Beclomethasone17-propionate(Beclomethasone-17-monopropionate)是Beclomethasonedipropionate的活性代谢产物，是糖皮质激素受体(GR)激动剂。Beclomethasone17-propionate对GR的亲和力比Beclomethasonedipropionate高。Beclomethasone17-propionate有效抑制慢性阻塞性肺疾病(COPD)肺巨噬细胞中细胞因子的产生。
Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate , is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages[1][2][3].
Metabolism of Beclomethasone dipropionate to 17-BMP is an important activation step. Beclomethasone 17-propionate inhibits LPS-stimulated CXCL8, TNFα and IL-6. The EC50 values of Beclomethasone 17-propionate for IL-6, TNFα and CXCL8 were 0.05 nM, 0.01 nM and 0.1 nM, respectively. Beclomethasone 17-propionate evokes upregulation of the GR dependent genes FKBP51 and GILZ[3].
[1]. Würthwein G, et al. Activation of beclomethasone dipropionate by hydrolysis to beclomethasone-17-monopropionate. Biopharm Drug Dispos. 1990 Jul;11(5):381-94. [2]. Roberts JK, et al. Metabolism of beclomethasone dipropionate by cytochrome P450 3A enzymes. J Pharmacol Exp Ther. 2013 May;345(2):308-16. [3]. Plumb J, et al. Evaluation of glucocorticoid receptor function in COPD lung macrophages using beclomethasone-17-monopropionate. PLoS One. 2013 May 21;8(5):e64257.
动态评分
0.0