Anticancer and antiinflammatory activities of cucurbitacins from Cucurbita andreana
Anticancer and antiinflammatory activities of cucurbitacins from Cucurbita andreana
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DOI：
10.1016/s0304-3835(02)00497-4
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发表时间：
2003-01-10
期刊：
影响因子：
9.7
通讯作者：
Nair, MG
中科院分区：
文献类型：
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作者：
Jayaprakasam, B;Seeram, NP;Nair, MG
在生物测定指导下，对葫芦瓜果实提取物进行纯化，得到葫芦素B(1)、D(2)、E(3)和1(4)。这些葫芦素对人结肠癌（HCT-116）、乳腺癌（MCF-7）、肺癌（NCI-H460）和中枢神经系统（SF-268）癌细胞系、环氧化酶-1 （COX-1）和环氧化酶-2 （COX-2）酶的生长和脂质过氧化的抑制作用进行了评估。葫芦素B(1)、D(2)、E(3)和1(4)在0.4 muM时对结肠的抑制活性分别为81.5、80.4、7和65%，对乳腺的抑制活性分别为87、78、66.5和12%，对肺的抑制活性分别为96、43、37和2%，对中枢神经系统的抑制活性分别为92、25、24和4%。以阿霉素（多柔比星）作为阳性对照，在0.3 × 10(-5) m浓度下，对HCT-116（结肠）、MCF-7（乳腺）、NCI-H460（肺）和SF-268（中枢神经系统）细胞系的抑制作用分别为64%、47%、45%和71%。化合物1、2、3和4在100马克杯/ml浓度下对COX-2酶的抑制作用分别为32%、29%、35%和27%。然而，这些化合物在这个浓度下对COX-1酶没有抑制作用。以市售抗炎药布洛芬、萘普生和万络为对照，分别在2.1、2.5和1.67马克杯/毫升浓度下检测COX-1和COX-2酶的抑制作用。布洛芬和萘普生的COX-1抑制活性分别为59%和95%，COX-2抑制活性分别为53%和79%。万络对COX-2的特异性抑制率为71%。此外，葫芦素1和4在100马克杯/毫升时分别抑制59%和23%的脂质过氧化。(C) 2003爱思唯尔科学爱尔兰有限公司版权所有。
Bioassay-guided purification of an extract of Cucurbita andreana fruits yielded cucurbitacins B (1), D (2), E (3), and 1 (4). These cucurbitacins were evaluated for their inhibitory effects on the growth of human colon (HCT-116), breast (MCF-7), lung (NCI-H460), and central nervous system (CNS) (SF-268) cancer cell lines, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes and on lipid peroxidation. Inhibitory activities of cucurbitacins B (1), D (2), E (3) and 1 (4), respectively, were for colon 81.5, 80.4, 7, and 65% at 0.4 muM, breast 87, 78, 66.5, and 12% at 0.4 muM, lung 96,43, 37 and 2% at 0.1 muM and CNS 92, 25, 24 and 4% at 0.05 muM. Adriamycin (doxorubicin) was used as a positive control, which showed 64,47,45 and 71% inhibition of HCT-116 (colon), MCF-7 (breast), NCI-H460 (lung) and SF-268 (CNS) cell lines, respectively, at 0.3 x 10(-5) M. Compounds 1, 2, 3, and 4 inhibited the COX-2 enzyme by 32, 29, 35, and 27%, respectively, at 100 mug/ml. However these compounds did not inhibit the COX-1 enzyme at this concentration. Ibuprofen, naproxen and vioxx, commercial antiinflammatory drugs, were tested as controls for the inhibition of COX-1 and COX-2 enzymes at concentrations of 2.1, 2.5 and 1.67 mug/ml, respectively. Ibuprofen and naproxen exhibited 59 and 95% COX-1, and 53 and 79% COX-2 inhibitory activities, respectively. Vioxx showed specific COX-2 inhibition by 71%. Also, cucurbitacins 1 and 4 inhibited lipid peroxidation by 59 and 23%, respectively, at 100 mug/ml. (C) 2003 Elsevier Science Ireland Ltd. All rights reserved.