Antitumoral effects of Santolina chameacyparissus on Non-Small Cell Lung Cancer Cells

Y. Saygıdeğer, Burcu Saygıdeğer Demir, Tuğba Taşkın Tok, A. Avcı, Aycan Sezan, Oya Baydar, E. Ozyilmaz
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引用次数: 6

Abstract

Santolina chameacyparissus (Santo) is an evergreen plant which is traditionally used for its anti-inflammatory effects in various diseases. In this study, we aimed to explore the effects of Santo in non-small cell lung cancer cells. We extracted volatile oil from the plant and evaluated cytotoxicity, apoptosis and motility effects of the extract on two non-small cell lung cancer (NSCLC) cell lines; one is a patient derived and the other one is a commercially available. We also identified its components via GS/MS and investigated possible targets of the major components of the plant using qPCR and docking studies. Cytotoxicity tests showed dose dependent cell killing activity and flow cytometry assays exposed apoptotic effects of Santo. The essential oil also remarkably decreased migration rate of A549 cells, therefore we evaluated the expression levels of epithelial to mesenchymal transition related genes E-cadherin and Vimentin ratio, ZEB1 and SNAIL and another motility related gene Ezrin. Santo did not change the expression of EMT related genes but decreased Ezrin levels. According to the results of the GS/MS analysis, Artemisia ketone and Camphor were identified as major molecules of the extract. Docking analysis also revealed that artemisia ketone, the major component of the Santo extract, potentially showed strong binding to the active site of ezrin protein and both artemisia ketone and camphor had ability to bind DNA. The results of the present study indicate that Santo and its components artemisia ketone and camphor are promising anti-cancer agents, and their potential in targeting DNA and oncogenic proteins in the lung cancer cells seems worth to focus on this plant in cancer related drug discovery science.
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金银花对非小细胞肺癌细胞的抗肿瘤作用
Santolina chameacyparissus (Santo)是一种常绿植物,传统上因其抗炎作用而被用于治疗各种疾病。在这项研究中,我们旨在探讨Santo在非小细胞肺癌细胞中的作用。我们从该植物中提取挥发油,并评估其对两种非小细胞肺癌(NSCLC)细胞株的细胞毒性、凋亡和运动作用;一种是病人衍生的另一种是市售的。我们还通过GS/MS鉴定了其成分,并利用qPCR和对接研究研究了该植物主要成分的可能靶点。细胞毒性试验显示剂量依赖性细胞杀伤活性,流式细胞术检测显示Santo的凋亡作用。因此,我们对A549细胞上皮向间质转化相关基因E-cadherin和Vimentin ratio、ZEB1和SNAIL以及另一个运动性相关基因Ezrin的表达水平进行了评估。Santo没有改变EMT相关基因的表达,但降低了Ezrin水平。GS/MS分析结果表明,提取物的主要成分为蒿酮和樟脑。对接分析还发现,桑托提取物的主要成分青蒿酮可能与ezrin蛋白活性位点结合较强,青蒿酮和樟脑均具有结合DNA的能力。本研究结果表明,桑托及其成分青蒿酮和樟脑是很有前景的抗癌药物,其靶向肺癌细胞DNA和致癌蛋白的潜力值得在癌症相关药物发现科学中关注。
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