4-Hydroxychalcone exhibits a diverse range of bioactivities across various biological pathways and targets. It demonstrates inhibitory effects on cell proliferation in murine P388, L1210 leukemia, human Molt 4/C8 T-lymphocyte, and Human CEM T-lymphocytes cells with IC50 values ranging from 8580.0 nM to 37900.0 nM. It induces NAD(P)H quinone reductase activity in Hepa 1c1c7 murine hepatoma cells with a CD of 33.0 µM, suggesting antioxidant or detoxifying properties. The compound also inhibits the recombinant rat androgen receptor with an IC50 of 47863.01 nM, blocks the human K+ channel in HEK293 cells with an IC50 > 50000.0 nM, and inhibits cobalt chloride-induced HIF-1 activation in mouse NIH3T3 cells with an IC50 > 20000.0 nM.
4-Hydroxychalcone exhibits antifungal activity against Candida albicans with a MIC of 62.5 µg/mL and a zone of inhibition diameter of 15.0 mm, and exhibits antifungal effects on Saccharomyces cerevisiae, Hansenula polymorpha, and Kluyveromyces lactis with MIC values > 40.0 µg/mL. It shows antibacterial activity against Staphylococcus aureus Rosenbach 209 and multidrug-resistant bacterial strains, with MIC values ranging from 32.0 µg/mL to 1000.0 µg/mL, demonstrating synergism with ciprofloxacin and doxycycline.
The compound also exhibits cytotoxicity against Homo sapiens HT-29 and SGC7901 cells with IC50 values of 24600.0 nM and 13740.0 nM, respectively, and against mouse NIH/3T3 cells with less than 5.0% activity after 8 hours. 4-Hydroxychalcone shows anti-inflammatory activity by inhibiting carrageenan-induced paw edema in rats at 25 mg/kg with an inhibition of 0.165%.
It inhibits TNFalpha-induced NF-kappaB activation in human A549 and K562 cells with IC50 values > 20000.0 nM and 24000.0 nM, respectively. The compound demonstrates anti-leishmanial activity against Leishmania major with an IC50 of 4000.0 nM and antioxidant activity, including DPPH radical scavenging and inhibition of bovine xanthine oxidase with IC50 values of 290000.0 nM.
4-Hydroxychalcone exhibits enzyme inhibition, notably affecting rhodanese, MDH, GroEL/GroES-mediated protein refolding, ATPase activity, and chaperone proteins such as Escherichia coli GroEL/GroES and human mitochondrial HSP60/HSP10. It inhibits PMA-induced ROS/RNS generation in human neutrophils with IC50 values of 8800.0 nM and 11600.0 nM at different glucose concentrations. Lastly, the compound also shows antidiabetic activity by decreasing glucose consumption in 3T3L1 cells, suggesting potential multifaceted therapeutic applications..
Note: Summary generated by AI. Data source: ChEMBL 