Volume 203, 5 May 2017, Pages 39–46
Abstract
Background
Ethno-botanical information from diabetic patients in Cuba led to the identification of Allophylus cominia as a possible source of new drugs for the treatment of type 2 diabetes mellitus (T2-DM).
Experimental
Chemical characterization of the extracts from A. cominia
was carried out using chromatographic and spectroscopic methods. The
extracts were tested for their activity on PTP1B, DPPIV, α-glucosidase
enzymes and α-amylase.
Results
The flavonoid rich fractions from A. cominia
inhibited DPPIV enzyme (75.3±2.33%) at 30 µg/ml and produced a
concentration-dependent inhibition against DPPIV with a Ki value of
2.6 µg/ml. At 30 µg/ml, flavonoids and pheophytins extracts
significantly inhibited PTP1B enzyme (100±2.6% and 68±1% respectively).
The flavonoids, pheophytin A and pheophytin B fractions showed
significant concentration-dependent inhibition against PTP1B with Ki
values of 3 µg/ml, 0.64 µg/ml and 0.88 µg/ml respectively. At 30 µg/ml,
the flavonoid fraction significantly inhibited α-glucosidase enzyme
(86±0.3%) in a concentration-dependent pattern with a Ki value of
2 µg/ml. None of the fractions showed significant effects on α-amylase.
Fatty acids, tannins, pheophytins A and B, and a mixture of flavonoids
were detected in the methanolic extract from A. cominia. The identified flavonoids were mearnsitrin, quercitrin, quercetin-3-alloside, and naringenin-7-glucoside.
Conclusion
The pharmacological effects of the extracts from A. cominia
earlier observed in experimental diabetic models was confirmed in this
study. Thus a new drug or formulation for the treatment of T2-DM could
be developed from A. cominia.
Graphical abstract
Abbreviations
- PTP1B, (Protein Tyrosine Phosphatase 1B);
- DPPIV, (Dipeptidyl peptidase-4);
- Ki, (inhibitory constant);
- TFMS (, [Bis(4-trifluoromethylsulfonamidophenyl)−1,4-diisopropylbenzine), P32/98 ({(3N-[(2S, 3S)−2-amino-3-methyl-pentanoyl]−1,3-thiazolidine) hemifumarate);
- T2-DM, type 2 diabetes mellitus)
Keywords
- Allophylus cominia;
- DPPIV;
- PTP1B;
- Alpha-glucosidase;
- And α-amylase
