Diabetes mellitus (DM) is a serious chronic metabolic disorder. Various diseases are being treated with medicinal plants and that is because of the less side effects of the current therapy. The diversity of plants in Armenia is due to the singularity of natural environment. However, biochemical activity of these plants has not been studied well. Thus, the goal was to investigate biochemical activity and antihyperglycemic properties of Rumex obtusifolius L. in rabbits with hyperglycemia. The high content of total phenolic compounds, flavonoids, and tannins has been determined in this plant extract. Oral administration of ethanol extract showed significant effect on hyperglycemia, reducing fasting glucose levels (57.3%, p<0.05), improving glucose tolerance, and increasing liver glycogen content (1.5-fold, p<0.01) compared to the hyperglycemic control group. Furthermore, ethanol extract of R. obtusifolius reduced total cholesterol, low-density lipoprotein cholesterol levels, and vice versa increased high-density lipoprotein cholesterol levels and also decreased liver enzymes levels (alanine aminotransferase and aspartate aminotransferase) compared with untreated group. These findings suggest that R. obtusifolius may have beneficial effects and should be supplement, as herbal remedy in the treatment of DM.