Pyridothiadiazine derivatives as aldose reductase inhibitors having antioxidant activity

Zhu, Shaojuan; Zhang, Shuzhen; Hao, Xin; Qin, Xiangyu; Parveen, Shahida; Yang, Shaoqi; Ma, Bing; Zhu, Changjin

doi:10.1080/14756366.2016.1178638

Cited by 6 publications

(5 citation statements)

References 20 publications

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“…Our findings are consistent with Zhu et al. (2016), who found that, with varied degrees of efficiency, thiadiazine derivatives prevented the generation of MDA and the thiobarbituric acid reactive substances (TBARS) and decreased the index of lipid peroxidation (Zhu et al., 2016). This agrees with the conclusions drawn using the total antioxidant capacity technique.…”

Section: Discussionsupporting

confidence: 93%

“…Treatment with the examined component also showed a noteworthy decline in MDA in kidney tissue by −9.36% (p < .01) and −19.86% (p < .01) in both the therapeutic and preventive groups, separately, equated with the EAC control group. Our findings are consistent with Zhu et al (2016), who found that, with varied degrees of efficiency, thiadiazine derivatives prevented the generation of MDA and the thiobarbituric acid reactive substances (TBARS) and decreased the index of lipid peroxidation (Zhu et al, 2016). This agrees with the conclusions drawn using the total antioxidant capacity technique.…”

Section: Discussionsupporting

confidence: 92%

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In vivo anticancer study of sodium 2‐[(4‐oxidobenzylidene)amino]‐6H‐1,3,4‐thiadiazine‐5‐olate against Ehrlich ascites carcinoma via targeting PI3K/mTOR pathway

Rizzk,

El‐Deen,

Behery

et al. 2024

Chem Biol Drug Des

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Abstract1,3,4‐Thiadiazine‐based components have gained the attention as they afford significant intervention for cancer therapy. We aimed at assessing the in vivo antitumor activity of sodium 2‐[(4‐oxidobenzylidene) amino]‐6H‐1,3,4‐thiadiazine‐5‐c (SOTA) versus Ehrlich ascites carcinoma (EAC) cells in female mice's peritoneal cavity. An advantageous interaction of the test compound with the receptors p53 (2J1X), Caspase‐3 (3KJF), mTOR (3QAR), and PI3K (4JPS) was revealed by the docking study. The in vivo study of the test compound against EAC, equated with the EAC control mice, EAC bearing mice that received the test compound by i.p. injection proven a substantial decrease in the viability of tumor cell by 70%. Treatment with the tested compound increased total antioxidants capacity and decreasing malondialdehyde levels. Also, the apoptotic activity of the test compound was confirmed by up regulation of caspase‐3 and p53 and downregulation of PI3K and mTOR. Through the liver, kidney, and heart function assessments, the examined component has no adverse effects on either of the two organs, which were supported by a histological study. Significant positive and negative associations among variables were discovered, according to our research. Through the induction of apoptosis and antioxidant effects, the test compound show potential anticancer activity against EAC cells. The treatment with SOTA eliminated most of the pathological abnormalities brought on by EAC cells in mice, according to the results of tests on the liver, kidney, and heart as well as the histological investigation. Taking together, the tested compound SOTA is promising chemotherapeutic agent as supported by targeting PI3k/mTOR pathway.

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Section: Discussionsupporting

confidence: 93%

Section: Discussionsupporting

confidence: 92%

In vivo anticancer study of sodium 2‐[(4‐oxidobenzylidene)amino]‐6H‐1,3,4‐thiadiazine‐5‐olate against Ehrlich ascites carcinoma via targeting PI3K/mTOR pathway

Rizzk,

El‐Deen,

Behery

et al. 2024

Chem Biol Drug Des

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“…It has been found that AR inhibitors can ameliorate diabetes mellitus . In fact, numerous AR inhibitors have been tested and evaluated . For example, the AR inhibitor zopolrestato can lower acetate utilization in the diabetic heart, indicating increased glucose combustion via the glycolytic pathway and the Krebs cycle, that otherwise is inhibited in diabetes.…”

Section: The Polyol Pathwaymentioning

confidence: 99%

Redox imbalance stress in diabetes mellitus: Role of the polyol pathway

2018

Anim Models and Exp Med

202

139

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In diabetes mellitus, the polyol pathway is highly active and consumes approximately 30% glucose in the body. This pathway contains 2 reactions catalyzed by aldose reductase (AR) and sorbitol dehydrogenase, respectively. AR reduces glucose to sorbitol at the expense of NADPH, while sorbitol dehydrogenase converts sorbitol to fructose at the expense of NAD+, leading to NADH production. Consumption of NADPH, accumulation of sorbitol, and generation of fructose and NADH have all been implicated in the pathogenesis of diabetes and its complications. In this review, the roles of this pathway in NADH/NAD+ redox imbalance stress and oxidative stress in diabetes are highlighted. A potential intervention using nicotinamide riboside to restore redox balance as an approach to fighting diabetes is also discussed.

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“…The design and use of ALR2 inhibitors having antioxidant activity is a promising strategic approach that is under active consideration [ 82 , 83 , 84 , 85 ]. The multi-target drugs for T2DM treatment is a good strategy as well [ 67 , 86 ].…”

Section: Resultsmentioning

confidence: 99%

Influence of Nitrosyl Iron Complex with Thiosulfate Ligands on Therapeutically Important Targets Related to Type 2 Diabetes Mellitus

et al. 2023

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The high prevalence of type 2 diabetes mellitus (T2DM), and the lack of effective therapy, determine the need for new treatment options. The present study is focused on the NO-donors drug class as effective antidiabetic agents. Since numerous biological systems are involved in the pathogenesis and progression of T2DM, the most promising approach to the development of effective drugs for the treatment of T2DM is the search for pharmacologically active compounds that are selective for a number of therapeutic targets for T2DM and its complications: oxidative stress, non-enzymatic protein glycation, polyol pathway. The nitrosyl iron complex with thiosulfate ligands was studied in this work. Binuclear iron nitrosyl complexes are synthetic analogues of [2Fe–2S] centers in the regulatory protein natural reservoirs of NO. Due to their ability to release NO without additional activation under physiological conditions, these compounds are of considerable interest for the development of potential drugs. The present study explores the effects of tetranitrosyl iron complex with thiosulfate ligands (TNIC-ThS) on T2DM and its complications regarding therapeutic targets in vitro, as well as its ability to bind liposomal membrane, inhibit lipid peroxidation (LPO), and non-enzymatic glycation of bovine serum albumin (BSA), as well as aldose reductase, the enzyme that catalyzes the reduction in glucose to sorbitol in the polyol pathway. Using the fluorescent probe method, it has been shown that TNIC-ThS molecules interact with both hydrophilic and hydrophobic regions of model membranes. TNIC-ThS inhibits lipid peroxidation, exhibiting antiradical activity due to releasing NO (IC50 = 21.5 ± 3.7 µM). TNIC-ThS was found to show non-competitive inhibition of aldose reductase with Ki value of 5.25 × 10−4 M. In addition, TNIC-ThS was shown to be an effective inhibitor of the process of non-enzymatic protein glycation in vitro (IC50 = 47.4 ± 7.6 µM). Thus, TNIC-ThS may be considered to contribute significantly to the treatment of T2DM and diabetic complications.

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Pyridothiadiazine derivatives as aldose reductase inhibitors having antioxidant activity

Cited by 6 publications

References 20 publications

In vivo anticancer study of sodium 2‐[(4‐oxidobenzylidene)amino]‐6H‐1,3,4‐thiadiazine‐5‐olate against Ehrlich ascites carcinoma via targeting PI3K/mTOR pathway

In vivo anticancer study of sodium 2‐[(4‐oxidobenzylidene)amino]‐6H‐1,3,4‐thiadiazine‐5‐olate against Ehrlich ascites carcinoma via targeting PI3K/mTOR pathway

Redox imbalance stress in diabetes mellitus: Role of the polyol pathway

Influence of Nitrosyl Iron Complex with Thiosulfate Ligands on Therapeutically Important Targets Related to Type 2 Diabetes Mellitus

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