Plumbagin exerts antiobesity effects through inhibition of pancreatic lipase and adipocyte differentiation

Plumbagin exerts antiobesity effects through inhibition of pancreatic lipase and adipocyte differentiation

Plumbagin is a naphthoquinone found in the roots of Plumbago zeylanica. Here, we report an investigation to evaluate its antiobesity activity. The preliminary binding affinity of plumbagin to human pancreatic lipase (PL) was determined using molecular docking simulation. The in vitro PL inhibitory p...

Full description

Saved in:
Bibliographic Details
Published in:Phytotherapy research Vol. 32; no. 8; pp. 1631 - 1635
Main Authors: Pai, S.A., Martis, E.A.F., Joshi, S.G., Munshi, R.P., Juvekar, A.R.
Format: Journal Article
Language:English
Published: England Wiley Subscription Services, Inc 01-08-2018
Subjects:
3T3-L1 Cells
Adipocytes
Adipocytes - cytology
Adipocytes - drug effects
Animals
antiobesity
Cell Differentiation - drug effects
Humans
Inhibition
Kinetics
Lipase
Lipase - antagonists & inhibitors
Lipase - metabolism
Male
Mice
Molecular docking
Molecular Docking Simulation
Naphthoquinones - pharmacology
Obesity - drug therapy
Optimization
oral fat tolerance test
Pancreas
pancreatic lipase
Plant Roots - chemistry
Plumbagin
Plumbaginaceae - chemistry
Rats
Rats, Wistar
Triglycerides
Triglycerides - blood
plumbagin
oral fat tolerance test
antiobesity
pancreatic lipase
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Plumbagin is a naphthoquinone found in the roots of Plumbago zeylanica. Here, we report an investigation to evaluate its antiobesity activity. The preliminary binding affinity of plumbagin to human pancreatic lipase (PL) was determined using molecular docking simulation. The in vitro PL inhibitory potential and the kinetics of inhibition were studied to validate and confirm the results obtained from molecular docking. The IC50 for PL was found to be 82.08 ± 9.47 μM, and the kinetics of inhibition was found to be of the mixed type. Further, the in vivo evaluation revealed that rats treated with plumbagin 1 mg/kg showed significant decrease in serum triglycerides (TG) and area under the curve of serum TG when compared with vehicle‐treated rats. It was also seen that plumbagin possessed significant antiadipogenic effect as demonstrated by reduced oil red O staining and decreased TG contents. Thus, we conclude that plumbagin is a promising molecule to combat obesity and further optimization of plumbagin to yield plumbagin analogues will result in its improved activity profile.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0951-418X
1099-1573
DOI:10.1002/ptr.6085