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Croton argyrophyllus Kunth., commonly known as "marmeleiro" or "cassetinga," is widely distributed in the Brazilian Northeast region. Its leaves and flowers are used in traditional medicine as tranquilizers to treat flu and headaches. This study was conducted to determine the chemical composition and toxicological safety of essential oil from C. argyrophyllus leaves using in vitro and in vivo models. The chemical composition of the essential oil was determined using a gas chromatograph coupled to a mass spectrometer. Cytotoxicity was tested in the HeLa, HT-29, and MCF-7 cell lines derived from human cells (Homo sapiens) and Vero cell lines derived from monkeys (Cercopithecus aethiops) using the MTT method. Acute toxicity, genotoxicity. Mutagenicity tests were performed in Swiss mice (Mus musculus), which were administered essential oil orally in a single dose of 2000 mg/kg by gavage. The main components of the essential oil were p -mentha-2- en -1-ol, α-terpineol, β-caryophyllene, and β-elemene. The essential oil exhibited more than 90% cytotoxicity in all cell lines tested. No deaths or behavioral, hematological, or biochemical changes were observed in mice, revealing no acute toxicity. In genotoxic and mutagenic analyses, there was no increase in micronuclei in polychromatic erythrocytes or in the damage and index in the comet assay. The essential oil was cytotoxic towards the tested cell lines but did not exert toxic effects or promote DNA damage when administered orally at a single dose of 2000 mg/kg in mice. [Display omitted] [ABSTRACT FROM AUTHOR]

• Croton essential oils blend shows larvicidal effect on Aedes aegypti. • Croton essential oils blend has adulticidal effect on Aedes aegypti. • In mammals the blend administered orally was non-toxic. • Camphor, iso-pinocampheol and (E) caryophyllene are the main compounds of the blend. • The blend has characteristics relevant to the formulation of botanical insecticides. New control alternatives to chemical insecticides, such as botanical essential oils, are important to reduce the population of mosquito vectors. In addition, the use of these oils as insecticides should be safe for mammals. The objective of this study was therefore to evaluate the insecticidal activity of a blend of essential oils from the leaves of Croton argyrophyllus Kunth. and Croton tetradenius Baill. on Aedes aegypti Linnaeus, 1762, as well as to evaluate its acute toxicity in Mus musculus Linnaeus, 1758, and to analyze the chemical composition of this blend. The blend was prepared from a combination of these essential oils in the proportion of 1:1 (m/m). Larvae and adults of Ae. aegypti were used for insecticidal evaluation. In the acute toxicity analysis, the essential oil blend was administered intraperitoneally and orally to M. musculus. Gas chromatography together with mass spectrometry was used for chemical evaluation. The blend presented insecticidal properties, with an additive effect on larvicidal activity (LC 50 =0.16 mg mL-1) and a synergistic effect on adulticidal activity (LC 50 =0.75 mg mL-1). When administered intraperitoneally to mice, the blend displayed intermediate acute toxicity (LD 50 =500 mg kg-1), and no toxicity was observed after oral administration (LD 50 =2500 mg kg-1). Camphor (15.9%), isopinocampheol (12.1%), and (E)-caryophyllene (9.5%) were the main components of this blend. Thus, the blend of essential oils of C. argyrophyllus and C. tetradenius has insecticidal properties against Ae. aegypti and is also safe for mammals, relevant characteristics for the formulation of botanical insecticides. [ABSTRACT FROM AUTHOR]

Aedes aegypti serves as the primary vector for viruses like dengue, Chikungunya, Zika, and yellow fever, posing a significant public health challenge in Brazil. Given the absence of approved vaccines for these diseases, effective mosquito control becomes paramount in preventing outbreaks. However, currently available chemical insecticides face issues related to toxicity and the emergence of resistance, necessitating the exploration of new active compounds. Drawing inspiration from natural products, we identified the 1,3-benzodioxole group as a key pharmacophore associated with insecticidal activity. Therefore, this study aimed to synthesize and assess the larvicidal activity of 1,3-benzodioxole acids against Ae. aegypti , as well as their toxicity in mammals. Among the compounds evaluated, 3,4-(methylenedioxy) cinnamic acid (compound 4) demonstrated larvicidal activity. It exhibited LC 50 and LC 90 values of 28.9 ± 5.6 and 162.7 ± 26.2 μM, respectively, after 24 h of exposure. For reference, the positive control, temephos, displayed both LC 50 and LC 90 values below 10.94 μM. These findings underline the significance of the 3,4-methylenedioxy substituent on the aromatic ring and the presence of a double bond in the aliphatic chain for biological activity. Furthermore, compound 4 exhibited no cytotoxicity towards human peripheral blood mononuclear cells, even at concentrations up to 5200 μM. Lastly, in mice treated with 2000 mg kg−1, compound 4 showed mild behavioral effects and displayed no structural signs of toxicity in vital organs such as the kidney, liver, spleen, and lungs. [Display omitted] • 3,4-(Methylenedioxy) cinnamic acid has larvicidal activity against Ae. aegypti. • 3,4-(Methylenedioxy) cinnamic acid showed no toxicity to mice nor human PBMC. • 3,4-(Methylenedioxy) cinnamic acid do not inhibit acetylcholinesterase. • 1,3-Benzodioxole subunit is an essential pharmacophore for insecticidal activity. • 3,4-(Methylenedioxy) cinnamic acid could be a new prototype for larvicidal agents. [ABSTRACT FROM AUTHOR]