Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Química Orgánica, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain; Instituto de Investigaciones Fármaco Bioquímicas, Facultad de Ciencias Farmacéuticas y Bioquímicas, Universidad Mayor de San Andrés, Avda. Saavedra 2224, Miraflores, La Paz, Bolivia.
Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain.
Fitoterapia. 2019 Apr;134:340-345. doi: 10.1016/j.fitote.2019.03.004. Epub 2019 Mar 3.
A phytochemical investigation of the ethanolic extract of leaves from Piper pseudoarboreum led to the isolation of 3-chlorosintenpyridone 1, an unprecedented chlorinated piperamide, together with the known compounds 2-12. Their structures were established based on 1D and 2D (COSY, ROESY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The proposed biosynthetic pathway of compound 1 is discussed. Compounds 1-12 were tested in vitro for their leishmanicidal potential against promastigote stages of Leishmania amazonensis, L braziliensis, L. guyanensis and L. infantum. Two compounds from this series, the alkamide 1 (IC 3.4-5.2 μM) and the fatty acid 9 (IC 18.7-29.6 μM) displayed higher or similar potency to Miltefosine, used as the reference drug.
从假蒟 Piper pseudoarboreum 的乙醇提取物中进行植物化学研究，分离得到了一种前所未有的氯化哌啶酰胺 3-氯辛特吡啶酮 1，以及已知化合物 2-12。它们的结构是基于 1D 和 2D（COSY、ROESY、HMQC 和 HMBC）NMR 光谱以及高分辨率质谱确定的。讨论了化合物 1 的可能生物合成途径。测试了化合物 1-12 对美洲利什曼原虫、巴西利什曼原虫、圭亚那利什曼原虫和婴儿利什曼原虫的前鞭毛体阶段的杀利什曼原虫活性。该系列中的两种化合物，酰胺 1（IC 3.4-5.2 μM）和脂肪酸 9（IC 18.7-29.6 μM）显示出与米替福新相似或更高的活性，米替福新被用作参考药物。
