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Antiplasmodial activity-aided isolation and identification of quercetin-4’-methyl ether in Chromolaena odorata leaf fraction with high activity against chloroquine-resistant Plasmodium falciparum

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Abstract

The present study was undertaken to evaluate the antiplasmodial activity of Chromolaena odorata leaf extract and gradient fractions through in vivo and in vitro tests, aimed at identifying its antiplasmodial constituents. Sub-fractions obtained from the most active gradient fraction were further tested for cytotoxicity against THP-1 cells, chloroquine-sensitive (HB3) and chloroquine-resistant (FCM29) Plasmodium falciparum. Our results showed the dichloromethane gradient fraction was most effective, significantly (P < 0.05) suppressing infection by 99.46 % at 100 mg/kg body weight. Amongst its 13 sub-fractions (DF1–DF13), DF11 was highly active, with IC50 of 4.8 and 6.74 μg/ml against P. falciparum HB3 and FCM29, respectively. Cytotoxicity of DF11 was estimated to be above 50 μg/ml, and its separation by column chromatography yielded a flavonoid which was characterized as 3, 5, 7, 3’ tetrahydroxy-4’-methoxyflavone from its spectroscopic data. It significantly suppressed infection (65.43–81.48 %) in mice at 2.5–5 mg/kg doses and compared favourably with the effects of chloroquine and artemisinin. It may therefore serve as a useful phytochemical and antiplasmodial activity marker of C. odorata leaves, which exhibit potential for development as medicine against malaria.

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Acknowledgments

The authors are grateful to Ranarivelo Lalasoanirina and Ratsimbasson Michel of CNARP Madagascar for assistance in conducting the antiplasmodial assays. Ezenyi IC is thankful to Dr Swati Joshi, Dr Dhiman Sarkar, and Dr Sourav Pal of the National Chemical Laboratory Pune and to the Government of India for the RTFDCS fellowship. We also acknowledge Dr. S. Okhale and Mr Abu Garba for conducting HPLC fingerprinting and melting point analysis, respectively. The study was supported by funds from L’Oreal-UNESCO regional fellowship for women in science, awarded to Ezenyi IC.

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The authors declare that they have no conflict of interest.

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Authors and Affiliations

  1. Department of Pharmacology and Toxicology, National Institute for Pharmaceutical Research and Development, Idu, Abuja, Nigeria

    I. C. Ezenyi & O. A. Salawu

  2. Organic Chemistry Division, National Chemical Laboratory, Pune, 411008, India

    I. C. Ezenyi & R. Kulkarni

  3. Centre for Nanomedicine and Biophysical Drug Delivery, Department of Pharmaceutical Technology and Raw Material Development, National Institute for Pharmaceutical Research and Development, Idu, Abuja, Nigeria

    M. Emeje

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  1. I. C. Ezenyi
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  2. O. A. Salawu
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  3. R. Kulkarni
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  4. M. Emeje
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Correspondence to I. C. Ezenyi.

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Ezenyi, I.C., Salawu, O.A., Kulkarni, R. et al. Antiplasmodial activity-aided isolation and identification of quercetin-4’-methyl ether in Chromolaena odorata leaf fraction with high activity against chloroquine-resistant Plasmodium falciparum . Parasitol Res 113, 4415–4422 (2014). https://doi.org/10.1007/s00436-014-4119-y

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