Pimarane Diterpenoids from the Seeds of Caesalpinia minax as PTP1B Inhibitors and Insulin Sensitizers.
Pimarane Diterpenoids from the Seeds of Caesalpinia minax as PTP1B Inhibitors and Insulin Sensitizers.
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云实种子中的海松烷二萜类化合物作为PTP1B抑制剂和胰岛素增敏剂。
DOI：
10.3390/molecules25204674
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发表时间：
2020-10-13
期刊：
影响因子：
--
通讯作者：
Lin L
中科院分区：
文献类型：
--
作者：
Xu Y;Feng Z;Zhang T;Lv P;Cao J;Li D;Peng C;Lin L
蛋白酪氨酸磷酸酶1B （PTP1B）被认为是治疗胰岛素抵抗的一个有希望的靶点。为了寻找天然存在的pttb1b拮抗剂，从海马兰种子中分离到两个新的海马兰二萜，分别命名为2α-羟基-7-氧-海马兰-8(9)，15-二烯(1)和19-羟基-2α-乙酰氧-7-氧-海马兰-8(9)，15-二烯(2)。它们的结构通过NMR和HR-ESIMS数据的广泛分析确定，它们的绝对构型通过电子圆二色（ECD）光谱确定。化合物1是PTP1B的竞争性抑制剂，IC50（半最大抑制浓度）值为19.44±2.39µM, Ki（抑制常数）值为13.69±2.72 μM。此外，化合物1通过激活胰岛素信号通路，剂量依赖性地促进胰岛素刺激的C2C12肌管葡萄糖摄取。化合物1可能作为胰岛素增敏剂进一步开发。
Protein-tyrosine phosphatase 1B (PTP1B) has been considered as a promising target for treating insulin resistance. In searching for naturally occurring PTB1B antagonists, two new pimarane diterpenoids, named 2α-hydroxy-7-oxo-pimara-8(9),15-diene (1) and 19-hydroxy-2α-acetoxy-7-oxo-pimara-8(9),15-diene (2), were isolated from the seeds of Caesalpinia minax. Their structures were determined by extensive analysis of NMR and HR-ESIMS data, and their absolute configurations were determined by electronic circular dichroism (ECD) spectra. Compound 1 was disclosed as a competitive inhibitor of PTP1B with an IC50 (the half-maximal inhibitory concentration) value of 19.44 ± 2.39 µM and a Ki (inhibition constant) value of 13.69 ± 2.72 μM. Moreover, compound 1 dose-dependently promoted insulin-stimulated glucose uptake in C2C12 myotubes through activating insulin signaling pathway. Compound 1 might be further developed as an insulin sensitizer.
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