Hydroxytriazenes incorporating sulphonamide derivatives: evaluation of antidiabetic, antioxidant, anti-inflammatory activities, and computational study

Chauhan, Laxmi Kunwar; Chopra, Jaishri; Vanangamudi, Murugesan; Tripathi, I. P.; Bhargava, Amit; Goswami, A. K.; Baroliya, Prabhat Kumar

doi:10.1007/s11030-022-10420-w

Cited by 4 publications

(2 citation statements)

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“…The oxidative stress–lowering effect of sulfisoxazole can be explained by the radical scavenging capacity of the phenyl and o/m‐alkyl substituted phenyl groups at the hydroxytriazene group. [ 45–47 ] Sulfisoxazole is generally known as an antibiotic. Antioxidant effects and antibacterial effects are not directly related, [ 48 ] although some antioxidants also show an antibacterial effect and some antibiotics can increase the endogenous level of antioxidants.…”

Section: Discussionmentioning

confidence: 99%

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Identification of Compounds Protecting Pancreatic Islets against Oxidative Stress using a 3D Pseudoislet Screening Platform

Rademakers,

Sthijns,

Paulino da Silva Filho

et al. 2023

Advanced Biology

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Oxidative stress leads to a lower success rate of clinical islet transplantation. Here, FDA‐approved compounds are screened for their potential to decrease oxidative stress and to protect or enhance pancreatic islet viability and function. Studies are performed on in vitro “pseudoislet” spheroids, which are pre‐incubated with 1280 different compounds and subjected to oxidative stress. Cell viability and oxidative stress levels are determined using a high‐throughput fluorescence microscopy pipeline. Initial screening on cell viability results in 59 candidates. The top ten candidates are subsequently screened for their potential to decrease induced oxidative stress, and eight compounds efficient reduction of induced oxidative stress in both alpha and beta cells by 2550%. After further characterization, the compound sulfisoxazole is found to be the most capable of reducing oxidative stress, also at short pre‐incubation times, which is validated in primary human islets, where low oxidative stress levels and islet function are maintained. This study shows an effective screening strategy with 3D cell aggregates based on cell viability and oxidative stress, which leads to the discovery of several compounds with antioxidant capacity. The top candidate, sulfisoxazole is effective after a 30 min pre‐incubation, maintains baseline islet function, and may help alleviate oxidative stress in pancreatic islets.

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Section: Discussionmentioning

confidence: 99%

“…The oxidative stress-lowering effect of sulfisoxazole can be explained by the radical scavenging capacity of the phenyl and o/m-alkyl substituted phenyl groups at the hydroxytriazene group. [45][46][47] Sulfisoxazole is generally known as an antibiotic.…”

Section: Discussionmentioning

confidence: 99%