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标题：6-Deoxy-6-[131I]iodo-L-ascorbic Acid for the in Vivo Study of Ascorbate: Autoradiography, Biodistribution in Normal and Hypolipidemic Rats, and in Tumor-Bearing Nude Mice
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作者：Jintaek Kim ; Fumihiko Yamamoto ; Shigeki Gondo 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2009
卷号：32
期号：11
页码：1906-1911
DOI：10.1248/bpb.32.1906
出版社：The Pharmaceutical Society of Japan
摘要：Normal female rat distribution studies showed high and specific uptake of 6-deoxy-6-[¹³¹I]iodo- L -ascorbic acid (6-¹³¹IAsA) into the adrenal glands, known to highly express the ascorbate sodium-dependent vitamin C transporter-2 (SVCT-2), and the adrenal gland was clearly visualized by whole-body autoradiography. Preinjection of sulfinpyrazone, a known blocker of ascorbate transport, with 6-¹³¹IAsA resulted in decreased uptake of radioactivity in rat adrenal glands compared to the control group, seemingly illustrating the participation of the SVCT transporter (probably the SVCT-2 subtype) in the uptake process in vivo . 4-Aminopyrazolo[3,4- d ]pyrimidine-induced hypolipidemic rats showed a 1.7-fold increase in adrenal uptake of radioactivity at 30 min postinjection of 6-¹³¹IAsA, compared to the control, with increased adrenal-to-liver and adrenal-to-kidney ratios. To further characterize 6-¹³¹IAsA for its tumor uptake properties, biodistribution studies were also performed using male nude mice implanted with either Y-1 adrenocortical tumor cells or adrenal medulla-derived PC12 cells. None of these tumors exhibited relevant uptake of 6-¹³¹IAsA while normal adrenal glands showed high uptake of radioactivity, suggesting that these tumors in this model have only a poor transport capacity for this agent. The present study demonstrates that the use of radioiodinated 6-IAsA may help to obtain information about functional alterations in diseased adrenal glands, but it does not exhibit desirable properties as a tumor-seeking agent for ascorbic acid bioactivity.
关键词：6-deoxy-6-[131I]iodo- L -ascorbic acid;adrenal gland;tissue distribution;ascorbate transporter