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Evaluation of guanylhydrazone derivatives as inhibitors of Candida rugosa digestive lipase: Biological, biophysical, theoretical studies and biotechnological application.

Abstract：

:This work aimed to evaluate the inhibition of Candida rugosa lipase by five guanylhydrazone derivatives through biological, biophysical and theoretical studies simulating physiologic conditions. The compound LQM11 (IC50 = 14.70 μM) presented the highest inhibition against the enzyme. Therefore, for a better understanding of the interaction process, spectroscopic and theoretical studies were performed. Fluorescence and UV-vis assays indicate a static quenching mechanism with non-fluorescent supramolecular complex formation and changing the native protein structure. The binding process was spontaneous (ΔG < 0) and electrostatic forces (ΔH < 0 and ΔS > 0) played a preferential role in stabilizing the complex ligand-lipase. The compounds were classified as non-competitive inhibitors using orlistat as a reference in competition studies. Based on the 1H NMR assays it was possible to propose the sites of ligand (epitope) that bind preferentially to the enzyme and the theoretical studies were consistent with the experimental results. Finally, LQM11 was efficient as a lipase inhibitor of the crude intestinal extract of larvae of Rhynchophorus palmarum, an important agricultural plague, showing potential for control of this pest. Within this context, the real potential of this biotechnological application deserves further studies.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Santana CC,Silva-Júnior EF,Santos JCN,Rodrigues ÉEDS,da Silva IM,Araújo-Júnior JX,do Nascimento TG,Oliveira Barbosa LA,Dornelas CB,Figueiredo IM,Santos JCC,Grillo LAM

doi

10.1016/j.bioorg.2019.03.030

subject

Has Abstract

pub_date

2019-06-01 00:00:00

pages

169-180

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)30807-1

journal_volume

87

pub_type

杂志文章

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