Substrate-like water soluble lipase inhibitors from Filipendula kamtschatica

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:22

Article

Kato, Eisuke¹  Yama, Michitsugu¹  Nakagomi, Ryo¹  Shibata, Toshiro²  Hosokawa, Keizo³  Kawabata, Jun¹ 

[1] Hokkaido Univ, Grad Sch Agr, Div Appl Biosci, Lab Food Biochem,Kita Ku, Sapporo, Hokkaido 0608589, Japan

[2] Natl Inst Biomed Innovat, Res Ctr Med Plant Resources, Hokkaido Div, Nayoro, Hokkaido 0960065, Japan

[3] Univ Hyogo, Fac Hlth Sci, Dept Nutr Management, Kakogawa, Hyogo 6750195, Japan

关键词: Filipendula kamtschatica;    Pancreatic lipase inhibitor;    Obesity;    Traditional medicine;   

DOI  :  10.1016/j.bmcl.2012.08.055

来源: Elsevier

【 摘 要 】

Filipendula kamtschatica is a plant utilized as a traditional medicine by Ainu people in Japan, but its chemical constituents are not much studied. Pancreatic lipase inhibitors are a promising tool for the treatment of obesity. We searched for natural lipase inhibitors from F. kamtschatica and two new compounds were isolated along with the known flavonoid glycoside. The structure elucidation of new compounds revealed these two to be 2-O-caffeoyl-4-O-galloyl-L-threonic acid and 3-O-caffeoyl-4-O-galloyl-L-threonic acid, which can be recognized as a pancreatic lipase's substrate-like structure. The isolated compounds all showed an inhibitory activity against porcine pancreatic lipase and one of the isomer, 3-O-caffeoyl-4-O-galloyl-L-threonic acid, possessed the most potent activity with IC50 value showing an order lower value compared to others. The substrate-like structure of the new compounds seemed to be important for their activity. (c) 2012 Elsevier Ltd. All rights reserved.

【 授权许可】

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