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蛋白质结合雌激素和雌激素共轭物对大鼠肾脏的选择性可用性。

Selective availability of protein bound estrogen and estrogen conjugates to the rat kidney.

作者信息

Chaudhuri G, Verheugen C, Pardridge W M, Judd H L

出版信息

J Endocrinol Invest. 1987 Jun;10(3):283-90. doi: 10.1007/BF03348131.

Abstract

Estrogen glucuronides are selectively cleared by the kidney as compared to estrogen sulfates. The selective trafficking of circulating serum estrogen conjugates to kidney and urine may arise from differential transport properties of the various estrogen conjugates in the renal microcirculation. In the present study, the effects of glomerular and peritubular permeability barriers, and plasma protein binding on the influx of unconjugated and conjugated estrogens into rat kidney were studied. Experiments were carried out utilizing an in vivo double isotope, single injection, timed tissue sampling technique. The extractions of these steroids by the renal cortex were examined utilizing inulin as the reference substance, as it is freely permeable through the glomerular and tubular capillary permeability barriers, but not extracted by tubular epithelial cells. The method was validated by studying the extraction of para-amino hippuric acid (PAH) before and after probenecid treatment. In the absence of plasma proteins, all the estrogens and estrogen conjugates readily diffused through both the glomerular and peritubular capillary permeability barriers and were extracted by tubular epithelia. The addition of 4% albumin to the injection solution led to significant inhibitions of extraction of estradiol (E2) and estrone sulphate (E1-S) only. The extraction of E1-S was reduced to a value less than that of inulin; the extraction of E2 was less than that of control value but significantly more than that of inulin. The addition to the injection solution of human pregnancy sera containing sex hormone binding globulin and albumin was associated with a reduction in the extraction of all estrogens and estrogen conjugates except estriol and E1-S to values approximating that of inulin.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

与硫酸雌激素相比,雌激素葡糖醛酸酯可被肾脏选择性清除。循环血清雌激素结合物向肾脏和尿液的选择性转运可能源于各种雌激素结合物在肾微循环中的不同转运特性。在本研究中,研究了肾小球和肾小管周围的通透性屏障以及血浆蛋白结合对未结合和结合雌激素流入大鼠肾脏的影响。实验采用体内双同位素、单次注射、定时组织采样技术进行。以菊粉作为参考物质,检测肾皮质对这些类固醇的摄取情况,因为菊粉可自由透过肾小球和肾小管毛细血管通透性屏障,但不会被肾小管上皮细胞摄取。通过研究丙磺舒治疗前后对氨基马尿酸(PAH)的摄取情况对该方法进行了验证。在没有血浆蛋白的情况下,所有雌激素和雌激素结合物都能轻易地透过肾小球和肾小管周围的毛细血管通透性屏障,并被肾小管上皮细胞摄取。向注射溶液中添加4%的白蛋白仅导致雌二醇(E2)和硫酸雌酮(E1-S)的摄取受到显著抑制。E1-S的摄取降至低于菊粉的值;E2的摄取低于对照值,但显著高于菊粉。向注射溶液中添加含有性激素结合球蛋白和白蛋白的人妊娠血清会导致除雌三醇和E1-S外的所有雌激素和雌激素结合物的摄取减少,其值接近菊粉。(摘要截断于250字)

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