Total synthesis and biological evaluation of methylgerambullone.
First total synthesis of methylgerambullone (MGB, 1) isolated from Glycosmis angustifolia was completed via a convergent route. The effect of MGB on the contractile responses of the isolated guinea-pig ileum induced by acetylcholine was investigated. As a result, it showed a potent relaxation rate (78.66+/-4.30% at 100mg/L) in a concentration-dependent manner on longitudinal smooth muscle contraction of isolated guinea-pig ileum induced by 1microM acetylcholine.
Moon
Jong Taik
JT
Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea.
Ha
Sung Hoon
SH
Lee
So Hyung
SH
Kwon
Tae Hui
TH
Oh
Chun Rim
CR
Kim
Young Deuk
YD
Kim
Jungahn
J
Choo
Dong Joon
DJ
Lee
Jae Yeol
JY
D000109:Acetylcholine / Q000494:pharmacology; D000178:Acrylamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001688:Biological Products / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006168:Guinea Pigs; D007085:Ilium / Q000187:drug effects; D009126:Muscle Relaxation / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D027821:Rutaceae / Q000737:chemistry; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000178:Acrylamides; D001688:Biological Products; D013450:Sulfones; C549129:methylgerambullone; D000109:Acetylcholine