Anti-inflammatory, Anti-bacterial and Anti-acetylcholinesterase Activities of two Isoquinoline Alkaloids Scoulerine and Cheilanthifoline

被引:0
作者
Wangchuk, Phurpa [1 ,2 ]
Sastraruji, Thanapat [3 ]
Taweechotipatr, Malai [4 ]
Keller, Paul A. [2 ]
Pyne, Stephen G. [2 ]
机构
[1] James Cook Univ, Australian Inst Trop Hlth & Med, Ctr Biodiscovery & Mol Dev Therapeut, Cairns, Qld, Australia
[2] Univ Wollongong, Sch Chem, Wollongong, NSW 2522, Australia
[3] Chiang Mai Univ, Fac Dent, Dept Oral Biol & Diagnost Sci, Ctr Excellence Oral & Maxillofacial Biol, Chiang Mai, Thailand
[4] Srinakharinwirot Univ, Fac Med, Dept Microbiol, Sukhumvit 23, Bangkok 10110, Thailand
基金
澳大利亚国家健康与医学研究理事会;
关键词
Acetylcholinesterase inhibitor; Isoquinoline alkaloid; Anti-inflammatory; Antimicrobial; Medicinal plant; Corydalis dubia; BUTYRYLCHOLINESTERASE INHIBITORY COMPOUNDS; BHUTANESE MEDICINAL-PLANTS; ANTIMICROBIAL ACTIVITY; NATURAL-PRODUCTS; DRUG DISCOVERY; ACETYLCHOLINESTERASE; CORYDALIS; EXTRACTS; PROTOPINE; PAPAVERACEAE;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Corydalis plants containing isoquinoline alkaloids are reported to possess promising pharmacological properties for the treatment of important diseases including cancer, inflammation, Alzheimer's disease and microbial infections. As part of a wider program investigating Bhutanese medicinal plants, we have previously identified eight isoquinoline alkaloids from C. dubia. Out of these, we report here on two of the major alkaloids, scoulerine (1) and cheilanthifoline (2) and their inhibitory activities against acetylcholinesterase (anti-AChE), tumor necrosis factor alpha (anti TNF-alpha) and a bacterial strain, Helicobacter pylori. Both alkaloids showed weak anti TNF-alpha and antibacterial activities. However, the anti-AChE activity of scoulerine (1) was promising as it significantly inhibited AChE with a minimum inhibitory requirement (MIR) value of 0.0015 nmol, which was two-fold better than the reference drug, galanthamine (MIR value of 0.003 nmol). As there are limited anti-Alzheimer's chemotherapeutics, scoulerine (1) is worthy of further exploration, including lead optimization, structure-activity-relationship studies, analog development, pharmacodynamics and in vivo animal studies.
引用
收藏
页码:1801 / 1804
页数:4
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