Background:
Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells[1]. Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities[3], protects against the development of arthritis in Rheumatoid arthritis (RA) animal models[2].
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[1].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[1].Koumine (25, 50, 100, and 200?μM) decreases the protein and mRNA levels of microglia M1 polarization factors in LPS-induced BV2 cells[3].
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)[2].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[2].Koumine (0.28, 7 mg/kg, s.c.) significantly reduces neuropathic pain after nerve injury. Koumine suppresses the increased Iba-1 protein level[3].
参考文献:
[1]. Zhang X, et al. Apoptotic Effect of Koumine on Human Breast Cancer Cells and the Mechanism Involved. Cell Biochem Biophys. 2015 Jun;72(2):411-6.
[2]. Yang J, et al. Effects of Koumine on Adjuvant- and Collagen-Induced Arthritis in Rats. J Nat Prod. 2016 Oct 28;79(10):2635-2643.
[3]. Jin GL, et al. Koumine Attenuates Neuroglia Activation and Inflammatory Response to Neuropathic Pain. Neural Plast. 2018 Mar 25;2018:9347696.
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