Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase

Rie Tanaka; Yuichi Sakano; Akito Nagatsu; Masaaki Shibuya; Yutaka Ebizuka; Yukihiro Goda

doi:10.1016/j.bmcl.2004.10.013

Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase

Bioorg Med Chem Lett. 2005 Jan 3;15(1):159-62. doi: 10.1016/j.bmcl.2004.10.013.

Authors

Rie Tanaka¹, Yuichi Sakano, Akito Nagatsu, Masaaki Shibuya, Yutaka Ebizuka, Yukihiro Goda

Affiliation

¹ National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-Ku, Tokyo 158-8501, Japan.

PMID: 15582431
DOI: 10.1016/j.bmcl.2004.10.013

Abstract

Digalactosyl and monogalactocyl diacylglycerols (DGDG and MGDG), which were identified as anti-hyperlipemia active components in Colocasia esculenta (Taro), were synthesized. The inhibitory activity of DGDG, MGDG and related compounds on human lanosterol synthase was evaluated as anti-hyperlipemic activity. DGDG with two myristoyl groups at both sn-1 and sn-2 positions and with an oleoyl group at the sn-1 position showed the most potent activity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Carbohydrate Sequence
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Galactolipids / chemical synthesis*
Galactolipids / chemistry
Galactolipids / pharmacology*
Humans
Intramolecular Transferases / antagonists & inhibitors*
Molecular Sequence Data
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Galactolipids
digalactosyldiacylglycerol
Intramolecular Transferases
lanosterol synthase