KINASE INHIBITORS FROM POLYGONUM-CUSPIDATUM

被引：224

作者：

JAYATILAKE, GS ^{[1
]}

JAYASURIYA, H ^{[1
]}

LEE, ES ^{[1
]}

KOONCHANOK, NM ^{[1
]}

GEAHLEN, RL ^{[1
]}

ASHENDEL, CL ^{[1
]}

MCLAUGHLIN, JL ^{[1
]}

CHANG, CJ ^{[1
]}

机构：

[1] PURDUE UNIV, SCH PHARM & PHARM SCI, DEPT MED CHEM & PHARMACOGNOSY, W LAFAYETTE, IN 47907 USA

来源：

JOURNAL OF NATURAL PRODUCTS | 1993年 / 56卷 / 10期

关键词：

D O I：

10.1021/np50100a021

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

Bioassay-directed fractionation of a medicinal plant, Polygonum cuspidatum (Polygonaceae), has led to the discovery of a hydroxystilbene, resveratrol [1], as an inhibitor of a protein-tyrosine kinase (p56lck) partially purified from bovine thymus. Both trans and cis isomers of resveratrol possess comparable protein-tyrosine kinase inhibitory activity. Comparison of the IC50 values of resveratrol for protein-tyrosine kinase inhibitory activity with those of piceid (resveratrol-O3-beta-glucoside) [2) and resveratrol-O4'-beta-glucoside [3] shows the requirement of free hydroxyl groups on both phenyl rings for the protein-tyrosine kinase inhibition. Protein kinase C inhibitory analysis suggests the requirements of two free hydroxyl groups on one phenyl ring only.

引用

页码：1805 / 1810

页数：6

共 40 条

[1] ARICHI H, 1982, CHEM PHARM BULL, V30, P1766
[2] STILBENE GLUCOSIDES IN BARK OF PICEA-SITCHENSIS
ARITOMI, M
DONNELLY, DMX
[J]. PHYTOCHEMISTRY, 1976, 15 (12) : 2006 - 2008
[3] IDENTIFICATION OF A CALCIUM-DEPENDENT AND PHOSPHOLIPID-DEPENDENT PHORBOL ESTER BINDING-ACTIVITY IN THE SOLUBLE FRACTION OF MOUSE-TISSUES
ASHENDEL, CL
STALLER, JM
BOUTWELL, RK
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1983, 111 (01) : 340 - 345
[4] Casnellie J E, 1991, Adv Pharmacol, V22, P167, DOI 10.1016/S1054-3589(08)60035-6
[5] PROTEIN-TYROSINE KINASE INHIBITION - MECHANISM-BASED DISCOVERY OF ANTITUMOR AGENTS
CHANG, CJ
GEAHLEN, RL
[J]. JOURNAL OF NATURAL PRODUCTS, 1992, 55 (11): : 1529 - 1560
[6] CREASY LL, 1988, J AM SOC HORTIC SCI, V113, P230
[7] DEBRUYN A, 1975, B SOC CHIM BELG, V84, P721
[8] Dobrusin EM, 1992, ANNU REP MED CHEM, V27, P169
[9] PICEATANNOL (3,4,3',5'-TETRAHYDROXY-TRANS-STILBENE) IS A NATURALLY-OCCURRING PROTEIN-TYROSINE KINASE INHIBITOR
GEAHLEN, RL
MCLAUGHLIN, JL
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 165 (01) : 241 - 245
[10] TOWARDS SELECTIVE PHARMACOLOGICAL MODULATION OF PROTEIN-KINASE-C - OPPORTUNITIES FOR THE DEVELOPMENT OF NOVEL ANTINEOPLASTIC AGENTS
GESCHER, A
[J]. BRITISH JOURNAL OF CANCER, 1992, 66 (01) : 10 - 19

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