Lycorine

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Lycorine

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

476-28-8

石蒜碱

Lycorine 是从石蒜科植物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。

生物活性

Lycorine is a natural alkaloid extracted from theAmaryllidaceaeplant. Lycorine is a potent and orally activeSCAPinhibitor with aK_dvalue 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription^[2]. Lycorine is also amelanoma vasculogenicinhibitor^[3]. Lycorine can be used for the study of prostatecancerand metabolic diseases^[2].

IC₅₀& Target

Kd: 15.24 nM (SCAP)^[1]

体外研究
(In Vitro)

Lycorine inhibits cell proliferation in a dose-dependent manner in the abovementioned 4 PCa cell lines, and the IC₅₀ranged from 5 μM to 10 μM., it also shows Lycorine has little effects on PNT1A cell's proliferation^[1].
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)^[2].
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^[2].
Lycorine (10-20 μM; 2-16 hours) dose- and time-dependently decreases the mature SREBF1 and SREBF2 proteins in HL-7702 cells^[2].
Lycorine (20 μM; 16 hours) neither activates NR1H3 transcription nor affect NR1H3 target genes, including ABCG5 and ABCG8, but Sterols activates NR1H3 transcription activity^[1].
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^[3].
Lycorine hydrochloride (0-25 μM; 48 hours) treatment markedly reduces VE-cadherin protein levels in C8161 cells in a dose-dependent fashion^[3].

Cell Viability Assay^[2]

Cell Line:	HL-7702/SRE-Luc cells
Concentration:	16 hours
Incubation Time:	5 μM; 10 μM; 20 μM; 40 μM
Result:	Had no cytotoxicity on HL-7702 cells.

Western Blot Analysis^[2]

Cell Line:	HL-7702/SRE-Luc cells
Concentration:	2 hours, 4 hours, 8 hours, 12 hours, 16 hours
Incubation Time:	10 μM; 20 μM
Result:	Decreased p-SREBF1, m-SREBF1, p-SREBF2 and p-SREBF1 protein expression.

RT-PCR^[3]

Cell Line:	C8161 cells
Concentration:	0 μM, 1.56 μM, 3.13 μM, 6.25 μM, 12.5 μM, 25 μM
Incubation Time:	48 hours
Result:	Markedly suppressed the expression of VE-cadherin in a dose-dependent manner and also slightly diminished the expression of Sema4D in C8161 cells.

体内研究
(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^[2].

Animal Model:	High-fat diet (HFD)-fed C57BL/6J mice^[2]
Dosage:	15 mg/kg, 30 mg/kg
Administration:	Oral chow; once daily
Result:	Ameliorated high-fat diet-induced hyperlipidemia, hepatic steatosis, and insulin resistance in mice.

分子量

287.31

性状

Solid

Formula

C₁₆H₁₇NO₄

CAS 号

476-28-8

中文名称

石蒜碱

结构分类

Alkaloids
Isoquinoline Alkaloids

Alkaloids
Pyrrole Alkaloids

来源

Plants
Amaryllidaceae

Plants
other families

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL(87.01 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.4806 mL	17.4028 mL	34.8056 mL
5 mM	0.6961 mL	3.4806 mL	6.9611 mL
10 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。