Comparative effect of berberine and its derivative 8-cetylberberine on attenuating atherosclerosis in ApoE−/− mice

• Published in: International immunopharmacology Vol. 43; pp. 195 - 202
• Main Authors: Feng, Min, Zou, Zongyao, Zhou, Xia, Hu, Yinran, Ma, Hang, Xiao, Yubo, Li, Xuegang, Ye, Xiaoli
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.02.2017
• Subjects: 8-cetylberberine; Animals; Anti-inflammatory; Anti-Inflammatory Agents - therapeutic use; Antioxidant; Antioxidants - therapeutic use; Aorta - drug effects; Aorta - pathology; Apolipoproteins E - genetics; Atherosclerosis; Atherosclerosis - drug therapy; Berberine; Berberine - analogs & derivatives; Berberine - therapeutic use; Cell Nucleus - metabolism; Cricetinae; Cytokines - metabolism; Disease Models, Animal; Drugs, Chinese Herbal; Humans; Inflammation Mediators - metabolism; Mice; Mice, Inbred C57BL; Mice, Knockout; NF-kappa B - metabolism; Nitric Oxide Synthase Type II - genetics; Nitric Oxide Synthase Type II - metabolism; Protein Transport; Berberine; 8-cetylberberine; Antioxidant; Anti-inflammatory; Atherosclerosis
• ISSN: 1567-5769; 1878-1705
• DOI: 10.1016/j.intimp.2016.12.001

Berberine (BBR), one of the main bioactive compounds in Rhizoma coptidis, has multiple pharmacological activities. It has been reported that 8-cetylberberine (8-BBR-C16) has increased anti-microbial property in vivo and a higher bioavailability in hamsters. Therefore, in the present study, we used apolipoprotein E-deficient mice (ApoE−/−) as an atherosclerosis model to investigate the anti-atherosclerosis effects of 8-BBR-C16. After 12weeks of treatment, the atherosclerotic plaque area of the aorta, serum lipid profile, the plasma redox state and the expression of inflammatory cytokines in ApoE−/− mice were determined. Both BBR and 8-BBR-C16 significantly decreased the atherosclerotic plaque area by suppressing inflammatory and oxidative markers in ApoE−/− mice. Treatment with BBR or 8-BBR-C16, decreased serum levels of IL-1β and TNF-α as well as mRNA levels of NF-κBp65, i-NOS, ICAM-1, IL-6 in the aorta. In addition, the expression of NF-κB p65 protein decreased in the nucleus, whereas IκBα levels increased in the cytosol. The anti-inflammatory and anti-oxidative effect of BBR and 8-BBR-C16 attributed to inhibition of the translocation of NF-κB to the nucleus. Since the dosage of BBR used was 10 fold higher than that of 8-cetylberberine, we conclude that 8-BBR-C16 is more efficient in treating atherosclerosis in ApoE−/− mice. •Both BBR and 8-BBR-C16 have potential anti-atherosclerosis effects in WT diet induced ApoE−/− mice.•Both BBR and 8-BBR-C16 inhibit oxidation and inflammation cytokine expressions.•BBR and 8-BBR-C16 inhibit the translocation of NF-κB to the nucleus.•8-BBR-C16 is more efficient in treating atherosclerosis in ApoE−/− mice than BBR.