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Tetrandrine

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Chemical Structure| 518-34-3 同义名 : 汉防己甲素 ;NSC-77037;d-Tetrandrine;TTD.;Sinomenine A;(S,S)-(+)-Tetrandrine;Fanchinine
CAS号 : 518-34-3
货号 : A256378
分子式 : C38H42N2O6
纯度 : 95%
分子量 : 622.75
MDL号 : -
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(6.42 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Calcium Channel
描述 Tetrandrine is a high-affinity blocker of the type II, maxi-Ca(2+)-activated K+ channel of the rat neurohypophysial terminals. The non-inactivating component of ICa was inhibited by external tetrandrine in a voltage- and dose-dependent manner, with an IC50 = 10.1 microM. IKCa was elicited by depolarizations when approximately 10 microM Ca2+ was present on the cytoplasmic side. Only externally applied tetrandrine, at 1 microM, decreased the amplitude of IKCa, whereas the fast inward Na+ current and transient outward K+ current were not affected[3]. Tetrandrine enhanced the ubiquitination and degradation of Syk (spleen tyrosine kinase) and consequently repressed the osteoclastogenesis and bone destruction through the AhR-c-src-c-Cbl (aryl hydrocarbon receptor) pathway[4]. Furthermore, Tetrandrine is a bisbenzylisoquinoline alkaloid known to exhibit anticancer activity against different cancers. Dose- and time-dependant cytotoxic effect of tetradrine on both MDA-MB-231 and PANC-1 cells (pancreatic PANC-1 and breast MDA-MB-231 cancer cells) with IC50 values ranging between 51 and 54 μM and 22 and 27 μM for 24 h and 48 h of incubation respectively[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.03mL

1.61mL

0.80mL

16.06mL

3.21mL

1.61mL
参考文献

[1]Fang QZ, Zhong N, et al. Tetrandrine inhibits Ca2+-activated chloride channel in cultured human umbilical vein endothelial cells. Acta Pharmacol Sin. 2004 Mar;25(3):327-33.

[2]Dong Y, Yang MM, Kwan CY. In vitro inhibition of proliferation of HL-60 cells by tetrandrine and coriolus versicolor peptide derived from Chinese medicinal herbs. Life Sci. 1997;60(8):PL135-40.

[3]Wang G, Lemos JR. Tetrandrine blocks a slow, large-conductance, Ca(2+)-activated potassium channel besides inhibiting a non-inactivating Ca2+ current in isolated nerve terminals of the rat neurohypophysis. Pflugers Arch. 1992; 421(6):558‐565

[4]Jia Y, Tao Y, Lv C, Xia Y, Wei Z, Dai Y. Tetrandrine enhances the ubiquitination and degradation of Syk through an AhR-c-src-c-Cbl pathway and consequently inhibits osteoclastogenesis and bone destruction in arthritis. Cell Death Dis. 2019; 10(2):38. Published 2019 Jan 15

[5]N B, Chandrashekar KR, Prabhu A, Rekha PD. Tetrandrine isolated from Cyclea peltata induces cytotoxicity and apoptosis through ROS and caspase pathways in breast and pancreatic cancer cells. In Vitro Cell Dev Biol Anim. 2019; 55(5):331‐340