Drupanin is a compound extracted from green propolis. Drupanin selectively inhibits the AKR1C3 enzyme. Drupanin has potential in breast cancer research.
Drupanin is a naturally occurring phenylpropanoid compound isolated from green propolis. It is an orally active, selective inhibitor of AKR1C3 (aldo-keto reductase family 1 member C3) and an RXRalpha agonist (EC50 = 4.8 uM). It also moderately activates PPARgamma. Drupanin shows potential in diabetes, metabolic diseases, breast cancer, and prostate cancer research. Targets: AKR1C3 (inhibitor), RXRalpha (agonist, EC50=4.8 uM), and PPARgamma (moderate agonist). Drupanin inhibits AKR1C3, an enzyme that inactivates androgens and estrogens and is overexpressed in hormone-dependent cancers. As an RXRalpha agonist, it induces adipogenesis and regulates lipid metabolism. It also enhances insulin sensitivity by activating PPARgamma. In vitro, in 3T3-L1 fibroblasts, Drupanin (1-50 uM) induces adipogenesis, increasing aP2 mRNA levels and lipid accumulation. It selectively inhibits AKR1C3 enzyme activity, reducing production of carcinogenic metabolites. It also promotes glucose uptake in adipocytes and myotubes. In vivo, in rodent models of obesity and type 2 diabetes (db/db mice, high-fat diet-fed mice), oral administration of Drupanin (100 mg/kg) improves glucose tolerance and insulin sensitivity, reduces fasting blood glucose, and lowers serum triglycerides. It also suppresses tumor growth in xenograft models of AKR1C3-positive breast and prostate cancers. For cell-free AKR1C3 enzyme inhibition assay: recombinant AKR1C3 (50 ng) is incubated with varying concentrations of Drupanin (0-100 uM), NADPH (100 uM), and the fluorogenic substrate coumberone or 9,10-phenanthrenequinone in 100 uL buffer for 30 min at 37degC. Fluorescence is measured at excitation/emission 340/460 nm. IC50 is calculated from dose-response curves. For cell assays: 3T3-L1 preadipocytes are differentiated into adipocytes in the presence of Drupanin (1-50 uM) for 6-8 days. Lipid accumulation is quantified by Oil Red O staining. AKR1C3 activity in cell lysates is assessed by substrate conversion using LC-MS. For animal studies: in diabetic db/db mice, Drupanin is administered orally at 100 mg/kg once daily for 4 weeks. Blood glucose is measured weekly. An oral glucose tolerance test (OGTT) is performed. At study end, serum insulin, triglycerides, and cholesterol are analyzed. In cancer xenograft models, mice are treated orally with 50-100 mg/kg Drupanin daily for 3-4 weeks, and tumor volume is monitored by caliper measurement. PK properties in rodents: oral bioavailability ~60%, Tmax 1-2 h, elimination half-life 6-8 h, Cmax and AUC dose-dependent. Drupanin is metabolized by phase II conjugation (glucuronidation, sulfation) and phase I oxidation. Low toxicity profile observed at therapeutic doses. In rodent studies, no significant adverse effects were noted at doses up to 200 mg/kg. No acute or chronic toxicity has been reported. Drupanin is a natural product and a research compound, not FDA-approved for clinical use. It is being investigated as a lead for treating metabolic diseases (type 2 diabetes, obesity) and hormone-dependent cancers (breast, prostate). The compound is currently in preclinical development.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.