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Abstract：
Ruta chalepensis is an herb used to treat various ailments, and its potential cytotoxic effects on different tumor cell lines have been extensively studied. The present study aimed to evaluate the cytotoxic activity of R. chalepensis methanol extract (RCME), sub-partitions obtained from solvents of increasing polarity, and major compounds, as well as their hemolytic, anti-hemolytic, and antioxidant potential. The in vitro cytotoxic activity against the human hepatocarcinoma (HEP-G2) and the murine lymphoma cell line (L5178Y-R) was evaluated using the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay, whereas selectivity indices (SIs) were determined by comparing cytotoxicity against normal African green monkey kidney cells (VERO) and human peripheral blood mononuclear cells (PBMC). Hemolytic and anti-hemolytic activities were evaluated on human erythrocytes. The most effective cytotoxic treatment was evaluated for nitric oxide release by J774A.1 macrophages. Antioxidant activity of R. chalepensis material was also determined. Results showed that RCME produced significant (p < 0.05) cytotoxicity in HEP-G2 (IC50 = 1.79 µg/mL) and L5178Y-R (IC50 = 1.60 µg/mL) cells and exhibited high SIs (291.50 and 114.80, respectively). In addition, the n-hexane fraction (RCHF) showed an IC50 of 18.31 µg/mL in HEP-G2 cells and an SI of 9.48 in VERO cells, whereas the chloroform fraction (RCCF) evidenced an IC50 of 1.60 µg/mL in L5178Y-R cells and an SI of 34.27 in PBMC cells. Chalepensin (CHL), rutamarin (RTM), and graveolin (GRV), which are major components of R. chalepensis, showed high activity against L5178Y-R cells, with IC50 of 9.15, 15.13 and SI of 45.08 µg/mL, respectively. In addition, CHL, RTM, and GRV showed SIs of 24.76, 9.98, and 3.52, respectively, when compared with PBMC cells. RCME at concentrations of 125 µg/mL and 250 µg/mL, significantly (p < 0.05) decreased nitrite production in J774A.1 cells, when exposed to lipopolysaccharide. This study demonstrated that RCME showed significant cytotoxic activity against HEP-G2 and L5178Y-R cells, without affecting normal VERO, PBMC, and J774A.1 cells.
摘要：
Rutachalepensis是一种用于治疗各种疾病的草药，及其对不同肿瘤细胞系的潜在细胞毒性作用已被广泛研究。本研究旨在评估R.chalepensis甲醇提取物（RCME）的细胞毒活性，从极性增加的溶剂中获得的子分区，和主要化合物，以及它们的溶血，抗溶血,和抗氧化潜力。使用比色法评估对人肝癌（HEP-G2）和鼠淋巴瘤细胞系（L5178Y-R）的体外细胞毒性活性3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四唑溴化物（MTT）还原试验，而选择性指数（SI）是通过比较对正常非洲绿猴肾细胞（VERO）和人外周血单核细胞（PBMC）的细胞毒性来确定的。在人红细胞上评估溶血和抗溶血活性。对J774A.1巨噬细胞的一氧化氮释放评估了最有效的细胞毒性治疗。还测定了R.chalepensis材料的抗氧化活性。结果表明，RCME在HEP-G2（IC50=1.79µg/mL）和L5178Y-R（IC50=1.60µg/mL）细胞中产生了显着（p<0.05）的细胞毒性，并表现出较高的SI（分别为291.50和114.80）。此外,正己烷部分（RCHF）在HEP-G2细胞中的IC50为18.31µg/mL，在VERO细胞中的SI为9.48，而氯仿级分（RCCF）在L5178Y-R细胞中的IC50为1.60µg/mL，在PBMC细胞中的SI为34.27。Chalepensin(CHL),rutamarin(RTM),和graveolin(GRV)，它们是R.chalepensis的主要组成部分，对L5178Y-R细胞显示高活性，IC50为9.15，15.13，SI为45.08µg/mL，分别。此外,CHL,RTM,和GRV显示SI分别为24.76、9.98和3.52，与PBMC细胞相比。RCME浓度为125µg/mL和250µg/mL，显著(p<0.05)降低J774A.1细胞的亚硝酸盐产量，当暴露于脂多糖时。这项研究表明，RCME对HEP-G2和L5178Y-R细胞显示出显著的细胞毒活性，不影响正常的VERO，PBMC,和J774A.1细胞。
