Effect of Glycerol-Related Compounds on Carrier-Mediated Glycerol Uptake in HCT-15 Human Colon Cancer Cell Line
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- FUJIMOTO Nami
- Graduate School of Pharmaceutical Sciences, Nagoya City University
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- INOUE Katsuhisa
- Graduate School of Pharmaceutical Sciences, Nagoya City University
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- HAYASHI Yayoi
- College of Pharmacy, Kinjo Gakuin University
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- YUASA Hiroaki
- Graduate School of Pharmaceutical Sciences, Nagoya City University
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The effect of several compounds, which are structurally analogous to glycerol, on carrier-mediated glycerol uptake was examined in HCT-15 cells to help clarifying the functional characteristics of the glycerol transport system. The carrier-mediated uptake of glycerol conformed to the Michaelis-Menten kinetics with a Michaelis constant of 21.1 μM and the tested compounds were all suggested to inhibit it competitively with the values of the inhibition constant (Ki) in the increasing order as follows: monobutyrin (41.0 μM)≤monoacetin (54.6 μM)<diglycerol (154 μM)<1,2-propanediol (1650 μM). Therefore, they all may possibly be substrates of the carrier-mediated glycerol transport system, for which the glycerol esters (monoacetin and monobutyrin) have the highest affinities among them. It was also found that S-(+)-enantiomer of 1,2-propanediol (Ki=484 μM) has a higher affinity than its R-(-)-enantiomer (Ki=19100 μM), indicating enantioselective recognition. These results support the suggestion that a specific carrier protein is involved in glycerol uptake in HCT-15 cells. It would be of interest to identify the carrier, which may be present also in some organs, and further investigate the possibility that glycerol ester derivatives of drugs might be delivered via the carrier.<br>
収録刊行物
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- Drug Metabolism and Pharmacokinetics
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Drug Metabolism and Pharmacokinetics 23 (3), 216-220, 2008
日本薬物動態学会
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詳細情報 詳細情報について
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- CRID
- 1390282680155141376
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- NII論文ID
- 10024188408
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- NII書誌ID
- AA1162652X
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- ISSN
- 18800920
- 13474367
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- Crossref
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可