In vitro cytotoxic and in silico activity of piperine isolated from Piper nigrum fruits Linn.

Padmaa M Paarakh,Dileep Chandra Sreeram,Shruthi S D,Sujan P S Ganapathy

doi:10.1186/s40203-015-0013-2

Abstract

BackgroundPiper nigrum [Piperaceae], commonly known as black pepper is used as medicine fairly throughout the greater part of India and as a spice globally.PurposeTo isolate piperine and evaluate in vitro cytotoxic [antiproliferative] activity and in silico method.MethodsPiperine was isolated from the fruits of P.nigrum. Piperine was characterized by UV,IR, 1H-NMR, 13C-NMR and Mass spectrum. Standardization of piperine was done also by HPTLC fingerprinting. In vitro cytotoxic activity was done using HeLa cell lines by MTT assay at different concentrations ranging from 20 to 100 μg/ml in triplicate and in silico docking studies using enzyme EGFR tyrosine kinase.ResultsFingerprinting of isolated piperine were done by HPTLC method. The IC50 value was found to be 61.94 ± 0.054 μg/ml in in vitro cytotoxic activity in HeLa Cell lines. Piperine was subjected to molecular docking studies for the inhibition of the enzyme EGFR tyrosine kinase, which is one of the targets for inhibition of cancer cells. It has shown −7.6 kJ mol−1 binding and 7.06 kJ mol−1 docking energy with two hydrogen bonds.Conclusionpiperine has shown to possess in vitro cytotoxic activity and in silico studies.

Highlights

Piper nigrum [Piperaceae], commonly known as black pepper is used as medicine fairly throughout the greater part of India and as a spice globally.Purpose: To isolate piperine and evaluate in vitro cytotoxic [antiproliferative] activity and in silico method
Piperine was subjected to molecular docking studies for the inhibition of the enzyme EGFR tyrosine kinase, which is one of the targets for inhibition of cancer cells
Drugs and chemicals DMEM medium (GIBCO), heat-inactivated fetal bovine serum (FBS), trypsin, ethylene-diaminetetraacetic acid (EDTA),PBS and MTT were purchased from Hi media concentrated to dryness at 60 °C

Summary

Introduction

Purpose: To isolate piperine and evaluate in vitro cytotoxic [antiproliferative] activity and in silico method. In the normal cells RTK activity is tightly controlled When they are mutated or structurally altered, they become potent oncoproteins which leads to abnormal activation of RTKs. Tyrosine kinases are an especially important target because they play an important role in the modulation of growth factor signaling. There are multiple types of targeted therapies available, including monoclonal antibodies, inhibitors of tyrosine kinases and antisense inhibitors of growth factor receptors. Tyrosine kinases play a critical role in the modulation of growth factor signaling. Activated forms of these enzymes can cause increases in tumor cell proliferation and growth, induce antiapoptotic effects and promote angiogenesis and metastasis.

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