α-Glucosidase inhibition, 15-lipoxygenase inhibition, and brine shrimp toxicity of extracts and isolated compounds from Terminalia macroptera leaves

Abstract

Context: Terminalia macroptera Guill. & Perr. (Combretaceae), a tree that grows in West Africa, has been used in traditional medicine against a variety of diseases such as hepatitis, gonorrhea, skin diseases, and diabetes.

Objective: To investigate enzyme inhibitory activity against α-glucosidase and 15-lipoxygenase (15-LO) and toxicity against brine shrimp of extracts and compounds from T. macroptera leaves.

Materials and methods: Methanol extract, ethyl acetate, and butanol extracts obtained from the methanol extract, six isolated polyphenols (chebulagic acid, chebulic acid trimethyl ester, corilagin, methyl gallate, narcissin, and rutin), and shikimic acid were evaluated for enzyme inhibition and toxicity.

Results: In enzyme inhibition assays, all extracts showed high or very high activity. Chebulagic acid showed an IC₅₀ value of 0.05 µM towards α-glucosidase and 24.9 ± 0.4 µM towards 15-LO, in contrast to positive controls (acarbose: IC₅₀ 201 ± 28 µM towards α-glucosidase, quercetin: 93 ± 3 µM towards 15-LO). Corilagin and narcissin were good 15-LO and α-glucosidase inhibitors, as well, while shikimic acid, methyl gallate, and chebulic acid trimethyl ester were less active or inactive. Rutin was a good α-glucosidase inhibitor (IC₅₀ ca. 3 µM), but less active towards 15-LO. None of the extracts or the isolated compounds seemed to be very toxic in the brine shrimp assay compared with the positive control podophyllotoxin.

Conclusion: Inhibition of α-glucosidase in the gastrointestinal tract may be a rationale for the medicinal use of T. macroptera leaves against diabetes in traditional medicine in Mali. The plant extracts and its constituents show strong inhibition of the peroxidative enzyme 15-LO.

• Chebulagic acid
• corilagin
• diabetes
• flavonoids
• polyphenols
• tannins

Acknowledgements

We are grateful to the healers of Mali for sharing their knowledge and experience with us.