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Title of Journal: Arch Pharm Res

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Abbravation: Archives of Pharmacal Research

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Pharmaceutical Society of Korea

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DOI

10.1002/chin.198701059

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1976-3786

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Inhibitory activities of the alkaloids from Coptid

Authors: Hyun Ah Jung Na Young Yoon Hyun Ju Bae ByungSun Min Jae Sue Choi
Publish Date: 2008/11/21
Volume: 31, Issue: 11, Pages: 1405-1412
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Abstract

As part of our ongoing search of natural sources for therapeutic and preventive agents for diabetic complications the rat lens aldose reductase RLAR inhibitory effect of Coptidis Rhizoma the rhizome of Coptis chinensis Franch was evaluated Its extract and fractions exhibited broad and moderate RLAR inhibitory activities of 389∼675 μg/mL In an attempt to identify bioactive components six quaternary protoberberinetype alkaloids berberine palmatine jateorrhizine epiberberine coptisine and groenlandicine and one quaternary aporphinetype alkaloid magnoflorine were isolated from the most active nBuOH fraction and the chemical structures therein were elucidated on the basis of spectroscopic evidence and comparison with published data The antidiabetic complications capacities of seven C chinensisderived alkaloids were evaluated via RLAR and human recombinant AR HRAR inhibitory assays Although berberine and palmatine were previously reported as prime contributors to AR inhibition these two major components exhibited no AR inhibitory effects at a higher concentration of 50 μg/ml in the present study Conversely epiberberine coptisine and groenlandicine exhibited moderate inhibitory effects with IC50 values of 1001 1184 1401 μM for RLAR and 1681 1873 1542 μM for HRAR The results clearly indicated that the presence of the dioxymethylene group in the D ring and the oxidized form of the dioxymethylene group in the A ring were partly responsible for the AR inhibitory activities of protoberberinetype alkaloids Therefore Coptidis Rhizoma and the alkaloids contained therein would clearly have beneficial uses in the development of therapeutic and preventive agents for diabetic complications and diabetes mellitus

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