Kinase inhibitors from Polygonum cuspidatum.
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.
Jayatilake
G S
GS
Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907.
Jayasuriya
H
H
Lee
E S
ES
Koonchanok
N M
NM
Geahlen
R L
RL
Ashendel
C L
CL
McLaughlin
J L
JL
Chang
C J
CJ
D000818:Animals; D002417:Cattle; D009682:Magnetic Resonance Spectroscopy; D008516:Medicine, Chinese Traditional; D010946:Plants, Medicinal / Q000737:chemistry*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D051381:Rats; D000077185:Resveratrol; D013056:Spectrophotometry, Ultraviolet; D013237:Stereoisomerism; D013267:Stilbenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D013950:Thymus Gland / Q000201:enzymology
D013267:Stilbenes; D011505:Protein-Tyrosine Kinases; D000077185:Resveratrol