Departments of Chemistry and Earth Ocean & Atmospheric Sciences, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia V6T 1Z1, Canada.
The Wistar Institute, Philadelphia, Pennsylvania 19104, United States.
J Nat Prod. 2022 May 27;85(5):1274-1281. doi: 10.1021/acs.jnatprod.1c01225. Epub 2022 May 6.
Five new minor sesterterpenoids, ansellones H (), I (), J (), and K () and phorone C (), have been isolated from a sp. marine sponge collected in British Columbia. Their structures have been elucidated by detailed analysis of NMR and MS data. Ansellone J () and phorone C () are potent HIV-1 latency reversal agents that are more potent than the reference compound and control protein kinase C activator prostratin (). The most potent sesterterpenoid, ansellone J (), was evaluated for HIV latency reversal in a primary cell context using CD4+ T cells obtained directly from four combination antiretroviral therapy-suppressed donors with HIV. To a first approximation, ansellone J () induced HIV latency reversal at levels similar to prostratin () , but at a 10-fold lower concentration.
从不列颠哥伦比亚省采集的一种 海绵中分离得到五个新的小倍半萜类化合物，安塞尔酮 H ()、I ()、J () 和 K () 和磷酮 C ()。通过对 NMR 和 MS 数据的详细分析，阐明了它们的结构。安塞尔酮 J () 和磷酮 C () 是有效的 HIV-1 潜伏期逆转剂，比参考化合物和蛋白激酶 C 激活剂普罗他汀 () 更有效。最有效的倍半萜类化合物安塞尔酮 J () 在直接从四个接受联合抗逆转录病毒治疗抑制的 HIV 供体获得的 CD4+ T 细胞中，在原代细胞环境中进行了 HIV 潜伏期逆转的评估。初步结果表明，安塞尔酮 J () 诱导 HIV 潜伏期逆转的水平与普罗他汀 () 相似，但浓度低 10 倍。
