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Tribulus terrestris (TT) is a member of the Zygophyllaceae family. Traditional Chinese medicine recommends the use of TT for treatment of a variety of diseases. In the present study we further investigated antiproliferative and cytotoxic effects of TT extract on normal and several malignant cell lines. For this purpose, TT was collected and after authentication, aqueous extract was prepared. Cytotoxic activity of TT extract at different doses (5-640μg/ml) was determined by LDH assay. Proliferative activity of TT extract was determined by trypan blue staining and cell counting methods. The results showed that IC50 of the extract for cancer cell line is 320 μg/ml and it is higher for hPBMC. On the other hand, we observed proliferative effect of TT extract on hPBMC but not on malignant cell lines.