Search In this Thesis
   Search In this Thesis  
العنوان
Discovery of natural rho-kinase inhibitors /
المؤلف
El-Diasty, Yhiya Yhiya Mohamed Amen.
هيئة الاعداد
باحث / يحيي يحيي محمد أمين الدياسطى
مشرف / محمد صفوت عطا عفيفى
مشرف / أحمد فؤاد أحمد حليم
مشرف / كونيوشى شيميزو
مشرف / أحمد عادل عاشور محمد
الموضوع
Protein Kinase Inhibitors. Enzyme Inhibitors. Enzyme inhibitors - Therapeutic use. Enzyme inhibitors - pharmacology.
تاريخ النشر
2017.
عدد الصفحات
401 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
الصيدلة ، علم السموم والصيدلانيات
تاريخ الإجازة
01/05/2017
مكان الإجازة
جامعة المنصورة - كلية الصيدلة - Pharmacognosy
الفهرس
Only 14 pages are availabe for public view

from 401

from 401

Abstract

The study includes 4 parts as follows: Part I : Chemical investigation of Ganoderma lingzhi mushrooms. This part resulted in isolation of 23 compounds, three of them are new natural products. Part II : Chemical investigation of Coix lacryma-jobi L. seeds. This part resulted in isolation of 10 compounds, one of them is new natural product. Part III : Chemical investigation of Kochia indica Wight. This part resulted in isolation of 11 compounds. All of these compounds are reported for the first time from this species. Part IV : Biological activities : 1.Rho-Kinase inhibitory activity and docking study : The activity of the total ethanol extract of Ganoderma lingzhi at a concentration of 1 mg/mL was tested against the two enzymes (ROCK-1 and ROCK-II). The inhibition percentages against ROCK-I and ROCK-II were 62.7 ± 3.6 (IC50 933.4 ± 9.8 μg/mL) and 60.2 ± 3.3 (IC50 966.1 ± 8.4 μg/mL), respectively. The activity of the total ethanol extract of Coix lachryma-jobi L. seeds at a concentration of 1 mg/mL was tested against the two enzymes (ROCK-1 and ROCK-II). The inhibition percentages against ROCK-I and ROCK-II were 55.2 ± 2.6 (IC50 1001.53 ± 4.7 μg/mL) and 53.37 ± 4.1 (IC50 1000.91 ± 5.3 μg/mL), respectively. The inhibition percentages of the total methanol extract of Kochia indica at a concentration of 1 mg/mL, against ROCK-I and ROCK-II were found to be 40.7 ± 1.7 (IC50 1021.6 ± 7.6 μg/mL) and 38.4 ± 3.9 (IC50 1022.8 ± 6.9 μg/mL) respectively. 2.Cytotoxic activities of some of the isolated compounds against several cancer and normal cell lines: Careful investigation of the activity of the cytotoxicity of the compounds and their Rho-kinase inhibitory activity, one can notice that lucidumol C showed a potent cytotoxic activity against several cancer cell lines in the same time, it showed a Rho-kinase inhibitory activity. Thus, Lucidumol C may exert its cytotoxic activity through inhibition of Rho-kinase pathway.