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虎刺梅(仙人掌科)叶片水提取物和甲醇提取物的抗增殖及致突变活性

Anti-proliferative and mutagenic activities of aqueous and methanol extracts of leaves from Pereskia bleo (Kunth) DC (Cactaceae).

作者信息

Er Hui Meng, Cheng En-Hsiang, Radhakrishnan Ammu Kutty

机构信息

Faculty of Medicine, International Medical University, No. 126 Jalan 19/155B, Bujit Jalil, 57000 Kuala Lumpur, Malaysia.

出版信息

J Ethnopharmacol. 2007 Sep 25;113(3):448-56. doi: 10.1016/j.jep.2007.06.026. Epub 2007 Jul 14.

Abstract

The anti-proliferative effects of the aqueous and methanol extracts of leaves of Pereskia bleo (Kunth) DC (Cactaceae) against a mouse mammary cancer cell line (4T1) and a normal mouse fibroblast cell line (NIH/3T3) were evaluated under an optimal (in culture medium containing 10% foetal bovine serum (FBS)) and a sub-optimal (in culture medium containing 0.5% FBS) conditions. Under the optimal condition, the aqueous extract showed a significant (p<0.05) anti-proliferative effect at 200 microg/mL and 300 microg/mL in 4T1 cells and 300 microg/mL in NIH/3T3 cells, whereas the methanol extract did not show any notable anti-proliferative effect in these cell lines, at any of the concentrations tested. Under the sub-optimal condition, the aqueous extract showed a significant (p<0.05) anti-proliferative effect at 200 microg/mL and 300 microg/mL in NIH/3T3 cells, whilst the methanol extract showed a significant (p<0.05) anti-proliferative effect at 200 microg/mL and 300 microg/mL in both cell lines. An upward trend of apoptosis was observed in both 4T1 and NIH/3T3 cells treated with increasing concentrations of the aqueous extract. The level of apoptosis observed at all the concentrations of the aqueous extract tested was consistently higher than necrosis. There was a significant (p<0.05) increase in the level of necrosis observed in the 4T1 cells treated with 300 microg/mL of the methanol extract. Generally, the level of necrosis was noted to be higher than that of apoptosis in the methanol extract-treated cells. The mutagenicity assay performed showed that in the absence of S-9 liver metabolic activation, the extract was not mutagenic up to the concentration of 165 microg/mL . However, in the presence of S-9 liver metabolic activation, the aqueous extract was mutagenic at all the concentrations tested. This study shows that both the aqueous and methanol extracts of the leaves from Pereskia bleo (Kunth) DC (Cactaceae) do not have appreciable anti-proliferative effect on the 4T1 and NIH/3T3 cells as the EC(50) values obtained are greater than 50 microg/mL when tested under optimal culture condition. Moreover, the aqueous extract may form mutagenic compound(s) upon the metabolisation by liver enzymes.

摘要

在最佳条件(含10%胎牛血清(FBS)的培养基中)和次佳条件(含0.5% FBS的培养基中)下,评估了阔叶麒麟(仙人掌科)叶片水提取物和甲醇提取物对小鼠乳腺癌细胞系(4T1)和正常小鼠成纤维细胞系(NIH/3T3)的抗增殖作用。在最佳条件下,水提取物在4T1细胞中200 μg/mL和300 μg/mL浓度以及在NIH/3T3细胞中300 μg/mL浓度时显示出显著(p<0.05)的抗增殖作用,而甲醇提取物在任何测试浓度下对这些细胞系均未显示出明显的抗增殖作用。在次佳条件下,水提取物在NIH/3T3细胞中200 μg/mL和300 μg/mL浓度时显示出显著(p<0.05)的抗增殖作用,而甲醇提取物在两种细胞系中200 μg/mL和300 μg/mL浓度时均显示出显著(p<0.05)的抗增殖作用。在用浓度递增的水提取物处理的4T1和NIH/3T3细胞中均观察到凋亡呈上升趋势。在所有测试的水提取物浓度下观察到的凋亡水平始终高于坏死水平。在用300 μg/mL甲醇提取物处理的4T1细胞中观察到坏死水平有显著(p<0.05)升高。一般来说,在甲醇提取物处理的细胞中,坏死水平高于凋亡水平。进行的致突变性试验表明,在没有S-9肝脏代谢激活的情况下,提取物在浓度高达165 μg/mL时无致突变性。然而,在有S-9肝脏代谢激活的情况下,水提取物在所有测试浓度下均具有致突变性。本研究表明,阔叶麒麟(仙人掌科)叶片的水提取物和甲醇提取物对4T1和NIH/3T3细胞均没有明显的抗增殖作用,因为在最佳培养条件下测试时获得的半数有效浓度(EC50)值大于50 μg/mL。此外,水提取物在经肝脏酶代谢后可能形成致突变化合物。

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