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Molecules 2018, 23(6), 1444; https://doi.org/10.3390/molecules23061444

Pentacyclic Triterpenes from Cecropia telenitida Can Function as Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1

1
Department of Chemical Sciences, Faculty of Natural Sciences, Universidad Icesi, Cali, Valle del Cauca 760031, Colombia
2
Department of Pharmaceutical Sciences, Faculty of Natural Sciences, Universidad Icesi, Calle 18 # 122–135, Cali, Valle del Cauca 760031, Colombia
*
Author to whom correspondence should be addressed.
Received: 2 May 2018 / Revised: 5 June 2018 / Accepted: 8 June 2018 / Published: 14 June 2018
(This article belongs to the Collection Bioactive Compounds)
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Abstract

Plant extracts from the genus Cecropia have been used by Latin-American traditional medicine to treat metabolic disorders and diabetes. Previous results have shown that roots of Cecropia telenitida contain pentacyclic triterpenes and these molecules display a hypoglycemic effect in an insulin-resistant murine model. The pharmacological target of these molecules, however, remains unknown. Several lines of evidence indicate that pentacyclic triterpenes inhibit the 11β-hydroxysteroid dehydrogenase type 1 enzyme, which highlights the potential use of this type of natural product as phytotherapeutic or botanical dietary supplements. The main goal of the study was the evaluation of the inhibitory effect of Cecropia telenitida molecules on 11β-hydroxysteroid dehydrogenase type 1 enzyme activity. A pre-fractionated chemical library was obtained from the roots of Cecropia telenitida using several automated chromatography separation steps and a homogeneous time resolved fluorescence assay was used for the bio-guided isolation of inhibiting molecules. The screening of a chemical library consisting of 125 chemical purified fractions obtained from Cecropia telenitida roots identified one fraction displaying 82% inhibition of the formation of cortisol by the 11β-hydroxysteroid dehydrogenase type 1 enzyme. Furthermore, a molecule displaying IC50 of 0.95 ± 0.09 µM was isolated from this purified fraction and structurally characterized, which confirms that a pentacyclic triterpene scaffold was responsible for the observed inhibition. Our results support the hypothesis that pentacyclic triterpene molecules from Cecropia telenitida can inhibit 11β-hydroxysteroid dehydrogenase type 1 enzyme activity. These findings highlight the potential ethnopharmacological use of plants from the genus Cecropia for the treatment of metabolic disorders and diabetes. View Full-Text
Keywords: BDS; botanical dietary supplement; PT; pentacyclic triterpene; HTRF; homogeneous time resolved fluorescence; 11β-HSD1; 11-β hydroxysteroid dehydrogenase type 1; CBX; carbenoxolone BDS; botanical dietary supplement; PT; pentacyclic triterpene; HTRF; homogeneous time resolved fluorescence; 11β-HSD1; 11-β hydroxysteroid dehydrogenase type 1; CBX; carbenoxolone
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Mosquera, C.; Panay, A.J.; Montoya, G. Pentacyclic Triterpenes from Cecropia telenitida Can Function as Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1. Molecules 2018, 23, 1444.

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