Hyperglycemia causes long-term health complications when left untreated, especially in persons with diabetes. Managing the level of blood sugar is an important aspect of its treatment. Pito-pito is a multi-component herbal formula that may provide bioactivities to prevent elevated blood sugar levels. This study presents Pito-pito extracts' antihyperglycemic and anti-inflammatory activities that may reveal their potential medicinal value in managing blood sugar levels. The extracts of Pito-pito and its plant ingredients water extract were screened for antihyperglycemic activity by inhibition of α-amylase and α-glucosidase enzymes and effect on the glucose uptake in yeast cells. NO inhibition determined the anti-inflammatory activity. The results showed that the ethanolic extracts exhibited the highest inhibition in α-amylase, while the aqueous extract was inactive. Four of the 7 ingredients in the aqueous extract were inactive, and the 3 exhibited low inhibition activity. All extracts exhibited high inhibition in α-glucosidase relative to acarbose by several folds. It was shown that L. speciosa, P. guajava, and M. indica greatly contributed to its activity. The water, methanol, ethanol, acetone, dichloromethane, and hexane extracts of Pito-pito increased glucose uptake in yeast cells. Water, methanol, and hexane extracts inhibited nitric oxide by 88.83 ± 1.40 and 91.10 ± 2.05%, respectively. Pito-pito extracts possess antihyperglycemic and anti-inflammatory activities. The water extract of Pito-pito exhibited no inhibitory activity on α-amylase but exhibited promising activity on inhibiting α-glucosidase, increased glucose uptake in yeast cells, and promising NO inhibition activity.
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