番石榴碱作用机制 - Medchemexpress - MCE中国

1、Product Data SheetLycorineCat. No.: HY-N0288CAS No.: 476-28-8分式: CHNO分量: 287.31作靶点: Fatty Acid Synthase (FAS); Virus Protease; Bacterial; Apoptosis作通路: Metabolic Enzyme/Protease; Anti-infection; Apoptosis储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 25 mg/mL

2、(87.01 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.4806 mL 17.4028 mL 34.8056 mL5 mM 0.6961 mL 3.4806 mL 6.9611 mL10 mM 0.3481 mL 1.7403 mL 3.4806 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在

3、 1 个内使。BIOLOGICAL ACTIVITY物活性 Lycorine从眼科植物科中提取的天然物碱。Lycorine 强效具有服活性的 SCAP 抑制剂，Kd 值 15.24 nM。Lycorine 下调 SCAP 蛋平不改变其转录。Lycorine 也 素瘤管成抑制剂。Lycorine 有潜于前列腺癌和代谢疾病的研究。IC & Target Kd: 15.24 nM (SCAP)1体外研究Lycorine inhibits cell proliferation in a dose-dependent manner in the abovementioned 4 PCa cell lin

4、es, and the IC50ranged from 5 M to 10 M., it also shows Lycorine has little effects on PNT1A cells proliferation1.SCAP (SREBF chaperone) is an ER-toGolgi transport protein, undergoes a conformational change, andregulates/preserves SREBFs in the ER by forming a complex with INSIG1 (insulin induced ge

5、ne 1)2.Lycorine (5-40 M; 16 hours) significantly suppresses SREBFs activity (up to -70%) in a dosedependent manner anddoes not cause obvious cytotoxicity in cells2.Page 1 of 2 www.MedChemELycorine (10-20 M; 2-16 hours) dose- and time-dependently decreases the mature SREBF1 and SREBF2 proteins inHL-7

6、702 cells2.Lycorine (20 M; 16 hours) neither activates NR1H3 transcription nor affect NR1H3 target genes, including ABCG5and ABCG8, but Sterols activates NR1H3 transcription activity1.Lycorine hydrochloride (0-25 M; 48 hours) treatment markedly suppresses the expression of vascular endothelial(VE)-c

7、adherin in a dose-dependent manner and also slightly diminishes the expression of Sema4D in C8161 cells.However, the expression of the other six genes is not affected3.Lycorine hydrochloride (0-25 M; 48 hours) treatment markedly reduces VE-cadherin protein levels in C8161 cells in adose-dependent fa

8、shion3.Cell Viability Assay2Cell Line: HL-7702/SRE-Luc cellsConcentration: 16 hoursIncubation Time: 5 M; 10 M; 20 M; 40 MResult: Had no cytotoxicity on HL-7702 cells.Western Blot Analysis2Cell Line: HL-7702/SRE-Luc cellsConcentration: 2 hours, 4 hours, 8 hours, 12 hours, 16 hoursIncubation Time: 10

9、M; 20 MResult: Decreased p-SREBF1, m-SREBF1, p-SREBF2 and p-SREBF1 protein expression.RT-PCR3Cell Line: C8161 cellsConcentration: 0 M, 1.56 M, 3.13 M, 6.25 M, 12.5 M, 25 MIncubation Time: 48 hoursResult: Markedly suppressed the expression of VE-cadherin in a dose-dependent mannerand also slightly di

10、minished the expression of Sema4D in C8161 cells.体内研究 Lycorine (oral chow; 15 mg/kg, 30 mg/kg; once daily) alleviates fat accumulation and metabolic syndrome, increaseslipolysis and betaoxidation of fatty acid along with precursor and mature SREBFs in mice 2.Animal Model: High-fat diet (HFD)-fed C57

11、BL/6J mice2Dosage: 15 mg/kg, 30 mg/kgAdministration: Oral chow; once dailyResult: Ameliorated high-fat diet-induced hyperlipidemia, hepatic steatosis, and insulinresistance in mice.REFERENCESPage 2 of 3 www.MedChemE1. Hu M, et al.Lycorine is a novel inhibitor of the growth and metastasis of hormone-

12、refractory prostate cancer.Oncotarget. 2015 Jun 20;6(17):15348-61.2. Zu-Guo Zheng, et al. Discovery of a Potent SCAP Degrader That Ameliorates HFD-induced Obesity, Hyperlipidemia and Insulin Resistance via anAutophagy-Independent Lysosomal Pathway. Autophagy. 2020 May 20;1-22.3. 1.Liu, R. et al. Lycorine hydrochloride inhibits metastatic melanoma cell-dominant vasculogenic mimicry. Pigment cell & melanoma research 25, 630-638, doi:10.1111/j.1755-148X.2012.01036.x (2012).McePdfHeightCaution: Product has