In the course of a screening program for tyrosine kinase inhibitors, the chloroform extract of a tropical plant, Desmos chinensis, strongly inhibited the enzyme activity. The active substance was purified by silica gel, gel filtration, and finally crystallized. The structure was elucidated by mass spectrometry and X-ray crystallography to be 8-formyl-2,5,7-trihydroxy-6-methylflavanone, and we named it desmal. Desmal competed with peptide substrate and non-competed with ATP. It inhibited tyrosine kinase in situ in epidermal growth factor (EGF) receptor-overexpressing NIH3T3 (ER 12) cells. It also inhibited EGF-induced inositol phosphate formation and morphological changes. © 1993.
Kakeya, H., Imoto, M., Tabata, Y., Iwami, J., Matsumoto, H., Nakamura, K., … Umezawa, K. (1993). Isolation of a novel substrate-competitive tyrosine kinase inhibitor, desmal, from the plant Desmos chinensis. FEBS Letters, 320(2), 169–172. https://doi.org/10.1016/0014-5793(93)80085-9