PURPACTINS, NEW INHIBITORS OF ACYL-COA - CHOLESTEROL ACYLTRANSFERASE PRODUCED BY PENICILLIUM-PURPUROGENUM .3. CHEMICAL MODIFICATION OF PURPACTIN-A

被引：10

作者：

NISHIDA, H

TOMODA, H

CAO, J

ARAKI, S

OKUDA, S

OMURA, S

机构：

[1] KITASATO INST,BIOL FUNCT RES CTR,MINATO KU,TOKYO 108,JAPAN

[2] KITASATO UNIV,SCH PHARMACEUT SCI,MINATO KU,TOKYO 108,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1991年 / 44卷 / 02期

关键词：

D O I：

10.7164/antibiotics.44.152

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Acylated drivatives of the C-1' and/or C-11 hydroxy group(s) of penicillide were synthesized and their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was studied. Introduction of long acyl group into either or both hydroxy residue(s) decreased the inhibitory activity. A small acyl moiety such as acetyl or n-butyryl at the C-1' hydroxy group is responsible for potent inhibitory activity against ACAT. The 1'-O-acetyl-11-O-tetrahydropyranyl derivative (11-O-2"-tetrahydropyranylpurpactin A) showed high selectivity (cytotoxic dose vs. effective dose) in a cell assay using J774 macrophages.

引用

页码：152 / 159

页数：8

共 5 条

[1]

HEIDER JG, 1983, J LIPID RES, V24, P1127

[2]

KATOCS AS, 1988, FASEB J, V2, pA1219

[3]

LARGIS EE, 1989, J LIPID RES, V30, P681

[4] PURPACTINS, NEW INHIBITORS OF ACYL-COA - CHOLESTEROL ACYLTRANSFERASE PRODUCED BY PENICILLIUM-PURPUROGENUM .2. STRUCTURE ELUCIDATION OF PURPACTIN-A, PURPACTIN-B AND PURPACTIN-C [J].