Vol 19, No 3 (2024)
- Year: 2024
- Articles: 6
- URL: https://rjonco.com/2772-4344/issue/view/10031
Medicine
Current Influenza Antiviral Drug Strategy Limitations and Future Development of both Preventative and Intervention Antiviral Therapies
179-181
Study of Antimicrobial Resistance (AMR) in Shigella spp. in India
Abstract
Antimicrobial agents are essential in reducing illness and mortality brought on by infectious diseases in both humans and animals. However, the therapeutic effect of antibiotics has diminished due to an increase in antimicrobial drug resistance (AMR).
:This article provides a retrospective analysis of AMR in Shigella infections in India, showing a rise in resistance that has contributed to a global burden.
:Shigella spp. are widespread and the second-leading cause of diarrheal death in people of all ages. The frequency and mortality rates of Shigella infections are decreased by antibiotic treatment. However, the growth of broad-spectrum antibiotic resistance is making it more difficult to treat many illnesses. Reduced cell permeability, efflux pumps, and the presence of enzymes that break down antibiotics are the causes of resistance.
:AMR is a multifaceted and cross-sectoral problem that affects humans, animals, food, and the environment.
:As a result, there is a growing need for new therapeutic approaches, and ongoing surveillance of Shigella spp. infections which should definitely be improved for disease prevention and management.
:This review emphasizes on the epidemiological data of India, and antimicrobial resistance in Shigella spp.
182-196
A Landscape on Lymphatic Filariasis with its Effects and Recent Advanced Treatments
Abstract
Lymphatic filariasis is an infection caused by parasites that poses a significant health, social, and economic burden, affecting a vast population that exceeds 120 million individuals globally. The Etiology of the infection is attributed to three nematode parasites, namely Wuchereria bancrofti, B. timori, and Brugia malayi, as well as which are phylogenetically related. These parasites are transmitted to humans via mosquitoes belonging to the Anopheles, Aedes genera, and Culex. As per the estimation provided by the WHO, the current number of individuals infected with filariasis stands at approximately 120 million across 81 countries. Furthermore, it is estimated that around 1.34 billion individuals reside in regions that are endemic to filariasis, thereby putting them at risk of contracting the disease. Different synthetic drugs such as Ivermectin, Doxycycline, Albendazole, and Suramin are used in the treatment. Some natural plants are Azadirachta indica, Tinospora cordifolia, Zingiber officinal, as well as, some marine sources are also included for better treatment. We also touch briefly on a few additional filarial diseases. Although there are only a few medications available to treat filariasis, their frequent usage may result in drug resistance. Furthermore, there is no effective vaccination for the treatment of filariasis. Due to these restrictions, it has been crucial to create new anti-filarial medications, which motivates researchers to find novel pharmaceuticals with anti-filarial action. In this article, we examine the latest achievements in the anti-filarial area, including the many forms of filariasis and their historical contexts, elimination programmes, various therapeutic classes (both synthetic and natural), investigated product-derived targets as well as clinical investigations.
197-215
Green Chemistry and In silico Techniques for Synthesis of Novel Pyranopyrazole and Pyrazolo-pyrano-pyrimidine Derivatives as Promising Antifungal Agents
Abstract
Background:Every year Invasive Fungal Infections (IFI) are globally affecting millions of people. Candida albicans and Aspergillus niger have been reported as the most infectious and mortality-inducing fungal strains among all pathogenic fungi.
Aim & Objective:To tackle this problem in the current study Pyranopyrazoles and Pyrazolopyrano- pyrimidine derivatives were developed using molecular hybridization, green chemistry and one-pot multicomponent reaction.
Material and Method:In the present work, New Chemical entities (NCEs) were developed on the basis of Structure activity relationship. All designed NCEs were screened for ADMET studies using the QikProp module of Schrodinger software. NCEs with zero violations were further docked on the crystal structure of 14α demethylase, cytochrome P450 and thymidine synthase (PDB ID: 5V5Z, 7SHI, 1BID). Selected molecules were synthesized using green chemistry techniques and evaluated for in vitro antifungal activity against Candida albicans and Aspergillus niger.
Result and Discussion:Designed NCEs (B1-12 and C1-11) showed favorable results in ADMET studies. In the docking study six compounds from series-B and five molecules from series- C showed good dock score and binding interaction when compared with the standard drugs. Compounds B-3 and C-4 showed the highest zone of inhibition activity against Candida albicans, where as B-1 and C-3 had shown highest zone of inhibition activity against Aspergillus niger.
Conclusion:Bicyclic ring (series B) showed better activity as compare to fused tricyclic ring (series C).
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Synthesis of Ursolic Acid-based Hybrids: In Vitro Antibacterial, Cytotoxicity Studies, In Silico Physicochemical and Pharmacokinetic Properties
Abstract
Background:Background
Objectives:Amine-linked ursolic acid-based hybrid compounds were prepared in good yields in the range of 60-68%.
Methods:Their molecular structures were successfully confirmed using different spectroscopic methods including 1H/13C NMR, UHPLC-HRMS and FTIR spectroscopy. The in vitro cytotoxicity of some of these hybrid molecules against three human tumour cells, such as MDA-MB23, MCF7, and HeLa was evaluated using the MTT colorimetric method.
Result:Their antibacterial efficacy was evaluated against eleven bacterial pathogens using a serial dilution assay. Majority of the bacterial strains were inhibited significantly by compounds 17 and 24, with the lowest MIC values in the range of 15.3-31.25 µg/mL. Compound 16 exhibited higher cytotoxicity against HeLa cells than ursolic acid, with an IC50 value of 43.64 g/mL.
Conclusion:The in vitro antibacterial activity and cytotoxicity of these hybrid compounds demonstrated that ursolic acid-based hybrid molecules are promising compounds. Further research into ursolic acid-based hybrid compounds is required.
232-253
The Efficacy of Colchicine as an Adjunct Therapy in Non-hospitalized COVID-19 Patients: A Randomized Placebo-Controlled Trial
Abstract
Background:The therapeutic potential of oral colchicine administration may help combat COVID-19 infection due to reduced disease severity and mortality risk.
Objective:This randomized trial aimed to assess the effect of colchicine treatment on the inflammatory and hematologic markers as well as clinical features in non-hospitalized patients with mild-to-moderate COVID-19 disease.
Method:In the present placebo-controlled randomized trial, 80 non-hospitalized COVID-19 patients were enrolled and followed for 14 days. Subjects randomly received oral colchicine or placebo tablets once a day for two weeks. The fever and cough clinical signs, as well as Creactive protein (CRP) and lymphopenia, were evaluated through the follow-up.
Results:No significant between-group differences were observed in terms of the duration of clinical symptoms, CRP, and lymphopenia at 0, 7, and 14 days of intervention. Although the proportion of participants with fever, cough, positive CRP, and lymphopenia was higher reduced in the colchicine group than the placebo during treatment, no significant differences were found between groups. Due to no adverse effects detected in this trial, colchicine therapy was well-tolerated and safe.
Conclusion:Our findings revealed that colchicine adjuvant therapy had no beneficial effect on clinical and para-clinical parameters in non-hospitalized COVID-19 patients during 14 days of intervention. The present trial does not support colchicine as a potential treatment against COVID-19 disease.
Clinical trial Registration:The present study protocol was approved by the IRCT (IRCT20200408046990N2, https://en.irct.ir/trial/47468).
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