Anti-adipogenic activity of compounds isolated from Idesia polycarpa on 3T3-L1 cells

Mina Lee, Hyang Hwa Lee, Jin Ku Lee, Sang Kyu Ye, Seung Hyun Kim, Sang Hyun Sung

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

Recently, obesity is a complex multifactorial chronic disease increasing the risk for type 2 diabetes, coronary heart disease and hypertension, and has become a major worldwide health problem. In the course of screening natural products employing 3T3-L1 cells as an in vitro system, the methanol extract of Idesia polycarpa Maxim. Fruits (Flacourtiaceae) significantly inhibited adipocyte differentiation by measuring lipid contents using oil red O staining. One new compound, 6-(oxymethyl)-2-hydroxyphenyl-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside (8), was isolated along with nine known compounds (1-7 and 9-10) from CHCl3 and n-BuOH fractions of the methanol extract of I. polycarpa fruits. Among them, idescarpin (1) with 1-hydroxy-6-oxo-2-cyclohexenecarboxylate moiety showed the most potent inhibitory activity on adipocyte differentiation with IC50 values of 23.2 μM. Idescarpin (1) dramatically suppressed the induction of C/EBPα expression, whereas it significantly increased the induction of PPARγ expression, supported by quantitative real time PCR and Western blot analysis. The down-regulation in mRNA levels of SREBP1c, SCD-1, and FAS by idescarpin (1) during adipocyte differentiation revealed that the inhibition of adipocyte differentiation was mediated by the regulation of lipogenesis. Taken together, we suggest that idescarpin (1) shows a great potential against obesity and diabetes though the anti-adipogenic activity and the up-regulation of PPARγ.

Original languageEnglish
Pages (from-to)3170-3174
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number11
DOIs
Publication statusPublished - 2013 Jun 1

Fingerprint

3T3-L1 Cells
Adipocytes
Medical problems
Peroxisome Proliferator-Activated Receptors
Fruits
Flacourtiaceae
Methanol
Fruit
Obesity
Lipogenesis
Biological Products
Type 2 Diabetes Mellitus
Inhibitory Concentration 50
Coronary Disease
Real-Time Polymerase Chain Reaction
Screening
Chronic Disease
Up-Regulation
Down-Regulation
Western Blotting

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Lee, Mina ; Lee, Hyang Hwa ; Lee, Jin Ku ; Ye, Sang Kyu ; Kim, Seung Hyun ; Sung, Sang Hyun. / Anti-adipogenic activity of compounds isolated from Idesia polycarpa on 3T3-L1 cells. In: Bioorganic and Medicinal Chemistry Letters. 2013 ; Vol. 23, No. 11. pp. 3170-3174.
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Anti-adipogenic activity of compounds isolated from Idesia polycarpa on 3T3-L1 cells. / Lee, Mina; Lee, Hyang Hwa; Lee, Jin Ku; Ye, Sang Kyu; Kim, Seung Hyun; Sung, Sang Hyun.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 11, 01.06.2013, p. 3170-3174.

Research output: Contribution to journalArticle

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T1 - Anti-adipogenic activity of compounds isolated from Idesia polycarpa on 3T3-L1 cells

AU - Lee, Mina

AU - Lee, Hyang Hwa

AU - Lee, Jin Ku

AU - Ye, Sang Kyu

AU - Kim, Seung Hyun

AU - Sung, Sang Hyun

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N2 - Recently, obesity is a complex multifactorial chronic disease increasing the risk for type 2 diabetes, coronary heart disease and hypertension, and has become a major worldwide health problem. In the course of screening natural products employing 3T3-L1 cells as an in vitro system, the methanol extract of Idesia polycarpa Maxim. Fruits (Flacourtiaceae) significantly inhibited adipocyte differentiation by measuring lipid contents using oil red O staining. One new compound, 6-(oxymethyl)-2-hydroxyphenyl-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside (8), was isolated along with nine known compounds (1-7 and 9-10) from CHCl3 and n-BuOH fractions of the methanol extract of I. polycarpa fruits. Among them, idescarpin (1) with 1-hydroxy-6-oxo-2-cyclohexenecarboxylate moiety showed the most potent inhibitory activity on adipocyte differentiation with IC50 values of 23.2 μM. Idescarpin (1) dramatically suppressed the induction of C/EBPα expression, whereas it significantly increased the induction of PPARγ expression, supported by quantitative real time PCR and Western blot analysis. The down-regulation in mRNA levels of SREBP1c, SCD-1, and FAS by idescarpin (1) during adipocyte differentiation revealed that the inhibition of adipocyte differentiation was mediated by the regulation of lipogenesis. Taken together, we suggest that idescarpin (1) shows a great potential against obesity and diabetes though the anti-adipogenic activity and the up-regulation of PPARγ.

AB - Recently, obesity is a complex multifactorial chronic disease increasing the risk for type 2 diabetes, coronary heart disease and hypertension, and has become a major worldwide health problem. In the course of screening natural products employing 3T3-L1 cells as an in vitro system, the methanol extract of Idesia polycarpa Maxim. Fruits (Flacourtiaceae) significantly inhibited adipocyte differentiation by measuring lipid contents using oil red O staining. One new compound, 6-(oxymethyl)-2-hydroxyphenyl-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside (8), was isolated along with nine known compounds (1-7 and 9-10) from CHCl3 and n-BuOH fractions of the methanol extract of I. polycarpa fruits. Among them, idescarpin (1) with 1-hydroxy-6-oxo-2-cyclohexenecarboxylate moiety showed the most potent inhibitory activity on adipocyte differentiation with IC50 values of 23.2 μM. Idescarpin (1) dramatically suppressed the induction of C/EBPα expression, whereas it significantly increased the induction of PPARγ expression, supported by quantitative real time PCR and Western blot analysis. The down-regulation in mRNA levels of SREBP1c, SCD-1, and FAS by idescarpin (1) during adipocyte differentiation revealed that the inhibition of adipocyte differentiation was mediated by the regulation of lipogenesis. Taken together, we suggest that idescarpin (1) shows a great potential against obesity and diabetes though the anti-adipogenic activity and the up-regulation of PPARγ.

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