• Qian Zhang, Jiao Jiao Zhao, Jian Xu, Feng Feng, and Wei Qu.
• Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
• J Ethnopharmacol. 2015 Sep 15; 173: 48-80.

Ethnopharmacological RelevanceThe genus Uncaria belongs to the family Rubiaceae, which mainly distributed in tropical regions, such as Southeast Asia, Africa and Southeast America. Their leaves and hooks have long been thought to have healing powers and are already being tested as a treatment for asthma, cancer, cirrhosis, diabetes, hypertension, stroke and rheumatism. The present review aims to provide systematically reorganized information on the ethnopharmacology, phytochemistry and pharmacology of the genus Uncaria to support for further therapeutic potential of this genus. To better understanding this genus, information on the stereo-chemistry and structure-activity relationships in indole alkaloids is also represented.Material And MethodsThe literature study of this review is based on various databases search (SCIFinder, Science Direct, CNKI, Wiley online library, Spring Link, Web of Science, PubMed, Wanfang Data, Medalink, Google scholar, ACS, Tropicos, Council of Heads of Australasian Herbaria, The New York Botanical Garden, African Plants Database at Genera Botanical Garden, The Plant List and SEINet) and library search for Biological Abstract and some local books on ethnopharmacology.Results19 species of the genus Uncaria are found to be important folk medicines in China, Malaysia, Phillippines, Africa and Southeast America, etc, and have been served for the treatment of asthma, rheumatism, hyperpyrexia, hypertension and headaches, etc. More than 200 compounds have been isolated from Uncaria, including indole alkaloids, triterpenes, flavonoids, phenols, phenylpropanoids, etc. As characteristic constituents, indole alkaloids have been considered as main efficacy component for hypertension, epilepsy, depressant, Parkinson's disease and Alzheimer's disease. In addition, pharmacokinetic and metabolism investigation reveal that the indole alkaloids are likely to be absorbed, metabolized and excreted at early time points. Moreover, the specific inhibition of CYP isozymes can regulate their hydroxylation metabolites at C-10 and C-11.ConclusionPreliminary investigations on pharmacological properties of the Uncaria species have enlightened their efficacious remedy for hypertension, asthma, cancer, diabetes, rheumatism and neurodegenerative diseases. To ensure the safety and effectiveness in clinical application, research on bioactive compounds, pharmacological mechanisms and toxicity of the genus Uncaria as well as the stereo-chemistry and structure-activity relationships of indole alkaloids seem very important.Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.

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