Berberine chloride (Synonyms: 盐酸小檗jian; Natural Yellow 18 chloride)
Berberine chloride 是一种生物碱，常用作抗生su。Berberine chloride 诱导活性氧 (ROS) 生成并抑制 DNA 拓扑异构酶 (topoisomerase)。
生物活性
Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
IC50 & Target
体外研究(In Vitro)
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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
| Cell Line: | Four colorectal carcinoma cell lines LoVo, HCT116, SW480, and HT-29 |
| Concentration: | 1.25, 2.5, 5, 10, 20, 40, 80, and 160 μM |
| Incubation Time: | 72 hours |
| Result: | Inhibited the proliferation of four cell lines. The IC50 ranged from 40.8±4.1 μM (LoVo) to 98.6±2.9 μM (HCT116). |
体内研究(In Vivo)
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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 5-week-old BALB/c nu/nu mice with human colorectal adenocarcinoma LoVo xenografts[1] |
| Dosage: | 10, 30, or 50 mg/kg/day |
| Administration: | Gastrointestinal gavage; for 10 consecutive days |
| Result: | Showed inhibitory rates of 33.1 % and 45.3 % at doses of 30 and 50 mg/kg/day. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03609892 | Xijing Hospital of Digestive Diseases | August 1, 2018 | Phase 4 | |
| NCT02226185 | Shanghai Jiao Tong University School of Medicine | November 2014 | Phase 2|Phase 3 | |
| NCT03378934 | Peking Union Medical College Hospital | September 26, 2018 | Phase 4 |
分子量：371.81
性状：Solid
Formula：C20H18ClNO4
CAS 号：633-65-8
中文名称：盐酸小檗jian；盐酸黄连su；盐酸黄莲素
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
DMSO : 12.5 mg/mL (33.62 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic) (insoluble)
| 浓度溶剂体积质量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6895 mL | 13.4477 mL | 26.8955 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3791 mL |
| 10 mM | 0.2690 mL | 1.3448 mL | 2.6895 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
- 1.
请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 11 mg/mL (29.59 mM); Suspended solution; Need ultrasonic
- 2.
请依序添加每种溶剂： PBS
Solubility: 10 mg/mL (26.90 mM); Suspended solution; Need ultrasonic
- 3.
请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (3.36 mM); Clear solution
- 4.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (3.36 mM); Clear solution
参考文献
[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. [Content Brief]
注：产品仅用于科研
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