4-Hydroxycoumarin exhibits a broad spectrum of biological activities including notable inhibitory activity against various enzymes, antioxidant properties, cytotoxicity against human and mouse cell lines, and specific bioactivities relevant to pharmaceutical and agricultural applications. Specifically, it inhibits HIV-1 integrase with an IC50 value greater than 100,000 nM and xanthine oxidase with an IC50 value of 195,000 nM. It shows antioxidant activity by scavenging DPPH and ABTS radicals, inhibiting hydroxyl radical production, and demonstrating a trolox equivalent antioxidant capacity of 186.0 umolequiv/g in the ABTS assay. The compound also displays notable inhibition against several human carbonic anhydrases, particularly CA9 (Ki = 410.0 nM) and moderate activity against CA1 (Ki = 95,000.0 nM).
4-Hydroxycoumarin is cytotoxic to various human and mouse cell lines, including TK10, UACC62, MCF7, and B16F10, with IC50 values ranging from 600.0 nM to over 200,000.0 nM, indicating varying degrees of potency. It shows some selectivity in its anticancer activity against melanoma cell lines SK-MEL3 (IC50 = 2100.0 nM) and SK-MEL-28 (IC50 = 1300.0 nM). The compound also exhibits antifungal activity against Aspergillus fumigatus at lower concentrations and stimulatory activity on the growth of Colletotrichum acutatum.
Additionally, 4-Hydroxycoumarin displays bioactivity in expressed human recombinant UGT enzymes, specifically showing activity in UGT1A7, UGT1A8, and UGT2A1. It provides gastric cytoprotection in male Wistar rats with a cytoprotective effect score of 4.62. The compound also inhibits alpha-glucosidase enzyme with an IC50 value of 400,000 uM and demonstrates binding affinity to CK2alpha as indicated by a delta melting temperature of 3.8 degrees Celsius. Overall, 4-Hydroxycoumarin shows potential for further development in various therapeutic and agricultural domains due to its diverse bioactivities..
Note: Summary generated by AI. Data source: ChEMBL 