Antihyperglycemic Effects of Salvia polystachya Cav. and Its Terpenoids: α-Glucosidase and SGLT1 Inhibitors

Abstract

The antihyperglycemic activity of ethanolic extract from Salvia polystachya (EESpS) and its products was evaluated using in vivo, ex vivo and in silico assays; additionally, an acute toxicity assay was evaluated. EESpS was classified as a nontoxic class 5 drug. EESpS, ethyl acetate fraction (EtOAcFr), secondary-6-fraction (SeFr6), ursolic acid (UA), and oleanolic acid (OA) reduced the hyperglycemia in DM2 mice. α-glucosidase inhibition was evaluated with oral sucrose and starch tolerance tests (OSuTT and OStTT), an intestinal sucrose hydrolysis (ISH) assay and molecular docking studies using acarbose as control. SGLT1 inhibition was evaluated with oral glucose and galactose tolerance tests (OGTT and OGaTT), an intestinal glucose absorption (IGA) assay and molecular docking studies using canagliflozin as the control. During the carbohydrate tolerance tests, all the treatments reduced the postprandial peak, similar to the control drugs. During the ISH, IC50 values of 739.9 and 726.3 µM for UA and OA, respectively, were calculated. During the IGA, IC50 values of 966.6 and 849.3 for UA, OA respectively, were calculated. Finally, during the molecular docking studies, UA and OA showed ∆G values of −6.41 and −5.48 kcal/mol−1, respectively, on α-glucosidase enzymes. During SGLT1, UA and OA showed ∆G values of −10.55 and −9.65, respectively.

Lavandula stoechas L. subsp. stoechas, a New Herbal Source for Ursolic Acid: Quantitative Analysis, Purification and Bioactivity Studies

“…This finding shows that ursolic acid was evaluated as a stronger inhibitor for α ‐glycosidase than acarbose, a commercial antidiabetic agent. In accordance with the results of the study, there were numerous reports on the potent inhibitory effects of ursolic acid isolated from various plant species on α ‐glycosidase [20,28,36,53–59] . Furthermore, the hyperglycemic property of ursolic acid isolated from Salvia polystachya was also confirmed by an in vivo study in DM2 mice [28] .…”

“…Furthermore, the hyperglycemic property of ursolic acid isolated from Salvia polystachya was also confirmed by an in vivo study in DM2 mice [28] . In this report, α ‐glycosidase inhibition of ursolic acid was determined with oral sucrose and starch tolerance tests and an intestinal sucrose hydrolysis assay, and it reduced the postprandial peak of the carbohydrates [28] …”

“…In accordance with the results of the study, there were numerous reports on the potent inhibitory effects of ursolic acid isolated from various plant species on α-glycosidase. [20,28,36,[53][54][55][56][57][58][59] Furthermore, the hyperglycemic property of ursolic acid isolated from Salvia polystachya was also confirmed by an in vivo study in DM2 mice. [28] In this report, α-glycosidase inhibition of ursolic acid was determined with oral sucrose and starch tolerance tests and an intestinal sucrose hydrolysis assay, and it reduced the postprandial peak of the carbohydrates.…”

“…Today, there has been mounting experimental data that either pure ursolic acid or plant extracts rich in this compound exert various in vitro and in vivo therapeutic potentials, such as neuroprotective, neuropsychiatric, cardioprotective, hepatoprotective, antimicrobial, antidiabetic, anti-oxidative, anti-inflammatory, anticancer, etc. [19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34][35][36] In particular, the potential neuroprotective and neuropsychiatric potentials of this molecule, which have been revealed by both in vivo and in vitro studies, are quite remarkable. [21][22][23][24][25]29,30,[32][33][34][35] Herein, the work on the determination of new plant species rich in ursolic acid and the purification of this molecule from crude extracts with practical and high efficiency is important for science.…”

Aktivitas Antihiperglikemik Ekstrak Etanol Daun Cincau Hitam Pada Mencit Putih Jantan Yang Diinduksi Aloksan

“…Berdasarkan tipenya, DM dapat dikelompokkan menjadi DM tipe 1 (DM 1) dan DM tipe 2 (DM 2). DM 1 umumnya mulai diderita pada masa pubertas dan merupakan kondisi autoimun di mana sel-sel β dari pankreas akan berkurang dan menyebabkan produksi insulin menjadi tidak mencukupi (Ortega et al, 2022). Sementara itu pada DM 2, pankreas dapat memproduksi insulin dalam jumlah yang memadai, tetapi sel-sel dari berbagai organ (lemak, hati dan otot) tidak merespons hormon ini dengan baik (Méril-Mamert et al, 2022).…”