Extracts and powders of Cissus quadrangularis have been used for many years to promote bone and tissues healing, as an analgesic, to treat infections, as an anabolic, and to promote weight loss and weight management. This review summarizes the studies in animals, humans and in vitro systems that have been conducted to determine the efficacy and safety of various Cissus preparations. Animal and in vitro studies provide support for the use of Cissus in promoting bone fracture healing and as an anti‐osteoporotic. Several human studies support the use of Cissus extracts in weight management. No studies have been conducted demonstrating that Cissus exhibits anabolic and body building activities. Based on studies to date, Cissus extracts appear to be exceedingly safe and free of adverse effects at the doses commonly used. A wide variety of chemical constituents have been isolated and identified from Cissus extracts, including steroids, flavonoids, stilbenes, iridoids, triterpenes and gallic acid derivatives. However, in few cases have specific physiological effects been related to identifiable constituents. Better standardization of extracts and more well‐controlled human studies are required. Copyright © 2012 John Wiley & Sons, Ltd.