Context
Lysiphyllum strychnifolium
(Craib) A. Schmitz (LS) (Fabaceae) has traditionally been used to treat diabetes mellitus.
Objective
This study demonstrates the antidiabetic and antioxidant effects of aqueous extract of LS leaves
in vivo
and
in vitro
.
Materials and methods
The effects of aqueous LS leaf extract on glucose uptake, sodium-dependent glucose cotransporter 1 (SGLT1) and glucose transporter 2 (GLUT2) mRNA expression in Caco-2 cells, α-glucosidase, and lipid peroxidation were evaluated
in vitro
. The antidiabetic effects were evaluated using an oral glucose tolerance test (OGTT) and a 28-day consecutive administration to streptozotocin (STZ)-nicotinamide (NA)-induced type 2 diabetic mice.
Results
The extract significantly inhibited glucose uptake (IC
50
: 236.2 ± 36.05 µg/mL) and downregulated SGLT1 and GLUT2 mRNA expression by approximately 90% in Caco-2 cells. Furthermore, it non-competitively inhibited α-glucosidase in a concentration-dependent manner with the IC
50
and
K
i
of 6.52 ± 0.42 and 1.32 µg/mL, respectively. The extract at 1000 mg/kg significantly reduced fasting blood glucose levels in both the OGTT and 28-day consecutive administration models as compared with untreated STZ-NA-induced diabetic mice (
p
< 0.05). Significant improvements of serum insulin, homeostasis model assessment of insulin resistance (HOMA-IR), and GLUT4 levels were observed. Furthermore, the extract markedly decreased oxidative stress markers by 37–53% reduction of superoxide dismutase 1 (SOD1) in muscle and malondialdehyde (MDA) in muscle and pancreas, which correlated with the reduction of MDA production
in vitro
(IC
50
: 24.80 ± 7.24 µg/mL).
Conclusion
The LS extract has potent antihyperglycemic activity to be used as alternative medicine to treat diabetes mellitus.