Coronaridine is an inhibitor of TCF/β-catenin, with an IC50 value of 5.8μM[1]. Coronaridine has been widely used in neurological function studies and in development of congeners[2].
In vitro, Coronaridine showed potent cytotoxic activity in the laryngeal carcinoma cell line Hep-2, with an IC50 value of 54.47µg/mL) after 24h treatment[3]. Coronaridine treatment (10μg/ml; 24h) exhibited potent antileishmanial activity, suppressing promastigote and amastigote growth[4].
In vivo, Coronaridine treatment (72mg/kg; p.o.) for 25 minutes produced a sedative effect and reduced spontaneous activity in Male CD-1 albino mice [5].
References:
[1] Ohishi K, Toume K, Arai M A, et al. Coronaridine, an iboga type alkaloid from Tabernaemontana divaricata, inhibits the Wnt signaling pathway by decreasing β-catenin mRNA expression[J]. Bioorganic & medicinal chemistry letters, 2015, 25(18): 3937-3940.
[2] Arias H R, Tae H S, Micheli L, et al. Coronaridine congeners decrease neuropathic pain in mice and inhibit α9α10 nicotinic acetylcholine receptors and CaV2. 2 channels[J]. Neuropharmacology, 2020, 175: 108194.
[3] Rizo W F, Ferreira L E, Colnaghi V, et al. Cytotoxicity and genotoxicity of coronaridine from Tabernaemontana catharinensis A. DC in a human laryngeal epithelial carcinoma cell line (Hep-2)[J]. Genetics and molecular biology, 2013, 36: 105-110.
[4] Delorenzi J C, Attias M, Gattass C R, et al. Antileishmanial activity of an indole alkaloid from Peschiera australis[J]. Antimicrobial Agents and chemotherapy, 2001, 45(5): 1349-1354.
[5] Arias H R, Tae H S, Micheli L, et al. Coronaridine congeners decrease neuropathic pain in mice and inhibit α9α10 nicotinic acetylcholine receptors and CaV2. 2 channels[J]. Neuropharmacology, 2020, 175: 108194.
Coronaridine是一种TCF/β-catenin抑制剂，IC50值为5.8μM [1]。Coronaridine被广泛应用于神经功能研究以及衍生物的开发[2]。
在体外，Coronaridine在喉癌细胞系Hep-2中表现出显著的细胞毒活性，24小时处理后的IC50值为54.47µg/mL[7]。以10μg/mL的浓度处理24小时，Coronaridine展现出强效的抗利什曼原虫活性，可抑制前鞭毛体和无鞭毛体的生长[4]。
在体内，口服给药72mg/kg剂量的Coronaridine 25分钟后，可在雄性CD-1白化小鼠体内产生镇静作用并减少小鼠自发活动[5]。