scholarly journals 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

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Sangilimuthu Alagar Yadav ◽  
Lukmanul Hakkim Faruck ◽  
Rajagopal Subramanium ◽  
Lakshmi K. Surendren ◽  
Hamid Bakshi

Abstract Background 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. Methods and material 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. Results 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. Conclusions This paper concluded that 5-HMP possesses antioxidant properties, cytotoxic effects and also it possesses good drug binding properties on bovine serum albumin.

2011 ◽  
Vol 31 (10) ◽  
pp. 1091-1095
Author(s):  
Xiao-lin LI ◽  
Yan-fang ZHANG ◽  
Kai TANG ◽  
Ying TANG ◽  
Ruo-bing JIN ◽  
...  

2013 ◽  
Vol 13 (3) ◽  
pp. 414-421 ◽  
Author(s):  
Raquel T. Lima ◽  
Gemma A. Barron ◽  
Joanna A. Grabowska ◽  
Giovanna Bermano ◽  
Simranjeet Kaur ◽  
...  

2021 ◽  
Vol 27 ◽  
pp. 101089
Author(s):  
Kazuo Ohara ◽  
Shintaro Kinoshita ◽  
Jun Ando ◽  
Yoko Azusawa ◽  
Midori Ishii ◽  
...  

2004 ◽  
Vol 95 (2) ◽  
pp. 142-148 ◽  
Author(s):  
Tatsuya Yoshimasu ◽  
Teruhisa Sakurai ◽  
Shoji Oura ◽  
Issei Hirai ◽  
Hirokazu Tanino ◽  
...  

Polyhedron ◽  
2021 ◽  
pp. 115415
Author(s):  
Emanuelle Fraga da Silva ◽  
Paulo Roberto dos Santos ◽  
Krist Helen Antunes ◽  
Caroline Marinho Franceschina ◽  
Deise Nascimento de Freitas ◽  
...  

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