Antitumor Activity of New Quinoxaline Analogues and Its Complexes

N. Yousif, A. A. Ismaeel, K. Ali, F. Mousa
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引用次数: 2

Abstract

This study shows synthesis of a new quinoxaline derivatives (LH) and preparation of copper (Cu-LH) and cobalt (Co-LH) complexes and studying the effect of these compounds on the activity of lactate dehydrogenase (LDH) a primary enzyme to the process of anaerobic glycolysis which is the source of energy in tumor cell. This study included of 40 women with recently diagnosed of malignancies Breast cancer; (20) subject women in stage I&(20)subject women in stage II who were admitted to Medical City Hospital with age ranged (37-45) years and 30 apparently healthy woman matched for age served as controls. Serum LDH activity was assayed on the time of the diagnosis in all cases and after addition of different concentrations (10 -1 , 10 -2 , 10 -3 ) of quinoxalin derivatives and transition metals complexes in vitro. The results revealed an inhibitory effect of LH and its complexes with Cu and Co in all concentrations used in this study on LDH activity. The inhibition percent’s increased with increase concentration for LH and its complexes. Also the results reveal that the inhibitory effect of LH in all concentrations used were more than inhibitory effect of its complexes. Moreover the inhibitory effect of LH-Co complex was more than inhibitory effect of LH-Cu complex in all concentrations used. The inhibition ability of quinoxaline derivative and its complexes on the enzyme lactate dehydrogenase leads to the fact that these compounds can be characterized as an active anti –cancer substances for one of the metabolic enzymes necessary to feed the cancer cells. Keyword: breast cancer, quinoxaline derivatives, copper and cobalt complexes, lactate dehydrogenase
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新型喹啉类似物及其配合物的抗肿瘤活性
本研究合成了一种新的喹诺啉衍生物(LH),制备了铜(Cu-LH)和钴(Co-LH)配合物,并研究了这些化合物对肿瘤细胞厌氧糖酵解过程中主要酶乳酸脱氢酶(LDH)活性的影响。乳酸脱氢酶是肿瘤细胞能量来源。这项研究包括40名最近被诊断为恶性肿瘤的妇女,乳腺癌;(20)名年龄在37 ~ 45岁的医学城市医院住院的i期和II期女性受试者,以及30名年龄匹配的明显健康女性作为对照。在诊断时及体外添加不同浓度(10 -1、10 -2、10 -3)喹诺啉衍生物和过渡金属配合物后测定血清LDH活性。结果显示,在本研究中使用的所有浓度的LH及其与Cu和Co的配合物对LDH活性都有抑制作用。对LH及其配合物的抑制率随浓度的增加而增加。结果还表明,在所有浓度下,LH的抑制作用都大于其配合物的抑制作用。而且在所有浓度下,LH-Co配合物的抑制作用都大于LH-Cu配合物的抑制作用。喹诺啉衍生物及其配合物对乳酸脱氢酶的抑制作用使得这些化合物可以被认为是一种活性的抗癌物质,用于癌细胞所需的一种代谢酶。关键词:乳腺癌,喹啉衍生物,铜钴配合物,乳酸脱氢酶
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