Anti-inflammatory, anti-bacterial and anti-acetylcholinesterase activities of two isoquinoline alkaloids–Scoulerine and Cceilanthifoline

Wangchuk, Phurpa, Sastraruji, Thanapat, Taweechotipatr, Malai, Keller, Paul A., and Pyne, Stephen G. (2016) Anti-inflammatory, anti-bacterial and anti-acetylcholinesterase activities of two isoquinoline alkaloids–Scoulerine and Cceilanthifoline. Natural Product Communications, 11 (12). pp. 1801-1804.

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Abstract

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-α) and a bacterial strain, Helicobacter pylori. Both alkaloids showed weak anti TNF-α 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.

Item ID: 45269
Item Type: Article (Research - C1)
ISSN: 1555-9475
Keywords: acetylcholinesterase inhibitor, isoquinoline alkaloid, anti-inflammatory, antimicrobial, medicinal plant, Corydalis dubia
Funders: Endeavour Award, National Health and Medical Research Council of Australia (NHMRC)
Date Deposited: 30 Aug 2016 01:37
FoR Codes: 03 CHEMICAL SCIENCES > 0304 Medicinal and Biomolecular Chemistry > 030401 Biologically Active Molecules @ 34%
03 CHEMICAL SCIENCES > 0305 Organic Chemistry > 030502 Natural Products Chemistry @ 33%
03 CHEMICAL SCIENCES > 0301 Analytical Chemistry > 030108 Separation Science @ 33%
SEO Codes: 92 HEALTH > 9204 Public Health (excl. Specific Population Health) > 920412 Preventive Medicine @ 100%
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