Warenius H M, Workman P, Bleehen N M
Br J Cancer. 1982 Jan;45(1):27-34. doi: 10.1038/bjc.1982.4.
The HT29R colonic adenocarcinoma xenograft has been shown to be rich in the enzyme beta-glucuronidase. Experiments in rodent systems have demonstrated a marked anti-tumour effect of the drug aniline mustard (AM) on tumours with high levels of this enzyme (e.g. the plasmacytomas PC5 and PC6). We have found that AM is no more effective than its analogue paramethyl aniline mustard (PMAM) or other alkylating agents against the HT29R xenograft. Amongst the possible explanations for this may be: (1) The wide shoulder on the cell-survival curve shown for exposure to alkylating agents of HT29R in vivo. (2) Lack of correlation between physiological availability of beta-glucuronidase and the high levels measured by the standard assay. (3) Increased beta-glucuronidase levels in host mouse marrow, making the latter potentially more susceptible to AM damage.
HT29R结肠腺癌异种移植瘤已被证明富含β-葡萄糖醛酸酶。在啮齿动物系统中进行的实验表明，药物苯胺氮芥（AM）对这种酶水平较高的肿瘤（如浆细胞瘤PC5和PC6）具有显著的抗肿瘤作用。我们发现，AM对HT29R异种移植瘤的疗效并不比其类似物对甲基苯胺氮芥（PMAM）或其他烷化剂更有效。对此可能的解释包括：（1）HT29R在体内暴露于烷化剂时细胞存活曲线上出现的宽坪。（2）β-葡萄糖醛酸酶的生理可用性与标准检测所测的高水平之间缺乏相关性。（3）宿主小鼠骨髓中β-葡萄糖醛酸酶水平升高，使得后者可能更容易受到AM的损伤。
