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

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 a...

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Published inInternational immunopharmacology Vol. 43; p. 195
Main Authors Feng, Min, Zou, Zongyao, Zhou, Xia, Hu, Yinran, Ma, Hang, Xiao, Yubo, Li, Xuegang, Ye, Xiaoli
Format Journal Article
LanguageEnglish
Published Amsterdam Elsevier BV 01.02.2017
Subjects
Antiinfectives and antibacterials
Aorta
Apolipoprotein E
Arteriosclerosis
Atherosclerosis
Berberine
Bioactive compounds
Bioavailability
Biocompatibility
Biological activity
Cytokines
Cytosol
Dosage
Hamsters
In vivo methods and tests
Inflammation
Intercellular adhesion molecule 1
Interleukin 6
Mice
Microorganisms
mRNA
Nitric-oxide synthase
Nuclei
Pharmacology
Redox properties
Serum levels
Synaptotagmin
Translocation
Tumor necrosis factor
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Summary: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 12 weeks 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.
ISSN:1567-5769
1878-1705