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一种谷胱甘肽的口服生物可利用(小鼠)前药。

An Orally Bioavailable (Mice) Prodrug of Glutathione.

作者信息

Crankshaw Daune L, Briggs Jacquie E, Vince Robert, Nagasawa Herbert T

机构信息

Center for Drug Design, University of Minnesota, Minneapolis, MN 55455, USA.

Department of Veterans Affairs Medical Center, One Veterans Drive, Minneapolis, MN 55417, USA.

出版信息

Antioxidants (Basel). 2021 Jun 10;10(6):939. doi: 10.3390/antiox10060939.

DOI:10.3390/antiox10060939
PMID:34200599
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8226670/
Abstract

L-Cysteine-glutathione mixed disulfide (CySSG), a prodrug of glutathione (GSH), was found to be orally bioavailable in mice, and protected mice against a toxic dose of acetaminophen. If oral bioavailability can also be demonstrated in humans, a wide range of applicability for CySSG can be envisioned.

摘要

L-半胱氨酸-谷胱甘肽混合二硫化物(CySSG)是谷胱甘肽(GSH)的前药,已发现其在小鼠中具有口服生物利用度,并能保护小鼠免受毒性剂量对乙酰氨基酚的伤害。如果在人体中也能证明其口服生物利用度,那么可以预想CySSG具有广泛的适用性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f73/8226670/2ef3e5195375/antioxidants-10-00939-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f73/8226670/2ef3e5195375/antioxidants-10-00939-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3f73/8226670/2ef3e5195375/antioxidants-10-00939-g001.jpg

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1
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Comparative efficacies of 2 cysteine prodrugs and a glutathione delivery agent in a colitis model.两种半胱氨酸前药和一种谷胱甘肽递送剂在结肠炎模型中的比较疗效
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Invest Ophthalmol Vis Sci. 1996 Apr;37(5):923-9.
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本文引用的文献

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The Role of Glutathione in Protecting against the Severe Inflammatory Response Triggered by COVID-19.谷胱甘肽在预防新型冠状病毒肺炎引发的严重炎症反应中的作用
Antioxidants (Basel). 2020 Jul 16;9(7):624. doi: 10.3390/antiox9070624.
2
Endogenous Deficiency of Glutathione as the Most Likely Cause of Serious Manifestations and Death in COVID-19 Patients.内源性谷胱甘肽缺乏是新冠患者出现严重症状和死亡的最可能原因。
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Glutamate cysteine ligase and the age-related decline in cellular glutathione: The therapeutic potential of γ-glutamylcysteine.
谷氨酸半胱氨酸连接酶与细胞内谷胱甘肽随年龄增长的下降:γ-谷氨酰半胱氨酸的治疗潜力
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Hepatoprotection by L-cysteine-glutathione mixed disulfide, a sulfhydryl-modified prodrug of glutathione.
J Biochem Mol Toxicol. 2003;17(2):95-7. doi: 10.1002/jbt.10069.
5
The reduction of the L-cysteine-glutathione mixed disulfide in rat liver. involvement of an enzyme catalyzing thiol-disulfide interchange.大鼠肝脏中L-半胱氨酸-谷胱甘肽混合二硫化物的还原。一种催化硫醇-二硫化物交换的酶的作用。
FEBS Lett. 1970 Mar 16;7(1):26-28. doi: 10.1016/0014-5793(70)80608-1.
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Age and gender dependent levels of glutathione and glutathione S-transferases in human lymphocytes.人类淋巴细胞中谷胱甘肽及谷胱甘肽S-转移酶水平的年龄和性别依赖性
Carcinogenesis. 1998 Oct;19(10):1873-5. doi: 10.1093/carcin/19.10.1873.
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Attenuation of acetaminophen hepatotoxicity in mice as evidence for the bioavailability of the cysteine in D-glucose-L-cysteine in vivo.
Toxicol Lett. 1994 Jan;70(1):101-8. doi: 10.1016/0378-4274(94)90149-x.
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The systemic availability of oral glutathione.口服谷胱甘肽的全身可用性。
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