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PF2405,黄芩标准化提取物,在体外和体内均可改善结肠炎。

PF2405, standardized fraction of Scutellaria baicalensis, ameliorates colitis in vitro and in vivo.

作者信息

Jiang Wen-Yi, Seo Geom Seog, Kim Youn-Chul, Sohn Dong Hwan, Lee Sung Hee

机构信息

Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan, Jeonbuk, 570-749, Republic of Korea.

出版信息

Arch Pharm Res. 2015 Jun;38(6):1127-37. doi: 10.1007/s12272-015-0553-3. Epub 2015 Jan 11.

DOI:10.1007/s12272-015-0553-3
PMID:25577335
Abstract

Standardized extraction procedures for herb are as important as their authentication to maintain their quality and ensure their safe use. We had prepared a standardized and purified Scutellaria baicalensis Georgi extract, PF2405, which was enriched with three major components, baicalein, oroxylin A and wogonin. In the present study, we investigated the potential anti-inflammatory effects of PF2405 in vitro and in two different experimental animal models of inflammatory bowel disease. Effect of PF2405 studied in tumor necrosis factor (TNF)-α-induced HT-29 cells in vitro. In vivo experimental colitis models were induced by administration of trinitrobenzene sulfonic acid (TNBS) or dextran sulfate sodium (DSS). PF2405 (50 μg/ml) decreased TNF-α-induced cyclooxygenase (COX)-2 expressions through inhibition of phosphorylation of c-Jun N-terminal kinases and p38 mitogen-activated protein kinase in HT-29 cells. Combination of baicalein (20 μg/ml), oroxylin A (8 μg/ml), and wogonin (2 μg/ml) markedly inhibits TNF-α-induced COX-2 expression when compared with individual components. PF2405 (25 mg/kg b.w.) treatment significantly reduced histopathological severity; suppressed expression of COX-2, TNF-α, and interleukin-1β in TNBS-induced mice. Moreover, PF2405 (25 mg/kg b.w.) has both potent preventive and therapeutic activities in DSS-induced colitis. Collectively, PF2405 shows prominent anti-inflammatory effect that can be used as a new therapeutic approach for intestinal inflammatory disorders.

摘要

草药的标准化提取程序与其鉴定一样重要,以维持其质量并确保其安全使用。我们制备了一种标准化和纯化的黄芩提取物PF2405,其富含三种主要成分,黄芩素、木犀草素A和汉黄芩素。在本研究中,我们研究了PF2405在体外以及两种不同的炎症性肠病实验动物模型中的潜在抗炎作用。在体外研究了PF2405对肿瘤坏死因子(TNF)-α诱导的HT-29细胞的作用。通过给予三硝基苯磺酸(TNBS)或硫酸葡聚糖钠(DSS)诱导体内实验性结肠炎模型。PF2405(50μg/ml)通过抑制HT-29细胞中c-Jun N端激酶和p38丝裂原活化蛋白激酶的磷酸化,降低TNF-α诱导的环氧化酶(COX)-2表达。与单个成分相比,黄芩素(20μg/ml)、木犀草素A(8μg/ml)和汉黄芩素(2μg/ml)的组合显著抑制TNF-α诱导的COX-2表达。PF2405(25mg/kg体重)治疗显著降低了组织病理学严重程度;抑制了TNBS诱导的小鼠中COX-2、TNF-α和白细胞介素-1β的表达。此外,PF2405(25mg/kg体重)在DSS诱导的结肠炎中具有强大的预防和治疗活性。总体而言,PF2405显示出显著的抗炎作用,可作为肠道炎症性疾病的一种新的治疗方法。

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