2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes. / Andersen, Charlotte; Kotowska, Dorota Ewa; Tortzen, Christian; Kristiansen, Karsten; Nielsen, John; Petersen, Rasmus Koefoed.

In: Bioorganic and Medicinal Chemistry, Vol. 22, No. 21, 2014, p. 6105-6111.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Andersen, C, Kotowska, DE, Tortzen, C, Kristiansen, K, Nielsen, J & Petersen, RK 2014, '2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes', Bioorganic and Medicinal Chemistry, vol. 22, no. 21, pp. 6105-6111. https://doi.org/10.1016/j.bmc.2014.08.037

APA

Andersen, C., Kotowska, D. E., Tortzen, C., Kristiansen, K., Nielsen, J., & Petersen, R. K. (2014). 2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes. Bioorganic and Medicinal Chemistry, 22(21), 6105-6111. https://doi.org/10.1016/j.bmc.2014.08.037

Vancouver

Andersen C, Kotowska DE, Tortzen C, Kristiansen K, Nielsen J, Petersen RK. 2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes. Bioorganic and Medicinal Chemistry. 2014;22(21):6105-6111. https://doi.org/10.1016/j.bmc.2014.08.037

Author

Andersen, Charlotte ; Kotowska, Dorota Ewa ; Tortzen, Christian ; Kristiansen, Karsten ; Nielsen, John ; Petersen, Rasmus Koefoed. / 2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes. In: Bioorganic and Medicinal Chemistry. 2014 ; Vol. 22, No. 21. pp. 6105-6111.

Bibtex

@article{7cd3c5c4ea154865b8b5ffe1e3375a5c,
title = "2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes",
abstract = "Isoflavones are bioactive compounds that have been shown to decrease lipid accumulation in vitro. However, the knowledge of the isoflavone formononetin is limited. The aim of the study was to assess the effects of formononetin and its two synthetic analogues, 2-(2-bromophenyl)-formononetin and 2-heptyl-formononetin, on lipid accumulation in 3T3-L1 adipocytes and investigate possible mechanisms. Formononetin and the two analogues were added day 0-8 or day 8-10 of the differentiation period, and lipid accumulation, glycerol release and gene expression were measured. Additionally, competitive peroxisome proliferator-activated receptor (PPAR)-γ binding assay, PPARγ transactivation assay and Western blot for phosphorylated AMP-activated protein kinase (AMPK) were performed. Chronic treatment (day 0-8) with formononetin increased lipid accumulation, whereas the two analogues decreased lipid accumulation partly due to decreased differentiation. The two analogues, but not formononetin, also decreased lipid content in mature adipocytes. 2-Heptyl-formononetin increased glycerol release and lipolytic gene expression and decreased lipogenic gene expression. Formononetin did not bind to or activate PPARγ whereas both analogues bound to the receptor and behaved as PPARγ partial agonists in the transactivation assay. Neither of the compounds affected phosphorylation of AMPK. In conclusion, the analogues of formononetin decreased lipid accumulation possibly in part by acting as PPARγ partial agonists.",
author = "Charlotte Andersen and Kotowska, {Dorota Ewa} and Christian Tortzen and Karsten Kristiansen and John Nielsen and Petersen, {Rasmus Koefoed}",
year = "2014",
doi = "10.1016/j.bmc.2014.08.037",
language = "English",
volume = "22",
pages = "6105--6111",
journal = "Bioorganic & Medicinal Chemistry",
issn = "0968-0896",
publisher = "Pergamon Press",
number = "21",

}

RIS

TY - JOUR

T1 - 2-(2-Bromophenyl)-formononetin and 2-heptyl-formononetin are PPARγ partial agonists and reduce lipid accumulation in 3T3-L1 adipocytes

AU - Andersen, Charlotte

AU - Kotowska, Dorota Ewa

AU - Tortzen, Christian

AU - Kristiansen, Karsten

AU - Nielsen, John

AU - Petersen, Rasmus Koefoed

PY - 2014

Y1 - 2014

N2 - Isoflavones are bioactive compounds that have been shown to decrease lipid accumulation in vitro. However, the knowledge of the isoflavone formononetin is limited. The aim of the study was to assess the effects of formononetin and its two synthetic analogues, 2-(2-bromophenyl)-formononetin and 2-heptyl-formononetin, on lipid accumulation in 3T3-L1 adipocytes and investigate possible mechanisms. Formononetin and the two analogues were added day 0-8 or day 8-10 of the differentiation period, and lipid accumulation, glycerol release and gene expression were measured. Additionally, competitive peroxisome proliferator-activated receptor (PPAR)-γ binding assay, PPARγ transactivation assay and Western blot for phosphorylated AMP-activated protein kinase (AMPK) were performed. Chronic treatment (day 0-8) with formononetin increased lipid accumulation, whereas the two analogues decreased lipid accumulation partly due to decreased differentiation. The two analogues, but not formononetin, also decreased lipid content in mature adipocytes. 2-Heptyl-formononetin increased glycerol release and lipolytic gene expression and decreased lipogenic gene expression. Formononetin did not bind to or activate PPARγ whereas both analogues bound to the receptor and behaved as PPARγ partial agonists in the transactivation assay. Neither of the compounds affected phosphorylation of AMPK. In conclusion, the analogues of formononetin decreased lipid accumulation possibly in part by acting as PPARγ partial agonists.

AB - Isoflavones are bioactive compounds that have been shown to decrease lipid accumulation in vitro. However, the knowledge of the isoflavone formononetin is limited. The aim of the study was to assess the effects of formononetin and its two synthetic analogues, 2-(2-bromophenyl)-formononetin and 2-heptyl-formononetin, on lipid accumulation in 3T3-L1 adipocytes and investigate possible mechanisms. Formononetin and the two analogues were added day 0-8 or day 8-10 of the differentiation period, and lipid accumulation, glycerol release and gene expression were measured. Additionally, competitive peroxisome proliferator-activated receptor (PPAR)-γ binding assay, PPARγ transactivation assay and Western blot for phosphorylated AMP-activated protein kinase (AMPK) were performed. Chronic treatment (day 0-8) with formononetin increased lipid accumulation, whereas the two analogues decreased lipid accumulation partly due to decreased differentiation. The two analogues, but not formononetin, also decreased lipid content in mature adipocytes. 2-Heptyl-formononetin increased glycerol release and lipolytic gene expression and decreased lipogenic gene expression. Formononetin did not bind to or activate PPARγ whereas both analogues bound to the receptor and behaved as PPARγ partial agonists in the transactivation assay. Neither of the compounds affected phosphorylation of AMPK. In conclusion, the analogues of formononetin decreased lipid accumulation possibly in part by acting as PPARγ partial agonists.

U2 - 10.1016/j.bmc.2014.08.037

DO - 10.1016/j.bmc.2014.08.037

M3 - Journal article

C2 - 25262940

AN - SCOPUS:84908440133

VL - 22

SP - 6105

EP - 6111

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

SN - 0968-0896

IS - 21

ER -

ID: 127671946