Cell lines

human hepatoma cell lines (HepG2 cells)

Preparation method

General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.5, 2.5, 5, 7.5, 10, 15 μg/ml, 24 h

Applications

Berberine as a new upregulator of liver LDLR (low-density lipoprotein receptor) expression. In HepG2 cells, the effect of berberine was also dose dependent. Northern blot showed a 50% increase in LDLR mRNA in cells treated with 2.5 μg/ml of berberine and a maximal increase of four fold of control was seen with a concentration of 15 μg/ml. The effect of BBR on LDLR was further confirmed in another human hepatoma cell line, Bel-7402. BBR at 2.5 μg/ml increased the LDLR mRNA in these cells by 2.3-fold.

Animal models

female golden hamsters

Dosage form

orally twice a day at 50 mg/kg/d or 100 mg/kg/d for 10 d.

Application

In hamsters, treatment of these hyperlipidemic animals with berberine by oral administration for 10 d resulted in dose-dependent decreases in both serum total cholesterol and LDL-c. After the 10-d treatment, berberine at a dose of 50 mg/kg/d reduced LDL-c by 26%, and at a dose of 100 mg/kg/d, reduced LDL-c by 42% as compared to the control animals on the same HFHC (high-fat and high-cholesterol) diet. The berberine effect was also time dependent. LDLR mRNA and protein levels were elevated in all berberine -treated hamsters in a dose-dependent manner. A 3.5-fold increase in mRNA and a 2.6-fold increase in protein in hamster livers treated with 100 mg/kg/d of berberine were detected.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties[1].

Berberine (1.25-160 μM; 72 hours) has potential inhibitory effects on the proliferation of four colorectal carcinoma cell lines LoVo, HCT116, SW480, and HT-29[1]. Berberine (1.25-160 μM; 24-72 hours) induces a time- and dose-dependent inhibition of LoVo cell growth[1]. LoVo cells are exposure to Berberine (10-80 μM) for 24 h. Cell cycle analysis of 40 μM Berberine-treated LoVo cells by flow cytometry shows accumulation of cells in the G2/M phase[1].Berberine (10-80 μM) suppresses cyclin B1, cdc2 and cdc25c protein expression after 24 h, especially at the dose of 80.0 μM[1].

Berberine (10, 30, or 50 mg/kg/day; gastrointestinal gavage; for 10 consecutive days) inhibits the growth of human colorectal adenocarcinoma in vivo. Berberine at doses of 30 and 50 mg/kg/day taken by gastrointestinal gavage shows inhibitory rates of 33.1% and 45.3% on the human colorectal adenocarcinoma xenograft growth in nude mice[1].

References:
[1]. Cai Y, et al. Berberine inhibits the growth of human colorectal adenocarcinoma in vitro and in vivo. J Nat Med. 2014 Jan;68(1):53-62.