Review
Copyright ©The Author(s) 2022. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Jul 14, 2022; 28(26): 3047-3062
Published online Jul 14, 2022. doi: 10.3748/wjg.v28.i26.3047
Role of baicalin as a potential therapeutic agent in hepatobiliary and gastrointestinal disorders: A review
Risha Ganguly, Ashutosh Gupta, Abhay K Pandey
Risha Ganguly, Ashutosh Gupta, Abhay K Pandey, Department of Biochemistry, University of Allahabad, Allahabad (Prayagraj) 211002, Uttar Pradesh, India
Author contributions: Ganguly R performed the literature review and wrote the manuscript; Ganguly R and Gupta A made the tables and figures; Pandey AK conceptualized the idea, critically reviewed and revised the manuscript; All authors have read and approved the final manuscript.
Supported by University Grants Commission, New Delhi, India in The Form of UGC-Junior and Senior Research Fellowships.
Conflict-of-interest statement: All the authors report no relevant conflicts of interest for this article.
Open-Access: This article is an open-access article that was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution NonCommercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: https://creativecommons.org/Licenses/by-nc/4.0/
Corresponding author: Abhay K Pandey, PhD, Full Professor, Department of Biochemistry, University of Allahabad, Faculty of Science, Katra, Allahabad (Prayagraj) 211002, Uttar Pradesh, India. akpandey23@rediffmail.com
Received: January 16, 2022
Peer-review started: January 16, 2022
First decision: March 8, 2022
Revised: March 21, 2022
Accepted: May 21, 2022
Article in press: May 21 2022
Published online: July 14, 2022
Abstract

Baicalin is a natural bioactive compound derived from Scutellaria baicalensis, which is extensively used in traditional Chinese medicine. A literature survey demonstrated the broad spectrum of health benefits of baicalin such as antioxidant, anticancer, anti-inflammatory, antimicrobial, cardio-protective, hepatoprotective, renal protective, and neuroprotective properties. Baicalin is hydrolyzed to its metabolite baicalein by the action of gut microbiota, which is further reconverted to baicalin via phase 2 metabolism in the liver. Many studies have suggested that baicalin exhibits therapeutic potential against several types of hepatic disorders including hepatic fibrosis, xenobiotic-induced liver injury, fatty liver disease, viral hepatitis, cholestasis, ulcerative colitis, hepatocellular and colorectal cancer. During in vitro and in vivo examinations, it has been observed that baicalin showed a protective role against liver and gut-associated abnormalities by modifying several signaling pathways such as nuclear factor-kappa B, transforming growth factor beta 1/SMAD3, sirtuin 1, p38/mitogen-activated protein kinase/Janus kinase, and calcium/calmodulin-dependent protein kinase kinaseβ/adenosine monophosphate-activated protein kinase/acetyl-coenzyme A carboxylase pathways. Furthermore, baicalin also regulates the expression of fibrotic genes such as smooth muscle actin, connective tissue growth factor, β-catenin, and inflammatory cytokines such as interferon gamma, interleukin-6 (IL-6), tumor necrosis factor-alpha, and IL-1β, and attenuates the production of apoptotic proteins such as caspase-3, caspase-9 and B-cell lymphoma 2. However, due to its low solubility and poor bioavailability, widespread therapeutic applications of baicalin still remain a challenge. This review summarized the hepatic and gastrointestinal protective attributes of baicalin with an emphasis on the molecular mechanisms that regulate the interaction of baicalin with the gut microbiota.

Keywords: Baicalin, Biotransformation, Gut microbiota, Hepatobiliary and gastrointestinal disorders, Signaling pathways

Core Tip: Baicalin possesses therapeutic efficacy against hepatic and gastrointestinal diseases including hepatic fibrosis, xenobiotic-induced liver injury, fatty liver disease, viral hepatitis, cholestasis, ulcerative colitis, hepatocellular and colorectal cancer. The drug action is mediated through its interaction with the gut microbiota, modulation of several signaling pathways, and inflammatory factors. The limitations of low solubility, permeability, and bioavailability pose challenges in the therapeutic applications. The different modes of drug delivery used in the transport of baicalin for ready absorption have paved the way for its use as a pharmacological agent against hepato-intestinal disorders.