Bioassay-guided purification and identification of PPARalpha/gamma agonists from Chlorella sorokiniana.
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 PPARgamma-active fraction, CE 3-3, was obtained from C. sorokiniana extracts, which was also able to activate PPARalphamediated 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 PPARgamma 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 PPARalpha/gamma via its unique FA constituents.
Chou
Yu-Cheng
YC
Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Taiwan, ROC.
Prakash
Ekambaranellore
E
Huang
Chien-Fu
CF
Lien
Tzu-Wen
TW
Chen
Xin
X
Su
Ih-Jen
IJ
Chao
Yu-Sheng
YS
Hsieh
Hsing-Pang
HP
Hsu
John Tsu-An
JT
D001681:Biological Assay / Q000379:methods*; D045744:Cell Line, Tumor; D002708:Chlorella / Q000737:chemistry*; D005227:Fatty Acids / Q000302:isolation & purification / Q000494:pharmacology; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D019787:Linoleic Acid / Q000302:isolation & purification / Q000494:pharmacology; D047493:PPAR alpha / Q000819:agonists* / Q000235:genetics; D047495:PPAR gamma / Q000819:agonists* / Q000235:genetics; D015533:Transcriptional Activation / Q000187:drug effects; D017962:alpha-Linolenic Acid / Q000302:isolation & purification / Q000494:pharmacology
D005227:Fatty Acids; D047493:PPAR alpha; D047495:PPAR gamma; D017962:alpha-Linolenic Acid; D019787:Linoleic Acid