苦参
药理学
趋化因子
化学
细胞因子
杨梅素
类黄酮
生物
生物化学
免疫学
受体
抗氧化剂
山奈酚
苦参碱
色谱法
作者
Chwan‐Fwu Lin,Ming‐Hsien Lin,Chi‐Feng Hung,Abdullah Alshetaili,Yung‐Fong Tsai,Chien‐Hung Jhong,Jia‐You Fang
摘要
Abstract The herb Sophora flavescens displays anti‐inflammatory activity and can provide a source of antipsoriatic medications. We aimed to evaluate whether S. flavescens extracts and compounds can relieve psoriasiform inflammation. The ability of flavonoids (maackiain, sophoraflavanone G, leachianone A) and alkaloids (matrine, oxymatrine) isolated from S. flavescens to inhibit production of cytokine/chemokines was examined in keratinocytes and macrophages. Physicochemical properties and skin absorption were determined by in silico molecular modeling and the in vitro permeation test (IVPT) to establish the structure‐permeation relationship (SPR). The ethyl acetate extract exhibited higher inhibition of interleukin (IL)‐6, IL‐8, and CXCL1 production in tumor necrosis factor‐α‐stimulated keratinocytes compared to the ethanol and water extracts. The flavonoids demonstrated higher cytokine/chemokine inhibition than alkaloids, with the prenylated flavanones (sophoraflavanone G, leachianone A) led to the highest suppression. Flavonoids exerted anti‐inflammatory effects via the extracellular signal‐regulated kinase, p38, activator protein‐1, and nuclear factor‐κB signaling pathways. In the IVPT, prenylation of the flavanone skeleton significantly promoted skin absorption from 0.01 to 0.22 nmol/mg (sophoraflavanone G vs. eriodictyol). Further methoxylation of a prenylated flavanone (leachianone A) elevated skin absorption to 2.65 nmol/mg. Topical leachianone A reduced the epidermal thickness in IMQ‐treated mice by 47%, and inhibited cutaneous scaling and cytokine/chemokine overexpression at comparable levels to a commercial betamethasone product. Thus, prenylation and methoxylation of S. flavescens flavanones may enable the design of novel antipsoriatic agents.
科研通智能强力驱动
Strongly Powered by AbleSci AI