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Daurisoline

CAS No. : 70553-76-3

MCE 国际站：Daurisoline

产品活性：Daurisoline 是一个 hERG 抑制剂，也是一种自噬抑制剂。

研究领域：Autophagy  |  Membrane Transporter/Ion Channel

作用靶点：Autophagy  |  Potassium Channel

结构分类：生物碱  |  异喹啉类生物碱  |  酚类  |  多酚类

来源：植物  |  其他科

In Vitro: Daurisoline (compound 1) shows a maximal inhibitory effect on the end of depolarization (I_hERG-step) at +20 mV and on the peak tail current (I_hERG-tail) at +60 mV. At concentrations of 1, 3, 10, and 30 μM, the inhibition ratios for current amplitude at the end of depolarization (I_hERG-step) are 32.2±4.2%, 41.6±2.6%, 62.1±5.9%, and 74.8±6.8%, respectively; the IC₅₀ is 9.1 μM. In turn, the inhibition ratios for I_hERG-tail are 16.7±5.8%, 31.1±4.5%, 55.1±7.2%, and 81.2±7.0%, respectively; the IC₅₀ is 9.6 μM. Daurisoline (DAS) inhibits the CPT-induced autophagy in different cancer cell lines, with IC₅₀s of 74.75±1.03, 50.54±1.02 and 80.81±1.10 μM in HeLa, A549 and HCT-116 cells, respectively. DAC and Daurisoline also impair lysosomal function and lysosomal acidification, via inhibiting the lysosome V-type ATPase acitivity in DAC and Daurisoline treated cells.

In Vivo: The results show that plasma concentration exists a biexponential decline following iv administration of Daurisoline (DS) or dauricine (Dau) 6 mg/kg. After iv Daurisoline and Dau 6 mg/kg in beagle dogs, HR, LVSP, dp/dtmax, and SBP are decreased. But the maximum pharmacological effects of both drugs peak at 10 to15 min later than the maximum plasma concentration is observed.

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