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ا.م.د/ ياسين الشاعر في الحلقات النقاشية بكلية الصيدلة

04-04-2019

تواصل كلية الصيدلة الحلقات النقاشية تحت رعاية الاستاذ الدكتور/ خالد ابو زيد محمد – عميد كلية الصيدلة وا.م.د/ ايناس علي ابراهيم – وكيل الكلية لشئون خدمة المجتمع و تنمية البيئة ، يوم الاثنبن الموافق 2019-4-8 و سوف يقدم ا.م.د. ياسين الشاعر في تمام الساعة التاسعة والنصف في قاعة السيمنار بالمبني الجديد اخر ابحاثه  تحت عنوان:

Hybrid Drug Candidates of Nitric Oxide Releasing Cucurbitacins-  Inspired  Estrone Analogs for the Treatment of Hepatocellular Carcinoma .


كما يختص البحث بالوصف التالي:

Development of hybrid drug candidates is well known strategy for designing antitumor agents. Herein, a novel class of nitric oxide donating cucurbitacin inspired estrone analogs (NO-CIEAs) were designed and synthesized as multi-target agents. Synthesized analogs were initially evaluated for their antihepatocellular carcinoma activities. Among the tested analogs, NO-CIEAs 17 and 20a exhibited more potent activity against HepG2 cells (IC50 = 4.69 and 12.5 µM, respectively) than the reference drug erlotinib (IC50 = 25 µM). Interestingly, NO-CIEA 17 exerted also a high potent activity against erlotinib-resistant HepG2 cell line (HepG2-R) (IC50 = 8.21 µM) giving insight about its important in drug resistance therapy. Intracellular measurements of NO revealed that NO-CIEAs 17 and 20a showed a significant increase in NO production in tumor cells after 1h of incubation comparable to the reference standard JS-K. Both NO-CIEAs 17 and 20a mainly arrested the HepG2 cells in the G0/G1 phase and exhibited a potential inhibitory activity towards the EGFR and MAPK (25% and 29% inhibition respectively). This data suggests the binding ability of NO-CIEA 17 to the EGFR and ERK to be well correlated along with the docking and cellular studies. Also, treatment of HepG2-R cells with NO-CIEA 17 showed a potential reduction of MRP2 expression in a dose dependent manner providing a significant impact on the chemotherapeutic resistance.
 

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