有忧郁症(W.somnifera)在改善神经活性疾病方面具有悠久的安全性。本研究旨在探索WithaniaSomnifera植物活性原理抗微生物,蚂蚁神经病,和抗炎活性,并利用纳米立方体利用其作用机制来修饰这些活动。采用生物引导分馏技术,为了确定最具植物活性的化合物,使用LC-MS-NMR在线技术和糖尿病的生物模型,神经病,和炎症。还监测了体外抗菌活性。HbA1c,体内抗氧化剂(血清过氧化氢酶,TBARS,和GSH),血清胰岛素,和促炎血清细胞因子(TNFα,IL-6,和IL-10)水平已被评估以建立抗神经性和抗炎机制。利用纳米立方体制剂(CUB1-3)来改善睡梦草最具活性的化合物功效。嗜血杆菌显示出十个主要峰值;凝血素Q(10.2%),二氢缩内酯A(2.4%),二氢含铁林D(1.8%),PhysagulinD(7.6%),与AnosideV(2.3%),与内酯A(WDA,10.3%),非洲A(4.9%),含D(7.7%),含酮9(9.9%),与NolideD(4.8%)。利用LC-MS-NMR技术的生物引导分级分离技术已证明,NituolideA(WDA)是大豆中最具植物活性的化合物。后者显示出比WDA更好的结果,这可能是由于Ws中的其他有效化合物。然而,CUB3(WDA纳米立方体分散体)显示出更突出的抗糖尿病作用,抗神经病,抗炎,和抗菌潜力比Ws和WDA。因此,CUB3修改了WDA活动,并提高了疗效。HbA1c水平正常化,增加胰岛素分泌的潜力,氧化应激的改善可能是潜在的Ws,WDA,和CUB3抗糖尿病神经病变机制。此外,TheWs,WDA,和CUB1-3抗炎机制可能是由于改善了促炎血清细胞因子(降低TNFα和IL-6水平和增加IL-10)。因此,CUB3可能是增强WithaniaSomnifera活性的强大工具,作为口服药物递送系统,并提高其对神经病变和炎症的疗效。
Withania somnifera (W. somnifera) has a long history of safety in the amelioration of neuro-active ailments. The current study aims to explore Withania somnifera phyto-active principle anti-microbial, ant-neuropathic, and anti-inflammatory activities, and to modify these activities utilizing nano-cubosomes exploiting their mechanisms of action. Bio-guided fractionation technique was utilized, to identify the most phyto-active compound, using LC-MS-NMR online technique and biological models of diabetes,
neuropathy, and inflammation. In-vitro antibacterial activity was also monitored. The HbA1c, in-vivo antioxidant (serum-catalase, TBARS, and GSH), serum insulin, and pro-inflammatory serum cytokines (TNF alpha, IL-six, and IL-ten) levels have been assessed to establish the anti-neuropathic and anti-inflammatory mechanisms. The nano-cubosomal formulations (CUB 1-3) were utilized to improve the W. somnifera most active compound efficacy. W. somnifera has shown ten major peaks; coagulin Q (10.2 %), dihydrowithanolide A (2.4 %), dihydrowithaferin D (1.8 %), physagulin D (7.6 %), withanoside V (2.3 %), withanolide A (WDA, 10.3 %), withafrin A (4.9 %), withaferin D (7.7 %), withanone 9 (9.9 %), withanolide D (4.8 %). The bio-guided fractionation technique utilizing LC-MS-NMR technique has proved that withanolide A (WDA) is the most phyto-active compound in W. somnifera. The latter has shown better results than WDA, which might be due to other effective compounds in Ws. However, CUB 3 (WDA nano-cubosomes dispersion) has shown more prominent anti-diabetic, anti-neuropathic, anti-inflammatory, and anti-bacterial potentials than Ws and WDA. Thus, CUB 3 modified WDA activity, and improved its efficacy. The normalization of HbA1c levels, increased insulin secretagogue potential, and the amelioration of the oxidative-stress may be the underlying Ws, WDA, and CUB 3 antidiabetic
neuropathy mechanism. Moreover, the Ws, WDA, and CUB 1-3 anti-inflammatory mechanism might be due to the amelioration of the pro-inflammatory serum cytokines (decreasing TNF alpha and IL-six levels and increasing IL-ten). Thus, CUB 3 might be a powerful tool in augmenting Withania somnifera activity as an oral drug-delivery system and improving its efficacy against
neuropathy and inflammation.