In Vitro and In Vivo Evaluation of Antidiabetic Properties and Mechanisms of Ficus tikoua Bur.

Abstract

In folk medicine, Ficus tikoua (F. tikoua) has been used to treat diabetes for a long time, but there is a rare modern pharmacological investigation for its antidiabetic effect and mechanisms. Our study aimed to evaluate its hypoglycemic effect using in vitro and in vivo experimental models and then explore the possible mechanisms. In the ethanol extracts and fractions of F. tikoua, n−butanol fraction (NBF) exhibited the most potent effect on inhibiting α-glucosidase activity (IC50 = 0.89 ± 0.04 μg/mL) and promoting glucose uptake in 3T3−L1 adipocytes. Further animal experiments showed that NBF could play an antidiabetic role by ameliorating random blood glucose, fasting blood glucose, oral glucose tolerance, HbA1c level, and islets damage in diabetic mice. Then, the activities of the five subfractions of NBF (NBF1−NBF5) were further evaluated; NBF2 showed stronger α−glucosidase inhibition activities (IC50 = 0.32 ± 0.05 μg/mL) than NBF. Moreover, NBF2 also possessed the ability to promote glucose uptake, which was mediated via P13K/AKT and AMPK pathways. This study demonstrated that F. tikoua possesses antidiabetic efficacy in vitro and in vivo and provided a scientific basis for its folk medicinal use. NBF2 might be potential natural candidate drugs to treat diabetes mellitus. It is the first time the antidiabetic activity and the potential mechanisms of NBF2 were reported.

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“…Furthermore, our results indicated that QG upregulated Akt phosphorylation in the presence of insulin, highlighting its potential role in activating insulin-dependent pathways ( Figure 5 ). A previous study exhibited that the ethanolic extract of Ficus tikoua improved glucose uptake through the AMPK and PI3K/Akt pathways in 3T3-L1 adipocytes and diabetic mice [ 44 ]. This finding implies that QG improves glucose absorbance in myoblasts by activating AMPK and insulin dependent Akt signaling via PTP inhibition.…”

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“… •The upregulation of p-PI3K and p-Akt in 3T3-L1 adipocytes might mediate the possible mechanism of NBF in increasing glucose uptake. [ 282 ] 3 Ganoderma resinaceum Triterpenoid lactones α-glucosidase inhibitor An in vitro α-glucosidase inhibitory assay Compounds 1 and 2 were more potent α-glucosidase inhibitors than acarbose, with IC50 values of 0.75 ± 0.018 mM and 1.64 ± 0.022 mM, respectively. [ 44 ] 4 Cyclocarya paliurus Triterpenoid glycosides isolated from leaves ethanol extract Increase glucose uptake via AMPK/p38 pathways An in vitro study in 3T3-L1 adipocytes and C2C12 myotubes Compound 1 significantly enhanced insulin-stimulated glucose uptake in 3T3-L1 adipocytes and C2C12 myotubes.…”