Synthesis, Molecular Docking Studies And Biological Evaluation Of Some Unsaturated Carbonyl Derivatives / By Hager Ahmed Sayed; Supervisor Prof. Dr. Ismail Abdelshafy Abdelhamid, Dr .Nada Sabry Ibraheem Abd Elhady, Dr.Marwa Mohamed Mohamed Ahmed Sharaky.

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Hager Ahmed Sayed Ali [preparation.]

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TextLanguage: English Summary language: English, Arabic Producer: 2024Description: 80 pages : illustrations ; 25 cm. + CDContent type:

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التحضير ودراسات الالتحام الجزيئي والتقييم البيولوجي لبعض مشتقات الكربونيل غير المشبعة الجديدة [Added title page title]

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Dissertation note: Thesis (M.Sc.) -Cairo University, 2024. Summary: Eight Novel chalcones were synthesized and their structures were confirmed by different spectral tools. All the prepared compounds were subjected to SRB cytotoxic screening against several cancer cell lines. Compound 5c exerted the most promising effect against MCF7 and HEP2 cells with IC50 values of 9.5 and 12 µg/mL, respectively. Real-time PCR demonstrated the inhibitory effect of compound 5c on the expression level of Antigen kiel 67 (KI-67), Survivin, Interleukin-1beta (IL-1B), Interleukin-6 (IL-6), Cyclooxygenase-2 (COX-2) and Protein kinase B (AKT1) genes. Flow-cytometric analysis of the cell cycle indicated that compound 5c stopped the cell cycle at the G0/G1 phase in MCF7 treated cells. ELISA assay showed that Caspase 8, Caspase 9, P53, BAX, and Glutathione (GSH) were extremely activated and Matrix metalloproteinase 2 (MMP2), Matrix metalloproteinase 9 (MMP9), BCL2, Malondialdehyde (MDA), and IL-6 were deactivated in 5c treated MCF7 and HEP2 cells. Wound healing revealed that chalcone 5c reduced the ability to close the scrape wound and decreased the number of migrating MCF7 and HEP2 cells compared to the untreated cells after 48 h. Theoretical molecular modeling against P53 cancer mutant Y220C and Bcl2 showed binding energies of -22.8 and -24.2 Kcal/mole, respectively which confirmed our ELISA results. Summary: لقد تم تحضير ثمانية من مركبات الشالكون وتم التاكد منهم باستخدام الوسائل الطيفية المختلفه,لقد تم عمل الدراسات النظريه مثل التصميم الجزيئي لتحديد ميكانزم عمل هذه المركبات ,نتائج التاثير السمي علي الخلايا اوضحت ان المركب 5c له تاثير قوي علي الخلايا MCF7و HEP2 وقد تم اختيارهم لعمل الدراسات الجزيئيه ,لقد اوضح تحلبل البي سي ار الكمي ان المركب تسبب في نقص التعبير الجيني لجينات ki67 and survivin، IL-1B، IL-6، COX-2، AKT1 ,التحليل الفلوسيتموتري اوضح ان توقف دورة الخليه لخلايا سرطان الثدي قد تم عند مرحلة G0/G1 , وقد اوضحت نتائج تحليل الاليزا زيادة نشاطCaspase 8،Caspase 9 ، P53، BAX و GSH,وتقليل نشاط MMP2,MMP9,BCL2,MDA and IL-6 واظهر فحص التئام الجروح ان مركب 5C قلل من عدد خلايا الثدي والحنجره السرطانيه المهاجره الي مكان الجرح.

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Item type	Current library	Home library	Call number	Status	Barcode
Thesis	قاعة الرسائل الجامعية - الدور الاول	المكتبة المركزبة الجديدة - جامعة القاهرة	Cai01.12.02.M.Sc.2024.Ha.S. (Browse shelf(Opens below))	Not for loan	01010110091166000

Thesis (M.Sc.) -Cairo University, 2024.

Bibliography: pages 71-80.

Eight Novel chalcones were synthesized and their structures were confirmed by different spectral tools. All the prepared compounds were subjected to SRB cytotoxic screening against several cancer cell lines. Compound 5c exerted the most promising effect against MCF7 and HEP2 cells with IC50 values of 9.5 and 12 µg/mL, respectively. Real-time PCR demonstrated the inhibitory effect of compound 5c on the expression level of Antigen kiel 67 (KI-67), Survivin, Interleukin-1beta (IL-1B), Interleukin-6 (IL-6), Cyclooxygenase-2 (COX-2) and Protein kinase B (AKT1) genes. Flow-cytometric analysis of the cell cycle indicated that compound 5c stopped the cell cycle at the G0/G1 phase in MCF7 treated cells. ELISA assay showed that Caspase 8, Caspase 9, P53, BAX, and Glutathione (GSH) were extremely activated and Matrix metalloproteinase 2 (MMP2), Matrix metalloproteinase 9 (MMP9), BCL2, Malondialdehyde (MDA), and IL-6 were deactivated in 5c treated MCF7 and HEP2 cells. Wound healing revealed that chalcone 5c reduced the ability to close the scrape wound and decreased the number of migrating MCF7 and HEP2 cells compared to the untreated cells after 48 h. Theoretical molecular modeling against P53 cancer mutant Y220C and Bcl2 showed binding energies of -22.8 and -24.2 Kcal/mole, respectively which confirmed our ELISA results.

لقد تم تحضير ثمانية من مركبات الشالكون وتم التاكد منهم باستخدام الوسائل الطيفية المختلفه,لقد تم عمل الدراسات النظريه مثل التصميم الجزيئي لتحديد ميكانزم عمل هذه المركبات ,نتائج التاثير السمي علي الخلايا اوضحت ان المركب 5c له تاثير قوي علي الخلايا MCF7و HEP2 وقد تم اختيارهم لعمل الدراسات الجزيئيه ,لقد اوضح تحلبل البي سي ار الكمي ان المركب تسبب في نقص التعبير الجيني لجينات ki67 and survivin، IL-1B، IL-6، COX-2، AKT1 ,التحليل الفلوسيتموتري اوضح ان توقف دورة الخليه لخلايا سرطان الثدي قد تم عند مرحلة G0/G1 , وقد اوضحت نتائج تحليل الاليزا زيادة نشاطCaspase 8،Caspase 9 ، P53، BAX و GSH,وتقليل نشاط MMP2,MMP9,BCL2,MDA and IL-6 واظهر فحص التئام الجروح ان مركب 5C قلل من عدد خلايا الثدي والحنجره السرطانيه المهاجره الي مكان الجرح.

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جامعة القاهرة

المكتبة المركزية الجديدة

مكتبة جامعة القاهرة الأهلية

Synthesis, Molecular Docking Studies And Biological Evaluation Of Some Unsaturated Carbonyl Derivatives / By Hager Ahmed Sayed; Supervisor Prof. Dr. Ismail Abdelshafy Abdelhamid, Dr .Nada Sabry Ibraheem Abd Elhady, Dr.Marwa Mohamed Mohamed Ahmed Sharaky.