The reciprocal EC50 value as a convenient measure of the potency of a compound in bioactivity-guided purification of natural products.

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  • Additional Information
    • Affiliation:
      Pharmacology Unit, School of Medicine, Western Sydney University, Campbelltown, NSW 2560, Australia
      QBiotics Group Limited, PO Box 1, Yungaburra, Queensland, Australia
      NICM Health Research Institute, Western Sydney University, Sydney, Campbelltown, NSW 2560, Australia
    • Subject Terms:
    • Subject Terms:
    • Abstract:
      Identification of potent natural products is a challenging task in which sophisticated separation processes including HPLC are employed. The bioactivity of HPLC fractions is determined with a bioassay, and the most potent compounds are progressed to structural elucidation. In pharmacology, the potency of a compound is expressed as the half-maximal effective concentration (EC 50), which refers to the concentration of a drug that induces a response halfway between the baseline and maximum. While expressing the potency of a compound by its EC 50 value makes sense in a clinical context, it is counterintuitive in the context of bioactivity-guided purification, as the potency of a compound is inversely related to its EC 50 value, and the most potent compound is the one with the lowest EC 50. In natural products chemistry, it would be more logical if an increase in potency would be reflected by an increase of a parameter reflecting the potency. In this study, we introduce the term "effective dilution volume (EDV 50)" as the reciprocal of the EC 50 (1/EC 50). We show how the EDV 50 can be used to identify potent compounds in chromatographic separations, allowing to easily graph and identify anti-inflammatory compounds. We show two examples of this approach by overlaying an HPLC chromatogram with the EDV 50 to point out the most potent compounds. We hope that the EDV 50 will make the illustration of active fractions containing potent compounds in a chromatogram obvious for the reader and will become a useful graphic tool in the natural products literature in the future. Unlabelled Image
    • Journal Subset:
      Alternative/Complementary Therapies; Continental Europe; Europe; Peer Reviewed
    • ISSN:
      0367-326X
    • MEDLINE Info:
      NLM UID: 16930290R
    • Grant Information:
      This research has received grant from Qbiotics Group Ltd.
    • Publication Date:
      20200514
    • Publication Date:
      20200514
    • DOI:
      http://dx.doi.org/10.1016/j.fitote.2020.104598
    • Accession Number:
      143160089
  • Citations
    • ABNT:
      SINGH, A. et al. The reciprocal EC50 value as a convenient measure of the potency of a compound in bioactivity-guided purification of natural products. Fitoterapia, [s. l.], v. 143, p. N.PAG, 2020. DOI 10.1016/j.fitote.2020.104598. Disponível em: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=rzh&AN=143160089. Acesso em: 10 ago. 2020.
    • AMA:
      Singh A, Raju R, Mrad M, Reddell P, Münch G. The reciprocal EC50 value as a convenient measure of the potency of a compound in bioactivity-guided purification of natural products. Fitoterapia. 2020;143:N.PAG. doi:10.1016/j.fitote.2020.104598
    • APA:
      Singh, A., Raju, R., Mrad, M., Reddell, P., & Münch, G. (2020). The reciprocal EC50 value as a convenient measure of the potency of a compound in bioactivity-guided purification of natural products. Fitoterapia, 143, N.PAG. https://doi.org/10.1016/j.fitote.2020.104598
    • Chicago/Turabian: Author-Date:
      Singh, Ahilya, Ritesh Raju, Melissa Mrad, Paul Reddell, and Gerald Münch. 2020. “The Reciprocal EC50 Value as a Convenient Measure of the Potency of a Compound in Bioactivity-Guided Purification of Natural Products.” Fitoterapia 143 (June): N.PAG. doi:10.1016/j.fitote.2020.104598.
    • Harvard:
      Singh, A. et al. (2020) ‘The reciprocal EC50 value as a convenient measure of the potency of a compound in bioactivity-guided purification of natural products’, Fitoterapia, 143, p. N.PAG. doi: 10.1016/j.fitote.2020.104598.
    • Harvard: Australian:
      Singh, A, Raju, R, Mrad, M, Reddell, P & Münch, G 2020, ‘The reciprocal EC50 value as a convenient measure of the potency of a compound in bioactivity-guided purification of natural products’, Fitoterapia, vol. 143, p. N.PAG, viewed 10 August 2020, .
    • MLA:
      Singh, Ahilya, et al. “The Reciprocal EC50 Value as a Convenient Measure of the Potency of a Compound in Bioactivity-Guided Purification of Natural Products.” Fitoterapia, vol. 143, June 2020, p. N.PAG. EBSCOhost, doi:10.1016/j.fitote.2020.104598.
    • Chicago/Turabian: Humanities:
      Singh, Ahilya, Ritesh Raju, Melissa Mrad, Paul Reddell, and Gerald Münch. “The Reciprocal EC50 Value as a Convenient Measure of the Potency of a Compound in Bioactivity-Guided Purification of Natural Products.” Fitoterapia 143 (June 2020): N.PAG. doi:10.1016/j.fitote.2020.104598.
    • Vancouver/ICMJE:
      Singh A, Raju R, Mrad M, Reddell P, Münch G. The reciprocal EC50 value as a convenient measure of the potency of a compound in bioactivity-guided purification of natural products. Fitoterapia [Internet]. 2020 Jun [cited 2020 Aug 10];143:N.PAG. Available from: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=rzh&AN=143160089