Department of Pharmacy, University of Pisa, Pisa, Italy.
CISUP - Centre for Instrumentation Sharing, University of Pisa, Pisa, Italy.
J Enzyme Inhib Med Chem. 2022 Dec;37(1):1812-1820. doi: 10.1080/14756366.2022.2091556.
Several epidemiological studies suggest that a diet rich in fruit and vegetables reduces the incidence of neurodegenerative diseases. Resveratrol (Res) and its dimethylated metabolite, pterostibene (Ptb), have been largely studied for their neuroprotective action. The clinical use of Res is limited because of its rapid metabolism and its poor bioavailability. Ptb with two methoxy groups and one hydroxyl group has a good membrane permeability, metabolic stability and higher bioavailability in comparison with Res. The metabolism and pharmacokinetics of Ptb are still sparse, probably due to the lack of tools that allow following the Ptb destiny both in living cells and . In this contest, we propose two Ptb fluorescent derivatives where Ptb has been functionalised by benzofurazan and rhodamine-B-isothiocyanate, compounds and , respectively. Here, we report the synthesis, the optical and structural characterisation of and , and, their putative cytotoxicity in two different cell lines.
几项流行病学研究表明，富含水果和蔬菜的饮食可降低神经退行性疾病的发病率。白藜芦醇（Res）及其二甲化代谢物，均二苯乙烯（Ptb），因其具有神经保护作用而受到广泛研究。由于其快速代谢和生物利用度差，Res 的临床应用受到限制。与 Res 相比，具有两个甲氧基和一个羟基的 Ptb 具有良好的膜透过性、代谢稳定性和更高的生物利用度。Ptb 的代谢和药代动力学仍然很少，这可能是由于缺乏工具，无法在活细胞和体内跟踪 Ptb 的命运。在这种情况下，我们提出了两种 Ptb 荧光衍生物，其中 Ptb 分别被苯并呋咱和罗丹明-B-异硫氰酸酯官能化，分别得到化合物和。在这里，我们报告了和的合成、光学和结构表征，以及它们在两种不同细胞系中的潜在细胞毒性。
