Design, synthesis and evaluation of a baicalin and berberine hybrid compound as therapeutic agent for ulcerative colitis

Jia, Dan; Dou, Yonghui; Li, Ziwen; Zhou, Xinxin; Gao, Ying; Chen, Ke-ji; Cong, Weihong; Ma, Min; Wu, Zhengzhi; Liu, Weimin

doi:10.1016/j.bmc.2020.115697

Cited by 12 publications

(7 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…After administration of baicalin-berberine hybrid compound to DSS-induced mice, the myeloperoxidase (MPO) activity in colon tissue and the expression of pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) were inhibited, and the development of inflammation was prevented. Besides, the therapeutic effect of baicalin-berberine complex was significantly better than that of baicalin and berberine ( 215 ).…”

Section: The Medication Of Ucmentioning

confidence: 96%

“…Couplet medicinal is a combination of two medicinal that enhances curative effect or reduces toxicity according to the principle of TCM treatment. It is also the basic unit of Chinese medicinal formula ( 215 ). Researches on couplet medicinals help to dispel the interactions between medicinals and explain the mechanism behind them.…”

Section: The Medication Of Ucmentioning

confidence: 99%

See 1 more Smart Citation

The Communication Between Intestinal Microbiota and Ulcerative Colitis: An Exploration of Pathogenesis, Animal Models, and Potential Therapeutic Strategies

et al. 2021

Front. Med.

View full text Add to dashboard Cite

Ulcerative Colitis (UC) is a chronic inflammatory bowel disease. The prolonged course of UC and the lack of effective treatment management make it difficult to cure, affecting the health and life safety of patients. Although UC has received more attention, the etiology and pathogenesis of UC are still unclear. Therefore, it is urgent to establish an updated and comprehensive understanding of UC and explore effective treatment strategies. Notably, sufficient evidence shows that the intestinal microbiota plays an important role in the pathogenesis of UC, and the treating method aimed at improving the balance of the intestinal microbiota exhibits a therapeutic potential for UC. This article reviews the relationship between the genetic, immunological and microbial risk factors with UC. At the same time, the UC animal models related to intestinal microbiota dysbiosis induced by chemical drugs were evaluated. Finally, the potential value of the therapeutic strategies for restoring intestinal microbial homeostasis and treating UC were also investigated. Comprehensively, this study may help to carry out preclinical research, treatment theory and methods, and health management strategy of UC, and provide some theoretical basis for TCM in the treatment of UC.

show abstract

Section: The Medication Of Ucmentioning

confidence: 96%

Section: The Medication Of Ucmentioning

confidence: 99%

The Communication Between Intestinal Microbiota and Ulcerative Colitis: An Exploration of Pathogenesis, Animal Models, and Potential Therapeutic Strategies

et al. 2021

Front. Med.

View full text Add to dashboard Cite

show abstract

“…Of the remaining articles, 52 records were removed by reading the titles and abstracts. Finally, 28 articles were finally included after full text assessment ( Hong et al, 2012 ; Li et al, 2016a ; Li et al, 2016b ; Zhang et al, 2017 ; Cui et al, 2018 ; Jing et al, 2018 ; Li and Shen, 2018 ; Yu et al, 2018 ; Li et al, 2019a ; Li et al, 2019b ; Hui et al, 2019 ; Liao et al, 2019 ; Zhu et al, 2019 ; Jia et al, 2020a ; Li et al, 2020a ; Jia et al, 2020b ; Li et al, 2020b ; Deng et al, 2020 ; Ding et al, 2020 ; Han et al, 2020 ; Liao et al, 2020 ; Yan et al, 2020 ; Zhai et al, 2020 ; Li et al, 2021a ; Li et al, 2021b ; Jiang et al, 2021 ; Zheng et al, 2021 ; Yang et al, 2022 ). The document screening flow chart is shown in Figure 2 .…”

Section: Resultsmentioning

confidence: 99%

“…A total of 508 animals were included, including 254 in the experimental group and 254 in the model group. Animal species included BALB/c mice ( Hong et al, 2012 ; Cui et al, 2018 ; Li and Shen, 2018 ; Yu et al, 2018 ; Li et al, 2019a ; Jia et al, 2020a ; Deng et al, 2020 ; Yan et al, 2020 ; Li et al, 2021a ; Li et al, 2021b ), C57BL/6 mice ( Li et al, 2016a ; Li et al, 2016b ; Zhang et al, 2017 ; Li et al, 2019b ; Li et al, 2020a ; Li et al, 2020b ; Ding et al, 2020 ; Han et al, 2020 ; Zhai et al, 2020 ; Yang et al, 2022 ), kunming mice ( Hui et al, 2019 ), Wistar rats ( Zhu et al, 2019 ; Jia et al, 2020b ), and Sprague-Dawley rats ( Jing et al, 2018 ; Liao et al, 2019 ; Liao et al, 2020 ; Jiang et al, 2021 ). One study ( Zheng et al, 2021 ) indicated the animals were mice, instead of mentioning their specific strain.…”

Section: Resultsmentioning

confidence: 99%

Pharmacological effects of berberine on models of ulcerative colitis: A meta-analysis and systematic review of animal studies

Wei

et al. 2022

Front. Pharmacol.

View full text Add to dashboard Cite

Berberine (BBR) is the main active constituent of the Rhizoma coptidis (Huanglian) and has multiple biological activities. Although current evidence suggests that the BBR has a multi-target effect in ulcerative colitis (UC), its action and mechanism are unclear. The purpose of this meta-analysis was to assess the pharmacological effects and potential mechanisms of BBR in UC models. Studies were searched from four databases (PubMed, Embase, Web of Science, and Cochrane Library) until March 2022. Standardized mean difference (SMD) and 95% confidence intervals (CI) were used for the adjudication of outcomes. Stata 15.0 software was used for statistical analysis. Twenty-eight publications and 29 studies involving 508 animals were included in the meta-analysis. The results showed that BBR reduced disease activity index (DAI) scores, alleviated UC-induced colon length (CL) loss, prevented weight loss, and reduced histological colitis score (HCS). Mechanistically, BBR was found to reduce myeloperoxidase (MPO) activity and malondialdehyde (MDA) levels, reduce levels of pro-inflammatory factors interleukin-1β (IL-1β), interleukin 6 (IL-6), tumor necrosis factor α (TNF-α), interferon-γ (IFN-γ) and mRNA expression of interleukin 17, increase levels of anti-inflammatory factor interleukin 10 (IL-10), and to increase levels of tight junction protein zonula occludens-1 (ZO-1) and occludin, which may involve antioxidant, anti-apoptotic, neuromodulation, anti-fibrotic, anti-inflammatory, barrier protection, and flora regulation aspects. However, additional attention should be paid to these outcomes due to the heterogeneity and methodological quality of the studies.

show abstract

“…is was especially apparent in Huang-Qin (Scutellaria baicalensis Georgi), which is an ingredient in Qingchang Huashi Formula [11]. In animal studies, many active components derived from Huang-Qin have been reported to be effective in the treatment of UC [12][13][14][15]. Of these active components, baicalin has been heavily researched and can be a potential candidate for new drug development.…”

Section: Introductionmentioning

confidence: 99%

Baicalin Ameliorates DSS-Induced Colitis by Protecting Goblet Cells through Activating NLRP6 Inflammasomes

Cheng

et al. 2022

Evidence-Based Complementary and Alternative Medicine

View full text Add to dashboard Cite

Objective. Baicalin is an active compound found in many natural herbs and has been used to treat intestinal disorders such as diarrhea and colon cancer. In this study, we used a dextran sodium sulfate (DSS)-induced colitis mouse model to investigate baicalin’s mechanisms in the treatment of colitis. Methods. 3% DSS was administered through the drinking supply for 7 days to induce colitis followed by the administration of 5-aminosalicylic acid and baicalin at three different doses (25, 50, and 100 mg/kg, W/W) for an additional 7 days. Body weight, stool consistency, and colon length were recorded. Colon tissue was stained with hematoxylin and eosin (H&E) to be used for histopathological scoring. Cytokine levels of the colon tissue and serum were evaluated using real-time quantitative reverse transcription-polymerase chain reaction (qRT-PCR) and enzyme-linked immunosorbent assay (ELISA), respectively. mRNA expression and protein levels of tight junctions (TJs) were detected with qRT-PCR and Western blotting. Goblet cells and the mucosal layer of the colon were visualized by Alcian Blue/periodic acid-Schiff (AB/PAS) staining. Mucin 2 (MUC2) was evaluated in both mRNA expression and protein levels. Nod-like receptor pyrin domain-containing protein 6 (NLRP6) inflammasomes were detected by immunohistochemistry and Western blotting. Results. Treatment with baicalin significantly relieved colitis as evidenced by reversing both weight loss and colon length shortening. In addition, baicalin inhibited inflammation by reducing proinflammatory cytokines and protected the intestinal barrier by upregulating tight junction proteins. Moreover, goblet cell count and intestinal mucosa thickness were both significantly increased after baicalin treatment. Giving baicalin could upregulate the expression of NLRP6 and interleukin (IL-18) both in mRNA and protein. Conclusion. Baicalin ameliorates DSS-induced colitis by protecting goblet cells through activating NLRP6 inflammasomes.

show abstract

Design, synthesis and evaluation of a baicalin and berberine hybrid compound as therapeutic agent for ulcerative colitis

Cited by 12 publications

References 32 publications

The Communication Between Intestinal Microbiota and Ulcerative Colitis: An Exploration of Pathogenesis, Animal Models, and Potential Therapeutic Strategies

The Communication Between Intestinal Microbiota and Ulcerative Colitis: An Exploration of Pathogenesis, Animal Models, and Potential Therapeutic Strategies

Pharmacological effects of berberine on models of ulcerative colitis: A meta-analysis and systematic review of animal studies

Baicalin Ameliorates DSS-Induced Colitis by Protecting Goblet Cells through Activating NLRP6 Inflammasomes

Contact Info

Product

Resources

About