المؤلفون: Mittal, Roopal^{1, 2, 1}, Goel, Prerna², Kushwah, Ajay Singh³, Ranga, Gurjant⁴

المصدر: Research Journal of Pharmacognosy and Phytochemistry 14(2):77-88. 2022

المؤلفون: Lu Dongming, Yaqoob Obaid, Kumar Manish, Kushwah Ajay Singh, Sharma Rahul Kumar, Kumar Devinder, Mavai Yogendra, Khan Rukaiya

المصدر: Acta Pharmaceutica, Vol 73, Iss 1, Pp 29-42 (2023)

مصطلحات موضوعية: covid-19, asthma, smoking, critical care, sars-cov-2, Pharmaceutical industry, HD9665-9675

الوصف: This century’s most serious catastrophe, COVID-19, has been dubbed “the most life-threatening disaster ever”. Asthmatic persons are even more prone to COVID-19’s complex interplay with the underlying inflammatory condition. In order to protect themselves against COVID-19, asthmatic patients must be very vigilant in their usage of therapeutic techniques and drugs (e.g., bronchodilators, 5-lipoxygenase inhibitors), which may be accessed to deal with mild, moderate, and severe COVID-19 indications. People with asthma may have more severe COVID-19 symptoms, which may lead to a worsening of their condition. Several cytokines were found to be elevated in the bronchial tracts of patients with acute instances of COVID-19, suggesting that this ailment may aggravate asthma episodes by increasing inflammation. The intensity of COVID-19 symptoms is lessened in patients with asthma who have superior levels of T-cells. Several antibiotics, antivirals, antipyretics, and anti-inflammatory drugs have been suggested to suppress COVID-19 symptoms in asthmatic persons. Furthermore, smokers are more likely to have aggravated repercussions in COVID-19 infection. Being hospitalized to critical care due to COVID-19, needing mechanical breathing, and suffering from serious health repercussions, are all possible outcomes for someone who has previously smoked. Smoking damages airways and alveoli, which significantly raises the risk of COVID-19-related health complications. Patients with a previous record of smoking are predisposed to severe COVID-19 disease symptoms that essentially require a combination of bronchodilators, mucolytics, antivirals, and antimuscarinic drugs, to cope with the situation. The present review discusses the care and management of asthmatic and smoker patients in COVID-19 infection.

وصف الملف: electronic resource

العلاقة: https://doaj.org/toc/1846-9558Test

الوصول الحر: https://doaj.org/article/3c36ee230c054c37943a477a43349588Test

المؤلفون: Mittal, Roopal, Sharma, Shailesh, Mittal, Amit, Kushwah, Ajay Singh

المصدر: Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry ; volume 23 ; ISSN 1871-5230

الوصف: Background: Non-communicable diseases are chronic systemic inflammation in humans that occurs because of enhanced inflammatory mediators of the arachidonic acid cas-cade. We aimed to explore whether the lead chalcone compounds could exhibit anti-inflam-matory activity via dual blockage of COX-2/5-LOX enzymes and their regulatory mechanism. Methods: RAW 264.7 macrophages were collected from NCC, Pune, for in-vitro experiments. The IC50 values of chalcone compounds C45 and C64 were calculated. RAW 264.7 macro-phages were treated with C45 and C64 (10%, 5%, 2.5%, 0.125%, and 0.0625% concentration). The cell viability was carried out with an MTT assay. The COX-1, COX-2, 5-LOX, PGE2, and LTB4 levels were detected by ELISA-based kits. The in-vivo evaluation was carried out in Male Wistar rats (250-300 g, 7-8 weeks old) with acute and chronic anti-inflammatory models and histopathological studies on the stomach, liver, and kidney. Results: The present study described the in-vitro and in-vivo biological evaluation of dual COX-2/5-LOX inhibitors in chalcone derivatives (C45 and C64) compounds showed the most effective COX-2 and 5-LOX inhibition with IC50 values 0.092 and 0.136μM respectively. Simultaneously, compound C64 showed comparable selectivity towards COX-2 with a Selec-tivity Index (SI) of 68.43 compared to etoricoxib, with an SI of 89.32. In-vivo carrageenan-induced rat paw oedema activity, the compound C64 showed a significant reduction in oedema with 78.28% compared to indomethacin with 88.07% inhibition. Furthermore, cotton pellet-induced granuloma activity revealed that compound C64 significantly reduced 32.85% com-pared with standard 40.13% granuloma inhibition. Conclusion: The chalcone compound C64, (E)-1-(4-Amino-2-hydroxyphenyl)-3-(3,4,5-tri-methoxyphenyl)-prop-2-en-1-one was proved to be a potent and novel Dual COX-2/5-LOX inhibitor with improved gastric safety profiling.

الإتاحة: https://doi.org/10.2174/0118715230301176240605072113Test

المؤلفون: Chauhan, Sakshi, Mittal, Roopal, Kumar, Manish, Mittal, Amit, Kushwah, Ajay Singh

المصدر: Combinatorial Chemistry & High Throughput Screening ; volume 27 ; ISSN 1386-2073

مصطلحات موضوعية: Organic Chemistry, Computer Science Applications, Drug Discovery, General Medicine

الوصف: Point of Care Diagnostics (POCD) is quintessential in hospitals and the healthcare sector as the secants uplift the quality of medical care and the life of a patient by facilitating quick identification of the underlying pathological condition. Nanotechnology can provide opportunities and has potential in the development of new-age sensing/diagnostic tools. Owing to extraordinary features (e.g., higher density, effective catalysis, good conduction, biocompatibility, inertness, and greater surface-to-volume ratio), gold nanoparticles (AuNPs) are frequently employed in POCT (Point-of-Care-Testing). Gold nanoparticles-based colorimetric methods are widely used in the rapid, sensitive, and selective detection of analytes/target molecules. AuNPs description is critical for their possible utility in prophylaxis, diagnostics, and treatment of an ailment. AuNPs interact with organic/inorganic target molecules to generate colorimetric shift that enables the accurate, precise, and subtle recognition of biologicals (e.g., microorganisms, cellular components, and proteins) and metal ions. This review focused on the need for AuNPs-based colorimetric application in prophylaxis, diagnostics, and treatment in healthcare and reviewed the future outlook of these AuNPs for biological applications. Different synthesis methods of AuNPs, their morphology, and characterization, including their surface functionalization, will be discussed in detail. AuNPs are very much preferable nanomaterials owing to exclusive optical, electrical, and photothermal features. AuNPs-based colorimetric biosensors are simple and possess great utility, yet these offer a robust technique to enable visual, quantitative analysis.

الإتاحة: https://doi.org/10.2174/0113862073293557240320065128Test

المؤلفون: Mittal, Roopal, Sharma, Shailesh, Kushwah, Ajay Singh, Yaqoob, Obaid, Kumari, Deepika

المصدر: Current Traditional Medicine ; volume 10, issue 1 ; ISSN 2215-0838

مصطلحات موضوعية: Complementary and alternative medicine, Drug Discovery

الوصف: Background: In recent decades, all-embracing research accounting for thousands of natural bioactive compounds have been detailed on behalf of their origin, pharmacological activity, active phytoconstituents, and therapeutic applications. Chalcones, secondary metabolites have shown therapeutic potential against various forms of inflammation, pain, and cancer in multiple research papers targeting their pathway inhibition and their significant therapeutic activity. Area Covered: Diverse aspects of chalcones have been focused on with their biological source, pathway inhibition, and pharmacological activity. Objectives: This study aims to focus on the chalcones being the origin of ethnopharmacological, possess extensive pharmacological activities, including anti-neoplastic, antimicrobial, anti-inflammatory, antioxidant, anti-acne, anti-aging, hepatoprotective, neuroprotective, psychoactive, anti-parasitic, and many others. Method: Chalcones display anti-inflammatory activity via COX-2, NO synthase, and TNF-α inhibition. Furthermore, comprehensive studies will be discussed with a viewpoint of the chalcones’s role in the alleviation of inflammation. According to recent advancements, chalcones clinically have been used in the treatment of inflammation, anti-aging, oxidative stress reduction, autophagy, and apoptosis. Conclusion: This article focuses on the molecular progression of inflammation and the chalcone role in combating inflammation by targeting inflammatory mediators and pathways.

الإتاحة: https://doi.org/10.2174/2215083809666230301085620Test
https://www.eurekaselect.com/214185/articleTest

المؤلفون: Mittal, Roopal, Sharma, Shailesh, Mittal, Amit, Kumar, Shubham, Kushwah, Ajay Singh

المصدر: Letters in Drug Design & Discovery ; volume 21, issue 2, page 270-288 ; ISSN 1570-1808

مصطلحات موضوعية: Drug Discovery, Pharmaceutical Science, Molecular Medicine

الوصف: Background: Chronic inflammation is usually combated with non-steroidal anti-inflammatory drugs (NSAIDs). However, long-term use of NSAIDs causes side effects comprising gastric ulceration, abdominal discomfort, lack of anti-thrombolytic activity, and myocardial infarction. Emerging reports indicate alteration of arachidonic acid metabolism, via cyclooxygenase and lipoxygenase pathways, being investigated as potential anti-inflammatory agents. There is a dynamic balance shift toward lipoxygenase on cyclooxygenase inhibition, therefore there is a need to identify naïve dual COX-2/5-LOX inhibitory agents with better therapeutic and minimal side effects. Objective: The current research focused on identifying a prospective natural candidate molecule (1,3- diphenyl-2-propene-1-one derivative) as a dual COX-2/5-LOX inhibitor by using structure-based database screening, molecular modelling, and in-silico ADMET analysis. Methods: Virtual screening using the ZINC database, molecular docking of potential compounds, and ADME analysis of hit compounds were performed. Results: A virtual library of 116 chalcone-based molecules was screened out. The molecules were docked for COX-2 (PDB ID-3LN1) and 5-LOX (PDB ID-3V99) enzymatic active pockets and resulted in compounds C96, C8, C83, C45, C20 better than zileuton. The potent compounds and zileuton showed good binding affinity in the range of -8.0 to -8.7Kcal/mol in the COX-2 and -7.0 to -8.7Kcal/mol in the 5- LOX active site respectively. These compounds were further subjected to ADME analysis giving two plausible lead compounds C45 and C64 following ideal pharmacokinetic properties. Conclusion: The research work provides abundant opportunities to explore computational and medicinal research areas which will facilitate the development of novel dual COX-2/5-LOX inhibitors in future experimental studies.

الإتاحة: https://doi.org/10.2174/1570180819666220523093435Test
https://www.eurekaselect.com/205104/articleTest

المؤلفون: Bhalla, Medha, Mittal, Roopal, Kumar, Manish, Bhatia, Rohit, Kushwah, Ajay Singh

المصدر: Current Drug Research Reviews ; volume 16, issue 3, page 333-348 ; ISSN 2589-9775

الوصف: Background: Cancer is amongst the most dreadful ailments of modern times, and its impact continuously worsens global health systems. Early diagnosis and suitable therapeutic agents are the prime keys to managing this disease. Metabolomics deals with the complete profiling of cells and physiological phenomena in their organelles, thus helping in keen knowledge of the pathological status of the disease. It has been proven to be one of the best strategies in the early screening of cancer. Objective: This review has covered the recent updates on the promising role of metabolomics in the identification of significant biochemical markers in cancer-prone individuals that could lead to the identification of cancer in the early stages. Methods: The literature was collected through various databases, like Scopus, PubMed, and Google Scholar, with stress laid on the last ten years' publications. Conclusion: It was assessed in this review that early recognition of cancerous growth could be achieved via complete metabolic profiling in association with transcriptomics and proteomics. The outcomes are rooted in various clinical studies that anticipated various biomarkers like tryptophan, phenylalanine, lactates, and different metabolic pathways associated with the Warburg effect. This metabolite imaging has been a fundamental step for the target acquisition, evaluation of predictive cancer biomarkers for early detection, and outlooks into cancer therapy along with critical evaluation. Significant efforts should be made to make this technique most reliable and easy.

الإتاحة: https://doi.org/10.2174/2589977516666230912120412Test
https://www.eurekaselect.com/220953/articleTest

المؤلفون: Singh, Nisha, Sharma, Rahul Kumar, Kushwah, Ajay Singh, Kumar, Manish

المصدر: Current Traditional Medicine ; volume 10, issue 4 ; ISSN 2215-0838

مصطلحات موضوعية: Complementary and alternative medicine, Drug Discovery

الوصف: Chronic fatigue syndrome (CFS) is a complex condition marked by severe exhaustion that lasts at least 6 months. The global prevalence of CFS ranging between 0.4% and 2.5% is growing. Women are affected by CFS more often than men. It is considered a common condition in developed countries. There is no approved treatment for CFS but symptoms can be managed and controlled persistent exhaustion causes significant impairment in daily routine activities. Lowered ATP synthesis, mitochondrial impairment, decreased oxidative phosphorylation, disruption of the hypothalamic–pituitary–adrenal (HPA) axis, and an imbalance of brain neurotransmitters play a major role in the pathophysiology of CFS. The purpose of the present study is to figure out the several plants that are used as a source of medication in chronic fatigue syndrome (CFS) and its current therapeutic approach. The Indian medicinal herbs described in this article are very efficacious in the management of chronic fatigue syndrome symptoms due to the presence of phytochemicals. This review article also covers the current therapeutic approach for chronic fatigue syndrome in a concise form that comprises CBT (Cognitive based therapy), GET (Graded exercise therapy), usage of immunoglobins, psychodynamic counseling, and yoga therapy that includes isometric yoga and yoga nidra are very beneficial in alleviating the symptoms of chronic fatigue syndrome. Antidepressants, immunomodulatory agents, and corticosteroids come under conventional medication for CFS. This article explores different Indian medicinal herbs, their pharmacological properties, and their potential role and current treatments for reducing the severity of symptoms of chronic fatigue syndrome.

الإتاحة: https://doi.org/10.2174/2215083810666230626115456Test
https://www.eurekaselect.com/218250/articleTest

المؤلفون: Gupta, Richa, Kushwah, Ajay Singh, Patil, Javesh Kashinath

المصدر: Food Supplements and Dietary Fiber in Health and Disease ; page 385-424 ; ISBN 9781003386308

الإتاحة: https://doi.org/10.1201/9781003386308-17Test

المؤلفون: Rather, Ishfaq Ahmad, Khan, Nadeem, Kushwah, Ajay Singh, Surampalli, Gurunath, Kumar, Manish

المصدر: Life Sciences ; volume 320, page 121543 ; ISSN 0024-3205

مصطلحات موضوعية: General Pharmacology, Toxicology and Pharmaceutics, General Biochemistry, Genetics and Molecular Biology, General Medicine

الإتاحة: https://doi.org/10.1016/j.lfs.2023.121543Test
https://api.elsevier.com/content/article/PII:S0024320523001777?httpAccept=text/xmlTest
https://api.elsevier.com/content/article/PII:S0024320523001777?httpAccept=text/plainTest