Core structure in roselipins essential for eliciting inhibitory activity against diacylglycerol acyltransferase.
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.
Tomoda
Hiroshi
H
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
Tabata
Noriko
N
Ohyama
Yukako
Y
Omura
Satoshi
S
D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D051048:Diacylglycerol O-Acyltransferase; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D005227:Fatty Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005658:Fungi / Q000187:drug effects; D020462:Gliocladium / Q000737:chemistry*; D009005:Monosaccharides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D005227:Fatty Acids; D009005:Monosaccharides; C401212:roselipin 1A; C401213:roselipin 2A; C472762:roselipin 3A; C472763:roselipin 3B; D000217:Acyltransferases; D051048:Diacylglycerol O-Acyltransferase