Koumine钩吻素子,1358-76-5

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Koumine

CAS No. : 1358-76-5

MCE 国际站：Koumine

产品活性：Koumine 是从钩吻 (Gelsemium elegans) 中得到的生物碱，具有高效抗肿瘤活性，在肿瘤细胞中能够增加 Bax/Bcl-2 的蛋白比例和 caspase-3 的表达。Koumine 具有抗焦虑、抗应激、抗银屑病活性，也可用于缓解疼痛的研究。在类风湿性关节炎动物模型中，Koumine 能够预防关节炎的发展。

研究领域：Apoptosis

作用靶点：Bcl-2 Family

In Vitro: Koumine (0.5, 1 and 2 mg/mL) dose- and time-dependently inhibits the proliferation of MCF-7 cells, with an IC₅₀ of 124 µg/mL at 72 h. Koumine induces apoptosis, causes cell cycle arrest at G2/M phase.
Koumine (0.5, 1 and 2 mg/mL) up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in a dose-dependent manner in MCF-7 Cells.
Koumine (25, 50, 100, and 200 μM) decreases the protein and mRNA levels of microglia M1 polarization factors in LPS-induced BV2 cells.

In Vivo: Koumine is less toxic, with the median lethal dose (LD₅₀) of 300.0 mg/kg on Wistar rats. Koumine (0.6, 3, or 15 mg/kg/per, p.o.) exhibits antirheumatic properties in rats with adjuvant-induced arthritis (AIA) and collagen-induced arthritis (CIA).
Koumine inhibits the increase in cytokines in joint tissue and TNF-α level in serum at 15 mg/kg, and suppresses the increase in the serum level of IL-1β at 3 and 15 mg/kg.
Koumine (0.28, 7 mg/kg, s.c.) significantly reduces neuropathic pain after nerve injury. Koumine suppresses the increased Iba-1 protein level.

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