Studying the Biological Activities and Molecular Docking of Some Novel Benzosultams and Benzosultones

Mukherjee, Suprabhat; Malakar, Suniti; Debnath, Sudarshan; Roy, Priya; Babu, Santi P. Sinha

doi:10.2174/1573407212666161028160745

Cited by 14 publications

(6 citation statements)

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“…Medicinal plant research is majorly based on the identification and application of the phytoextracts/compounds for treating parasitic infections. Synthetic compounds are preferred in the pharma industry due to several advantages like controlled synthesis, the ability to modify the structure according to the needs and availability [30, 31]. Natural products are preferred for their abundant distribution in nature, wide range of bio-activities, cost-effectiveness in preparing the therapeutic formulation and limited extent of side effects on non-targeted cells and tissues.…”

Section: Discussionmentioning

confidence: 99%

Polyphenol enriched ethanolic extract of Cajanus scarabaeoides (L.) Thouars exerts potential antifilarial activity by inducing oxidative stress and programmed cell death

et al. 2018

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Development of antifilarial drug from the natural sources is considered as one of the most efficacious, safe, and affordable approaches. In this study, we report the antifilarial activity of a leguminous plant Cajanus scarabaeoides (L.) Thouars. The polyphenol-rich ethanolic extract obtained from the stem part of the plant C. scarabaeoides (EECs) was found to be efficient in killing the filarial nematode Setaria cervi in all the three developmental stages viz. oocytes, microfilariae (Mf) and adults with LD50 values of 2.5, 10 and 35 μg/ml, respectively. While studying the molecular mechanism of action, we found that induction of oxidative stress plays the key role in inducing the mortality in S. cervi. The redox imbalance finally results in activation of the nematode CED pathway that executes the death of the parasite. Intriguingly, EECs was found to be selectively active against the worm and absolutely non-toxic to the mammalian cells and tissues. Taken together, our experimental data demonstrate that C. scarabaeoides can be chosen as an affordable natural therapeutic for treating filarial infection in the future with high efficacy and less toxicity.

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Section: Discussionmentioning

confidence: 99%

Polyphenol enriched ethanolic extract of Cajanus scarabaeoides (L.) Thouars exerts potential antifilarial activity by inducing oxidative stress and programmed cell death

et al. 2018

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“…It was also found that compound 5l exerts its action at low dose with maximum efficacy, as the bactericidal activity peaked at a MIC dose of 10 μg mL −1 against both types of bacteria tested, while compounds 5a , 5b , 5c , 5d , 5e , 5h , 5i and 5j showed to have moderate activity with MICs of 40–100 μg mL −1 . 35 When analyzing the structure of the compounds, it was found that O -alkyl substitution of the sultam moieties (compounds 5e , 5f and 5k ) resulted in the loss of or weak antibacterial activity. Hence, it can be deduced that the presence of sultam moieties was responsible for the antibacterial action.…”

Section: Sultams As Antimicrobialsmentioning

confidence: 99%

Unveiling sultam in drug discovery: spotlight on the underexplored scaffold

Chong,

Ong,

Yeong

2024

RSC Med. Chem.

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“…They can establish either proinflammatory or anti‐inflammatory milieu within the host, responsible for overt immunopathology. Taking ideas from these findings, recent studies have made significant progress in designing antifilarial immunotherapeutic agents, including vaccines and antibodies to eliminate filarial infection and restore immune homeostasis 153,192–195 . Antifilarial potential of these future therapeutics could be investigated in the context of apoptosis and this could provide us with very insightful directions.…”

Section: Future Directionmentioning

confidence: 99%

“…Synthetic cyclic sulfonamide, sultam, sultone and cyclic sulfonates are biologically very active compounds exhibiting antiviral, antifungal and antiparasitic activities. 153 Among these, quinolone‐fused cyclic sulfonamide (4,7‐dimethyl‐3,4,7,8‐tetrahydro‐3λ6‐[1,2]thiazino[4,3‐ f ]quinoline‐3,3,8‐trione) 8 L is a hybrid compound synthesized by fusion of coumarin and quinolone and is imperative to accumulate ROS that increases oxidative stress and later signals for apoptosis by triggering both extrinsic and intrinsic pathways against all the developmental stages of S. cervi . Moreover, 8 L is also beneficial against Wolbachia infection.…”

Section: Apoptosis Inducers As Antifilarial Agentsmentioning

confidence: 99%

Programmed cell death pathways as targets for developing antifilarial drugs: Lessons from the recent findings

Das,

Chakraborty,

Nandy

et al. 2023

J Cellular Molecular Medi

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More than half a century has passed since the introduction of the National Filariasis Control Program; however, as of 2023, lymphatic filariasis (LF) still prevails globally, particularly in the tropical and subtropical regions, posing a substantial challenge to the objective of worldwide elimination. LF is affecting human beings and its economically important livestock leading to a crucial contributor to morbidities and disabilities. The current scenario has been blowing up alarms of attention to develop potent therapeutics and strategies having efficiency against the adult stage of filarial nematodes. In this context, the exploration of a suitable drug target that ensures lethality to macro and microfilariae is now our first goal to achieve. Apoptosis has been the potential target across all three stages of filarial nematodes viz. oocytes, microfilariae (mf) and adults resulting in filarial death after receiving the signal from the reactive oxygen species (ROS) and executed through intrinsic and extrinsic pathways. Hence, it is considered a leading target for developing antifilarial drugs. Herein, we have shown the efficacy of several natural and synthetic compounds/nanoformulations in triggering the apoptotic death of filarial parasites with little or no toxicity to the host body system.

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Studying the Biological Activities and Molecular Docking of Some Novel Benzosultams and Benzosultones

Cited by 14 publications

References 0 publications

Polyphenol enriched ethanolic extract of Cajanus scarabaeoides (L.) Thouars exerts potential antifilarial activity by inducing oxidative stress and programmed cell death

Polyphenol enriched ethanolic extract of Cajanus scarabaeoides (L.) Thouars exerts potential antifilarial activity by inducing oxidative stress and programmed cell death

Unveiling sultam in drug discovery: spotlight on the underexplored scaffold

Programmed cell death pathways as targets for developing antifilarial drugs: Lessons from the recent findings

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