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红树植物总状卤蕨成分的抗氧化和细胞毒性活性的体外评估

In vitro evaluation of the antioxidant and cytotoxic activities of constituents of the mangrove Lumnitzera racemosa Willd.

作者信息

Nguyen Phuong Thao, Bui Thi Thuy Luyen, Chau Ngoc Diep, Bui Huu Tai, Kim Eun Ji, Kang Hee Kyoung, Lee Sang Hyun, Jang Hae Dong, Nguyen The Cuong, Nguyen Van Thanh, Nguyen Xuan Cuong, Nguyen Hoai Nam, Chau Van Minh, Kim Young Ho

机构信息

College of Pharmacy, Chungnam National University, Daejeon, 305-764, Republic of Korea.

出版信息

Arch Pharm Res. 2015 Apr;38(4):446-55. doi: 10.1007/s12272-014-0429-y. Epub 2014 Jul 9.

DOI:10.1007/s12272-014-0429-y
PMID:25001899
Abstract

This study performed phytochemical and bioactive assessments of the mangrove Lumnitzera racemosa Willd. leaves. Bioassay-guided fractionation of the methanolic extracts led to the identification of thirty-six compounds (1-36), their structures were elucidated using detailed NMR spectroscopic and MS analysis. The extracts, fractions, and the isolated compounds were screened for potential antioxidant and cytotoxic activities. Antioxidant assays were performed using peroxyl radical-scavenging and reducing assays, whereas cytotoxicity was measured using MTT assays in HL-60 and Hel-299 cell lines. The methanolic extract, CH2Cl2 and n-BuOH fractions (10.0 μg/mL) exhibited potent antioxidant activity, with Trolox equivalent (TE) values of 24.94 ± 0.59, 28.34 ± 0.20, and 27.09 ± 0.37 (μM), respectively. In addition, the isolated compounds exerted cytotoxic effects in a dose-dependent manner; compounds 1 and 14 exhibited the most potent cytotoxicity in HL-60 cells, with IC50 values of 0.15 ± 0.29 and 0.60 ± 0.16 μM, respectively. To clarify the mechanism(s) behind these cytotoxic effects, we measured the time-dependent changes in apoptotic markers including the condensation and fragmentation of nuclear chromatin, and the downregulation of p-ERK1/2, p-AKT, and c-Myc levels.

摘要

本研究对红树植物总序卤蕨(Lumnitzera racemosa Willd.)的叶子进行了植物化学和生物活性评估。通过生物测定指导的甲醇提取物分级分离,鉴定出了36种化合物(1 - 36),利用详细的核磁共振光谱和质谱分析阐明了它们的结构。对提取物、馏分和分离出的化合物进行了潜在抗氧化和细胞毒性活性的筛选。抗氧化测定采用过氧自由基清除和还原测定法,而细胞毒性则通过在HL - 60和Hel - 299细胞系中使用MTT测定法进行测量。甲醇提取物、二氯甲烷和正丁醇馏分(10.0μg/mL)表现出较强的抗氧化活性,其Trolox等效值(TE)分别为24.94±0.59、28.34±0.20和27.09±0.37(μM)。此外,分离出的化合物呈现出剂量依赖性的细胞毒性作用;化合物1和14在HL - 60细胞中表现出最强的细胞毒性,IC50值分别为0.15±0.29和0.60±0.16μM。为了阐明这些细胞毒性作用背后的机制,我们测量了凋亡标志物随时间的变化,包括核染色质的凝聚和碎片化,以及p-ERK1/2、p-AKT和c-Myc水平的下调。

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