Alves Gomes Fernanda Torlania, Boleti Ana Paula de Araújo, Leandro Lidiam M, Squinello Diego, Aranha Ellen S P, Vasconcelos Marne C, Cos Paul, Veiga-Junior Valdir F, Lima Emerson Silva
Biological Activity Laboratory, Faculty of Pharmaceutical Sciences, Federal University of Amazonas, Manaus, Amazonas, Brazil.
Chemistry Department, Exact Sciences Institute, Federal University of Amazonas, Manaus, Amazonas, Brazil.
Pharmacogn Mag. 2017 Oct-Dec;13(52):542-552. doi: 10.4103/pm.pm_552_16. Epub 2017 Nov 13.
The oil-resin of Ducke has been used in popular medicine similarly to the copaiba oil ( spp.).
This study aimed to investigate the effects of the acid fraction of oil-resin (AFEOR) on cell proliferation, collagen production in human fibroblasts, inhibition of metalloproteinases, and cytotoxicity against tumor cell lines.
Acid fraction of was fractionated in the ion exchange column chromatography. Cytotoxicity and genotoxicity were evaluated by Alamar Blue and Cometa assay. The inhibition of metalloproteinases was performed by zymography and Western blotting.
The predominant acidic diterpenes in the AFEOR were copalic and hardwickiic acids. AFEOR caused morphology alteration and decrease of proliferation at concentrations higher than 5 μg/mL. It also caused significant collagen proliferation in fibroblasts. It showed cytotoxicity against tumoral and nontumoral cell lines, with IC values ranging from 13 to 50 μg/mL, and a hemolytic activity with an IC value of 38.29 μg/mL. AFEOR inhibited collagenase activity, with an IC value of 46.64 μg/mL, and matrix metalloproteinase-2 (MMP)-2 and MMP-9 in HaCaT cells or MMP-1 expression in MRC-5 cells. AFEOR induced genotoxicity in MRC-5 cells with a DNA damage index between 40% and 60% when compared to the negative controls (0%-20%).
For the first time, biological activities from oil-resin demonstrated ratifying somehow its popular use.
Analysis of crude oil-resin and fractionation of diterpenic fraction was performance using selective ion-exchange column chromatographyCytotoxicity analysis and morphology were performed with different cell linesCollagen production in human fibroblasts, inhibition of metalloproteinases were demonstrated by zymography and Western blotting. AFEOR: oil-resin.
杜克油树脂在民间医学中的使用方式与古巴香脂油( spp.)类似。
本研究旨在探究杜克油树脂酸馏分(AFEOR)对细胞增殖、人成纤维细胞中胶原蛋白生成、金属蛋白酶抑制以及对肿瘤细胞系的细胞毒性的影响。
通过离子交换柱色谱法对杜克油树脂进行酸馏分分离。采用阿拉玛蓝法和彗星试验评估细胞毒性和遗传毒性。通过酶谱法和蛋白质免疫印迹法检测金属蛋白酶的抑制情况。
AFEOR中主要的酸性二萜类化合物为古巴香脂酸和哈迪威克酸。当浓度高于5μg/mL时,AFEOR会导致形态改变并降低细胞增殖。它还能显著促进成纤维细胞中的胶原蛋白增殖。它对肿瘤细胞系和非肿瘤细胞系均表现出细胞毒性,IC值范围为13至50μg/mL,溶血活性的IC值为38.29μg/mL。AFEOR抑制胶原酶活性,IC值为46.64μg/mL,对HaCaT细胞中的基质金属蛋白酶-2(MMP)-2和MMP-9或MRC-5细胞中的MMP-1表达也有抑制作用。与阴性对照(0%-20%)相比,AFEOR在MRC-5细胞中诱导遗传毒性,DNA损伤指数在40%至60%之间。
首次证明杜克油树脂的生物活性在一定程度上证实了其民间用途。
使用选择性离子交换柱色谱法对原油树脂进行分析并分离二萜馏分,对不同细胞系进行细胞毒性分析和形态学观察,通过酶谱法和蛋白质免疫印迹法证明人成纤维细胞中的胶原蛋白生成以及金属蛋白酶的抑制情况。AFEOR:杜克油树脂。