Koumine

Koumine is an alkaloid that has been found in Gelsemium elegans and has diverse biological activities.^1,2,3,4 It inhibits the proliferation of MCF-7 breast cancer cells (IC₅₀ = 124 µg/ml) as well as induces apoptosis and cell cycle arrest at the G₂/M phase in the same cells.¹ Koumine (200 and 400 µg/ml) reduces LPS-induced increases in inducible nitric oxide synthase (iNOS), IL-1β, IL-6, and TNF-α levels in RAW 264.7 macrophages.² It inhibits acetic acid-induced writhing and formalin-induced paw licking and biting in mice when administered at doses of 2 and 10 mg/kg.³ Koumine (0.4-10 mg/kg) increases the number of entries into and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.⁴

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1. Zhang, X., Chen, Y., Gao, B., et al. Apoptotic effect of koumine on human breast cancer cells and the mechanism involved. Cell Biochem. Biophys. 72(2), 411-416 (2015).

2. Yuan, Z., Matias, F.B., Wu, J., et al. Koumine attenuates lipopolysaccaride-stimulated inflammation in RAW264.7 macrophages, coincidentally associated with inhibition of NF-κB, ERK and p38 pathways. Int. J. Mol. Sci. 17(3), 430 (2016).

3. Liu, M., Huang, H.-H., Yang, J., et al. The active alkaloids of Gelsemium elegans Benth. are potent anxiolytics. Psychopharmacology (Berl) 225(4), 839-851 (2013).

4. Xu, Y., Qiu, H.-Q., Liu, H., et al. Effects of koumine, an alkaloid of Gelsemium elegans Benth., on inflammatory and neuropathic pain models and possible mechanism with allopregnanolone. Pharmacol. Biochem. Behav. 101(3), 504-514 (2012).