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In Vitro Evaluation of Anti-Parasitic Activities of Quinolone-Coumarin Hybrids Derived from Fluoroquinolones and Novobiocin Against Toxoplasma gondii

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Abstract

Purpose

Toxoplasmosis is caused by the parasite Toxoplasma gondii (T. gondii). In immunocompetent individuals, the infection is often asymptomatic; however, in expectant mothers and those with immune system deficiencies, complications may arise. Consequently, there is a need for new drugs that cause minimal damage to host cells. The purpose of this study was to investigate the in vitro antiparasitic efficacy of quinolone–coumarin hybrids QC1–QC12, derived from quinolone antibacterials and novobiocin, against T. gondii.

Methods

The derivatives were compared with novobiocin and ciprofloxacin during testing, with pyrimethamine used as a positive control. We conducted the MTT assay to examine the anti-toxoplasmic effects of the test compounds and novobiocin. Evaluation included the infection and proliferation indices, as well as the size and number of plaques, based on the viability of both healthy and infected cells.

Results

The in vitro assays revealed that QC1, QC3, QC6, and novobiocin, with selectivity indices (SIs) of 7.27, 13.43, and 8.23, respectively, had the least toxic effect on healthy cells and the highest effect on infected cells compared to pyrimethamine (SI = 3.05). Compared to pyrimethamine, QC1, QC3, QC6, and novobiocin Without having a significant effect on cell viability, demonstrated a significant effect on reducing in both infection index and proliferation index, in addition to reducing the quantity and dimensions of plaques ( P < 0.05).

Conclusion

Based on our results, QC1, QC3, QC6, and novobiocin due to their significant therapeutic effects could be considered as potential new leads in the development of novel anti-Toxoplasma agents.

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Acknowledgements

Hereby, the authors of the current study express their appreciation for the financial assistance they received from the Mazandaran University of Medical Sciences in Sari, Iran. The Mazandaran University of Medical Sciences Student Research Committee is gratefully acknowledged by the authors.

Funding

This research received no specific grant from any funding agency, commercial or not-for-profit sectors.

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Authors and Affiliations

  1. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran

    Saeed Emami

  2. Toxoplasmosis Research Center, Communicable Disease Institute, Mazandaran University of Medical Sciences, Sari, Iran

    Mitra Sadeghi, Shayesteh Shahdin, Ahmad Daryani, Seyed Abdollah Hosseini, Mahboobeh Montazeri, Zahra Hosseini Nejad & Shahabeddin Sarvi

  3. Student Research Committee, Mazandaran University of Medical Sciences, Sari, Iran

    Mitra Sadeghi

  4. Department of Parasitology and Mycology, School of Medicine, Mazandaran University of Medical Science, Sari, Iran

    Ahmad Daryani, Seyed Abdollah Hosseini & Shahabeddin Sarvi

  5. Biostatistics Department, Mazandaran University of Medical Sciences, Sari, Iran

    Alireza Khalilian

  6. Department of Parasitology, Tarbiat Modares University of Medical Science, Tehran, Iran

    Majid Pirestani

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  1. Saeed Emami
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Contributions

The research’s design involved SHS, SE, and AD. The experiments were carried out by MS, MM, and ShSh. Data was examined by Akh. The essay was written by MS, ZHN, SAH and MP. The manuscript was heavily corrected by SE and SHS. All authors read and an approved the final manuscript.

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Correspondence to Shahabeddin Sarvi.

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Emami, S., Sadeghi, M., Shahdin, S. et al. In Vitro Evaluation of Anti-Parasitic Activities of Quinolone-Coumarin Hybrids Derived from Fluoroquinolones and Novobiocin Against Toxoplasma gondii. Acta Parasit. (2024). https://doi.org/10.1007/s11686-024-00852-9

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