首页> 美国卫生研究院文献>British Journal of Cancer >Uptake and retention of estramustine and the presence of estramustine binding protein in malignant brain tumours in humans.
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Uptake and retention of estramustine and the presence of estramustine binding protein in malignant brain tumours in humans.

机译:人类恶性脑肿瘤中雌莫司汀的摄取和保留以及雌莫司汀结合蛋白的存在。

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摘要

Estraumustine phosphate (EMP), a cytotoxic drug used in the treatment of prostatic carcinoma, has been shown to exert cytotoxic effects on glioma cells in vitro. The drug uptake is assumed to depend on a specific estramustine binding protein (EMBP). One of the main difficulties in achieving cytotoxic effect in malignant brain tumours is believed to be due to the poor penetration of cytotoxic drugs into tumour tissue. In patients with malignant supratentorial brain tumours we have analysed the uptake of EMP metabolites in tumour tissue after oral administration and demonstrated EMBP in the same tissue specimens. Sixteen patients were given 280 mg EMP orally 14 h prior to surgery. Specimens from brain tumour tissue, cystic fluid, and serum were collected during surgery. Using gas chromatography the metabolites of EMP, estramustine (EaM) and estromustine (EoM), were quantified, EMBP was demonstrated by immunohistochemistry. The mean concentrations of EaM and EoM, expressed in ng g-1, were 60.3 and 38.4 in tumour tissue and 3.5 and 56.3 in serum, respectively. An accumulation of EaM in tumour tissue was found with a mean concentration gradient of 16.1 versus serum, while the gradient for EoM was 0.76. EMBP was demonstrated with a high degree of staining in all but one tumour. The high concentrations of EaM and EoM found in malignant brain tumour tissue correspond to potentially cytotoxic levels. The present results as well as the earlier in vitro demonstrated cytotoxic effects on glioma cells strengthen the possibility of a therapeutic effect of EMP in the treatment of malignant brain tumours.
机译:磷酸雌莫司汀(EMP)是一种用于治疗前列腺癌的细胞毒性药物,已显示出在体外对神经胶质瘤细胞产生细胞毒性作用。假定药物吸收取决于特定的雌莫司汀结合蛋白(EMBP)。人们认为,在恶性脑肿瘤中获得细胞毒性作用的主要困难之一是由于细胞毒性药物难以渗透到肿瘤组织中。对于恶性幕上脑肿瘤患者,我们分析了口服给药后肿瘤组织中EMP代谢物的摄取情况,并证明了相同组织标本中的EMBP。十六名患者在手术前14小时口服280 mg EMP。手术期间从脑肿瘤组织,囊性液体和血清中收集标本。使用气相色谱法对EMP,雌莫司汀(EaM)和雌莫司汀(EoM)的代谢产物进行定量,并通过免疫组织化学证明了EMBP。以ng g-1表示的EaM和EoM的平均浓度在肿瘤组织中分别为60.3和38.4,在血清中分别为3.5和56.3。发现EaM在肿瘤组织中的积累相对于血清的平均浓度梯度为16.1,而EoM的梯度为0.76。 EMBP被证明在一个肿瘤以外的所有肿瘤中都具有高度染色。在恶性脑肿瘤组织中发现的高浓度的EaM和EoM对应于潜在的细胞毒性水平。目前的结果以及较早的体外研究表明,对神经胶质瘤细胞的细胞毒性作用增强了EMP在治疗恶性脑肿瘤中产生治疗作用的可能性。

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