ChemicalBook CAS DataBase List 68030-18-2

68030-18-2

Name	Berberine (chloride hydrate)
CAS	68030-18-2
Molecular Formula	C20H20ClNO5
Molecular Weight	389.83
MOL File	68030-18-2.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO: ≥ 3.9 mg/mL (10.00 mM); Water: 1.25 mg/mL (3.21 mM)
form	Solid
color	Light yellow to yellow

Hazard Information

Uses

Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid that acts as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].

Biological Activity

Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid isolated from Chinese herbal medicine Coptis chinensis and is commonly used as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase.

in vitro

Berberine chloride hydrate ( Natural Yellow 18 chloride hydrate; 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.
Berberine chloride hydrate (1.25-160 μM; 24-72 hours) induces a time- and dose-dependent inhibition of LoVo cell growth.
LoVo cells are exposure to Berberine chloride hydrate (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.
Berberine chloride hydrate (10-80 μM) suppresses cyclin B1, cdc2 and cdc25c protein expression after 24 h, especially at the dose of 80.0 μM.

Cell Proliferation Assay

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: < /td>	Inhibited the proliferation of four cell lines. The IC ₅₀ ranged from 40.8±4.1 μM (LoVo) to 98.6±2.9 μM (HCT116).

Cell Proliferation Assay

Cell Line:	Colorectal carcinoma cell lines LoVo
Concentration:	1.25, 2.5, 5, 10, 20, 40, 80, and 160 μM
Incubation Time:	24, 48, 72 hours
Result:	Induced a time- and dose-dependent inhibition of cell growth. By 72 h, 160.0 μM induced 71.1±1.9 % growth inh ibitions in LoVo cells.

Cell Cycle Analysis

Cell Line:	LoVo cells
Concentration:	0, 10, 20, 40, or 80 μM
Incubation Time:	24 hours
Result:	Exposure to 40.0 μM induced G2/M-phase cell cycle arrest, an increase in the G2/M-phase population and a progressive decline in the G1 population.

Western Blot Analysis

< /tr>

Cell Line:	LoVo cells
Concentration:	10, 20, 40, or 80 μM
Incubation Time:	24 hours
Result:	Suppressed cyclin B1, cdc2 and cdc25c protein expression.

in vivo

Berberine chloride hydrate (Natural Yellow 18 chloride hydrate; 10, 30, or 50 mg/kg/day; gastrointestinal gavage; for 10 consecutive days) inhibits the growth of human colorectal adenocarcinoma in vivo. Berberine chloride hydrate 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.

Animal Model: < /td>	5-week-old BALB/c nu/nu mice with human colorectal adenocarcinoma LoVo xenografts
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.

target

ROS
DNA topoisomerase

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. DOI:10.1007/s11418-013-0766-z

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