Aim To investigate the effect in berberine chloride （BER） on experimental ulcerative colitis in mice. Methods BALB/C mice in 6 groups were allowed to drink either 4% dextran sulfate sodium （DSS） solution or distil...Aim To investigate the effect in berberine chloride （BER） on experimental ulcerative colitis in mice. Methods BALB/C mice in 6 groups were allowed to drink either 4% dextran sulfate sodium （DSS） solution or distilled water freely with different doses of BER （15 mg·kg^-1, 45 mg·kg^-1, 150 mg·kg^-1） or sallcylazosulfapyridine （SASP, 520 mg·kg^-1）, and solvent （0. 2 mL/10 mg Wt） once a day for 7 d, respectively. The symptom of ulcerative colitis was evaluated by disease activity index （DAI）. Myeloperoxidase （MPO） and superoxide dismutase （SOD） activities and malondialdehyde （MDA） content were determined by HE staining and immunohistochemistry of expressions of NF-κB p65 and intercellular adhesion molecule 1 （ ICAM-1 ） proteins to observe the damage to colon tissues and possible mechanisms. Results DAI, MPO activity, MDA content and expressions of ICAM-1 and NF-κB p65 were markedly increased, while SOD activity decreased in DSS-treated mice. Treatment of mice with different doses of BER or SASP significantly decreased DAI, MPO activity and MDA content, improved histological changes of colon tissues, blunted the expressions of NF-κB p65 and ICAM-1 proteins, and enhanced SOD activity. Conclusion Berberine chloride has excellent therapeutic effect on ulcerative colitis caused by DSS in mice. The possible mechanism may be related to its antioxidant and anti-inflammatory activities associated with inhibiting the NF-κB activation and ICAM-1 expression.展开更多
Berberine hydrochloride is commonly used to treat bacterial dysentery,gastroenteritis and other diseases.Many manufacturers are available on the market today,while the production process and formulation are quite diff...Berberine hydrochloride is commonly used to treat bacterial dysentery,gastroenteritis and other diseases.Many manufacturers are available on the market today,while the production process and formulation are quite different,which may directly affect the therapeutic effect of the drug.To this end,11 different production producers of berberine hydrochloride tablets were collected according to the pharmacopeia berberine hydrochloride dissolution method(basket method).In addition the dissolution process was carried out in four elution media with different pH,and the difference was similar(f2).Factors were calculated to evaluate in vitro dissolution requirements,and in vitro dissolution of different manufacturers of berberine hydrochloride tablets was determined by high performance liquid chromatography(HPLC).The method was verified by linearity,precision,stability and robustness.Based on the f2 value,there was a significant difference in the dissolution behavior of the formulations of most berberine hydrochloride tablet brands.This research provided the basis for further in-depth research in the later period.Although the drug specifications(0.1 g)were the same,the dissolution curve was different.This phenomenon may be attributed to the fact that the excipients and crystal form of the tablets affected the release and dissolution of the tablets in vitro.展开更多
基金AProject of the Health Bureau of Chongqing (No.2004-B-31)
文摘Aim To investigate the effect in berberine chloride （BER） on experimental ulcerative colitis in mice. Methods BALB/C mice in 6 groups were allowed to drink either 4% dextran sulfate sodium （DSS） solution or distilled water freely with different doses of BER （15 mg·kg^-1, 45 mg·kg^-1, 150 mg·kg^-1） or sallcylazosulfapyridine （SASP, 520 mg·kg^-1）, and solvent （0. 2 mL/10 mg Wt） once a day for 7 d, respectively. The symptom of ulcerative colitis was evaluated by disease activity index （DAI）. Myeloperoxidase （MPO） and superoxide dismutase （SOD） activities and malondialdehyde （MDA） content were determined by HE staining and immunohistochemistry of expressions of NF-κB p65 and intercellular adhesion molecule 1 （ ICAM-1 ） proteins to observe the damage to colon tissues and possible mechanisms. Results DAI, MPO activity, MDA content and expressions of ICAM-1 and NF-κB p65 were markedly increased, while SOD activity decreased in DSS-treated mice. Treatment of mice with different doses of BER or SASP significantly decreased DAI, MPO activity and MDA content, improved histological changes of colon tissues, blunted the expressions of NF-κB p65 and ICAM-1 proteins, and enhanced SOD activity. Conclusion Berberine chloride has excellent therapeutic effect on ulcerative colitis caused by DSS in mice. The possible mechanism may be related to its antioxidant and anti-inflammatory activities associated with inhibiting the NF-κB activation and ICAM-1 expression.
基金National Institutes for Food and Drug Control(Grant No.017ZX09101001).
文摘Berberine hydrochloride is commonly used to treat bacterial dysentery,gastroenteritis and other diseases.Many manufacturers are available on the market today,while the production process and formulation are quite different,which may directly affect the therapeutic effect of the drug.To this end,11 different production producers of berberine hydrochloride tablets were collected according to the pharmacopeia berberine hydrochloride dissolution method(basket method).In addition the dissolution process was carried out in four elution media with different pH,and the difference was similar(f2).Factors were calculated to evaluate in vitro dissolution requirements,and in vitro dissolution of different manufacturers of berberine hydrochloride tablets was determined by high performance liquid chromatography(HPLC).The method was verified by linearity,precision,stability and robustness.Based on the f2 value,there was a significant difference in the dissolution behavior of the formulations of most berberine hydrochloride tablet brands.This research provided the basis for further in-depth research in the later period.Although the drug specifications(0.1 g)were the same,the dissolution curve was different.This phenomenon may be attributed to the fact that the excipients and crystal form of the tablets affected the release and dissolution of the tablets in vitro.
