Liposomal nanoformulations with trans-caryophyllene and caryophyllene oxide: do they have an inhibitory action on the efflux pumps NorA, Tet(K), MsrA, and MepA?

This study aimed to evaluate the antibacterial and inhibitory action of NorA, Tet(K), MsrA and MepA efflux pumps in S. aureus strains using the sesquiterpenes named trans-caryophyllene and caryophyllene oxide, both isolated and encapsulated in liposomes. The antibacterial and inhibitory action of these efflux pumps was evaluated through the serial microdilution test in 96-well microplates. Each sesquiterpene and liposome/sesquiterpene was combined with antibiotics and ethidium bromide (EtBr). The antibiotics named norfloxacin, tetracycline and erythromycin were used. The 1199 B, IS-58, RN4220 and K2068 S. aureus strains carrying NorA, Tet(K), MsrA and MepA, respectively, were tested. In the fluorescence measurement test, K2068 S. aureus was incubated with the sesquiterpenes and EtBr, and the fluorescence emission by EtBr was measured. The tested substances did not show direct antibacterial activity, with MIC >1024 µg/mL. Nonetheless, the isolated trans-caryophyllene and caryophyllene oxide reduced the MIC of antibiotics and EtBr, indicating inhibition of NorA, Tet(K) and MsrA. In the fluorescence test, these same sesquiterpenes increased fluorescence emission, indicating inhibition of MepA. Therefore, the sesquiterpenes named trans-caryophyllene and caryophyllene oxide did not show direct antibacterial action; however, in their isolated form, they showed possible inhibitory action on NorA, Tet(K), MsrA and MepA efflux pumps. They may also act in antibiotic potentiation. Further studies are needed to identify the mechanisms involved in antibiotic potentiation and efflux pump inhibitory action.

Exploring the Fluconazole-Resistance Modifying Activity and Potential Mechanism of Action of Fixed Oil from Caryocar coriaceum Wittm. (Caryocaraceae) against Candida Species.

The fixed oil from the inner mesocarp of Caryocar coriaceum Wittm. is used in the Chapada do Araripe region of Brazil for the treatment of genitourinary candidiasis. This study aimed to evaluate the chemical composition, antifungal activity, reduction of fungal virulence, and the preliminary toxicity of the fixed oil from the inner mesocarp of C. coriaceum tested against three Candida yeasts. The oil was characterized by gas chromatography (GC-MS and GC-FID). Antifungal activity was assessed using the serial microdilution method. Additionally, the potential of the oil as an enhancer of fluconazole action was tested at sub-inhibitory concentrations (MIC/8). The mechanism of action of C. coriaceum fixed oil was determined by evaluating the inhibition of morphological transition in Candida spp. The chemical composition of the fixed oil of C. coriaceum comprised both unsaturated and saturated fatty acids. Oleic (61 %) and palmitic (33 %) acids were the major constituents. Regarding its anti-Candida activity, the oil inhibited the growth of C. albicans (IC50 : 371 µg/mL) and C. tropicalis (IC50 : 830 µg/mL). Furthermore, the oil reversed the antifungal resistance of C. albicans and C. tropicalis, restoring the susceptibility to fluconazole and reducing their IC50 from 12.33 µg/mL and 362 µg/mL to 0.22 µg/mL and 13.93 µg/mL, respectively. The fixed oil of C. coriaceum completely inhibited the morphological transition of C. albicans and C. tropicalis at a concentration of 512 µg/mL, but exhibited limited low antifungal potential against C. krusei. The observed antifungal activity may be attributed to the overproduction of reactive oxygen species. Additionally, the oil showed no toxic effect on the Drosophila melanogaster in vivo model. The fixed oil from the inner mesocarp of C. coriaceum emerge as a strong candidate for the development of new pharmaceutical formulations to treat infections caused by Candida spp.

Chemical composition, antifungal, and anti-virulence action of the stem bark of Hancornia speciosa Gomes (Apocynaceae) against Candida spp.

ETHNOPHARMACOLOGICAL RELEVANCE: Hancornia speciosa Gomes is a fruit and medicinal species used for treating infectious diseases of the genitourinary system. However, its mechanism of action against microbes is still not fully understood. Infections in the genitourinary system caused by Candida spp. are associated with its fungal resistance and pathogenicity. New plant-derived compounds are an alternative to fight these Candida infections. AIM OF THE STUDY: The objective of this study was to evaluate the anti-Candida effects of extracts of the stem bark of H. speciosa. This research investigated the chemical composition of sulfuric ether (EEHS) and methanolic (MEHS) extracts, their drug-modifying action on fluconazole, and their anti-virulence action on the morphological transition of Candida species. MATERIALS AND METHODS: The extracts (EEHS and MEHS) of the stem bark of H. speciosa were chemically characterized via qualitative phytochemical screening and by liquid chromatography coupled with mass spectrometry (UPLC-MS-ESI-QTOF). The extracts were evaluated regarding their antifungal effects and fluconazole-modifying activity against Candida albicans, Candida krusei, and Candida tropicalis using the broth microdilution method. Additionally, the study evaluated the inhibition of fungal virulence in Candida species through morphological transition assays. RESULTS: The phytochemical screening revealed the presence of anthocyanidins, anthocyanins, aurones, catechins, chalcones, flavones, flavonols, flavanones, leucoanthocyanidins, tannins (condensed and pyrogallic), and xanthones in both extracts of the stem bark of H. speciosa. The UPLC-MS-ESI-QTOF analysis identified the same compounds in both extracts, predominating phenolic compounds. Some compounds were first time recorded in this species: gluconic acid, cinchonain IIb, cinchonain Ib isomer, and lariciresinol hexoside isomers. Most of the intrinsic antifungal activity was observed for the MEHS against C. krusei (IC50: 58.41 µg/mL). At subinhibitory concentrations (MC/8), the EEHS enhanced the action of fluconazole against all Candida strains. The MEHS exhibited greater efficacy than fluconazole inhibiting C. krusei growth. The EEHS completely inhibited hyphae appearance and reduced pseudohyphae formation in C. albicans. CONCLUSION: The stem bark of H. speciosa is a rich source of bioactive compounds, especially phenolic. Phenolic compounds can have important roles in fighting infectious diseases of the genitourinary system, such as candidiasis. The extracts of H. speciosa improved the action of the drug fluconazole against Candida species, inhibited hyphae appearance, and reduced pseudohyphae formation. The results of this study can support the development of new therapeutics against resistant strains of Candida.

Caryocar coriaceum fruits as a potential alternative to combat fungal and bacterial infections: In vitro evaluation of methanolic extracts.

Caryocar coriaceum, commonly known as 'pequi', is a medicinal species used traditionally for the herbal treatment of infectious and parasitic diseases in the Brazilian Northeast region. In this study, we investigated whether the fruits of C. coriaceum have bioactive chemical constituents against etiological agents of infectious diseases. The methanolic extract of the internal mesocarp of the fruits of C. coriaceum (MECC) was chemically analyzed and evaluated for its antimicrobial and drug-enhancing activity against multidrug-resistant pathogenic bacteria (Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus), and Candida spp. strains. The extract had flavones, flavonols, xanthones, catechins, and flavanones as major classes. A total of 11.26 mg GAE/g of phenolics, and 5.98 mg QE/g of flavonoids were found. No intrinsic antibacterial activity was observed; however, the extract was able to intensify the action of gentamicin and erythromycin against multi-resistant strains. The anti-Candida effect observed in this study was mainly due to the formation of reactive oxygen species. The extract was capable of causing damage to the plasmatic membrane of Candida tropicalis through pores formation. Our findings partially support the ethnopharmacological uses of the fruit pulp of C. coriaceum against infectious and parasitic diseases.

Chemical composition and antimicrobial potential of Acrocomia aculeata (Jacq.) Lodd. ex Mart. and Syagrus cearensis Noblick (Arecaceae).

This study aimed to evaluate the antibiotic effects of the fixed oils of Acrocomia aculeata (FOAA) and Syagrus cearenses (FOSC) against the bacterial strains and the fungi strains of the genus Candida spp. The method of serial microdilution using different concentrations was used for measuring the individual biological activity of the fixed oils. The fixed oil of A. aculeata showed the presence of oleic acid (24.36%), while the oil of S. cearensis displayed the content of myristic acid (18.29%), compounds detected in high concentration. The combination FOAA + Norfloxacin, and FOSC + Norfloxacin showed antibacterial activity against E. coli and S. aureus strains, demonstrating possible synergism and potentiation of the antibiotic action against multidrug-resistant strains. The combination FOAA + Fluconazole displayed a significant effect against Candida albicans (IC50 = 15.54), C. krusei (IC50 = 78.58), and C. tropicalis (IC50 = 1588 µg/mL). Regarding FOSC + Fluconazole, it was also observed their combined effect against the strains of C. albicans (IC50 = 3385 µg/mL), C. krusei (IC50 = 26.67 µg/mL), and C. tropicalis (IC50 = 1164 µg/mL). The findings of this study showed a significant synergism for both fixed oils tested when combined with the antibiotic.

LC-MS Analysis and Antifungal Activity of Turnera subulata Sm.

Fungi of the Candida genus are responsible for invasive candidiasis, which affects people all over the world and has high mortality rates. This is due to their virulence factors, which give them great resistance and pathogenicity. In addition, the emergence of multidrug-resistant strains makes it difficult to treat these infections. In this way, natural products have emerged as an alternative to standard drugs, where plants known for their medicinal properties such as Turnera subulata become attractive to research. The present work aimed to analyze the ethanol extract of Turnera subulata leaves against standard strains of Candida albicans, Candida krusei and Candida tropicalis using broth microdilution techniques. The identification of the compounds in T. subulata leaves by LC-MS revealed the presence of a wide variety of substances such as carboxylic acids and terpenes, with flavonoids and fatty acids being more evident. The antifungal assays showed that the extract was not able to inhibit the growth of the tested strains at concentrations with a clinical relevance. However, at higher concentrations, it was able to inhibit the fungal dimorphism of C. albicans and C. tropicalis. It is possible that the T. subulata extract has potential as an inhibitor of fungal virulence factors without affecting the cell viability. Further research should be carried out in order to assess its inhibitory potential for other fungal virulence factors.

Chemical Composition and Antimicrobial Potential of Essential Oil of Acritopappus confertus (Gardner) R.M.King & H.Rob. (Asteraceae).

Microbial resistance has become a worrying problem in recent decades after the abusive use of antibiotics causing the selection of resistant microorganisms. In order to circumvent such resistance, researchers have invested efforts in the search for promising natural substances, such as essential oils. Thus, the objective of this work was to determine the chemical composition of the essential oil of Acritopappus confertus leaves, to evaluate its intrinsic effect and its effects in combination with drugs against pathogenic fungi and bacteria, in addition to verifying the inhibition of virulence in Candida strains. To this end, the oil was verified by gas chromatography coupled with mass spectrometry (GC/MS). Candida strains were used for antifungal assays by means of the serial microdilution technique, in order to determine the average inhibitory concentration (IC50), and for the modification assays, sub-inhibitory concentrations (MIC/8) were used. Finally, the natural product's ability to inhibit the formation of filamentous structures was evaluated. In antibacterial tests, the MIC of the oil against strains of Staphylococcus aureus and Escherichia coli and its modifying effects in association with gentamicin, erythromycin, and norfloxacin were determined. The major constituent of the essential oil was the monoterpene myrcene (54.71%). The results show that the essential oil has an antifungal effect, with C. albicans strains being the most susceptible. Furthermore, the oil can potentiate the effect of fluconazole against strains of C. tropicalis and C. albicans. Regarding its effect on micromorphology, the oil was also able to inhibit the filaments in all strains. In combination with antibiotics, the oil potentiated the drug's action by reducing the MIC against E. coli and S. aureus. It can be concluded that the essential oil of A. confertus has potential against pathogenic fungi and bacteria, making it a target for the development of an antimicrobial drug.

Caryocar coriaceum Wittm. (Caryocaraceae): Botany, Ethnomedicinal Uses, Biological Activities, Phytochemistry, Extractivism and Conservation Needs.

Caryocar coriaceum is an endemic tree of Brazil, occurring mainly in the northeast region in the Cerrado environment. The species, popularly known as "pequi", produces fruits that are used in the manufacture of oil for food and medicinal purposes. This work reviewed studies conducted with the species, highlighting its ethnomedicinal use, its pharmacological potential, including its chemical constituents, and its cultural and socioeconomic importance. Information was obtained through the main scientific research platforms. The keyword "Caryocar coriaceum" was used as the main index for searching the following platforms: PubMed®, PubMed Central®, SciElo, Scopus® and Web of ScienceTM. The compiled papers demonstrate that C. coriaceum has great medicinal, economic and cultural importance for northeastern Brazil. Popularly, the fruits of C. coriaceum are used to treat broncho-pulmonary diseases (bronchitis, colds and flu). The fixed oil is widely used to relieve pain from various causes in the treatment of inflammation, flu, eczema, burns, fever, rickets, indigestion, heart murmurs, fatigue and erectile dysfunction. Some of these uses are corroborated by pharmacological trials, which have demonstrated the antioxidant, healing, anti-inflammatory, gastroprotective, antinociceptive and antimicrobial properties of the species. Chemically, fatty acids and phenolic compounds are the main constituents recorded for the species. Due to its medicinal properties, the fruits and oil of C. coriaceum have a high commercial demand and are one of the main forms of subsistence activities for local populations. On the other hand, the extractive practice of the fruits, associated with anthropic factors and its physiological nature, makes the species threatened with extinction. Thus, public management policies are highly necessary in order to avoid its extinction.

The Genus Miconia Ruiz & Pav. (Melastomataceae): Ethnomedicinal Uses, Pharmacology, and Phytochemistry.

Species of the genus Miconia are used in traditional medicine for the treatment of diseases, such as pain, throat infections, fever, and cold, and they used as depuratives, diuretics, and sedatives. This work reviewed studies carried out with Miconia species, highlighting its ethnomedicinal uses and pharmacological and phytochemical potential. This information was collected in the main platforms of scientific research (PubMed, Scopus, and Web of Science). Our findings show that some of the traditional uses of Miconia are corroborated by biological and/or pharmacological assays, which demonstrated, among other properties, anti-inflammatory, analgesic, antimutagenic, antiparasitic, antioxidant, cytotoxic, and antimicrobial activities. A total of 148 chemical compounds were identified in Miconia species, with phenolic compounds being the main constituents found in the species of this genus. Such phytochemical investigations have demonstrated the potential of species belonging to this genus as a source of bioactive substances, thus reinforcing their medicinal and pharmacological importance.

Phytochemical Analysis, Antibacterial Activity and Modulating Effect of Essential Oil from Syzygium cumini (L.) Skeels.

One of the main global problems that affect human health is the development of bacterial resistance to different drugs. As a result, the growing number of multidrug-resistant pathogens has contributed to an increase in resistant infections and represents a public health problem. The present work seeks to investigate the chemical composition and antibacterial activity of the essential oil of Syzygium cumini leaves. To identify its chemical composition, gas chromatography coupled to mass spectrometry was used. The antibacterial activity test was performed with the standard strains Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 25853 and Staphylococcus aureus ATCC 25923 and multidrug-resistant clinical isolates E. coli 06, P. aeruginosa 24 and S. aureus 10. The minimum inhibitory concentration (MIC) was determined by serial microdilution as well as the verification of the modulating effect of the antibiotic effect. In this test, the oil was used in a subinhibitory concentration. The test reading was performed after 24 h of incubation at 37 °C. The results show that the major chemical constituent is α-pinene (53.21%). The oil showed moderate activity against E. coli ATCC 25922, with the MIC of 512 µg/mL; there was no activity against the other strains. The oil potentiated the effect of antibiotics demonstrating possible synergism when associated with gentamicin, erythromycin and norfloxacin against E. coli 06 and S. aureus 10.

Traditional Uses, Phytochemistry, and Bioactivities of Mesosphaerum suaveolens (L.) Kuntze.

Mesosphaerum suaveolens (L.) Kuntze is a species widely used traditionally in the treatment of ailments, such as stomach pain, hemorrhoids, cough, verminosis, ulcer, liver disease, fever, influenza, nasal congestion, and inflammation. This review aims to provide a survey of available information on seven international electronic databases (Google Scholar, Medline, ResearchGate, Web of Science, Scopus, Science Direct, and PubMed) about botanical aspects, traditional uses, phytochemistry, and biological activities of M. suaveolens. Mesosphaerum suaveolens is a tropical America native species, but it can be found in several parts of the world as a ruderal plant. The species is the most studied species of the genus Lamiaceae due its phytochemical aspect, especially regarding the chemical composition of its essential oil. Besides the essential oils, M. suaveolens is a source of numerous secondary compounds such as triterpenes, diterpenes, and phenolic compounds, which are related to its biological activities, such as allelopathic, antibacterial, antifungal, insecticidal, and larvicidal activities as described in the literature.

HPLC-DAD analysis and antimicrobial activities of Spondias mombin L. (Anacardiaceae).

Spondias mombin is used in the folk medicine for the treatment of diarrhea and dysentery, indicating that extracts obtained from this species may present pharmacological activities against pathogenic microorganisms. The purpose of this work was to investigate the chemical composition and evaluate the antimicrobial activity of extracts obtained from the leaves (aqueous) and bark (hydroethanolic) of S. mombin both as single treatments and in combination with conventional drugs. Following a qualitative chemical prospection, the extracts were analyzed by HPLC-DAD. The antimicrobial activities were evaluated by microdilution. The combined activity of drugs and extracts was verified by adding a subinhibitory concentration of the extract in the presence of variable drug concentrations. The Minimum Fungicidal Concentration (MFC) was determined by a subculture of the microdilution test, while the effect of the in vitro treatments on morphological transition was analyzed by subculture in moist chambers. While the qualitative analysis detected the presence of phenols and flavonoids, the HPLC analysis identified quercetin, caffeic acid, and catechin as major components in the leaf extract, whereas kaempferol and quercetin were found as major compounds in the bark extract. The extracts showed effective antibacterial activities only against the Gram-negative strains. With regard to the combined activity, the leaf extract potentiated the action of gentamicin and imipenem (against Staphylococcus aureus), while the bark extract potentiated the effect of norfloxacin (against S. aureus), imipenem (against Escherichia coli), and norfloxacin (against Pseudomonas aeruginosa). A more significant antifungal (fungistatic) effect was achieved with the bark extract (even though at high concentrations), which further enhanced the activity of fluconazole. The extracts also inhibited the emission of filaments by Candida albicans and Candida tropicalis. Together, these findings suggest that that the extract constituents may act by favoring the permeability of microbial cells to conventional drugs, as well as by affecting virulence mechanisms in Candida strains.

Chemical Constituents and Biological Activities of Croton heliotropiifolius Kunth.

Croton heliotropiifolius Kunth (Euphorbiaceae), whose occurrence has already been registered in the most varied Brazilian biomes, is commonly found in the Chapada do Araripe, Ceará. The species is traditionally used to treat fungal, parasitic, and degenerative diseases. This study investigated the chemical composition and pharmacological potential (antioxidant, antifungal, antiparasitic, and cytotoxic) of an aqueous extract obtained from the roots of C. heliotropiifolius. Following a qualitative phytochemical screening, the chemical constituents were identified by ultra-efficiency liquid chromatography coupled witha quadrupole/time-of-flight system (UPLC-QTOF). The antioxidant potential was verified by thin-layer chromatography (TLC). The direct and combined antifungal activity of the extract against opportunistic Candida strains was investigated using the microdilution method. The minimal fungicidal concentration (MFC) was determined by subculture, while the modulation of the morphological transition (fungal virulence) was evaluated by light microscopy. The in vitro antiparasitic activity was analyzed using epimastigotes of Trypanosoma cruzi and promastigotes of Leishmania braziliensis and Leishmania infantum, while cytotoxicity was determined in cultures of mouse fibroblasts. The phytochemical analysis identified the presence of acids, terpenes, flavonoids, lignans, and alkaloids. Among these constituents, the presence of polar and non-polar phenolic compounds with known antioxidant action was highlighted. While the extract showed clinically ineffective antifungal effects, it could enhance the effectiveness of fluconazole, in addition to inhibiting the morphological transition associated with increased virulence in Candida strains. Although the extract showed low cytotoxicity against fibroblasts, it also had weak antiparasitic effects. In conclusion, Croton heliotropiifolius is a source of natural products with antifungal and antioxidant potential.

In vitro Antibiotic and Modulatory Activity of Mesosphaerum suaveolens (L.) Kuntze against Candida strains.

The emergence of fungal resistance to commercial drugs has been a major problem for the WHO. In this context, research with natural products is promising in the discovery of new active substances. Thus, this work evaluated the antifungal effect of a medicinal plant (i.e., Mesosphaerum suaveolens) against strains of the genus Candida, tested the combined effect with the drug fluconazole, and, finally, determined the phenolic constituents present in the species. Initially, aqueous extracts of leaves (AELMs) and aerial parts (AEAPMs) of the species were prepared. For microbiological assays, the minimum fungicidal concentration was determined by broth microdilution, and the combined effect of fluconazole extracts were verified by sub-inhibitory microdilution concentrations (CFM/8) followed by spectrophotometric readings which were used to determine the IC50. HPLC detected the presence of flavonoids and phenolic acids, detecting eight compounds present in the samples of which caffeic acid and quercetin were major components. The AELMs modulated fluconazole activity since it decreased fluconazole's IC50 from 7.8 µg/mL to an IC50 of 4.7 µg/mL (CA LM 77) and from 28.8 µg/mL to 18.26 µg/mL (CA INCQS 40006) for the C. albicans strains. The AEAPMs were able to potentiate the effect of fluconazole more effectively than the AELMs. Such an effect was significant for the 16 µg/mL concentration for CA LM 77 and 32 µg/mL for CA INCQS 40006. The AEAPMs as well as the AELMs presented clinically relevant activities for C. tropicalis strains. For the C. tropicalis LM 23 strain, the AEPMs obtained an IC50 of 25 µg/mL and the AELMs an IC50 of 359.9 µg/mL.

Chemical composition, antimicrobial, modulator and antioxidant activity of essential oil of Dysphania ambrosioides (L.) Mosyakin & Clemants.

The oil presented the α-Terpinene as the major compound with 54.09% presence. Antibacterial activity demonstrated significant MIC against Staphylococcus aureus (256 µg/mL) and moderate against Pseudomonas aeruginosa (512 µg/mL). The modulating effect of antibiotics was significant against P. aeruginosa potentiating the effect of all the antibiotics tested. The IC50 observed for CT LM 23 was clinically relevant (19.3 µg/mL), similar to that obtained for CA INCQS 40006 (25.2 µg/mL). The combined effect with fluconazole also showed significant results, 0.1 and 22.7 µg/mL, for CT LM 23 and CA INCQS 40006, respectively. For CA LM 77 the IC50 was 101.9 µg/mL and for CT INCQS 40042 a value of 53.3 µg/mL. Regarding the modulation, both were considered of clinical relevance, 3.3 and 6.4 µg/mL. OEDA has low antioxidant activity (>1024 µg/mL). Therefore, the popular use against infections was corroborated by this work.

Mesosphaerum suaveolens (L. ) Kuntze (bamburral) planta medicinal com potencial antioxidante e rica em polifenóis / Mesosphaerum suaveolens (L.) Kuntze (pignut) a medicinal plant with antioxidant potential and abundant polyphenols

Introducción: Mesosphaerum suaveolens (L.) Kuntze (Lamiaceae), planta conocida como bamburral, se utiliza en la medicina popular; sin embargo, poco se sabe de sus componentes químicos, sus efectos tóxicos y sus propiedades terapéuticas. Objetivo: Caracterizar los compuestos polifenólicos de los extractos de M. suaveolens, así como su actividad antioxidante y tóxica. Métodos: Se analizaron los componentes químicos de los extractos acuoso y etanólico de las hojas frescas mediante HPLC-DAD, la actividad antioxidante de los extractos en diversas concentraciones (entre 4 y 1024 µg/mL) frente al radical libre DPPH acompañado de un control positivo (ácido ascórbico) y se evaluó la actividad tóxica de los extractos contra Artemia salina. Resultados: Los resultados indican que los extractos acuoso y etanólico tienen como compuesto mayoritario el ácido cafeico (13.27 y 15.09 mg/g, respectivamente). Los extractos posee elevada actividad antioxidante con concentración de inhibición al 50 % (IC50) de 7.06 µg/mL para el extracto etanólico, 20.32 µg/mL para el acuoso y 6.69 µg/mL para el ácido ascórbico. Ninguno de los extractos presentó toxicidad con el método analizado (p> 0,05). Conclusiones: Por lo tanto, se demuestra que los extractos no presentan toxicidad, pero presentan una gran capacidad para eliminar los radicales libres en el organismo y son una fuente natural para fabricar medicamentos.

Introduction: The species Mesosphaerum suaveolens (L.) Kuntze (Lamiaceae), commonly known as pignut, is used in folk medicine. However, little information is available about its chemical components, toxic effects and therapeutic properties. Objective: Characterize the polyphenolic compounds contained in M. suaveolens extracts, as well as their antioxidant and toxic activity. Methods: The chemical components of aqueous and ethanolic fresh leaf extracts were analyzed by HPLC-DAD. Evaluation was performed of the antioxidant activity of the extracts against DPPH free radical at various concentrations (between 4 and 1 1024 µg/ml) accompanied by a positive control (ascorbic acid), as well as their toxic activity against Artemia salina. Results: Caffeic acid is the most abundant compound in the aqueous and the ethanolic extracts (13.27 and 15.09 mg/g, respectively). The extracts display high antioxidant activity with a 50% inhibition concentration (IC50) of 7.06 µg/ml for the ethanolic extract, 20.32 µg/ml for the aqueous extract and 6.69 µg/ml for ascorbic acid. Neither extract displayed toxicity by the method used (p> 0.05). Conclusions: It was found that the extracts do not display any toxicity, are capable of eliminating free radicals from the body and are a natural source of raw materials for drug manufacture.

Estudo químico-biológico do óleo essencial de Lantana montevidensis (chumbinho) (Spreng.) Briq. (Verbenaceae) contra Drosophila melanogaster / Chemical-biological study of the essential oil of Lantana montevidensis (chumbinho) (Spreng.) Briq. (Verbenaceae) against Drosophila melanogaster

Introdução: O uso de plantas como inseticidas podem substituir muitos produtos sintéticos por apresentarem baixa toxicidade para os animais e biodegradação no ambiente. A espécie Lantana montevidensis (Spreng.) Briq. (Verbenaceae), chumbinho, é um vegetal subarbustivo rico de compostos secundários para a sua defesa. O modelo experimental com Drosophila melanogaster tem sido usada para estudos, por apresentar vantagens, pois tem fácil manuseio e rápida taxa de reprodução. Objetivo: Avaliar a composição química e efeito inseticida do óleo essencial (OE) de L. montevidensis contra D. melanogaster. Metodos: O OE das folhas secas provenientes do Crato-CE, Brasil, foi extraído por hidrodestilação e foi analisado por CG/EMS para identificação dos constituintes. No ensaio foi avaliada a mortalidade e geotaxia negativa das moscas, em que elas foram expostas a diferentes concentrações do OE (3-30,5 µg/mL do óleo essencial/ar). Um total de vinte moscas adultas foram submetidas à diapausa por meio de resfriamento e em seguidas foram colocadas em frascos de 300 mL, cuja parte inferior havia papel filtro impregnado com 1 mL de sacarose a 20 por cento em água destilada. Na parte superior (tampa) foi afixado um papel filtro para a aplicação do produto a ser testado, nesse caso o OELM. As leituras foram realizadas a cada 3, 6, 12 e 24 h. Resultados: Os resultados mostraram que o OE apresentou o ß-Cariofileno (34,96 por cento), o Germacreno D (25,49 por cento) e o Biciclogermacreno (9, 78 por cento) como componentes majoritários, no ensaio inseticida houve uma CL50 na concentração de 15,14 µg/mL em 3 h de exposição, e houve um efeito significativo nos danos do aparelho locomotor das moscas.mConclusão: Este estudo fornece evidências que esse OE apresenta-se como um potencial bioinseticida(AU)

Introducción: el uso de plantas como insecticidas puede sustituir muchos productos sintéticos porque tienen baja toxicidad para los animales y son fácilmente biodegradables en el medio ambiente. La especie Lantana montevidensis (Spreng.) Briq. (Verbenaceae), Chumbinho, es una planta sub-arbustiva rica en metabolitos secundarios para su defensa. El modelo experimental en Drosophila melanogaster se ha utilizado para varios tipos de estudios, presenta algunas ventajas como: fácil manejo y tasa de reproducción rápida. Objetivo: evaluar la composición química y el efecto insecticida de aceite esencial (OE) de L. montevidensis contra las D. melanogaster. Métodos: el OE de hojas secas del Crato-CE, Brasil, se extrajo por hidrodestilación y se analizó por GC/EMS para identificar los constituyentes. En el test se evaluó la mortalidad y geotaxia negativas de las moscas, donde fueron expuestos a diferentes concentraciones de OE (3-30,5 µg/mL de aceite esencial/aire). Un total de veinte moscas adultas se sometieron a diapausa por enfriamiento y seguido se colocaron en botellas de 300 mL, la parte inferior contenido papel de filtro impregnado con 1 mL de 20 por ciento de sacarosa en agua destilada. En la parte superior (tapa) se haya colocado un papel de filtro para la aplicación del producto a ensayar, la OELM. Las lecturas se realizaron cada 3, 6, 12 y 24 h. Resultados: Los resultados mostraron que el OE presenta la ß-cariofileno (34,96 por ciento), el germacreno D (25,49 por ciento) y bicyclogermacrene (9,78 por ciento) como componentes principales en el ensayo insecticida había una CL50 de la concentración de 15,14 µg/mL en 3 h de exposición, y había un un efecto significativo en el daño del aparato locomotor de las moscas. Conclusión: este estudio proporciona evidencia de que este OE o se presenta como un biopesticida potencial(AU

Introduction: The use of plants as insecticides may be an alternative to many synthetic products because their toxicity to animals is low and they are easily biodegradable in the environment. The species Lantana montevidensis (Spreng.) Briq. (Verbenaceae), chumbinho, is a subshrub rich in secondary metabolites it uses for its own defence. The experimental model for Drosophila melanogaster has been used in several types of studies. Some of its advantages are its easy management and its fast rate of reproduction. Objective: Evaluate the chemical composition and insecticidal effect of the essential oil (EO) of L. montevidensis against D. melanogaster. Method: EO of dry leaves from Crato-CE, Brazil, was extracted by hydrodistillation and analyzed by GC/EMS to identify its constituents. As part of the test, evaluation was conducted or the mortality and negative geotaxis of the flies, to attain which they were exposed to different concentrations of the EO (3-30.5 µg/mL essential oil/air). A total 20 adult flies were subjected to cold diapause and placed in 300 mL bottles with filter paper in their lower section impregnated with 1 mL of 20 percent saccharose in distilled water. Filter paper was also attached to the upper section (lid) to apply the test product OELM. Readings were taken every 3, 6, 12 and 24 h. Results: Results showed that the principal components of the EO are ?-caryophyllene (34.96 percent), germacrene D (25.49 percent) and bicyclogermacrene (9.78 percent). In the insecticide test there was a CL50 for the concentration of 15.14 µg/ml in 3 h exposure, and significant damage to the locomotor system of the flies. Conclusion: The study provides evidence that the EO analyzed is a potential biopesticide(AU)

Estudo químico-biológico do óleo essencial de Lantana montevidensis (chumbinho) (Spreng.) Briq. (Verbenaceae) contra Drosophila melanogaster / Estudio químico-biológico del aceite esencial de Lantana montevidensis (Chumbinho) (Spreng.) Briq. (Verbenaceae) contra Drosophila melanogaster / Chemical-biological study of the essential oil of Lantana montevidensis (chumbinho) (Spreng.) Briq. (Verbenaceae) against Drosophila melanogaster

Introdução: O uso de plantas como inseticidas podem substituir muitos produtos sintéticos por apresentarem baixa toxicidade para os animais e biodegradação no ambiente. A espécie Lantana montevidensis (Spreng.) Briq. (Verbenaceae), chumbinho, é um vegetal subarbustivo rico de compostos secundários para a sua defesa. O modelo experimental com Drosophila melanogaster tem sido usada para estudos, por apresentar vantagens, pois tem fácil manuseio e rápida taxa de reprodução. Objetivo: Avaliar a composição química e efeito inseticida do óleo essencial (OE) de L. montevidensis contra D. melanogaster. Metodos: O OE das folhas secas provenientes do Crato-CE, Brasil, foi extraído por hidrodestilação e foi analisado por CG/EMS para identificação dos constituintes. No ensaio foi avaliada a mortalidade e geotaxia negativa das moscas, em que elas foram expostas a diferentes concentrações do OE (3-30,5 µg/mL do óleo essencial/ar). Um total de vinte moscas adultas foram submetidas à diapausa por meio de resfriamento e em seguidas foram colocadas em frascos de 300 mL, cuja parte inferior havia papel filtro impregnado com 1 mL de sacarose a 20 por cento em água destilada. Na parte superior (tampa) foi afixado um papel filtro para a aplicação do produto a ser testado, nesse caso o OELM. As leituras foram realizadas a cada 3, 6, 12 e 24 h. Resultados: Os resultados mostraram que o OE apresentou o ß-Cariofileno (34,96 por cento), o Germacreno D (25,49 por cento) e o Biciclogermacreno (9, 78 por cento) como componentes majoritários, no ensaio inseticida houve uma CL50 na concentração de 15,14 µg/mL em 3 h de exposição, e houve um efeito significativo nos danos do aparelho locomotor das moscas.mConclusão: Este estudo fornece evidências que esse OE apresenta-se como um potencial bioinseticida(AU)

Introducción: el uso de plantas como insecticidas puede sustituir muchos productos sintéticos porque tienen baja toxicidad para los animales y son fácilmente biodegradables en el medio ambiente. La especie Lantana montevidensis (Spreng.) Briq. (Verbenaceae), Chumbinho, es una planta sub-arbustiva rica en metabolitos secundarios para su defensa. El modelo experimental en Drosophila melanogaster se ha utilizado para varios tipos de estudios, presenta algunas ventajas como: fácil manejo y tasa de reproducción rápida. Objetivo: evaluar la composición química y el efecto insecticida de aceite esencial (OE) de L. montevidensis contra las D. melanogaster. Métodos: el OE de hojas secas del Crato-CE, Brasil, se extrajo por hidrodestilación y se analizó por GC/EMS para identificar los constituyentes. En el test se evaluó la mortalidad y geotaxia negativas de las moscas, donde fueron expuestos a diferentes concentraciones de OE (3-30,5 µg/mL de aceite esencial/aire). Un total de veinte moscas adultas se sometieron a diapausa por enfriamiento y seguido se colocaron en botellas de 300 mL, la parte inferior contenido papel de filtro impregnado con 1 mL de 20 por ciento de sacarosa en agua destilada. En la parte superior (tapa) se haya colocado un papel de filtro para la aplicación del producto a ensayar, la OELM. Las lecturas se realizaron cada 3, 6, 12 y 24 h. Resultados: Los resultados mostraron que el OE presenta la ß-cariofileno (34,96 por ciento), el germacreno D (25,49 por ciento) y bicyclogermacrene (9,78 por ciento) como componentes principales en el ensayo insecticida había una CL50 de la concentración de 15,14 µg/mL en 3 h de exposición, y había un un efecto significativo en el daño del aparato locomotor de las moscas. Conclusión: este estudio proporciona evidencia de que este OE o se presenta como un biopesticida potencial(AU

Introduction: The use of plants as insecticides may be an alternative to many synthetic products because their toxicity to animals is low and they are easily biodegradable in the environment. The species Lantana montevidensis (Spreng.) Briq. (Verbenaceae), chumbinho, is a subshrub rich in secondary metabolites it uses for its own defence. The experimental model for Drosophila melanogaster has been used in several types of studies. Some of its advantages are its easy management and its fast rate of reproduction. Objective: Evaluate the chemical composition and insecticidal effect of the essential oil (EO) of L. montevidensis against D. melanogaster. Method: EO of dry leaves from Crato-CE, Brazil, was extracted by hydrodistillation and analyzed by GC/EMS to identify its constituents. As part of the test, evaluation was conducted or the mortality and negative geotaxis of the flies, to attain which they were exposed to different concentrations of the EO (3-30.5 µg/mL essential oil/air). A total 20 adult flies were subjected to cold diapause and placed in 300 mL bottles with filter paper in their lower section impregnated with 1 mL of 20 percent saccharose in distilled water. Filter paper was also attached to the upper section (lid) to apply the test product OELM. Readings were taken every 3, 6, 12 and 24 h. Results: Results showed that the principal components of the EO are ?-caryophyllene (34.96 percent), germacrene D (25.49 percent) and bicyclogermacrene (9.78 percent). In the insecticide test there was a CL50 for the concentration of 15.14 µg/ml in 3 h exposure, and significant damage to the locomotor system of the flies. Conclusion: The study provides evidence that the EO analyzed is a potential biopesticide(AU)