花椒中唇丹和海麻二萜抗分枝杆菌活性的研究

Joana M. Andrade, A. Romagnoli, Joana F. Almeida, Inês M. Ferreira, C. Garcia, A. Díaz-Lanza, G. Fimia, P. Rijo
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引用次数: 1

摘要

天然产物是药物化学先导化合物的独特来源。据报道,从Plectranthus spp.中分离出的几种二萜具有有趣的抗结核活性和P. ornatus Codd。在巴西的一些地区被用作抗感染药。在此之前,从P. ornatus Codd中分离出大量具有halimane和labdane骨架的二萜。我们评估了这些化合物的抗分枝杆菌活性,对无毒的耻垢分枝杆菌菌株进行了初步试验。用乳酸脱氢酶法测定了二萜对卤烷和labdane骨架的细胞毒性,在25 μg.mL-1时未发现明显的细胞毒性作用。随后,采用微量稀释法测定其对耻垢分枝杆菌的最小抑制浓度(MIC)。抑制非毒力分枝杆菌生长≥99%的MIC为100 μg。具有卤烷骨架的二萜的mL-1大于100 μg.mL-1。据我们所知,这是第一次报道从P. ornatus中分离到的具有halimane和labdane骨架的二萜对巨噬细胞的细胞毒性,以及抗分枝杆菌活性的初步测定。建议进一步研究结核分枝杆菌,特别是具有卤烷骨架的二萜。
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Anti-mycobacterial activity of labdane and halimane diterpenes obtained from Plectranthus ornatus Codd
Natural products are a unique source of lead compounds for medicinal chemistry. Several diterpenes isolated from Plectranthus spp. have been reported to have interesting tuberculostatic activity and P. ornatus Codd. has been used in some regions of Brazil as an anti-infective. Previously, diterpenes with halimane and labdane skeletons were isolated in large quantities from P. ornatus Codd. We assessed the anti-mycobacterial activity of these compounds, performing a preliminar assay with the non-virulent strain Mycobacterium smegmatis. The cytotoxicity of the diterpenes with halimane and labdane skeletons was tested with the lactate dehydrogenase assay, where no considerable cytotoxic effects were found up to 25 μg.mL-1. Subsequently, the microdilution method was used to determine the minimum inhibitory concentration (MIC) against M. smegmatis. The MIC that inhibited the growth of the non-virulent mycobacteria by ≥99% was 100 μg.mL-1 for the diterpene with halimane skeleton, whereas for the diterpene with a labdane skeleton was >100 μg.mL-1. To the best of our knowledge, this is the first report on diterpenes with halimane and labdane skeletons isolated from P. ornatus in macrophages cytotoxicity, and in a preliminar assay for anti-mycobacterial activity. Further studies are suggested on M. tuberculosis, particularly for the diterpenes with halimane skeleton.
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