Verticilide, a new ryanodine-binding inhibitor, produced by Verticillium sp. FKI-1033.
A new ryanodine-binding inhibitor, verticilide, was isolated from the cultured broth of a fungus, Verticillium sp. FKI-1033. It is a 24-membered ring cyclic depsipeptide, its structure being elucidated as cyclo[(2R)-2-hydroxyheptanoyl-N-methyl- L-alanyl](4). Verticilide inhibited ryanodine binding to ryanodine receptors in the cockroach at an IC(50) value of 4.2 microM, whereas inhibition against mouse ryanodine receptors was weak (IC(50)=53.9 microM).
Shiomi
Kazuro
K
Kitasato Institute for Life Sciences, Graduate School of Infection Control Sciences, Kitasato University, Tokyo, Japan. shiomi@lisci.kitasato-u.ac.jp
Matsui
Ryosuke
R
Kakei
Atsuo
A
Yamaguchi
Yuichi
Y
Masuma
Rokuro
R
Hatano
Hiroko
H
Arai
Noriko
N
Isozaki
Miki
M
Tanaka
Haruo
H
Kobayashi
Susumu
S
Turberg
Andreas
A
Omura
Satoshi
S
D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D003058:Cockroaches; D047630:Depsipeptides / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D051379:Mice; D008967:Molecular Biology; D018485:Muscle Fibers, Skeletal / Q000378:metabolism; D011485:Protein Binding; D012433:Ryanodine / Q000037:antagonists & inhibitors*; D019837:Ryanodine Receptor Calcium Release Channel / Q000378:metabolism*; D013329:Structure-Activity Relationship; D020172:Verticillium / Q000378:metabolism*
D047630:Depsipeptides; D019837:Ryanodine Receptor Calcium Release Channel; C522755:verticilide; D012433:Ryanodine