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

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.

In vitro cytotoxic potential of Gymnema sylvestre fractions on HT-29 cell line

“…The current data imply that after G. sylvestre treatment, carcinogen damages the colon cells which further decrease the growth. The extracts of Gymnema sylvestre is thought to prevent the development of colon cancer (Yadav et al, 2021).…”