Bongkrekic acid as a selective activator of the peroxisome proliferator-activated receptor γ (PPARγ) isoform

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  • Okazaki Hiroyuki
    Drug Innovation Research Center, Daiichi University of Pharmacy
  • Takeda Shuso
    Department of Molecular Biology, Daiichi University of Pharmacy Laboratory of Xenobiotic Metabolism and Environmental Toxicology, Faculty of Pharmaceutical Sciences, Hiroshima International University (HIU)
  • Ikeda Eriko
    Department of Molecular Biology, Daiichi University of Pharmacy
  • Fukunishi Yoshifumi
    Molecular Profiling Research Center for Drug Discovery (molprof), National Institute of Advanced Industrial Science and Technology (AIST)
  • Ishii Hiroyuki
    Department of Molecular Biology, Daiichi University of Pharmacy
  • Taniguchi Aya
    Department of Molecular Biology, Daiichi University of Pharmacy
  • Tokuyasu Miki
    Department of Molecular Biology, Daiichi University of Pharmacy
  • Himeno Taichi
    Department of Molecular Biology, Daiichi University of Pharmacy
  • Kakizoe Kazuhiro
    Department of Molecular Biology, Daiichi University of Pharmacy
  • Matsumoto Kenji
    Institute for Materials Chemistry and Engineering, Kyushu University
  • Shindo Mitsuru
    Institute for Materials Chemistry and Engineering, Kyushu University
  • Aramaki Hironori
    Drug Innovation Research Center, Daiichi University of Pharmacy Department of Molecular Biology, Daiichi University of Pharmacy

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Abstract

Bongkrekic acid (BKA), an antibiotic isolated from Pseudomonas cocovenans, is an inhibitory molecule of adenine nucleotide translocase. Since this translocase is a core component of the mitochondrial permeability transition pore (MPTP) formed by apoptotic stimuli, BKA has been used as a tool to abrogate apoptosis. However, the other biochemical properties of BKA have not yet been resolved. Although the definition of a fatty acid is a carboxylic acid (-COOH) with a long hydrocarbon chain (tail), when focused on the chemical structure of BKA, the molecule was revealed to be a branched unsaturated tricarboxylic acid that resembled the structure of polyunsaturated fatty acids (PUFAs). Peroxisome proliferator-activated receptors (PPARs) consist of a subfamily of three isoforms: α, β, and γ, the ligands of which include PUFAs. Using completely synthesized BKA together with simplified BKA derivatives (purity: > 98%), we herein demonstrated the utility of BKA as a selective activator of the human PPARγ isoform, which may not be associated with the anti-apoptotic nature of BKA. We also discussed the possible usefulness of BKA.

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