Inhibition of Human Lanosterol Synthase by the Constituents of Colocasia esculenta (Taro)

Inhibition of Human Lanosterol Synthase by the Constituents of Colocasia esculenta (Taro)
February 2005
Yuichi Sakano1), Motoh Mutsuga2), Rie Tanaka2), Hiroyuki Suganuma3), Takahiro Inakuma3), Masatake Toyoda2), Yukihiro Goda2), Masaaki Shibuya1) and Yutaka Ebizuka1)
1) Graduate School of Pharmaceutical Sciences, The University of Tokyo
2) National Institute of Health Sciences, Japan
3) Research Institute, Kagome Company Ltd.
Biological & Pharmaceutical Bulletin Vol. 28 (2005) , No. 2 299
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Abstract
Ethanol extracts of lyophilized vegetables were tested for inhibition of human lanosterol synthase (hOSC) in order to find the compounds to suppress cholesterol biosynthesis. Of 130 samples tested, twelve samples showed significant inhibition. Among them, Colocasia esculenta (taro) showed the highest inhibition (55% inhibition at 300 ?g/ml). Examination of activity variation among eight taro cultivars indicated that ?Aichi-wase? and ?Yatsugashira? had the most potent activity for hOSC inhibition. In order to identify the active constituent of taro, ethanol extracts of ?Aichi-wase? were partitioned with hexane and aqueous methanol, and fractionated by silica gel column chromatography. Inhibitory activity was concentrated in two major active fractions. Further purification of these fractions by preparative HPLC gave three monogalactosyldiacylglycerols and five digalactosyldiacylglycerols as active compounds that showed 28 to 67% inhibitory activities at the concentration 300 ?g/ml.
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