Role of baicalin as a potential therapeutic agent in hepatobiliary and gastrointestinal disorders: A review

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.

Therapeutic Potential of Bioactive Components from Scutellaria baicalensis Georgi in Inflammatory Bowel Disease and Colorectal Cancer: A Review

“…Major aglycones baicalein and wogonin can be produced from glycosides baicalin and wogonoside, respectively [93]. Baicalin is hydrolyzed into baicalein by the action of the gut microbiota and reconverted back to baicalin through phase 2 metabolism in the liver [94,95]. Deglycosylation of wogonoside and its conversion to wogonin can be achieved via transformation of the enteric microbiome, enzyme catalysis, or herbal processing, such as soaking in water [96].…”

Effects of oxidative stress regulation in inflammation-associated gastric cancer progression treated using traditional Chinese medicines: A review

“…[67] Baicalin (BI) is an active flavonoid isolated from TCM Scutellarin baicalinase , which has outstanding anti-inflammatory, antioxidant, and immunomodulatory effects. [93] Niu demonstrated that BI had a protective effects on the gastric mucosa of CAG model rats and could promote the serum expression of NO and SOD, promote CAG cell apoptosis, and relieve oxidative stress. This mechanism was related to the activation of the OPG/RANKL axis.…”

Baicalin Promotes Apoptosis of Human Medullary Breast Cancer via the ERK/p38 MAPK Pathway

“…Baicalin (BAI), a flavonoid isolated from Scutellaria baicalensis Georgi derived from the Shanxi and Shandong provinces of China, is known as a major Traditional Chinese Medicine herb. Baicalin exhibits a variety of pharmaceutical properties, including antioxidant, anti-inflammatory, antiallergic, embryo-protective, cardioprotective, hepatoprotective, renal-protective, neuroprotective, antimicrobial, antipyretic, detoxifying, and antipathogen (Ganguly et al, 2022; Wang et al, 2018). Also, it has a long history of use in the treatment of plenty of symptoms related to cancer (Cheng et al, 2018).…”