Liensinine 是一种自噬/线粒体自噬抑制剂

Liensinine

中文名：莲心碱

CAS：2586-96-1

品牌：MedChemExpress (MCE)

存储条件：4°C, protect from light

生物活性：Liensinine 是一种自噬/线粒体自噬抑制剂。莲心碱是一种主要的异喹啉生物碱，提取自Nelumbo nucifera Gaertn的种子胚，具有广泛的生物活性，包括抗心律失常、抗高血压、抗肺纤维化、舒张血管平滑肌等肌肉等[1]。

体内：Liensinine (口服灌胃，100或200mg/kg，每日一次，10周) 可有效处理牙周炎，与甲硝唑类药物相似，具有一定的剂量依赖性[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: KM mice[2] Dosage: 100 mg/kg, 200 mg/kg Administration: oral gavage, daily, 10 weeks Result: Reduced the gingival index and increased the SOD levels, the CAT, GSH-Px levels and decreased the NO, MDA, and ET levels compared to the control group. Animal Model: Institute of Cancer Research (ICR) mice (male, 20-22 g)[3] Dosage: Administration: 5 mg/kg by oral administration; 1 mg/kg by intravenous administration Result: The pharmacokinetic parameters of Liensinine in mice Parameters po (5 mg/kg) iv (1 mg/kg) AUC(0-t) (ng/mL*h) 18.8 ± 2.7 211.2 ± 54.9 AUC(0-∞) (ng/mL*h) 19.1 ± 2.8 227.9 ± 60.1 MRT(0-t)( h) 3.2 ± 0.4 2.6 ± 0.5 MRT(0-∞) (h) 3.4 ± 0.5 3.5 ± 0.9 t1/2z (h) 1.9 ± 0.2 3.8 ± 0.8 CLz/F (L/h/kg) 266.0 ± 41.3 4.7 ± 1.2 Vz/F (L/kg) 708.5 ± 79.9 25.9 ± 11.0 Cmax (ng/mL) 5.3 ± 0.2 169.5 ± 53.5 Clinical Trial

参考文献：

[1]. Zhou J, et al. A novel autophagy/mitophagy inhibitor liensinine sensitizes breast cancer cells to chemotherapy through DNM1L-mediated mitochondrial fission. Autophagy. 2015;11(8):1259-79.
[2]. Liang Pang, et al. Protective effect of liensinine on periodontitis through its antioxidant effect in mice. Journal of the Korean Society for Applied Biological Chemistry volume 58, pages927-936
[3]. Shuhua Tong, et al. Pharmacokinetics and bioavailability of liensinine in mouse blood by UPLC-MS/MS. Acta Chromatographica,Volume 33: Issue 4,14 Oct 2020.