Emodin, a protein tyrosine kinase inhibitor from Polygonum cuspidatum.
Bioassay-directed fractionation of a Chinese medicinal plant, Polygonum cuspidatum (Polygonaceae), has led to the discovery of an anthraquinone, emodin [1], as a strong inhibitor of a protein tyrosine kinase (p56lck) partially purified from bovine thymus. Comparison of the IC50 values of emodin for protein tyrosine kinase inhibitory activity with physcion [2] and emodin-O8-D-glucoside [3], also isolated from the same plant, reveal the importance of the hydroxyl groups at C-6 and C-8 for the observed activity.
Jayasuriya
H
H
Department of Medicinal Chemistry and Pharmacognosy, Purdue University, West Lafayette, Indiana 47907.
Koonchanok
N M
NM
Geahlen
R L
RL
McLaughlin
J L
JL
Chang
C J
CJ
D000818:Animals; D002417:Cattle; D004642:Emodin / Q000302:isolation & purification / Q000494:pharmacology*; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck); D010946:Plants, Medicinal / Q000737:chemistry*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*
D011505:Protein-Tyrosine Kinases; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck); D004642:Emodin