The mode of inhibitory action of alpha-mangostin, a novel inhibitor, on the sarcoplasmic reticulum Ca2+-pumping ATPase from rabbit skeletal muscle

被引：13
|
作者：
Furukawa, K [1 ]
Shibusawa, K [1 ]
Chairungsrilerd, N [1 ]
Ohta, T [1 ]
Nozoe, S [1 ]
Ohizumi, Y [1 ]
机构：
[1] TOHOKU UNIV,FAC PHARMACEUT SCI,DEPT PHARMACOGNOSY,AOBA KU,SENDAI,MIYAGI 980,JAPAN
来源：
JAPANESE JOURNAL OF PHARMACOLOGY | 1996年 / 71卷 / 04期
关键词：
alpha-mangostin; Ca2+-pumping ATPase; sarcoplasmic reticulum;
D O I：
10.1254/jjp.71.337
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
alpha-Mangostin, the principal ingredient of the fruit hull of Garcinia mangostana, caused a concentration-dependent decrease in the activities of both Ca2+-ATPase and Ca2+-transport of the sarcoplasmic reticulum from rabbit skeletal muscle with an IC50 value of 5 mu M. Neither Ca2+ release nor other enzyme activities were affected by alpha-mangostin. Kinetic analysis of the inhibitory effects of alpha-mangostin on Ca2+-ATPase suggests that the inhibition of the ATPase is a noncompetitive-type with respect to ATP or Ca2+. alpha-Mangostin may become a useful pharmacological tool for clarifying the physiological functions of Ca2+-pumping ATPase and sarcoplasmic reticulum.
引用
收藏
页码：337 / 340
页数：4
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