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3486-66-6

中文名稱 硫酸黃連堿
英文名稱 COPTISINE
CAS 3486-66-6
分子式 C19H14NO4+
分子量 320.32
MOL 文件 3486-66-6.mol
更新日期 2024/10/25 15:25:59
3486-66-6 結(jié)構(gòu)式 3486-66-6 結(jié)構(gòu)式

基本信息

中文別名
黃蓮鹼
硫酸黃連堿
黃連堿(標(biāo)準(zhǔn)品)
黃連堿, 來源于黃連
COPTISINE 黃連堿
英文別名
Coptisin
COPTISINE
COPTISINE(P)
Coptisine Sulfate
Coptisine, 98%, from Coptis chinensis Franch.
6,7-Dihydrobis[1,3]benzodioxolo[5,6-a:4',5'-g]quinolizinium
Bis[1,3]benzodioxolo[5,6-a:4',5'-g]quinolizinium,6,7-dihydro-
5,6-Dihydro-2,3:9,10-bis(methylenedioxy)dibenzo[a,g]quinolizinium
所屬類別
生物化工:中草藥成分

物理化學(xué)性質(zhì)

外觀性狀極略微溶于水, 微溶于乙醇, 溶于堿。 來源于罌粟科植物白屈菜根
熔點(diǎn)212-217 °C
儲存條件儲存于 2-8°C
溶解度Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
形態(tài)粉末

應(yīng)用領(lǐng)域

用途1
用于含量測定/鑒定/藥理實(shí)驗(yàn)等。
藥理藥效:有抗微生物活性, 其抗卡爾酵母菌的效力比小檗堿、巴馬汀及非洲防己堿都強(qiáng);殺蟲活性;誘導(dǎo)神經(jīng)細(xì)胞分化;對胃粘膜有保護(hù)作用;抗癌作用;免疫系統(tǒng)的作用;平滑肌松弛作用;抗腎炎作用。

安全數(shù)據(jù)

毒害物質(zhì)數(shù)據(jù)3486-66-6(Hazardous Substances Data)

常見問題列表

生物活性
Coptisine 是從黃連中分離到的生物堿,是一種有效的非競爭性的 IDO 抑制劑,Ki 值為 5.8 μM,IC50 值為 6.3 μM。
靶點(diǎn)

IDO

6.3 μM (IC 50 )

IDO

5.8 μM (Ki)

體外研究

Coptisine is an efficient uncompetitive IDO inhibitor with a K i value of 5.8 μM and an IC 50 value of 6.3 μM. Coptisine (0.1-100 μM) inhibits the proliferation of A549, H460, H2170, MDA-MB-231 and HT-29 cells, with IC 50 s of 18.09, 29.50, 21.60, 20.15 and 26.60?μM, respectively. Coptisine (12.5, 25, 50 μM) upregulates the expression of pH2AX and p21, reduces expression of cyclin B1, cdc2, and cdc25C, and induces G2/M arrest and apoptosis of A549 cells in a concentration-dependent manner. Coptisine (12.5, 25, 50 μM) also induces mitochondrial dysfunction and activates caspases activities in A549 cells. Furthermore, Coptisine (50 μM) increases ROS levels in a time-dependent manner (0.5, 1, 2, 4, 12, and 24?h).

體內(nèi)研究

Coptisine shows increased toxicity in mice in a concentration dependent manner, with LD 50 value of 880.18 mg/kg. Coptisine (154 mg/kg/day, 90 days) shows no toxicity on SD rats. Coptisine (23.35, 46.7, 70.05 mg/kg, p.o.) dose-dependently decreases the levels of TC, TG, and LDL-c and increases HDL-c content in serum of hamsters to different degree, slows down weight gain induced by the HFHC diet, and raises the level of cholesterol and TBA in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR protein expression level and induces the protein expression of SREBP-2, LDLR, and CYP7A1 involved in cholesterol metabolism.

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