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香豆素在前列腺癌模型中的抗肿瘤活性评估。

Evaluation of the antitumour activity of coumarin in prostate cancer models.

作者信息

Maucher A, Kager M, von Angerer E

机构信息

Institut für Pharmazie, Regensburg, Federal Republic of Germany.

出版信息

J Cancer Res Clin Oncol. 1993;119(3):150-4. doi: 10.1007/BF01229529.

Abstract

Responses to coumarin have been reported for patients suffering from malignant melanoma, metastatic renal carcinoma and, recently, advanced prostate cancer. These data together with some experimental evidence for antiprostatic effect prompted us to study the activity of coumarin in various prostate tumour models and evaluate the endocrine properties of this drug. In rats no antiandrogenic activity was found. The growth of Noble Nb-R prostate tumours of the rat was strongly inhibited by coumarin (40 mg/kg; administered three times per week), whereas the hormonally more sensitive Dunning R3327-G rat prostate carcinoma did not respond to coumarin (40 mg) even when the drug was administered daily. Coumarin was also shown to possess antimetastatic activity in a Dunning R3327-MatLu tumour model. In this model small pieces of the hormone-independent tumour were implanted into the ear of the animal and later resected to mimic the clinical situation where primary tumours have been removed. The number of lung metastases was reduced significantly by 40%-50% following the administration of coumarin (40 mg daily).

摘要

据报道,患有恶性黑色素瘤、转移性肾癌以及最近的晚期前列腺癌的患者对香豆素会产生反应。这些数据以及一些关于抗前列腺作用的实验证据促使我们研究香豆素在各种前列腺肿瘤模型中的活性,并评估该药物的内分泌特性。在大鼠中未发现抗雄激素活性。香豆素(40毫克/千克;每周给药三次)强烈抑制大鼠Noble Nb-R前列腺肿瘤的生长,而激素敏感性更高的Dunning R3327-G大鼠前列腺癌即使每天给药也对香豆素(40毫克)无反应。在Dunning R3327-MatLu肿瘤模型中,香豆素还显示出具有抗转移活性。在该模型中,将小块激素非依赖性肿瘤植入动物耳部,随后切除以模拟原发性肿瘤已被切除的临床情况。每天给予香豆素(40毫克)后,肺转移瘤数量显著减少40%-50%。

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