N-(Isobutyl)-3,4-methylenedioxy Cinnamoyl Amide
N-(Isobutyl)-3,4-methylenedioxy Cinnamoyl Amide
复制标题
DOI：
10.3390/m1070
复制
发表时间：
2019-09-01
期刊：
影响因子：
0.6
通讯作者：
Kyeremeh, Kwaku
中科院分区：
文献类型：
--
作者：
Dofuor, Aboagye Kwarteng;Kwain, Samuel;Kyeremeh, Kwaku
植物Zanthoxylum zanthoxyloides (Lam.) Zepern。 & Timler 是非洲大陆最重要的花椒属药用物种之一。它用于撒哈拉以南非洲地区寄生虫病的治疗和管理。这些特性激发了科学家们研究该属物种的生物活性化合物。然而，目前还没有一项详细介绍从花椒属中提取和分离抗寄生虫化合物的光谱、光谱测定和生物活性指导的研究。 Tortozanthoxylamide (1) 是已知化合物 Armatamide 的衍生物，是从 Z. zanthoxyloides 中分离出来的，并使用 UV、IR、1D/2D-NMR 和高分辨率液相色谱串联质谱 (HRESI-LC-MS) 数据确定了完整结构。当针对布氏锥虫亚种进行测试时。 brucei 是导致撒哈拉以南非洲动物非洲锥虫病的寄生虫，1 (IC50 7.78 mu M) 的活性仅比市售药物二氨基氮烯乙酸酯 (IC50 1.88 mu M) 低四倍。 Diminazene aceturate 是治疗非洲动物锥虫病的有效药物。 Tortozanthoxylamide (1) 通过显着改变 T. brucei subsp. 的细胞周期，表现出显着的抗锥虫活性。 brucei，但它对小鼠巨噬细胞 RAW 264.7 细胞系选择性无毒。这表明 1 可被视为进一步开发天然抗锥虫化合物的支架。
The plant Zanthoxylum zanthoxyloides (Lam.) Zepern. & Timler is one of the most important medicinal species of the genus Zanthoxylum on the African continent. It is used in the treatment and management of parasitic diseases in sub-Saharan Africa. These properties have inspired scientists to investigate species within the genus for bioactive compounds. However, a study, which details a spectroscopic, spectrometric and bioactivity guided extraction and isolation of antiparasitic compounds from the genus Zanthoxylum is currently non-existent. Tortozanthoxylamide (1), which is a derivative of the known compound armatamide was isolated from Z. zanthoxyloides and the full structure determined using UV, IR, 1D/2D-NMR and high-resolution liquid chromatography tandem mass spectrometry (HRESI-LC-MS) data. When tested against Trypanosoma brucei subsp. brucei, the parasite responsible for animal African trypanosomiasis in sub-Saharan Africa, 1 (IC50 7.78 mu M) was just four times less active than the commercially available drug diminazene aceturate (IC50 1.88 mu M). Diminazene aceturate is a potent drug for the treatment of animal African trypanosomiasis. Tortozanthoxylamide (1) exhibits a significant antitrypanosomal activity through remarkable alteration of the cell cycle in T. brucei subsp. brucei, but it is selectively non-toxic to mouse macrophages RAW 264.7 cell lines. This suggests that 1 may be considered as a scaffold for the further development of natural antitrypanosomal compounds.