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a Universidade Regional do Cariri, URCA, Cel Ant^onio Luis, 1161, 63105-000, Pimenta, Crato, CE, Brazil b Universidade Federal do Paran a, UFPR, XV de Novembro, 1299, 80.060-000, Centro, Curitiba, PR, Brazil c Universidade Regional de Blumenau, FURB, Ant^onio da Veiga, 140, 89030-903, Itoupava Seca, Blumenau, SC, Brazil d Laborat orio de investiga¸c~ao em Gen etica e Hematologia Translacional, Instituto Gon¸calo Moniz (IGM), Funda¸c~ao Oswaldo Cruz (FIOCRUZ), Salvador, BA 40296- 710, Brazil e Centro Universit ario Doutor Le~ao Sampaio (Unile~ao), Av. Maria Leticia Leite Pereira s/n, Lagoa Seca, Juazeiro do Norte, Brazil

Achyrocline satureioides (Lam.) DC is a plant in the Asteraceae family that is commonly known as macela or marcela. It has antidiarrheal, antispasmodic, analgesic, anti-inflammatory and antimicrobial properties. The species Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli are of great clinical importance, thus more evidence on the discovery of new compounds from plant species is required. The aim of this study was to evaluate the phytochemical profile and in vitro antimicrobial potential of essential oils from A. satureioides. A Minimal Inhibitory Concentration (MIC) test was performed using microdilution, and the chemical composition of the essential oil was analyzed using Gas Chromatography coupled to Mass spectrometry (GC / MS). Using the GC / MS analysis, we identified alpha-pinene and (E)-cariophilene as major phytoconstituents. We observed synergisms when the essential oil was combined with gentamicin and ampicillin against the S. aureus strain, as well as against E. coli when combined with gentamicin and norfloxacin. The results were promising, but further research is needed to assess the toxicity of A. satureioides oil and its potential for therapeutic use in humans.

Infectious diseases caused by multidrug-resistant microorganisms has increased in the last years. Piper species have been reported as a natural source of phytochemicals that can help in combating fungal and bacterial infections. This study had as objectives characterize the chemical composition of the essential oil from Piper caldense (EOPC), evaluate its potential antimicrobial activity, and investigate the synergistic effect with Norfloxacin against multidrug-resistant S. aureus overproducing efflux pumps, as well as, verify the EOPC ability to inhibit the Candida albicans filamentation. EOPC was extracted by hydrodistillation, and the chemical constituents were identified by gas chromatography, allowing the identification of 24 compounds (91.9%) classified as hydrocarbon sesquiterpenes (49.6%) and oxygenated sesquiterpenes (39.5%). Antimicrobial tests were performed using a 96-well plate microdilution method against C. albicans ATCC 10231, Escherichia coli ATCC 25922 and Staphylococcus aureus ATCC 25923 standard strains, as well as against multidrug-resistant strains S. aureus SA1199B (overexpressing norA gene), S. aureus K2068 (overexpressing mepA gene) and S. aureus K4100 (overexpressing qacC gene). The oil showed activity against C. albicans ATCC 10231 (≥ 512 µg/mL) and was able to inhibit hyphae formation, an important mechanism of virulence of C. albicans. On the other hand, EOPC was inactive against all bacterial strains tested (≤ 1,024 µg mL). However, when combined with Norfloxacin at subinhibitory concentration EOPC reduced the Norfloxacin and Ethidium bromide MIC values against S. aureus strains SA1199B, K2068 and K4100. These results indicate that EOPC is a source of phytochemicals acting as NorA, MepA and QacC inhibitors.

This study aimed to investigate the chemical composition and antifungal potential of the essential oil of Baccharis trimera (Less.) DC. against Candida strains. The half maximal inhibitory concentration (IC50) was assessed by the microdilution method using the essential oil at a concentration range of 8192 to 8 μg/mL. The minimum fungicide concentration (MFC) was determined by subculture in solid medium. The ability of the essential oil to modulate the activity of antifungals was determined in wells treated simultaneously with the oil at a subinhibitory concentration (MFC/16) and fluconazole (FCZ). The fungal morphology was analyzed by microscopy. Gas chromatography coupled with mass spectrometry (GC/MS) was used to identify the chemical composition. The essential oil presented an CI50 of 11.24 and 1.45 μg/mL, which was found to potentiate the effect of FCZ against Candida albicans. On the other hand, this combined treatment resulted in antagonism against Candida tropicalis and no evident modulation against Candida krusei was observed. The essential oil significantly inhibited hyphae growth. However, with a MFC ≥ 16,384 μg/mL, it is assumed that it has a fungistatic action. The antifungal properties demonstrated in this study might be related to the presence of sesquiterpenes and monoterpenes, and the interaction between them. In conclusion, Baccharis trimera showed promising anti-Candida effects, in addition to potentiating the activity of FCZ against Candida albicans, affecting its morphological transition. Therefore, this species constitutes a source of chemical compounds with the potential to be used in the combat of fungal infections.

The objective of this study was to determine the chemical profile and to evaluate the antibacterial activity of the essential oils of Piper species and modulation of the antibiotic activity, using the microdilution method to determine the minimum inhibitory concentration. The chemical components were characterized by gas chromatography coupled to mass spectrometry, which revealed β-copaen-4-α-ol (31.38%), spathulenol (25.92%), and germacrene B (21.53%) as major constituents of the essential oils of Piper arboreum, Piper aduncum, and Piper gaudichaudianum, respectively. The essential oils analyzed in this study did not present a clinically relevant activity against standard and multiresistant Escherichia coli. However, in the case of multiresistant Staphylococcus aureus, there was a significant activity, corroborating with reports in the literature, where Gram-positive bacteria are more susceptible to antimicrobial activity. The essential oils modulated the effect of the antibiotics norfloxacin and gentamicin, having on the latter greater modulating effect; however, for erythromycin, no statistically significant effect was observed. In conclusion, the results obtained in this study demonstrated that the essential oils of the analyzed Piper species present an inhibitory effect against S. aureus and modulate antibiotic activity, most of which presents synergistic activity.

Background: Aloysia gratissima (Verbenaceae), popularly known as bee-brush or whitebrush, has been widely used in Brazilian folk medicine as analgesic, expectorant and antimicrobial. Phytochemical studies have identified β-caryophyllene as one of the major components of the essential oil of this plant. This bioactive sesquiterpene has been shown to have anti-inflammatory and antibacterial activities. Purpose: The present study aimed to characterize the chemical profile and evaluate the antibacterial and antibiotic-enhancing activities of the essential oil obtained from Aloysia gratíssima (EOAG) and β-caryophyllene. Methods: The phytochemical analysis was performed by gas chromatography coupled to mass spectrometry (GC-MS). The antibacterial activity against Pseudomonas aeruginosa 24, Staphylococcus aureus 10, and Escherichia coli 06 was assessed by determining the minimum inhibitory concentration (MIC) using the broth microdilution method. The potentiation of the antibiotic activity by the EOAG and the β-caryophyllene was performed using the MIC evaluation of the antibiotic alone or in association with the essential oil and its main compound. To evaluate the minimum reduction of the drug concentration necessary, the Dose Reduction Index (DRI) was calculated. Results: A reduction in the MIC of the antibiotics against strains treated simultaneously with the essential oil or β-caryophyllene was observed. The GC-MS analysis of the EOAG identified 30 compounds, including β-caryophyllene as the major component. Both OEAG and β-caryophyllene presented antibacterial activity against S. aureus, in addition to potentiating the action of norfloxacin against S. aureus, P. aeruginosa, and E. coli. Conclusions: These substances also reversed the antibiotic resistance to gentamicin and erythromycin against of S. aureus and P. aeruginosa, respectively.

In a recent study, our research group demonstrated that the essential oil of Ocotea odorifera (EOOO) and its major compound safrole potentiated the action fluoroquinolones, modulating bacterial resistance possibly due to direct inhibition of efflux pumps. Thus, in the present study, we investigated whether these treatments could enhance the activity of gentamicin and erythromycin against multidrug-resistant (MDR) bacteria. The EOOO was extracted by hydrodistillation, and the phytochemical analysis was performed by gas chromatography coupled to mass spectrometry (GC–MS). The antibiotic-enhancing effect of the EOOO and safrole against MDR strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa was analyzed by the broth microdilution method. The chemical analysis confirmed the presence of safrole as a major component among the 16 compounds identified in the EOOO. Both the essential oil and the isolated compound showed clinically relevant antibacterial activities against S. aureus. Regarding the modulation of antibiotic resistance, the EOOO was found to enhance the activity of erythromycin against the strains of P. aeruginosa and S. aureus, as well as improving the action of gentamicin against S. aureus. On the other hand, safrole potentiated the activity of gentamicin against the S. aureus strain alone. It is concluded, therefore, that the EOOO and safrole can enhance the activity of macrolides and aminoglycosides, and as such are useful in the development of therapeutic tools to combat bacterial resistance against these classes of antibiotics.

The Atlantic Forest is regarded a rich source of aromatic plants with a broad spectrum of biological properties. The leaves of seven Piper species were collected from the Atlantic Forest domain in the coastal region of Paraná state in winter (W) and spring (S). The volatile oils were extracted from the leaves through hydrodistillation method. The volatile oils were characterized by means of GC-FID and GC-MS. Sesquiterpenes were among the major compounds in all species studied, with many dozens of representatives. However, very low concentrations of monoterpenes were observed; α-pinene in Piper mosenii and P. cernuum, δ-3-carene in P. rivinoides, camphene and β-pinene in P. cernuum are exceptions. The arylpropanoides myristicine and elemicin were found in considerable amount in P. diospyrifolium (26.2%/S) and P. mosenii (16.4%/W), respectively. These oils were also screened for inhibitory activities against acetylcholinesterase (AChE) and α-glucosidase (AG). For AChE the most active samples were P. diospyrifolium, P. aduncum and P. cernuum, with inhibiting level > 93%. For the less sensitive AG, the most promising candidates were P. diospyrifolium and P. mosenii, with inhibiting level > 65%. These results highlight the importance of native plants as renewable source of new inhibitors for AChE and AG. Further investigation is required to identify the most active constituents or fractions from the selected volatile oils. Resumo A Floresta Atlântica é considerada uma rica fonte de plantas aromáticas com amplo espectro de propriedades biológicas. Na busca de novos inibidores da acetilcolinesterase (AChE) e α-glicosidase (AG), folhas de diferentes espécies de Piper localizadas na Floresta Atlântica no litoral do Paraná - Brasil, foram submetidas a hidrodestilação e seus óleos voláteis caracterizados por CG-DIC e CG-EM. A coleta ocorreu em duas estações distintas, inverno (I) e primavera (P), de 7 diferentes espécies. Sesquiterpenos foram identificados entre os compostos majoritários em todas as espécies estudadas, com dezenas de representantes. No entanto, foram observadas baixas concentrações de monoterpenos; α-pinene in Piper mosenii and P. cernuum, δ-3-carene in P. rivinoides, camphene and β-pinene in P. cernuum são exceções. Os arilpropanoides miristicina e elemicina foram identificadas em quantidades significativas em P. diospyrifolium (26.2%/P) e P. mosenii (16.4%/I), respectivamente. Para a AChE as amostras mais ativas foram P. diospyrifolium, P. aduncum e P. cernuum, com níveis de inibição > 93%. Para a AG, que se mostrou menos sensível às amostras, os candidatos mais promissores foram P. diospyrifolium e P. mosenii, ambos com níveis de inibição > 65%. Esses resultados destacam a importância das plantas nativas como fontes renováveis de novos inibidores para AChE e AG. Estudos adicionais se fazem necessários para identificar os constituintes ou frações mais ativas dos óleos voláteis selecionados.

A wide-ranging organism, such as plants, fungi, insects, marine organisms, and bacteria are the main sources of bioactive substances. Among them, medicinal plants offer harmless elusive means to improve our health conditions. Moreover, plant-derived bioactive is an inspiration for developing several therapeutic agents having extensively diverse chemo-structures and exhibit superior biological properties like antimicrobial, anticancer, and antioxidant, anti-inflammatory properties. Hence, many of them are used in therapeutic applications to treat various human ailments. Markedly, tropical countries harbor the maximum global biodiversity and constitute several vital plant species with pharmacological potential. Hence, they are being explored for bioactive compounds, and other raw materials to manufacture herbal medicines or chemo-drugs. In the present time, the emergence of microbial resistance to conventional antibiotics has become a major threat in treating microbial infections. Further, side effects caused by classical antibiotics have forced scientists to work toward exploring novel antimicrobial agents to overcome these hitches. Phytoconstituents have been shown to have prospective antimicrobial properties against both sensitive and resistant pathogenic microbes by exerting diverse mode of action. In this chapter, the potential of tropical plant species with antibacterial and antifungal activities are reviewed in detail.

Considering the evidence that essential oils, as well as safrole, could modulate bacterial growth in different resistant strains, this study aims to characterize the phytochemical profile and evaluate the antibacterial and antibiotic-modulating properties of the essential oil Ocotea odor&iacute, fera (EOOO) and safrole against efflux pump (EP)-carrying strains. The EOOO was extracted by hydrodistillation, and the phytochemical analysis was performed by gas chromatography coupled to mass spectrometry (GC-MS). The antibacterial and antibiotic-modulating activities of the EOOO and safrole against resistant strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa were analyzed through the broth microdilution method. The EP-inhibiting potential of safrole in association with ethidium bromide or antibiotics was evaluated using the S. aureus 1199B and K2068 strains, which carry genes encoding efflux proteins associated with antibiotic resistance to norfloxacin and ciprofloxacin, respectively. A reduction in the MIC of ethidium bromide or antibiotics was used as a parameter of EP inhibition. The phytochemical analysis identified 16 different compounds in the EOOO including safrole as the principal constituent. While the EOOO and safrole exerted clinically relevant antibacterial effects against S. aureus only, they potentiated the antibacterial activity of norfloxacin against all strains evaluated by our study. The ethidium bromide and antibiotic assays using the strains of S. aureus SA1119B and K2068, as well as molecular docking analysis, indicated that safrole inhibits the NorA and MepA efflux pumps in S. aureus. In conclusion, Ocotea odorifera and safrole presented promising antibacterial and antibiotic-enhancing properties, which should be explored in the development of drugs to combat antibacterial resistance, especially in strains bearing genes encoding efflux proteins.

Essential oils are secondary metabolites with immense pharmacological potential.These substances are abundantly produced by plants of the family Asteraceae, such as Baccharis coridifolia. Previous studies have demonstrated that this species has pharmacological properties that make it a promising source of new antibacterial agents. Therefore, the present study aimed to evaluate the antibacterial and antibiotic-modulating activity of Baccharis coridifolia essential oil against multidrug-resistant (MDR) strains. The phytochemical analysis was carried out by gas chromatography coupled to Mass Spectroscopy (GC/MS), and realized the Minimum Inhibitory Concentation (MIC) and antibiotic-modulation from the microdilution method in 96-well plates. It was revealed the presence of germacrene D (23.7%), bicyclogermacrene (17.1%), and (E)-caryophyllene (8.4%) as major components. The minimum inhibitory concentration of essential oil against strains of Pseudomonas aeruginosa (512 μg/mL) and Staphylococcus aureus (128 μg/mL) demonstrated clinically relevant antibacterial activity. In addition, the combination of subinhibitory doses of the oil with conventional antibiotics showed synergism, indicating potentiation of the antibacterial effect. In conclusion, the essential oil of Baccharis coridifolia (EOBc) presented antibacterial and antibiotic-modulating activities that place this species as a source of molecules useful in the fight against bacterial resistance.

One of the major challenges today for research groups on natural products distributed around the world is the discovery of substances that are bioactive, as well as their respective analogues. Thus, plants represent an important study target in the search for these new substances, being considered a promising source of molecular diversity for selective enzymatic inhibitors and synthesis for numerous bioactive compounds. The Brazilian biodiversity is one of the richest on the planet: it encompasses from 15 to 25% of all plant species, with a high rate of biological endemism, dispersed in unique biomes. A wide variety of micro- and macromolecular metabolites have been obtained, and several substances present biological and pharmacological activities with potential for the development of supplements alimentary, pharmaceuticals, and pesticides prototypes. In this context, this chapter documents the enzyme inhibitory potential of Myrtaceae, Lauraceae, and Piperaceae families from Brazilian Flora.

This study is a pioneer in reporting the antibacterial properties of the species Croton ceanothifolius Baill. The genus Croton belongs to the family Euphorbiaceae composed of numerous species with documented biological activities. However, the pharmacological properties of C. ceanothifolius remain poorly understood. The leaves of this plant were submitted to hydrodistillation for essential oil (CcEO) extraction and the phytochemical characterization of the oil was performed by GC/MS. The minimum inhibitory concentration of the CcEO was determined for the evaluation of antibacterial activity against multiresistant strains of Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. The antibiotic-modulating activity of the oil, in combination with antibiotics, was also evaluated. The combination of the CcEO with penicillin, norfloxacin, and gentamicin presented a synergistic effect. This effect was more significant for the association with antibiotics of the quinolone and aminoglycoside classes against Escherichia coli. The association of oil with gentamicin showed better results with regard to the Gram-positive strain. The association of the oil with norfloxacin against P. aeruginosa also showed synergism, but the association with penicillin did not change the effect of this antibiotic. Thus, it is concluded that C. ceanothifolius essential oil selectively potentiates the action of antibiotics against multiresistant strains.

This chapter discusses on the search for active substances, originating from essential oil plant species occurring in the Atlantic Rain Forest of Brazil. Despite its diminished state, the Atlantic Forest still ranks as a global conservation priority. Although it is just a small fraction of the size of the great Amazon rainforest, the Atlantic Forest still harbors a wide range of biological diversity similar to that of the Amazon. In this biome, around 20,000 species of plants, representing 8% of the Earth’s plants can be found. Some of these plants exhibit numerous therapeutical properties that are mainly attributed to their phytochemicals. Moreover, the essential oils extracted from plants constitute a diverse array of phytocompounds with biological significance. In this context, this chapter describes different plant species, their essential oil chemical composition, and their potential uses and pharmacological applications.

The present study had as its objective to evaluate the antibacterial and antibiotic modulatory activity of the Baccharis dracunculifolia (DC) essential oil (EOBD), a species commonly known as “Alecrim do campo”. The essential oil chemical composition analysis and the direct in vitro antibiotic activity evaluation, as well as in combination with the antibiotics Ampicillin, Gentamicin, and Norfloxacin against standard Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 9027, and Staphylococcus aureus ATCC 25923 strains, as well as E. coli 06, P. aeruginosa 24, and S. aureus 10 resistant strains, were performed. Gas chromatography-mass spectrometry (GC–MS) revealed the major terpenoids: Germacrene D (18.4%), (E)-Nerolidol (14.0%), Mustacone (11.2%), Spathulenol (11%), β-pinene (9.5%) and Bicyclogermacrene (8.4%). A direct B. dracunculifolia essential oil antibacterial activity against S. aureus 25923 with a MIC of 102 μg/mL and one of 512 μg/mL against S. aureus 10 were observed. The EOBD synergistically modulated the Norfloxacin antibiotic against P. aeruginosa 24, with a MIC reduction from 50.8 to 6.35 μg/mL, a Gentamicin MIC reduction from 20.16 to 4 μg/mL, and an Ampicillin MIC reduction from 645.1 to 512 μg/mL. The essential oil synergistically modified Norfloxacin activity against E. coli 06 with a MIC reduction from 40.32 to 3.17 μg/mL, and a Gentamicin MIC reduction from 50.8 to 25.4 μg/mL. The essential oil also showed synergism against S. aureus 10 when associated with Norfloxacin, with a MIC reduction from 322.54 to 203.2 μg/mL, whilst when associated with Ampicillin, it demonstrated synergism by reducing the MIC from 80.6 to 20.16 μg/ml. Results from this research revealed that the EOBD is a promising natural product with antimicrobial potential, both directly and in combination with antibiotics, for clinical use against Gram-positive and Gram-negative bacteria.

The essential oil yield and composition of 17 species of the Asteraceae family were evaluated. Samples were obtained by hydrodistillation of the leaves and inflorescences and they were analyzed by GC-MS and GC-FID. A total of 13 species presented essential oils with yields ranging from 0.06 to 3.36% in fresh samples and from 0.07 to 2.53% in dried samples. Erechtites valerianifolius (Wolf) DC. produced the highest essential oil yield from both fresh and dried samples. Seventy-nine constituents were identified in essential oils from Asteraceae species, mainly consisting of monoterpenes and sesquiterpenes.

We re-assess the taxonomic status of Owenia Delle Chiaje, 1841 from Southern Brazil based on estuarine specimens from Paranaguá Bay (Paraná) and Babitonga Bay (Santa Catarina), and literature records. Owenia caissara sp. n. is diagnosed by a branchial crown with five pairs of tentacles, branched close to the base of the crown, rectilinear collar with a pronounced lateral slit, two ventrolateral ocelli partially covered by the collar, up to 23 hooks on a single row in the first abdominal segment, regularly curved nuchal shape, regularly moderate teeth curvature, and long and thin scales with oval transition. The description of Owenia caissara sp. n. reinforces the idea that Owenia fusiformis sensu lato is a complex of closely related species that can be distinguished on the basis of both macro- and micro- morphological traits.

The objective of this work was to evaluate the phytochemical composition and the antibacterial and antibiotic-modulating activities of the essential oils of Eugenia brasiliensis Lam (OEEb) and Piper mosenii C. DC (OEPm) singly or in association with blue LED (Light-emitting diode) light. The antibacterial and antibiotic-modulatory activities of the essential oils on the activity of aminoglycosides were evaluated to determine the minimum inhibitory concentration (MIC, &mu, g/mL) in the presence or absence of exposure to blue LED light. The chemical analysis showed &alpha, pinene and bicyclogermacrene as major constituents of OEPm, whereas &alpha, muurolol was the main compound of OEEb. Both OEEb and OEPm showed MIC &ge, 512 &mu, g/mL against the strains under study. However, the association of these oils with the blue LED light enhanced the action of the aminoglycosides amikacin and gentamicin. In conclusion, the association of aminoglycosides with the blue LED light and essential oils was effective against resistant bacteria.

The secular use of plants in popular medicine has emerged as a source for the discovery of new compounds capable of curing infections. Among microbial resistance to commercial drugs, species such as Piper diospyrifolium Kunth, which are used in popular therapy, are targets for pharmacological studies. With this in mind, antimicrobial experiments with the essential oil from the P. diospyrifolium (PDEO) species were performed and its constituents were elucidated. The oil compounds were identified by gas chromatography coupled to mass spectrometry (GC/MS). The broth microdilution method with colorimetric readings for bacterial tests (Escherichia coli and Staphylococcus aureus) and spectrophotometric readings for fungal tests (Candida albicans and Candida tropicalis), whose data were used to create a cell viability curve and calculate its IC50 against fungal cells, were used to determine the minimum inhibitory concentration of the oil and its combined action with commercial drugs. The oil's minimal fungicidal concentration and its action over fungal morphological transition were analyzed by subculture and microculture, respectively. Chemical analysis revealed Z-Carpacin, Pogostol and E-Caryophyllene as the most abundant compounds. Results from the intrinsic analysis were considered clinically irrelevant, however the oil presented a synergistic effect against multiresistant E. coli and S. aureus strains when associated with gentamicin, and against the standard and isolated C. tropicalis strains with fluconazole. A fungicidal effect was observed against the C. albicans isolate. Candida spp. hyphae inhibition was verified for all strains at the highest tested concentrations. The P. diospyrifolium essential oil presented a promising effect when associated with commercial drugs and against a fungal virulence factor. Thus, the oil presented active compounds which may help the development of new drugs, however, new studies are needed in order to clarify the oil's mechanism of action, as well as to identify its active constituents.

Arctium species are known for a variety of pharmacological effects due to their diverse volatile and non-volatile secondary metabolites. Representatives of Arctium species contain non-volatile compounds including lignans, fatty acids, acetylenic compounds, phytosterols, polysaccharides, caffeoylquinic acid derivatives, flavonoids, terpenes/terpenoids and volatile compounds such as hydrocarbons, aldehydes, methoxypyrazines, carboxylic and fatty acids, monoterpenes and sesquiterpenes. Arctium species also possess bioactive properties such as anti-cancer, anti-diabetic, anti-oxidant, hepatoprotective, gastroprotective, antibacterial, antiviral, antimicrobial, anti-allergic, and anti-inflammatory effects. This review aims to provide a complete overview of the chemistry and biological activities of the secondary metabolites found in therapeutically used Arctium species. Summary of pharmacopeias and monographs contents indicating the relevant phytochemicals and therapeutic effects are also discussed, along with possible safety considerations.

The family Piperaceae is known for presenting in its species flavoring, healing and antimicrobial properties among others. The objective of the present study was: to study the chemical profile of the essential oil of Piper rivinoides (EOPR); to analyze its anti-bacterial and antifungal potential, as well as to evaluate the antifungal and antibiotic-modifying capacity. The chemical constituents were identified by gas chromatography with flame ionization detector (GC-FID), allowing the identification of 7 constituents of a total of 86.99%. E-Isoelemicin was identified as the main constituent of petroleum (40.81%). Clinically relevant MIC results were obtained against fungi in which the inhibitory concentration remained

Essential oils are broadly used in the food, perfume, and pharmaceutical industries. These are associated with ecological functions of defense and attraction of pollinators, and usually undergo quantitative and qualitative variation in response to the environment. Thus, the aim of this chapter is to highlight the essential oil content, chemical composition, and biological activities of Baccharis milleflora.

The genus Baccharis (Asteraceae) demonstrated the presence of compounds with antibacterial, antifungal and antioxidant activities. Because of the increasing rates of antimicrobial resistance, adequate treatment of infections caused by Gram-negative bacteria has become challenging. The objective of the present study was evaluate the antibacterial and antibiotic-modifying activity of the essential oil obtained from Baccharis reticulata (Ruiz & Pav.) Pers. and the compound α-pinene against Pseudomonas aeruginosa and other multiresistant bacteria. An analysis by gas chromatography associated with mass spectrometry (GC/MS) revealed the presence of dilapiol (33.8 %), α-pinene (31.7 %) and β-pinene (9.4 %) as major components of the oil. The determination of the Minimum Inhibitory Concentration (MIC) revealed that the oil has antibacterial activity against S. aureus only. However, the oil potentiated the norfloxacin and gentamicin against all strains evaluated. Also, α-pinene increased the activity of norfloxacin against E. coli, as well as potentiated the activity of norfloxacin and gentamicin against S. aureus. Therefore, the authors conclude that the essential oil of B. reticulata, as well as the compound α-pinene, have antibacterial and antibiotic-modulating activities that make them useful in the development of new weapons against bacterial resistance.

Infections by multiresistant microorganisms have led to a continuous investigation of substances acting as modifiers of this resistance. By following this approach, the chemical composition of the essential oil from Piper caldense leaf and its antimicrobial potential were investigated. The antimicrobial activity was determined by broth microdilution method providing values for minimum inhibitory concentration (MIC), IC50, and minimum fungicidal concentration (MFC). The essential oil was tested as a modulator for several antibiotics, and its effect on the morphology of Candida albicans (CA) strains was also investigated. The chemical characterization revealed an oil composed mainly of sesquiterpenes. Among them are caryophyllene oxide (13.9%), spathulenol (9.1%), &delta, cadinene (7.6%) and bicyclogermacrene (6.7%) with the highest concentrations. The essential oil showed very low activity against the strains of CA with the lowest values for IC50 and MFC of 1790 &mu, g/mL and 8192 &mu, g/mL, respectively. The essential oil modulated the activity of fluconazole against CA URM 4387 strain, which was demonstrated by the lower IC50 obtained, 2.7 &mu, g/mL, whereas fluconazole itself presented an IC50 of 7.76 &mu, g/mL. No modulating effect was observed in the MFC bioassays. The effect on fungal morphology was observed for both CA INCQS 40006 and URM 4387 strains. The hyphae projection was completely inhibited at 4096 &mu, g/mL and 2048 &mu, g/mL, respectively. Thus, the oil has potential as an adjuvant in antimicrobial formulations.

The Piper mikanianum species were investigated by the antimicrobial potential and chemical composition. Chemical analysis was performed by gas chromatography coupled to mass spectrometry (GC/MS). The Minimum Inhibitory Concentration (MIC) as well as the 50% Inhibitory Concentration against Candida strains were determined by microdilution. The effect of the drug-oil combination was also evaluated to verify possible synergism. The Minimum Fungicidal Concentration (MFC) was evaluated by subculturing the microdilution in Petri dishes and the anti-pleomorphism potential of the oil was tested in humid chambers. Chemical analysis revealed safrol as the major compound. The results from the intrinsic activity evaluation of the oil did not reveal a clinical importance, however, it presented a synergistic effect when associated with gentamicin against the multidrug resistant E. coli strain and when associated with fluconazole against fungal strains. Moreover, the oil possessed a fungistatic effect. Total inhibition of filamentous structures occurred in both Candida species in the anti-virulence test. The P. mikanianum essential oil showed a potentiating activity of drugs for which resistance exists and an inhibitory effect of one of the main virulence factors of the Candida genus, morphological transition, which has been previously shown to be responsible for causing invasive infections in human tissues.

1 recurso en línea (páginas 491-499), Las especies nativas de Piper presentan importantes actividades biológicas repelentes, antimicrobianos, insecticidas, antitumoral y anti-protozoario. Los estudios sobre nuevas especies representan potenciales descubrimientos sin publicar y la propagación vegetativa es necesario para el desarrollo del protocolo de cultivo; además, reduce la extracción natural. El objetivo de esta investigación fue evaluar el enraizamiento de esquejes de P. arboreum, P. cernuum y P. diospyrifolium con diferentes tratamientos que contienen dosis del ácido indolbutirico (0, 500, 1.000, 1.500, 2.000 y 3.000 mg L-1). Ramas fueran colectadas en la Reserva Biológica Bom Jesus, estado de Paraná, Brasil. Los cortes con una longitud de 12 cm y el diámetro promedio de 6 mm se instalaron en tubos de plástico de 53 cm3 usando el sustrato comercial Tropstrato HP® y riego por nebulización intermitente. Después de 90 días se evaluaron las tasas de supervivencia, mortalidad y esquejes con nuevos brotes, número y longitud de las tres raíces principales. Los porcentajes de enraizamiento alcanzaron un promedio de 67,5% para P. arboreum, 51,6% para P. cernuum y 50,4% para P. diospyrifolium. Se encontró respuesta positiva de los tratamientos que contienen el regulador vegetal para las variables de enraizamiento, porcentaje de esquejes con brotes y número de raíces por estaca, pero hubo variaciones en las respuestas de cada especie. La permanencia de hojas fue un factor importante para el proceso de enraizamiento adventicio en las especies evaluadas., biological activities. Studies on new species can discover unpublished potentialities and vegetative propagation for the development of cultivation protocols and reduce the natural extraction. The objective of this study was to evaluate the rooting of P. arboreum, P. cernuum and P. diospyrifolium stem cuttings with different treatments containing doses of indole butyric acid (0, 500; 1,000; 1,500; 2,000 and 3,000 mg L-1). Branches were collected in the “Bom Jesus Biological Reserve”, Parana state, Brazil. The cuttings, with a length of 12 cm and average diameter of 6 mm, were placed in 53 cm3 plastic tubes with the commercial substrate Tropstrato HP® and intermittent misting. After 90 days, the survival, mortality, cuttings with new shoots, number and length of the three main roots were evaluated. The percentages of rooting reached an average of 67.5% for P. arboreum, 51.6% for P. cernuum and 50.4% for P. diospyrifolium. A positive effect in the treatments containing the plant regulator was observed for rooting development, percentage of cuttings with shoots and number of roots per propagule, but there were variations in the responses of each species. Leaf retention was an important factor for the adventitious rooting formation in all evaluated species., Bibliografía y webgrafía: páginas 498-499

In this paper, we have experimentally assessed tube-building strategies of Owenia caissara Silva & Lana, 2017 , including the particle size preferences. After acclimation, individual tubes were broken by their mid-region, and placed in experimental aquaria with four types of homogeneous substrates (from silt-clay to coarse sand) and four types of mixed substrates. Animals completely removed from their tubes were unable to build new tubes. Adults in broken tubes were able to use a wide range of particles, from fine to coarse sand, but not silt-clay. Owenia caissara showed a clear preference for coarse sediment particles. In extreme conditions, individuals were able to rebuild their tubes using only filamentous debris. Owenia caissara may display higher selection ability and preference for larger particles when growing, although adults can also adapt to bottoms with predominantly smaller particles such as fine sand.

RESUMO A família Annonaceae possui representantes de grande interesse medicinal e o gênero Xylopia é um dos que merecem destaque. Composta por aproximadamente 160 espécies distribuídas na América do Sul, América central, África e Ásia, as espécies desse gênero podem ser arbustivas ou arbóreas. No Brasil são encontradas nas regiões Norte, Nordeste, Centro-Oeste e Centro Sul. Este gênero produz uma variedade de metabólitos incluindo alcalóides, amidas, lignóides, acetogeninas e terpenóides e têm sido investigados como fonte potencial de acetogeninas, compostos esses que apresentam uma ampla variedade de propriedades biológicas com destaque para: citotóxica, antitumoral, antiparasitária, antimicrobial, inseticida e antimalarial. Neste estudo, efetuou-se uma revisão das principais espécies de Xylopiaencontradas no Brasil, já estudadas e descritas na literatura, abordando os aspectos químico-farmacológicos, destacando os constituintes químicos isolados bem como a ação farmacológica evidenciada. ABSTRACT The family Annonaceae has representatives of great medical interest, and the Xylopia species deserves attention. The Xylopia genus is composed by approximately 160 species, with geographic distribution in tropical and subtropical regions of America, Africa and Asia. This genus can present shrubs or trees. In Brazil, they can be found at the North, North-west, Central-West and Central-South Regions. The phytochemical investigations resulted mainly in the isolation of alkaloids, diterpenos, quinolines and acetogenins, with the latter presenting very interesting biological properties such as the cytotoxic, antiprotozoal and the insecticide activities.This study aimed to review the botanical, chemical and pharmacological aspects of the Xylopia genus found in Brazil, highlighting the chemical components, as the well-known pharmacological effect .

The Myrtaceae family has great occurrence in Brazil, mainly in the Atlantic Forest of the South and Southeast regions and presents potential for essential oil production. This work aimed to evaluate the essential oil yield and composition of the species Myrciaria delicatula, Campomanesia xantocarpha, Campomanesia aurea, Calyptranthes clusiifolia, Myrcia splendens, Eugenia osoriana, Myrciaria tenella, Myrceugenia reitzii, Calyptranthes concinna e Myrcia arborensis from a segment of the Atlantic Forest of Parana State. The essential oil extraction was carried out by hydrodistillation of fresh and dried leaves using a Clevenger type apparatus and the chemical composition was analyzed by gas phase chromatography coupled with mass spectrometry (GC/MS). Myrceugenia reitzii showed eesential oil yield superior to other species and the essential oil yield of all species increased after drying. The chemical composition in the samples showed mono and sesquiterpenes , being the sesquiterpenes in higher percentages. The drying conditions affected the essential oil composition of the for the majority of the evaluated species.

In this study, the Piper cernuum Essential Oil (EOPC) was tested against bacterial and fungal strains using the microdilution method to evaluate its minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC), as well as its antibiotic modifying effect, in addition to observing the oils ability to cause fungal dimorphism and to generate an IC50 cell viability curve. The EO was obtained through hydrodistillation using a Clevenger-type apparatus with the dry leaves and analyzed by GC-FID, allowing the identification of 14 compounds, with the main compound being 4-epi-cis-dihydromarofuran (28.97%). An EOPC intrinsic activity was identified only against Candida albicans 4127 (IC50 56.851 μg/mL). Given the MIC results from the EOPC intrinsic activity against Staphylococcus aureus 10 at the concentration of 406 μg/mL, its association with fluconazole potentiated it’s antifungal action. The action of gentamicin was potentiated by the addition of the EOPC to Staphylococcus aureus 10 and Escherichia coli 06 strains, both with MIC

SUMMARYLeishmaniasis is one of the neglected diseases. High cost, systemic toxicity, and diminished efficacy due to development of resistance by the parasites has a negative impact on the current treatment options. Thus, the search for a new, effective and safer anti-leishmanial drug becomes of paramount importance. Compounds derived from natural products may be a better and cheaper source in this regard. This study evaluated the in vitro anti-leishmanial activity of Spiranthera odoratíssima (Rutaceae) fractions and isolated compounds, using promastigote and amastigote forms of different Leishmania species. J774 A.1 macrophage was used as the parasite host cell for the in vitro assays. Evaluations of cytoxicity, nitric oxide (NO), interleukin-10 and in silico analysis were carried out. In vitro experiments showed that the fruit hexanic fraction (Fhf) and its alkaloid skimmianine (Skm) have a significant (PL. braziliensis. This anti-L. braziliensis activity of Fhf and Skm was due to increased production of NO and attenuation of IL-10 production in the macrophages at concentrations ranging from 1·6 to 40·0 μg/ml. The in silico assay demonstrated significant interaction between Skm and amino acid residues of NOS2. Skm is thus a promising drug candidate for L. braziliensis due to its potent immunomodulatory activity.

The present paper reports the synthesis and antiprotozoal activity of N-quinolin-8-yl-arylsulfonamides and their copper and zinc complexes. Sulfonamides 2-5 were synthesized by reacting 8-aminoquinoline with several commercial arylsulfonyl chlorides. The corresponding complexes 6-13 were obtained using copper (II) acetate or zinc chloride in methanol. In vitro activity was carried out against promastigote forms of Leishmania braziliensis and L. chagasi, and epimastigote forms of Trypanosoma cruzi. Selected compounds were tested against axenic amastigote forms of L. braziliensis. The new 2,5-dichlorobenzenesulfonamide ligand was found to be inactive under the selected bioassays, however its copper complex 8 was active with the highest selective indexes (SI) against L. braziliensis promastigote and amastigote forms, with IC50 values of 2.59 and 0.35 μM, respectively. Difluorinated copper 10 and zinc 11 complexes were most active against L. braziliensis, with IC50 of 1.11 μM and 1.25 μM, respectively. However, the SI values were about 12 for both compounds. In general, the complexation of sulfonamides increases the antiprotozoal activity, as well as the cytotoxicity on Vero cells. These results confirm the antiprotozoal potential of sulfonamides and metal-based sulfonamides.

Plant secondary metabolites have attracted considerable attention from the industry as consumers are increasing their interest for natural products over chemically synthesized reagents to be used as additives in food, cosmetics or pharmaceuticals. Some plant essential oils show significant antimicrobial properties and this could be exploited to produce new food preservatives or novel antimicrobial formulations. Here we describe the extraction, chemical analysis and antimicrobial properties of grass lemon Cymbopogon citratus and Cymbopogon flexuosus essential oils. Essential oils were extracted from dried leaves using hydrodestilation and their composition was established by gas chromatography coupled to mass spectrometry. Agar diffusion assays indicated that C. citratus and C. flexuosus essential oils act as antimicrobial agents against both gram negative and gram positive model organisms. These data support that lemon grass essential oils can be used as an alternative for microbiological control.

In the present paper 12 N-quinolin-8-yl-arylsulfonamides synthesized by coupling 8-aminoquinolines with various arylsulfonylchlorides were assayed in vitro against Leishmania amazonensis, Leishmania chagasi and Trypanosoma cruzi strains. This series of new compounds were found to be selective for Leishmania spp. promastigote and amastigote forms. The most active compound was the N-(8-quinolyl)-3,5-difluoro-benzenesulfonamide 10 with an IC50 against L. amazonensis and L. chagasi of 2.12 and 0.45 μM, respectively. The less cytotoxic biphenyl derivative 7 was very effective against intracellular L. amazonensis with a reduction of macrophage cell infection of 82.1% at 25 μM. In addition, a copper complex 17 of an inactive ligand was readily synthesized and showed high leishmanicidal and trypanocidal activity against both extra and intracellular forms.

O gênero Acosmium possui 17 espécies com distribuição geográfica que se estende do sudeste do México até o Nordeste da Argentina, sendo que a maioria das espécies está localizada no Brasil. A. dasycarpum, A. panamense, A. subelegans são as espécies mais utilizadas popularmente no tratamento de enfermidades. Uma busca na literatura, resguardando aspectos químicos e farmacológicos destas plantas, indicam atividade citotóxica, ação antitérmica, efeito hipoglicêmico, bem como tem sido usada no tratamento da doença de Alzheimer e desordens no sistema nervoso central. Investigação fitoquímica resultou principalmente no isolamento de terpenos, ácido cafêico, alcalóides do tipo diaza-adamantano e quinolizidínicos bem como pironas. The genus Acosmium is composed by c.a. 17 species, with geographic distribution from southeastern Mexico to Northwestern Argentina. Most of the species, however, are located in Brazil. A. dasycarpum, A. panamense, A. subelegans are used in folk medicine to treat several ailments. A search in the literature regarding the chemical and pharmacological aspects of these plants indicates cytotoxic activity, antithermal and hypoglycemic effects, as well as their use to treat Alzheimer's disease and CNS disorders. Phytochemical investigations resulted mainly in the isolation of terpenes, caffeic acid, diaza-adamantane and quinolizidines alkaloids as well as pyrones.

The compound 4-(Phenylsulfonyl) morpholine belongs to the class of sulfonamides, which are widely used in the treatment of a large number of diseases caused by microorganisms. This compound has a morpholine group, which is also known for its antimicrobial properties. The aim of the present study was to investigate the antimicrobial and modulating activity of 4-(Phenylsulfonyl) morpholine against standard and multi-resistant strains of Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and strains of the fungi Candida albicans, C. tropicalis and C. krusei. Antimicrobial activity was assessed based on the minimum inhibitory concentration (MIC) using the microdilution method. MIC was ⩾1024μg/mL for all microorganisms. Regarding modulating activity, the most representative effect occurred with the combination of 4-(Phenylsulfonyl) morpholine at a concentration of 128μg/mL (MIC 1/8) and amikacin against P. aeruginosa 03, with a reduction in MIC from 312.5 to 39.06μg/mL.