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来自巴西补血草的黄烷-3-醇和原花青素通过与牙龈蛋白酶相互作用,抑制牙龈卟啉单胞菌对上皮宿主细胞的黏附。

Flavan-3-ols and proanthocyanidins from Limonium brasiliense inhibit the adhesion of Porphyromonas gingivalis to epithelial host cells by interaction with gingipains.

作者信息

de Oliveira Caleare Angelo, Hensel Andreas, Mello João Carlos Palazzo, Pinha Andressa Blainski, Panizzon Gean Pier, Lechtenberg Matthias, Petereit Frank, Nakamura Celso Vataru

机构信息

State University of Maringá, Postgraduate Program in Biological Sciences, Laboratory of Technological Innovation in the Development of Drugs and Cosmetics, BR-87020-900, Maringá, Brazil.

University of Münster, Institute of Pharmaceutical Biology and Phytochemistry, Corrensstraße 48, D-48149 Münster, Germany.

出版信息

Fitoterapia. 2017 Apr;118:87-93. doi: 10.1016/j.fitote.2017.03.002. Epub 2017 Mar 11.

DOI:10.1016/j.fitote.2017.03.002
PMID:28288871
Abstract

Porphyromonas gingivalis is a pathogen strongly involved in chronic and aggressive forms of periodontitis. Natural products, mainly polyphenols, have been described for advanced treatment of periodontitis by inhibition of the bacterial adhesion of P. gingivalis to the epithelial host cells. An acetone:water extract (LBE) from the rhizomes of Limonium brasiliense (Boiss.) Kuntze was tested under in vitro conditions for potential antiadhesive effects against P. gingivalis to human KB cells and for inhibition of the proteolytic activity of gingipains, the main virulence factor of P. gingivalis. LBE≤100μg/mL had no cytotoxicity against the bacteria and did not influence the cell physiology of human epithelial KB cells. At 100μg/mL LBE reduced the adhesion of P. gingivalis to KB cells significantly by about 80%. LBE at 20μg/mL reduced the proteolytic activity of the arginin-specific Rgp gingipain by about 75%. Chemical profiling of LBE indicated the presence of gallic acid, epigallocatechin-3-O-gallate and samarangenins A and B as lead compounds. UHPLC by using MS and UV detection displays a suitable method for quality control of the extract for identification and quantification of the lead compounds.

摘要

牙龈卟啉单胞菌是一种与慢性和侵袭性牙周炎密切相关的病原体。天然产物,主要是多酚类,已被描述用于通过抑制牙龈卟啉单胞菌与上皮宿主细胞的细菌粘附来进行牙周炎的进阶治疗。对巴西补血草(Boiss.)Kuntze根茎的丙酮:水提取物(LBE)在体外条件下测试其对牙龈卟啉单胞菌与人KB细胞的潜在抗粘附作用以及对牙龈蛋白酶(牙龈卟啉单胞菌的主要毒力因子)蛋白水解活性的抑制作用。LBE≤100μg/mL对细菌无细胞毒性,且不影响人上皮KB细胞的细胞生理。在100μg/mL时,LBE显著降低牙龈卟啉单胞菌对KB细胞的粘附约80%。在20μg/mL时,LBE使精氨酸特异性Rgp牙龈蛋白酶的蛋白水解活性降低约75%。LBE的化学分析表明存在没食子酸、表没食子儿茶素-3-O-没食子酸酯以及3,5-二咖啡酰奎宁酸和3,4-二咖啡酰奎宁酸作为主要化合物。使用质谱和紫外检测的超高效液相色谱法是用于提取物质量控制以鉴定和定量主要化合物的合适方法。

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