CATharanthine 是长春花中的一种生物碱,可抑制电压门控 L 型钙离子通道,具有抗肿瘤和降血压活性。
产品描述
Catharanthine suppresses nicotinic receptor-mediated diaphragm contractions (IC50=59.6 μM).
体外活性
Catharanthine evokes a concentration-dependent attenuation of carbachol responses in the rat ileum preparation, producing rightward curve displacements and decreases in maximal agonist responses. The mixture of serpentine, plus ajmalicine and catharanthine reveals a concentration-dependent inhibitory effect of acethylcholinesterase (AchE), with an IC50 at ca. 2.25 μg/mL. [1] Catharanthine can induce the self-association of tubulin into linear indefinite polymers with an efficacy that is 75% that of vinblastine or vincristine. Catharanthine binds to tubulin alpha-beta dimer with binding constant of 2.8 mM. [2] Catharanthine stimulates release of amylase from pancreatic fragments and to cause extensive degranulation of pancreatic acinar cells with accumulation of membrane material in the Golgi region. Catharanthine induces a delayed release of Ca2+ from prelabeled pancreatic fragments as compared to bethanechol. [3] Catharanthine inhibits epibatidine-induced Ca(2+) influx in TE671-α, -β, -γ, -δ cells in a noncompetitive manner with similar potencies IC50 of 17 mM-25 mM. Catharanthine inhibits [3H]TCP binding to the desensitized Torpedo AChR with higher affinity compared to the resting AChR. Catharanthine enhances [3H]cytisine binding to resting but activatable Torpedo AChRs, suggesting desensitizing properties. [4]
Cas No.
2468-21-5
分子式
C21H24N2O2
分子量
336.435
别名
长春质碱;(+)-3, 4-Didehydrocoronaridine;(+)-3,4-Didehydrocoronaridine
储存和溶解度
Ethanol:1 mg/mL(3 mM)
DMSO:62 mg/mL (184.3 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years