Abstract

Activity-guided fractionations of Jatropha macrantha Müll. Arg. led to the isolation of pomolic acid (1) and euscaphic acid (2). The potential for inhibition against NF-κB and HIF-1α production of these two compounds was tested in different tumour cell lines. Compounds 1 and 2 showed an inhibitory activity of HIF-1α in the SK-MEL-28 (IC₅₀=3.01 ± 0.02 μM and 3.78 ± 0.02 μM), A549 (IC₅₀=9.97 ± 0.01 μM and 10.25 ± 0.01 μM) and U-373 MG (IC₅₀=6.34 ± 0.02 μM and 8.85 ± 0.02 μM) cell lines. In addition, compounds 1 and 2 showed an inhibitory activity on NF-κB in SK-MEL-28 (IC₅₀=1.05 ± 0.02 μM and 2.71 ± 0.01 μM), A549 (IC₅₀=3.63 ± 0.01 μM and 3.73 ± 0.02 μM) and U-373 MG (IC₅₀=2.55 ± 0.02 μM and 3.39 ± 0.01 μM) cell lines. This is the first report that isolates these compounds from J. macrantha and tests their antitumor potential.

摘要

麻风树Müll的活动引导分馏。精氨酸。导致分离出pomolic acid ( 1 ) 和eucaphic acid ( 2 )。在不同的肿瘤细胞系中测试了这两种化合物抑制 NF-κB 和 HIF-1α 产生的潜力。化合物1和2在 SK-MEL-28 (IC ₅₀ =3.01 ± 0.02  μ M 和 3.78 ± 0.02  μ M)、A549 (IC ₅₀ = 9.97 ± 0.01  μ M 和 10.25 ± 0.01  )中显示出 HIF-1α 抑制活性μ M) 和 U-373 MG (IC ₅₀ =6.34 ± 0.02  μ M 和 8.85 ± 0.02  μM) 细胞系。此外，化合物1和2在 SK-MEL-28 (IC ₅₀ =1.05 ± 0.02  μ M 和 2.71 ± 0.01  μ M)、A549 (IC ₅₀ =3.63 ± 0.01  μ M 和 3.73 )中显示出对 NF-κB 的抑制活性± 0.02  μ M) 和 U-373 MG (IC ₅₀ =2.55 ± 0.02  μ M 和 3.39 ± 0.01  μ M) 细胞系。这是第一份从J. macrantha中分离出这些化合物并测试其抗肿瘤潜力的报告。