Reference - Detail
| RRC ID | 44609 |
|---|---|
| Author | Gamo K, Shiraki T, Matsuura N, Miyachi H. |
| Title | Mechanism of peroxisome proliferator-activated receptor gamma (PPARγ) transactivation by hesperetin glucuronides is distinct from that by a thiazolidine-2,4-dione agent. |
| Journal | Chem Pharm Bull (Tokyo) |
| Abstract |
Hesperidin, a flavanone glycoside present abundantly in citrus fruits, is predominantly metabolized to hesperetin-7-O-β-D-glucuronide (H7-OG) and hesperetin-3'-O-β-D-glucuronide (H3'-OG), which exhibit partial agonistic activity towards peroxisome proliferator-activated receptor gamma (PPARγ). Here, in order to understand the mechanism(s) of action of PPARγ transactivation elicited by hesperetin glucuronides, we compared the transactivation activities of PPARγ (ligand-binding domain (LBD)) mutants by hesperetin glucuronides and troglitazone, a thiazolidine-2,4-dione class PPARγ full agonist. The assay results indicated that the mechanisms of activation of PPARγ by hesperetin glucuronides and by troglitazone are distinct, probably due to a difference in the binding sites of these compounds on the PPARγ LBD. Flavanone-class PPARγ partial agonists, luteolin and hesperetin glucuronides, showed similar activation profiles of the PPARγ LBD mutants, even though they have different side chain functionalities. |
| Volume | 62(5) |
| Pages | 491-3 |
| Published | 2014-1-1 |
| DOI | 10.1248/cpb.c14-00021 |
| PII | DN/JST.JSTAGE/cpb/c14-00021 |
| PMID | 24789933 |
| MeSH | Animals Binding Sites / drug effects COS Cells Cells, Cultured Chlorocebus aethiops Hesperidin / chemical synthesis Hesperidin / chemistry Hesperidin / pharmacology* Humans Models, Molecular Molecular Structure PPAR gamma / agonists* PPAR gamma / genetics PPAR gamma / metabolism Structure-Activity Relationship Thiazolidinediones / chemical synthesis Thiazolidinediones / chemistry Thiazolidinediones / pharmacology* |
| Times Cited | 6 |
| WOS Category | CHEMISTRY, ANALYTICAL BIOCHEMICAL RESEARCH METHODS BIOCHEMISTRY & MOLECULAR BIOLOGY |
| Resource | |
| Human and Animal Cells | COS-1(RCB0143) |