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Anti-inflammatory and anticholinesterase activity of six flavonoids isolated from Polygonum and Dorstenia species

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Abstract

This study was aimed at investigating the anti-inflammatory and anticholinesterase activity of six naturally occurring flavonoids: (−) pinostrobin (1), 2′,4′-dihydroxy-3′,6′-dimethoxychalcone (2), 6-8-diprenyleriodictyol (3), isobavachalcone (4), 4-hydroxylonchocarpin (5) and 6-prenylapigenin (6). These compounds were isolated from Dorstenia and Polygonum species used traditionally to treat pain. The anti-inflammatory activity was determined by using the Griess assay and the 15-lipoxygenase inhibitory activity was determined with the ferrous oxidation-xylenol orange assay. Acetylcholinesterase inhibition was determined by the Ellman’s method. At the lowest concentration tested (3.12 µg/ml), compounds 2, 3 and 4 had significant NO inhibitory activity with 90.71, 84.65 and 79.57 % inhibition respectively compared to the positive control quercetin (67.93 %). At this concentration there was no significant cytotoxicity against macrophages with 91.67, 72.86 and 70.86 % cell viability respectively, compared to 73.1 % for quercetin. Compound 4 had the most potent lipoxygenase inhibitory activity (IC50 of 25.92 µg/ml). With the exception of (−) pinostrobin (1), all the flavonoids had selective anticholinesterase activity with IC50 values ranging between 5.93 and 8.76 µg/ml compared to the IC50 4.94 µg/ml of eserine the positive control. These results indicate that the studied flavonoids especially isobavachalcone are potential anti-inflammatory natural products that may have the potential to be developed as therapeutic agents against inflammatory conditions and even Alzheimer’s disease.

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Acknowledgments

The University of Pretoria provided a postdoctoral fellowship to JPD. The National Research Foundation (NRF) and Medical Research Council (MRC) provided funding to support this study.

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The authors declare that they have no conflict of interest.

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Authors and Affiliations

  1. Phytomedicine Programme, Department of Paraclinical Sciences, Faculty of Veterinary Science, University of Pretoria, Private Bag X04, Onderstepoort, Pretoria, 0110, South Africa

    Jean Paul Dzoyem & Jacobus N. Eloff

  2. Department of Biochemistry, Faculty of Science, University of Dschang, P.O. Box 67, Dschang, Cameroon

    Jean Paul Dzoyem

  3. Department of Organic Chemistry, Faculty of Science, University of Dschang, P.O. Box 67, Dschang, Cameroon

    Antoine H. L. Nkuete

  4. Faculty of Medicine and Biomedical Sciences, University of Yaounde I, P.O. Box 1364, Dschang, Cameroon

    Barthelemy Ngameni

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  1. Jean Paul Dzoyem
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  2. Antoine H. L. Nkuete
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  3. Barthelemy Ngameni
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  4. Jacobus N. Eloff
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Correspondence to Jean Paul Dzoyem or Jacobus N. Eloff.

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Dzoyem, J.P., Nkuete, A.H.L., Ngameni, B. et al. Anti-inflammatory and anticholinesterase activity of six flavonoids isolated from Polygonum and Dorstenia species. Arch. Pharm. Res. 40, 1129–1134 (2017). https://doi.org/10.1007/s12272-015-0612-9

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