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Screening and assessment of molecular mechanistic actions of 5-hydroxy-1-methylpiperidin-2-one against free radicals, lung cancer cell line (A549), and binding properties on bovine serum albumin
Sangilimuthu Alagar Yadav
1
,
Lukmanul Hakkim Faruck
2, 3
,
Rajagopal Subramanium
4
,
Lakshmi K Surendren
5
,
Hamid Bakshi
6
5
Department of Biotechnology, Kongunadu College of Arts and Science, Coimbatore, India
|
Publication type: Journal Article
Publication date: 2021-06-29
wos Q2
SJR: —
CiteScore: —
Impact factor: 3.0
ISSN: 23147245, 23147253
Abstract
Natural products play a key role in treating different ailment including diabetes, asthma, skin diseases, and cancer. It is well known that synthetic drugs elicit significant toxicity when used in the clinic. A higher drug affinity towards carrier protein Bovine Serum Albumin (BSA) would enhance a higher drug bioavailability which in turn leads to a higher therapeutic efficacy. The focus of the present study was to investigate antioxidant and anti-cancer potential of 5-hyrdoxy1-methylpiperidin-2-one (5-HMP) isolated from leaves of Tragia involucrata. In vitro free radical scavenging assays and MTT assay were employed to assess the antioxidant activity of 5-HMP and cytotoxicity of 5-HMP on lung cancer cell line, A549, respectively. In addition, attempts were made to investigate 5-HMP binding capacity on BSA by spectral studies and molecular docking. The antioxidant data revealed that 5-HMP inhibited the radicals with an IC50 value of 49.55 ± 0.75 μg/ml which was comparable with the IC50 values afforded by l-ascorbic acid. 5-HMP exhibited a dose-dependent cytotoxicity on A549 cells with an IC50 value of 30.00 ± 0.55 μg/ml. further 5-HMP induced a cell cycle arrest in A549 at S and G2/M phase. The fluorescence quenching was observed when an increasing concentration of 5-HMP, reacts with a fixed concentration of BSA (1.0 μM). The fluorescence quenching of BSA by 5-HMP indicated a binding constant of K5-HMP = 2.8 ± 1.4 × 104M−1 with corresponding binding free energy (ΔG)−6.06 K.cal/mole. This paper concluded that 5-HMP possesses antioxidant properties, cytotoxic effects and also it possesses good drug binding properties on bovine serum albumin.
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Yadav S. A. et al. Screening and assessment of molecular mechanistic actions of 5-hydroxy-1-methylpiperidin-2-one against free radicals, lung cancer cell line (A549), and binding properties on bovine serum albumin // Future Journal of Pharmaceutical Sciences. 2021. Vol. 7. No. 1. 129
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Yadav S. A., Faruck L. H., Subramanium R., Surendren L. K., Bakshi H. Screening and assessment of molecular mechanistic actions of 5-hydroxy-1-methylpiperidin-2-one against free radicals, lung cancer cell line (A549), and binding properties on bovine serum albumin // Future Journal of Pharmaceutical Sciences. 2021. Vol. 7. No. 1. 129
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TY - JOUR
DO - 10.1186/s43094-021-00277-5
UR - https://doi.org/10.1186/s43094-021-00277-5
TI - Screening and assessment of molecular mechanistic actions of 5-hydroxy-1-methylpiperidin-2-one against free radicals, lung cancer cell line (A549), and binding properties on bovine serum albumin
T2 - Future Journal of Pharmaceutical Sciences
AU - Yadav, Sangilimuthu Alagar
AU - Faruck, Lukmanul Hakkim
AU - Subramanium, Rajagopal
AU - Surendren, Lakshmi K
AU - Bakshi, Hamid
PY - 2021
DA - 2021/06/29
PB - Springer Nature
IS - 1
VL - 7
SN - 2314-7245
SN - 2314-7253
ER -
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@article{2021_Yadav,
author = {Sangilimuthu Alagar Yadav and Lukmanul Hakkim Faruck and Rajagopal Subramanium and Lakshmi K Surendren and Hamid Bakshi},
title = {Screening and assessment of molecular mechanistic actions of 5-hydroxy-1-methylpiperidin-2-one against free radicals, lung cancer cell line (A549), and binding properties on bovine serum albumin},
journal = {Future Journal of Pharmaceutical Sciences},
year = {2021},
volume = {7},
publisher = {Springer Nature},
month = {jun},
url = {https://doi.org/10.1186/s43094-021-00277-5},
number = {1},
pages = {129},
doi = {10.1186/s43094-021-00277-5}
}