Hepatoprotective properties and biotransformation of berberine and berberrubine by cell suspension cultures of Dodonaea viscosa and Ocimum basilicum

El-Salam, Mohamed Abd; Mekky, Hattem; El-Naggar, El Motaz Bellah; Ghareeb, Doaa A.; El-Demellawy, Maha; El-Fiky, Fathy K.

doi:10.1016/j.sajb.2015.01.005

Cited by 33 publications

(14 citation statements)

References 10 publications

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“…In the current work, BB, the demethylation metabolite of BBR, was found to be more pharmacologically active than BBR in alleviating the DSS-induced colitis in mice, which was in concert with previous reports that BB possessed better hepatoprotective property [ 55 ] and OH scavenging activity [ 56 ] than BBR. These results suggested that the metabolite BB might contribute to the biological activities of BBR in vivo .…”

Section: Discussionsupporting

confidence: 89%

Berberrubine attenuates mucosal lesions and inflammation in dextran sodium sulfate-induced colitis in mice

Huang

et al. 2018

PLoS ONE

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Ulcerative colitis (UC) is a chronic relapsing disease without satisfactory treatments, in which intestinal inflammation and disrupted intestinal epithelial barrier are two main pathogeneses triggering UC. Berberrubine (BB) is deemed as one of the major active metabolite of berberine (BBR), a naturally-occurring isoquinoline alkaloid with appreciable anti-UC effect. This study aimed to comparatively investigate the therapeutic effects of BB and BBR on dextran sodium sulfate (DSS)-induced mouse colitis model, and explore the potential underlying mechanism. Results revealed that BB (20 mg/kg) produced a comparable therapeutic effect as BBR (50 mg/kg) and positive control sulfasalazine (200 mg/kg) by significantly reducing the disease activity index (DAI) with prolonged colon length and increased bodyweight as compared with the DSS group. BB treatment was shown to significantly ameliorate the DSS-induced colonic pathological alternations and decreased histological scores. In addition, BB markedly attenuated colonic inflammation by alleviating inflammatory cell infiltration and inhibiting myeloperoxidase (MPO) and cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10) productions in DSS mice. Furthermore, BB treatment substantially upregulated the expression of tight junction (TJ) proteins (zonula occludens-1, zonula occludens-2, claudin-1, occludin) and mRNA expression of mucins (mucin-1 and mucin-2), and decreased the Bax/Bcl-2 ratio. In summary, BB exerted similar effect to its analogue BBR and positive control in attenuating DSS-induced UC with much lower dosage and similar mechanism. The protective effect observed may be intimately associated with maintaining the integrity of the intestinal mucosal barrier and mitigating intestinal inflammation, which were mediated at least partially, via favorable modulation of TJ proteins and mucins and inhibition of inflammatory mediators productions in the colonic tissue. This is the first report to demonstrate that BB possesses pronounced anti-UC effect similar to BBR and sulfasalazine with much smaller dosage. BB might have the potential to be further developed into a promising therapeutic option in the treatment of UC.

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Section: Discussionsupporting

confidence: 89%

Berberrubine attenuates mucosal lesions and inflammation in dextran sodium sulfate-induced colitis in mice

Huang

et al. 2018

PLoS ONE

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“…Many studies have already demonstrated that the metabolites of berberine showed similar bio-activities to berberine [20,21,22]. For example, berberrubine exhibited hepatoprotective properties [23], hypolipidemic effects [24] and antitumor activities [25], etc. Demethyleneberberine showed hypolipidemic effects [26], hepatoprotective and anti-fibrotic effects [27], etc.…”

Section: Resultsmentioning

confidence: 99%

Rapid Identification of Berberine Metabolites in Rat Plasma by UHPLC-Q-TOF-MS

et al. 2019

Molecules

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In this study, a reliable and rapid method based on ultra high performance liquid chromatography combined with quadrupole time-of-flight tandem mass spectrometry (UHPLC-Q-TOF-MS) technology and MetabolitePilotMT software was developed for berberine metabolites identification in rat plasma. The chemical structures of the metabolites and their product ions were tentatively characterized or identified according to the molecular weights detected and MS/MS data. In all, nine metabolites, including M1 (demethyleneberberine, C19H18NO4, m/z 324), M2 (glucuronic acid-conjugated demethyleneberberine, C25H26NO10, m/z 500), M3 (diglucuronide-conjugated demethyleneberberine, C31H34NO16, m/z 676), M4 (glucuronic acid-conjugated jatrorrhizine or glucuronic acid-conjugated columbamine, C26H28NO10, m/z 514), M5 (berberrubine or thalifendine, C19H16NO4, m/z 322), M6 (glucuronic acid-conjugated berberrubine or glucuronic acid-conjugated thalifendine, C25H24NO10, m/z 498), M7 (sulfite-conjugated berberrubine or sulfite-conjugated thalifendine, C19H16NO7S, m/z 402), M8 (dihydroxy berberrubine or dihydroxy thalifendine, C19H16NO6, m/z 354) and M9 (dihydroxy berberine, C20H18NO6, m/z 368) were tentatively characterized or identified. Several new deposition patterns and three new metabolites (M7, M8 and M9) are reported in this paper for the first time. This work not only provides significant insights into the understanding of the metabolic pathways of berberine, but also contributes in identifying potential active drug candidates from the metabolites.

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“…A berberine-rich fraction (2.5 g) was obtained by using gradient elution with CHCl 3 : MeOH (9 : 1; 8 : 2) and finally methanol [ 35 ]. The presence of berberine in the fraction was identified using TLC, melting point [ 36 ], HPLC [ 27 ], and 1 H-NMR [ 37 ]. The obtained powder was dissolved in polyethylene glycol (20%) to be administrated to rats.…”

Section: Methodsmentioning

confidence: 99%

The Ameliorating Effect of Berberine-Rich Fraction against Gossypol-Induced Testicular Inflammation and Oxidative Stress

Saleh

Attia

Ghareeb

2018

Oxidative Medicine and Cellular Longevity

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This study was aimed at evaluating the efficacy of berberine-rich fraction (BF) as a protective and/or a therapeutic agent against inflammation and oxidative stress during male infertility. Sexually mature Sprague-Dawley male rats were divided into five groups treated with either corn oil, BF (100 mg/kg BW, orally, daily for 30 days), gossypol acetate (5 mg/kg BW, i.p.) eight times for 16 days, BF alone for 14 days then coadministered with gossypol acetate for the next 16 days (protected group), or gossypol acetate for 16 days then treated with BF for 30 days (treated group). All animals completed the experimental period (46 days) without obtaining any treatments in the gap period. Sperm parameters, oxidative index, and inflammatory markers were measured. Gossypol injection significantly decreased the semen quality and testosterone level that resulted from the elevation of testicular reactive oxygen and nitrogen species (TBARS and NO), TNF-α, TNF-α-converting enzyme, and interleukins (IL-1β, IL-6, and IL-18) by 230, 180, 12.5, 97.9, and 300%, respectively, while interleukin-12 and tissue inhibitors of metalloproteinases-3 were significantly decreased by 59 and 66%, respectively. BF (protected and treated groups) significantly improved the semen quality, oxidative stress, and inflammation associated with male infertility. It is suitable to use more advanced studies to validate these findings.

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Hepatoprotective properties and biotransformation of berberine and berberrubine by cell suspension cultures of Dodonaea viscosa and Ocimum basilicum

Cited by 33 publications

References 10 publications

Berberrubine attenuates mucosal lesions and inflammation in dextran sodium sulfate-induced colitis in mice

Berberrubine attenuates mucosal lesions and inflammation in dextran sodium sulfate-induced colitis in mice

Rapid Identification of Berberine Metabolites in Rat Plasma by UHPLC-Q-TOF-MS

The Ameliorating Effect of Berberine-Rich Fraction against Gossypol-Induced Testicular Inflammation and Oxidative Stress

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