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Phenylpropanoids from Croton velutinus with cytotoxic, trypanocidal and anti-inflammatory activities.
Fitoterapia ( IF 3.4 ) Pub Date : 2020-05-22 , DOI: 10.1016/j.fitote.2020.104632
Lucas Silva Abreu 1 , Yuri Mangueira do Nascimento 1 , Renan Fernandes do Espirito-Santo 2 , Cássio Santana Meira 2 , Ivanilson Pimenta Santos 2 , Railda Batista Brandão 3 , Augusto Lopes Souto 1 , Maria Lenise Silva Guedes 4 , Milena Botelho Pereira Soares 2 , Cristiane Flora Villarreal 3 , Marcelo Sobral da Silva 1 , Eudes da Silva Velozo 3 , Josean Fechine Tavares 1
Affiliation  

This current study presents the phytochemical analysis of Croton velutinus, describing phenylpropanoids obtained from this species. The fractionation of the roots hexane extract led to the isolation of four new phenylpropanoids derivatives, velutines A-D (1-4) and three known (5-7). Their structures were established based on spectroscopic (1D-2D NMR; HRMS and IR) analysis. Cytotoxic, trypanocidal and anti-inflammatory activities of compounds 1-7 were evaluated. Only compounds 2 and 5 showed cytotoxic activity against cancer cell lines (B16F10, HL-60, HCT116, MCF-7 and HepG2), with IC50 values ranging from 6.8 to 18.3 μM and 11.1 to 18.3 μM, respectively. Compounds 2 and 5 also showed trypanocidal activity against bloodstream trypomastigotes with EC50 values of 9.0 and 9.58 μM, respectively. Finally, the anti-inflammatory potential of these compounds was evaluated on cultures of activated macrophages. All compounds exhibited concentration-dependent suppressive activity on the production of nitrite and IL-1β by macrophages stimulated with LPS and IFN-γ. These results indicate phenylpropanoids esters (2 and 5) from C. velutinus as promising cytotoxic, trypanocidal and anti-inflammatory candidates that warrants further studies.

中文翻译:

巴豆绒中的苯丙烷类具有细胞毒,锥虫和抗炎活性。

这项当前的研究提供了巴豆的植物化学分析,描述了从该物种获得的苯丙烷。根己烷提取物的分馏导致分离出四种新的苯基丙烷衍生物,天鹅绒素AD(1-4)和三种已知的(5-7)。基于光谱分析(1D-2D NMR; HRMS和IR)确定了它们的结构。评价了化合物1-7的细胞毒,锥虫和抗炎活性。仅化合物2和5对癌细胞系(B16F10,HL-60,HCT116,MCF-7和HepG2)表现出细胞毒活性,IC50值分别为6.8至18.3μM和11.1至18.3μM。化合物2和5还显示出针对血流锥虫的锥虫杀虫活性,EC50值分别为9.0和9.58μM。最后,在活化的巨噬细胞培养物中评估了这些化合物的抗炎潜力。所有化合物对由LPS和IFN-γ刺激的巨噬细胞对亚硝酸盐和IL-1β的产生均表现出浓度依赖性的抑制活性。这些结果表明,来自C. velutinus的苯丙酸酯(2和5)是有希望的细胞毒性,锥虫和抗炎候选药物,值得进一步研究。
更新日期:2020-05-22
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