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体外生物测定法指导下从紫苏叶中鉴定对MDA - MB - 231细胞系的抗癌特性

In Vitro Bioassay-Guided Identification of Anticancer Properties from Lam. Leaf against the MDA-MB-231 Cell Line.

作者信息

Wisitpongpun Prapakorn, Suphrom Nungruthai, Potup Pachuen, Nuengchamnong Nitra, Calder Philip C, Usuwanthim Kanchana

机构信息

Cellular and Molecular Immunology Research Unit (CMIRU), Faculty of Allied Health Sciences, Naresuan University, Phitsanulok 65000, Thailand.

Department of Chemistry, Faculty of Science and Center of Excellence for Innovation in Chemistry, Naresuan University, Phitsanulok 65000, Thailand.

出版信息

Pharmaceuticals (Basel). 2020 Dec 15;13(12):464. doi: 10.3390/ph13120464.

Abstract

Lam. (MO) is a medicinal plant distributed across the Middle East, Asia, and Africa. MO has been used in the traditional treatment of various diseases including cancer. This study aimed to perform bioassay-guided fractionation and identification of bioactive compounds from MO leaf against MDA-MB-231 breast cancer cells. MO leaf was sequentially extracted with hexane, ethyl acetate (EtOAc), and ethanol. The most effective extract was subjected to fractionation. MO extract and its derived fractions were continuously screened for anti-cancer activities. The strongest fraction was selected for re-fractionation and identification of bioactive compounds using LC-ESI-QTOF-MS/MS analysis. The best anticancer activities were related to the fraction no. 7-derived crude EtOAc extract. This fraction significantly reduced cell viability and clonogenic growth and increased cells apoptosis. Moreover, sub-fraction no. 7.7-derived fraction no. 7 was selected for the identification of bioactive compounds. There were 10 candidate compounds tentatively identified by LC-ESI-QTOF-MS. Three of identified compounds (7-octenoic acid, oleamide, and 1-phenyl-2-pentanol) showed anticancer activities by inducing cell cycle arrest and triggering apoptosis through suppressed Bcl-2 expression which subsequently promotes activation of caspase 3, indicators for the apoptosis pathway. This study identified 10 candidate compounds that may have potential in the field of anticancer substances.

摘要

拉莫(MO)是一种分布于中东、亚洲和非洲的药用植物。MO已被用于包括癌症在内的各种疾病的传统治疗。本研究旨在对MO叶进行生物测定指导的分级分离,并鉴定其对MDA-MB-231乳腺癌细胞具有生物活性的化合物。用己烷、乙酸乙酯(EtOAc)和乙醇依次提取MO叶。对最有效的提取物进行分级分离。对MO提取物及其衍生级分持续筛选抗癌活性。选择最强的级分进行再分级分离,并使用液相色谱-电喷雾-四极杆飞行时间串联质谱(LC-ESI-QTOF-MS/MS)分析鉴定生物活性化合物。最佳抗癌活性与7号衍生的粗乙酸乙酯提取物级分有关。该级分显著降低细胞活力和克隆形成生长,并增加细胞凋亡。此外,选择7.7号亚级分衍生的7号级分鉴定生物活性化合物。通过LC-ESI-QTOF-MS初步鉴定出10种候选化合物。鉴定出的三种化合物(7-辛烯酸、油酰胺和1-苯基-2-戊醇)通过诱导细胞周期停滞和抑制Bcl-2表达触发凋亡,从而显示出抗癌活性,Bcl-2表达的抑制随后促进了半胱天冬酶3的激活,这是凋亡途径的指标。本研究鉴定出10种可能在抗癌物质领域具有潜力的候选化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2c9/7765196/24efa0f9b966/pharmaceuticals-13-00464-g001.jpg

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