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姜黄素纳米结构脂质载体共递送芳樟醇和香叶醇单萜作为. 的乙酰胆碱酯酶抑制剂

Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of .

机构信息

Supplementary General Sciences Department, Faculty of Oral and Dental Medicine, Future University in Egypt, Cairo 11835, Egypt.

Department of Entomology, Faculty of Science, Cairo University, Giza 12613, Egypt.

出版信息

Molecules. 2024 Jan 4;29(1):271. doi: 10.3390/molecules29010271.

Abstract

(1) Background: A molecular hybridization docking approach was employed to develop and detect a new category of naturally activated compounds against as acetylcholinesterase inhibitors via designing a one-pot multicomponent nano-delivery system. (2) Methods: A nanostructure lipid carrier (NLC), as a second generation of solid lipid nanoparticles, was used as a carrier to deliver the active components of curcumin (Cur), geraniol (G), and linalool (L) in one nanoformulation after studying their applicability in replacing the co-crystallized ligand imidacloprid. (3) Results: The prepared nanostructure showed spherical-shaped, polydisperse particles ranging in size from 50 nm to 300 nm, as found using a transmission electron microscope. Additionally, dynamic light scattering confirmed an average size of 169 nm and a highly stable dispersed solution, as indicated by the zeta potential (-38 mV). The prepared NLC-Cur-LG displayed competitive, high-malignancy insecticidal activity against fourth instar with an elevated rate of death of 0.649 µg/mL. The treatment, due to the prepared nanostructure, affects oxidative stress enzymes, e.g., hydrogen peroxide (4 ppm), superoxide dismutase (SOD) (0.03 OD/mg), and protein carbonyl (0.08 OD/mg), and there are observable upward and downward fluctuations when using different concentrations of NLC-Cur-LG, suggesting significant problems in its foreseeable insecticidal activity. The acetylcholinesterase activity was assessed by an enzyme inhibition assay, and strengthened inhibition occurred due to the encapsulated NLCs (IC = 1.95 µg/mL). An investigation of the gene expression by Western blotting, due to treatment with NLC-Cur-LG, revealed a severe reduction of nearly a quarter of what was seen in the untreated group. As a preliminary safety step, the nanoformulation's toxicity against normal cell lines was tested, and a reassuring result was obtained of IC = 158.1 µg/mL for the normal lung fibroblast cell line. (4) Conclusions: the synthesized nanoformulation, NLC-Cur-LG, is a useful insecticide in field conditions.

摘要

(1)背景:采用分子杂交对接方法,通过设计一锅多组分纳米递药系统,开发并检测新型天然激活化合物作为乙酰胆碱酯酶抑制剂。(2)方法:纳米结构脂质载体(NLC)作为第二代固体脂质纳米粒,被用作载体,将姜黄素(Cur)、香叶醇(G)和芳樟醇(L)的活性成分在一种纳米制剂中递送,此前研究了它们替代共结晶配体吡虫啉的适用性。(3)结果:用透射电子显微镜发现,所制备的纳米结构呈球形,多分散颗粒大小在 50nm 至 300nm 之间。此外,动态光散射证实平均粒径为 169nm,zeta 电位(-38mV)表明高度稳定的分散溶液。制备的 NLC-Cur-LG 对第四龄期 表现出竞争性、高恶性杀虫活性,死亡率为 0.649μg/mL。由于制备的纳米结构,处理会影响氧化应激酶,例如过氧化氢(4ppm)、超氧化物歧化酶(SOD)(0.03 OD/mg)和蛋白质羰基(0.08 OD/mg),并且当使用不同浓度的 NLC-Cur-LG 时,会观察到向上和向下波动,表明其在可预见的杀虫活性方面存在显著问题。乙酰胆碱酯酶活性通过酶抑制测定进行评估,由于包裹的 NLC 而发生增强抑制(IC=1.95μg/mL)。通过 Western 印迹法对基因表达进行研究,由于用 NLC-Cur-LG 处理,发现未经处理组的近四分之一严重减少。作为初步的安全步骤,测试了纳米制剂对正常细胞系的毒性,得到了令人放心的结果,即正常肺成纤维细胞系的 IC=158.1μg/mL。(4)结论:合成的纳米制剂 NLC-Cur-LG 是田间条件下有用的杀虫剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cac1/10780757/9701fc7c5683/molecules-29-00271-g001.jpg

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