Search Results (5)

This study investigates the therapeutic potential of Lippia origanoides essential oil (LOEO) in neurological and pharmaceutical applications. The chemical composition of LOEO was analyzed using gas chromatography–mass spectrometry (GC-MS), revealing major constituents, such as carvacrol, thymol, and γ-gurjunene, known for their antioxidant and antimicrobial properties. LOEO demonstrated significant acetylcholinesterase (AChE)-inhibitory activity, particularly in a nanoformulation that enhances bioavailability and stability. Additionally, the major constituent carvacrol, when tested in isolation, also exhibited AChE-inhibitory activity comparable to that of the nanoformulation. Molecular docking analysis indicated strong binding affinities between LOEO compounds and AChE, supporting its therapeutic potential for neurodegenerative diseases like Alzheimer’s. Additionally, in silico pharmacokinetic predictions revealed favorable absorption and blood–brain barrier penetration profiles for key constituents. Despite promising results, this study acknowledges the need for in vivo validation and long-term stability assessments of the nanoformulation. Future research should focus on pharmacodynamic studies and evaluating the oil’s effectiveness in animal models. These findings highlight LOEO as a valuable candidate for developing natural therapies for neurodegenerative diseases. Full article

Diseases transmitted by vectors such as Aedes aegypti and Culex quinquefasciatus (Diptera: Culicidae) have been responsible for endemics and epidemics in several countries, causing irreparable damage to human health. For this reason, vector control is one of the main strategies to prevent the contamination and dissemination of these etiological agents. In this study, the essential oil (EO) of Ocimum basilicum was obtained by hydrodistillation, and the compounds were identified by GC/MS. A nanoemulsion was obtained through a low-energy input method and evaluated by photon correlation spectroscopy. Bioassays were performed against 4th instar larvae of A. aegypti and C. quinquefasciatus. Furthermore, additional in silico studies of biological activity prediction and molecular docking for the acetylcholinesterase enzyme and juvenile hormone protein targets were performed with the 53 identified compounds of the EO. The major compounds identified in greater quantity were linalool (32.66%) and anethole (32.48%). The obtained nanoemulsion had an average size diameter between 244.6 and 280.4 nm and a polydispersity index below 0.250 during the entire storage period. The nanoemulsion was tested at concentrations of 10, 20, 30, 40, and 50 mg/L and the following activity values were observed: LC₅₀ = 42.15 mg/L and 40.94 mg/L and LC₉₀ = 50.35 mg/L and 48.87 mg/L for A. aegypti (24 h and 48 h); LC₅₀ = 39.64 mg/L and 38.08 mg/L and LC₉₀ = 52.58 mg/L and 54.26 mg/L for C. quinquefasciatus (24 h and 48 h). The in silico results showed better activity values for linalool, anethole, carvone, α-selinene, eugenol, and limonene. The α-selinene compound showed the best binding affinity with the insect acetylcholinesterase enzyme (−9.1 Kcal) in molecular docking, showing the importance of antagonist compounds in elucidating the mechanism of action for the investigated targets. Thus, the studied nanoemulsion was considered active against the tested species, becoming a potential alternative as an ecological bioinsecticide due to bioactivity and simplicity of formulation. Full article

Aceclofenac (ACF) is a widely used non-steroidal anti-inflammatory drug (NSAID) known for its effectiveness in treating pain and inflammation. Recent studies have demonstrated that ACF possesses antiproliferative properties, inhibiting the growth of cancer cells in various cancer cell lines. Citronellol, a monoterpenoid alcohol found in essential oils, exhibits antioxidant properties and activities such as inhibiting cell growth and acetylcholinesterase inhibition. In this study, the objective was to formulate and evaluate an aceclofenac/citronellol oil nanoemulsion for its antiproliferative effects on melanoma. The optimal concentrations of citronellol oil, Tween 80, and Transcutol HP were determined using a pseudoternary phase diagram. The formulated nanoemulsions were characterized for droplet size, zeta potential, thermophysical stability, and in vitro release. The selected formula (F1) consisted of citronellol oil (1 gm%), Tween 80 (4 gm%), and Transcutol HP (1 gm%). F1 exhibited a spherical appearance with high drug content, small droplet size, and acceptable negative zeta potential. The amorphous state of the drug in the nanoemulsion was confirmed by Differential Scanning Calorimetry, while FTIR analysis indicated its homogenous solubility. The nanoemulsion showed significant antiproliferative activity, with a lower IC50 value compared to aceclofenac or citronellol alone. Flow cytometric analysis revealed cell cycle arrest and increased apoptosis induced by the nanoemulsion. In silico studies provided insights into the molecular mechanism underlying the observed antitumor activity. In conclusion, the developed aceclofenac/citronellol oil nanoemulsion exhibited potent cytotoxicity and pro-apoptotic effects, suggesting its potential as a repurposed antiproliferative agent for melanoma treatment. In a future plan, further animal model research for validation is suggested. Full article

Organosulfur compounds, phenolic acids and flavonoids in raw and black garlic were determined, and followed by preparation of black garlic nanoemulsion for studying their effects on deoxycorticosterone acetate-salt-induced hypertension and associated mild cognitive impairment in rats. Three organosulfur compounds, including diallyl sulfide (87.8 μg/g), diallyl disulfide (203.9 μg/g) and diallyl trisulfide (282.6 μg/g) were detected in black garlic by GC-MS, while gallic acid (19.19 μg/g), p-coumaric acid (27.03 μg/g) and quercetin (22.77 μg/g) were detected by UPLC-MS/MS. High doses of both black garlic extract and nanoemulsion prepared using Tween-80, glycerol, grapeseed oil and water could decrease systolic blood pressure through the elevation of bradykinin and nitric oxide levels as well as diminish aldosterone and angiotensin II levels in rats. In Morris water maze test, they could significantly decrease escape latency and swimming distance and increase the time spent in the target quadrant, accompanied by a decline of acetylcholinesterase activity and malondialdehyde level in the hippocampus as well as a rise in glutathione level and activities of superoxide dismutase, catalase and glutathione peroxidase. In addition, the levels of tumor necrosis factor, interleukin-6 and interleukin-1β were reduced. Effects of lowering blood pressure and improving learning/memory ability in rats followed the order: lisinopril > black garlic nanoemulsion > black garlic extract. Full article

Baccharis reticularia DC. is a plant species from the Asteraceae family that is endemic to Brazil. Despite the great importance of Baccharis genus, no study has been carried out regarding either the phytochemical composition of B. reticularia or the evaluation of its larvicidal potential. Considering the intrinsic immiscibility of essential oils, this study shows larvicidal nanoemulsions containing the B. reticularia phytochemically characterized essential oil and its main constituent against Aedes aegypti. The major compound found was d-limonene (25.7%). The essential oil inhibited the acetylcholinesterase, one of the main targets of insecticides. The required hydrophile-lipophile balance of both nanoemulsions was 15.0. The mean droplet sizes were around 90.0 nm, and no major alterations were observed after 24 h of preparation for both formulations. After 48 h of treatment, the estimated LC₅₀ values were 118.94 μg mL⁻¹ and 81.19 μg mL⁻¹ for B. reticularia essential oil and d-limonene nanoemulsions, respectively. Morphological alterations evidenced by scanning electron micrography were observed on the larvae treated with the d-limonene nanoemulsion. This paper demonstrated a simple and ecofriendly method for obtaining B. reticularia essential oil and d-limonene aqueous nanoemulsions by a non-heating and solvent-free method, as promising alternatives for Aedes aegypti control. Full article