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

• 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

抄録

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.

収録刊行物

• Ｔｈｅ　Ｊｏｕｒｎａｌ　ｏｆ　Ｔｏｘｉｃｏｌｏｇｉｃａｌ　Ｓｃｉｅｎｃｅｓ

  Ｔｈｅ　Ｊｏｕｒｎａｌ　ｏｆ　Ｔｏｘｉｃｏｌｏｇｉｃａｌ　Ｓｃｉｅｎｃｅｓ 40 (2), 223-233, 2015

  一般社団法人　日本毒性学会

キーワード

• Bongkrekic acid
• Peroxisome proliferator-activated receptor γ
• Adenine nucleotide translocase
• 15-Lipoxygenase
• Apoptosis

詳細情報

• CRID: 1390001204905868032
• NII論文ID: 130004904039
• NII書誌ID: AN00002808
• DOI: 10.2131/jts.40.223
• ISSN: 18803989
• ISSN: 03881350
• NDL書誌ID: 026318992
• PubMed: 25786526
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I026318992
• Web Site: https://www.jstage.jst.go.jp/article/jts/40/2/40_223/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2016001687
• 本文言語コード: en
• データソース種別:
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  • Crossref
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