Assessment of the α-glucosidase and α-amylase inhibitory potential of Paliurus spina-christi Mill. and its terpenic compounds

Abstract

Type II diabetes mellitus is a common disease in the world and characterized by hyperglycemia. Prevention of diabetes by reducing hyperglycemia depends on the inhibition of α-amylase and α-glucosidase enzymes. In this study, antidiabetic pro les of Paliurus spina-christi Mill. phytochemicals and extracts were investigated. The plant is used in folk medicine in Turkey as antidiabetic. α-Amylase and α-glucosidase inhibitory effect studies were conducted to prove this effect. The n-hexane extract (IC 50 = 445.7 ± 8.5 µg/mL) possessed potent inhibitory activity against α-glucosidase than that of acarbose (IC 50 = 4212.6 ± 130.0 µg/mL), unlike their slight/no inhibition on α-amylase. Phytochemical investigation of the n-hexane extract of the fruits of P. spina-christi led to the isolation of triterpenes, betulin (1a), betulinic acid (1b), lupeol (2) and a sterol, β-sitosterol (3). The structures of compounds 1-3 were elucidated by extensive 1D-and 2D-NMR and comparison with literature. Betulin (1a), betulinic acid (1b) and lupeol (2) are reported for the rst time from this species. All isolated compounds, especially betulin (1a) and betulinic acid (1b) mixture (IC 50 = 248 ± 12 µM) showed higher α-glucosidase inhibitory activity than acarbose (IC 50 = 6561 ± 207 µM). As extracts, the compounds were also found to be ineffective against α-amylase.

Multi-target action of Garcinia livingstonei extract and secondary metabolites against fatty acid synthase, α-glucosidase, and xanthine oxidase

“…Previous studies on lupeol and betulin and betulinic acid mixture reported good α-amylase and α-glucosidase inhibitory activities, and another work on amentoflavone showed its potent inhibitory activity against α-glucosidase. ( Rathinavel et al, 2021 , Yuca et al, 2022 , Li et al, 2023 ). Molecular docking analysis was performed to explore the binding modes of our isolated phytochemicals against α-glucosidase.…”

Assessment of the Hypoglycemic and Hypolipidemic Activity of Flavonoid-Rich Extract from Angelica keiskei

“…We used the method of Yuca et al [ 26 ], with slight modifications. The α-amylase solution (1 U/mL) was mixed into samples at varying concentrations and preheated in 37 °C water bath for 5 min, followed by addition of 1% preheated starch solution.…”

Recent Updates on Phytoconstituent Alpha-Glucosidase Inhibitors: An Approach towards the Treatment of Type Two Diabetes

“…Among the phenolic compounds isolated from C. humilis methanol extract in this study, myricetin, avicularin, pruning, quercitrin, guajavarin and isoquercitrin were accountable for their α-glucosidase activity. The Paliurus spina-christi mill fruit is used as an antidiabetic traditional medicine in Turkey, and a recent study showed that n -hexane fractions derived from the methanolic fruit extract have remarkably higher α-glucosidase inhibitory effects than acarbose with IC 50 of 445.7 ± 8.5 and 4212.6 ± 130.0 µg/mL, respectively [ 85 ]. The phytochemical analysis of the fruit extract identified three terpenic compounds (betulin, betulinic acid and lupeol) with a higher α-glucosidase inhibitory activity than acarbose.…”

“…Recently, Yuca et al evaluated the antidiabetic properties of the triterpenes isolated from Paliurus spina-christi mill fruit. Interestingly, the mixture of betulin ( Figure 5 c) and betulinic acid ( Figure 5 d) mixture (IC50 = 248 ± 12 µM) inhibited α-glucosidase 26 times better than acarbose (IC50 = 6561 ± 207 µM) [ 85 ]. In light of these findings, it may be intriguing to study the synergistic and antagonistic effects of various terpenoid compounds on α-glucosidase inhibition.…”