Bioactive supra decorated thiazolidine-4-carboxylic acid derivatives attenuate cellular oxidative stress by enhancing catalase activity

Rizvi, Masood Ahmad; Hussain, Zakir; Ali, Fasil; Amin, Asif; Mir, Sajjad Husain; Rydzek, Gaulthier; Jagtap, Rohidas M.; Pardeshi, Satish K.; Qadri, Raies A.; Ariga, Katsuhiko

doi:10.1039/d0cp00253d

Cited by 13 publications

(6 citation statements)

References 51 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In contrast, gamma-glutamylcysteine is abundant in mammals and is involved in the synthesis of glutathione in the presence of its ligase [ 29 ], preventing potential adverse reactions associated with reactive oxygen species and associated redox reactions that may induce oxidative stress and may be linked to innate detoxification processes, ensuring, to some extent, healthy organism growth. Thiazolidine-4-carboxylic acid was modified by bioactivity and inhibited apoptosis caused by oxidative stress by enhancing the activity of catalase and improving the ability to bind to proteins, thereby regulating bioactivity [ 30 ]. The increased thiazolidine-4-carboxylic acid content in the pancreas effectively alleviated the stressful behavior of yak calves, creating favorable conditions for their healthy growth and development.…”

Section: Discussionmentioning

confidence: 99%

The Effect of Supplemental Concentrate Feeding on the Morphological and Functional Development of the Pancreas in Early Weaned Yak Calves

Jiao

Liu

Zhou

et al. 2022

Animals

View full text Add to dashboard Cite

This experiment was conducted to investigate the effect of supplemental concentrate feeding on the pancreatic development of yak calves. Twenty one-month-old yak calves with healthy body condition and similar body weight were selected as experimental animals and randomly divided into two groups, five replicates in each group. The control group yak calves were fed milk replacer and alfalfa hay, the experimental group yak calves were fed milk replacer, alfalfa hay and concentrate. The pre-feeding period of this experiment was thirty days, the trial period was one hundred days. At the end of feeding trail, five yak calves from each group were selected and slaughtered and the pancreas tissues of yak calves were collected and determined. The results showed that: (1) Dry matter and body weight of yak calves in the test group were significantly higher than those of the control group. (2) The apparent nutrient digestibility of crude protein, crude fat, calcium and phosphorus in the test group of yak calves was significantly higher than that of the control group, while the apparent nutrient digestibility of neutral detergent fiber and acid detergent fiber in the test group was significantly lower than that of the control group. (3) Pancreatic weight, organ index, total ratio of exocrine part area and total ratio of endocrine area of yak calves in the test group were significantly higher than those in the control group, while the ratio of exocrine area was significantly lower in the test group than that of the control group. (4) The activities of the main pancreatic digestive enzymes: pancreatic amylase, pancreatic lipase, pancreatic protease and chymotrypsin were significantly higher in the test group than those of the control group, as were the hormonal contents of glucagon, insulin and pancreatic polypeptide. (5) The main differential metabolites of the pancreas in the test group were significantly higher than those of the control group, such as D-proline, hypoxanthine, acetylcysteine, gamma-glutamylcysteine, thiazolidine-4-carboxylic acid, piperidinic acid, ellagic acid, nicotinamide, tropolone, D-serine, ribulose-5-phosphate, (+/-)5(6)-epoxyeicosatrienoic acid(EET), 2-hydroxycinnamic acid, L-phenylalanine, creatinine, tetrahydrocorticosterone, pyridoxamine, xanthine, 5-oxoproline, asparagine, DL-tryptophan, in-dole-3-acrylic acid, thymine, trehalose, docosapentaenoic acid, docosahexaenoic acid, fatty acid esters of hydroxy fatty acids(FAHFA) (18:1/20:3), fatty acid esters of hydroxy fatty acids(FAHFA) (18:2/20:4), adrenic acid and xanthosine. In conclusion, supplemental concentrate feeding promoted the good development of morphological and functional properties of the pancreas in early weaned yak calves to improve the digestion and absorption of feed nutrients, so as to enhance the growth and development quality of early weaned yak calves.

show abstract

Section: Discussionmentioning

confidence: 99%

The Effect of Supplemental Concentrate Feeding on the Morphological and Functional Development of the Pancreas in Early Weaned Yak Calves

Jiao

Liu

Zhou

et al. 2022

Animals

View full text Add to dashboard Cite

show abstract

“…From the pharmaceutical perspectives of bioavailability, and drug stability under physiological conditions, we investigated interaction of 5j and 5p with BSA through molecular dynamic simulations and further substantiated with various biophysical methods. 40 For an insight in the interaction of 5j and 5p with BSA carrier protein, MD simulations were performed on their best docked pose. The essential descriptors: RMSD, RMSF and number of contacts formed throughout the simulation were calculated for both 5j and 5p with BSA.…”

Section: Lead Molecules Of Benzyl-pyrrolidine-3ol Analogues Stably Interact With Bovine Serum Albuminmentioning

confidence: 99%

In vitro and In silico Evaluation of Structurally Diverse Benzyl-pyrrolidine-3-ol Analogues as Apoptotic Agents via Caspase Activation

Naqvi¹,

Amin

Ali

et al. 2021

ACSi

Self Cite

View full text Add to dashboard Cite

The activation of caspases is central to apoptotic process in living systems. Defects in apoptosis have been implicated with carcinogenesis. Need to develop smart agents capable of inducing apoptosis in tumor cells is obvious. With this motive, diversity oriented synthesis of 1-benzylpyrrolidin-3-ol analogues was envisaged. The multi component Ugi reaction synthesized library of electronically diverse analogues was explored for cytotoxic propensity towards a panel of human cancer cell lines at 10 μM. The lead compounds exhibit a selective cytotoxicity towards HL-60 cells as compared to cell lines derived from solid tumors. Besides, their milder cytotoxic effect on non-cancerous cell lines reaffirm their selective action towards cancer cells only.The lead molecules were tested for their ability to target caspase-3, as a vital protease triggering apoptosis. The lead compounds were observed to induce apoptosis in HL-60 cells around 10 μM concentration. The lead compounds exhibited various non-covalent supra type interactions with caspase-3 key residues around the active site. The binding ability of lead compounds with caspase-3 was studied via molecular docking and molecular dynamic (MD) simulations. MD simulations indicated the stability of compound-caspase-3 complex throughout the 50 ns simulation run. The stability and bio-availability of the lead compounds under physiological conditions was assessed by their interaction with Bovine Serum Albumin (BSA) as model protein. BSA interactions of lead compounds were studied by various bio-physical methods and further substantiated with in silico MD simulations.

show abstract

“…In continuation of our interests in exploring chemico–biological interactions of systems, − ,, the present study was therefore designed to elucidate the DPDSe-induced inhibition of AChE and for identification of any novel allosteric binding sites. For this purpose, structural and functional integrity of AChE in the presence of DPDSe was evaluated through in vitro and in silico (molecular docking and simulation) approaches with ebselen as a control.…”

Section: Introductionmentioning

confidence: 99%

Organoselenium Compounds as Acetylcholinesterase Inhibitors: Evidence and Mechanism of Mixed Inhibition

et al. 2021

Self Cite

View full text Add to dashboard Cite

Acetylcholinesterase (AChE) inhibitors are actively used for the effective treatment of Alzheimer’s disease. In recent years, the neuroprotective effects of organoselenium compounds such as ebselen and diselenides on the AChE activity have been investigated as potential therapeutic agents. In this work, we have carried out systematic kinetic and intrinsic fluorescence assays in combination with docking and molecular dynamics (MD) simulations to elucidate the molecular mechanism of the mixed inhibition of AChE by ebselen and diphenyl diselenide (DPDSe) molecules. Our MD simulations demonstrate significant heterogeneity in the binding modes and allosteric hotspots for DPDSe on AChE due to non-specific interactions. We have further identified that both ebselen and DPDSe can strongly bind around the peripheral anionic site (PAS), leading to non-competitive inhibition similar to other PAS-binding inhibitors. We also illustrate the entry of the DPDSe molecule into the gorge through a “side door”, which offers an alternate entry point for AChE inhibitors as compared to the usual substrate entry point of the gorge. Together with results from experiments, these simulations provide mechanistic insights into the mixed type of inhibition for AChE using DPDSe as a promising inhibitor for AChE.

show abstract

Bioactive supra decorated thiazolidine-4-carboxylic acid derivatives attenuate cellular oxidative stress by enhancing catalase activity

Abstract: Bioactive (2S,4R)-3-(tert-butoxycarbonyl)-2-(2-hydroxyphenyl)thiazolidine-4-carboxylic acid molecules restructure enzymes through complexation, allowing enhancing their activity to protect cells from oxidative stress.

Cited by 13 publications

References 51 publications

The Effect of Supplemental Concentrate Feeding on the Morphological and Functional Development of the Pancreas in Early Weaned Yak Calves

The Effect of Supplemental Concentrate Feeding on the Morphological and Functional Development of the Pancreas in Early Weaned Yak Calves

In vitro and In silico Evaluation of Structurally Diverse Benzyl-pyrrolidine-3-ol Analogues as Apoptotic Agents via Caspase Activation

Organoselenium Compounds as Acetylcholinesterase Inhibitors: Evidence and Mechanism of Mixed Inhibition

Contact Info

Product

Resources

About