title: Comparative effect of berberine and its derivative 8-cetylberberine on attenuating atherosclerosis in ApoE-/-mice.
abstract: 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.
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China; Chongqing Key Lab of Catalysis & Functional Organic Molecules, College of Environment and Resource, Chongqing Technology and Business University, Chongqing 400067, PR China.
authors.forename: Min
authors.initials: M
authors.lastname: Feng
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China; Engineer Research Center of Chongqing Pharmaceutical Process and Quality Control, Chongqing, 401122, PR China.
authors.forename: Zongyao
authors.initials: Z
authors.lastname: Zou
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China; Engineer Research Center of Chongqing Pharmaceutical Process and Quality Control, Chongqing, 401122, PR China.
authors.forename: Xia
authors.initials: X
authors.lastname: Zhou
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China.
authors.forename: Yinran
authors.initials: Y
authors.lastname: Hu
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China.
authors.forename: Hang
authors.initials: H
authors.lastname: Ma
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China.
authors.forename: Yubo
authors.initials: Y
authors.lastname: Xiao
authors.affiliation: School of Pharmaceutical Sciences, Southwest University, Chongqing, 400715, PR China; Engineer Research Center of Chongqing Pharmaceutical Process and Quality Control, Chongqing, 401122, PR China. Electronic address: Xuegangli@swu.edu.cn.
authors.forename: Xuegang
authors.initials: X
authors.lastname: Li
authors.affiliation: Engineer Research Center of Chongqing Pharmaceutical Process and Quality Control, Chongqing, 401122, PR China. Electronic address: yexiaoli@swu.edu.cn.
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Ye
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000627:therapeutic use*; D000975:Antioxidants / Q000627:therapeutic use*; D001011:Aorta / Q000187:drug effects* / Q000473:pathology; D001057:Apolipoproteins E / Q000235:genetics; D050197:Atherosclerosis / Q000188:drug therapy*; D001599:Berberine / Q000031:analogs & derivatives* / Q000627:therapeutic use*; D002467:Cell Nucleus / Q000378:metabolism*; D000089042:Coptis chinensis; D006224:Cricetinae; D016207:Cytokines / Q000378:metabolism; D004195:Disease Models, Animal; D004365:Drugs, Chinese Herbal; D006801:Humans; D018836:Inflammation Mediators / Q000378:metabolism; D051379:Mice; D008810:Mice, Inbred C57BL; D018345:Mice, Knockout; D016328:NF-kappa B / Q000378:metabolism*; D052247:Nitric Oxide Synthase Type II / Q000235:genetics / Q000378:metabolism; D021381:Protein Transport
chemical_list: C000604411:8-cetylberberine; D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D001057:Apolipoproteins E; D016207:Cytokines; D004365:Drugs, Chinese Herbal; D018836:Inflammation Mediators; D016328:NF-kappa B; D001599:Berberine; C107393:Coptidis rhizoma extract; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse
keywords: 8-cetylberberine; Anti-inflammatory; Antioxidant; Atherosclerosis; Berberine