College of Pharmacy, Chungnam National University, Daejeon, 34134, Republic of Korea.
Department of Health Care & Science, Jeonju University, Jeonju, 55069, Republic of Korea.
Arch Pharm Res. 2018 May;41(5):490-496. doi: 10.1007/s12272-018-1032-4. Epub 2018 May 2.
Ten compounds (1-10) isolated from the seeds of Cassia tora were evaluated for tyrosinase inhibition. Compounds 3, 4, and 7 inhibited tyrosinase enzymatic activity in a dose-dependent manner, with IC values of 3.0 ± 0.8, 7.0 ± 0.4, and 9.2 ± 3.4 μM, respectively. Kinetic analyses revealed a mechanism consistent with competitive inhibition. In silico molecular docking showed that compounds 3 and 4 docked in the active site of tyrosinase, whereas 7 interacted with Ala246 and Val248 at outside of the active site, and His244 and Glu256 at inside. Additionally, compounds 3, 4, and 7 suppressed melanogenesis in α-MSH-treated B16F10 melanoma cells at a concentration of 10 μM.
从苦豆子种子中分离得到的 10 种化合物（1-10）进行了酪氨酸酶抑制活性评价。化合物 3、4 和 7 呈剂量依赖性抑制酪氨酸酶的酶活性，IC 值分别为 3.0 ± 0.8、7.0 ± 0.4 和 9.2 ± 3.4 μM。动力学分析表明，其抑制机制符合竞争性抑制。分子对接显示化合物 3 和 4 与酪氨酸酶的活性部位结合，而 7 则与活性部位以外的 Ala246 和 Val248 以及活性部位以内的 His244 和 Glu256 相互作用。此外，化合物 3、4 和 7 在 10 μM 浓度下抑制 α-MSH 处理的 B16F10 黑素瘤细胞中的黑色素生成。
