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1.
  • El-Garawani, Islam, et al. (author)
  • The Ameliorative Role of Acacia senegal Gum against the Oxidative Stress and Genotoxicity Induced by the Radiographic Contrast Medium (Ioxitalamate) in Albino Rats
  • 2021
  • In: Antioxidants. - : MDPI AG. - 2076-3921. ; 10:2
  • Journal article (peer-reviewed)abstract
    • Arabic gum (Acacia senegal, AG) is proven effective antioxidant and cytoprotective agent. The present study was designed to test this notion by investigating the possible role of AG against the radiographic contrast medium (Ioxitalamate, Telebrix-35®, TBX)-induced oxidative stress and genotoxicity. Albino rats were divided into four groups and supplied with either; distilled water, daily 10% (w/v) AG, an intravenous dose of TBX (1600 mg I/kg b.wt) and co-administration of TBX and AG. Rats were sacrificed and blood samples were collected to assess the genotoxicity employing the peripheral blood leucocytes fluorescent double staining; namely the acridine orange/ethidium bromide (AO/EB) staining and alkaline comet assay. Further, chromosomal analyses were done in bone marrow cells. Serum urea and creatinine levels, in addition to malondialdehyde (MDA), nitric oxide (NO), catalase (CAT) and glutathione (GSH) levels in kidney tissues were measured. Liquid chromatography-mass spectrophotometry (LC-MS-MS) was performed to identify the chemical composition of AG extract. Kidney functions, single/double-stranded DNA damage, chromosomal aberrations, mitotic index, MDA and NO levels were significantly (p < 0.001) increased in TBX-treated group compared to the control and AG-treated one. Meanwhile, CAT and GSH activities were significantly diminished and the AG supplementation significantly (p < 0.001) ameliorated these effects compared with the control and AG-treated groups. Five compounds have been identified using GNPS networking including 7,3′,4′-Trihydroxyisoflavone, Noscapine, Tetrahydropapaveroline, Costunolide, Hesperidin. In conclusion, results of the present study suggest that AG exerted a protective role against TBX-induced oxidative stress and genotoxicity which may be attributed to the active metabolites in the gum.
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2.
  • Khalifa, Shaden A. M., et al. (author)
  • Comprehensive Overview on Multiple Strategies Fighting COVID-19
  • 2020
  • In: International Journal of Environmental Research and Public Health. - : MDPI AG. - 1661-7827 .- 1660-4601. ; 17:16
  • Research review (peer-reviewed)abstract
    • Lately, myriad of novel viruses have emerged causing epidemics such as SARS, MERS, and SARS-CoV-2, leading to high mortality rates worldwide. Thus, these viruses represented a challenging threat to mankind, especially considering the miniscule data available at our disposal regarding these novel viruses. The entire world established coordinative relations in research projects regarding drug and vaccine development on the external range, whereas on the internal range, all countries declared it an emergency case through imposing different restrictions related to their border control, large gatherings, school attendance, and most social activities. Pandemic combating plans prioritized all sectors including normal people, medical staff politicians, and scientists collectively shouldered the burden. Through planning and learning the previous lessons from SARS and MERS, healthcare systems could succeed in combating the viral spread and implications of these new pandemics. Different management strategies including social distance, social awareness and isolation represented successful ways to slow down the spread of the pandemic. Furthermore, pre-preparedness of some countries for emergencies is crucial to minimize the consequences of the crisis.
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3.
  • Samak, Dalia H., et al. (author)
  • Developmental toxicity of carbon nanoparticles during embryogenesis in chicken
  • 2020
  • In: Environmental Science and Pollution Research. - : Springer Nature. - 0944-1344 .- 1614-7499. ; 27:16, s. 19058-19072
  • Journal article (peer-reviewed)abstract
    • Nanoparticles (NPs) are very small particles present in a wide range of materials. There is a dearth of knowledge regarding their potential secondary effects on the health of living organisms and the environment. Increasing research attention, however, has been directed toward determining the effects on humans exposed to NPs in the environment. Although the majority of studies focus on adult animals or populations, embryos of various species are considered more susceptible to environmental effects and pollutants. Hence, research studies dealing mainly with the impacts of NPs on embryogenesis have emerged recently, as this has become a major concern. Chicken embryos occupy a special place among animal models used in toxicity and developmental investigations and have also contributed significantly to the fields of genetics, virology, immunology, cell biology, and cancer. Their rapid development and easy accessibility for experimental observance and manipulation are just a few of the advantages that have made them the vertebrate model of choice for more than two millennia. The early stages of chicken embryogenesis, which are characterized by rapid embryonic growth, provide a sensitive model for studying the possible toxic effects on organ development, body weight, and oxidative stress. The objective of this review was to evaluate the toxicity of various types of carbon black nanomaterials administered at the beginning of embryogenesis in a chicken embryo model. In addition, the effects of diamond and graphene NPs and carbon nanotubes are reviewed.
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4.
  • Abd El-Wahed, Aida, et al. (author)
  • Wasp Venom Biochemical Components and Their Potential in Biological Applications and Nanotechnological Interventions
  • 2021
  • In: Toxins. - : MDPI AG. - 2072-6651. ; 13:3
  • Research review (peer-reviewed)abstract
    • Wasps, members of the order Hymenoptera, are distributed in different parts of the world, including Brazil, Thailand, Japan, Korea, and Argentina. The lifestyles of the wasps are solitary and social. Social wasps use venom as a defensive measure to protect their colonies, whereas solitary wasps use their venom to capture prey. Chemically, wasp venom possesses a wide variety of enzymes, proteins, peptides, volatile compounds, and bioactive constituents, which include phospholipase A2, antigen 5, mastoparan, and decoralin. The bioactive constituents have anticancer, antimicrobial, and anti-inflammatory effects. However, the limited quantities of wasp venom and the scarcity of advanced strategies for the synthesis of wasp venom’s bioactive compounds remain a challenge facing the effective usage of wasp venom. Solid-phase peptide synthesis is currently used to prepare wasp venom peptides and their analogs such as mastoparan, anoplin, decoralin, polybia-CP, and polydim-I. The goal of the current review is to highlight the medicinal value of the wasp venom compounds, as well as limitations and possibilities. Wasp venom could be a potential and novel natural source to develop innovative pharmaceuticals and new agents for drug discovery.
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5.
  • Reda, Eman H., et al. (author)
  • Comparative Study on the Essential Oils from Five Wild Egyptian Centaurea Species : Effective Extraction Techniques, Antimicrobial Activity and In-Silico Analyses
  • 2021
  • In: Antibiotics. - : MDPI AG. - 2079-6382. ; 10:3
  • Journal article (peer-reviewed)abstract
    • The genus Centaurea is recognized in folk medicine for anti-inflammatory, anti-itch, antitussive, purgative, astringent, and tonic activities. To study the chemical determinant for antimicrobial activity essential oils (EOs), five Centaurea species were analyzed including: C. scoparia, C. calcitrapa, C. glomerata, C. lipii and C. alexandrina. Conventional hydro-distillation (HD) and microwave-assisted extraction (MAE), as new green technologies, were compared for the extraction of essential oils. GC/MS analysis identified 120 EOs including mostly terpenoid except from C. lipii and C. alexandrina in which nonterpenoids were the major constituents. Major terpenoids included spathulenol, caryophyllene oxide and alloaromadendrene oxide-2. To probe antibacterial activity, potential EO inhibitors of a bacterial type II DNA topoisomerase, DNA gyrase B were screened via an in silico molecular docking approach. Spathulenol and alloaromadendrene oxide-2 possessed the best binding affinity in the ATP- binding pocket of Gyrase B enzyme. Principal component analysis and agglomerative hierarchical clustering were used for sample classification and revealed that sesquiterpenes contributed the most for accessions classification. In vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli and Aspergillus niger for all EOs were also evaluated. EOs from C. lipii, C. glomerata and C. calcitrapa exhibited significant MIC against S. aureus with an MIC value of 31.25 µg/mL.
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6.
  • El-Seedi, Hesham, et al. (author)
  • A Spotlight on the Egyptian Honeybee (Apis mellifera lamarckii)
  • 2022
  • In: Animals. - : MDPI AG. - 2076-2615. ; 12:20
  • 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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7.
  • El-Seedi, Hesham R., et al. (author)
  • Anti-schistosomiasis triterpene glycoside from the Egyptian medicinal plant Asparagus stipularis
  • 2011
  • In: REV BRAS FARMACOGN. - : SOC BRASILEIRA FARMACOGNOSIA. - 0102-695X. ; 22:2, s. 314-318
  • Journal article (peer-reviewed)abstract
    • Bioassay-guided isolation using an in vitro assay testing for anti-schistosomiasis yielded a novel triterpene saponin, asparagalin A, from the n-butanol extract of the roots of Asparagus stipularis Forssk., Asparagaceae. The structure was elucidated by spectroscopic analysis and chemical transformations. Administration of asparagalin A resulted in a retardation of worm growth and locomotion at the first day and showed a significant activity of egg-laying suppression at 200 mu g/mL concentration.
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8.
  • El-Seedi, Hesham R., et al. (author)
  • Plant extracts and compounds for combating schistosomiasis
  • 2023
  • In: Phytochemistry Reviews. - : Springer Science and Business Media LLC. - 1568-7767 .- 1572-980X. ; 22:6, s. 1691-1806
  • Journal article (peer-reviewed)abstract
    • Schistosomiasis is a vector-borne water-based disease caused by Schistosoma blood flukes. It mostly affects people in low-income regions, 90% of reported cases being in developing countries. Schistosoma has a complex lifecycle, alternately infecting mammalian hosts and snails. The snails hosting the parasite are the most viable targets. Selective preparations for reducing the parasite pool in snails and infected water are required as current molluscicides are also nontoxic to other organisms, including fish, and thus affect food supplies in infected areas. Plants (e.g. Annona crassiflora Mart., A. muricata L., and A. montana Macfad.) are attractive potential sources as alternative molluscicides and novel entity to treat the disease owned to their diverse biologically potent compounds including; saponins, alkaloids, terpenoids, and tannins. Additionally, they can be locally cultivated, providing income for farmers and reducing treatment costs. Here, we review plants, plant extracts and isolated compounds that have shown activities against the host snails or Schistosoma in various parts of its life cycle. Plants have a lot of potential and will continue to contribute feasible, effective medicines and/or pesticides; more research is warranted to fully explore their future applications.
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9.
  • El-Seedi, Hesham R., et al. (author)
  • Plant extracts and compounds for combating schistosomiasis
  • 2023
  • In: Phytochemistry Reviews. - : Springer. - 1568-7767 .- 1572-980X. ; 22:6, s. 1691-1806
  • Journal article (peer-reviewed)abstract
    • Schistosomiasis is a vector-borne water-based disease caused by Schistosoma blood flukes. It mostly affects people in low-income regions, 90% of reported cases being in developing countries. Schistosoma has a complex lifecycle, alternately infecting mammalian hosts and snails. The snails hosting the parasite are the most viable targets. Selective preparations for reducing the parasite pool in snails and infected water are required as current molluscicides are also nontoxic to other organisms, including fish, and thus affect food supplies in infected areas. Plants (e.g. Annona crassiflora Mart., A. muricata L., and A. montana Macfad.) are attractive potential sources as alternative molluscicides and novel entity to treat the disease owned to their diverse biologically potent compounds including; saponins, alkaloids, terpenoids, and tannins. Additionally, they can be locally cultivated, providing income for farmers and reducing treatment costs. Here, we review plants, plant extracts and isolated compounds that have shown activities against the host snails or Schistosoma in various parts of its life cycle. Plants have a lot of potential and will continue to contribute feasible, effective medicines and/or pesticides; more research is warranted to fully explore their future applications.
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10.
  • El-Seedi, Hesham R., et al. (author)
  • Recent insights into the biosynthesis and biological activities of natural xanthones
  • 2010
  • In: Current Medicinal Chemistry. - : Bentham Science Publishers Ltd.. - 0929-8673 .- 1875-533X. ; 17:9, s. 854-901
  • Research review (peer-reviewed)abstract
    • This review focuses on recent advances in our understanding of the complex biosynthetic pathways and diverse biological activities of naturally occurring xanthones. The biosynthesis section covers studies published from 1989 to 2008 on xanthone production in plants and fungi, while the bioactivity review presents tabulated activities of more than 250 xanthones described in studies published from 2001 to 2008, together with structural information and indications of their wide-ranging potential uses as pharmacological tools. A large number of relevant papers have been published on these subjects (128 cited here), illustrating the diversity of the xanthones and their possible uses.
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11.
  • Khalifa, Shaden A. M., et al. (author)
  • Screening for natural and derived bio-active compounds in preclinical and clinical studies : One of the frontlines of fighting the coronaviruses pandemic
  • 2021
  • In: Phytomedicine. - : Elsevier BV. - 0944-7113 .- 1618-095X. ; 85
  • 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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12.
  • Zahra, Maram Hussein, et al. (author)
  • Alpinia zerumbet (Pers.) : Food and Medicinal Plant with Potential In Vitro and In Vivo Anti-Cancer Activities
  • 2019
  • 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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13.
  • Algethami, Jari S., et al. (author)
  • Bee Pollen : Clinical Trials and Patent Applications
  • 2022
  • In: Nutrients. - : MDPI AG. - 2072-6643. ; 14:14
  • Research review (peer-reviewed)abstract
    • Bee pollen is a natural cocktail of floral nectar, flower pollen, enzymes, and salivary secretions produced by honeybees. Bee pollen is one of the bee products most enriched in proteins, polysaccharides, polyphenols, lipids, minerals, and vitamins. It has a significant health and medicinal impact and provides protection against many diseases, including diabetes, cancer, infectious, and cardiovascular. Bee pollen is commonly promoted as a cost-effective functional food. In particular, bee pollen has been applied in clinical trials for allergies and prostate illnesses, with a few investigations on cancer and skin problems. However, it is involved in several patents and health recipes to combat chronic health problems. This review aimed to highlight the clinical trials and patents involving bee pollen for different cases and to present the role of bee pollen as a supplementary food and a potential product in cosmetic applications.
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14.
  • El-Seedi, Hesham, et al. (author)
  • Chemistry and the Potential Antiviral, Anticancer, and Anti-Inflammatory Activities of Cardiotonic Steroids Derived from Toads
  • 2022
  • In: Molecules. - : MDPI AG. - 1431-5157 .- 1420-3049. ; 27:19
  • 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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15.
  • El-Seedi, Hesham R., et al. (author)
  • Naturally occurring xanthones; latest investigations : isolation, structure elucidation and chemosystematic significance
  • 2009
  • In: Current Medicinal Chemistry. - : Bentham Science Publishers Ltd.. - 0929-8673 .- 1875-533X. ; 16:20, s. 2581-2626
  • Research review (peer-reviewed)abstract
    • In this review, an updated literature survey covering the reports of naturally occurring xanthones in the period of 2005-2008 is presented. In some 143 studies, the isolation of 264 different xanthones from 36 plant species (representing 15 genera in 6 families of higher plants), 7 species of fungi, and 1 lichen species were reported. Of these, 122 compounds were isolated for the first time from nature. We discuss plant origin, the way of separation, and spectral analysis done for structure elucidation, along with a brief discussion of the chemosystematic significance.
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16.
  • Khalifa, Shaden A. M., et al. (author)
  • Cyanobacteria-From the Oceans to the Potential Biotechnological and Biomedical Applications
  • 2021
  • In: Marine Drugs. - : MDPI AG. - 1660-3397. ; 19:5
  • Research review (peer-reviewed)abstract
    • Cyanobacteria are photosynthetic prokaryotic organisms which represent a significant source of novel, bioactive, secondary metabolites, and they are also considered an abundant source of bioactive compounds/drugs, such as dolastatin, cryptophycin 1, curacin toyocamycin, phytoalexin, cyanovirin-N and phycocyanin. Some of these compounds have displayed promising results in successful Phase I, II, III and IV clinical trials. Additionally, the cyanobacterial compounds applied to medical research have demonstrated an exciting future with great potential to be developed into new medicines. Most of these compounds have exhibited strong pharmacological activities, including neurotoxicity, cytotoxicity and antiviral activity against HCMV, HSV-1, HHV-6 and HIV-1, so these metabolites could be promising candidates for COVID-19 treatment. Therefore, the effective large-scale production of natural marine products through synthesis is important for resolving the existing issues associated with chemical isolation, including small yields, and may be necessary to better investigate their biological activities. Herein, we highlight the total synthesized and stereochemical determinations of the cyanobacterial bioactive compounds. Furthermore, this review primarily focuses on the biotechnological applications of cyanobacteria, including applications as cosmetics, food supplements, and the nanobiotechnological applications of cyanobacterial bioactive compounds in potential medicinal applications for various human diseases are discussed.
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17.
  • Khalifa, Shaden A. M., et al. (author)
  • Frankincense of Boswellia sacra: Traditional and modern applied uses, pharmacological activities, and clinical trials
  • 2023
  • In: Industrial crops and products (Print). - : Elsevier. - 0926-6690 .- 1872-633X. ; 203
  • Journal article (peer-reviewed)abstract
    • Since Boswellia sacra (Burseraceae) was studied in the 19th century, it has been known for its economic and cultural values. It is cultivated mainly in the southwest regions of Oman and some regions of Yemen, and is a natural source of frankincense, "Luban" in Arabic, around the world. Frankincense, the aromatic resin of B. sacra, is used widely both for traditional purposes and for the treatment of various ailments; e.g., dental infections, tumors, dysentery, vomiting, and fevers. Recently, many reports provided evidence for the potential biological activities of B. sacra, its synonym Boswellia carteri, and their constituent chemical compounds. These activities include cytotoxic, anti-inflammatory, antimicrobial, anti-diabetes, immunomodulatory, and anticoagulant effects. B. sacra was also tested for effects against gastric, hepatic, neurological, and skin disorders in vitro and in vivo. Clinical trials revealed good effects against carcinomas and gliomas, as well as against bladder and brain tumors. Its uses as a plant-based agent in nanotechnology displayed promising results. More efforts should be directed to further investigate these safe, plant-based bio-preservatives, and best practices should be outlined to protect these trees from extinction.
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18.
  • Saifullah, S., et al. (author)
  • Surface functionalized magnetic nanoparticles for targeted cancer therapy and diagnosis
  • 2019
  • In: Metal Nanoparticles for Drug Delivery and Diagnostic Applications. - : Elsevier Inc.. ; , s. 215-236
  • Book chapter (other academic/artistic)abstract
    • In the last few decades, magnetic nanoparticles (MNPs) have had significant interest and became more remarkable in the field of oncology. MNPs has been proven to be the most suitable and promising nanomaterials for tumor targeting. This is mainly due to its intrinsic magnetic property which makes them characteristic agents to inducing magnetic hyperthermia and magnetic resonance imaging. The MNPs have usually been employed for cancer imaging through a passive approach. The modern techniques have enabled multimodal imaging, drug delivery, and specific cells targeting by MNPs. To synthesize more extravagant MNPs, the design criteria considerations, such as core metal, hydrodynamic size, shape, surface coating, and molecular functionalization, become very essential. In this chapter, the design parameters of MNPs including surface functionalization and physiochemical properties are summarized to overcome biological barriers. Furthermore, the chemistry of MNPs surface modification is discussed in detail to describe its nature and binding type.
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19.
  • El-Seedi, Hesham R., et al. (author)
  • Essential oil analysis of Micromeria nubigena HBK and its antimicrobial activity
  • 2008
  • In: The journal of essential oil research. - 1041-2905 .- 2163-8152. ; 20:5, s. 452-456
  • Journal article (peer-reviewed)abstract
    • Water-distilled essential oil from leaves and flowers of Micromeria nubigena H.B.K. (Lamiaceae) were analyzed by GC and GUMS systems. The major components identified were thymol (36.9%), carvacrol (16.7%), pulegone (10.8%), caryophyllene oxide (4.6%) and (E)-phytol (3.2%). The major volatiles released by beta P-glucosidase treatment of the aqueous plant residue were (Z)-3-hexenol (31.2%), (4-2-hexenol (18.3%) and delta-cadinene (3.4%). The oil showed significant antibacterial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, and Pseudomonas aeruginosa, and antifungal activity against Candida albicans, Botrytis cinerea and Aspergillus niger, while the beta-glucosidase-liberated fraction was inactive.
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20.
  • Hegazy, Mohamed-Elamir F., et al. (author)
  • Terpenoid bio-transformations and applications via cell/organ cultures : a systematic review
  • 2020
  • In: Critical reviews in biotechnology. - : Informa UK Limited. - 0738-8551 .- 1549-7801. ; 40:1, s. 64-82
  • Research review (peer-reviewed)abstract
    • Structurally diverse natural products are valued for their targeted biological activity. The challenge of working with such metabolites is their low natural abundance and complex structure, often with multiple stereocenters, precludes large-scale or unsophisticated chemical synthesis. Since select plants contain the enzymatic machinery necessary to produce specialized compounds, tissue cultures can be used to achieve key transformations for large-scale chemical and/or pharmaceutical applications. In this context, plant tissue-culture bio-transformations have demonstrated great promise in the preparation of pharmaceutical products. This review describes the capacity of cultured plant cells to transform terpenoid natural products and the specific application of such transformations over the past three decades (1988-2019).
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21.
  • Ibrahim, Mahmoud A. A., et al. (author)
  • Blue Biotechnology : Computational Screening of Sarcophyton Cembranoid Diterpenes for SARS-CoV-2 Main Protease Inhibition
  • 2021
  • In: Marine Drugs. - : MDPI. - 1660-3397. ; 19:7
  • Journal article (peer-reviewed)abstract
    • The coronavirus pandemic has affected more than 150 million people, while over 3.25 million people have died from the coronavirus disease 2019 (COVID-19). As there are no established therapies for COVID-19 treatment, drugs that inhibit viral replication are a promising target; specifically, the main protease (M-pro) that process CoV-encoded polyproteins serves as an Achilles heel for assembly of replication-transcription machinery as well as down-stream viral replication. In the search for potential antiviral drugs that target M-pro, a series of cembranoid diterpenes from the biologically active soft-coral genus Sarcophyton have been examined as SARS-CoV-2 M-pro inhibitors. Over 360 metabolites from the genus were screened using molecular docking calculations. Promising diterpenes were further characterized by molecular dynamics (MD) simulations based on molecular mechanics-generalized Born surface area (MM-GBSA) binding energy calculations. According to in silico calculations, five cembranoid diterpenes manifested adequate binding affinities as M-pro inhibitors with Delta G(binding) < -33.0 kcal/mol. Binding energy and structural analyses of the most potent Sarcophyton inhibitor, bislatumlide A (340), was compared to darunavir, an HIV protease inhibitor that has been recently subjected to clinical-trial as an anti-COVID-19 drug. In silico analysis indicates that 340 has a higher binding affinity against M-pro than darunavir with Delta G(binding) values of -43.8 and -34.8 kcal/mol, respectively throughout 100 ns MD simulations. Drug-likeness calculations revealed robust bioavailability and protein-protein interactions were identified for 340; biochemical signaling genes included ACE, MAPK14 and ESR1 as identified based on a STRING database. Pathway enrichment analysis combined with reactome mining revealed that 340 has the capability to re-modulate the p38 MAPK pathway hijacked by SARS-CoV-2 and antagonize injurious effects. These findings justify further in vivo and in vitro testing of 340 as an antiviral agent against SARS-CoV-2.
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22.
  • Khalifa, Shaden A. M., et al. (author)
  • Beyond the Pandemic : COVID-19 Pandemic Changed the Face of Life
  • 2021
  • In: International Journal of Environmental Research and Public Health. - : MDPI AG. - 1661-7827 .- 1660-4601. ; 18:11
  • Research review (peer-reviewed)abstract
    • The COVID-19 pandemic is a serious challenge for societies around the globe as entire populations have fallen victim to the infectious spread and have taken up social distancing. In many countries, people have had to self-isolate and to be confined to their homes for several weeks to months to prevent the spread of the virus. Social distancing measures have had both negative and positive impacts on various aspects of economies, lifestyles, education, transportation, food supply, health, social life, and mental wellbeing. On other hands, due to reduced population movements and the decline in human activities, gas emissions decreased and the ozone layer improved; this had a positive impact on Earth's weather and environment. Overall, the COVID-19 pandemic has negative effects on human activities and positive impacts on nature. This study discusses the impact of the COVID-19 pandemic on different life aspects including the economy, social life, health, education, and the environment.
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23.
  • Khan, Farooq-Ahmad, et al. (author)
  • Ruthenium Nanoparticles Intercalated in Montmorillonite (nano-Ru@MMT) Is Highly Efficient Catalyst for the Selective Hydrogenation of 2-Furaldehyde in Benign Aqueous Medium
  • 2021
  • In: Catalysts. - : MDPI AG. - 2073-4344. ; 11:1
  • Journal article (peer-reviewed)abstract
    • Chemoselective hydrogenation of 2-furaldehyde to furfuryl alcohol using green solvents is an important research area to get eco-friendly fuels and fine chemicals. Herein, we report ruthenium nanoparticles (similar to 1.8 nm) intercalated in montmorillonite as an efficient catalytic system, which can selectively hydrogenate 2-furaldehyde in a benign aqueous medium. The complete conversion was observed at 40 degrees C with 1 MPa H-2, the selectivity of furfuryl alcohol being >99%, and turnover number 1165. After a catalytic run, the montmorillonite-supported ruthenium nanoparticles can be recycled and reused without losing their activity and selectivity.
  •  
24.
  • Mohamed, Tarik A., et al. (author)
  • Plant cell cultures : An enzymatic tool for polyphenolic and flavonoid transformations
  • 2022
  • In: Phytomedicine. - : Elsevier BV. - 0944-7113 .- 1618-095X. ; 100
  • Journal article (peer-reviewed)abstract
    • Background: In the pharmaceutical sector, tissue culture techniques for large-scale production of natural chemicals can be a less expensive alternative to large-scale synthesis. Although recent biotransformation research have used plant cell cultures to target a wide range of bioactive compounds, more compiled information and synopses are needed to better understand metabolic pathways and improve biotransformation efficiencies.Purpose: This report reviews the biochemical transformation of phenolic natural products by plant cell cultures in order to identify potential novel biotechnological approaches for ensuring more homogeneous and stable phenolic production year-round under controlled environmental conditions.Methods: Articles on the use of plant cell culture for polyphenolic and flavonoid transformations (1988 - 2021) were retrieved from SciFinder, PubMed, Scopus, and Web of Science through electronic and manual search in English. Following that, the authors chose the required papers based on the criteria they defined. The following keywords were used for the online search: biotransformation, Plant cell cultures, flavonoids, phenolics, and pharmaceutical products.Results: The initial search found a total of 96 articles. However, only 70 of them were selected as they met the inclusion criteria defined by the authors. The analysis of these studies revealed that plant tissue culture is applicable for the large-scale production of plant secondary metabolites including the phenolics, which have high therapeutic value.Conclusion: Plant tissue cultures could be employed as an efficient technique for producing secondary metabolites including phenolics. Phenolics possess a wide range of therapeutic benefits, as anti-oxidant, anti-cancer, and antiinflammatory properties. Callus culture, suspension cultures, transformation, and other procedures have been used to improve the synthesis of phenolics. Their production on a large scale is now achievable. More breakthroughs will lead to newer insights and, without a doubt, to a new era of phenolics-based pharmacological agents for the treatment of a variety of infectious and degenerative disorders.
  •  
25.
  • Saeed, A., et al. (author)
  • Synthesis, Antibacterial and Antileishmanial Activity, Cytotoxicity, and Molecular Docking of New Heteroleptic Copper(I) Complexes with Thiourea Ligands and Triphenylphosphine
  • 2018
  • In: Russian journal of general chemistry. - : MAIK NAUKA/INTERPERIODICA/SPRINGER. - 1070-3632 .- 1608-3350. ; 88:3, s. 541-550
  • Journal article (peer-reviewed)abstract
    • A series of copper(I) complexes with triphenylphosphine and N-acyl-N'-arylthioureas were synthesized and characterized by elemental analysis and IR and NMR (H-1, C-13, P-31) spectroscopy. The thiourea ligands and their copper(I) triphenylphosphine complexes were screened for antibacterial and antileishmanial activities and cytotoxicity. The synthesized compounds showed much better activity as compared to glucantime and Kanamycin used as reference drugs. The thiourea ligands showed better activity than their Cu(I) complexes. The molecular docking technique was utilized to ascertain the mechanism of action toward molecular targets (GP63 and 16S-rRNA A-site). It was found that the ligands and complexes were stabilized at the active site by electrostatic and hydrophobic forces, consistent with the corresponding experimental results. The in silico study of the binding pattern predicted that one of the synthesized ligands, N-(5-chloro-2-nitrophenyl)-N'-pentanoylthiourea, can serve as a potential surrogate for hit-to-lead generation and design of novel antibacterial and antileishmanial agents.
  •  
26.
  • Yosri, Nermeen, et al. (author)
  • Anti-Viral and Immunomodulatory Properties of Propolis : Chemical Diversity, Pharmacological Properties, Preclinical and Clinical Applications, and In Silico Potential against SARS-CoV-2
  • 2021
  • In: Foods. - : MDPI AG. - 2304-8158. ; 10:8
  • Research review (peer-reviewed)abstract
    • Propolis, a resin produced by honeybees, has long been used as a dietary supplement and folk remedy, and more recent preclinical investigations have demonstrated a large spectrum of potential therapeutic bioactivities, including antioxidant, antibacterial, anti-inflammatory, neuroprotective, immunomodulatory, anticancer, and antiviral properties. As an antiviral agent, propolis and various constituents have shown promising preclinical efficacy against adenoviruses, influenza viruses, respiratory tract viruses, herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), human immunodeficiency virus (HIV), and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Over 300 chemical components have been identified in propolis, including terpenes, flavonoids, and phenolic acids, with the specific constituent profile varying widely according to geographic origin and regional flora. Propolis and its constituents have demonstrated potential efficacy against SARS-CoV-2 by modulating multiple pathogenic and antiviral pathways. Molecular docking studies have demonstrated high binding affinities of propolis derivatives to multiple SARS-CoV-2 proteins, including 3C-like protease (3CL(pro)), papain-like protease (PLpro), RNA-dependent RNA polymerase (RdRp), the receptor-binding domain (RBD) of the spike protein (S-protein), and helicase (NSP13), as well as to the viral target angiotensin-converting enzyme 2 (ACE2). Among these compounds, retusapurpurin A has shown high affinity to 3CL(pro) (Delta G = -9.4 kcal/mol), RdRp (-7.5), RBD (-7.2), NSP13 (-9.4), and ACE2 (-10.4) and potent inhibition of viral entry by forming hydrogen bonds with amino acid residues within viral and human target proteins. In addition, propolis-derived baccharin demonstrated even higher binding affinity towards PLpro (-8.2 kcal/mol). Measures of drug-likeness parameters, including metabolism, distribution, absorption, excretion, and toxicity (ADMET) characteristics, also support the potential of propolis as an effective agent to combat COVID-19.
  •  
27.
  • Abdelmoniem, Amr M., et al. (author)
  • Synthesis, Chemistry and Utilities of Diaminoazoles with Special Reference to 3,5-Diaminopyrazoles
  • 2018
  • In: Current Organic Synthesis. - : BENTHAM SCIENCE PUBL LTD. - 1570-1794 .- 1875-6271. ; 15:4, s. 487-514
  • Research review (peer-reviewed)abstract
    • Background: Although the chemistry of heteroaromatic monoamino azoles has been surveyed more than once in the last decade, the chemistry of the di- and triaminoazoles has not been reviewed. In this article we will survey the synthesis, chemistry and utility of the diaminoazoles. In this review, the chemistry of the diaminoazoles as well as their most important utilities will be surveyed. Objective: The review focuses on recent progress in diaminoazoles (i.e. diaminopyrazoles, diaminoimidazoles, diaminotriazoles and diaminothiazole) with especial references to diaminopyrazoles. The synthesis as well as pharmaceutical utilities are reported. There are several methods for synthesis of diaminopyrazoles. 3,5-Diaminopyrazole and its derivatives are prepared through the reaction of malononitrile or arylhydrazononitrile with hydrazine derivatives. 3,4-Diaminopyrazoles are prepared via nitration of 3-aminopyrazole with subsequent reduction of the produced compound. The diaminopyrazoles have several applications in cosmetic and pharmaceutical industries. They also have useful utilities as a constituent in oxidative hair dyes. Conclusion: We managed to report the common methods for the synthesis of diaminoazoles with especial reference to aminopyrazoles that are prepared through the reaction of malononitrile or hydrazononitriles with hydrazine derivatives. Some important applications that include pharmaceutical utilities such as hair dye constituents are reported.
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28.
  • Bhat, M. A., et al. (author)
  • Synthesis, Anti-inflammatory, and Neuroprotective Activity of N-Substituted Phthalimide Derivatives
  • 2023
  • In: Russian journal of general chemistry. - : Pleiades Publishing Ltd. - 1070-3632 .- 1608-3350. ; 93:11, s. 2935-2940
  • Journal article (peer-reviewed)abstract
    • A new series of N-substituted phthalimide compounds was synthesized in good yield. All the compounds were characterized by spectroscopic data and were evaluated for their inhibitory activity against the expression of cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS) and pro-inflammatory proteins in the bacterial lipopolysaccharide (LPS)-induced murine macrophage (RAW 264.7) cells. All the compounds significantly (p <0.05) downregulated the LPS-stimulated COX-2 and iNOS expression from 100% to the ranges of 61.9±5.1–84.5±4.1% and 41.1±5.4–85.3±1.9%) at 10 µM, respectively. Among others, 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N′-[(3,4-dichlorophenyl)methylidene]benzohydrazide displayed the most potent inhibition to the level of (41.1±5.4%) iNOS expression, about half of the potency of dexamethasone (23.0±3.3%). Moreover, the neuroprotective activity of the compounds was assessed against the 6-hydroxydopamine (6-OHDA)-challenged neuroblastoma SH-ST5Y cells, and all compounds exhibited significant (p <0.05) protection with variable potencies. 4-(1,3-Dioxo-1,3-dihydro-2H-isoindol-2-yl)-N′-[(3,4-dihydroxyphenyl)methylidene]benzohydrazide was found to display more than 70% relative neuroprotection against 6-OHDA-induced cell death with the additional advantage of keeping the highest cell viability index (83.3±4.5%) to the cells.
  •  
29.
  • El-Seedi, H, et al. (author)
  • Cyclopeptide alkaloids
  • 2007
  • In: Phytochemistry Reviews. - : Springer Science and Business Media LLC. - 1568-7767 .- 1572-980X. ; 6:1, s. 143-165
  • Journal article (peer-reviewed)abstract
    • In this review, we discuss cyclopeptide alkaloids, their plant origin, and the way of separation, spectral analysis done for structure elucidation, stereochemistry, and their biological activities. In addition, we discuss briefly the chemosystematic significance of the cyclopeptide alkaloids based on their discovery in the family Olacaceae.
  •  
30.
  • El-Seedi, Hesham R., et al. (author)
  • Essential oils of aromatic Egyptian plants repel nymphs of the tick Ixodes ricinus (Acari : Ixodidae)
  • 2017
  • In: Experimental & applied acarology. - : Springer. - 0168-8162 .- 1572-9702. ; 73:1, s. 139-157
  • 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.
  •  
31.
  • El-Seedi, H. R., et al. (author)
  • Hydroxycinnamic Acids : Natural Sources, Biosynthesis, Possible Biological Activities, and Roles in Islamic Medicine
  • 2017
  • In: Studies in Natural Products Chemistry. - : Elsevier B.V.. ; , s. 1-29
  • Book chapter (peer-reviewed)abstract
    • Hydroxycinnamic acids are the most widely distributed phenolic acids in plants. Broadly speaking, they can be defined as compounds derived from cinnamic acid. They are present at high concentrations in many food products, including fruits, vegetables, tea, cocoa, and wine. Cinnamic acid has received great attention in oriental research where it has been used as an antioxidant in food additives in Asia and especially in medical studies in China after being proven to be an effective component of medicinal herbs used by traditional medicine. Cinnamic acid is a phenolic acid widely distributed in the plant kingdom. It presents a wide range of potential therapeutic effects useful in the treatments of cancer, diabetes, lung, and cardiovascular diseases, as well as hepatic, neuro-, and photoprotective effects and antimicrobial and antiinflammatory activities. Overall, the pharmaceutical potential of cinnamic acid can be attributed to its ability to scavenge free radicals. However, recent studies have revealed that cinnamic acid presents pharmacological properties beyond those related to its antioxidant activity, such as the ability to competitively inhibit HMG-CoA reductase and activate glucokinase, contributing to reduce hypercholesterolemia and hyperglycemia, respectively. A diet rich in hydroxycinnamic acids is thought to be associated with beneficial health effects such as a reduced risk of cardiovascular disease. The impact of hydroxycinnamic acids on health depends on their intake and pharmacokinetic properties. It can be found free, dimerized or esterified with proteins and polysaccharides in the cell wall, such as arabinoxylans in grasses and xyloglucans in bamboo. Cinnamic acid is an important biological and structural component of the plant cell wall. Due to its ability to stop radical chain reactions by resonance followed by polymerization, cinnamic acid offers protection against UV radiation and is responsible for cross-linking polysaccharides and other cell wall polymers. Cinnamic acid can be absorbed by the small intestine and excreted in the urine, where therapeutic efficacy is dependent on its physiological concentrations and pharmacokinetic properties, which include absorption, distribution, metabolism, and excretion of metabolites. Mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy, especially 2D NMR (COSY, NOESY, HMQC, and HMBC), are the most useful analytical techniques for the structural elucidation of hydroxycinnamic acids besides UV, IR, CD, X-ray analysis, and chemical degradation. In this chapter, we update the reader about the therapeutic properties of cinnamic acid, reviewing its dietary sources, the pharmacokinetic profile, antioxidant action mechanisms, and therapeutic effects in the treatment and prevention of various diseases, in order to provide a basis for understanding its pharmaceutical potential.
  •  
32.
  • Farag, Mohamed A., et al. (author)
  • Phytochemical Profiles and Antimicrobial Activities of Allium cepa Red cv. and A. sativum Subjected to Different Drying Methods : A Comparative MS-Based Metabolomics
  • 2017
  • In: Molecules. - : MDPI AG. - 1431-5157 .- 1420-3049. ; 22:5
  • Journal article (peer-reviewed)abstract
    • Plants of the Allium genus produce sulphur compounds that give them a characteristic (alliaceous) flavour and mediate for their medicinal use. In this study, the chemical composition and antimicrobial properties of Allium cepa red cv. and A. sativum in the context of three different drying processes were assessed using metabolomics. Bulbs were dried using either microwave, air drying, or freeze drying and further subjected to chemical analysis of their composition of volatile and non-volatile metabolites. Volatiles were collected using solid phase micro-extraction (SPME) coupled to gas chromatography-mass spectrometry (GC/MS) with 42 identified volatiles including 30 sulphur compounds, four nitriles, three aromatics, and three esters. Profiling of the polar non-volatile metabolites via ultra-performance liquid chromatography coupled to high resolution MS (UPLC/MS) annotated 51 metabolites including dipeptides, flavonoids, phenolic acids, and fatty acids. Major peaks in GC/MS or UPLC/MS contributing to the discrimination between A. sativum and A. cepa red cv. were assigned to sulphur compounds and flavonoids. Whereas sulphur conjugates amounted to the major forms in A. sativum, flavonoids predominated in the chemical composition of A. cepa red cv. With regard to drying impact on Allium metabolites, notable and clear separations among specimens were revealed using principal component analysis (PCA). The PCA scores plot of the UPLC/MS dataset showed closer metabolite composition of microwave dried specimens to freeze dried ones, and distant from air dried bulbs, observed in both A. cepa and A. sativum. Compared to GC/MS, the UPLC/MS derived PCA model was more consistent and better in assessing the impact of drying on Allium metabolism. A phthalate derivative was found exclusively in a commercial garlic preparation via GC/MS, of yet unknown origin. The freeze dried samples of both Allium species exhibited stronger antimicrobial activities compared to dried specimens with A. sativum being in general more active than A. cepa red cv.
  •  
33.
  • Ibrahim, Mahmoud A. A., et al. (author)
  • In silico drug discovery of major metabolites from spices as SARS-CoV-2 main protease inhibitors
  • 2020
  • In: Computers in Biology and Medicine. - : Elsevier BV. - 0010-4825 .- 1879-0534. ; 126
  • Journal article (peer-reviewed)abstract
    • Coronavirus Disease 2019 (COVID-19) is an infectious illness caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), originally identified in Wuhan, China (December 2019) and has since expanded into a pandemic. Here, we investigate metabolites present in several common spices as possible inhibitors of COVID-19. Specifically, 32 compounds isolated from 14 cooking seasonings were examined as inhibitors for SARS-CoV-2 main protease (MPrn), which is required for viral multiplication. Using a drug discovery approach to identify possible antiviral leads, in silico molecular docking studies were performed. Docking calculations revealed a high potency of salvianolic acid A and curcumin as MPr inhibitors with binding energies of 9.7 and 9.2 kcal/mol, respectively. Binding mode analysis demonstrated the ability of salvianolic acid A and curcumin to form nine and six hydrogen bonds, respectively with amino acids proximal to MPr 's active site. Stabilities and binding affinities of the two identified natural spices were calculated over 40 ns molecular dynamics simulations and compared to an antiviral protease inhibitor (lopinavir). Molecular mechanics-generalized Born surface area energy calculations revealed greater salvianolic acid A affinity for the enzyme over curcumin and lopinavir with energies of 44.8, 34.2 and 34.8 kcal/mol, respectively. Using a STRING database, protein-protein interactions were identified for salvianolic acid A included the biochemical signaling genes ACE, MAPK14 and ESR1; and for curcumin, EGFR and TNF. This study establishes salvianolic acid A as an in silico natural product inhibitor against the SARS-CoV-2 main protease and provides a promising inhibitor lead for in vitro enzyme testing.
  •  
34.
  • Ibrahim, Mahmoud A. A., et al. (author)
  • In Silico Mining of Terpenes from Red-Sea Invertebrates for SARS-CoV-2 Main Protease (M-pro) Inhibitors
  • 2021
  • In: Molecules. - : MDPI AG. - 1431-5157 .- 1420-3049. ; 26:7
  • Journal article (peer-reviewed)abstract
    • Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the causative agent for the COVID-19 pandemic, which generated more than 1.82 million deaths in 2020 alone, in addition to 83.8 million infections. Currently, there is no antiviral medication to treat COVID-19. In the search for drug leads, marine-derived metabolites are reported here as prospective SARS-CoV-2 inhibitors. Two hundred and twenty-seven terpene natural products isolated from the biodiverse Red-Sea ecosystem were screened for inhibitor activity against the SARS-CoV-2 main protease (M-pro) using molecular docking and molecular dynamics (MD) simulations combined with molecular mechanics/generalized Born surface area binding energy calculations. On the basis of in silico analyses, six terpenes demonstrated high potency as M-pro inhibitors with Delta G(binding) <= -40.0 kcal/mol. The stability and binding affinity of the most potent metabolite, erylosides B, were compared to the human immunodeficiency virus protease inhibitor, lopinavir. Erylosides B showed greater binding affinity towards SARS-CoV-2 M-pro than lopinavir over 100 ns with Delta G(binding) values of -51.9 vs. -33.6 kcal/mol, respectively. Protein-protein interactions indicate that erylosides B biochemical signaling shares gene components that mediate severe acute respiratory syndrome diseases, including the cytokine- and immune-signaling components BCL2L1, IL2, and PRKC. Pathway enrichment analysis and Boolean network modeling were performed towards a deep dissection and mining of the erylosides B target-function interactions. The current study identifies erylosides B as a promising anti-COVID-19 drug lead that warrants further in vitro and in vivo testing.
  •  
35.
  • Ibrahim, N. A., et al. (author)
  • Constituents and biological activity of the chloroform extract and essential oil of Cupressus sempervirens
  • 2009
  • In: Chemistry of Natural Compounds. - : Springer Science and Business Media LLC. - 0009-3130 .- 1573-8388. ; 45:3, s. 309-313
  • Journal article (peer-reviewed)abstract
    • The essential oil of the leaves of Cupressus sempervirens L. was isolated by hydrodistillation and tested against gram positive and gram negative bacteria, showing remarkable antimicrobial activity against Bacillus subtilis with minimum inhibitory concentration (MIC) 75%. The antiviral activity of the essential oil was tested against Herpes simplex virus type 1 (HSV-1), showing antiviral activity with virucidal percentages of 68.0% and 53.2% at concentrations of 1:32 and 1:64, respectively. We firstly reported the isolation of two epi-betulin esters of fatty acids from the CHCl3 fraction of Cupressus sempervirens L. leaves, which were isolated and purified using HPLC, and identified using PMR and MS. The CHCl3 fraction showed significant cytotoxicity against HeLa cells.
  •  
36.
  • Shokry, Dina M., et al. (author)
  • Moringa oleifera leaves extract enhances fresh and cryopreserved semen characters of Barki rams
  • 2020
  • In: Theriogenology. - : ELSEVIER SCIENCE INC. - 0093-691X .- 1879-3231. ; 153, s. 133-142
  • Journal article (peer-reviewed)abstract
    • This study was carried out to evaluate the efficacy of Moringa oleifera leaves extract (MOLE) to improve the characters of fresh and cryopreserved semen of Barki rams compared to vitamin E and Selenium combination. Twenty-four mature Barki rams (50-70 Kg) were randomly assigned into three groups, eight rams each. The first group was given distilled water orally. The second group was given MOLE orally daily at a dose of 40 mg/kg. The third group was injected with a combination of vitamin E and selenium at a dose of 3 ml (4.5 mg sodium selenite and 204 mg vitamin E)/head i.m twice a week for 64 days. Moringa oleifera leaves extract increased semen volume, sperm concentration, activities of seminal plasma catalase, glutathione peroxidase (GPx), glutathione reductase (GR), superoxide dismutase (SOD), alkaline phosphatase (ALP), acid phosphatase (ACP), levels of ascorbic acid and total antioxidant capacity (TAC). In addition, it significantly increased post thawing sperms motility, viability index, membrane integrity, and the activities of post thawing semen antioxidant enzymes. While it decreased seminal plasma concentration of malondialdehyde (MDA) and acrosomal defects and DNA fragmentation of sperm in cryopreserved semen. Vitamin E and selenium decreased semin volume, sperm concentration, seminal plasma ascorbic acid, TAC concentrations and activities of antioxidant enzymes while it increased sperm abnormalities, DNA fragmentation and MDA concentration in seminal plasma. This study indicated that Moringa oleifera leaves extract improved the characters of the fresh and cryopreserved semen of Barki rams via improving seminal plasma antioxidant defense mechanism. (C) 2020 Elsevier Inc. All rights reserved.
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