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Ayman A. Ghfar Mohammad Magdy El-Metwally Mohamed Shaaban Sami A. Gabr Nada S. Gabr Marwa S. M. Diab Ahmad Aqel Mohamed A. Habila Wahidah H. Al-Qahtani Mohammad Y. Alfaifi Serag Eldin I. Elbehairi Bayan Ahmed AlJumah 《Molecules (Basel, Switzerland)》2021,26(9)
The anticancer activity of terretonin N (1) and butyrolactone I (2), obtained from the thermophilic fungus Aspergillus terreus TM8, was intensively studied against prostate adenocarcinoma (PC-3) and ovary adenocarcinoma (SKOV3) human cell lines. According to this study, both compounds showed potent cytotoxicity towards ovarian adenocarcinoma cells (SKOV3) with IC50 1.2 and 0.6 μg/mL, respectively. With respect to metastatic prostate cells (PC-3), the two compounds 1 and 2 showed a significantly promising cytotoxicity effect with IC50 of 7.4 and 4.5 μg/mL, respectively. The tested fungal metabolites showed higher rates of early and late apoptosis with little or no necrotic apoptotic pathway in all treated prostate adenocarcinoma (PC-3) and ovary adenocarcinoma (SKOV3) human cell lines, respectively. The results reported in this study confirmed the promising biological properties of terretonin N (1) and butyrolactone I (2) as anticancer agents via the induction of cellular apoptosis. However, further studies are needed to elucidate the molecular mechanism by which cellular apoptosis is induced in cancer cells. 相似文献
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Mohamed A.A. Radwan Osamah Al Rugaie Waleed Al Abdulmonem Mohammad Y. Alfaifi Serag Eldin I. Elbehairi 《Arabian Journal of Chemistry》2021,14(7):103209
The current approach described the synthesis of a new series of indolylpyrrole derivatives through multicomponent reaction of α-cyano chalcones, appropriate aldehydes, and ammonium acetate in refluxed acetic acid. The chemical structures of the designed compounds were confirmed with spectroscopic data and elemental analysis and then tested for their in vitro cytotoxic activity by SRB assay method towards three cell lines involving human Prostate adenocarcinoma; metastatic cells (PC-3), human ovary adenocarcinoma (SKOV3) and human dukes' type B, colorectal adenocarcinoma (LS 174 T). Most significant activity provided with compounds 5c, 5h and, 5j against prostate cancer cells (PC-3) with IC50s of 3.30 ± 0.20, 3.60 ± 0.10, and 3.60 ± 0.90 µg/ml, respectively. In human ovarian carcinoma (SKOV3), the compounds 5a, and 5i have stronger cytotoxicity with IC50s of 1.20 ± 0.04, 1.90 ± 0.50 µg/ml, respectively than the standard doxorubicin (IC50 = 2.20 ± 0.02 µg/ml). On the other hand, only compound 5a has the ability to diminish the viability of LS174T cells in an active manner with IC50 2.80 ± 0.10 µg/ml. Consequently, this effort offers groundwork for additional examination of nominated indolylpyrroles as antiproliferative agents. 相似文献
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Mostafa I. Abdelglil Sanaa O. Abdallah Mohamed A. El-Desouky Mohammad Y. Alfaifi Serag Eldin I. Elbehairi Aly F. Mohamed 《Molecules (Basel, Switzerland)》2021,26(22)
We aimed to evaluate the anticancer potential of crude venom (CV), γ irradiated Certastes cerastes venom (IRRV), and propolis ethanolic extract (PEE). IRRV showed a higher toxicity than CV, while CV-PEE showed higher toxicity than IRRV and CV against lung [A549] and prostate [PC3] cancer cells. Toxicity to [A549] and [PC3] cells was concentration and cell type dependent. In comparison to controls, apoptotic genes showed a significant upregulation of P53 and Casp-3 and a downregulation of Bcl-2. Also, induced elevated DNA accumulation in the [S] phase post PC3 cell treatment with IRRV and CV, as well as a significant DNA accumulation at G2/M phase after IRRV treatment of A549 cells. In contrast, PC3 cells showed a negligible cellular DNA accumulation after PEE treatment. Glutathione reductase [GR] was reduced in case of PC3 and A549 cell treated with IRRV, CV, and PEE compared with its values in untreated cell control. The Malondialdehyde [MDA] values in both cells recorded a significant elevation post IRRV treatment compared to the rest of the treatment regimen and untreated cell control. Similarly, IRRV and CV-PEE mix showed obviously higher reactive oxygen species [ROS] values than PC3 and A549 cell treatments with CV and PEE. 相似文献
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Mohamed-Elamir F. Hegazy Alaa Y. Moustfa Abou El-Hamd H. Mohamed Montaser A. Alhammady Serag Eldin I. Elbehairi Shinji Ohta Paul W. Paré 《Tetrahedron letters》2014
Two new sesquiterpenes, oculiferane (1) and epi-obtusane (2) have been isolated and identified from an acetone extract of the digestive gland of the sea hare, Aplysia oculifera. The structures were elucidated by spectroscopic analysis including HREIMS, 1H, 13C, DEPT, 1H–1H COSY, HMQC, and HMBC NMR; the relative configuration was confirmed by X-ray analysis. Compounds 1 and 2 exhibited cytotoxic activity in vitro against several human cancer cell lines with IC50 values in the low μg/ml range. 相似文献
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Abdulrahman Alsayari Abdullatif Bin Muhsinah Yahya I. Asiri Mohammad Y. Alfaifi Serag Eldin I. Elbehairi Fatima Alatibi Nahed Nasser E. El-Sayed Yahia N. Mabkhot 《Journal of heterocyclic chemistry》2020,57(7):2911-2922
5-(2-Bromoacetyl)-2,3,4-trisubstituted-thiophene was used as a synthetic intermediate to prepare a series of thiophene derivatives and thiophene incorporating oxazole, imidazole, thiazole, pyrrole, and pyridine rings via substitution and cyclo-condensation reactions. The data were extracted from the spectra of the resulting products confirmed their suggested structures. The newly synthesized compounds were screened to evaluate their in vitro antimicrobial activity vs several positive and negative gram bacteria and fungi. The screening data revealed that the thiophene derivative 7a , incorporating a thiazole ring, displayed strong activity against all tested microorganisms when compared with the antibiotics used. 相似文献
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Yasser S. Mostafa Saad A. Alamri Mohammad Y. Alfaifi Sulaiman A. Alrumman Serag Eldin I. Elbehairi Tarek H. Taha Mohamed Hashem 《Molecules (Basel, Switzerland)》2021,26(7)
L-glutaminase is an important anticancer agent that is used extensively worldwide by depriving cancer cells of L-glutamine. The marine bacterium, Halomonas meridian was isolated from the Red Sea and selected as the more active L-glutaminase-producing bacteria. L-glutaminase fermentation was optimized at 36 h, pH 8.0, 37 °C, and 3.0% NaCl, using glucose at 1.5% and soybean meal at 2%. The purified enzyme showed a specific activity of 36.08 U/mg, and the molecular weight was found to be 57 kDa by the SDS-PAGE analysis. The enzyme was highly active at pH 8.0 and 37 °C. The kinetics’ parameters of Km and Vmax were 12.2 × 10−6 M and 121.95 μmol/mL/min, respectively, which reflects a higher affinity for its substrate. The anticancer efficiency of the enzyme showed significant toxic activity toward colorectal adenocarcinoma cells; LS 174 T (IC50 7.0 μg/mL) and HCT 116 (IC50 13.2 μg/mL). A higher incidence of cell death was observed with early apoptosis in HCT 116 than in LS 174 T, whereas late apoptosis was observed in LS 174 T more than in HCT 116. Also, the L-glutaminase induction nuclear fragmentation in HCT 116 was more than that in the LS 174T cells. This is the first report on Halomonas meridiana as an L-glutaminase producer that is used as an anti-colorectal cancer agent. 相似文献
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Khadijah A. Jabal Hossam M. Abdallah Gamal A. Mohamed Ibrahim A. Shehata Mohammad Y. Alfaifi Serag Eldin I. Elbehairi 《Natural product research》2020,34(15):2167-2172
AbstractThe CHCl3 fraction of MeOH extract of Periploca somaliensis (family Asclepiadaceae) fruits afforded a new scalarane sesterterpene, namely perisomalien A (1), along with lupeol acetate (2), β-amyrin (3), cycloart-23Z-ene-3β,25-diol (4), and β-sitosterol-3-O-β-D-glucopyranoside (5). Their chemical structures were established by various spectroscopic analyses, in addition to comparison with the formerly reported data. Moreover, the cytotoxic activity of these metabolites was assessed towards MCF-7, HepG2, and HCT-116 tumour cell lines using sulforhodamine B (SRB) assay. Compound 4 showed the most potent cytotoxic profile with IC50 9.0?µM towards MCF-7, compared to doxorubicin (IC50 0.18?µM). Also, 1 and 4 possessed the most potent effect towards HepG2 with IC50s 26.7 and 25.9?μM, respectively. In addition, all tested compounds showed cytotoxic effects with IC50 values ranging from 19.9 to 39.3?µM against HCT-116. 相似文献
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