The aqueous (250, 500 mg/kg) extract of aerial parts of Mollugo pentaphylla Linn (Molluginaceae) was evaluated for its hypoglycemic potential in normoglycemic rats followed by alloxan and glucose loaded hyperglycemic rats by single oral administration. The plant extract was subjected to the determination of presence of different phytoconstituents by using standard qualitative chemical methods. The preliminary antioxidant potential of the extract was evaluated by spectrophotometric method, according to the Folin–Ciocalteu procedure for estimation of total phenolic content and calculated as gallic acid equivalents (GAE), whereas total flavonoid content was determined spectrophotometrically and expressed as quercetin equivalents. The related parameters like hematological, biochemical profiles including body weight variation study were also carried out in 30-days treated diabetic rats. The study report showed that the plant extract significantly (p<0.01 to p<0.001) reduces blood glucose level both in normoglycemic and hyperglycemic rats induced by alloxan and oral glucose loaded methods till the end of 10h and 4h respectively during the course of experiment. The preliminary phytochemical study report revealed that the test extract contain carbohydrate, glycosides, saponin, tannins, alkaloids, flavonoids, terpenoids, steroids; as phytoconstituents, whereas the Total phenolic and Total flavonoid content of the extract registered 75.16 μg of pyrocatechol equivalent /500mg, 9.58 mg equivalent of quercetin/gm respectively. The hematological, biochemical and loss of body weight study report are in good agreement with the activity and safety profile of the plant extract. The experimental results of the above studies indicate that the aqueous extract of the leaves of Mollugo pentaphylla Linn endowed with potential antihyperglycemic activity presumably due to free radical scavenging potential of the test extract