Browsing by Author "Gupta, G."
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- ItemBiological databases and tools for neurological disorders(IMR Press Limited, 2022) Usman, M.B.; Ojha, S.; Jha, S.K.; Chellappan, D.K.; Gupta, G.; Singh, S.K.; Dua, K.; Roychoudhury, S.; Kumar, N.; Khan, F.A.; Dureja, H.; Upadhye, V.; Zacconi, Flavia C. M.; Prasanna, P.; Kesari, K.K.; Ashraf, G.M.; Alexiou, A.; Jha, N.K.Computational approaches to study of neuronal impairment is rapidly evolving, as experiments and intuition alone do not explain the complexity of the brain system. An overwhelming increase in the amount of new data from both theory and computational modeling necessitate the development of databases and tools for analysis, visualization and interpretation of neuroscience data. To ensure the sustainability of this development, consistent update and training of young professionals is imperative. For this purpose, relevant articles, chapters, and modules are essential to keep abreast of developments. This review seeks to outline the biological databases and analytical tools along with their applications. It is envisaged that such knowledge could provide a ''training recipe'' for young scientists and a guide for professionals and researchers in neuroscience.
- ItemChitosan modified 5-fluorouracil nanostructured lipid carriers for treatment of diabetic retinopathy in rats: a new dimension to an anticancer drug(Elsevier B.V., 2022) Sharma, D.S.; Wadhwa, S.; Gulati, M.; Kumar, B.; Vishwas, S.; Khursheed, R.; Saini, S.; Kumar, A.; Parveen, S.R.; Singh, S.K.; Dua, K.; Chitranshi, N.; Gupta, V.K.; Alrouji, M.; Alhajlah, S.; AlOmeir, O.; Gupta, G.; Zacconi, Flavia C. M.; Chellappan, D.K.; Morris, A.; Loebenberg, R.Diabetic retinopathy (DR) is one of the chronic complications of diabetes. It includes retinal blood vessels' damage. If untreated, it leads to loss of vision. The existing treatment strategies for DR are expensive, invasive, and need expertise during administration. Hence, there is a need to develop a non-invasive topical formulation that can penetrate deep to the posterior segment of retina and treat the damaged retinal vessels. In addition, it should also provide sustained release. In recent years, novel drug delivery systems (NDDS) have been explored for treating DR and found successful. In this study, chitosan (CS) modified 5-Fluorouracil Nanostructured Lipid Carriers (CS-5-FU-NLCs) were prepared by modified melt emulsification-ultrasonication method and optimized by Box-Behnken Design. The size, polydispersity index, zeta potential and entrapment efficiency of CS-5-FU-NLCs were 163.2 ± 2.3 nm, 0.28 ± 1.52, 21.4 ± 0.5 mV and 85.0 ± 0.2 %, respectively. The in vitro drug release and ex vivo permeation study confirmed higher and sustained drug release in CS-5-FU-NLCs as compared to 5-FU solution. HET-CAM Model ensured the non-irritant nature of CS-5-FU-NLCs. In vivo ocular studies of CS-5-FU-NLCs confirmed antiangiogenic effect of 5-FU by CAM model and diabetic retinopathy induced rat model, indicating successful delivery of 5-FU to the retina.
- ItemHybrid molecules based on 1,3,5-triazine as potential therapeutics: A focused review(2020) Prasher, P.; Sharma, M.; Aljabali, Alaa A. A.; Gupta, G.; Negi, P.; Kapoor, D. N.; Singh, I.; Zacconi, Flavia C. M.; Andreoli Pinto, T. de J.; Webba da Silva, M.; Bakshi, H.; Chellappan, D. K.; Tambuwala, M. M.; Dua, K.Majority of the representative drugs customarily interact with multiple targets manifesting unintended side effects. In addition, drug resistance and over expression of the cellular efflux-pumps render certain classes of drugs ineffective. With only a few innovative formulations in development, it is necessary to identify pharmacophores and novel strategies for creating new drugs. The conjugation of dissimilar pharmacophoric moieties to design hybrid molecules with an attractive therapeutic profile is an emerging paradigm in the contemporary drug development regime. The recent decade witnessed the remarkable biological potential of 1,3,5-triazine framework in the development of various chemotherapeutics. The appending of the 1,3,5-triazine nucleus to biologically relevant moieties has delivered exciting results. The present review focuses on 1,3,5-triazine based hybrid molecules in the development of pharmaceuticals.
- ItemMultifaceted role of synbiotics as nutraceuticals, therapeutics and carrier for drug delivery(Elsevier Ireland Ltd, 2022) Khursheed, R.; Gulati, M.; Wadhwa, S.; Vishwas, S.; Sharma, D.S.; Corrie, L.; Singh, S.K.; Steel, A.; Adams, J.; Dua, K.; Alam, A.; Alnasser, S.M.; Aba, Alkhayl F.F.; Parveen, Z.; Nammi, S.; Chellappan, D.K.; Gupta, G.; Zacconi, Flavia C. M.; Jha, N.K.Synbiotics, are a combination of probiotics and prebiotics. They play an important role in metabolizing different nutritional substrates and thus helps in the maintenance of human health. Any disbalance in the gut microflora, known as dysbiosis, is known to lead to a number of diseased conditions. It can be reverted by the administration of synbiotics. Present review highlights various mechanistic pathways through which synbiotics act as therapeutics. The dual role of synbiotics as nutraceutical and excipient in developing oral formulations are entailed with case studies. The findings entailed that there exist numerous studies on prebiotics as well as probiotics have been carried out to show their effects in several diseases. However, the concept of combining together them for prevention and treatment of various pathological conditions accruing from dysbiosis is relatively new. Synbiotics, however, face challenge of low stability during their sojourn in the GIT, which is generally overcome by various encapsulation techniques. Various studies also showed potential role of synbiotics in drug delivery. However, it is an emerging area and lacks clinical correlation. It is important to focus on clinical trials of formulations wherein synbiotics have been used as therapeutic moiety as well as pharmaceutical carrier for treating various diseases.
- ItemSynthesis and Anticancer Properties of 'azole' based Chemotherapeutics as Emerging Chemical Moieties: A Comprehensive Review(2020) Prasher, P.; Sharma, M.; Zacconi, Flavia C. M.; Gupta, G.; Ajabali, Alaa A. A.; Mishra, V.; Tambuwala, M. M.; Kapoor, D. N.; Negi, P.; Andreoli Pinto, Terezinha de Jesús; Singh, I.; Chellappan, D.; Dua, KamalAzole frameworks serve as privileged scaffolds in the contemporary drug design paradigm owing to their unique physicochemical profile that promotes the development of highly selective, physiological benevolent chemotherapeutics. Several azole nuclei function as bioisostere in medicinal chemistry and prompt the development of tailored therapeutics for targeting the desired biological entities. Besides, the azole scaffold forms an integral part in the advanced drug designing methodologies, such as target template insitu drug synthesis, that assists in rapid identification of the hit molecules form a diverse pool of leads; and direct biomolecule-drug conjugation, along with bioorthogonal strategies that ensure localization, and superior target specificity of the directed therapeutic. Lastly, the structural diversity of azole framework and high yielding click synthetic methods provide a comprehensive Structure-Activity Relationship analysis for design optimization of the potential drug molecules by fine-tuning the placement of different substituents critical for the activity. This review provides a comprehensive analysis of the synthesis and anticancer potential of azole based chemotherapeutics.
- ItemTargeting eosinophils in respiratory diseases: biological axis, emerging therapeutics and treatment modalities(2021) Lee, L.-Y.; Hew, G.S.Y.; Mehta, M.; Shukla, S.D.; Satija, S.; Khurana, N.; Anand, K.; Dureja, H.; Singh, S.K.; Mishra, V.; Singh, P.K.; Gulati, M.; Prasher, P.; Aljabali, A.A.A.; Tambuwala, M.M.; Thangavelu, L.; Panneerselvam, J.; Gupta, G.; Zacconi, Flavia C. M.; Shastri, M.; Jha, N.K.; Xenaki, D.; MacLoughlin, R.; Oliver, B.G.; Chellappan, D.K.; Dua, K.Eosinophils are bi-lobed, multi-functional innate immune cells with diverse cell surface receptors that regulate local immune and inflammatory responses. Several inflammatory and infectious diseases are triggered with their build up in the blood and tissues. The mobilization of eosinophils into the lungs is regulated by a cascade of processes guided by Th2 cytokine generating T-cells. Recruitment of eosinophils essentially leads to a characteristic immune response followed by airway hyperresponsiveness and remodeling, which are hallmarks of chronic respiratory diseases. By analysing the dynamic interactions of eosinophils with their extracellular environment, which also involve signaling molecules and tissues, various therapies have been invented and developed to target respiratory diseases. Having entered clinical testing, several eosinophil targeting therapeutic agents have shown much promise and have further bridged the gap between theory and practice. Moreover, researchers now have a clearer understanding of the roles and mechanisms of eosinophils. These factors have successfully assisted molecular biologists to block specific pathways in the growth, migration and activation of eosinophils. The primary purpose of this review is to provide an overview of the eosinophil biology with a special emphasis on potential pharmacotherapeutic targets. The review also summarizes promising eosinophil-targeting agents, along with their mechanisms and rationale for use, including those in developmental pipeline, in clinical trials, or approved for other respiratory disorders.