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Peroxisome proliferator-activated receptor transactivational effects in HepG2 cells of cembranoids from the soft coral Lobophytum crassum Von Marenzeller

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Abstract

Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors that regulate the expression of multiple genes involved in metabolic, anti-inflammatory, and developmental processes. This study evaluated the PPARs transactivational effects of thirteen cembranoid diterpenoids 1–13 from the soft coral Lobophytum crassum, using PPAR-responsive elements–luciferase reporter and GAL4–PPAR chimera assays. All isolated compounds activated the transcription of PPARs in a dose-dependent manner, with EC50 values ranging from 2.07 ± 1.73 to 130.20 ± 1.85 μM. Moreover, compounds 6–9 affected the transactivation of all three PPAR types, PPARα, γ, β(δ), in a dose-dependent manner, with EC50 values in a ranging from 11.92 ± 1.23 to 122.50 ± 2.12 μM. These results provide a scientific rationale for further studies on the soft coral L. crassum and its diterpenoid constituents to develop medicinal products against inflammatory and metabolic diseases.

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Acknowledgments

This study was supported by a grant from the Vietnam National Foundation for Science & Technology Development (Project No: 104.01-2012.37) and the framework of international cooperation program managed by National Research Foundation of Korea (2012-K2A1A2032970) and Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Education, Science, and Technology (2012-0006681), Republic of Korea.

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Authors and Affiliations

  1. Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Nghiado, Caugiay, Hanoi, Vietnam

    Nguyen Phuong Thao, Bui Thi Thuy Luyen, Le Duc Dat, Nguyen Xuan Cuong, Nguyen Hoai Nam, Phan Van Kiem & Chau Van Minh

  2. College of Pharmacy, Chungnam National University, Daejeon, 305-764, Republic of Korea

    Nguyen Phuong Thao, Bui Thi Thuy Luyen, Nguyen Thi Thanh Ngan, Le Duc Dat, Seok Bean Song & Young Ho Kim

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  1. Nguyen Phuong Thao
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  2. Bui Thi Thuy Luyen
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  4. Le Duc Dat
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  5. Nguyen Xuan Cuong
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  9. Chau Van Minh
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Correspondence to Chau Van Minh or Young Ho Kim.

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Thao, N.P., Luyen, B.T.T., Ngan, N.T.T. et al. Peroxisome proliferator-activated receptor transactivational effects in HepG2 cells of cembranoids from the soft coral Lobophytum crassum Von Marenzeller . Arch. Pharm. Res. 38, 769–775 (2015). https://doi.org/10.1007/s12272-014-0382-9

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