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Vernolide-A and Vernodaline: Sesquiterpene Lactones with Cytotoxicity against Cancer
Journal of Environmental Pathology, Toxicology and Oncology ( IF 2.4 ) Pub Date : 2020-01-01 , DOI: 10.1615/jenvironpatholtoxicoloncol.2020034066
Hoai Nguyen Nguyen , Minh Tan Nguyen , Anh Thu Do , Phuong Trinh Tran , Xuan Nam Vo , Bich Hang Do

Vernolide-A and vernodaline are sesquiterpene lactones isolated from genera of Vernonia. Vernolide-A and vernodaline have shown promising therapeutic properties, including antibacterial, antihelminth, and antioxidant activities. Recently, the anticancer properties of these sesquiterpene lactones have been investigated with the elucidation of effects on cell proliferation, metastasis, angiogenesis, and apoptosis. The antiproliferation and antimetastatic activities arise from targeting extracellular signal-regulated kinase 1 (ERK-1), extracellular signal-regulated kinase 2 (ERK-2), nuclear factor-κB (NF-κB), signal transducer and activator of transcription 3 (STAT3), matrix metalloproteinase 2 (MMP-2), and matrix metalloproteinase 9 (MMP9). The induction of apoptosis is due to the enhancement of caspase 9, caspase 3, while inhibition of Bcl-2 and Bcl-xL results in the release of cytochrome c into the cytosol. The activity of vernolide-A and vernodaline is hypothesized to be due to thiol reactivity through the α-methylene-γ-lactone group of sesquiterpene lactones. This review will give a brief summary of the anticancer activity of vernolide-A and vernodaline and provide information on the underlying molecular mechanisms.

中文翻译:

Vernolide-A和Vernodaline:倍半萜烯内酯具有抗癌细胞毒性

Vernolide-A和vernodaline是从Vernonia属中分离的倍半萜内酯。Vernolide-A和vernodaline已显示出令人鼓舞的治疗特性,包括抗菌,抗蠕虫和抗氧化活性。最近,已经研究了这些倍半萜内酯的抗癌特性,并阐明了对细胞增殖,转移,血管生成和凋亡的影响。抗增殖和抗转移活性来自靶向细胞外信号调节激酶1(ERK-1),细胞外信号调节激酶2(ERK-2),核因子-κB(NF-κB),信号转导子和转录激活子3( STAT3),基质金属蛋白酶2(MMP-2)和基质金属蛋白酶9(MMP9)。凋亡的诱导是由于caspase 9,caspase 3的增强,而抑制Bcl-2和Bcl-xL会导致细胞色素c释放到细胞质中。假定藜芦内酯A和藜芦碱的活性归因于倍半萜内酯的α-亚甲基-γ-内酯基团通过巯基反应。这篇综述将简要概述维诺内酯-A和维诺达林的抗癌活性,并提供有关潜在分子机制的信息。
更新日期:2020-01-01
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