Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>

(1) Background: A molecular hybridization docking approach was employed to develop and detect a new category of naturally activated compounds against <i>Culex pipiens</i> as acetylcholinesterase inhibitors via designing a one-pot multicomponent nano-delivery system. (2) Methods: A nanost...

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Main Authors: Ibrahim Taha Radwan, Nirvina Abdel Raouf Ghazawy, Abeer Mousa Alkhaibari, Hattan S. Gattan, Mohammed H. Alruhaili, Abdelfattah Selim, Mostafa E. Salem, Eman Alaaeldin AbdelFattah, Heba M. Hamama
Format: Article
Language:English
Published: MDPI AG 2024-01-01
Series:Molecules
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Online Access:https://www.mdpi.com/1420-3049/29/1/271
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author Ibrahim Taha Radwan
Nirvina Abdel Raouf Ghazawy
Abeer Mousa Alkhaibari
Hattan S. Gattan
Mohammed H. Alruhaili
Abdelfattah Selim
Mostafa E. Salem
Eman Alaaeldin AbdelFattah
Heba M. Hamama
author_facet Ibrahim Taha Radwan
Nirvina Abdel Raouf Ghazawy
Abeer Mousa Alkhaibari
Hattan S. Gattan
Mohammed H. Alruhaili
Abdelfattah Selim
Mostafa E. Salem
Eman Alaaeldin AbdelFattah
Heba M. Hamama
author_sort Ibrahim Taha Radwan
collection DOAJ
description (1) Background: A molecular hybridization docking approach was employed to develop and detect a new category of naturally activated compounds against <i>Culex pipiens</i> 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 <i>C. pipiens</i> 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<sub>50</sub> = 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<sub>50</sub> = 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.
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spelling doaj.art-b7116bbde8014d2980b5be80b17d2d992024-01-10T15:04:42ZengMDPI AGMolecules1420-30492024-01-0129127110.3390/molecules29010271Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>Ibrahim Taha Radwan0Nirvina Abdel Raouf Ghazawy1Abeer Mousa Alkhaibari2Hattan S. Gattan3Mohammed H. Alruhaili4Abdelfattah Selim5Mostafa E. Salem6Eman Alaaeldin AbdelFattah7Heba M. Hamama8Supplementary General Sciences Department, Faculty of Oral and Dental Medicine, Future University in Egypt, Cairo 11835, EgyptDepartment of Entomology, Faculty of Science, Cairo University, Giza 12613, EgyptDepartment of Biology, Faculty of Science, University of Tabuk, Tabuk 71491, Saudi ArabiaDepartment of Medical Laboratory Sciences, Faculty of Applied Medical Sciences, King Abdulaziz University, Jeddah 22254, Saudi ArabiaSpecial Infectious Agents Unit, King Fahad Medical Research Center, King AbdulAziz University, Jeddah 21362, Saudi ArabiaDepartment of Animal Medicine (Infectious Diseases), Faculty of Veterinary Medicine, Benha University, Toukh 13736, EgyptDepartment of Chemistry, College of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), P.O. Box 90950, Riyadh 11623, Saudi ArabiaDepartment of Entomology, Faculty of Science, Cairo University, Giza 12613, EgyptDepartment of Entomology, Faculty of Science, Cairo University, Giza 12613, Egypt(1) Background: A molecular hybridization docking approach was employed to develop and detect a new category of naturally activated compounds against <i>Culex pipiens</i> 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 <i>C. pipiens</i> 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<sub>50</sub> = 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<sub>50</sub> = 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.https://www.mdpi.com/1420-3049/29/1/271curcumin<i>Culex pipeins</i>nanostructure lipid carrierenzyme activitymolecular docking
spellingShingle Ibrahim Taha Radwan
Nirvina Abdel Raouf Ghazawy
Abeer Mousa Alkhaibari
Hattan S. Gattan
Mohammed H. Alruhaili
Abdelfattah Selim
Mostafa E. Salem
Eman Alaaeldin AbdelFattah
Heba M. Hamama
Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>
Molecules
curcumin
<i>Culex pipeins</i>
nanostructure lipid carrier
enzyme activity
molecular docking
title Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>
title_full Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>
title_fullStr Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>
title_full_unstemmed Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>
title_short Nanostructure Lipid Carrier of Curcumin Co-Delivered with Linalool and Geraniol Monoterpenes as Acetylcholinesterase Inhibitor of <i>Culex pipiens</i>
title_sort nanostructure lipid carrier of curcumin co delivered with linalool and geraniol monoterpenes as acetylcholinesterase inhibitor of i culex pipiens i
topic curcumin
<i>Culex pipeins</i>
nanostructure lipid carrier
enzyme activity
molecular docking
url https://www.mdpi.com/1420-3049/29/1/271
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