| Geraniol targets K(V)1.3 ion channel and exhibits anti-inflammatory activity in vitro and in vivo |
| Ye, CJ; Li, SA; Zhang, Y ; Lee, WH
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| 2019
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| 发表期刊 | FITOTERAPIA
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| ISSN | 0367-326X
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| 卷号 | 139页码:- |
| 摘要 | Naturally occurring monoterpenes are known for their various pharmacological activities including anti-inflammation. K(V)1.3 ion channel is a voltage-gated potassium channel and has been validated as a drug target for autoimmune and chronic inflammatory diseases like psoriasis. Here we experimentally test the direct interaction between monoterpenes and K(V)1.3 ion channel. Our electrophysiological analysis determined that monoterpenes (geraniol, nerol, beta-citronellol, citral and linalool) have inhibitory effects on K(V)1.3 ion channel. Representatively, geraniol reversibly blocked K(V)1.3 currents in a voltage-dependent manner with an IC50 of 490.50 +/- 1.04 mu M at + 40 mV in HEK293T cells. At the effective concentrations, geraniol also inhibited cytokine secretion of activated human T cells, including IL-2, TNF-alpha and IFN-gamma. In an imiquimod-induced psoriasis-like animal model, geraniol administration significantly reduced psoriasis area and severity index scores, ameliorated the deteriorating histopathology and decreased the degree of splenomegaly. Together, our findings not only suggest that monoterpenes may serve as lead molecules for the development of K(V)1.3 inhibitors, but also indicate that geraniol could be considered as a promising therapeutic candidate to treat autoimmune diseases. |
| 收录类别 | SCI
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| 语种 | 英语
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| 文献类型 | 期刊论文
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| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/13096
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| 专题 | 科研部门_生物毒素与人类疾病（张云）
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推荐引用方式
GB/T 7714 |
Ye, CJ,Li, SA,Zhang, Y,et al. Geraniol targets K(V)1.3 ion channel and exhibits anti-inflammatory activity in vitro and in vivo[J]. FITOTERAPIA,2019,139:-.
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| APA |
Ye, CJ,Li, SA,Zhang, Y,&Lee, WH.(2019).Geraniol targets K(V)1.3 ion channel and exhibits anti-inflammatory activity in vitro and in vivo.FITOTERAPIA,139,-.
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| MLA |
Ye, CJ,et al."Geraniol targets K(V)1.3 ion channel and exhibits anti-inflammatory activity in vitro and in vivo".FITOTERAPIA 139(2019):-.
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