An insight into the medicinal attributes of berberine derivatives: A review

Gaba, Sobhi; Saini, Anjali; Singh, Gurpreet; Monga, Vikramdeep

doi:10.1016/j.bmc.2021.116143

Cited by 74 publications

(56 citation statements)

References 119 publications

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“…Our previous studies reported that berberine could reduce ischemia/reperfusion-induced myocardial apoptosis, improve mesenteric artery insulin sensitivity in diabetes [ 26 ], and reduce diabetic myocardial damage by inhibiting IGF-1R signaling [ 13 ]. However, low bioavailability and an unidentified pharmacological mechanism are the main barriers to clinical application of berberine [ 27 ]. In addition to its pharmacological anti-diabetic roles in peripheral organs, it has been shown that berberine inhibits the function of disaccharide, promotes the release of GLP-1 to regulate metabolism, and modulates the component part of intestinal microbiota [ 28 ].…”

Section: Discussionmentioning

confidence: 99%

Berberine Decreases Intestinal GLUT2 Translocation and Reduces Intestinal Glucose Absorption in Mice

Zhang

Yang

et al. 2021

IJMS

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Postprandial hyperglycemia is an important causative factor of type 2 diabetes mellitus, and permanent localization of intestinal GLUT2 in the brush border membrane is an important reason of postprandial hyperglycemia. Berberine, a small molecule derived from Coptidis rhizome, has been found to be potent at lowering blood glucose, but how berberine lowers postprandial blood glucose is still elusive. Here, we investigated the effect of berberine on intestinal glucose transporter 2 (GLUT2) translocation and intestinal glucose absorption in type 2 diabetes mouse model. Type 2 diabetes was induced by feeding of a high-fat diet and injection of streptozotocin and diabetic mice were treated with berberine for 6 weeks. The effects of berberine on intestinal glucose transport and GLUT2 translocation were accessed in isolated intestines and intestinal epithelial cells (IEC-6), respectively. We found that berberine treatment improved glucose tolerance and systemic insulin sensitivity in diabetic mice. Furthermore, berberine decreased intestinal glucose transport and inhibited GLUT2 translocation from cytoplasm to brush border membrane in intestinal epithelial cells. Mechanistically, berberine inhibited intestinal insulin-like growth factor 1 (IGF-1R) phosphorylation and thus reduced localization of PLC-β2 in the membrane, leading to decreased GLUT2 translocation. These results suggest that berberine reduces intestinal glucose absorption through inhibiting IGF-1R-PLC-β2-GLUT2 signal pathway.

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Section: Discussionmentioning

confidence: 99%

Berberine Decreases Intestinal GLUT2 Translocation and Reduces Intestinal Glucose Absorption in Mice

Zhang

Yang

et al. 2021

IJMS

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“…For instance, to achieve therapeutic efficacy, berberine has to be used at relatively large oral doses in mice ( Turner et al, 2008 ), which limits the development and application of berberine as the pharmacological preparation. Therefore, the design and structural modification of these natural chemicals to get eligible derivatives with good pharmacological and pharmacokinetic profile are extremely important for the future development of mitochondrial targeting medicine ( Gaba et al, 2021 ). Recently, combination therapy is considered as a potential therapeutic option for the mitochondria-related liver disorders.…”

Section: Discussionmentioning

confidence: 99%

Mitochondrial Targeting Therapeutics: Promising Role of Natural Products in Non-alcoholic Fatty Liver Disease

Shen

Yuan

et al. 2021

Front. Pharmacol.

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Non-alcoholic fatty liver disease (NAFLD) has become one of the most common chronic liver diseases worldwide, and its prevalence is still growing rapidly. However, the efficient therapies for this liver disease are still limited. Mitochondrial dysfunction has been proven to be closely associated with NAFLD. The mitochondrial injury caused reactive oxygen species (ROS) production, and oxidative stress can aggravate the hepatic lipid accumulation, inflammation, and fibrosis. which contribute to the pathogenesis and progression of NAFLD. Therefore, pharmacological therapies that target mitochondria could be a promising way for the NAFLD intervention. Recently, natural products targeting mitochondria have been extensively studied and have shown promising pharmacological activity. In this review, the recent research progress on therapeutic effects of natural-product-derived compounds that target mitochondria and combat NAFLD was summarized, aiming to provide new potential therapeutic lead compounds and reference for the innovative drug development and clinical treatment of NAFLD.

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“…In China, Coptis chinensis Franch (CCF), especially the dried root of Coptis chinensis Makino, has been widely used in traditional medicine and food consumption for its functions of clearing heat and detoxification ( Meng et al, 2018 ; Wang et al, 2018 ). Currently, the compounds in CCF have been reported to exhibit a wide spectrum of pharmacological properties, including antibacterial ( Jamshaid et al, 2020 ; Gaba et al, 2021 ), anti-inflammatory ( Tarabasz and Kukula-Koch, 2020 ; Gaba et al, 2021 ), and immunoregulatory effects ( Wang et al, 2018 ; Kwon et al, 2021 ) among others. Besides, almost most of the articles have constantly given special emphasis on the alkaloids of CCF, especially palmatine, berberine, and berberrubine ( Meng et al, 2018 ; Wang et al, 2018 ; Jamshaid et al, 2020 ; Tarabasz and Kukula-Koch, 2020 ; Gaba et al, 2021 ; Kwon et al, 2021 ).…”

Section: Introductionmentioning

confidence: 99%

“…Currently, the compounds in CCF have been reported to exhibit a wide spectrum of pharmacological properties, including antibacterial ( Jamshaid et al, 2020 ; Gaba et al, 2021 ), anti-inflammatory ( Tarabasz and Kukula-Koch, 2020 ; Gaba et al, 2021 ), and immunoregulatory effects ( Wang et al, 2018 ; Kwon et al, 2021 ) among others. Besides, almost most of the articles have constantly given special emphasis on the alkaloids of CCF, especially palmatine, berberine, and berberrubine ( Meng et al, 2018 ; Wang et al, 2018 ; Jamshaid et al, 2020 ; Tarabasz and Kukula-Koch, 2020 ; Gaba et al, 2021 ; Kwon et al, 2021 ). Actually, CCF is tackled as a whole herb in traditional Chinese medicine (TCM) for thousands of years.…”

Section: Introductionmentioning

confidence: 99%

Dissecting and Evaluating the Therapeutic Targets of Coptis Chinensis Franch in the Treatment of Urinary Tract Infections Induced by Escherichia coli

et al. 2022

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Coptis chinensis Franch (CCF) is extensively used in the treatment of inflammatory-related diseases. Accumulating studies have previously demonstrated the anti-inflammatory properties of CCF, yet data on its exact targets against urinary tract infections (UTIs) remain largely unknown. Therefore, the present study decodes the potential targets of action of CCF against UTIs by network pharmacology combined with experiment evaluations. Based on the pharmacology network analysis, the current study yielded six core ingredients: quercetin, palmatine (R)-canadine, berlambine, berberine, and berberrubine. The protein–protein interaction network (PPI) was generated by the string database, and then, four targets (IL6, FOS, MYC, and EGFR) were perceived as the major CCF targets using the CytoNCA plug-in. The results of molecular docking showed that the six core constituents of CCF had strong binding affinities toward the four key targets of UTIs after docking into the crystal structure. The enrichment analysis indicated that the possible regulatory mechanisms of CCF against UTIs were based on the modules of inflammation, immune responses, and apoptosis among others. Experimentally, the Escherichia coli (E. coli) strain CFT073 was applied to establish in vivo and in vitro models. In vivo results revealed that the key targets, IL6 and FOS, are significantly upregulated in rat bladder tissues of UTIs, whereas the expression of MYC and EGFR remained steady. Last, in vitro results further confirmed the therapeutic potential of CCF by reducing the expression of IL6 and FOS. In conclusion, IL6 and FOS were generally upregulated in the progression of E. coli–induced UTIs, whereas the CCF intervention exerted a preventive role in host cells stimulated by E. coli, partially due to inhibiting the expression of IL6 and FOS.

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An insight into the medicinal attributes of berberine derivatives: A review

Cited by 74 publications

References 119 publications

Berberine Decreases Intestinal GLUT2 Translocation and Reduces Intestinal Glucose Absorption in Mice

Berberine Decreases Intestinal GLUT2 Translocation and Reduces Intestinal Glucose Absorption in Mice

Mitochondrial Targeting Therapeutics: Promising Role of Natural Products in Non-alcoholic Fatty Liver Disease

Dissecting and Evaluating the Therapeutic Targets of Coptis Chinensis Franch in the Treatment of Urinary Tract Infections Induced by Escherichia coli

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