Dihydroberberine, an isoquinoline alkaloid, exhibits protective effect against dextran sulfate sodium-induced ulcerative colitis in mice.

BACKGROUND: As a chronic inflammatory disease, ulcerative colitis (UC) is relevant to a rising risk of colorectal cancer. Dihydroberberine (DHBB), a natural occurring isoquinoline alkaloid with various bioactivities, was found in many plants including Coptis chinensis Franch. (Ranunculaceae), Phellodendron chinense Schneid. (Rutaceae), and Chelidonium majus L. (Papaveraceae). However, its protective effect on UC is sparsely dissected out. PURPOSE: To explore the protective role and underlying mechanism of DHBB on a model of colitis. METHODS: Acute colitis model was established by gavage with 3% dextran sulfate sodium (DSS) for 8 days. Influence of DHBB on DSS-induced clinical symptoms and disease activity index (DAI) was monitored and analyzed. Pathological injury of colon tissues was examined by hematoxylin-eosin and Alcian blue staining. The expression of intestinal mucosal barrier function proteins, immune-inflammation related biomarkers and signal pathway key targets were determined by ELISA kit, Western blot, immunohistochemistry and qRT-PCR. RESULTS: DHBB treatment effectively alleviated DSS-induced UC by relieving clinical manifestations, DAI scores and pathological damage, which exerted similar beneficial effect to azathioprine (AZA), and better than berberine (BBR). In addition, DHBB significantly improved the gut barrier function through up-regulating the levels of tight junction proteins and mucins. Furthermore, DHBB dramatically ameliorated colonic immune-inflammation state, which was related to the decrease of colonic pro-inflammatory cytokines and immunoglobulin through blocking TLR4/MyD88/NF-κB signal pathway. CONCLUSION: These results demonstrated that DHBB exerted a significant protective effect on DSS-induced experimental UC, at least partly through suppressing immune-inflammatory response and maintaining gut barrier function.

Zanthoxylum nitidum (Roxb.) DC: Traditional uses, phytochemistry, pharmacological activities and toxicology.

ETHNOPHARMACOLOGICAL RELEVANCE: Zanthoxylum nitidum (Roxb.) DC. (Z. nitidum), which is known in China as Liang-Mian-Zhen, is mainly distributed in southern China and is widely used in traditional Chinese medicine. It is traditionally used for treating stomach ache, toothache, rheumatic arthralgia, traumatic injury and venomous snake bites. Additional medical applications include the treatment of inflammations, various types of cancer, bacterial and viral infections, gastric and oral ulcers and liver damage. AIM OF THIS REVIEW: This paper aims to offer up-to-date information on the botany, traditional uses, phytochemistry, pharmacology and toxicity of Z. nitidum. This review also discussed the perspectives for possible future research on Z. nitidum. MATERIALS AND METHODS: A comprehensive review was carried out on studies about Z. nitidum conducted in the past 60 years by using different resources, including Flora of China, Pharmacopoeia of the People's Republic of China and academic databases. RESULTS: At present, more than 150 chemical constituents have been separated and identified from Z. nitidum, most of which include alkaloids. Biological activities, including anti-inflammation, analgesia, haemostasis, anticancer and antibacterial, were determined via in vitro and in vivo studies. The variations in the efficacy of Z. nitidum can be attributed to the biological activities of its natural products, especially alkaloids. Toxicity studies on Z. nitidum are relatively few, thus requiring further study. CONCLUSIONS: This article generalises the current research achievements related to Z. nitidum, which is an important medicinal material in China. Some traditional uses of Z. nitidum have been assessed by pharmacological studies. Unresolved problems remain, including molecular mechanisms underlying biological activities, pharmacokinetics, toxicology and therapeutic effect, which are still being studied and explored before Z. nitidum can be integrated into clinical medicine.