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首例人体研究证明血红素加氧酶-1在人体内的药理学激活作用。

First-in-human study demonstrating pharmacological activation of heme oxygenase-1 in humans.

机构信息

Enteric Neurosciences Program, Division of Gastroenterology and Hepatology, Mayo Clinic and Mayo Foundation, Rochester, Minnesota, USA.

出版信息

Clin Pharmacol Ther. 2010 Feb;87(2):187-90. doi: 10.1038/clpt.2009.221. Epub 2009 Dec 2.

Abstract

Heme oxygenase (HO)-1 degrades heme and protects against oxidative stress, but it has not been pharmacologically induced in humans. In this randomized study of 10 healthy volunteers, hemin (3 mg/kg intravenously in 25% albumin) was shown to increase plasma HO-1 protein concentration four- to fivefold and HO-1 activity ~15-fold relative to baseline at 24 and 48 h (placebo -56.41 +/- 6.31 (baseline), 69.79 +/- 13.00 (24 h), 77.44 +/- 10.62 (48 h) vs. hemin -71.70 +/- 9.20 (baseline), 1,126.20 +/- 293.30 (24 h), 1,192.20 +/- 333.30 (48 h)) in four of five subjects as compared with albumin alone (P </= 0.03). This represents the overcoming of a fundamental hurdle to HO-1 research in humans.

摘要

血红素加氧酶-1(HO-1)可降解血红素并抵抗氧化应激,但尚未在人体中进行药理学诱导。在这项针对 10 名健康志愿者的随机研究中,与单独使用白蛋白相比,静脉内给予 3mg/kg 的血红素(25%白蛋白)可使血浆 HO-1 蛋白浓度在 24 和 48 小时时增加 4-5 倍,HO-1 活性增加 15 倍(安慰剂-56.41 +/- 6.31(基线),69.79 +/- 13.00(24 小时),77.44 +/- 10.62(48 小时)vs. 血红素-71.70 +/- 9.20(基线),1126.20 +/- 293.30(24 小时),1192.20 +/- 333.30(48 小时)),在五名受试者中的四名中(P </= 0.03)。这代表着在人体 HO-1 研究中克服了一个基本障碍。

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