Department of Pharmacognosy, Semmelweis University, Budapest H-1085, Hungary.
Department of Pharmacognosy, Semmelweis University, Budapest H-1085, Hungary.
J Pharm Biomed Anal. 2020 Jan 5;177:112820. doi: 10.1016/j.jpba.2019.112820. Epub 2019 Aug 19.
Ginger, the rhizome of Zingiber officinale Roscoe is of great importance in the traditional medicine for the treatment of various diseases. More than 400 constituents have been reported in the plant, the most important ones being the gingerol and shogaol derivatives. Positive effects of ginger extracts and isolated [6]-gingerol have been proved in animal models of anxiety, Alzheimer's disease, Parkinson's disease and epilepsy. Taken in consideration these promising positive effects of ginger and its constituents in the central nervous system, the isolation of gingerol and shogaol derivatives ([6]-gingerol (1), [8]-gingerol (2), [10]-gingerol (3), [6]-shogaol (4), [10]-shogaol (5), 1-dehydro-[6]-gingerdione (6), 1-dehydro-[10]-gingerdione (7)) and investigation of their transcellular passive diffusion across the blood-brain barrier (BBB) were carried out. For this purpose, a Parallel Artificial Membrane Permeability Assay for the Blood-Brain Barrier (PAMPA-BBB) was chosen that had previously been validated for natural compounds. Based on our results, [6]-gingerol, [8]-gingerol and [6]-shogaol were found to be able to penetrate the BBB via passive diffusion, suggesting them to contribute to the positive effects of ginger extracts in the central nervous system.
生姜是姜属植物的根茎，在传统医学中对于治疗各种疾病具有重要意义。该植物中已报道有超过 400 种成分，其中最重要的是姜辣素和姜烯酚衍生物。生姜提取物和分离得到的[6]-姜辣素在焦虑、阿尔茨海默病、帕金森病和癫痫的动物模型中已被证明具有积极作用。鉴于生姜及其成分在中枢神经系统中具有这些有前景的积极作用，对姜辣素和姜烯酚衍生物（[6]-姜辣素（1）、[8]-姜辣素（2）、[10]-姜辣素（3）、[6]-姜烯酚（4）、[10]-姜烯酚（5）、1-脱氢-[6]-姜二酮（6）、1-脱氢-[10]-姜二酮（7））进行了分离，并研究了它们在跨血脑屏障（BBB）的被动扩散。为此，选择了先前已针对天然化合物进行验证的用于血脑屏障的平行人工膜透过性测定法（PAMPA-BBB）。根据我们的结果，发现[6]-姜辣素、[8]-姜辣素和[6]-姜烯酚能够通过被动扩散穿透 BBB，这表明它们有助于生姜提取物在中枢神经系统中的积极作用。
