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抗氧化、抗肿瘤、抗转移作用及抑制 Eleutherine bulbosa(达雅克洋葱)提取物胶原酶活性的作用:体外、体内和计算机模拟方法。

Antioxidant, antitumoral, antimetastatic effect and inhibition of collagenase enzyme activity of Eleutherine bulbosa (Dayak onion) extract: In vitro, in vivo and in silico approaches.

机构信息

School of Sciences, Humanities and Languages, Department of Biotechnology, Laboratory of Phytotherapic and Natural Products, São Paulo State University (UNESP), Assis, São Paulo, Brazil; Institute of Chemistry, São Paulo State University (UNESP), Araraquara, São Paulo, Brazil.

School of Sciences, Humanities and Languages, Department of Biotechnology, Laboratory of Phytotherapic and Natural Products, São Paulo State University (UNESP), Assis, São Paulo, Brazil.

出版信息

J Ethnopharmacol. 2024 Jan 10;318(Pt B):117005. doi: 10.1016/j.jep.2023.117005. Epub 2023 Aug 5.

DOI:10.1016/j.jep.2023.117005
PMID:37544339
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Eleutherine bulbosa (Mill.) Urb., known in Brazil as "marupazinho", is a medicinal plant native to the Amazon region. The bulbs of this species are traditionally used in the form of tea or consumed in natura (salads) for the treatment of hypertension, diabetes, gastrointestinal problems, breast cancer, and female fertility. It has been reported that this species possess cytotoxic compounds with anticancer action and limited underlying mechanisms.

AIM OF THE STUDY

This study aimed to analyze extract of E. bulbosa bulbs and evaluate antioxidant activity, antitumor and antimetastatic effects against murine B16F10-Nex2 melanoma cells, and collagenase inhibitory activity by in vitro, in vivo, and in silico approaches.

MATERIALS AND METHODS

Determination of total polyphenols, flavonoids and anthocyanins content were performed. In addition, high performance liquid chromatography-mass spectrometry (HPLC-MS) was carried out to identify phytoconstituents from extract. Antioxidant evaluation was performed using DPPH radical scavenging, ferric ion reducing antioxidant power (FRAP), Thiobarbituric acid reactive species (TBARS) and nitric oxide (NO) tests. Antitumoral and antimetastatic activities of extract on murine B16F10-Nex2 melanoma cells were determined and inhibitory activity on collagenase was evaluated. Molecular interactions between compounds and DNA or collagenase was evaluated by molecular docking analyses.

RESULTS

Phytochemical evaluation demonstrated the presence of polyphenols, flavonoids and anthocyanins, and HPLC-MS identified the major presence of eleutherin, isoeleutherin and eleutherinol. Antioxidant evaluation showed that the extract present significant activity in all methods evaluated. In silico assay demonstrated interaction between bioactive compounds and DNA or collagenase. In addition, extract exhibited antitumor and antimetastatic actions promoted by melanoma cells and showed collagenase inhibitory activity.

CONCLUSIONS

The results showed that E. bulbosa bulb extract contains bioactive compounds as flavonoids, anthocyanins and quinones of which may be responsible for the antioxidant, antitumor, antimetastatic and collagenase enzyme inhibitory activity observed in this study by in vivo, in vitro and in silico bioassays.

摘要

民族药理学相关性

Eleutherine bulbosa(Mill.)Urb.,在巴西被称为“marupazinho”,是一种原产于亚马逊地区的药用植物。该物种的鳞茎传统上以茶的形式使用或生吃(沙拉)用于治疗高血压、糖尿病、胃肠道问题、乳腺癌和女性生育能力。据报道,该物种具有细胞毒性化合物,具有抗癌作用和有限的潜在机制。

研究目的

本研究旨在分析 Eleutherine bulbosa 鳞茎提取物,并通过体内、体外和计算机模拟方法评估其抗氧化活性、抗肿瘤和抗转移作用以及对胶原蛋白酶的抑制活性。

材料和方法

测定总多酚、类黄酮和花青素含量。此外,还进行了高效液相色谱-质谱(HPLC-MS)分析,以鉴定提取物中的植物成分。通过 DPPH 自由基清除、铁还原抗氧化能力(FRAP)、硫代巴比妥酸反应性物质(TBARS)和一氧化氮(NO)测试评估抗氧化活性。测定提取物对小鼠 B16F10-Nex2 黑素瘤细胞的抗肿瘤和抗转移活性,并评价其对胶原蛋白酶的抑制活性。通过分子对接分析评估化合物与 DNA 或胶原蛋白酶之间的分子相互作用。

结果

植物化学评价表明存在多酚、类黄酮和花青素,HPLC-MS 鉴定出主要存在的 eleutherin、isoeleutherin 和 eleutherinol。抗氧化评价表明,提取物在所有评估方法中均表现出显著的活性。计算机模拟试验表明,生物活性化合物与 DNA 或胶原蛋白酶之间存在相互作用。此外,提取物表现出抗肿瘤和抗转移作用,促进黑色素瘤细胞的发生,并表现出胶原蛋白酶抑制活性。

结论

结果表明, Eleutherine bulbosa 鳞茎提取物含有生物活性化合物,如类黄酮、花青素和醌,这些化合物可能是通过体内、体外和计算机模拟生物测定观察到的抗氧化、抗肿瘤、抗转移和胶原蛋白酶抑制活性的原因。

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