Yoon Goo, Lee Woojung, Kim Su-Nam, Cheon Seung Hoon
KIST Gangneung Institute, Gangneung, Republic of Korea.
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5155-7. doi: 10.1016/j.bmcl.2009.07.054. Epub 2009 Jul 24.
Compounds (1-6) isolated from the CH(2)Cl(2) extract of Glycyrrhiza inflata and semisynthetic licochalcone A derivatives (7-14) were evaluated for their protein tyrosine phosphatase 1B (PTP1B) inhibitory activities. Licochalcones A (4) and E (6), each with an allyl group at position 5 in the B ring exhibited significant inhibitory effects. Licochalcone A derivative 7, the most potent among the series, had an IC(50) value of 11.7+/-2.0 microM, ca. twofold better than that of licochalcone A (4).
对从胀果甘草的二氯甲烷提取物中分离得到的化合物（1 - 6）以及半合成的甘草查尔酮A衍生物（7 - 14）进行了蛋白酪氨酸磷酸酶1B（PTP1B）抑制活性评估。B环5位带有烯丙基的甘草查尔酮A（4）和E（6）均表现出显著的抑制作用。该系列中活性最强的甘草查尔酮A衍生物7的IC50值为11.7±2.0微摩尔，约为甘草查尔酮A（4）的两倍。
