文摘
An extract of Humicola fuscoatra (UCSC strain no. 108111A) was shown to reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells. We report the bioassay-guided isolation and structure determination of several resorcyclic acid lactones, including four known compounds, radicicol (1, aka. monorden) and pochonins B (2), C (3), and N (4), and three new analogues, radicicols B鈥揇 (5鈥?b>7). Compounds 1鈥?b>3 and 5 showed moderate activities in the memory T cell model of HIV-1 latency. Radicicol (1) displayed lower potency in reactivating latent HIV-1 (EC50 = 9.1 渭M) relative to the HDAC inhibitors apicidin (EC50 = 0.3 渭M), romidepsin (EC50 = 0.003 渭M), and SAHA (EC50 = 0.6 渭M); however, it achieved equivalent maximum efficacy relative to the positive control compounds (98% of SAHA and romidepsin).