V Saraswathi, V Mathuram, S Subramanian, S Govindasamy
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引用次数: 0
摘要
氯Echitamine chloride (EC)是从石桐树皮中提取的吲哚类生物碱,具有很好的抗癌作用。研究了该药物对180肉瘤小鼠微粒体药物解毒系统的影响。在携带saroma -180的小鼠中观察到,皮下给药剂量为5mg /kg体重时,能够改变受损的药物解毒系统。测定各组小鼠微粒体蛋白、Cyt-P450、Cyt-b5、nadh - cyt - c -还原酶、nadph - cyt - c -还原酶、葡聚糖-6磷酸酶水平。S-180小鼠体内这些药物代谢酶水平降低。EC治疗使这些酶和微粒体血红蛋白接近正常水平。为了了解EC治疗后蛋白水平下降及其正常化的机制,我们进行了3h -苯丙氨酸掺入研究。结果表明,载脂蛋白的合成在荷瘤动物中也发生了改变。所有这些在荷瘤动物中观察到的变化在用EC治疗后被纠正到接近正常水平。
Modulation of the impaired drug metabolism in sarcoma-180-bearing mice by echitamine chloride.
Echitamine chloride (EC), an indole alkaloid, extracted from the bark of Alstonia scholaris has got highly promising anticancer effect. The effect of this drug on the microsomal drug detoxifying system was studied in sarcoma-180 induced mice. When given sub-cutaneously at a dosage of 5 mg/kg body weight, it was able to alter the impaired drug detoxifying system which was observed in the Sarcoma-180 bearing mice. The levels of microsomal protein, Cyt-P450, Cyt-b5, NADH-Cyt-C-reductase, NADPH-Cyt-C-reductase, and glu-6 phosphatase were determined. The levels of these drug metabolizing enzymes were decreased in S-180 bearing mice. EC treatment corrected to near normal levels of these enzymes and microsomal hemeproteins. In order to understand the mechanism responsible for the decreased protein level and its normalization after treatment with EC, 3H-Phenylalanine incorporation study was carried out. From the results, it is observed that the synthesis of apoproteins is also altered in tumor-bearing animals. All these changes which were observed in tumor-bearing animals were corrected to near normal levels after treatment with EC.