Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, Porto Alegre, Brazil.
Laboratory of Cellular and Molecular Immunology, Federal University of Health Sciences of Porto Alegre, Porto Alegre, RS, Brazil; Graduate Program in Rehabilitation Sciences, Federal University of Health Sciences of Porto Alegre, Porto Alegre, RS, Brazil.
Phytomedicine. 2019 May;58:152748. doi: 10.1016/j.phymed.2018.11.009. Epub 2018 Nov 12.
Several species of Salvia are used as medicinal plants around the world. Biological activities of isolated compounds have been described, being diterpenes frequently responsible for the effects.
Isolation of diterpenes from Salvia uliginosa Benth. and evaluation of the antichemotactic and leishmanicidal activities of the isolated compounds.
To isolate diterpenes from S. uliginosa and evaluate their antichemotactic and leishmanicidal activities in vitro.
The exudate of S. uliginosa was obtained by rapidly dipping the aerial parts in dichloromethane. The compounds were isolated by repeated column chromatography over silica gel. The effects on L. amazonensis growth, survival, DNA degradation, ROS generation, as well as the antichemotactic activity and cytotoxicity of the compounds towards human erythrocytes and macrophages were evaluated.
A novel icetexane diterpene, isoicetexone (IsoICT) along with the known diterpenes icetexone (ICT), and 7-acetoxy-6,7-dihydroicetexone were isolated from the dichloromethane surface exudate of S. uliginosa. The structures were elucidated using NMR and MS experiments, and by comparison with previously reported data. IsoICT and ICT at low concentrations caused completely inhibition of neutrophils migration in vitro. In addition, IsoICT and ICT showed high leishmanicidal activity against L. amazonensis, induced ROS production in parasites and presented low cytotoxicity against macrophages and human erythrocytes, and moderate to high selectivity index.
These data indicated that IsoICT and ICT exhibit potent antichemotactic and leishmanicidal effects. Further studies are needed in order to evaluate the in vivo activities as well as the toxicity of the compounds.
几种鼠尾草属植物被用作世界各地的药用植物。已描述了分离化合物的生物活性，二萜类化合物通常是这些活性的主要原因。
从乌苏里鼠尾草中分离二萜类化合物，并评估分离化合物的抗趋化和杀利什曼原虫活性。
从乌苏里鼠尾草中分离二萜类化合物，并评估其体外抗趋化和杀利什曼原虫活性。
通过快速将地上部分浸入二氯甲烷中，从乌苏里鼠尾草中获得渗出物。通过在硅胶上反复柱层析分离化合物。评估化合物对 L. amazonensis 生长、存活、DNA 降解、ROS 生成的影响，以及化合物对人红细胞和巨噬细胞的趋化活性和细胞毒性。
从乌苏里鼠尾草的二氯甲烷表面渗出物中分离出一种新型的异艾酮二萜，异艾酮（IsoICT）以及已知的二萜艾酮（ICT）和 7-乙酰氧基-6,7-二氢艾酮。结构通过 NMR 和 MS 实验以及与以前报道的数据进行比较来阐明。低浓度的 IsoICT 和 ICT 可完全抑制体外中性粒细胞的迁移。此外，IsoICT 和 ICT 对 L. amazonensis 具有很高的杀利什曼原虫活性，诱导寄生虫产生 ROS，并对巨噬细胞和人红细胞的细胞毒性低，对选择性指数具有中等至高的选择性。
这些数据表明 IsoICT 和 ICT 具有很强的抗趋化和杀利什曼原虫作用。需要进一步研究以评估化合物的体内活性和毒性。
