Herbal plant materials have huge potential in the field of medicine, nutraceuticals, perfumery, beverages, fragrances, cosmetics and dyeing industry. Centella asiatica (L.) Urban (family: Apiaceae) (C. asiatica) is a very popular medicinal herb in Sri Lanka, Madagascar, India and other parts of Asia. Gotu kola, Brahmi and Mandukparniin are the synonyms of C. asiatica which is mainly used for improving memory power. The pharmacological importance of C. asiatica is mainly because of triterpenes such as asiatic acid, asiaticoside, madecassoside and madecassic acid, etc. C. asiatica is mainly used for the treatment of mental fatigue, anxiety, epidermal wound, eczema, leprosy, asthma, psoriasis, ulcers and vein diseases. Asiaticoside is a pentacyclic triterpenoid saponin having anti-depression, anti-tumor, anti-inflammatory, antioxidant properties and further it also possesses wound healing, antiulcer and anti-hepatofibrotic activities. It improved cognitive impairment in diabetic condition because of the decreased oxidative stress. Quantification of asiaticoside in C. asiatica has been done by several methods which were mainly based on high performance liquid chromatography methods using different compositions of mobile phase sand detection systems. In these days scientists are trying to discover novel medicine from natural sources for the development of better drugs. In this review we have collected information of asiaticoside in respect to its medicinal values, pharmacological activities, extraction, isolation, and other analytical aspects. So the present review will be supportive to the scientists who are trying to develop some novel medicines from asiaticoside for the better health prospects.