Berberine hydrochloride
(Synonyms: 盐酸小檗碱; Natural Yellow 18 chloride) 目录号 : GN10208
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，具有抗肿瘤、抗炎、降血糖等多种药理活性。
Cas No.:633-65-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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]。
|
Cell experiment [1]: |
|
|
Cell lines |
Four colorectal carcinoma cell lines LoVo, HCT116, SW480, and HT-29 |
|
Preparation method |
Cells were treated with 0-160 μM berberine for 72 hours or for different time periods (24-72 hours). Add water-soluble tetrazolium salt (WST-1) and continue incubation for another 4 hours. Then use a microplate reader to read the OD value at a test wavelength of 440 nm and a reference wavelength of 620 nm. |
|
Reaction Conditions |
0-160 μM; 24-72 hours |
|
Applications |
Inhibited the proliferation of four cell lines. The IC50 ranged from 40.8±4.1 μM (LoVo) to 98.6±2.9 μM (HCT116). |
|
Cell experiment [2]: |
|
|
Cell lines |
MG-63 human osteosarcoma cell line (wild type) |
|
Preparation method |
MG-63 cells were seeded at a density of 1x104cells//well in 100 μl of cell culture medium and then placed in a 96-well plate. Followi ng 12 h of incubation, the cells were treated with 0, 20, 40, 80 μM berberi ine for 12 and 24 h. |
|
Reaction Conditions |
0, 20, 40, 80 μM; 12 and 24 h |
|
Applications |
Berberine induced a significant increase in apoptosis in MG63 cells in a concentration and timedependent manner. |
|
Animal experiment [1]: |
|
|
Animal models |
BALB/c nu/nu mice |
|
Preparation method |
Fragments (6-8 mm) of colorectal adenocarcinoma were implanted subcutaneously. in the flank of 5-week-old BALB/c nu/nu mice. Tumors were allowed to develop for 2 weeks. Once tumors were established, mice were randomly divided into five groups. The berberine treatment group (10 animals in each group) was given 10, 30 or 50 mg/kg berberine by gastrointestinal gavage for 10 consecutive days. |
|
Dosage form |
10, 30, or 50 mg/kg/day; Gastrointestinal gavage; for 10 consecutive days |
|
Applications |
Showed inhibitory rates of 33.1 % and 45.3 % at doses of 30 and 50 mg/kg/day. |
|
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]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). |
|
| Cas No. | 633-65-8 | SDF | |
| 别名 | 盐酸小檗碱; Natural Yellow 18 chloride | ||
| 化学名 | 9,10-dimethoxy-5,6-dihydro-[1,3]dioxolo[4,5-g]isoquinolino[3,2-a]isoquinolin-7-ium chloride | ||
| Canonical SMILES | [H]C(C([H])([H])C1=C2[H])([H])[N+](C([H])=C(C(OC([H])([H])[H])=C3OC([H])([H])[H])C(C([H])=C3[H])=C4[H])=C4C1=C([H])C5=C2OC([H])([H])O5.[Cl-] | ||
| 分子式 | C20H18ClNO4 | 分子量 | 371.81 |
| 溶解度 | ≥ 18.6mg/mL in DMSO with gentle warming | 储存条件 | Store at 2-8°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 | 0.269 mL | 1.3448 mL | 2.6895 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet