Formula Optimization of the Jiashitang Scar Removal Ointment and Antiinflammatory Compounds Screening by NF-κB Bioactivity-guided Dual-luciferase Reporter Assay System

被引：16

作者：

Gao, Jie ^{[1
,2
]}

Tao, Jin ^{[1
,2
]}

Zhang, Nannan ^{[1
,2
]}

Liu, Yanjie ^{[1
,2
]}

Jiang, Min ^{[1
,2
]}

Hou, Yuanyuan ^{[1
,2
]}

Wang, Qian ^{[3
]}

Bai, Gang ^{[1
,2
]}

机构：

[1] Nankai Univ, State Key Lab Med Chem Biol, Tianjin 300071, Peoples R China

[2] Nankai Univ, Coll Pharm, Tianjin 300071, Peoples R China

[3] Henan Radio & Televis Univ, Zhengzhou 450008, Peoples R China

来源：

PHYTOTHERAPY RESEARCH | 2015年 / 29卷 / 02期

基金：

中国国家自然科学基金;

关键词：

optimization; response surface methodology; UPLC/Q-TOF; inflammation; NF-kappa B; FLIGHT MASS-SPECTROMETRY; IN-VITRO; PATHWAY; IDENTIFICATION; ACTIVATION; MECHANISMS; INHIBITORS; AGONISTS; INJURY; CELLS;

D O I：

10.1002/ptr.5244

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inflammation plays a role in scar formation; therefore, decreasing inflammation benefits scar removal. Jiashitang scar removal ointment (JST) is a commercially available traditional Chinese medicinal formulation. It is composed of extracts from Carthamus tinctorius L. (Car), Rheum officinale Baill. (Rhe), Salvia miltiorrhiza Beg. (Sal), and Panax notoginseng (Burk.) F.H. Chen (Pan), which are all herbs with potent antiinflammatory activities. Our aims are to optimize the formula of JST and to elucidate its antiinflammatory active components. Response surface methodology was applied to optimize proportions of the four herb extracts. The antiinflammatory effects were evaluated using in vitro and in vivo models. To screen for active components in this formula, a bioactivity-based ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry analysis was performed. After optimization, the antiinflammatory effects of the new formula were significantly superior to the original one. Screening identified 13 active ingredients: a series of saffiomin, emodin, salvianolic acid, tanshinone, and triterpenoid saponin derivatives. These active ingredients were predicted to exert nuclear factor-B inhibiting effects through MAPK, PI3K/AKT, and NIK-IKK pathways. In conclusion, the original formula was successfully optimized with more potent antiinflammatory activity. These methods can be applied to researches of other formulas. Copyright (c) 2014 John Wiley & Sons, Ltd.

引用

页码：241 / 250

页数：10