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1.
Nabiel A.M. Saleh Zeinab A.R. El-karemy Ragaa M.A. Mansour Abdel-Aziz A. Fayed 《Phytochemistry》1983,22(11):2501-2505
The flavonoids of five Geranium, fourteen Erodium and four Monsonia species were studied. Quercetin was the most common aglycone with lesse 相似文献
2.
Salem MH Mekkawy MY Ahmed NA Abdel-Aziz IY Mohamed AA El-Oksh HA Pursel VG 《Theriogenology》1992,37(5):1061-1074
Ejaculated washed ram spermatozoa showed consistent increases in the intracellular concentration of cyclic 3', 5'-adenosine monophosphate (cAMP) after incubation for 15 minutes with the phosphodiesterase (PDE)-inhibitors, theophylline and caffeine. In vitro addition of cAMP or PDE-inhibitors to ram semen also stimulated and maintained sperm motility and enhanced the rate of fructose utilization. The same doses of cAMP or theophylline significantly stimulated the rate of protein synthesis by the washed spermatozoa, while the PDE-stimulator, imidazole, inhibited protein synthesis significantly. The stimulatory effect of cAMP on sperm protein synthesis was not affected by cycloheximide, but was abolished by the mitochondrial inhibitor, chloramphenicol. The present results indicate a positive correlation between the intracellular concentration of cAMP and the rates of progressive motility, fructose utilization, and protein synthesis by ram spermatozoa. The results suggest that the effect of cAMP is associated with the synthesis of mitochndrial proteins which may be involved with the observed enhancement of sperm motility and metabolism. The data also indicate that cAMP map act either as a first or a second messenger in mature spermatoza. 相似文献
3.
Extraction with hydrochloric acid (pH 2.5) of the brown alga Padina pavonia afforded water-soluble and water-insoluble polysaccharides comprising D-glucuronic acid, L-fucose, D-xylose, D-mannose, D-glucose and D- galactose residues. The water-soluble polysaccharide was fractionated by using ethanol, and cetylpyridinium chloride and by chromatography on DEAE-cellulose. A neutral laminaran-like glucan, a sulphated heteropolysaccharide composed of the aforementioned sugars and a protein moiety were obtained. The isolated heteropolysaccharide showed high anticoagulation activity. 相似文献
4.
5.
Ahmed M. Alafeefy Semra Isik Nabila A. Al-Jaber Daniela Vullo Hatem A. Abdel-Aziz Abdelkader E. Ashour Amani S. Awaad Clemente Capasso Claudiu T. Supuran 《Bioorganic & medicinal chemistry letters》2013,23(12):3570-3575
A series of benzenesulfonamides incorporating cyanoacrylamide moieties (tyrphostine analogs) were assayed as inhibitors of the β-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA. Some of these compounds were low nanomolar or subnanomolar ScCA inhibitors and showed selectivity ratios in the range of 4.91–69.86 for inhibiting the yeast enzyme over the offtarget human (h) isoforms hCA I and of 6.46–13.52 for inhibiting ScCA over hCA II. The model organism S. cerevisiae and this particular enzyme may be useful for detecting antifungals with a novel mechanism of action compared to the classical azole drugs to which significant drug resistance emerged. Indeed, some of these sulfonamides inhibited the growth of the yeast with CC50-s in the range of 0.73–6.54 μM. 相似文献
6.
Christopher Weidner Morten Rousseau Annabell Plauth Sylvia J. Wowro Cornelius Fischer Heba Abdel-Aziz Sascha Sauer 《PloS one》2016,11(4)
Massively increasing global incidences of colorectal cancer require efficient treatment and prevention strategies. Here, we report unexpected anticancerogenic effects of hydroethanolic Iberis amara extract (IAE), which is known as a widely used phytomedical product for treating gastrointestinal complaints. IAE significantly inhibited the proliferation of HT-29 and T84 colon carcinoma cells with an inhibitory concentration (IC50) of 6 and 9 μg/ml, respectively, and further generated inhibitory effects in PC-3 prostate and MCF7 breast cancer cells. Inhibition of proliferation in HT-29 cells was associated with a G2/M phase cell cycle arrest including reduced expression of various regulatory marker proteins. Notably, in HT-29 cells IAE further induced apoptosis by intracellular formation of reactive oxygen species (ROS). Consistent with predictions derived from our in vitro experiments, bidaily oral gavage of 50 mg/kg of IAE over 4 weeks resulted in significant inhibition of tumor growth in a mouse HT-29 tumor xenograft model. Taken together, Iberis amara extracts could become useful alternatives for preventing and treating the progression of colon cancer. 相似文献
7.
Ibrahim A. Al-Suwaidan Alaa A.-M. Abdel-Aziz Taghreed Z. Shawer Rezk R. Ayyad Amer M. Alanazi Ahmad M. El-Morsy 《Journal of enzyme inhibition and medicinal chemistry》2016,31(1):78-89
A novel series of 3-benzyl-substituted-4(3H)-quinazolinones were designed, synthesized and evaluated for their in vitro antitumor activity. The results of this study demonstrated that 2-(3-benzyl-6-methyl-4-oxo-3,4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl)acetamide, 2-(3-benzyl-6,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl)acetamide and 3-(3-benzyl-6-methyl-4-oxo-3,4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl)-propanamide have shown amazing broad spectrum antitumor activity with mean GI50 (10.47, 7.24 and 14.12?µM. respectively), and are nearly 1.5–3.0-fold more potent compared with the positive control 5-FU with mean GI50, 22.60?µM. On the other hand, compounds 6 and 10 yielded selective activities toward CNS, renal and breast cancer cell lines, whereas compound 9 showed selective activities towards leukemia cell lines. Molecular docking methodology was performed for compounds 7 and 8 into ATP binding site of EGFR-TK which showed similar binding mode to erlotinib, while compound 11 into ATP binding site of B-RAF kinase inhibited the growth of melanoma cell lines through inhibition of B-RAF kinase, similar to PLX4032. 相似文献
8.
Amer M. Alanazi Alaa A.-M. Abdel-Aziz Taghreed Z. Shawer Rezk R. Ayyad Abdulrahman M. Al-Obaid Mohamed H. M. Al-Agamy 《Journal of enzyme inhibition and medicinal chemistry》2016,31(5):721-735
Some new derivatives of substituted-4(3H)-quinazolinones were synthesized and evaluated for their in vitro antitumor and antimicrobial activities. The results of this study demonstrated that compound 5 yielded selective activities toward NSC Lung Cancer EKVX cell line, Colon Cancer HCT-15 cell line and Breast Cancer MDA-MB-231/ATCC cell line, while NSC Lung Cancer EKVX cell line and CNS Cancer SF-295 cell line were sensitive to compound 8. Additionally, compounds 12 and 13 showed moderate effectiveness toward numerous cell lines belonging to different tumor subpanels. On the other hand, the results of antimicrobial screening revealed that compounds 1, 9 and 14 are the most active against Staphylococcus aureus ATCC 29213 with minimum inhibitory concentration (MIC) of 16, 32 and 32?μg/mL respectively, while compound 14 possessed antimicrobial activities against all tested strains with the lowest MIC compared with other tested compounds. In silico study, ADME-Tox prediction and molecular docking methodology were used to study the antitumor activity and to identify the structural features required for antitumor activity. 相似文献
9.
Badria FA Dawidar AA Houssen WE Shier WT 《Zeitschrift für Naturforschung. C, Journal of biosciences》2005,60(1-2):139-142
There is a wealth of evidence that hepatic stellate cells (HSCs) orchestrate most of the important events in liver fibrogenesis. After liver injury, HSCs become activated to a profibrogenic myofibroblastic phenotype and can regulate net deposition of collagens and other matrix proteins in the liver. The proliferation of HSCs is mainly stimulated by the platelet-derived growth factor (PDGF). In this study, some compounds from natural resources have been tested for their activity to inhibit PDGF-driven proliferative activity of rat HSCs. Apigenin, quercetin, genistein, daidzin, and biochanin A exhibited > 75% inhibitory activity against HSC-T6. It was found that, gamma-linolenic (gamma-Ln), eicosapentanoic (EPA) and a- linolenic (alpha-Ln) acids showed a high inhibitory effect on proliferation of rat HSCs at 50 nmol/1. Cholest-4-ene-3,6-dione and stigmastone-4-en-3,6-dione are the most active steroids with inhibitory activities > 80% and this is most likely due to the presence of the 4-en-3,6-dione moiety in both compounds. These results revealed that the compounds which effectively blocked HSC proliferation may be beneficial in liver fibrosis. Structure-activity relationships (SAR) may provide a basis for rational structure modification. 相似文献
10.
Salem ML Al-Khami AA El-Nagaar SA Zidan AA Al-Sharkawi IM Marcela Díaz-Montero C Cole DJ 《Cellular immunology》2012,276(1-2):67-74
Recently, we showed that post cyclophosphamide (CTX) microenvironment benefits the function of transferred T cells. Analysis of the kinetics of cellular recovery after CTX treatment showed that a single 4 mg/mouse CTX treatment decreased the absolute number of leukocytes in the peripheral blood (PBL) at days 3-15, and in the spleen and bone marrow (BM) at days 3-6. The absolute numbers of CD11c(+)CD11b(-) and CD11c(+)CD11b(+) dendritic cells (DCs), CD11b(+) and Ly6G(+) myeloid cells, T and B cells, CD4(+)CD25(+) T regulatory (T(reg)) cells, and NK1.1(+) cells also decreased. The cell numbers returned to control levels during the recovery phase. The absolute numbers of B cells remained low for 3 weeks. The numbers of DCs increased in PBL and spleen at day 9 but returned to control levels at day 15. These data indicate that CTX alters the cellular microenvironment in kinetics that might be precisely targeted to benefit the host. 相似文献