An aporphine alkaloid with diverse biological activities
Crebanine is an aporphine alkaloid that has been found in Stephania venosa and has diverse biological activities.1,2,3,4,5 It is an antagonist of α7 nicotinic acetylcholine receptors (nAChRs; IC50 = 19.1 ?M) and inhibits sodium currents (INa) in isolated guinea pig ventricular myocytes (IC50 = 283 ?M).1,2 Crebanine is active against the Gram-positive bacteria M. lysodeikticus, B. cereus, B. megaterium, B. subtilis, and S. aureus (MICs = 0.312, 0.213, 0.312, 0.312, and 0.312 g/L, respectively), as well as the plant pathogenic fungi C. kaki, G. haraeanum, P. oryzae, R. solani, and C. graminicola (EC50s = 111, 64.7, 18.9, 42.5, and 40.5 mg/L, respectively).3 It inhibits the LPS-induced production of TNF-α, IL-6, nitric oxide (NO), and prostaglandin E2 in RAW 264.7 macrophages when used at a concentration of 29.5 ?M.4 Crebanine inhibits the proliferation of A549 lung, MDA-MB-231 and MCF-7 breast, and SKOV3 and Caov-3 ovarian cells and reduces TNF-α induced invasion and migration of A549 cells in a concentration-dependent manner.5 It prevents scopolamine-induced memory deficits in the Morris water maze in mice when administered at a dose of 25 mg/kg.1
1.Rojsanga, P., Boonyarat, C., Utsintong, M., et al.The effect of crebanine on memory and cognition impairment via the alpha-7 nicotinic acetylcholine receptorLife Sci.91(3-4)107-114(2012) 2.Xiao-Shan, H., Qing, L., Yun-Shu, M., et al.Crebanine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytesChin. J. Nat. Med.12(1)20-23(2014) 3.Deng, Y., Yu, Y., Luo, H., et al.Antimicrobial activity of extract and two alkaloids from traditional Chinese medicinal plant Stephania dielsianaFood Chem.124(4)1556-1560(2011) 4.Intayoung, P., Limtrakul, P., and Yodkeeree, S.Antiinflammatory activities of crebanine by inhibition of NF-κB and AP-1 activation through suppressing MAPKs and Akt signaling in LPS-induced RAW264.7 macrophagesBiol. Pharm. Bull.39(1)54-61(2016) 5.Yodkeeree, S., Pompimon, W., and Limtrakul, P.Crebanine, an aporphine alkaloid, sensitizes TNF-α-induced apoptosis and suppressed invasion of human lung adenocarcinoma cells A549 by blocking NF-κB-regulated gene productsTumour Biol.35(9)8615-8624(2014)
动态评分
0.0