应对中枢神经系统疾病复杂性的最有希望的方法之一是新的多靶标定向配体(MTDL)。五种药用物种(Cereusgrandiflorus(L.)磨坊。,HysopusofficinalisL.,:水飞蓟花L.Gaertn.还有TurneradiffusaWilld.ExSchult),选择了它们的民族药理学相关性,是体外筛选的对象。白花蛇舌草的水提物显示出最强的神经活性潜能,抑制单胺氧化酶-A(IC50=129.80±11.97μg/mL),乙酰和丁酰胆碱酯酶(IC25=0.352±0.011和0.370±0.036mg/mL,分别)。通过HPLC-DAD-ESI/MSn首次建立了其酚谱。在该物种中,新发现了37种化合物中的26种。用这种富含类黄酮的提取物进行的预处理促进了谷氨酸浓度神经元细胞(SH-SY5Y)死亡反应曲线的向右移动。此外,它显着减少了谷氨酸和t-BHP暴露后细胞内反应物质的早期形成,这表明SH-SY5Y细胞的神经保护作用,在某种程度上,由抗氧化机制介导。
One of the most promising approaches to confront the complexity of central nervous system disorders are new multi-target directed ligands (MTDLs). Five medicinal species (Cereus grandiflorus (L.) Mill., Hyssopus officinalis L., Acorus calamus L., Silybum marianum L. Gaertn. and Turnera diffusa Willd. Ex Schult), selected for their ethnopharmacological relevance, were object for in vitro screening. The aqueous extract of T. diffusa revealed the strongest neuroactive potential, inhibiting monoamine oxidase-A (IC50 = 129.80 ± 11.97 μg/mL), and acetyl- and butyrylcholinesterase (IC25 = 0.352 ± 0.011 and 0.370 ± 0.036 mg/mL, respectively). Its phenolic profile was established for the first time by HPLC-DAD-ESI/MSn. Twenty-six out of thirty-seven compounds were newly identified in this species. The pre-treatment with this flavonoid-rich extract promoted a rightward shift of the glutamate concentration neuronal cell (SH-SY5Y) death response curve. Furthermore, it significantly reduced the early phase formation of intracellular reactive species after glutamate and t-BHP exposure, suggesting that neuroprotection in SH-SY5Y cells was, in part, mediated by antioxidant mechanisms.