Addo Ermias Mekuria, Adu-Ampratwum Daniel, Kaweesa Elizabeth N, Agarwal Garima, Uchenik Dmitriy, Ninh Tran N, Soejarto Djaja D, Burdette Joanna E, Fuchs James R, Kinghorn A Douglas, Rakotondraibe Harinantenaina L
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.
Department of Pharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois 60612, United States.
J Nat Prod. 2025 Mar 28;88(3):662-670. doi: 10.1021/acs.jnatprod.4c01247. Epub 2025 Mar 4.
The tropical plant is known to produce cyclopenta[]benzofuran and other types of rocaglate derivatives including silvestrol () and 5‴-episilvestrol () that are of current pharmacological interest. In the present work, further investigation of roots collected in Vietnam has yielded two new rocaglate acetonide derivatives ( and ) and a known pentanor-3,4--dammarane triterpenoid () found for the first time as a natural product, in addition to four known rocaglates (-). The structures of compounds and were confirmed by partial synthesis experiments, and their potential occurrence as extraction artifacts was investigated by targeted selective ion monitoring using UHPLC-MS. All compounds obtained were evaluated against a panel of four human cancer cell lines, in which the six rocaglate derivatives (-) tested all showed submicromolar potencies.
已知这种热带植物能产生环戊并[ ]苯并呋喃以及其他类型的洛卡林衍生物,包括目前具有药理学研究价值的silvestrol( )和5‴-表silvestrol( )。在本研究中,对采自越南的该植物根部进行进一步研究,除了四种已知的洛卡林(-)外,还得到了两种新的洛卡林丙酮化物衍生物( 和 )以及首次作为天然产物发现的一种已知的五环-3,4-二氢达玛烷三萜( )。通过部分合成实验确定了化合物 和 的结构,并使用超高效液相色谱-质谱联用仪通过靶向选择性离子监测研究了它们作为提取假象的潜在可能性。对所获得的所有化合物针对一组四种人类癌细胞系进行了评估,其中所测试的六种洛卡林衍生物(-)均显示出亚微摩尔级别的活性。