Background: The nature is a fascinating source of biologic active substances, many of which are showing promising antitumor activities [1, 2]. The triterpenes are an important class of phytochemicals, classified in accordance with isoprene units [3, 4]. These chemicals are synthesized by the plants through cyclic processing of squalen. About 20000 of triterpens, such as cucurbitanes, cycloartanes, friedelanes, holostanes, hopanes, lanostanes, lupanes, oleananes, dammaranes, euphanes, tirucallanes, isomalabaricanes, ursanes and others are identified at the moment. From a wide diversity of triterpenes, the pentacyclic derivatives were the most frequent studied chemicals, due to their anti-inflammatory, analgesic, hepatoprotective, cardiotonic, antialergic, anti-microbial and anti-tumor properties [5-9]. Ursolic acid or 3β-hydroxi-urs-12-en-28-oic acid is a triterpen’s pentacyclic acid was discovered in plants, such as Ocimum sanctum L.(Holy Basil), Prunus laurocerasus L. (Cherry laurel leaves), Vaccinum myrtillus L. (Bilberry), Crataegus laevigata (Hawthorn), Harpagophytum procumbens DC (Devil’s Claw), Thymus vulgaris L. (Thyme), Sambucus nigra L. (Elder Flowers), Origanum vulgare L. (Oregano), Lavandula augustifolia Mill. (Lavender), Vinca minor L. (Periwinkle), as well as in the wax from apples, plums and pears peels [10]. It is a pentacyclic triterpenoid which belongs to cyclosqualenoid family [11]. This acid can be determined free or as aglicon of saponins. The recent results are supporting the anti-inflammatory, anti-proliferative, pro-apoptotic, anti-metastatic, anti-angiogenic and anti-parasite functions of this chemical [7,12]. The aim of this study was to highlight in details the anti-tumor activity of ursolic acid, by pointing out its influence on cells proliferating, apoptosis and metastatic property. Conclusions: Ursolic acid is a promising compound in tumor prevention and treatment, with many mechanisms of action on cell’s proliferation. Its derivatives usually are more biologically effective than initial compound, so obtaining of new ursolic derivatives makes further investigations in this field have a particular relevance.