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Abstract Title:

Triterpenic Acids as Non-Competitiveα-Glucosidase Inhibitors fromwith Structure-Activity Relationship: In Vitro and In Silico Studies.

Abstract Source:

Biomolecules. 2020 May 12 ;10(5). Epub 2020 May 12. PMID: 32408614

Abstract Author(s):

Najeeb Ur Rehman, Sobia Ahsan Halim, Mohammed Al-Azri, Majid Khan, Ajmal Khan, Kashif Rafiq, Ahmed Al-Rawahi, Rene Csuk, Ahmed Al-Harrasi

Article Affiliation:

Najeeb Ur Rehman

Abstract:

Fourteen triterpene acids, viz., three tirucallane-type (-), eight ursane-type (-), two oleanane-type (,) and one lupane type (), along with boswellic aldehyde (),α-amyrine (), epi-amyrine (), straight chain acid (), sesquiterpene () and two cembrane-type diterpenes (,) were isolated, first time, from the methanol extract ofresin. Compound () was isolated for first time as a natural product, while the remaining compounds (‒) were reported for first time fromThe structures of all compounds were confirmed by advanced spectroscopic techniques including mass spectrometry and also by comparison with the reported literature. Eight compounds (-and) were further screened for in vitroα-glucosidase inhibitory activity. Compounds-andshowed significant activity againstα-glucosidase with ICvalues ranging from 9.9-56.8μM. Compound(IC= 9.9± 0.48 μM) demonstrated higher inhibition followed by(IC= 14.9± 1.31 μM),(IC= 20.9± 0.05 μM) and(IC= 56.8± 1.30 μM), indicating that carboxylic acid play a key role in α-glucosidase inhibition. Kinetics studies on the active compounds-andwere carried out to investigate their mechanism (mode of inhibition and dissociation constants). All compounds were found to be non-competitive inhibitors withvalues in the range of 7.05± 0.17-51.15 ± 0.25 µM. Moreover, in silico docking was performed to search the allosteric hotspot for ligand binding which is targeted by our active compounds investigates the binding mode of active compounds and it was identified that compounds preferentially bind in the allosteric binding sites of α-glucosidase. The results obtained from docking study suggested that the carboxylic group is responsible for their biologic activities. Furthermore, the α-glucosidase inhibitory potential of the active compounds is reported here for the first time.

Study Type : In Vitro Study

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