巴西红蜂胶提取物:ESI-MS/MS (ESI+)化学成分及对结肠癌细胞系的细胞毒性研究

Denis Amilton dos Santos , Fernanda Mosena Munari , Caroline Olivieri da Silva Frozza , Sidnei Moura , Thiago Barcellos , João Antonio Pêgas Henriques , Mariana Roesch-Ely
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引用次数: 19

摘要

红蜂胶是一种由蜜蜂生产的天然树脂混合物,是具有多种生物活性的活性化合物的来源。在本研究中,我们描述了巴西红蜂胶总提取物及其组分的化学性质和潜在的抗肿瘤活性。通过柱层析得到14种不同的化合物,并在阳性模式下通过ESI-MS/MS裂解途径与其他等压线分子进行鉴定。通过片段途径将顺式细辛烷和反式异茴香素等分子与茴香素化合物区分开来,并将异茴香醇和新茴香醇区分开来。从黄豆素中分离出了异黄豆素和刺芒柄花素等重要化合物。MTT活性试验表明,总提取物和部分提取物对细胞系的毒性不同。与正常细胞相比,组分05和组分06分别对HT-29和HCT-116癌细胞具有更高的选择性。蜂胶总提取物的IC50值(72.45±6.57 ~ 73.58±1.00 μg/mL)低于文献报道。May-Grunwald/Giemsa染色显示暴露于高浓度红色蜂胶提取物后的细胞形态学变化。分离技术有助于减少蜂胶混合物中已证实的化学多样性,产生具有更高生物活性的组分,并有助于开发新的策略来发现抗癌的天然化合物。
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Brazilian red propolis extracts: study of chemical composition by ESI-MS/MS (ESI+) and cytotoxic profiles against colon cancer cell lines

Red propolis is a natural resin mixture produced by honeybees and presents a source of active compounds with a variety of biological activities. In this study, we describe the chemical characterization and potential antitumor activity of total extract of Brazilian red propolis and its fractions. Fractions were obtained through column chromatography revealing 14 different compounds in all samples, which were determined and distinguished of other isobar molecules by fragmentation pathways by ESI-MS/MS in positive mode. Some molecules as cis-asarone or trans-isoelemicin were identified and distinguish from elemicin compound and vestitol or isovestitol were also distinguished from neovestitol by fragmention pathway. Other important compounds as liquiritigenin was differentiated from isoliquiritigenin and formononetin from dalbergin.

MTT viability assay showed different toxicity in cell lines after exposition to total extract and fractions. Fractions 05 and 06 had more selectivity against HT-29 and HCT-116 cancer cells, respectively, in relation to normal cells. IC50 (ranging of 72.45 ± 6.57 to 73.58 ± 1.00 μg/mL) in cancer cells were lower than reported in total extracts of propolis. May-Grunwald/Giemsa staining revealed cellular morphological changes after exposition to higher concentrations of red propolis extracts. Fractionation techniques can contribute to reduce chemical diversity verified in propolis mixtures, generating fractions with improved biological activity and contributing to the development of new strategies for discovery of natural compounds against cancer.

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