Berberine chloride (Synonyms: 鹽酸小檗jian; Natural Yellow 18 chloride)
Berberine chloride 是一種生物堿，常用作抗生su。Berberine chloride 誘導(dǎo)活性氧 (ROS) 生成并抑制 DNA 拓?fù)洚悩?gòu)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
體外研究(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). |
體內(nèi)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
性狀：Solid
Formula：C20H18ClNO4
CAS 號：633-65-8
中文名稱：鹽酸小檗jian；鹽酸黃連su；鹽酸黃蓮素
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式：
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性數(shù)據(jù)
DMSO : 12.5 mg/mL (33.62 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic) (insoluble)
| 濃度溶劑體積質(zhì)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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時(shí)，請?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 0.5% CMC-Na/saline water
Solubility: 11 mg/mL (29.59 mM); Suspended solution; Need ultrasonic
- 2.
請依序添加每種溶劑： PBS
Solubility: 10 mg/mL (26.90 mM); Suspended solution; Need ultrasonic
- 3.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (3.36 mM); Clear solution
- 4.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (3.36 mM); Clear solution
參考文獻(xiàn)
[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：產(chǎn)品僅用于科研
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