Ent-kaurenoic acid-enriched Mikania glomerata leaves-complexed ß-cyclodextrin: Pharmaceutical development and in vivo antitumor activity in a sarcoma 180 mouse model.

The extract obtained from Mikania glomerata leaves rich in ent-kaurenoic acid (ERKA) shows cytotoxic activity in vitro, but its hydrophobic nature and thermosensitivity are issues to be solved prior to in vivo antitumor studies. The purpose of this study was to investigate the antitumor activity of inclusion complexes formed between ERKA and ß-cyclodextrin (ERKA:ß-CD) in rodents. ERKA:ß-CD complexes obtained by malaxation (MX) and co-evaporation (CE) methods were firstly characterized regarding their physical properties, encapsulation efficiency, and cytotoxicity againts L929 cells. The antitumor activity study was then performed in mice with sarcoma 180 treated with saline, 5-fluouracil (5FU) and ERKA:ß-CD at 30, 100 and 300 µg/kg. The weight, volume, percentage of inhibition growth, gross and pathological features and positivity for TUNEL, ki67, NFκB and NRF2 in the tumors were assessed. Serum lactate-dehydrogenase activity (LDH), white blood cells count (WBC) and both gross and pathological features of the liver, kidneys and spleen were also evaluated. The formation of the inclusion complexes was confirmed by thermal analysis and FTIR, and they were non-toxic for L929 cells. The MX provided a better complexation efficiency. ERKA:ß-CD300 promoted significant tumor growth inhibition, and attenuated the tumor mitotic activity and necrosis content, comparable to 5-fluorouracil. ERKA:ß-CD300 also increased TUNEL-detected cell death, reduced Ki67 and NF-kB immunoexpression, and partially inhibited the serum LDH activity. No side effect was observed in ERKA:ß-CD300-treated animals. The ERKA:ß-CD inclusion complexes at 300 µg/kg displays antitumour activity in mice with low systemic toxicity, likely due to inhibition on the NF-kB signaling pathway and LDH activity.

Synergistic effect of aromatic plant essential oils on the ant Acromyrmex balzani (Hymenoptera: Formicidae) and antifungal activity on its symbiotic fungus Leucoagaricus gongylophorus (Agaricales: Agaricaceae).

Leaf-cutting ants have great potential for damage to agricultural and forest crops. Although chemical control is the most used method for the management of this pest, more friendly alternative methods have been investigated. Thus, this study aimed to evaluate the insecticidal and antifungal potential of essential oils obtained from Aristolochia trilobata, as well as the potential of two chemotypes of Myrcia lundiana and their major compounds (isopulegol and citral) on Acromyrmex balzani and its symbiotic fungus Leucoagaricus gongylophorus. Toxicity and synergism and/or antagonism tests were performed using essential oils and their major compounds on A. balzani ants. The antifungal activity of these compounds was tested on the fungus L. gongylophorus. The essential oils and their major compounds were toxic to A. balzani. The mixture of essential oils of A. trilobata with those of M. lundiana had higher toxicity to the ants. This synergistic effect is mainly due to the interactions between the citral compound and the major compounds present in A. trilobata essential oil. The essential oils of M. lundiana chemotypes showed antifungal properties against L. gongylophorus, and the citral compound proved to have fungicidal activity. These results show that the use of M. lundiana and A. trilobata essential oils and their major compounds is a potential alternative for the management of leaf-cutting ants A. balzani, as they have a toxic effect on worker ants and antifungal activity on their symbiotic fungus.

Essential oils from Varronia curassavica (Cordiaceae) accessions and their compounds (E)-caryophyllene and α-humulene as an alternative to control Dorymyrmex thoracius (Formicidae: Dolichoderinae).

The process of urbanization of natural environments has dramatically increased the incidence of pest insects. To control these organisms in urban environments, the last decades have been marked by an increase in the use of synthetic insecticides. However, the intensive and indiscriminate use of synthetic insecticides has provoked a series of environmental problems and human health. In this way, the concern and the searching for environmentally safer alternatives for the control of urban pests is increasing. In the present study we evaluated the lethal and sublethal effects of essential oils (EOs) of six accessions of Varronia curassavica (Jacq.) (Cordiaceae) and their constituents (E)-caryophyllene and α-humulene on the ant Dorymyrmex thoracicus Gallardo, 1916 (Formicidae: Dolichoderinae), a species commonly found in urban environments and which can cause damage to human health. Bioassays of fumigation toxicity and locomotor activity in partially treated arenas were performed. The lethal concentrations to kill 50% of the D. thoracicus population ranged from 0.69 to 2.48 µL/L for EOs and from 3.75 to 1.49 µL/L for the (E)-caryophyllene and α-humulene compounds. The survival of the ants exposed to LC95 of the treatments was reduced over time, ranging from 4.2 to 35.6 h to kill 50% of the D. thoracicus population. In general, EOs of V. curassavica caused repellency and affected the locomotor activity of the ants. Our results indicate that EOs of V. curassavica are a promising source for the control of the urban ant D. thoracicus.

Apis mellifera (Insecta: Hymenoptera) in the target of neonicotinoids: A one-way ticket? Bioinsecticides can be an alternative.

The recent decline of Apis mellifera populations around the world has been subject of intense research due to ecological and economic damages resulting from the loss of pollination services. The intensive use of insecticides from the neonicotinoids group is among the possible causal factors of this decline, including also sub-lethal effects. However, the use of synthetic insecticides has been increased on a global scale in the recent decades. In order to evaluate an alternative to the use of neonicotinoids, this work investigated the effects of a bioinsecticide and its major compound on A. mellifera (Apidae: Hymenoptera), one of the main pollinators of crop plants. For this, bees were exposed, by contact and ingestion, to the essential oil of Cymbopogon martinii (Poaceae: Poales), to geraniol (major compound) and the insecticide imidacloprid to evaluate the toxicity and behavioral effects as well as the locomotion changes and immune responses of bees treated with these compounds. In general, toxicity was greater through ingestion and the insecticide imidacloprid was more toxic to A. mellifera compared to the essential oil and its major compound. The individual and collective behaviors (i.e. trophallaxis, grooming, avoidance) as well as the immune responses of bees were not significantly affected by bioinsecticides. However, the locomotion response and flight orientation of the bees were significantly altered by insecticide when administered by ingestion. Our results highlight the potential of C. martinii essential oil and its major compound as a possible alternative to mitigate the harmful effects of neonicotinoids on bees.

Alternative control of Aedes aegypti resistant to pyrethroids: lethal and sublethal effects of monoterpene bioinsecticides.

BACKGROUND: The mosquito Aedes aegypti is intensively controlled because it is a vector of viruses that cause numerous diseases, especially in tropical regions. As a consequence of the indiscriminate use of insecticides, populations from different regions have become resistant to pyrethroids. Here, we analyzed the lethal and sublethal effects of essential oil of Aristolochia trilobata and its major compounds on A. aegypti from susceptible and pyrethroid-resistant populations. RESULTS: Our results showed that the toxicity of the different compounds and behavioral changes in response to them are dependent on the stage of the insect life cycle. The monoterpene ρ-cymene caused high mortality in both larvae and adult females of A. aegypti, including those from the pyrethroid-resistant population. The monoterpenes limonene and linalool caused a sublethal effect in the larvae, triggering changes in the swimming pattern. CONCLUSION: This study highlights the potential of the essential oil of A. trilobata and its major compounds ρ-cymene and limonene for the control of A. aegypti and reveals the importance of analyzing sublethal effects on the population dynamics of the A. aegypti mosquito. © 2017 Society of Chemical Industry.

Essential Oil of Aristolochia trilobata: Synthesis, Routes of Exposure, Acute Toxicity, Binary Mixtures and Behavioral Effects on Leaf-Cutting Ants.

Plants of the genus Aristolochia have been frequently reported as important medicinal plants. Despite their high bioactive potential, to date, there are no reports of their effects on leaf-cutting ants. Therefore, the present study aimed to evaluate the insecticidal activity of the essential oil of Aristolochia trilobata and its major components on Atta sexdens and Acromyrmex balzani, two species of leaf-cutting ants. The bioassays were performed regarding routes of exposure, acute toxicity, binary mixtures of the major components and behavioral effects. Twenty-five components were identified in the essential oil of A. trilobata using a gas chromatographic system equipped with a mass spectrometer and a flame ionization detector. The components found in higher proportions were sulcatyl acetate, limonene, p-cymene and linalool. The essential oil of A. trilobata and its individual major components were efficient against A. balzani and A. sexdens workers when applied by fumigation. These components showed fast and efficient insecticidal activity on ants. The components acted synergistically and additively on A. balzani and A. sexdens, respectively, and caused a strong repellency/irritability in the ants. Thus, our results demonstrate the great potential of the essential oil of A. trilobata and its major components for the development of new insecticides.