Department of Chemistry and Virginia Tech Center for Drug Discovery, M/C 0212, Virginia Tech, Blacksburg, Virginia 24061, USA.
J Nat Prod. 2013 Mar 22;76(3):388-93. doi: 10.1021/np300750q. Epub 2013 Jan 3.
Bioassay-guided fractionation of an ethanol extract of the leaves and inflorescence of Mallotus oppositifolius collected in Madagascar led to the isolation of the two new bioactive dimeric phloroglucinols mallotojaponins B (1) and C (2), together with the known mallotophenone (3). The structures of the new compounds were determined on the basis of spectroscopic evidence, including their 1D- and 2D-NMR spectra, mass spectrometry, and an X-ray crystal structure. Compounds 1 and 2 showed potent antimalarial activity against chloroquine-resistant Plasmodium falciparum, with IC50 values of 0.75 ± 0.30 and 0.14 ± 0.04 μM, while 3 was inactive in this assay. Compounds 1-3 also displayed strong antiproliferative activity against the A2780 human ovarian cancer cell line (IC50 1.10 ± 0.05, 1.3 ± 0.1 and 6.3 ± 0.4 μM, respectively).
从马达加斯加采集的桃叶珊瑚叶和花序的乙醇提取物经生物测定指导分离，得到了两种新的具有生物活性的二聚苯并呋喃醇衍生物：桃叶珊瑚苷 B（1）和 C（2），以及已知的桃叶珊瑚酮（3）。新化合物的结构是基于光谱证据确定的，包括它们的 1D 和 2D-NMR 光谱、质谱和 X 射线晶体结构。化合物 1 和 2 对氯喹耐药的恶性疟原虫表现出很强的抗疟活性，IC50 值分别为 0.75 ± 0.30 和 0.14 ± 0.04 μM，而 3 在该测定中没有活性。化合物 1-3 对 A2780 人卵巢癌细胞系也表现出很强的增殖抑制活性（IC50 值分别为 1.10 ± 0.05、1.3 ± 0.1 和 6.3 ± 0.4 μM）。
