Institute of TCM & Natural Products, College of Pharmacy, Jinan University, Guangzhou 510623, People's Republic of China.
Institute of Synthetic Biology, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, People's Republic of China.
Food Funct. 2020 Oct 21;11(10):8825-8836. doi: 10.1039/d0fo01678k.
Crocins, a series of hydrophilic carotenoids that are either mono- or di-glycosyl polyene esters of crocetin extracted from dried saffron stigma or fruits of gardenia, are attracting much attention due to their wide range of pharmacological effects. In our previous study, GJ-4, a mixture of crocin analogues, was obtained and derived from gardenia fruits. Mainly 18 crocin analogues were identified from GJ-4 and found to exhibit neuroprotective effects in in vitro and in vivo models. In this present study, we continue to investigate the therapeutic effects of GJ-4 on learning and memory impairments in a 2VO-induced VaD model, and the potential mechanism. In addition, the metabolic profiles and pharmacokinetic properties of GJ-4 were determined using liquid chromatography-electrospray ionization-mass spectrometry after single and multiple oral doses. All these findings presented here will serve as a solid basis to develop GJ-4 as a new therapeutic agent for dementia.
西红花柱头或栀子果实中提取的西红花酸的一系列亲水性类胡萝卜素，即西红花苷单或二糖苷多烯酯，由于其广泛的药理作用而备受关注。在我们之前的研究中，从栀子果实中获得了一种西红花苷类似物混合物 GJ-4。从 GJ-4 中主要鉴定出 18 种西红花苷类似物，并在体外和体内模型中发现具有神经保护作用。在本研究中，我们继续研究 GJ-4 在 2VO 诱导的 VaD 模型中对学习和记忆障碍的治疗作用及其潜在机制。此外，还使用液相色谱-电喷雾电离-质谱法在单次和多次口服给药后测定了 GJ-4 的代谢谱和药代动力学特性。本研究中的所有这些发现将为将 GJ-4 开发为治疗痴呆症的新型治疗剂提供坚实的基础。
