Inhibition of acidic sphingomyelinase by xanthone compounds isolated from Garcinia speciosa

被引：42

作者：

Okudaira, C

Ikeda, Y

Kondo, S

Furuya, S

Hirabayashi, Y

Koyano, T

Saito, Y

Umezawa, K

机构：

[1] Keio Univ, Fac Sci & Technol, Dept Appl Chem, Kohoku Ku, Yokohama, Kanagawa 2230061, Japan

[2] Inst Microbial Chem, Shinagawa Ku, Tokyo 1410021, Japan

[3] RIKEN, Inst Phys & Chem Res, Frontier Res Program, Wako, Saitama 3510106, Japan

[4] Temko Corp, Nakano Ku, Tokyo 1640012, Japan

来源：

JOURNAL OF ENZYME INHIBITION | 2000年 / 15卷 / 02期

关键词：

sphingomyelinase; Garcinia speciosa; alpha-mangostin; cowanin; cowanol;

D O I：

10.1080/14756360009030346

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Sphingomyelinase is considered to be involved in the regulation of apoptosis and cell growth. In the course of our screening for acidic sphingomyelinase inhibitors we isolated three xanthone compounds, alpha-mangostin, cowanin, and cowanol, from the bark of Garcinia speciosa. These compounds competitively inhibited bovine brain-derived acidic sphingomyelinase with IC50 values of 14.1, 19.2, and 10.9 mu M, respectively and inhibited the acidic sphingomyelinase more effectively than the neutral sphingomyelinase of bovine brain. alpha-Mangostin inhibited the acidic sphingomyelinase in the most selective manner, alpha-Mangostin was chemically modified and its structure-activity relationships are discussed.

引用

页码：129 / 138

页数：10

共 33 条

[1] A novel cytoplasmic domain of the p55 tumor necrosis factor receptor initiates the neutral sphingomyelinase pathway [J].