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富勒烯多酚提取物通过抑制苯并[a]芘诱导的 P2X7 激活和毒性作用的体外化学预防潜力。

In Vitro Chemopreventive Potential of Phlorotannins-Rich Extract from Brown Algae by Inhibition of Benzo[a]pyrene-Induced P2X7 Activation and Toxic Effects.

机构信息

Recherche & Développement, Yslab, 29000 Quimper, France.

Faculté de Pharmacie de Paris, UMR CNRS 8038, Université de Paris, 75006 Paris, France.

出版信息

Mar Drugs. 2021 Jan 14;19(1):34. doi: 10.3390/md19010034.

Abstract

Phlorotannins are polyphenols occurring exclusively in some species of brown algae, known for numerous biological activities, e.g., antioxidant, antiproliferative, antidiabetic, and antiallergic properties. Their effects on the response of human lung cells to benzo[a]pyrene (B[a]P) has not been characterized. Our objective was to in vitro evaluate the effects of a phlorotannin-rich extract obtained from the brown algae and on B[a]P cytotoxic effects. The A549 cell line was incubated with B[a]P for 48 and 72 h in the presence or absence of the brown algae extract. Cytochrome P450 activity, activation of P2X7 receptor, F-actin disorganization, and loss of E-cadherin expression were assessed using microplate cytometry and fluorescence microscopy. Relative to control, incubation with the brown algae extract was associated with lower B[a]P-induced CYP1 activity, lower P2X7 receptor activation, and lower reactive oxygen species production. The brown algae extract inhibited the alterations of F-actin arrangement and the downregulation of E-cadherin expression. We identified a phlorotannins-rich extract that could be deeper investigated as a cancer chemopreventive agent to block B[a]P-mediated carcinogenesis.

摘要

岩藻黄质是仅存在于某些褐藻物种中的多酚类化合物,具有多种生物活性,如抗氧化、抗增殖、抗糖尿病和抗过敏特性。然而,其对人体肺细胞对苯并[a]芘(B[a]P)反应的影响尚未得到描述。我们的目的是在体外评估从褐藻 和 中获得的富含岩藻黄质的提取物对 B[a]P 细胞毒性的影响。A549 细胞系在存在或不存在褐藻提取物的情况下,分别用 B[a]P 孵育 48 和 72 小时。使用微孔板细胞仪和荧光显微镜评估细胞色素 P450 活性、P2X7 受体的激活、F-肌动蛋白解聚以及 E-钙粘蛋白表达的丧失。与对照相比,用褐藻提取物孵育与 B[a]P 诱导的 CYP1 活性降低、P2X7 受体激活降低和活性氧产生降低有关。褐藻提取物抑制 F-肌动蛋白排列的改变和 E-钙粘蛋白表达的下调。我们鉴定出一种富含岩藻黄质的提取物,它可以作为一种癌症化学预防剂,更深入地研究其对 B[a]P 介导的致癌作用的阻断作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1cc/7828825/ce6a513c6a20/marinedrugs-19-00034-g001.jpg

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