Oxyberberine is an important alkaloid class phytochemical found to be present in the Coptidis Rhizoma, Thalictrum longistylum, Thalictrum lucidum, Thalictrum podocarpum and Phellodendron amurense. Coptidis Rhizoma is a classical Chinese medicinal botanical drug for the treatment of gastrointestinal disorders. In order to give scientific information on the pharmacological activities and medicinal uses of oxyberberine, a large number of scientific databases were examined and scientific data about oxyberberine was gathered for this review article. Furthermore, the ultimate goal of this review is to provide scientific information on oxyberberine to facilitate its application in the treatment of human diseases. Here, keywords related to oxyberberine, Coptidis Rhizoma, herbal medicine and phytochemicals were searched in the scientific databases such as Science Direct, Google Scholar, and PubMed. The scientific data of this review demonstrate the biological potential of oxyberberine in medicine due to its therapeutic effectiveness on human diseases. Here we discussed the pharmacological activities of oxyberberine in colitis, lung injury, liver disease, intestinal mucositis, cardiotoxicity and lipoxygenase. The scientific evidence also described the therapeutic effects of oxyberberine in medicine due to its anti-cancer, anti-inflammatory, anti-bacterial, and hypoglycemic effects. However, its role in multidrug resistance and pharmacokinetic parameters was also discussed, which justifies conducting further preclinical research and clinical trials in the scientific field for future prospects of oxyberberine in the medicinal field.