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一种穿心莲内酯在调节牙周细胞转录因子和靶基因差异表达中的功效的离体评价及其在牙周病治疗中的潜在作用。

An ex vivo evaluation of the efficacy of andrographolide in modulating differential expression of transcription factors and target genes in periodontal cells and its potential role in treating periodontal diseases.

机构信息

PMS College of Dental Sciences and Research, Trivandrum 695028, Kerala, India.

Government Dental College, Trivandrum 695011, Kerala, India.

出版信息

J Ethnopharmacol. 2017 Jan 20;196:160-167. doi: 10.1016/j.jep.2016.12.029. Epub 2016 Dec 16.

Abstract

ETHANOPHARMACOLOGICAL RELEVANCE

Andrographolide is a herbal extract traditionally used in South Asian countries for treating inflammatory diseases.

AIM OF THE STUDY

To evaluate the efficacy of andrographolide in management of periodontal disease which is a highly prevalent oral disease.

MATERIALS AND METHODS

Periodontal ligament fibroblasts (PDLF) were cultured from healthy and diseased periodontium using explant culture methods. The safe dose of AG was determined using MTT assay. LPS (lipopolysaccharide) of the most important periodontopathogen, P gingivalis was used to activate NF-κB and STAT3 in PDLF. The efficacy of AG in inhibiting NF-κB and STAT3 was analyzed using immunofluorescence. Down regulation of expression of target genes of these transcription factors related to inflammation and bone resorption were analyzed using real time PCR.

RESULTS

AG up to the concentration of 25μM was found to be safe as determined by MTT assay. Statistically significant activation of NF-κB and STAT3 in cultured PDLF was observed in diseased group compared to healthy controls before and after LPS challenge. 5μM AG pretreatment significantly inhibited activation of NF-κB and STAT3 and down regulated expression of inflammatory and bone resorptive genes in cultured PDLF.

CONCLUSIONS

The findings of the present study propose the adjunctive use of a novel herbal drug andrographolide as a promising host modulation agent for periodontal therapy by inhibiting NF-κB and STAT3 activation and inhibition of inflammation and bone resorption related genes.

摘要

药代动力学相关性

穿心莲内酯是一种传统的草药提取物,在南亚国家用于治疗炎症性疾病。

研究目的

评估穿心莲内酯在治疗牙周病中的疗效,牙周病是一种高发的口腔疾病。

材料和方法

采用组织块培养法从健康和患病牙周组织中培养牙周韧带成纤维细胞(PDLF)。采用 MTT 法测定 AG 的安全剂量。用最主要的牙周致病菌 P gingivalis 的 LPS(脂多糖)激活 PDLF 中的 NF-κB 和 STAT3。用免疫荧光法分析 AG 抑制 NF-κB 和 STAT3 的效果。采用实时 PCR 分析与炎症和骨吸收相关的这些转录因子的靶基因表达下调情况。

结果

MTT 测定结果表明,高达 25μM 的 AG 是安全的。与健康对照组相比,LPS 刺激前后培养的 PDLF 中,患病组 NF-κB 和 STAT3 的激活明显增加。5μM AG 预处理可显著抑制 NF-κB 和 STAT3 的激活,并下调培养的 PDLF 中炎症和骨吸收相关基因的表达。

结论

本研究的结果表明,穿心莲内酯作为一种新型的草药药物,可以作为牙周治疗的辅助药物,通过抑制 NF-κB 和 STAT3 的激活以及抑制炎症和骨吸收相关基因的表达,具有很大的潜力。

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