辣木种子中潜在抗癌化合物辣木素的快速分离方法

S. Habtemariam
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引用次数: 9

摘要

辣木(Moringa stenopetala)的种子富含硫代葡萄糖苷(glucosinolates),主要是葡萄糖合成素(gluccomoringin),但在体外测试中显示其抗癌效果有限。在本研究中,正己烷去脂后的水提物对HepG2细胞(IC50, 6.28±0.55 μg/ml)和SH-SY5Y人神经母细胞瘤细胞(IC50, 9.81±1.30 μg/ml)具有较强的细胞毒活性。甲醇提取液对HepG2人肝癌细胞有较弱的细胞毒活性,浓度为500 μg/ml;己烷提取液对HepG2人肝癌细胞无细胞毒作用,其脂肪酸成分以油酸为主(75%)。通过高效液相色谱法和C-18硅胶体系的一步组合色谱系统对水提物的成分进行监测,发现其主要活性成分(异硫氰酸糖木苷或辣木苷;分离得到4(α- l -鼠李糖氧基)-异硫氰酸苄酯。辣木苷对HepG2和SH-Sy5Y细胞株的毒力分别是依托泊苷的6.3倍和2.4倍。本文讨论了在不需要多步骤色谱和酶解纯化步骤的情况下,从狭叶草种子中分离出这种有效的潜在抗癌化合物。
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Methodology for Rapid Isolation of Moringin: Potential AnticancerCompound from the Seeds of Moringa stenopetala
The seeds of Moringa stenopetala which are known to be rich sources of glucosinolates, primarily glucomoringin, have been shown to have limited anticancer effects when tested in vitro. In the present study, however, the water extract of the seeds obtained following defatting by hexane displayed potent cytotoxic activity against HepG2 (IC50, 6.28 ± 0.55 μg/ml) and the SH-SY5Y human neuroblastoma (IC50, 9.81 ± 1.30 μg/ml) cells. The methanol extract displayed a weak cytotoxic activity against the HepG2 human hepatocellular cancer cells when tested upto 500 μg/ml, while extraction with hexane yielded the non-cytotoxic fixed oil which fatty acid composition was primarily oleic acid (75%). By monitoring the constituents of the water extract by HPLC and a one-step combiflash chromatographic system using C-18 silica gel system, the principal active constituent (glucomoringin isothiocyanate or moringin; 4(α-L-rhamnosyloxy)-benzyl isothiocyanate) was isolated. Moringin was 6.3 and 2.4 times more potent than etoposide in the HepG2 and SH-Sy5Y cell lines respectively. The isolation of this potent potential anticancer compound from the seeds of M. stenopetala without the need for multi-step chromatographic and enzyme-digestionbased purification steps are discussed.
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