Researches on betulins health benefits actually started out on the anti-HIV property of its derivatives, as early as 1998 and 2001, American and Japanese scientists discovered and studied the anti-HIV activity of betulin derivatives.  according to their findings, several betulin-derived compounds feature anti-HIV properties. More studies on betulin itself came out recently on its anti-cancer and anti-inflammatory properties. In Poland, in vitro characterization of the anticancer activity of betulin in a range of human tumour cell lines demonstrated a remarkable anti-proliferative effect of betulin in all tested tumour cell cultures. Furthermore, betulin altered tumour cells morphology, decreased their motility and induced apoptotic cell death. And Korean scientists revealed that betulin showed anticancer activity on human lung cancer A549 cells by inducing apoptosis and changes in protein expression profiles were observed . And in Taiwan, China, researchers revealed that the anti-inflammatory mechanism of betulin may be related to increasing the activities of antioxidant enzymes in animal organ

These findings demonstrate the anti-cancer potential of betulin and suggest that they may be applied as an adjunctive measure in cancer treatment.

Betulinic acid, converted from betulin, is more active than betulin itself, most of the studies on this compound are focused on its anti-tumor activity. In 1995, betulinic acid was reported as a selective of human . Then it was demonstrated, that betulinic acid induces in human melanoma and model systems. Currently it is undergoing development with assistance from the program of the . Also betulinic acid was found active against neuroectodermal (, , ) and malignant brain tumors, , in human HL-60 cells, malignant head and neck squamous cell carcinoma SCC25 and SCC9 cell lines. In contrast, epithelial tumors, such as , , and as well as cells were completely refractory to treatment with betulinic acid.

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