New calogenin pregnane glycoside derivative from Huernia saudi- arabica and its Lipase and α-Glucosidase Inhibitory Activities - 30/05/20
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• | A new steroidal pregnane glycoside (Huernioside A) was isolated from dichloromethane fraction; it was identified as 3β, 11, 14β, 20(R)-tetrahydroxy-pregna-5,9(11)-diene-3-O-β-D-thevetopyranosyl-(1-4)-β-D-cymaropyranoside |
• | The alcoholic extract of the aerial part, dichloromethane fraction and Huernioside A were showed inhibitory potential against pancreatic lipase compared to orilstat. |
• | Moderate α-glucosidase inhibitory activities were evidenced for alcoholic extract and Huernioside A compared to acarbose. |
• | Enzyme kinetics and docking studies were performed to decipher the lipase inhibitory activity. |
Abstract |
As ongoing investigation of Huernia saudi-arabica D.V.Field (Asclepiadaceae), a new steroidal pregnane glycoside (Huernioside A) was isolated from dichloromethane fraction (DCM); it was identified as 3β, 11, 14β, 20(R)-tetrahydroxy-pregna-5,9(11)-diene-3-O-β-D-thevetopyranosyl-(1-4)-β-D-cymaropyranoside(HCP) through analysis of 1D, 2D NMR besides ESI-MS data. The alcoholic extract of the aerial part (ALE), DCM and HCP showed inhibitory potential against pancreatic lipase compared to orilstat. Among the tested samples, the ALE and HCP exhibited a promising pancreatic lipase inhibitory commotion through IC50 values of 0.61 ± 0.15, 1.23 ± 0.07 mg/ml (equivalent to 88.8 μM), respectively. HCP was prevailed to have a mixed mode of inhibition as exposed by enzyme kinetic studies. Hydrophobic interactions were the major forces involved in ligand enzyme interactions. In contrast, moderate α-glucosidase inhibitory activities were evidenced for ALE and HCP (% inhibition: 24.8 ± 1.8 and 26.6 ± 2.5, respectively) compared to acarbose. This investigation is the first to report on the possible in vitro anti-obesity and anti-diabetic impact of H. saudi-arabica.
Le texte complet de cet article est disponible en PDF.Keywords : Docking, Huernia saudi-arabica, Obesity, α-Glucosidase, Pancreatic lipase, Pregnane glycoside
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