) to cure aliments such as trachoma. The use of truffles is justified by many recent research findings with regards to their anti-inflammatory, anti-bacterial, anti-oxidant, and anti-cancer properties. Although the molecular mechanism and functions of the different truffle species have been intensively studied, we look forward to translating these traditional remedies into preclinical and clinical applications.
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| 23. |
- Khurshid, Asma, et al.
(author)
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Experimental and Hirshfeld Surface Investigations for Unexpected Aminophenazone Cocrystal Formation under Thiourea Reaction Conditions via Possible Enamine Assisted Rearrangement
- 2022
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In: Crystals. - : MDPI AG. - 2073-4352. ; 12:5
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Journal article (peer-reviewed)abstract
- Considering the astounding biomedicine properties of pharmaceutically active drug, 4-aminophenazone, also known as 4-aminoantipyrine, the work reported in this manuscript details the formation of novel cocrystals of rearranged 4-aminophenazone and 4-nitro-N-(4-nitrobenzoyl) benzamide in 1:1 stoichiometry under employed conditions for thiourea synthesis by exploiting the use of its active amino component. However, detailed analysis via various characterization techniques such as FT-IR, nuclear magnetic resonance spectroscopy and single crystal XRD, for this unforeseen, but useful cocrystalline synthetic adduct (4 and 5) prompted us to delve into its mechanistic pathway under provided reaction conditions. The coformer 4-nitro-N-(4-nitrobenzoyl) benzamide originates via nucleophilic addition reaction following tetrahedral mechanism between para-nitro substituted benzoyl amide and its acid halide (1). While the enamine nucleophilic addition reaction by 4-aminophenazone on 4-nitrosubstituted aroyl isothiocyanates under reflux temperature suggests the emergence of rearranged counterpart of cocrystal named N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carbonothioyl)-4-nitrobenzamide. Crystallographic studies reveal triclinic system P-1 space group for cocrystal (4 and 5) and depicts two different crystallographically independent molecules with prominent C-H center dot center dot center dot O and N-H center dot center dot center dot O hydrogen bonding effective for structure stabilization. Hirshfeld surface analysis also displays hydrogen bonding and van der Waals interactions as dominant interactions in crystal packing. Further insight into the cocrystal synthetic methodologies supported the occurrence of solution-based evaporation/cocrystallization methodology in our case during purification step, promoting the synthesis of this first-ever reported novel cocrystal of 4-aminophenazone with promising future application in medicinal industry.
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| 24. |
- Larik, Fayaz Ali, et al.
(author)
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Synthetic approaches towards the multi target drug spironolactone and its potent analogues/derivatives
- 2017
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In: Steroids. - : Elsevier BV. - 0039-128X .- 1878-5867. ; 118, s. 76-92
-
Research review (peer-reviewed)abstract
- Spironolactone is a well-known multi-target drug and is specifically used for the treatment of high blood pressure and heart failure. It is also used for the treatment of edema, cirrhosis of the liver, malignant, pediatric, nephrosis and primary hyperaldosteronism. Spironolactone in association with thiazide diuretics treats hypertension and in association with furosemide treats bronchopulmonary dyspepsia. The therapeutic mechanism of action of spironolactone involves binding to intracellular mineralocorticoids receptors (MRs) in kidney epithelial cells, thereby inhibiting the binding of aldosterone. Since its first synthesis in 1957 there are several synthetic approaches have been reported throughout the years, Synthetic community has devoted efforts to improve the synthesis of spironolactone and to synthesize its analogues and derivatives. This review aims to provide comprehensive insight for the synthetic endeavors devoted towards the synthesis of a versatile drug spironolactone and its analogues/derivatives.
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| 25. |
- Larik, Fayaz Ali, et al.
(author)
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The role of Lawesson's reagent in the total synthesis of macrocyclic natural products
- 2017
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In: Phosphorus Sulfur and Silicon and the Related Elements. - : TAYLOR & FRANCIS LTD. - 1042-6507 .- 1563-5325. ; 192:5, s. 490-502
-
Research review (peer-reviewed)abstract
- This review, including 111 references, describes the applications of Lawesson's reagent (LR) [2,4-bis(p-methoxyphenyl)-1,3,2,4-dithiadiphosphetane-2,4-dithione] for the total synthesis of macrocyclic natural products. LR is a versatile reagent and shows excellent regioselectivity, chemoselectivity, and offers the products in high yield. The thionation of carbonyl moieties present in macrocyclic natural products, and cyclization to construct key heterocyclic fragments is described. Moreover, this review highlights the medicinal significance of the natural products. [GRAPHICS] .
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| 26. |
- Park, Seung Hyun, et al.
(author)
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Nonpharmaceutical interventions reduce the incidence and mortality of COVID-19: A study based on the survey from the International COVID-19 Research Network (ICRN)
- 2023
-
In: Journal of Medical Virology. - : WILEY. - 0146-6615 .- 1096-9071. ; 95:2
-
Journal article (peer-reviewed)abstract
- The recently emerged novel coronavirus, "severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2)," caused a highly contagious disease called coronavirus disease 2019 (COVID-19). It has severely damaged the worlds most developed countries and has turned into a major threat for low- and middle-income countries. Since its emergence in late 2019, medical interventions have been substantial, and most countries relied on public health measures collectively known as nonpharmaceutical interventions (NPIs). We aimed to centralize the accumulative knowledge of NPIs against COVID-19 for each country under one worldwide consortium. International COVID-19 Research Network collaborators developed a cross-sectional online survey to assess the implications of NPIs and sanitary supply on the incidence and mortality of COVID-19. The survey was conducted between January 1 and February 1, 2021, and participants from 92 countries/territories completed it. The association between NPIs, sanitation supplies, and incidence and mortality were examined by multivariate regression, with the log-transformed value of population as an offset value. The majority of countries/territories applied several preventive strategies, including social distancing (100.0%), quarantine (100.0%), isolation (98.9%), and school closure (97.8%). Individual-level preventive measures such as personal hygiene (100.0%) and wearing facial masks (94.6% at hospitals; 93.5% at mass transportation; 91.3% in mass gathering facilities) were also frequently applied. Quarantine at a designated place was negatively associated with incidence and mortality compared to home quarantine. Isolation at a designated place was also associated with reduced mortality compared to home isolation. Recommendations to use sanitizer for personal hygiene reduced incidence compared to the recommendation to use soap. Deprivation of masks was associated with increased incidence. Higher incidence and mortality were found in countries/territories with higher economic levels. Mask deprivation was pervasive regardless of economic level. NPIs against COVID-19 such as using sanitizer, quarantine, and isolation can decrease the incidence and mortality of COVID-19.
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| 27. |
- Saeed, Aamer, et al.
(author)
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Advances in transition-metal-catalyzed synthesis of 3-substituted isocoumarins
- 2017
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In: Journal of Organometallic Chemistry. - : ELSEVIER SCIENCE SA. - 0022-328X .- 1872-8561. ; 834, s. 88-103
-
Research review (peer-reviewed)abstract
- 3-Substituted isocoumarins are the most abundant class of naturally isocoumarins, found in several biologically active scaffolds and are precursors towards complex natural products. Considerable attempts have been devoted to the synthesis of these isocoumarins both by metal free or transition-metalcatalyzed reactions. Among the metal catalyzed reactions, the use of palladium, copper, gold, iron, nickel, rhodium, ruthenium, zinc, chromium, iridium, silver or thallium salts/complexes for the construction of 3-substituted isocoumarin ring is noteworthy due to being economical and good functional group tolerance. The current review focusses the recent reports on the Pd-, Cu-, Ag-, Fe-, Ni-, Rh-, Ru-, Zn, Cr-, Ir-, Ag- and Ti -catalyzed synthesis of isocoumarins.
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| 28. |
- Saeed, Aamer, et al.
(author)
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Design, synthesis, biochemical and in silico characterization of novel naphthalene-thiourea conjugates as potential and selective inhibitors of alkaline phosphatase
- 2023
-
In: Medicinal Chemistry Research. - : Springer Nature. - 1054-2523 .- 1554-8120. ; 32:6, s. 1077-1086
-
Journal article (peer-reviewed)abstract
- Naphthalene ring is present in a number of FDA-approved, commercially available medications, including naphyrone, terbinafine, propranolol, naproxen, duloxetine, lasofoxetine, and bedaquiline. By reacting newly obtained 1-naphthoyl isothiocyanate with properly modified anilines, a library of ten novel naphthalene-thiourea conjugates (5a-5j) were produced with good to exceptional yields and high purity. The newly synthesized compounds were observed for their potential to inhibit alkaline phosphatase (ALP) and scavenge free radicals. All of the investigated compounds displayed a more powerful inhibitory profile than the reference agent, KH2PO4 particularly compound 5h and 5a exhibited strong inhibitory potential against ALP with IC50 value of 0.365 +/- 0.011 and 0.436 +/- 0.057 mu M respectively. In addition, Lineweaver-Burk plots revealed the non-competitive inhibition mode of the most powerful derivative i.e., 5h (ki value 0.5 mu M). To investigate the putative binding mode of selective inhibitor interactions, molecular docking was performed. It is recommended that future research will focus on developing selective alkaline phosphatase inhibitors by modifying the structure of the 5h derivative.
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| 29. |
- Saeed, Aamer, et al.
(author)
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Developments in the synthesis of the antiplatelet and antithrombotic drug (S)-clopidogrel
- 2017
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In: Chirality. - : Wiley. - 0899-0042 .- 1520-636X. ; 29:11, s. 684-707
-
Research review (peer-reviewed)abstract
- S-(+)-Methyl 2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)acetate, also known as (S)-clopidogrel, is marketed under the trade names Plavix and Iscover. It is a potent thienopyridine-class of antithrombotic and antiplatelet drug (antiaggregant). Among the two available stereoisomers of clopidogrel, for pharmaceutical activities only the S-enantiomer is applicable, as no antithrombotic activity is observed in the R-enantiomer and causes political upheavals and social turmoil in animal experiments. Worldwide sales of Plavix amounted to $6.4 billion yearly, which ranks second. Attributed to the increased demand of (S)-clopidogrel drug, it provoked the synthetic community to devise facile synthetic approaches. This review aims to summarize the synthetic methods of (S)-clopidogrel drug reported in the literature. The present review discusses the pros and cons of each synthetic methodology, which would be beneficial to the scientific community for further developments in the synthetic methodologies for (S)-clopidogrel. In addition, the compilation approach of literature-reported synthetic strategies of (S)-clopidogrel in one platform is advantageous, supportive, and crucial for the synthetic community to elect the best synthetic methodology of (S)-clopidogrel and to create new synthesis ideas.
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| 30. |
- Saeed, Aamer, et al.
(author)
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Identification of novel C-2 symmetric Bis-Azo-Azamethine molecules as competitive inhibitors of mushroom tyrosinase and free radical scavengers : synthesis, kinetics, and molecular docking studies
- 2022
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In: Journal of Biomolecular Structure and Dynamics. - : Taylor & Francis. - 0739-1102 .- 1538-0254. ; 40:10, s. 4419-4428
-
Journal article (peer-reviewed)abstract
- Tyrosinase is a multi-copper enzyme found in plants, animals and microorganisms, plays a critical role in the melanogenesis and browning process critical to cosmetics and food industries. Many natural, semi-synthetic and synthetic inhibitors have been discovered. To this end, a small library of symmetrical Bis-Azo-Azamethine hybrids 5a–j was synthesized and characterized through spectroscopic and analytical data and explored for mushroom tyrosinase and free radical scavenging activity. All of the molecules 5a–j explicated better potential compared to the standard Kojic acid. On the whole, compound 5i having IC50 value 0.002 ± 0.004 µM was found to be the most potent derivative. The Kinetic studies were performed for 5i and indicating the mode of inhibition in a competitive manner. Structure Activity Relationship (SAR) analysis and docking studies were carried out. Thus compound 5i bearing bulky naphthyl groups was most potent and, The molecular docking indicated formation of two hydrogen bonds with Arg268 and one hydrophobic interaction with Glu322. The carbonyl oxygen of 5i interacts with Arg268 and form two hydrogen bonds having lengths 2.44 and 2.62 Å, respectively. In the same way, compounds 5a–j were appraised for DPPH free radical scavenging ability and five of them 5d, 5e, 5h, 5i and 5j were found to exhibit higher % scavenging potency compared with vitamin C, as the standard. Interesting compound 5i was again the most potent in the series. The current investigation points towards the role of naphthyl group in design of new inhibitors of melanogenesis and the antioxidants with improved efficacy.
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| 31. |
- Saeed, Aamer, et al.
(author)
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Novel N-(benzo[d]oxazol-2-yl)alkanamides : synthesis and carbonic anhydrase II inhibition studies
- 2020
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In: Journal of Heterocyclic Chemistry. - : WILEY. - 0022-152X .- 1943-5193. ; 57:7, s. 2831-2843
-
Journal article (peer-reviewed)abstract
- Carbonic anhydrase (CA II) inhibitors are very important therapeutic targets in drug design for treatment of neuropathic pain and in eradication of glaucoma, cancer, epilepsy, ulcer and obesity. In this study, some two2-substituted benzoxazoles (3a-j) were developed as a new family of carbonic anhydrase II inhibitors by employing acyl thiourea chemistry via a simple and expedient protocol and evaluated for CA II inhibitor activity and radical scavenging ability. Compounds 3f and 3j were found to be the most potent inhibitors, with IC50 values of 0.00564 and 0.00596 mu M, respectively which are several times better than that of the standard, acetazolamide (IC50 value 0.997 +/- 0.0586 mu M). Docking experiments were carried out against the carbonic anhydrase II crystal structure to better rationalize the inhibitory activities of these new structures. Moreover, the results of a DPPH radical scavenging assay showed that the antioxidant profile of compound 3i is superior to those of other derivatives. The results have revealed that derivatives 3f and 3j behave as CA-II inhibitors significantly better than standard and 3i has good anti-oxidation potential.
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| 32. |
- Saeed, Aamer, et al.
(author)
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Recent Progress in Pyridine Containing Heterocycles as High Performance Host Materials for Blue PHOLEDs
- 2018
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In: Mini-Reviews in Organic Chemistry. - 1570-193X .- 1875-6298. ; 15:4, s. 261-273
-
Research review (peer-reviewed)abstract
- Phosphorescent Organic Light-Emitting Diodes (PHOLEDs) have an advantage of stability for a lifetime in comparison with the conventional Organic Light-Emitting Diodes (OLEDs). Green and red OLEDs have already achieved success, but for the last decade, blue OLEDs have observed a surge in the attention towards them from academia as well as the industry. There are incessant efforts devoted towards the improvement of external quantum efficiency from 25-30%. The host materials (or host compounds), hole transporting and electron transporting are the preeminent factors for the enhancement of External Quantum Efficiency (EQE). This review aims at highlighting the role of pyridine as an efficient Electron Transporting Material (ETM) for blue PHOLEDs. Pyridine having electron withdrawing nature can serve as valuable host compounds for electron transport material in PHOLEDs of a blue color. The presence of nitrogen atom in pyridine facilitates in lowering HOMO/LUMO energy levels compared to benzene ring and this assists in adding phenyl rings at the periphery of pyridine ring.
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| 33. |
- Saeed, Aamer, et al.
(author)
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Recent resurgence toward the oxidation of heteroatoms using dimethyldioxirane as an exquisite oxidant
- 2017
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In: Synthetic Communications. - : TAYLOR & FRANCIS INC. - 0039-7911 .- 1532-2432. ; 47:9, s. 835-852
-
Research review (peer-reviewed)abstract
- This review covers the literature from 2005 to till date. Oxidation chemistry is a dynamic field of organic synthesis as it keeps evolving with the passage of time. There is a recent surge in that area to switch over from inorganic oxidants to organic oxidants. The oxidation of heteroatom is an intriguing task for the synthetic chemists, as it requires mild oxidant with no harmful side products. Dimethyldioxirane serves as a super-effective oxidant as it shows high functional group tolerance and possess acetone as byproducts which is also eco-friendly. This review summarizes the heteroatom oxidation of sulfur, nitrogen, iodine, selenium, phosphorous, and platinum atoms using DMDO as an oxidant.
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| 34. |
- Saeed, Aamer, et al.
(author)
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Synthesis of and molecular docking studies of azomethine-tethered sulfonamides as carbonic anhydrase II & 15-lipoxygenase inhibitors
- 2021
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In: Journal of Molecular Structure. - : Elsevier. - 0022-2860 .- 1872-8014. ; 1243
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Journal article (peer-reviewed)abstract
- The use of sulfanilamide in organic synthesis has become a classical strategy for the synthesis of several biologically active compounds. In this study, a series of hydrazine-carbonyl tethered sulfonamides derivatives 5(a-j) was synthesized as carbonic anhydrase isoform II (bCA II) and 15-Lipoxygenase enzyme (15-LOX) inhibitors. The Sulfanilamide (1) was treated with ethyl acrylate (2) to yield propanoate ethyl ester (3) which on reaction with hydrazine hydrate, was successively converted into hydrazide (4). The hydrazide (4) on condensation with a variety of substituted aromatic aldehydes, resulted in hydrazinecarbonyl tethered sulfonamides 5(a-j). The characterization data of the synthesized derivatives confirmed the formation of final products. Against bCA II, all the compounds showed inhibitory effects but derivative 5j exhibited the most potent activity with an value of IC50 0.11 ± 0.01 μM and it was found more active than standard acetazolamide (IC50). When the inhibitory effects of these compounds were observed against 15-LOX, only two compounds 5 h and 5j exhibited significant inhibitory activity. The molecular docking investigations of the most active inhibitor of both bCA II and 15-LOX enzymes were carried out which further confirmed that the potent derivatives bind well inside the active binding site of the targeted enzyme, respectively. In addition, the free radical scavenging potential of these compounds (5a-j) was evaluated and found to have antioxidant potential. Based on our investigations, this study has identified few new scaffolds which may act as dual inhibitor and serve as a core structures for the discovery of effective drugs against carbonic anhydrase-II and 15-Lipoxygenase associated disorders such as inflammation, pancreatic carcinoma, and gastric carcinomas.
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| 35. |
- Shahid, Shereena, et al.
(author)
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A Review on the Scope of TFDO-Mediated Oxidation in Organic Synthesis-Reactivity and Selectivity
- 2018
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In: Current Organic Synthesis. - : Bentham Science Publishers Ltd.. - 1570-1794 .- 1875-6271. ; 15:8, s. 1091-1108
-
Research review (peer-reviewed)abstract
- Dioxiranes are three-membered strained ring peroxides that are typical archetype examples of electrophilic entities. A dioxirane-based oxidant named 3-methyl(trifluoromethyl)dioxirane (TFDO) is a fluorinated analogue of the extremely valuable oxidant dimethyldioxirane (DMDO). Owing to the strained three-membered ring and presence of electron-withdrawing trifluoromethyl group, TFDO is several times more reactive than DMDO and acts as a significant chemical reagent. Moreover, TFDO exhibits high regio-, chemo- and stereo-selectivity even under unusual reaction conditions, i.e. at pH values close to neutrality and at sub-ambient temperatures. The TFDO transfers an oxygen atom to "unactivated" carbon-hydrogen bonds of alkanes as well as to the double bonds of alkenes and also helps in oxidation of compounds containing heteroatoms having a lone pair of electrons, such as sulfides and amines. TFDO-mediated oxidation is considered to be one of the main procedures in the 21st century for the synthesis of oxygen-containing organic molecules. This review throws light on the applications of TFDO in organic syntheses to provide an insight into the future research and gives a comprehensive summary of the selective functionalization of activated and non-activated organic compounds.
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| 36. |
- Shahzad, Danish, et al.
(author)
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Novel C-2 Symmetric Molecules as -Glucosidase and -Amylase Inhibitors : Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics
- 2019
-
In: Molecules. - : MDPI. - 1431-5157 .- 1420-3049. ; 24:8
-
Journal article (peer-reviewed)abstract
- A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a-5h, have been synthesized, characterized by H-1-NMR and C-13-NMR, and evaluated for their in vitro -glucosidase and -amylase inhibitory activities. All the synthesized compounds efficiently inhibited both enzymes. Compound 5g was the most potent derivative in the series, and powerfully inhibited both -glucosidase and -amylase. The IC50 of 5g against -glucosidase was 0.35917 +/- 0.0189 mu M (standard acarbose IC50 = 6.109 +/- 0.329 mu M), and the IC50 value of 5g against -amylase was 0.4379 +/- 0.0423 mu M (standard acarbose IC50 = 33.178 +/- 2.392 mu M). The Lineweaver-Burk plot indicated that compound 5g is a competitive inhibitor of -glucosidase. The binding interactions of the most active analogues were confirmed through molecular docking studies. Docking studies showed that 5g interacts with the residues Trp690, Asp548, Arg425, and Glu426, which form hydrogen bonds to 5g with distances of 2.05, 2.20, 2.10 and 2.18 angstrom, respectively. All compounds showed high mutagenic and tumorigenic behaviors, and only 5e showed irritant properties. In addition, all the derivatives showed good antioxidant activities. The pharmacokinetic evaluation also revealed promising results
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| 37. |
- Ujan, Rabail, et al.
(author)
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Drug-1,3,4-Thiadiazole Conjugates as Novel Mixed-Type Inhibitors of Acetylcholinesterase : Synthesis, Molecular Docking, Pharmacokinetics, and ADMET Evaluation
- 2019
-
In: Molecules. - : MDPI. - 1431-5157 .- 1420-3049. ; 24:5
-
Journal article (peer-reviewed)abstract
- A small library of new drug-1,3,4-thiazidazole hybrid compounds (3a-3i) was synthesized, characterized, and assessed for their acetyl cholinesterase enzyme (AChE) inhibitory and free radical scavenging activities. The newly synthesized derivatives showed promising activities against AChE, especially compound 3b (IC50 18.1 +/- 0.9 nM), which was the most promising molecule in the series, and was substantially more active than the reference drug (neostigmine methyl sulfate; IC50 2186.5 +/- 98.0 nM). Kinetic studies were performed to elucidate the mode of inhibition of the enzyme, and the compounds showed mixed-type mechanisms for inhibiting AChE. The Ki of 3b (0.0031 mu M) indicates that it can be very effective, even at low concentrations. Compounds 3a-3i all complied with Lipinski's Rule of Five, and showed high drug-likeness scores. The pharmacokinetic parameters revealed notable lead-like properties with insignificant liver and skin-penetrating effects. The structure-activity relationship (SAR) analysis indicated pi-pi interactions with key amino acid residues related to Tyr124, Trp286, and Tyr341.
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| 38. |
- Yosri, Nermeen, et al.
(author)
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Arctium lappa (Burdock) : Insights from ethnopharmacology potential, chemical constituents, clinical studies, pharmacological utility and nanomedicine
- 2023
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In: Biomedicine and Pharmacotherapy. - : Elsevier. - 0753-3322 .- 1950-6007. ; 158
-
Research review (peer-reviewed)abstract
- Arctium lappa L. is a medicinal edible homologous plant, commonly known as burdock or bardana, which belongs to the Asteraceae family. It is widely distributed throughout Northern Asia, Europe, and North America and has been utilized for hundreds of years. The roots, fruits, seeds, and leaves of A. lappa have been extensively used in traditional Chinese Medicine (TCM). A. lappa has attracted a great deal of attention due to its possession of highly recognized bioactive metabolites with significant therapeutic potential. Numerous pharmacological effects have been demonstrated in vitro and in vivo by A. lappa and its bioactive metabolites, including antimicrobial, antiobesity, antioxidant, anticancer, anti-inflammatory, anti-diabetic, anti-allergic, antiviral, gastroprotective, hepatoprotective, and neuroprotective activities. Additionally, A. lappa has demonstrated considerable clinical efficacies and valuable applications in nanomedicine. Collectively, this review covers the properties of A. lappa and its bioactive metabolites, ethnopharmacology aspects, pharmacological effects, clinical trials, and applications in the field of nanomedicine. Hence, a significant attention should be paid to clinical trials and industrial applications of this plant with particular emphasis, on drug discovery and nanotechnology.
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| 39. |
- Zahra, Maram Hussein, et al.
(author)
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Alpinia zerumbet (Pers.) : Food and Medicinal Plant with Potential In Vitro and In Vivo Anti-Cancer Activities
- 2019
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In: Molecules. - : MDPI AG. - 1431-5157 .- 1420-3049. ; 24:13
-
Journal article (peer-reviewed)abstract
- Background/Aim: Plants play an important role in anti-cancer drug discovery, therefore, the current study aimed to evaluate the biological activity of Alpinia zerumbet (A. zerumbet) flowers. Methods: The phytochemical and biological criteria of A. zerumbet were in vitro investigated as well as in mouse xenograft model. Results: A. zerumbet extracts, specially CH2Cl2 and MeOH extracts, exhibited the highest potent anti-tumor activity against Ehrlich ascites carcinoma (EAC) cells. The most active CH2Cl2 extract was subjected to bioassay-guided fractionation leading to isolatation of the naturally occurring 5,6-dehydrokawain (DK) which was characterized by IR, MS, H-1-NMR and C-13-NMR. A. zerumbet extracts, specially MeOH and CH2Cl2 extracts, exhibited significant inhibitory activity towards tumor volume (TV). Furthermore, A. zerumbet extracts declined the high level of malonaldehyde (MDA) as well as elevated the levels of superoxide dismutase (SOD) and catalase (CAT) in liver tissue homogenate. Moreover, DK showed anti-proliferative action on different human cancer cell lines. The recorded IC50 values against breast carcinoma (MCF-7), liver carcinoma (Hep-G2) and larynx carcinoma cells (HEP-2) were 3.08, 6.8, and 8.7 mu g/mL, respectively. Conclusion: Taken together, these findings open the door for further investigations in order to explore the potential medicinal properties of A. zerumbet.
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