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In Silico Study, Physicochemical, and In Vitro Lipase Inhibitory Activity of α,β-Amyrenone Inclusion Complexes with
Luana Carvalho de Oliveira1, Danielle Lima Bezerra de Menezes1, Valéria Costa da Silva1
1Pharmacy Department, Federal University of Rio Grande do Norte, Natal 59012-570, RN, Brazil.
International Journal of Molecular Sciences
|September 28, 2021
Summary
This study developed novel inclusion complexes (ICs) of alpha,beta-amyrenone (ABAME) with cyclodextrins (CDs) to enhance its properties. These ABAME-CD complexes show improved physicochemical characteristics and potent lipase inhibition for potential anti-obesity applications.
Area of Science:
- Pharmacology
- Materials Science
- Biochemistry
Background:
- Alpha,beta-amyrenone (ABAME) is a triterpene with biological activities but limited pharmaceutical use due to poor water solubility.
- Cyclodextrins (CDs) are widely used to improve the solubility and bioavailability of poorly soluble compounds.
Purpose of the Study:
- To develop and characterize inclusion complexes (ICs) of ABAME with gamma- and beta-cyclodextrins (CD).
- To evaluate the potential anti-obesity properties of these ICs through in vitro lipase inhibition assays.
Main Methods:
- In silico molecular modeling studies to predict IC stability.
- Physicochemical characterization using FTIR, XRD, DSC, TGA, and SEM.
- In vitro lipase inhibition assays comparing ICs with Orlistat and native ABAME.
Main Results:
- Molecular modeling suggested higher stability for 2:1 molar ratio CD:ABAME ICs.
- Physicochemical analyses confirmed IC formation and altered ABAME properties.
- ABAME-CD ICs demonstrated superior lipase inhibition compared to Orlistat and potentiated ABAME's effects.
Conclusions:
- Novel ABAME-CD inclusion complexes were successfully developed.
- The ICs exhibit improved physicochemical properties and significant lipase inhibitory activity.
- These findings suggest ABAME-CD ICs as promising candidates for anti-obesity pharmaceutical formulations.
