Assessment of the α-glucosidase and α-amylase inhibitory potential of Paliurus spina-christi Mill. and its terpenic compounds
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 wer...
Gespeichert in:
Veröffentlicht in: | Medicinal chemistry research 2022-08, Vol.31 (8), p.1393-1399 |
---|---|
Hauptverfasser: | , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | 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 (IC
50
= 445.7 ± 8.5 µg/mL) showed greater inhibitory activity against
α
-glucosidase than acarbose (IC
50
= 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 (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.
Graphical abstract
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. |
---|---|
ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-022-02921-y |