Screening for inhibitor of protein kinase from microbial and plant extracts

Kua, Shwu Fun (2007) Screening for inhibitor of protein kinase from microbial and plant extracts. Universiti Malaysia Sabah. (Unpublished)


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Microbial and plant extracts are productive sources of new bioactive metabolites for drug discovery. Screening for secondary metabolites is an established method to identify novel biologically active molecules. The screening system used in this study was yeast-based screening system. The glycogen synthase kinase-3 beta (GSK-3β) and mitogen-activated protein kinase kinase (MAPKK) were the molecular targets of this study since these kinases play a vital role in tumorigenesis, apoptosis, and cell proliferation. Mutant yeasts strain MKK p386 and H10075 were used as models for searching MAPKK and GSK-3β inhibitors. The acetone extract of actinomycete strain H7667 showed GSK-3p inhibitory activity but not against MAPKK inhibitory activity. The active acetone extract of H7667 was dried and subjected to liquid-liquid extraction with butanol and aqueous at ratio of 1:1. The obtained butanol extract of H7667 gave five significant peaks with retention time at 4.5 min, 18.4 min, 19.0 min, 21.4 min and 23.5 min respectively as analysed using RP-HPLC. The fractions of this extract showed negative results against the GSK-3β possibly due to small amount of bioactive compounds after fractionation. Five of the 27 plant extracts (crude, chloroform, methanol: aqueous and n-butanol extracts of Allium cepa, and aqueous extract of Tinospora crispa) had shown potent inhibitory activity against the MAPKK, whereas the Piper nigrum crude and chlorofoml extracts had shown to be potential inhibitors against GSK-3β. The n-butanol extract of Allium sativum showed toxicity against both MAPKK and GSK-3p. The Allium cepa, Tinospora crispa and Piper nigrum are potent anti-MAPKK and anti-GSK-3β agents which can be further developed as drugs for cancer and Alzheimer's diseases treatments.

Item Type: Academic Exercise
Keyword: drug, screening system, mitogen-activated protein kinase kinase, acetone extract, cancer and Alzheimer's diseases treatments, toxicity
Subjects: Q Science > QH Natural history > QH301-705.5 Biology (General)
Department: SCHOOL > School of Science and Technology
Date Deposited: 14 Feb 2014 12:16
Last Modified: 12 Oct 2017 08:02

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