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

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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, the antidiabetic profiles of the Paliurus spina-christi Mill. fruit were investigated. The fruit of this species is used as an antidiabetic in folk medicine in Turkey. α-amylase and α-glucosidase inhibitory effect studies were conducted to prove this effect. The n-hexane sub-extract of the methanolic fruit extract (IC50 = 445.7 ± 8.5 µg/mL) showed greater inhibitory activity against α-glucosidase than acarbose (IC50 = 4212.6 ± 130.0 µg/mL), in contrast to its slight/no inhibitory effect on α-amylase. The phytochemical investigation of the n-hexane sub-extract of the P. spina-christi fruit led to the isolation of three triterpenes, namely betulin (1a), betulinic acid (1b), and lupeol (2), and a sterol (β-sitosterol) (3). The structures of compounds 1-3 were further analyzed using extensive 1D- and 2D-NMR, and the results were compared with literature. Betulin (1a), betulinic acid (1b), and lupeol (2) are reported from this species for the first time. All the isolated compounds, especially betulin (1a) and betulinic acid (1b) mixture (IC50 = 248 ± 12 µM) showed higher α-glucosidase inhibitory activity than acarbose (IC50 = 6561 ± 207 µM). As extracts, the compounds were also found to be ineffective against α-amylase.

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Highlights

  • P. spina christi fruit extract were investigated for their hypoglycemic effects.

  • Three triterpenes, namely betulin (1a), betulinic acid (1b), and lupeol (2) were isolated.

  • One sterol, β-sitosterol (3), was isolated.

  • Compounds 1a, 1b, and 2 were isolated from this species for the first time.

  • Betulin and betulinic acid were found to be responsible for the hypoglycemic activity of this species.

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Acknowledgements

The authors thank forest engineer MSc Mehmet ÖNAL from the Eastern Anatolia Forestry Research Institute for the identification of the plant.

Funding

This study was financially supported by the Scientific and Technological Research Council of Turkey (TÜBİTAK) 3001 – Starting R&D Projects Funding Program (No. 217S206).

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Authors and Affiliations

  1. Department of Pharmacognosy, Faculty of Pharmacy, Ataturk University, 25240, Erzurum, Turkey

    Hafize Yuca, Hilal Özbek & Zühal Güvenalp

  2. Ataturk University Medicinal and Aromatic Plant and Drug Research Center, 25240, Erzurum, Turkey

    Hafize Yuca, Hilal Özbek & Zühal Güvenalp

  3. Department of Pharmacognosy, Faculty of Pharmacy, Hacettepe University, 06100, Ankara, Turkey

    Lütfiye Ömür Demirezer

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  1. Hafize Yuca
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  2. Hilal Özbek
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  4. Zühal Güvenalp
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Correspondence to Hafize Yuca.

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Yuca, H., Özbek, H., Demirezer, L.Ö. et al. Assessment of the α-glucosidase and α-amylase inhibitory potential of Paliurus spina-christi Mill. and its terpenic compounds. Med Chem Res 31, 1393–1399 (2022). https://doi.org/10.1007/s00044-022-02921-y

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