Inhibitory kinetics and bioactivities of Nuciferine and Methyl Ganoderate on Mucor miehei lipase and 3T3-L1 preadipocytes.

Abstract:

:In this study, inhibitory kinetics of Nuciferine and Methyl Ganoderate extrated from Lotus Leaves and Ganoderma lucidum on Mucor miehei Lipase were studied first. The molecular structure of Nuciferine and Methyl Ganoderate were determined. The inhibitory effects of two extracts on lipase were reversible, with the IC50 values of 0.194 and 0.332 mg/mL, respectively. The inhibition kinetic analysis by Lineweaver-Burk plots showed that they were a mixed-type inhibitor of lipase, with inhibition constants KI of 0.16 and 0.29 mg/mL, and KIS of 0.36 and 0.49 mg/mL, respectively. Results of spectral analysis showed that the UV absorption and the molecule fluorescence spectrum of the lipase hydrolyzate were significantly decreased after the inhibitor was added. The molecular docking further suggested that the interaction site between the active substance and inhibitor was located in an α-helix and a β-sheet of the lipase, and the lipase active site was interfered by the inhibitor near the cap structure. In addition, the proliferation and differentiation of 3 T3-L1 preadipocytes were inhibited by two extracts. Total triglycerides and cholesterol were significantly reduced in the cells. The results confirmed that Nuciferine and Methyl Ganoderate can be used as potential obesity treatment drugs.

journal_name

Int J Biol Macromol

authors

Liu XT,Liu TT,Xu HL,Chen QX,Wang Q

doi

10.1016/j.ijbiomac.2020.09.127

subject

Has Abstract

pub_date

2020-11-15 00:00:00

pages

1719-1728

eissn

0141-8130

issn

1879-0003

pii

S0141-8130(20)34487-1

journal_volume

163

pub_type

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