Chikungunya is a notorious viral infection, which affects a large segment of world populations in absence of vaccines and antivirals. The current study evaluates of anti-chikungunya activities of Psidium guajava leaves extract and their green synthesized silver nanoparticles. Green synthesized nanoparticles were well characterized for their size and stability by dynamic light scattering (DLS), zeta potential, scanning electron microscopy (SEM) and their functional groups were analyzed by FTIR. Maximum non-toxic doses (MNTD) of extracts and nanoparticles were analysed by using Vero cell-lines. Anti-chikungunya activities of extracts and nano-particles were determined on Vero cells and their effects on cell viability were measured by MTT assay. The P. guajava nano-particles and extracts revealed the anti-chikungunya activities in the Vero cell. The cells viability was increased by 40% and 60% as compared to the virus control, when these cells were treated with MNTD of P. guajava nano-particles and extracts, respectively. To know the reason for antiviral activity, molecular docking of phytochemicals was done against a replication essential cysteine protease (nsP2) of Chikungunya. It was found that phytochemicals; Longifollen and Quercetin showed the minimum binding energy with nsP2. P. guajava extracts can be exploited to develop an effective anti-chikungunya agent. In the absence of CHIKV vaccines and antivirals, P. guajava may be used to develop rapid, responsive, specific, and cost-effective anti-chikungunya agents. Supplementary Information The online version contains supplementary material available at 10.1007/s13337-021-00685-4.

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Abstract:: Enzyme prodrug therapy has gained momentum in the recent years due to their ability to improve therapeutic index (benefits versus toxic side-effects) and efficacy of chemotherapy in cancer treatment. Inactive prodrugs used in this system are converted into active anti-cancerous drugs by enzymes, specifically within the tumor cells. This therapy involves three components namely prodrug, enzyme and gene delivery vector. Past reports have clearly indicated that the choice of enzyme used, is the major determinant for the success of this therapy. Generally, enzymes from non-human sources are employed to avoid off-target toxicity. Exogenous enzymes also give a better control to the clinician regarding the calibration of treatment by site-specific initiation. Amongst these exo-enzymes, microbial enzymes are preferred due to their high productivity, stability and ease of manipulation. The present review focuses on the commonly used microbial enzymes particularly cytosine deaminase, nitroreductase, carboxypeptidase, purine nucleoside phosphorylase in prodrug activation therapy. Various aspects viz. source of the enzymes, types of cancer targeted, mode of action and efficacy of the enzyme/prodrug system, efficient vectors used and recent research developments of each of these enzymes are comprehensively elaborated. Further, the results of the clinical trials and various strategies to improve their clinical applicability are also discussed.

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