Department of Immunology, Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México, Ciudad de México, México.
Consejo Nacional de Ciencia y Tecnología-Instituto de Investigaciones Químico Biológicas, Universidad Michoacana de San Nicolás de Hidalgo, Morelia, Michoacán, México.
Planta Med. 2020 Apr;86(6):425-433. doi: 10.1055/a-1111-9566. Epub 2020 Feb 27.
has been traditionally used by indigenous and socioeconomically disadvantaged people to treat infectious and parasitic diseases, including amoebiasis. The goal of this study was to assess the effect of a crude methanolic extract, an alkaloid extract, and aporphine alkaloids from leaves of on the viability of trophozoite cultures and to identify the mechanism of action. Different concentrations of the extracts and alkaloids purpureine (1: ), 3-hydroxyglaucine (2: ), norpurpureine (3: ) glaziovine (4: ), and oxopurpureine (5: ) were added to the cultures, and dead parasites were counted after 24 h using a tetrazolium dye reduction assay and analyzed by flow cytometry. The crude extract did not affect the viability of amoebae, but the alkaloid extract and the derived alkaloid glaziovine (4: ) had important anti-amoebic activity with an IC of 33.5 µM compared to that shown by metronidazole (6.8 µM). The treatments induced significant morphological changes in the trophozoites, and most parasites killed by the alkaloid extract were positive for Annexin V, suggesting that apoptosis was the main mechanism of action. In contrast, glaziovine (4: ) induced less apoptosis with more amoebic lysis. This study supports the idea that aporphine alkaloids from , mainly (+)-()-glaziovine (4: ), could contribute to the development of new formulations for the treatment of amoebiasis. In addition, X-ray diffraction structural analysis and complete H and C NMR assignments of (+)-()-glaziovine (4: ) were performed and reported for the first time.
一直被土著和社会经济弱势群体用于治疗感染和寄生虫病，包括阿米巴病。本研究的目的是评估 叶的粗甲醇提取物、生物碱提取物和阿朴啡生物碱对滋养体培养物活力的影响，并确定其作用机制。将不同浓度的提取物和生物碱紫堇定（1: ）、3-羟基鸭脚木碱（2: ）、去甲紫堇定（3: ）、glaziovine（4: ）和氧化紫堇定（5: ）添加到培养物中，24 小时后使用四唑染料还原法计数死亡寄生虫，并通过流式细胞术进行分析。粗提取物不会影响变形虫的活力，但生物碱提取物和衍生的生物碱 glaziovine（4: ）具有重要的抗阿米巴活性，IC 为 33.5μM，而甲硝唑（6.8μM）。处理诱导滋养体发生显著的形态变化，并且用生物碱提取物杀死的大多数寄生虫对 Annexin V 呈阳性，表明细胞凋亡是主要的作用机制。相比之下，glaziovine（4: ）诱导的细胞凋亡较少，而溶胞作用较多。这项研究支持了 叶中的阿朴啡生物碱，主要是（+）-()-glaziovine（4: ），可能有助于开发治疗阿米巴病的新配方的观点。此外，首次进行并报道了（+）-()-glaziovine（4: ）的 X 射线衍射结构分析和完整的 H 和 C NMR 分配。
