| 1. |
- El-Seedi, Hesham R., et al.
(författare)
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Cardenolides : Insights from chemical structure and pharmacological utility
- 2019
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Ingår i: Pharmacological Research. - : Academic Press. - 1043-6618 .- 1096-1186. ; 141, s. 123-175
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Tidskriftsartikel (refereegranskat)abstract
- Cardiac glycosides (CGs) are a class of naturally occurring steroid-like compounds, and members of this class have been in clinical use for more than 1500 years. They have been used in folk medicine as arrow poisons, abortifacients, heart tonics, emetics, and diuretics as well as in other applications. The major use of CGs today is based on their ability to inhibit the membrane-bound Na + /K + -ATPase enzyme, and they are regarded as an effective treatment for congestive heart failure (CHF), cardiac arrhythmia and atrial fibrillation. Furthermore, increasing evidence has indicated the potential cytotoxic effects of CGs against various types of cancer. In this review, we highlight some of the structural features of this class of natural products that are crucial for their efficacy, some methods of isolating these compounds from natural resources, and the structural elucidation tools that have been used. We also describe their physicochemical properties and several modern biotechnological approaches for preparing CGs that do not require plant sources.
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| 2. |
- Sayed, Abdelwahed R., et al.
(författare)
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One-Pot Synthesis of Novel Thiazoles as Potential Anti-Cancer Agents
- 2020
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Ingår i: Drug Design, Development and Therapy. - 1177-8881. ; 14, s. 1363-1375
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Tidskriftsartikel (refereegranskat)abstract
- Background: Thiazole and thiosemicarbazone derivatives are known to have potential anticancer activity with a mechanism of action related to inhibition of matrix metallo-proteinases, kinases and anti-apoptotic BCL2 family proteins.Materials and Methods: A novel three series of 5-(1-(2-(thiazol-2-yl)hydrazono)ethyl) thiazole derivatives were prepared in a one-pot three-component reaction using 2-(2-benzylidene hydrazinyl)-4-methylthiazole as a starting precursor. MS, IR, H-1-NMR and C-13-NMR were used to elucidate the structures of the synthesized compounds. Most of the synthesized products were evaluated for their in vitro anticancer screening against HCT-116, HT-29 and HepG2 using the MTT colorimetric assay.Results: The results indicated that compounds 4c, 4d and 8c showed growth inhibition activity against HCT-116 with IC50 values of 3.80 +/- 0.80, 3.65 +/- 0.90 and 3.16 +/- 0.90 mu M, respectively, compared to harmine (IC50 = 2.40 +/- 0.12 mu M) and cisplatin (IC50 = 5.18 +/- 0.94 mu M) reference drugs. Also, compounds 8c, 4d and 4c showed promising IC(50 )values of 3.47 +/- 0.79, 4.13 +/- 0.51 and 7.24 +/- 0.62 mu M, respectively, against the more resistant human colorectal cancer (HT-29) cell line compared with harmine (IC50 = 4.59 +/- 0.67 mu M) and cisplatin (IC50 = 11.68 +/- 1.54 mu M). On the other hand, compounds 4d, 4c, 8c and llc were the most active (IC50 values of 2.31 +/- 0.43, 2.94 +/- 0.62, 4.57 +/- 0.85 and 9.86 +/- 0.78 mu M, respectively) against the hepatocellular carcinoma (HepG2) cell line compared with harmine (IC50 = 2.54 +/- 0.82 mu M) and cisplatin (IC50 = 41 +/- 0.63 pM). The study also suggested that the mechanism of the anticancer action exerted by the most active compounds (4c, 4d and 8c) inside HCT-116 cells was apoptosis through the Bcl-2 family.Conclusion: Thiazole scaffolds 4c, 4d and 8c showed anticancer activities in the micromolar range and are appropriate as a candidate for cancer treatment.
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| 3. |
- El-Seedi, Hesham R., et al.
(författare)
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Chemical Composition and Repellency of Essential Oils From Four Medicinal Plants Against Ixodes ricinus Nymphs : (Acari Ixodidae)
- 2012
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Ingår i: Journal of medical entomology. - 0022-2585 .- 1938-2928. ; 49:5, s. 1067-1075
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Tidskriftsartikel (refereegranskat)abstract
- In our search for effective tick repellents from plant origin, we investigated the effect of essential oils of four medicinal and culinary plants belonging to the family Lamiaceae on nymphs of the tick Ixodes ricinus (L.). The essential oils of the dry leaves of Rosmarinus officinalis (Rosemary) (L.), Mentha spicata (Spearmint) (L.), Origanum majorana (Majoram) (L.), and Ocimum basilicum (Basil) (L.) were isolated by steam distillation and 15 mu g/cm(2) concentration of oils was tested against ticks in a laboratory bioassay. The oils of R. officinalis, M. spicata, and O. majorana showed strong repellency against the ticks 100, 93.2, and 84.3%, respectively, whereas O. basilicum only showed 64.5% repellency. When tested in the field, the oils of R. officinalis and M. spicata showed 68.3 and 59.4% repellency at a concentration of 6.5 mu g/cm(2) on the test cloths. The oils were analyzed by gas chromatography mass spectrometry and the major compounds from the most repellent oils were 1,8-cineole, camphor, linalool, 4-terpineol, borneol, and carvone.
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| 4. |
- Hussein, Mohammad H., et al.
(författare)
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Beta 2 -adrenergic receptor gene haplotypes and bronchodilator response in Egyptian patients with chronic obstructive pulmonary disease
- 2017
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Ingår i: Advances in Medical Sciences. - Warsaw, Poland : Elsevier. - 1896-1126 .- 1898-4002. ; 62:1, s. 193-201
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Tidskriftsartikel (refereegranskat)abstract
- Purpose: Chronic obstructive pulmonary disease (COPD) is a multi-factorial disorder caused by environmental determinants and genetic risk factors. Understanding the genetic predisposition of COPD is essential to develop personalized treatment regimens. Beta2-adrenergic receptor (ADRB2) gene polymorphisms have been implicated in the pathogenesis of obstructive pulmonary diseases. This study was conducted to assess the genetic association between Arg16Gly and Gln27Glu polymorphisms and COPD in the Egyptian patients, and to analyze their impact on the clinical outcome and therapeutic response.Patients/methods: The study population included 115 participants (61 COPD patients and 54 healthy controls) were genotyped for the Arg16Gly (rs1042713) and Gln27Glu (rs1042714) polymorphisms. Pulmonary function test was done and repeated in patients after salbutamol inhalation.Results: The Gly16 and Gln27 alleles represented 57% and 70% of the whole study population, and only 3 haplotypes were detected; Arg16/Gln27, Gly16/Gln27, and Gly16/Glu27. Genotypes and haplotypes homozygous for Arg16 and Gln27 were more likely to develop COPD (p<0.05). However, individuals carrying Glu27 allele conferred protection against COPD development (p=0.002). Furthermore, Arg16 genotypes and haplotypes were significantly associated with higher grades of dyspnea, more COPD symptoms and frequent exacerbations. In contrast, patients carrying Glu27 allele had better bronchial airway responsiveness to β2-agonists.Conclusions: Our findings suggested that the ADRB2 gene polymorphisms may have vital role in COPD risk, severity, and bronchodilator response among Egyptian population. Larger epidemiological studies are needed for results validation.
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| 5. |
- Maher, Shymaa, et al.
(författare)
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Comparison of the osteogenic differentiation potential of mesenchymal cells isolated from human bone marrow, umbilical cord blood and placenta derived stem cells
- 2015
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Ingår i: Beni-Suef University Journal of Basic and Applied Sciences. - Heidelberg, Germany : Springer. - 2314-8535. ; 4:1, s. 80-85
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Tidskriftsartikel (refereegranskat)abstract
- Bone marrow has been considered for long time as the main source for mesenchymal stem cells. However, bone marrow aspiration is an invasive process that can be associated with morbidity as well as few numbers of obtained cells. Umbilical cord blood and placental tissues are other potential sources for the same type of cells. These sources are abundant, accessible and associated with no harm to the donor. This study aimed at determining the differentiation of the three cell types towards the osteogenic lineage in short term culture and in classical osteogenic conditions. The gene expression profile showed that bone marrow derived cells were the most responsive to the culture conditions while umbilical cord blood derived cells were next, as shown by the expression by the osteogenic key transcription factors ‘Runx-2’ and osterix. At the meantime, umbilical cord blood and placenta derived cells showed significant enhancement of the gene expression over the study course, which denoted potential response of the cells. Based on these results and the availability of these two sources, umbilical cord blood and placenta should still be considered as potential sources for mesenchymal stem cells in osteogenic research program. However their differentiation potential will need further enhancement.
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