School of Pharmacy, National Cheng Kung University Medical College, Tainan 70101, Taiwan.
Department of Anesthesiology, National Cheng Kung University Hospital, College of Medicine, National Cheng Kung University, Tainan 70101, Taiwan.
Int J Mol Sci. 2020 Feb 13;21(4):1268. doi: 10.3390/ijms21041268.
Croton is an extensive flowering plant genus in the spurge family, Euphorbiaceae. Three croton compounds with the common ent-kaurane skeleton have been purified from roton tonkinensis.
We examined any modifications of croton components (i.e., croton-01 [ent-18-acetoxy-7α-hydroxykaur-16-en-15-one], croton-02 [ent-7α,14β-dihydroxykaur-16-en-15-one] and croton-03 [ent-1β-acetoxy-7α,14β-dihydroxykaur-16-en-15-one] on either hyperpolarization-activated cation current (I) or -mediated K current identified in pituitary tumor (GH) cells and in rat insulin-secreting (INS-1) cells via patch-clamp methods.
Addition of croton-01, croton-02, or croton-03 effectively and differentially depressed amplitude. Croton-03 (3 μM) shifted the activation curve of to a more negative potential by approximately 11 mV. The voltage-dependent hysteresis of was also diminished by croton-03 administration. Croton-03-induced depression of could not be attenuated by SQ-22536 (10 μM), an inhibitor of adenylate cyclase, but indeed reversed by oxaliplatin (10 μM). The in INS-1 cells was also depressed effectively by croton-03.
Our study highlights the evidence that these -kaurane diterpenoids might conceivably perturb these ionic currents through which they have high influence on the functional activities of endocrine or neuroendocrine cells.
巴豆是大戟科巴豆属的一种开花植物。已从越南巴豆中分离出三种具有共同-ent-贝壳杉烷骨架的巴豆化合物。
我们通过膜片钳技术检测了巴豆成分（即 croton-01 [ent-18-乙酰氧基-7α-羟基贝壳杉-16-烯-15-酮]、croton-02 [ent-7α，14β-二羟基贝壳杉-16-烯-15-酮]和 croton-03 [ent-1β-乙酰氧基-7α，14β-二羟基贝壳杉-16-烯-15-酮]）对垂体肿瘤（GH）细胞和大鼠胰岛素分泌（INS-1）细胞中已鉴定的超极化激活阳离子电流（I）或介导的 K 电流的任何修饰。
添加 croton-01、croton-02 或 croton-03 可有效且有差异地抑制 幅度。croton-03（3 μM）使 激活曲线向更负的电位约 11 mV 偏移。croton-03 给药还减小了 的电压依赖性滞后。SQ-22536（10 μM），一种环腺苷酸酶抑制剂，不能减弱 croton-03 诱导的 抑制，但 oxaliplatin（10 μM）确实逆转了抑制作用。croton-03 也有效抑制了 INS-1 细胞中的 。
我们的研究强调了这些-ent-贝壳杉烷二萜类化合物可能通过它们对内分泌或神经内分泌细胞的功能活动有很大影响的离子电流的证据。
