Comparative pharmacokinetics of bergenin, a main active constituent of Saxifraga stolonifera Curt., in normal and hepatic injury rats after oral administration

Pan, Ronghua; He, Hongmei; Dai, Yue; Xia, Yufeng

doi:10.1016/s1875-5364(16)30092-9

Cited by 4 publications

(1 citation statement)

References 25 publications

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“…Pan et al. ( 2016 ) have reported that the plasma C max values of bergenin in rats treated with an oral dose (100 mg/kg) were less than 300 ng/mL (0.9 μM). Therefore, the rat plasma concentrations of bergenin were much lower than the K i and IC 50 values of bergenin determined in this study, and severe drug–drug interaction might not occur if bergenin were co-administered with the substrates of the CYP3A4, 2E1 and 2C9.…”

Section: Discussionmentioning

confidence: 99%

In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes

Dong

Zhou

Song

2018

Pharmaceutical Biology

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Context: Bergenin, isolated from the herb of Bergenia purpurascens (Hook. f. et Thoms.) Engl., has anti-inflammatory, antitussive, and wound healing activities. However, whether bergenin affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear.Materials and methods: In this study, the inhibitory effects of bergenin (100 μM) on the eight human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19 and 2C8) were investigated, enzyme kinetics and time-dependent inhibition studies were also performed in vitro using human liver microsomes (HLMs).Results: The results showed that bergenin inhibited the activity of CYP3A4, 2E1 and 2C9, with IC50 values of 14.39, 22.83 and 15.11 μM, respectively, but other CYP isoforms were not affected. Enzyme kinetic studies showed that bergenin was not only a non-competitive inhibitor of CYP3A4, but also a competitive inhibitor of CYP2E1 and 2C9, with Ki values of 7.71, 11.39 and 8.89 μM, respectively. In addition, bergenin is a time-dependent inhibitor for CYP3A4 with Kinact/KI value of 0.025/3.50 μM−1 min−1.Discussion and conclusions: The in vitro studies of bergenin with CYP isoforms indicate that bergenin has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP3A4, 2E1 and 2C9. Further clinical studies are needed to evaluate the significance of this interaction.

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Section: Discussionmentioning

confidence: 99%

In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes

Dong

Zhou

Song

2018

Pharmaceutical Biology

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Bergenia ciliata as a future candidate for liver diseases: a concise review

Latief

Tung

Singh

et al. 2022

JoBAZ

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Liver cirrhosis, alcoholic liver diseases, non-alcoholic fatty liver and steatohepatitis are the major risk factors for liver damage leading to hepatocellular carcinoma. Oxidative stress and insulin resistance are the main pathogenetic mechanisms leading the hepatic cell injury and damage in these patients. The present review is the first attempt which focuses on the biological activities of Bergenia ciliata to explore its benefits and possible applications in the treatment of liver ailments. Bergenia ciliata is an evergreen herb belonging to the family saxifragaceae and is regarded as a miracle herb due to its wide medicinal applications. The data published in India and other nations are methodically reviewed and summarized in this article. It covers the facts collected from scientific journals, theses and online bibliographical databases: PubMed, Scopus, Google Scholar and Web of Science from year 1995–2020. The phytochemical studies on B. ciliata have shown the presence of many phytochemicals belonging to phenols, flavonoids, fatty acid, glycosides, terpenoids, etc. Due to the presence of a multitude of these bioactives, the whole plant of B. ciliata has numerous medicinal applications such as diuretic, antipyretic, α-glucosidase, antiviral, antibacterial, anti-inflammatory and insecticidal activity. Therefore in the present study, we invite the attention of scientists and researchers to carry out further clinical and toxicological studies on this valuable plant in order to discover and develop novel hepatoprotective medicine with fewer side effects on human beings.

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Bergenin - A Biologically Active Scaffold: Nanotechnological Perspectives

Madaan

Singla

Kumar

et al. 2022

CTMC

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: Bergenin, 4-O-methyl gallic acid glucoside, is a bioactive compound present in various plants belonging to different families. The present work compiles scattered information on pharmacology, structure activity relationship and nanotechnological aspects of bergenin, collected from various electronic databases such as Sci Finder, PubMed, Google scholar, etc. Bergenin has been reported to exhibit hepatoprotective, anti-inflammatory, anticancer, neuroprotective, antiviral and antimicrobial activities. Molecular docking studies have shown that isocoumarin pharmacophore of bergenin is essential for its bioactivities. Bergenin holds a great potential to be used as lead molecule and also as a therapeutic agent for development of more efficacious and safer semisynthetic derivatives. Nanotechnological concepts can be employed to overcome poor bioavailability of bergenin. Finally, it is concluded that bergenin can be emerged as clinically potential medicine in modern therapeutics.

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Comparative pharmacokinetics of bergenin, a main active constituent of Saxifraga stolonifera Curt., in normal and hepatic injury rats after oral administration

Cited by 4 publications

References 25 publications

In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes

In vitro inhibitory effects of bergenin on human liver cytochrome P450 enzymes

Bergenia ciliata as a future candidate for liver diseases: a concise review

Bergenin - A Biologically Active Scaffold: Nanotechnological Perspectives

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