Inhibition of protein tyrosine phosphatase 1B by diterpenoids isolated from Acanthopanax koreanum

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Title
Inhibition of protein tyrosine phosphatase 1B by diterpenoids isolated from Acanthopanax koreanum
Author(s)
Min Kyun Na; Won Keun Oh; Y H Kim; X F Cai; S H Kim; Bo Yeon KimJong Seog Ahn
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 11, pp. 3061-3064
Publication Year
2006
Abstract
Inhibition of protein tyrosine phosphatase 1B (PTP1B) has been proposed as a therapy to treat type 2 diabetes and obesity. In our preliminary screening study on the PTP1B inhibitory activity, a CH2Cl2-soluble extract of the roots of Acanthopanax koreanum (Araliaceae) was found to inhibit PTP1B activity at 30 μg/ml. Eight diterpenoids were isolated from the active fraction and were evaluated for their inhibitory effect on PTP1B. A kaurane-type diterpene, 16αH,17-isovaleryloxy-ent-kauran-19-oic acid (7), inhibited PTP1B with an IC50 value of 7.1 ± 0.9 μM in a non-competitive manner. Acanthoic acid (2) and ent-kaur-16-en-19-oic acid (5) also inhibited PTP1B in dose-dependent manners. Either introduction of a hydroxyl group or reduction of a carboxyl group at C-19 in pimarane-type to alcohol abolished the inhibitory effects toward PTP1B.
Keyword
Acanthopanax koreanumAraliaceaeDiterpenoidsNon-competitive inhibitorProtein tyrosine phosphatase 1B (PTP1B)
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2006.02.053
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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