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41.
42.
Mohammed M. Alanazi Elwan Alaa Nawaf A. Alsaif Ahmad J. Obaidullah Hamad M. Alkahtani Abdulrahman A. Al-Mehizia Sultan M. Alsubaie Mohammed S. Taghour Ibrahim H. Eissa 《Journal of enzyme inhibition and medicinal chemistry》2021,36(1):1732
There is an urgent need to design new anticancer agents that can prevent cancer cell proliferation even with minimal side effects. Accordingly, two new series of 3-methylquinoxalin-2(1H)-one and 3-methylquinoxaline-2-thiol derivatives were designed to act as VEGFR-2 inhibitors. The designed derivatives were synthesised and evaluated in vitro as cytotoxic agents against two human cancer cell lines namely, HepG-2 and MCF-7. Also, the synthesised derivatives were assessed for their VEGFR-2inhibitory effect. The most promising member 11e were further investigated to reach a valuable insight about its apoptotic effect through cell cycle and apoptosis analyses. Moreover, deep investigations were carried out for compound 11e using western-plot analyses to detect its effect against some apoptotic and apoptotic parameters including caspase-9, caspase-3, BAX, and Bcl-2. Many in silico investigations including docking, ADMET, toxicity studies were performed to predict binding affinity, pharmacokinetic, drug likeness, and toxicity of the synthesised compounds. The results revealed that compounds 11e, 11g, 12e, 12g, and 12k exhibited promising cytotoxic activities (IC50 range is 2.1 − 9.8 µM), comparing to sorafenib (IC50 = 3.4 and 2.2 µM against MCF-7 and HepG2, respectively). Moreover, 11b, 11f, 11g, 12e, 12f, 12g, and 12k showed the highest VEGFR-2 inhibitory activities (IC50 range is 2.9 − 5.4 µM), comparing to sorafenib (IC50 = 3.07 nM). Additionally, compound 11e had good potential to arrest the HepG2 cell growth at G2/M phase and to induce apoptosis by 49.14% compared to the control cells (9.71%). As well, such compound showed a significant increase in the level of caspase-3 (2.34-fold), caspase-9 (2.34-fold), and BAX (3.14-fold), and a significant decrease in Bcl-2 level (3.13-fold). For in silico studies, the synthesised compounds showed binding mode similar to that of the reference compound (sorafenib). 相似文献
43.
K. Kamel M. Umar W. Ibrahim A. Mansour F. Gaballah O. Selim A. Azim S. Hamza F. Sabry N. Moafy A. El-Naggar K. Hoerman 《American journal of physical anthropology》1975,43(1):103-111
Anthropological studies were done on 1276 Libyans from the Mediterranean cities of Tripoli and Benghazi, and from Sabha southward in The Sahara. The incidences of hemoglobin (Hb)-S and glucose-6-phosphate dehydrogenase (G-6-PD) deficiency were low in the coastal areas and significantly high in Sabha. Hb-C occurred sporadically in Tripoli and Sabha, and was absent from Benghazi in the east. One case of Hb-J Benghazi was noted. There were no significant differences in the ABO blood group and Rh0 (D) type distributions in the three localities. G-6-PD gene GdA frequency was significantly high in Sabha. The lowest value of 6-phosphogluconate dehydrogenase (6-PGD) gene PGDA frequency and highest value of the gene PGDC were in Sabha. Adenylate kinase (AK) gene AK2 was only detectable in Tripoli. Acid phosphatase (AP) gene Pa frequency in Sabha was more than twice that in Tripoli and Benghazi, while Pc was distinctly lower in Sabha than in the northern cities. Haptoglobin gene Hp1 frequency was almost identical in all areas. Anthropometric measurements revealed overall homogeneity of the three samples, closer similarity in the coastal region to adjacent North African populations, and Negroid influence in the Saharan Libyans. Anthropometry substantiated findings from blood markers. 相似文献
44.
Hassan A. Hemeg Ihab M. Moussa Sherin Ibrahim Turki M. Dawoud Jwaher H. Alhaji Ayman S. Mubarak Saleh A. Kabli Roua A. Alsubki Azza M. Tawfik Sherif A. Marouf 《Saudi Journal of Biological Sciences》2020,27(12):3221-3227
This study evaluates the antimicrobial effects of ethanolic extract of five herbal plants; Guava (Psidium guajava), Sage (Salvia officinalis), Rhamnus (Ziziphusspina Christi), Mulberry (Morusalba L.), and Olive (Oleaeuropaea L) leaves against several microbial population representing Gram positive, Gram negative and Mollicutes; S. aureus, E. coli, Pasteurella multocida, B. cereus, Salmonella Enteritidis and M. gallisepticum using standard agar disc diffusion technique and minimal inhibitory concentration (MIC). Different extracts reveal variable results against the microorganism under study. All extracts have no antibacterial potency for Mycoplasma gallisepticum except Psidium guajava. The results of minimal inhibitory concentration (MIC) and Minimum bactericidal concentration (MBC) of the extracts against the six bacteria ranged from 625 to 5000 μg/ml. The used herbal extract could inhibit the selected microorganism under study with variable minimal inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). 相似文献
45.
Baioumy Asmaa Ali Swelim Hamdy Hamed Ibrahim Ahmed Adly Mohamed Fatma El‑Sayed Marzouk Aleya Soliman El‑Alfy Sherif Helmy 《Experimental & applied acarology》2022,86(4):609-610
Experimental and Applied Acarology - 相似文献
46.
Mohamed Elmarasi Ibrahim Elmakaty Basel Elsayed Abdelrahman Elsayed Jana Al Zein Ammar Boudaka Ali H. Eid 《Journal of cellular physiology》2024,239(4):e31200
Vascular smooth muscle cells (VSMCs) play a critical role in regulating vasotone, and their phenotypic plasticity is a key contributor to the pathogenesis of various vascular diseases. Two main VSMC phenotypes have been well described: contractile and synthetic. Contractile VSMCs are typically found in the tunica media of the vessel wall, and are responsible for regulating vascular tone and diameter. Synthetic VSMCs, on the other hand, are typically found in the tunica intima and adventitia, and are involved in vascular repair and remodeling. Switching between contractile and synthetic phenotypes occurs in response to various insults and stimuli, such as injury or inflammation, and this allows VSMCs to adapt to changing environmental cues and regulate vascular tone, growth, and repair. Furthermore, VSMCs can also switch to osteoblast-like and chondrocyte-like cell phenotypes, which may contribute to vascular calcification and other pathological processes like the formation of atherosclerotic plaques. This provides discusses the mechanisms that regulate VSMC phenotypic switching and its role in the development of vascular diseases. A better understanding of these processes is essential for the development of effective diagnostic and therapeutic strategies. 相似文献
47.
48.
Siva S. Panda Mohamed A. Ibrahim Said A. El‐Feky Alan R. Katritzky 《Journal of peptide science》2013,19(2):110-117
Nα‐Boc‐Nim‐(4‐toluenesulfonyl‐l ‐histidylbenzotriazole) enables convenient acylation of N‐, O‐, S‐, and C‐nucleophiles with no detectable racemization. We report efficient syntheses of novel histidine‐containing di‐, tri‐, and tetra‐peptides and models for the preparation of potentially biologically active histidine N‐, O‐, S‐, and C‐conjugates. Copyright © 2013 European Peptide Society and John Wiley & Sons, Ltd. 相似文献
49.
T J McMahon J S Hood B D Nossaman I N Ibrahim C J Feng P J Kadowitz 《Journal of applied physiology》1991,71(5):2012-2018
The effects of SQ 30741, a thromboxane A2 (TxA2) receptor blocking agent, on responses to the TxA2 mimic, U-46619, were investigated in the pulmonary vascular bed of the intact-chest cat under constant-flow conditions. The administration of SQ 30741 in doses of 1-2 mg/kg iv markedly reduced vasoconstrictor responses to U-46619 without altering responses to prostaglandin (PG) F2 alpha or PGD2 and serotonin. SQ 30741 had no significant effect on mean vascular pressures in the cat, and the dose-response curve for U-46619 was shifted to the right in a parallel manner with a similar apparent maximal response. In addition to not altering responses to PGF2 alpha, PGD2 alpha, or serotonin, SQ 30741 (2 mg/kg iv) was without significant effect on pulmonary vasoconstrictor responses to the PGD2 metabolite 9 alpha, 11 beta-PGF2, norepinephrine, angiotensin II, BAY K 8644, endothelin 1, or endothelin 2. Although responses to vasoconstrictor agents, which act through a variety of mechanisms, were not altered, responses to the PG and TxA2 precursor, arachidonic acid, were reduced significantly. The duration of the TxA2 receptor blockade was approximately 30 and 75 min at the 1- and 2-mg/kg iv doses of the antagonist, respectively. The present data show that SQ 30741 selectively blocks TxA2 receptor-mediated responses in a competitive and reversible manner in the pulmonary vascular bed. These data suggest that responses to arachidonic acid are due in large part to the formation of TxA2 and that discrete TxA2 receptors unrelated to receptors activated by PGD2 or PGF2 alpha are most likely located in resistance vessel elements in the feline pulmonary vascular bed. 相似文献
50.