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将生物信息学与药理学评价相结合,阐明了复方胶艾合剂抑制肺癌的作用机制。

Integrating bioinformatics with pharmacological evaluation for illustrating the action mechanism of herbal formula Jiao'e mixture in suppressing lung carcinoma.

机构信息

Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, 71000, Xi'an, China; College of Pharmacy, Shaanxi University of Chinese Medicine, 712046, Xianyang, China.

Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, 71000, Xi'an, China.

出版信息

J Ethnopharmacol. 2021 Dec 5;281:114513. doi: 10.1016/j.jep.2021.114513. Epub 2021 Aug 13.

DOI:10.1016/j.jep.2021.114513
PMID:34400263
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Lung carcinoma (LC) is not only a kind of disease that seriously threatens human life but also an intractable problem in modern medicine. Jiao'e Mixture (JEM) is an innovative Chinese medicine formula with Chinese patent, which is composed of two herbal extracts with a specific ratio-zedoary turmeric oil and medicinal Zanthoxylum bungeanum Maxim(Z. bungeanum Maxim) seeds oil (ZMSO). Zedoary turmeric oil is extracted from dried rhizomes of Curcuma wenyujin Y.H.Chen et C. Ling, which has been reported have an anti-cancer effects. Medicinal ZMSO is a by-product of Z. bungeanum Maxim, refined from kernel shell separation, modern cold soaking and refining technology; JEM is used to treat Lung carcinoma (LC) patients in folk for many years. However, its therapeutic mechanisms for treating LC have not been fully explored.

AIM OF THE STUDY

The purpose of this study was to explore the therapeutic mechanisms of JEM for treating LC.

MATERIALS AND METHODS

The action mechanism of JEM in LC treatment was analysed by comprehensive network pharmacology approach combined with experimental validation (in vivo and in vitro).

RESULTS

Seventeen active compounds and 457 related targets were collected from the HERB, TCMSP, and Swiss Target Prediction platforms. Nine hundred and thirty-eight LC related targets were obtained from Gene Cards and OMIM databases. Finally, 140 overlapping targets were obtained, which representing the target of JEM in LC treatment. The pathway analysis showed that PI3K-AKT could be a potential pathway for JEM in LC treatment. In vivo results presented that JEM had a good effect in inhibiting the growth of LC tumour cells with high efficacy and low toxicity. In vitro experiments validated that JEM had inhibited LC cells' proliferation, migration and invasion, and had induced cell apoptosis mainly via PI3K/Akt signalling pathways.

CONCLUSION

The anti-LC activity of JEM might via regulating the PI3K-AKT signalling pathways.This study may provide further evidence for the potential use of JEM in LC treatment.

摘要

民族药理学相关性

肺癌(LC)不仅是一种严重威胁人类生命的疾病,也是现代医学中的一个难题。椒莪合剂(JEM)是一种具有中国专利的创新中药配方,由两种草药提取物按特定比例组成——莪术油和药用花椒籽油(ZMSO)。莪术油是从温郁金干燥根茎中提取的,已报道其具有抗癌作用。药用 ZMSO 是花椒的副产物,采用现代冷浸精炼技术,从仁壳分离中精制而成;JEM 多年来一直用于民间治疗肺癌(LC)患者。然而,其治疗 LC 的机制尚未得到充分探索。

研究目的

本研究旨在探讨 JEM 治疗 LC 的作用机制。

材料和方法

采用综合网络药理学方法结合实验验证(体内和体外)分析 JEM 治疗 LC 的作用机制。

结果

从 HERB、TCMSP 和 Swiss Target Prediction 平台收集了 17 种活性化合物和 457 个相关靶点。从 GeneCards 和 OMIM 数据库获得了 938 个与 LC 相关的靶点。最终获得了 140 个重叠靶点,代表了 JEM 治疗 LC 的靶点。通路分析表明,PI3K-AKT 可能是 JEM 治疗 LC 的潜在通路。体内结果表明,JEM 对 LC 肿瘤细胞的生长具有良好的抑制作用,疗效高,毒性低。体外实验验证了 JEM 通过 PI3K/Akt 信号通路抑制 LC 细胞增殖、迁移和侵袭,并诱导细胞凋亡。

结论

JEM 的抗 LC 活性可能通过调节 PI3K-AKT 信号通路发挥作用。本研究可为 JEM 治疗 LC 的潜在应用提供进一步的证据。

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