Multifunctional epiberberine mediates multi-therapeutic effects

Liu, Linqiu; Li, Junjun; He, Yang

doi:10.1016/j.fitote.2020.104771

Cited by 26 publications

(15 citation statements)

References 79 publications

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“…et al, 2020 ). Meanwhile, epiberberine also inhibits telomerase by disrupting telomere maintenance and capping to induce cell apoptosis ( Liu L. et al, 2020 ). Furthermore, epiberberine induces low expression of Bcl-2 and the X-linked inhibitor of apoptosis protein (XIAP), the high expression of Bax, p53 and release of cytochrome C, and the activation of Caspase-3 to promote gastric cancer cell apoptosis ( Liu L. et al, 2020 ).…”

Section: Antitumor Effects and Corresponding Mechanismsmentioning

confidence: 99%

“…Meanwhile, epiberberine also inhibits telomerase by disrupting telomere maintenance and capping to induce cell apoptosis ( Liu L. et al, 2020 ). Furthermore, epiberberine induces low expression of Bcl-2 and the X-linked inhibitor of apoptosis protein (XIAP), the high expression of Bax, p53 and release of cytochrome C, and the activation of Caspase-3 to promote gastric cancer cell apoptosis ( Liu L. et al, 2020 ). Oxyepiberberine has been reported to inhibit proliferation of CRC LS-1034 cells both in vitro and in vivo , accompanied by inducing apoptosis and inhibiting migration and tubulin polymerization ( Ning et al, 2021 ).…”

Section: Antitumor Effects and Corresponding Mechanismsmentioning

confidence: 99%

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Current Advances in Coptidis Rhizoma for Gastrointestinal and Other Cancers

Chen

Liang

et al. 2022

Front. Pharmacol.

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Cancer is a serious disease with an increasing number of reported cases and high mortality worldwide. Gastrointestinal cancer defines a group of cancers in the digestive system, e.g., liver cancer, colorectal cancer, and gastric cancer. Coptidis Rhizoma (C. Rhizoma; Huanglian, in Chinese) is a classical Chinese medicinal botanical drug for the treatment of gastrointestinal disorders and has been shown to have a wide variety of pharmacological activity, including antifungal, antivirus, anticancer, antidiabetic, hypoglycemic, and cardioprotective effects. Recent studies on C. Rhizoma present significant progress on its anticancer effects and the corresponding mechanisms as well as its clinical applications. Herein, keywords related to C. Rhizoma, cancer, gastrointestinal cancer, and omics were searched in PubMed and the Web of Science databases, and more than three hundred recent publications were reviewed and discussed. C. Rhizoma extract along with its main components, berberine, palmatine, coptisine, magnoflorine, jatrorrhizine, epiberberine, oxyepiberberine, oxyberberine, dihydroberberine, columbamine, limonin, and derivatives, are reviewed. We describe novel and classic anticancer mechanisms from various perspectives of pharmacology, pharmaceutical chemistry, and pharmaceutics. Researchers have transformed the chemical structures and drug delivery systems of these components to obtain better efficacy and bioavailability of C. Rhizoma. Furthermore, C. Rhizoma in combination with other drugs and their clinical application are also summarized. Taken together, C. Rhizoma has broad prospects as a potential adjuvant candidate against cancers, making it reasonable to conduct additional preclinical studies and clinical trials in gastrointestinal cancer in the future.

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Section: Antitumor Effects and Corresponding Mechanismsmentioning

confidence: 99%

Section: Antitumor Effects and Corresponding Mechanismsmentioning

confidence: 99%

Current Advances in Coptidis Rhizoma for Gastrointestinal and Other Cancers

Chen

Liang

et al. 2022

Front. Pharmacol.

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“…In addition, berberine from C. chinensis was shown to alleviate fibrosis by suppressing HIF-1 α activation ( Hu et al, 2018 ). Furthermore, epiberberine extracted from C. chinensis and the water extract of C. fraxini were shown to regulate AKT and ERK pathways ( Li et al, 2015b ; Liu et al, 2020 ), with phellodendronoside A from P. chinense inhibiting the activation of ERK and p38MAPK ( Si et al, 2021 ). Thus, targeting the AKT-mTOR signaling pathway, especially PKCs and ERK1/2, might be a potential therapeutic approach in the treatment of CD fibrosis.…”

Section: Discussionmentioning

confidence: 99%

Network Pharmacology-Based Strategy to Identify the Pharmacological Mechanisms of Pulsatilla Decoction against Crohn’s Disease

et al. 2022

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Purpose: To explore pharmacological mechanisms of Pulsatilla decoction (PD) against Crohn’s disease (CD) via network pharmacology analysis followed by experimental validation.Methods: Public databases were searched to identify bioactive compounds and related targets of PD as well as related genes in patients with CD. Analyses using the drug–compound–target–disease network, the protein–protein interaction (PPI) network, and Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed to predict the core targets and pathways of PD against CD. Colon tissue resected from patients with CD and tissue samples from a mouse model of CD fibrosis treated with PD were assessed to verify the major targets of PD in CD predicted by network pharmacologic analysis.Results: A search of the targets of bioactive compounds in PD and targets in CD identified 134 intersection targets. The target HSP90AA1, which was common to the drug–compound–target–disease and PPI networks, was used to simulate molecular docking with the corresponding bioactive compound. GO and KEGG enrichment analyses showed that multiple targets in the antifibrotic pathway were enriched and could be experimentally validated in CD patients and in a mouse model of CD fibrosis. Assays of colon tissues from CD patients showed that intestinal fibrosis was greater in stenoses than in nonstenoses, with upregulation of p-AKT, AKT, p-mTOR, mTOR, p-ERK1/2, ERK1/2, p-PKC, and PKC targets. Treatment of CD fibrosis mice with PD reduced the degree of fibrosis, with downregulation of the p-AKT, AKT, p-mTOR, mTOR, p-ERK1/2, ERK1/2, and PKC targets.Conclusion: Network pharmacology analysis was able to predict bioactive compounds in PD and their potential targets in CD. Several of these targets were validated experimentally, providing insight into the pharmacological mechanisms underlying the biological activities of PD in patients with CD.

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“…Berberrubine is deemed as one of the major active metabolites of berberine; berberrubine exerted multiple activities, including anti-inflammation, antimicrobial, lipid-lowering, and antioxidation [35]. Epiberberine has antiadipogenesis, antidyslipidemia, and other effects [9]. Based on the analysis of network, the key targets of DRD2, SLC6A4, CDK2, DPP4, ESR1, AKT2, AKT1, and PGR were selected.…”

Section: Discussionmentioning

confidence: 99%

“…It has been reported that the extracts and compounds of RC have the effects of improving insulin resistance and regulating glycolipid metabolism, antiobesity, and myocardial protection. And they have potential therapeutic effects on many kinds of diseases, for instance, PCOS, diabetes, obesity, hyperlipidemia, and cardiovascular disease [ 9 – 11 ]. But the potential molecular mechanism of RC has not been entirely elucidated.…”

Section: Introductionmentioning

confidence: 99%

The Potential Effect of Rhizoma coptidis on Polycystic Ovary Syndrome Based on Network Pharmacology and Molecular Docking

Duan

Jin

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Background. Rhizoma coptidis (RC) showed a significant effect on PCOS, but its mechanism in PCOS remains unclear. Methods. The components of RC were searched by TCMSP. The Smiles number of the active ingredients was queried through PubChem, and the predicted targets were obtained from the SwissTargetPrediction database. The DrugBank, GeneCards, and DisGeNET databases were retrieved to acquire the related targets of PCOS. Then, the network of compound-target was constructed. The core targets were analyzed using protein-protein interaction (PPI) analysis, and the binding activities were verified by molecular docking. The enriched pathways of key targets were examined by GO and KEGG. Results. 13 components and 250 targets of RC on PCOS were screened. The core network was filtered based on topological parameters, and the key components were palmatine, berberine, berberrubine, quercetin, and epiberberine. The key targets included DRD2, SLC6A4, CDK2, DPP4, ESR1, AKT2, PGR, and AKT1. Molecular docking displayed that the active ingredients of RC had good binding activities with potential targets of PCOS. After enrichment analysis, 30 functional pathways were obtained, including neuroactive ligand-receptor interaction, dopaminergic synapse, and cAMP signaling pathway. Conclusion. In summary, this study clarified the potential effect of RC on PCOS, which is helpful to provide references for clinical practice. It is also conducive to the secondary development of RC and its monomer components.

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Multifunctional epiberberine mediates multi-therapeutic effects

Cited by 26 publications

References 79 publications

Current Advances in Coptidis Rhizoma for Gastrointestinal and Other Cancers

Current Advances in Coptidis Rhizoma for Gastrointestinal and Other Cancers

Network Pharmacology-Based Strategy to Identify the Pharmacological Mechanisms of Pulsatilla Decoction against Crohn’s Disease

The Potential Effect of Rhizoma coptidis on Polycystic Ovary Syndrome Based on Network Pharmacology and Molecular Docking

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