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虎杖的分子特征化溶剂提取物和皂苷具有高抗血管生成、抗肿瘤、卤虫毒性及对成纤维细胞NIH/3T3细胞系的细胞毒性。

Molecularly Characterized Solvent Extracts and Saponins from Polygonum hydropiper L. Show High Anti-Angiogenic, Anti-Tumor, Brine Shrimp, and Fibroblast NIH/3T3 Cell Line Cytotoxicity.

作者信息

Ayaz Muhammad, Junaid Muhammad, Ullah Farhat, Sadiq Abdul, Subhan Fazal, Khan Mir Azam, Ahmad Waqar, Ali Gowhar, Imran Muhammad, Ahmad Sajjad

机构信息

Department of Pharmacy, University of Malakand Khyber Pakhtoonkhwa, Pakistan.

Department of Pharmacy, University of Peshawar Peshawar, Pakistan.

出版信息

Front Pharmacol. 2016 Mar 31;7:74. doi: 10.3389/fphar.2016.00074. eCollection 2016.

Abstract

Polygonum hydropiper is used as anti-cancer and anti-rheumatic agent in folk medicine. This study was designed to investigate the anti-angiogenic, anti-tumor, and cytotoxic potentials of different solvent extracts and isolated saponins. Samples were analyzed using GC, Gas Chromatography-Mass Spectrometry (GC-MS) to identify major and bioactive compounds. Quantitation of antiangiogenesis for the plant's samples including methanolic extract (Ph.Cr), its subsequent fractions; n-hexane (Ph.Hex), chloroform (Ph.Chf), ethyl acetate (Ph.EtAc), n-Butanol (Ph.Bt), aqueous (Ph.Aq), saponins (Ph.Sp) were performed using the chick embryo chorioallantoic membrane (CAM) assay. Potato disc anti-tumor assay was performed on Agrobacterium tumefaciens containing tumor inducing plasmid. Cytotoxicity was performed against Artemia salina and mouse embryonic fibroblast NIH/3T3 cell line following contact toxicity and MTT cells viability assays, respectively. The GC-MS analysis of Ph.Cr, Ph.Hex, Ph.Chf, Ph.Bt, and Ph.EtAc identified 126, 124, 153, 131, and 164 compounds, respectively. In anti-angiogenic assay, Ph.Chf, Ph.Sp, Ph.EtAc, and Ph.Cr exhibited highest activity with IC50 of 28.65, 19.21, 88.75, and 461.53 μg/ml, respectively. In anti-tumor assay, Ph.Sp, Ph.Chf, Ph.EtAc, and Ph.Cr were most potent with IC50 of 18.39, 73.81, 217.19, and 342.53 μg/ml, respectively. In MTT cells viability assay, Ph.Chf, Ph.EtAc, Ph.Sp were most active causing 79.00, 72.50, and 71.50% cytotoxicity, respectively, at 1000 μg/ml with the LD50 of 140, 160, and 175 μg/ml, respectively. In overall study, Ph.Chf and Ph.Sp have shown overwhelming results which signifies their potentials as sources of therapeutic agents against cancer.

摘要

水蓼在民间医学中被用作抗癌和抗风湿药物。本研究旨在调查不同溶剂提取物和分离出的皂苷的抗血管生成、抗肿瘤和细胞毒性潜力。使用气相色谱(GC)、气相色谱 - 质谱联用(GC-MS)对样品进行分析,以鉴定主要和生物活性化合物。采用鸡胚绒毛尿囊膜(CAM)试验对该植物样品进行抗血管生成定量分析,这些样品包括甲醇提取物(Ph.Cr)及其后续馏分;正己烷(Ph.Hex)、氯仿(Ph.Chf)、乙酸乙酯(Ph.EtAc)、正丁醇(Ph.Bt)、水相(Ph.Aq)、皂苷(Ph.Sp)。对含有肿瘤诱导质粒的根癌土壤杆菌进行马铃薯圆盘抗肿瘤试验。分别通过接触毒性试验和MTT细胞活力试验,对卤虫和小鼠胚胎成纤维细胞NIH/3T3细胞系进行细胞毒性试验。对Ph.Cr、Ph.Hex、Ph.Chf、Ph.Bt和Ph.EtAc的GC-MS分析分别鉴定出126、124、153、131和164种化合物。在抗血管生成试验中,Ph.Chf、Ph.Sp、Ph.EtAc和Ph.Cr表现出最高活性,IC50分别为28.65、19.21、88.75和461.53μg/ml。在抗肿瘤试验中,Ph.Sp、Ph.Chf、Ph.EtAc和Ph.Cr最有效,IC50分别为18.39、73.81、217.19和342.53μg/ml。在MTT细胞活力试验中,Ph.Chf、Ph.EtAc、Ph.Sp最具活性,在1000μg/ml时分别引起79.00%、72.50%和71.50%的细胞毒性,LD50分别为140、160和175μg/ml。在整体研究中,Ph.Chf和Ph.Sp显示出压倒性的结果,这表明它们作为抗癌治疗剂来源的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2cf0/4814464/3b63b700109f/fphar-07-00074-g0001.jpg

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