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Molecular insights to explore abietane diterpenes as new LOX inhibitors

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Abstract

Lipoxygenase (LOX) inhibitors are well known for their anti-inflammatory effects derived from both natural products and synthetic sources. Taxus wallichiana Zucc is traditionally used in the treatment of various diseases including inflammation. In a recent study, it was used to conduce the isolation of the bioactive compounds from Taxus wallichiana Zucc. thanks to its ethnopharmacological use in diseases including inflammation. Phytochemical studies lead to the isolation of abietane diterpenoids, namely Taxusabietane C (TC) and Taxamairin F (TF). Test compounds showed significant LOX inhibitory effects. IC50 values of TC and TF were 69 ± 0.31 and 73 ± 0.14 μM, respectively. The standard compound Baicalein and Tenidap sodium showed the IC50 value being 22.1 ± 0.03 and 41.6 ± 0.02 μM. Significant LOX inhibitory activities were supported by a molecular docking simulation to explore molecular interactions of the compounds with the active (catalytic) site of LOX.

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Authors and Affiliations

  1. Department of Pharmacy, University of Peshawar, Peshawar, 25120, Pakistan

    Inamullah Khan, Amir Zada Khan &  Samiullah

  2. Institute of Chemical Sciences, University of Peshawar, Peshawar, 25120, Pakistan

    Muhammad Nisar & Hazrat Amin

  3. Department of Chemical Sciences, University of Naples “Federico II”, Naples, Italy

    Armando Zarrelli & Giovanni Di Fabio

  4. Pharmacology Section, PCSIR Lab Complex, Peshawar, 25000, Pakistan

    Farah Gul & Syed Naeemuddin Gilani

  5. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan

    Muhammad Raza Shah

Authors
  1. Inamullah Khan
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  2. Muhammad Nisar
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  3. Armando Zarrelli
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  4. Giovanni Di Fabio
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  5. Farah Gul
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  6. Syed Naeemuddin Gilani
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  7. Muhammad Raza Shah
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  8. Amir Zada Khan
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  9. Samiullah
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  10. Hazrat Amin
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Corresponding authors

Correspondence to Inamullah Khan or Armando Zarrelli.

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Khan, I., Nisar, M., Zarrelli, A. et al. Molecular insights to explore abietane diterpenes as new LOX inhibitors. Med Chem Res 22, 5809–5813 (2013). https://doi.org/10.1007/s00044-013-0559-7

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  • DOI: https://doi.org/10.1007/s00044-013-0559-7

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