Yoshida Jun, Nomura Satomi, Nishizawa Naoyuki, Ito Yoshiaki, Kimura Ken-ichi
The United Graduate School of Agricultural Sciences, Iwate University, Morioka, Iwate 020-8550, Japan.
Biosci Biotechnol Biochem. 2011;75(1):136-9. doi: 10.1271/bbb.100507. Epub 2011 Jan 7.
A new biological activity of 6-(methylsulfinyl)hexyl isothiocyanate derived from Wasabia japonica was discovered as an inhibitor of glycogen synthase kinase-3β. The most potent isothiocyanate, 9-(methylsulfinyl)hexyl isothiocyanate, inhibited glycogen synthase kinase-3β at a K(i) value of 10.5 µM and showed ATP competitive inhibition. The structure-activity relationship revealed an inhibitory potency of methylsulfinyl isothiocyanate dependent on the alkyl chain length and the sulfoxide, sulfone, and/or the isothiocyanate moiety.
源自山葵的6-(甲基亚磺酰基)己基异硫氰酸酯被发现具有一种新的生物活性，即作为糖原合酶激酶-3β的抑制剂。最有效的异硫氰酸酯，9-(甲基亚磺酰基)己基异硫氰酸酯，以10.5 μM的K(i)值抑制糖原合酶激酶-3β，并表现出ATP竞争性抑制。构效关系表明，甲基亚磺酰基异硫氰酸酯的抑制效力取决于烷基链长度以及亚砜、砜和/或异硫氰酸酯部分。
