Abstract
Background: Pathogenic yeasts resistance to current drugs emphasizes the need for new, safe, and cost-effective drugs. Also, new inhibitors are needed to control the effects of enzymes that are implicated in metabolic dysfunctions such as cancer, obesity, and epilepsy. Methods: The anti-yeast extract from Terminalia mantaly (Combretaceae) was fractionated and the structures of the isolated compounds established by means of spectroscopic analysis and comparison with literature data. Activity was assessed against Candida albicans, C. parapsilosis and C. krusei using the microdilution method, and against four enzymes of metabolic significance: glucose-6-phosphate dehydrogenase, human erythrocyte carbonic anhydrase I and II, and glutathione S-transferase. Results: Seven compounds, 3,3′-di-O-methylellagic acid 4′-O-α-rhamnopyranoside; 3-O-methylellagic acid; arjungenin or 2,3,19,23-tetrahydroxyolean-12-en-28-oïc acid; arjunglucoside or 2,3,19,23-tetrahydroxyolean-12-en-28-oïc acid glucopyranoside; 2α,3α,24-trihydroxyolean-11,13(18)-dien-28-oïc acid; stigmasterol; and stigmasterol 3-O-β-d-glucopyranoside were isolated from the extract. Among those, 3,3′-di-O-methylellagic acid 4′-O-α-rhamnopyranoside, 3-O-methylellagic acid, and arjunglucoside showed anti-yeast activity comparable to that of reference fluconazole with minimal inhibitory concentrations (MIC) below 32 µg/mL. Besides, Arjunglucoside potently inhibited the tested enzymes with 50% inhibitory concentrations (IC50) below 4 µM and inhibitory constant (Ki) <3 µM. Conclusions: The results achieved indicate that further SAR studies will likely identify potent hit derivatives that should subsequently enter the drug development pipeline.
Highlights
Fungal diseases affect 3–4 million people worldwide every year
We report in this paper the inhibitory potential of compounds isolated from this extract against some pathogenic yeasts and some enzymes of metabolic significance
The methanol extract of the stem bark of T. mantaly was screened for anti-yeast activity in vitro against three clinical isolates consisting of C. albicans, C. krusei and C. parapsilosis
Summary
Fungal diseases affect 3–4 million people worldwide every year. Of particular importance, the increasing resistance of pathogenic opportunistic yeasts to current drugs is a serious concern and has attracted the attention of the scientific community. In Cameroon, extracts from medicinal plants such as Terminalia mantaly (Combretaceae) are widely used by traditional healers to control diverse infections or associated symptoms, including but not limited to dysentery, gastroenteritis, hypertension, diabetes, and oral, dental, cutaneous and genital affections [8]. In spite of the work done on Terminalia species, no investigation has been attempted yet on the enzyme inhibition properties of their extracts and constituents targeting glucose-6-phosphate dehydrogenase, carbonic anhydrase and glutathione. Pathogenic yeasts resistance to current drugs emphasizes the need for new, safe, and cost-effective drugs. Methods: The anti-yeast extract from Terminalia mantaly (Combretaceae) was fractionated and the structures of the isolated compounds established by means of spectroscopic analysis and comparison with literature data.
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