人小肠刷状缘膜囊泡中青霉素G摄取的特征分析
Characterisation of penicillin G uptake in human small intestinal brush border membrane vesicles.
作者信息
Poschet J F, Hammond S M, Fairclough P D
机构信息
Digestive Disease Research Centre, St Bartholomew's and the Royal London School of Medicine and Dentistry, Turner Street, London E1 2AD, UK.
出版信息
Gut. 1999 May;44(5):620-4. doi: 10.1136/gut.44.5.620.
BACKGROUND
Many beta lactams are well absorbed by the small intestine, although the reasons for this are poorly understood.
AIMS
To characterise the uptake of penicillin G into human small intestinal brush border membrane vesicles (BBMV) and to compare the uptake characteristics to those of rabbit BBMV.
METHODS AND RESULTS
Uptake of penicillin G was studied in human BBMV. Penicillin G was actively transported into the lumen of BBMV via an H+ dependent, Na+ independent uptake system. The carrier mediated process was saturable and adhered to Michaelis-Menten kinetics (Vmax 52 nmol penicillin G per mg protein per 30 seconds, Km 13.9 mM). These results are similar to those previously reported in rabbit BBMV.
CONCLUSIONS
It is suggested that penicillin G can be used as a model molecule for peptide and beta lactam transport studies as it is cheap and readily available in isotopically labelled form. Furthermore, rabbit BBMV may be used as an acceptable substitute for human BBMV for the study of penicillin transport.
背景
许多β-内酰胺类药物在小肠中吸收良好，尽管其原因尚不清楚。
目的
表征青霉素G进入人小肠刷状缘膜囊泡（BBMV）的摄取情况，并将摄取特征与兔BBMV的进行比较。
方法与结果
在人BBMV中研究了青霉素G的摄取。青霉素G通过H⁺依赖性、Na⁺非依赖性摄取系统被主动转运到BBMV腔中。载体介导的过程是可饱和的，符合米氏动力学（Vmax为每毫克蛋白质每30秒52纳摩尔青霉素G，Km为13.9毫摩尔）。这些结果与先前在兔BBMV中报道的结果相似。
结论
建议青霉素G可作为肽和β-内酰胺类转运研究的模型分子，因为它价格便宜且易于以同位素标记形式获得。此外，兔BBMV可作为人BBMV的可接受替代品用于青霉素转运研究。
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