Core structure in roselipins essential for eliciting inhibitory activity against diacylglycerol acyltransferase

Hiroshi Tomoda; Noriko Tabata; Yukako Ohyama; Satoshi Omura

doi:10.7164/antibiotics.56.24

Core structure in roselipins essential for eliciting inhibitory activity against diacylglycerol acyltransferase

J Antibiot (Tokyo). 2003 Jan;56(1):24-9. doi: 10.7164/antibiotics.56.24.

Authors

Hiroshi Tomoda¹, Noriko Tabata, Yukako Ohyama, Satoshi Omura

Affiliation

¹ Kitasato Institute for Life Sciences & Graduate School of Infection Control Sciences, Kitasato University, Shirokane, Minato-ku, Tokyo 108-8641, Japan. tomoda@lisci.kitasato-u.ac.jp

PMID: 12670046
DOI: 10.7164/antibiotics.56.24

Abstract

Fungal roselipins, discovered as inhibitors of diacylglycerol acyltransferase (DGAT), consist of three parts; highly methylated C20 fatty acid, mannose and arabinitol. Demannosyl and/or dearabinitoyl roselipins were prepared chemically or enzymatically. Demannnosyl roselipins conserved the DGAT inhibitory activity, but the others lost the activity, indicating that the arabinitoyl fatty acid core is essential for eliciting the activity.

MeSH terms

Acyltransferases / antagonists & inhibitors*
Anti-Bacterial Agents
Anti-Infective Agents / chemistry
Anti-Infective Agents / pharmacology
Bacteria / drug effects
Diacylglycerol O-Acyltransferase
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Fatty Acids / chemical synthesis
Fatty Acids / chemistry
Fatty Acids / pharmacology*
Fungi / drug effects
Gliocladium / chemistry*
Monosaccharides / chemical synthesis
Monosaccharides / chemistry
Monosaccharides / pharmacology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Anti-Infective Agents
Enzyme Inhibitors
Fatty Acids
Monosaccharides
roselipin 1A
roselipin 2A
roselipin 3A
roselipin 3B
Acyltransferases
Diacylglycerol O-Acyltransferase