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Bioassay‐guided purification and identification of PPAR α / γ agonists from Chlorella sorokiniana
Author(s) -
Chou YuCheng,
Prakash Ekambaranellore,
Huang ChienFu,
Lien TzuWen,
Chen Xin,
Su IhJen,
Chao YuSheng,
Hsieh HsingPang,
Hsu John TsuAn
Publication year - 2008
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.2280
Subject(s) - chlorella sorokiniana , bioassay , reporter gene , biology , biochemistry , luciferase , peroxisome proliferator activated receptor , biological activity , biochanin a , peroxisome , receptor , pharmacology , gene expression , gene , chlorella , botany , in vitro , algae , transfection , endocrinology , genetics , daidzein , genistein
This study isolated agonists of peroxisome proliferator activated receptors (PPARs) from the green algae Chlorella sorokiniana , using a bioassay‐guided purification strategy. PPARs are widely recognized as the molecular drug targets for many diseases including hyperglycemia, diabetes, obesity and cancer. Two independent bioassays were developed. The first is the scintillation proximity assay, a ligand binding assay. The other is the cell‐based transcriptional activation assay which uses the Dual‐Luciferase ® reporter system as the reporter gene under the control of the PPAR response element. Using these two assays, a PPAR γ ‐active fraction, CE 3‐3, was obtained from C. sorokiniana extracts, which was also able to activate PPAR α mediated gene expression. To elucidate the active ingredients in the CE 3‐3 fraction, GC‐MS analysis was employed. The results showed that the CE 3‐3 fraction consisted of at least ten fatty acids (FAs). The bioactivities of several of the individual FAs were evaluated for their PPAR γ activity and the results showed that linolenic acid and linoleic acid were the most potent FAs tested. Our studies indicate that Chlorella sorokiniana could have potential health benefits through the dual activation of PPAR α / γ via its unique FA constituents. Copyright © 2008 John Wiley & Sons, Ltd.