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从诃子中提取的富含 eschweilenol C 的部分的抗真菌和抗炎潜力。

Antifungal and anti-inflammatory potential of eschweilenol C-rich fraction derived from Terminalia fagifolia Mart.

机构信息

The Northeast Biotechnology Network, RENORBIO, Federal University of Piaui, Teresina, PI, Brazil.

Biotechnology and Biodiversity Center Research, Biotec, Federal University of Piaui, Parnaíba, Piaui, Brazil.

出版信息

J Ethnopharmacol. 2019 Aug 10;240:111941. doi: 10.1016/j.jep.2019.111941. Epub 2019 May 15.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Folk knowledge transmitted between generations allows traditional populations to maintain the use of medicinal plants for the treatment of several diseases. In this context, the species Terminalia fagifolia Mart., native to Brazil, is used for the treatment of chronic and infectious diseases. Plants rich in secondary metabolites, such as this species and their derivatives, may represent therapeutic alternatives for the treatment of diseases that reduce the quality of life of people.

AIM OF THE STUDY

The aim of this study was to evaluate the antifungal and anti-inflammatory potential of aqueous fraction from ethanolic extract of T. fagifolia, with in silico study of the major compound of the fraction.

MATERIAL AND METHODS

The phytochemical study of the aqueous fraction was performed by HPLC, LC/MS and NMR. The antifungal activity was evaluated against yeasts, by determination of the minimum inhibitory concentration and minimum fungicidal concentration. The effect on Candida albicans was analyzed by AFM. The antibiofilm potential against biofilms of C. albicans was also tested. The anti-inflammatory potential of the aqueous fraction was evaluated in vivo by the carrageenan-induced paw edema and peritonitis. A microglial model of LPS-induced neuroinflammation was also studied. Further insights on the activation mechanism were studied using quantum chemistry computer simulations. Toxicity was evaluated in the Galleria mellonella and human erythrocytes models.

RESULTS

Eschweilenol C was identified as the major constituent of the aqueous fraction of the ethanolic extract of T. fagifolia. The aqueous fraction was active against all Candida strains used (sensitive and resistant to Fluconazole) with MICs ranging from 1000 to 0.4 μg/mL. By AFM it was possible to observe morphological alterations in treated Candida cells. The fraction significantly (p < 0.05) inhibited paw edema and decreased levels of malondialdehyde induced by carrageenan. In a microglial cell model, aqueous fraction demonstrated the ability to inhibit NF-κB after induction with lipopolysaccharide. The theoretical studies showed structural similarity between eschweilenol C and indomethacin and an excellent antioxidant potential. The aqueous fraction did not present toxicity in the studied models.

CONCLUSION

The results indicate that the aqueous fraction of T. fagifolia has potential for biomedical applications with low toxicity. This finding can be attributed to the predominance of eschweilenol C in the aqueous fraction.

摘要

民族药理学相关性

世代相传的民间知识使传统人群能够使用药用植物治疗多种疾病。在这种情况下,原产于巴西的Terminalia fagifolia Mart. 被用于治疗慢性和传染性疾病。富含次生代谢产物的植物,如该物种及其衍生物,可能为治疗降低人们生活质量的疾病提供治疗选择。

研究目的

本研究旨在评估来自 T. fagifolia 乙醇提取物的水相部分的抗真菌和抗炎潜力,并对该部分的主要化合物进行计算机模拟研究。

材料和方法

通过 HPLC、LC/MS 和 NMR 对水相部分进行植物化学研究。通过测定最小抑菌浓度和最小杀菌浓度评估抗真菌活性。通过原子力显微镜 (AFM) 分析对白色念珠菌的作用。还测试了水相部分对白色念珠菌生物膜的抗生物膜潜力。通过角叉菜胶诱导的爪肿胀和腹膜炎评估水相部分的抗炎潜力。还研究了 LPS 诱导的神经炎症的小胶质细胞模型。使用量子化学计算机模拟进一步研究了激活机制的见解。在 Galleria mellonella 和人红细胞模型中评估了毒性。

结果

鉴定出水相部分的主要成分为 eschweilenol C。水相部分对所有使用的白色念珠菌菌株均有效(对氟康唑敏感和耐药),MIC 范围为 1000 至 0.4 μg/mL。通过 AFM 可以观察到处理过的白色念珠菌细胞的形态改变。该部分显著(p<0.05)抑制了角叉菜胶诱导的爪肿胀,并降低了 MDA 的水平。在小胶质细胞模型中,水相部分在脂多糖诱导后显示出抑制 NF-κB 的能力。理论研究表明,eschweilenol C 与吲哚美辛在结构上具有相似性,且具有良好的抗氧化潜力。水相部分在研究的模型中没有表现出毒性。

结论

结果表明,T. fagifolia 的水相部分具有低毒性的生物医学应用潜力。这一发现可以归因于水相部分中 eschweilenol C 的优势。

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