Search

Background: The development of novel and ecofriendly tools plays an important role in insect pest management. Nanoemulsions (NEs) based on essential oils (EOs) offer a safer alternative for human health and the environment. This study aimed to elaborate and evaluate the toxicological effects of NEs containing peppermint or palmarosa EOs combined with β‐cypermethrin (β‐CP) using ultrasound technique. Results: The optimized ratio of active ingredients to surfactant was 1:2. The NEs containing peppermint EO combined with β‐CP (NEs peppermint/β‐CP) were polydisperse with two peaks at 12.77 nm (33.4% intensity) and 299.1 nm (66.6% intensity). However, the NEs containing palmarosa EO combined with β‐CP (NEs palmarosa/β‐CP) were monodisperse with a size of 104.5 nm. Both NEs were transparent and stable for 2 months. The insecticidal effect of NEs was evaluated against Tribolium castaneum and Sitophilus oryzae adults, as well as Culex pipiens pipiens larvae. On all these insects, NEs peppermint/β‐CP enhanced pyrethroid bioactivity from 4.22‐ to 16‐folds while NEs palmarosa/β‐CP, from 3.90‐ to 10.6‐folds. Moreover, both NEs maintained high insecticidal activities against all insects for 2 months, although a slight increase of the particle size was detected. Conclusion: The NEs elaborated in this work can be considered as highly promising formulations for the development of new insecticides. © 2023 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Chemical constituents and acetylcholinesterase inhibition was investigated in both essential oil and dichloromethane subextract obtained from the aerial parts of Senecio ventanensis, an endemic Asteraceae. The chemical composition of the oil was determined by GC and GC-MS. The major constituents were -terpinene (12.2%), limonene (11.9%), -humulene (10.5%), sabinene (9.1%), terpinolene (8.8%), p-cymene (8.1%) and α-ocimene (7.3%). The bioassay guided isolation of the constituents of the active dichloromethane subextract (IC50 = 361.6 µg/mL) led us to the isolation of two diastereoisomers of a sesquiterpene endoperoxide 3,6- epidioxy-1,10-bisaboladiene (1 and 2), reported here for the first time in S. ventanensis. The identification was achieved by comprehensive analyses of its ¹H and 13C NMR spectroscopic data (including 2D experiments) and mass spectrometric data. Their absolute configuration is proposed on the basis of AM1 calculations and NOESY experiments. This is the first time that compounds 1 and 2 have been separated as well as the first phytochemical investigation of S. ventanensis. [ABSTRACT FROM AUTHOR]

The volatile fraction from aerial parts (flowers, stems and leaves) of Discaria americana Gillies & Hook (Rhamnaceae) was obtained by hydrodistillation and the chemical composition of this oil was determined by gas chromatography and gas chromatography-mass spectrometry. The major constituents resulted to be 4-methylphenol (15.5%), eugenol (11%), 3-methylindole (9.7%) and α-terpineol (6.2%). The essential oil of this plant displayed strong antioxidant activity (DPPH assay) that could be explained by the presence of active compounds like eugenol, 4-methylphenol, α-terpineol, linalool, thymol and cis-nerolidol. [ABSTRACT FROM AUTHOR]

Since the development of the "cholinergic hypothesis" as an important therapeutic approach in the treatment of Alzheimer's disease (AD), the scientific community has made a remarkable effort to discover new and effective molecules with the ability to inhibit the enzyme acetylcholinesterase (AChE). The natural function of this enzyme is to catalyze the hydrolysis of the neurotransmitter acetylcholine in the brain. Thus, its inhibition increases the levels of this neurochemical and improves the cholinergic functions in patients with AD alleviating the symptoms of this neurological disorder. In recent years, attention has also been focused on the role of another enzyme, butyrylcholinesterase (BChE), mainly in the advanced stages of AD, transforming this enzyme into another target of interest in the search for new anticholinesterase agents. Over the past decades, Nature has proven to be a rich source of bioactive compounds relevant to the discovery of new molecules with potential applications in AD therapy. Bioprospecting of new cholinesterase inhibitors among natural products has led to the discovery of an important number of new AChE and BChE inhibitors that became potential lead compounds for the development of anti-AD drugs. This review summarizes a total of 260 active compounds from 142 studies which correspond to the most relevant (IC 50 ≤ 15 μM) research work published during 2012-2022 on plant-derived anticholinesterase compounds, as well as several potent inhibitors obtained from other sources like fungi, algae, and animals., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

A bioactivity-guided approach was taken to identify the acetylcholinesterase (AChE) inhibitory agents in the ethanolic extract of Chuquiraga erinacea D. Don. subsp. erinacea leaves using a bioautographic method. This permitted the isolation of the pentacyclic triterpenes calenduladiol (1), faradiol (2), heliantriol B2 (3), lupeol (4), and a mixture of alpha-and beta-amyrin ( 5A and 5B) as active constituents. Pseudotaraxasterol (6) and taraxasterol (7) were also isolated from this extract and showed no activity at the same analytical conditions. Compound 1 showed the highest AChE inhibitory activity with 31.2 % of inhibition at 0.5 mM. Looking forward to improve the water solubility of the active compounds, the sodium sulfate ester of 1 was prepared by reaction with the (CH3)3N.SO3 complex. The semisynthetic derivative disodium calenduladiol disulfate (8) elicited higher AChE inhibition than 1 with 94.1 % of inhibition at 0.5 mM (IC (50) = 0.190 +/- 0.003 mM). Compounds 1, 2, 3, 5, 6, and 7 are reported here for the first time in C. erinacea. This is the first report of AChE inhibition from calenduladiol (1) as well as from a sulfate derived from a natural product., (Georg Thieme Verlag KG Stuttgart.New York.)