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Anti-adipogenic activity of Carduus crispus and its constituent apigenin in 3T3-L1 adipocytes by downregulating PPARγ and C/EBPα

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Abstract

Carduus crispus, native to Europe and Asia, is a traditional herbal medicine used for treating inflammatory disorders in Korea. Obesity is characterized by a state of chronic inflammation with increased inflammatory markers along with the expression and release of inflammation-related adipokines. Most anti-obesity drugs have been developed based on this concept. Our research for anti-obesity agents derived from C. crispus utilized the 3T3-L1 cell line. The methanol extract was initially screened and exhibited significant inhibition of adipogenesis in 3T3-L1 adipocytes. Among five liquid–liquid partition fractions, the ethyl acetate (EA) fraction showed the most potent suppressive effect compared with hexane, chloroform, n-butanol, and water. The EA fraction was considered for further study because of the presence of abundant polyphenols, including flavonoids. To isolate the active components from the EA fraction, elution–extrusion countercurrent chromatography was used. Among the seven fractions from the EA layer, fraction 6 inhibited lipid accumulation as well as CCAAT/enhancer-binding protein alpha and peroxisome proliferator-activated receptor gamma protein expression levels. The active component apigenin (fraction 6) was confirmed using high-performance liquid chromatography, electrospray ionization mass spectrometry, and one-dimensional nuclear magnetic resonance spectroscopy. The present data suggest that apigenin is one of the main bioactive compounds from C. crispus for inhibiting adipogenesis in 3T3-L1 adipocytes via the activation of AMP-activated protein kinase.

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Abbreviations

HSCCC:

High-speed countercurrent chromatography

EECCC:

Elution–extrusion countercurrent chromatography

CH:

Hexane-soluble layer of the methanol extract from C. crispus

CC:

Chloroform-soluble layer of the methanol extract from C. crispus

CE:

Ethyl acetate-soluble layer of the methanol extract from C. crispus

CB:

n-Butanol-soluble layer of the methanol extract from C. crispus

CW:

Water-soluble layer of the methanol extract from C. crispus

DMI:

Cocktail of 1 μM dexamethasone, 0.5 mM IBMX, and 1 μg/mL insulin

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Acknowledgments

This work was supported by Grants (NRF-2013R1A1A2A10005492 and MRC 2009-93146) from the National Research Foundation of Korea.

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Authors and Affiliations

  1. Natural Products Research Institute, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 151-742, Republic of Korea

    Yoo Na Hong, Jaemoo Chun & Yeong Shik Kim

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  1. Yoo Na Hong
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  2. Jaemoo Chun
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Correspondence to Yeong Shik Kim.

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Hong, Y.N., Chun, J. & Kim, Y.S. Anti-adipogenic activity of Carduus crispus and its constituent apigenin in 3T3-L1 adipocytes by downregulating PPARγ and C/EBPα. Eur Food Res Technol 242, 1555–1563 (2016). https://doi.org/10.1007/s00217-016-2656-6

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  • DOI: https://doi.org/10.1007/s00217-016-2656-6

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