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香叶中的生物活性 clerodane 二萜

Bioactive Clerodane Diterpenoids from the Leaves of Vent.

机构信息

Laboratory of Pharmacognosy, Center of Interdisciplinary Research on Medicines, CIRM, University of Liège, Avenue Hippocrate 15, 4000 Liège, Belgium.

Laboratory of Biology of Tumor and Development, GIGA/CIRM, University of Liège, Avenue Hippocrate 15, 4000 Liège, Belgium.

出版信息

Molecules. 2023 Jan 25;28(3):1197. doi: 10.3390/molecules28031197.

Abstract

Vent., an endemic plant from the Mascarene Islands, was investigated following its antiplasmodial potentialities highlighted during a previous screening. Three clerodane diterpene compounds were isolated and identified as being responsible for the antiplasmodial activity of the leaves of the plant: caseamembrin T (), corybulosin I (), and isocaseamembrin E (), which exhibited half maximal inhibitory concentrations (IC) of 0.25 to 0.51 µg/mL. These compounds were tested on two other parasites, and , to identify possible selectivity in one of them. Although these products possess both antileishmanial and antitrypanosomal properties, they displayed selectivity for the malaria parasite, with a selectivity index between 6 and 12 regarding antitrypanosomal activity and between 25 and 100 regarding antileishmanial activity. These compounds were tested on three cell lines, breast cancer cells MDA-MB-231, pulmonary adenocarcinoma cells A549, and pancreatic carcinoma cells PANC-1, to evaluate their selectivity towards . This has not enabled us to establish selectivity for , but has revealed the promising activity of compounds - (IC < 2 µg/mL), particularly against pancreatic carcinoma cells (IC < 1 µg/mL). The toxicity of the main compound, caseamembrin T (), was then evaluated on zebrafish embryos to extend our cytotoxicity study to normal, non-cancerous cells. This highlighted the non-negligible toxicity of caseamembrin T ().

摘要

万特(Vent.)是一种来自马斯克林群岛的特有植物,在先前的筛选中因其抗疟原虫特性而受到关注。从该植物的叶子中分离并鉴定出三种 clerodane 二萜化合物,它们是植物抗疟原虫活性的主要成分:桉脂素 T()、考布素 I()和异桉脂素 E(),它们的半数最大抑制浓度(IC)分别为 0.25 至 0.51 µg/mL。这些化合物在另外两种寄生虫,和 中进行了测试,以确定其中一种可能的选择性。尽管这些产品具有抗利什曼原虫和抗锥虫的特性,但它们对疟原虫表现出选择性,其抗锥虫活性的选择性指数在 6 到 12 之间,抗利什曼原虫活性的选择性指数在 25 到 100 之间。这些化合物在三种细胞系,乳腺癌细胞 MDA-MB-231、肺腺癌细胞 A549 和胰腺癌细胞 PANC-1 上进行了测试,以评估它们对 的选择性。这不能确定对 的选择性,但显示了化合物 -(IC < 2 µg/mL)的有希望的活性,特别是对胰腺癌细胞(IC < 1 µg/mL)。然后,主要化合物桉脂素 T()在斑马鱼胚胎上的毒性进行了评估,以将我们的细胞毒性研究扩展到正常的非癌细胞。这突出了桉脂素 T()的不可忽视的毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8000/9918898/5dde04e9a73d/molecules-28-01197-g001.jpg

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