Nanostructured Lipid Carriers (NLC) for Biologically Active Green Tea and Fennel Natural Oils Delivery: Larvicidal and Adulticidal Activities against Culex pipiens

(1) Background: The control of mosquitoes with essential oils is a growing demand. (2) Methods: This study evaluated the novel larvicidal and adulticidal activity of fennel and green tea oils and their nanostructured lipid carriers (NLC) against Culex pipiens (C. pipiens) in the laboratory, field conditions and evaluated their effect against non-target organisms. SLN type II nanoformulations were synthesized and characterized using dynamic light scattering (DLS), zeta potential and transmission electron microscope. (3) Results: The synthesized NLCs showed spherical shaped, homogenous, narrow, and monomodal particle size distribution. The mortality percent (MO%) post-treatment (PT) with 2000 ppm for 24 h with fennel oil and NLC fennel (NLC-F) reached 85% (LC₅₀ = 643.81 ppm) and 100% (LC₅₀ = 251.71), whereas MO% for green tea oil and NLC green tea (NLC-GT) were 80% (LC₅₀ = 746.52 ppm) and 100% (LC₅₀ = 278.63 ppm), respectively. Field trial data showed that the larval reduction percent of fennel oil and NLC-F reached 89.8% and 97.4%, 24 h PT and the reduction percent of green tea oil and NLC-GT reached 89% and 93%, 24 h PT with persistence reached 8 and 7 days, for NLC-F and NLC-GT, respectively. The adulticidal effects showed that NLC-F and NLC-GT (100% mortality) were more effective than fennel and green tea oils (90.0% and 83.33%), with 24 h PT, respectively. Moreover, their reduction of adult density after spraying with LC₉₅ X2 for 15 min, with fennel oil, NLC-F, and green tea oil, NLC-GT were 83.6%, 100%, 79.1%, and 100%, respectively, with persistence (>50%) lasting for three days. The predation rate of the mosquitofish, Gambusia affinis, and the bug, Sphaerodema urinator, was not affected in both oil and its NLC, while the predation rate of the beetle, Cybister tripunctatus increased (66% and 68.3%) by green tea oil and NLC-GT, respectively. (4) Conclusions: NLCs nanoformulation encapsulated essential oils was prepared successfully with unique properties of size, morphology, and stability. In vitro larvicidal and adulticidal effects against C. pipiens supported with field evaluations have been performed using essential oils and their nanoformulations. The biological evaluation of nanoformulations manifested potential results toward both larvicidal and adulticidal compared to the essential oils themselves, especially NLC encapsulated fennel oil which had promising larvicidal and adulticidal activity.     

Quantum Computational Investigation of (E)-1-(4-methoxyphenyl)-5-methyl-N′-(3-phenoxybenzylidene)-1H-1,2,3-triazole-4-carbohydrazide

The title compound was synthesized and structurally characterized. Theoretical IR, NMR (with the GIAO technique), UV, and nonlinear optical properties (NLO) in four different solvents were calculated for the compound. The calculated HOMO–LUMO energies using time-dependent (TD) DFT revealed that charge transfer occurs within the molecule, and probable transitions in the four solvents were identified. The in silico absorption, distribution, metabolism, and excretion (ADME) analysis was performed in order to determine some physicochemical, lipophilicity, water solubility, pharmacokinetics, drug-likeness, and medicinal properties of the molecule. Finally, molecular docking calculation was performed, and the results were evaluated in detail.     

Screening of Plant Pollen Sources,Polyphenolic Compounds,Fatty Acids and Antioxidant/Antimicrobial Activity from Bee Pollen

In this study, the botanical origin, total flavonoid and phenolic content, antioxidant activity, phenolic profile and fatty acid composition of mixed bee pollen loads collected in Bayburt, Turkey, were determined. In addition to these assays, antibacterial activity of bee-collected pollen extract (BCPE) against a variety of food-borne pathogenic bacteria was determined in vitro. Pollen loads were classified into five botanical families based on their color: Asteraceae, Fabaceae, Campanulaceae, Cistaceae and Rosaceae. Total flavonoid, total phenolic, CUPRAC and CERAC concentrations were 173.52 mg GAE/g, 79.21 mg QE/g, 85.59 mg Trolox/g and 118.13 mg Trolox/g, respectively. Twenty-three phenolic compounds were scanned in bee pollen extract by LC-MS/MS, with rutin being the most abundant. Cis-4,7,10,13,16,19 docosahexaenoic acid was the predominant fatty acid, followed by cis-11-eicosenoic acid, palmitic acid, and alfa linolenic acid. In addition, the agar well diffusion (AWD) and micro-broth dilution methods were used to determine of the antibacterial activity of the BCPE sample. MIC values were observed to vary between 2.5–5 mg/mL for Gram-positive bacteria and 5–10 mg/mL for Gram-negative bacteria. These findings indicate that bee pollen could be a potential source of antioxidants and antimicrobials.     

Polyphenolics with Strong Antioxidant Activity from Acacia nilotica Ameliorate Some Biochemical Signs of Arsenic-Induced Neurotoxicity and Oxidative Stress in Mice

Neurotoxicity is a serious health problem of patients chronically exposed to arsenic. There is no specific treatment of this problem. Oxidative stress has been implicated in the pathological process of neurotoxicity. Polyphenolics have proven antioxidant activity, thereby offering protection against oxidative stress. In this study, we have isolated the polyphenolics from Acacia nilotica and investigated its effect against arsenic-induced neurotoxicity and oxidative stress in mice. Acacia nilotica polyphenolics prepared from column chromatography of the crude methanol extract using diaion resin contained a phenolic content of 452.185 ± 7.879 mg gallic acid equivalent/gm of sample and flavonoid content of 200.075 ± 0.755 mg catechin equivalent/gm of sample. The polyphenolics exhibited potent antioxidant activity with respect to free radical scavenging ability, total antioxidant activity and inhibition of lipid peroxidation. Administration of arsenic in mice showed a reduction of acetylcholinesterase activity in the brain which was counteracted by Acacia nilotica polyphenolics. Similarly, elevation of lipid peroxidation and depletion of glutathione in the brain of mice was effectively restored to normal level by Acacia nilotica polyphenolics. Gallic acid methyl ester, catechin and catechin-7-gallate were identified in the polyphenolics as the major active compounds. These results suggest that Acacia nilotica polyphenolics due to its strong antioxidant potential might be effective in the management of arsenic induced neurotoxicity.     

In Vitro and In Silico Study of Analogs of Plant Product Plastoquinone to Be Effective in Colorectal Cancer Treatment

Plants have paved the way for the attainment of molecules with a wide-range of biological activities. However, plant products occasionally show low biological activities and/or poor pharmacokinetic properties. In that case, development of their derivatives as drugs from the plant world has been actively performed. As plant products, plastoquinones (PQs) have been of high importance in anticancer drug design and discovery; we have previously evaluated and reported the potential cytotoxic effects of a series of PQ analogs. Among these analogs, PQ2, PQ3 and PQ10 were selected for National Cancer Institute (NCI) for in vitro screening of anticancer activity against a wide range of cancer cell lines. The apparent superior anticancer potency of PQ2 on the HCT-116 colorectal cancer cell line than that of PQ3 and PQ10 compared to other tested cell lines has encouraged us to perform further mechanistic studies to enlighten the mode of anti-colorectal cancer action of PQ2. For this purpose, its apoptotic effects on the HCT-116 cell line, DNA binding capacity and several crucial pharmacokinetic properties were investigated. Initially, MTT assay was conducted for PQ2 at different concentrations against HCT-116 cells. Results indicated that PQ2 exhibited significant cytotoxicity in HCT-116 cells with an IC₅₀ value of 4.97 ± 1.93 μM compared to cisplatin (IC₅₀ = 26.65 ± 7.85 μM). Moreover, apoptotic effects of PQ2 on HCT-116 cells were investigated by the annexin V/ethidium homodimer III staining method and PQ2 significantly induced apoptosis in HCT-116 cells compared to cisplatin. Based on the potent DNA cleavage capacity of PQ2, molecular docking studies were conducted in the minor groove of the double helix of DNA and PQ2 presented a key hydrogen bonding through its methoxy moiety. Overall, both in vitro and in silico studies indicated that effective, orally bioavailable drug-like PQ2 attracted attention for colorectal cancer treatment. The most important point to emerge from this study is that appropriate derivatization of a plant product leads to unique biologically active compounds.     

Bifunctional polytetrahydrofuran initiator for sequential photochemical and thermal initiation

The polymerization of tetrahydrofuran was initiated with 4,4′-azobis(4-cyanovaleryl chloride) in conjunction with silver hexafluoroantimonate and the living polytetrahydrofuran (PTHF) was terminated with pyridinium N-oxide derivatives. The resulting PTHF-macroinitiator possesses both a thermally and photochemically labile group.     

Diffraction of electromagnetic waves by a resistive half-plane in magneto-ionic plasma

The interaction of magnetic polarized electromagnetic wave with a resistive half-plane in magneto-ionic plasma is investigated. The method of transition boundary is used for the evaluation of the diffracted wave. The excitation of surface waves is examined in the medium and their diffracted fields are derived by using the diffraction theory for grazing incidence. The uniform field expressions are obtained with the aid of the uniform theory for evanescent waves. The behaviours of the derived scattered waves are studied numerically.     

Influences of Crystal-Field and Interlayer Coupling Interactions on Dynamic Phase Diagrams of a Mixed-Spin(3/2,2) Bilayer System

Influences of crystal-fields(D_A and D_B) and interlayer coupling interactions(J_3) on dynamic magnetic critical behaviors of a mixed-spin(3/2, 2) bilayer system under an oscillating magnetic field are investigated by the Glauber-type stochastic dynamics based on the mean-field theory. For this purpose, dynamic phase diagrams are constructed in the reduced temperature and magnetic field amplitude plane for the ferromagnetic/ferromagnetic(FM/FM),antiferromagnetic/ferromagnetic(AFM/FM) and AFM/AFM interactions in detail. We observe that the influences of D_A, D_B and J_3 interactions parameters on the behavior of the dynamic phase diagrams are very much.