Phytochemistry and antiplasmodial activity of <i>Xylopia sericea</i> leaves

Aiming to investigate the antiplasmodial activity and the phytochemical composition of <i>Xylopia sericea</i> leaves, the essential oil and dichloromethane extract were analyzed by gas and liquid chromatography, respectively, both of them coupled to mass spectrometry, and were evaluated against the chloroquine-resistant <i>Plasmodium falciparum</i> strain (W2) and for cytotoxicity to HepG2 cells. Low growth inhibition of <i>P. falciparum</i> as well as low cytotoxicity to HepG2 cells were observed for the essential oil. The leaves dichloromethane extract showed moderate growth inhibition of <i>P. falciparum</i> and low cytotoxicity to HepG2 cells. Bioguided chromatographic fractionation of this extract led to fractions with increased antiplasmodial activity from which liriodenine (IC₅₀ 6.1 ± 0.1 μg/mL, CC₅₀ &gt; 1000.0 μg/mL, SI &gt; 164), an aporphine alkaloid, and an acetogenin-rich fraction containing mainly isomers of annomontacin and 4-deoxy-annomontacin (IC₅₀ 22.7 ± 1.9 µg/mL, CC₅₀ 336.1 ± 15.5 µg/mL, SI = 15) might be highlighted for their antiplasmodial activity.

为探究银叶紫玉盘（Xylopia sericea）叶片的抗疟活性与植物化学组成，研究人员分别采用气相色谱-质谱联用与液相色谱-质谱联用技术，对其精油及二氯甲烷提取物进行分析，并针对耐氯喹恶性疟原虫（Plasmodium falciparum）W2菌株开展抗疟活性评价，同时检测其对HepG2细胞的细胞毒性。结果显示，该精油对恶性疟原虫的生长抑制活性较弱，且对HepG2细胞的细胞毒性亦较低。该叶片的二氯甲烷提取物则表现出中等强度的恶性疟原虫生长抑制活性，同时对HepG2细胞的毒性较低。通过对该提取物进行生物导向色谱分级分离，研究人员获得了抗疟活性显著提升的分级组分。其中，鹅掌楸碱（liriodenine，IC₅₀ 6.1 ± 0.1 μg/mL，CC₅₀ > 1000.0 μg/mL，选择指数SI > 164）这一阿朴菲类生物碱，以及以安诺蒙它辛（annomontacin）与4-脱氧安诺蒙它辛异构体为主要成分的富含番荔枝内酯（acetogenin）的分级组分（IC₅₀ 22.7 ± 1.9 μg/mL，CC₅₀ 336.1 ± 15.5 μg/mL，选择指数SI = 15），因其突出的抗疟活性而值得重点关注。

搜集汇总

背景与挑战

背景概述

该数据集聚焦于Xylopia sericea叶子的植物化学分析和抗疟活性研究，通过色谱-质谱技术评估了精油和二氯甲烷提取物对氯喹抗性疟原虫的抑制效果及细胞毒性。研究发现二氯甲烷提取物具有中度抗疟活性，并从中分离出liriodenine和乙酰精素富集部分等潜在抗疟化合物，为天然产物抗疟研究提供了数据支持。