二苯乙烯苷衍生物 2, 4, 5-三脱氧己吡喃糖苷的合成及抗癌活性。
2, 4, 5-Trideoxyhexopyranosides derivatives of diphyllin: Synthesis and anticancer activity.
机构信息
Department of Pharmacy, Changzhou maternal and Child Health Care Hospital, Changzhou Medical Center, Nanjing Medical University, Changzhou, China.
School of Pharmacy, Nantong University, Nantong, China.
出版信息
Chem Biol Drug Des. 2022 Aug;100(2):256-266. doi: 10.1111/cbdd.14095. Epub 2022 Jun 2.
Diphyllin and its natural derivatives were identified as potent vacuolar H -ATPase (V-ATPase) inhibitors. In this study, twelve 2, 4, 5-trideoxyhexopyranosides derivatives of diphyllin were synthesized. Most of these compounds showed potent abilities to inhibit the growth of HT-29, MCF-7, HepG2 cancer cells with IC values at submicromolar concentration. The compounds 5c3 and 5c4 showed the best inhibitory activity on breast cancer cell lines MCF-7 with IC values of 0.09 and 0.10 μM. Compounds 5c3 and 5c4 showed similar V-ATPase inhibitory potency to diphyllin. Molecular docking showed that a hydrogen bond was found between the hydroxyl of 5c3 and SerA534 in the pocket of the V-ATPase receptor.
二叶钩藤苷及其天然衍生物被鉴定为有效的液泡型 H+-ATP 酶（V-ATPase）抑制剂。在这项研究中，合成了 12 种二叶钩藤苷的 2,4,5-三脱氧己糖基衍生物。这些化合物大多数具有抑制 HT-29、MCF-7、HepG2 癌细胞生长的能力，其 IC 值在亚微摩尔浓度范围内。化合物 5c3 和 5c4 对乳腺癌细胞系 MCF-7 的抑制活性最好，IC 值分别为 0.09 和 0.10 μM。化合物 5c3 和 5c4 对 V-ATPase 的抑制活性与二叶钩藤苷相似。分子对接显示，化合物 5c3 的羟基与 V-ATPase 受体口袋中 SerA534 之间形成氢键。
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