Berberine hydrochloride

Berberine hydrochloride is a bioactive alkaloid of the isoquinoline class derived from the medicinal plant Coptis chinensis of the Ranunculaceae family, possessing a wide range of pharmacological functions with applications in cancer, inflammation, diabetes, depression, hypertension, and various infections. Berberine hydrochloride can induce oxidative DNA damage in cancer cells^[1]. It is a dual inhibitor of topoisomerase I and II and a potential autophagy modulator ^[2]. Due to its activating effect on AMPK, it can improve insulin sensitivity and reduce blood sugar levels ^[3].

In vitro, berberine hydrochloride (1.25-160μM; 72 hours) exhibits potential inhibitory effects on the proliferation of four colorectal cancer cell lines, LoVo, HCT116, SW480, and HT-29, with IC₅₀ values ranging from 40.8±4.1 μM (LoVo) to 98.6±2.9μM (HCT116) ^[1]. Berberine hydrochloride (40.0μM) can induce G2/M phase cell cycle arrest, with an increase in the G2/M cell population and a progressive decrease in the G1 cell population ^[1]. It induces a significant increase in apoptosis in MG63 cells in a concentration- and time-dependent manner ^[4].

In vivo, oral doses of berberine hydrochloride at 30 and 50 mg/kg/day inhibited the growth of human colorectal adenocarcinoma xenografts in nude mice by 33.1% and 45.3%,respectively^[1].Berberine hydrochloride alleviates lipopolysaccharide-induced mouse enteritis by inhibiting the activation of the NF-κB signaling pathway ^[5].

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.
[2] Md. Reyad-ul F, et al. Berberine chloride (dual topoisomerase I and II inhibitor) modulate mitochondrial uncoupling protein (UCP1) in molecular docking and dynamic with in-vitro cytotoxic and mitochondrial ATP production.Journal of Biomolecular Structure and Dynamics. 2022 May;41: 1704-1714.
[3] J Yin, J Ye, W Jia, et al. Effects and mechanisms of berberine in diabetes treatment[J]. Acta Pharmaceutica Sinica B, 2012.
[4] Zhu Y , Ma N , Li H X ,et al.Berberine induces apoptosis and DNA damage in MG-63 human osteosarcoma cells[J].Molecular Medicine Reports, 2014, 10(4).
[5] Fu K , Lv X , Li W ,et al.Berberine hydrochloride attenuates lipopolysaccharide-induced endometritis in mice by suppressing activation of NF-kB signal pathway[J].INTERNATIONAL IMMUNOPHARMACOLOGY, 2015.

盐酸小檗碱是来源于毛茛科药用植物黄连的一种异喹啉类生物碱，具有广泛的药理功能，在癌症、炎症、糖尿病、抑郁症、高血压和各种感染领域中具有应用。盐酸小檗碱能够诱导癌细胞中的氧化DNA损伤^[1]。盐酸小檗碱是拓扑异构酶I和II的双效抑制剂，也是一个潜在的自噬调节剂^[2]。由于盐酸小檗碱对AMPK具有激活作用，它能够改善胰岛素敏感性和降低血糖水平^[3]。

在体外，盐酸小檗碱 (1.25-160 μM；72 hours) 对四种结直肠癌细胞系 LoVo、HCT116、SW480 和 HT-29 的增殖具有潜在的抑制作用，IC₅₀范围为 40.8±4.1 μM (LoVo) 至 98.6±2.9 μM (HCT116) ^[1]。盐酸小檗碱（40.0 μM）能诱导G2/M期细胞周期停滞，G2/M期细胞群增加，G1期细胞群进行性下降^[1]。盐酸小檗碱以浓度和时间依赖性方式诱导 MG63 细胞凋亡显着增加^[4]。

在体内，胃肠道灌胃剂量为30和50 mg/kg/day 的盐酸小檗碱对人结直肠腺癌裸鼠异种移植物生长的抑制率分别为 33.1% 和 45.3%^[1]。盐酸小檗碱通过抑制NF-κB信号通路活化减轻脂多糖诱导的小鼠肠炎^[5]。