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Lycorine

CAS No. : 476-28-8

MCE 站：Lycorine

产品活性：Lycorine 是从金眼科植物科中提取的天然生物碱。Lycorine 是强效具有口服活性的 SCAP?抑制剂，K_d 值 15.24 nM。Lycorine 下调 SCAP 蛋白水平而不改变其转录。Lycorine 也是黑色素瘤血管生成抑制剂。Lycorine 有潜力用于前列腺癌和代谢疾病的研究。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection  |  Apoptosis

作用靶点：Fatty Acid Synthase (FAS)  |  Virus Protease  |  Bacterial  |  Apoptosis

In Vitro: Lycorine inhibits cell proliferation in a dose-dependent manner in the abovementioned 4 PCa cell lines, and the IC₅₀ ranged from 5 μM to 10 μM., it also shows Lycorine has little effects on PNT1A cell´s proliferation.
SCAP (SREBF chaperone) is an ER-toGolgi transport protein, undergoes a conformational change, and regulates/preserves SREBFs in the ER by forming a complex with INSIG1 (insulin induced gene 1).
Lycorine (5-40 μM; 16 hours) significantly suppresses SREBFs activity (up to -70%) in a dosedependent manner and does not cause obvious cytotoxicity in cells.
Lycorine (10-20 μM; 2-16 hours) dose- and time-dependently decreases the mature SREBF1 and SREBF2 proteins in HL-7702 cells.
Lycorine (20 μM; 16 hours) neither activates NR1H3 transcription nor affect NR1H3 target genes, including ABCG5 and ABCG8, but Sterols activates NR1H3 transcription activity.
Lycorine hydrochloride (0-25 μM; 48 hours) treatment markedly suppresses the expression of vascular endothelial (VE)-cadherin 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 affected.
Lycorine hydrochloride (0-25 μM; 48 hours) treatment markedly reduces VE-cadherin protein levels in C8161 cells in a dose-dependent fashion.

In Vivo: Lycorine (oral chow; 15 mg/kg, 30 mg/kg; once daily) alleviates fat accumulation and metabolic syndrome, increases lipolysis and betaoxidation of fatty acid along with precursor and mature SREBFs in mice .

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