Screening and characterization of traditional herbal medicine for ligands which activate or inhibit the receptors related to steroidal activity

Abstract

<P>PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR) ACTIVATORS HAVE BEEN USED IN THE TREATMENT OF TYPE II DIABETES MELLITUS, DYSLIPIDAEMIA, ATHEROSCLEROSIS AND OBESITY, AND TO THE PROCESSES OF CARCINOGENESIS AND INFLAMMATION. WE HAVE IDENTIFIED SEVERAL PLANT EXTRACTS THAT ACTIVATE PPAR AND ONE OF THESE IS THE ASTRAGALUS MEMBRANACEUS (AM) EXTRACT, WHICH SIGNIFICANTLY STIMULATED PPARA AND PPARG. OTHER THAN THAT, THIS PLANT EXTRACT ALSO DISPLAYED UNIQUE ANDROGEN RECEPTOR (AR), PROGESTERONE RECEPTOR (PR) AND GLUCOCORTICOID RECEPTOR (GR) ACTIVATION PROPERTIES. WHILE AM EXTRACTS DID NOT ACTIVATE THESE RECEPTORS, IN THE PRESENCE OF THE RESPECTIVE RECEPTORSA?? COGNATE LIGANDS, IT AUGMENTED THE ACTIVITY OF THESE LIGANDED-RECEPTORS. BIOASSAY GUIDED FRACTIONATION OF AM EXTRACTS LED US TO ISOLATE NEW LIGANDS FOR PPAR, AND THESE COMPOUNDS ALSO EXHIBITED THE UNUSUAL AR-STIMULATING PROPERTIES. THE AUGMENTATIVE EFFECTS OF THESE COMPOUNDS WERE STUDIED AND APPARENTLY THESE COMPOUNDS DISPLAYED SIMILAR P