Search

The inappropriate use of antimicrobials, along with environmental conditions, can lead to the emergence of resistant microorganisms. The use of phytopharmaceuticals and herbal medicines has a positive impact and represents a promising alternative. Psidium guajava extracts have been widely reported to have antimicrobial potential; however, studies reporting their activity against resistant bacterial strains are scarce. Because of the emerging resistance, the aim of this study was to analyze the antimicrobial capacity of the aqueous extract of guava leaves against wild-type and resistant bacterial strains. The aqueous extract obtained from the leaves of P. guajava was evaluated by HPLC for the content of total phenolics and tannins, antioxidant activity, and chemical composition. The antimicrobial activity of the extracts was analyzed by the disk diffusion and broth microdilution methods. The results of the chemical analysis of the extracts showed total phenolics content of 17.02 ± 6.87 mg/g of dry extract, total tannin content of 14.09 ± 1.20 mg of tannic acid equivalents/g of dry extract, and moderate antioxidant capacity with an EC50 value of 140 µg/mL. Flavonoids are the major compounds (rutin, hesperidin, and quercetin), followed by phenolic acids. Disk diffusion test results showed the presence of inhibition halos for Gram-positive bacteria (Staphylococcus aureus, sensitive and resistant; Staphylococcuspseudintermedius, sensitive and resistant; and Streptococcus spp., beta-hemolytic), while for Gram-negative bacteria (Escherichia coli, sensitive and resistant), there was no inhibition in the tested concentration range. The Minimal Inhibitory Concentration was 6.8 mg/mL for all Gram-positive strains evaluated. The present study demonstrated the antimicrobial activity of the aqueous extract of P. guajava against sensitive and resistant Gram-positive bacteria. The better antimicrobial activity found in the present study compared with previously reported activity should be highlighted and may be related to the higher concentration of total phenolics present in the tested extract. Moreover, the content of tannins found suggests a species with high quality that produces tannins. These new findings suggest an innovative profile regarding therapeutic resources that can be adopted to combat resistant microbial strains.

Cannabis is used in the treatment of several human conditions; however, its use is still less explored in veterinary medicine. This systematic review aims to summarize the evidence of efficacy and safety of the use of cannabis for the treatment of animal disease. A literature search was performed for studies published until 16 March 2021 in five databases. Randomized clinical trials (RCTs) that reported the efficacy or safety of cannabis in the treatment of animal disease were included. The RoB 2 Tool was used to assess the risk of bias. A total of 2427 records were identified, of which six studies fully met the eligibility criteria. RCTs were conducted in dogs with osteoarthritis (n = 4), with epilepsy (n = 1), and with behavioral disorders (n = 1). All studies used cannabidiol (CBD) oil in monotherapy or in combination with other drugs. Studies used CBD at 2 or 2.5 mg kg−1 twice daily (n = 4), orally (n = 5), during 4 or 6 weeks (n = 3), and compared CBD with placebo (n = 5). CBD significantly reduced pain and increased activity in dogs with osteoarthritis (n = 3). Moreover, CBD significantly reduced the frequency of seizures in dogs with epilepsy (n = 1) and the aggressive behavior of dogs (n = 1). Although promising results were identified, studies were heterogeneous and presented risks of bias that required caution in the interpretation of findings. Therefore, there was some evidence to support the use of CBD in dogs with osteoarthritis to reduce pain and increased activity, but limited evidence against epilepsy and behavioral problems. In addition, CBD was well tolerated with mild adverse effects. More RCTs with high quality of evidence are needed, including greater numbers of animal subjects, additional species, and clear readout measures to confirm these findings.

Petroselinum crispum var. neapolitanum Danert (Apiaceae) (PC), popularly known as parsley, is an herb native to the Mediterranean region widely cultivated around the world for culinary and ethnomedicinal purposes. The herb is traditionally used in various parts of the world to treat arterial hypertension, hemorrhoid, nose bleeding, hyperlipidemia, and pain, among other indications. The aim of this study was to evaluate the antithrombotic activity of an aqueous extract PC in rats. Aerial parts of a flat-leaf variety of parsley were extracted by decoction. In vivo thrombosis in rat models as well as ex vivo assays were used in the evaluation of PC antithrombotic effects. Intravenous administration of PC (25 mg/kg.b.w), 5 min before thrombosis induction, reduced the venous thrombus formation by 98.2%, while oral administration (125 mg/kg.b.w) impaired it by 76.2%. In the arterial thrombosis model, the oral administration of PC at 15 or 25 mg/kg.b.w, 60 min before thrombosis induction, increased the carotid artery occlusion time by 150% (37.0 ± 6.44 min) and 240% (more than 60 min), respectively. A HPLC-DAD-MS/MS profile of PC extract used in this study was provided. Apiin showed to be the most abundant phenolic compound in the extract. It also revealed the presence of many coumaric acid derivatives. Our results indicate that PC is a potential candidate for the development of a phytotherapeutic drug in the treatment of thromboembolic diseases and provide a detailed chemical profile useful for controlling PC extract production in view of phytotherapy.

Leishmaniasis consists of a group of neglected diseases, which affect millions of people worldwide. First- and second-line chemotherapies, which present high toxicity and variable efficacy, have been available for decades leading to the appearance of resistance. Globally, volatile oils have received much attention due to their increase use as effective bioactive compounds in folk medicine. They have been employed against Leishmania parasites with a positive impact in the treatment of this neglected disease. In this review, the leishmanicidal activity of volatile oils and their isolates have been described as promising novel candidate molecules for the development of leishmanicidal drugs. The purpose of this review is to critically discuss several works published between 2000 and 2020 that have described the utilization of volatile oils and some of their active principles from diverse plant sources against different species of Leishmania.

Parsley (Petroselinum crispum var. neapolitanum Danert) is a vegetable species with potential for pharmaceutical use because it contains apiin, a flavonoid that stands out for having biological activities, such as antioxidant. The aim of this study is to evaluate the influence of chemical or organic fertilizers on the nitrogen metabolism and production of flavonoids in parsley at different stages of development, aiming to establish the most appropriate management of this crop. The experiment was carried out in flower beds with three treatments: Without fertilizer, chemical fertilization and organic fertilization (Bokashi), with two harvest times, 28 and 56 days after germination (DAG). The harvest period significantly influenced the analyzed variables, but the fertilizer source used did not. In this sense, for the production of apiin, fertilization is unnecessary when the soil used has good fertility conditions. It is also recommended to harvest all the plants at 28 DAG, dispensing with late cultivation, thus resulting in reduced production costs. Key words: Parsley, soluble fractions, fertilizer, chemical fertilization, Bokashi, flavonoids.

The aim of the present study was to evaluate the insecticidal effect of the cassia, thyme and oregano volatile oils against the immature and adult flea’s stages. For this purpose, the tested samples were chemically characterized by GC-FID and GC-MS. The mortality of larvae and adult fleas, eggs, and pupae of Ctenocephalides felis felis was performed through in vitro tests at different concentration levels. Inhibition of development and residual efficacy were also determined. The chemical characterization of the cassia, thyme, and oregano volatile oils presented cinnamaldehyde (91%), thymol (44.7%), and carvacrol (76.2%), respectively, as major constituents. In general, the samples showed insecticidal activity for both immature and adult flea’s stages. The best LC50 values for adults were obtained by oregano volatile oils (33.5 and 21.8 μg·cm−2, respectively, 24 and 48 h). Cassia volatile oils showed the best results against larvae (17.2 and 10.3 μg·cm−2, respectively, 24 and 48 h), eggs (3 μg.cm−2), and pupae (34.6 μg·cm−2), as well as the lowest value for inhibition of development (2.3 μg·cm−2). The oregano and thyme volatile oils showed residual efficacy greater than 80% for 6 days while cassia showed this result for 4 days. The results demonstrated the potential of volatile oils for flea control in all stages of the life cycle, with emphasis on cassia. The residual effects of the volatile oils are promising for the development of new and environmentally friendly phyto-pesticides for veterinary uses.

Volatile oils have great economic importance, mainly in the flavor and fragrance sectors, regarding their utility and application in the food, cosmetic, and pharmaceutical industries. In this work, volatile oils extracted by hydrodistillation from dried leaves of Varronia curassavica Jacq., Boraginaceae, and Laurus nobilis L., Lauraceae, including their chemical composition and extraction kinetics, were evaluated. β-Caryophyllene (15.2%), β-sinensal (7.9%), (Z)-α-trans-bergamotol (7%), α-humulene (5.6%), and β-bisabolene (5.5%) were V. curassavica volatile oil’s major components, while eucalyptol (19.2%), linalool (18.4%), and α-terpineol acetate (13.5%) were the major components of L. nobilis. The kinetics of volatile oil extraction showed a hyperbolic distribution for the two species: the contents of monoterpenes and sesquiterpenes extracted from V. curassavica, in the time frame analyzed, showed exponential decline followed by growth, respectively, while the content of these volatiles from L. nobilis showed an individual decrease and linear increase. Monoterpene extraction was faster than sesquiterpene extraction, but both processes presented hyperbolic distributions. Extraction kinetics for eucalyptol, linalool, α-terpineol, α-humulene, and β-caryophyllene and other compounds can be found in this analytical study.

Essential oils (EOs) are considered a new class of ecological products aimed at the control of insects for industrial and domestic use; however, there still is a lack of studies involving the control of fleas. Ctenocephalides felis felis, the most observed parasite in dogs and cats, is associated with several diseases. The aim of this study was to evaluate the in vitro activity, the establishment of LC50 and toxicity of EOs from Alpinia zerumbet (Pers.) B. L. Burtt & R. M. Sm, Cinnamomum spp., Laurus nobilis L., Mentha spicata L., Ocimum gratissimum L. and Cymbopogon nardus (L.) Rendle against immature stages and adults of C. felis felis. Bioassay results suggest that the method of evaluation was able to perform a pre-screening of the activity of several EOs, including the discriminatory evaluation of flea stages by their LC50. Ocimum gratissimum EO was the most effective in the in vitro assays against all flea stages, presenting adulticide (LC50 = 5.85 μg cm−2), ovicidal (LC50 = 1.79 μg cm−2) and larvicidal (LC50 = 1.21 μg cm−2) mortality at low doses. It also presented an excellent profile in a toxicological eukaryotic model. These findings may support studies involving the development of non-toxic products for the control of fleas in dogs and cats.

Aedes aegypti transmits arbovirus, which is a public health concern. Certain filamentous fungi have the potential to control the disease. Here, the effects of Metarhizium anisopliae s.l. CG 153, Beauveria bassiana s.l. CG 206 and Schinus molle L. were investigated against Aedes aegypti larvae. In addition, the effect of essential oil on fungal development was analyzed. Fungal germination was assessed after combination with essential oil at 0.0025 %, 0.0075 %, 0.005 %, or 0.01 %; all of the oil concentrations affected germination except 0.0025 % (v/v). Larvae were exposed to 0.0025 %, 0.0075 %, 0.005 %, or 0.01 % of the essential oil or Tween 80 at 0.01 %; however, only the essential oil at 0.0025 % achieved similar results as the control. Larvae were exposed to fungi at 10sup7/supconidia mLsup-1/supalone or in combination with the essential oil at 0.0025 %. Regardless of the combination, M. anisopliae reduced the median survival time of mosquitoes more than B. bassiana. The cumulative survival of mosquitoes exposed to M. anisopliae alone or in combination with essential oil was 7.5 % and 2 %, respectively, and for B. bassiana, it was 75 % and 71 %, respectively. M. anisopliae + essential oil had a synergistic effect against larvae, whereas B. bassiana + essential oil was antagonistic. Scanning and transmission electron microscopy, and histopathology confirmed that the interaction of M. anisopliae was through the gut and hemocoel. In contrast, the mosquito's gut was the main route for invasion by B. bassiana. Results from gas chromatography studies demonstrated sabinene and bicyclogermacrene as the main compounds of S. molle, and the in-silico investigation found evidence that both compounds affect a wide range of biological activity. For the first time, we demonstrated the potential of S. molle and its interaction with both fungal strains against A. aegypti larvae. Moreover, for the first time, we reported that S. molle might be responsible for significant changes in larval physiology. This study provides new insights into host-pathogen interplay and contributes to a better understanding of pathogenesis in mosquitoes, which have significant consequences for biological control strategies.

Psychotria ipecacuanha, commonly known as Ipeca, is a medicinal plant of pharmacological and economic value. The species is distylous; it has populations with two floral morphs, one with long and one with short styles. Apart from the presence of two floral morphs in a balanced ratio (1:1), reciprocal herkogamy of the reproductive organs between alternative morphs is desirable to maintain cross-pollination. The risk factors for genetic erosion and conditions for sexual reproduction in natural populations of P. ipecacuanha were investigated. The main risks for genetic erosion in four populations studied were: habitat change in the forest fragment where they occurred and in the surrounding area over the last 20 years; proximity to agricultural areas; frequency of drought affecting the forest fragment; and the area occupied by the species within the forest fragment. All evaluated populations were isoplethic with the reciprocity of reproductive organs varying across populations. Anthropogenic factors, associated with morphological and reproductive characteristics (e.g., low reciprocity between anther and stigma and low pollen production), indicate risks for the maintenance and reproduction of Ipeca in the population of the municipality of Denise. Habitat loss, small clusters, and the low number of reproductive plants jeopardize the survival of the studied populations.

O uso de oleos essenciais para o controle de ectoparasitos de interesse veterinario pode ser uma excelente alternativa aos compostos sinteticos comercializados como forma de reduzir os impactos negativos na saude humana e no meio ambiente. A incidencia de diferentes especies de carrapatos em diferentes locais e resultado das caracteristicas ambientais do territorio nacional. Entre as especies de interesse veterinario estao Amblyomma sculptum, Rhipicephalus microplus e Rhipicephalus sanguineus . Oleos essenciais (OEs) de Ocimum sp exibem uma gama de atividades biologicas, como inseticida, acaricida e repelencia de insetos. O objetivo deste estudo foi avaliar a atividade in vitro e estabelecer a CL 50 do OE de Ocimum gratissimum contra larvas de A. sculptum , R. microplus e R. sanguineus , a fim de explorar o potencial de uso desse OE no controle de carrapatos. Os resultados do bioensaio mostraram que o OE de O. gratissimum apresentou grande atividade acaricida contra todas as larvas testadas na faixa de concentracao avaliada. A atividade larvicida foi mais pronunciada para R. microplus (CL 50 = 2,0 mg.mL -1 ) quando comparada a A. sculptum (CL 50 = 5,5 mg.mL -1 ) e R. sanguineus (CL 50 = 6,2 mg.mL -1 ). Estes resultados sao promissores para o desenvolvimento de produtos fitoterapicos para obtencao de um metodo alternativo de controle de larvas de carrapatos, minimizando o uso de produtos sinteticos

the objective of this study was to determine the yield and chemical composition of the essential oils of the dry leaves of four accessions of false pepper tree ( Schinus molle L.) collected at four different sites in the city of Volta Redonda, Rio de Janeiro, Brazil, in four seasons of the year. After hydrodistillation extraction and chemical analysis of the essential oils by GC-FID and GC-MS, bicyclogermacrene and sabinene were found to be the major chemicals in the essential oils obtained during the summer (34.34% and 26.54%), autumn (23.63% and 45.4%) and spring (21.06% and 45.39%), while myrcene and sabinene were the main chemicals found during winter (21.97% and 27.32%) respectively. It was observed that the metabolic profile of Schinus molle has strong influence of seasonality, since this was variable throughout the year.

Fleas and ticks are among the main ectoparasites that affect pets. The indiscriminate and incorrect use of chemical antiparasitics may be related to increased insect resistance and environmental contamination, requiring prospection for active ingredients that are less harmful to animals, humans and the environment. The use of essential oils and their isolated compounds has been reported as a potential alternative to synthetic antiparasitics, but there is a lack of studies involving the design and development of stable and safe natural products-based formulations. Therefore, the aim of this study was to establish LC

Twenty-nine flavonoid glycosides were identified in the aqueous extract (PC) of Petroselinum crispum var. crispum leaves and apiin, the major compound, was isolated thereof. Apigenin was obtained (90% purity) by the hydrolysis of apiin. A high content of phenolics (12.49 ± 1.70 mg GAE per g of parsley extract - Folin-Ciocalteu method) and total flavonoids (15.05 ± 2.20 mg of quercetin equivalents per g of parsley extract - aluminum chloride method) was quantified in P. crispum, as well as high antioxidant activity ((EC50 - 15.50 mg mL-1, DPPH method) and (189.8 mM Fe(ii) per mg of dry plant aqueous extract - FRAP method)). In vivo analysis with Saccharomyces cerevisiae cells showed low toxicity of the aqueous extract of parsley, however, it revealed a high dose-dependent antioxidant potential, mainly in the lipoperoxidation assay. In addition, flavonoid apiin also showed antioxidant action on yeast cells under oxidative stress in the cell viability assay (0.1 mM) and lipid peroxidation (0.01 and 0.1 mM), while apigenin was slightly antioxidant. Therefore, it is likely that the antioxidant activity of apiin is related to the total antioxidant capacity of parsley.

About 17.7 million people die each year from cardiovascular disorders and the essential oils have great importance in the development of research. The aim was to evaluate the chemical composition of the essential oil from Schinus molle (EOSM) and their antihemostatic activity. EOSM was obtained from leaves by hydrodistillation and characterized by GC-FID-MS. Anticoagulant assay was performed by activated Partial Thromboplastin Time (aPTT) and Prothrombin Time (PT) assays, and the platelet aggregation assays were performed using adenosine diphosphate (ADP) and collagen as inducers. Forty-one compounds were identified mainly sesquiterpenes (88.1%) of which epi-α-cadinol (22.8%) and γ-cadinene (9.7%) are the major compounds. EOSM does not showed anticoagulant activity (40-400 mg mL-1). EOSM oil was activity against ADP inducer at 5 mg mL-1 (80%) and 40 mg mL-1 (48%), but against collagen the EOSM did was not activity. This is the first report of antiplatelet action of Schinus molle.

The aim of this study was to evaluate the in vitro activity of Syzygium aromaticum essential oil (SAEO) and its main constituent eugenol (EG) against adult fleas and their action in the maturation of eggs into adults of Ctenocephalides felis felis. In order to evaluate the pulicidal activity, 10 adult fleas were exposed to a filter paper impregnated with SAEO and EG at increasing concentrations of 0.047; 0.094; 0.188; 0.375; 0.750; 1.50; 3.00; 6.00; 12.00 and 24.00 μg cm−2. Flea mortality was evaluated 24 and 48 h after exposure. In order to evaluate the inhibition of the maturation of eggs into adults, 10 eggs were exposed to filter paper impregnated with SAEO and EG at the same concentrations used in the pulicidal test, and the evaluation was performed 30 days after incubation. Untreated repetitions were maintained in both studies (control group). The lethal concentration 50 (LC50) of pulicidal activity to SAEO was 5.70 μg cm−2 in 24 h and 3.91 μg cm−2 in 48 h. The LC90 was 16.10 μg cm−2 and 15.80 μg cm−2 in 24 and 48 h, respectively. The LC50 of inhibition of the maturation of eggs into adults was 0.30 μg cm−2 and the LC90 3.44 μg cm−2. The LC50 of pulicidal activity to EG was 2.40 μg cm−2 in 24 h and 1.40 μg cm−2 in 48 h; the LC90 was 8.10 μg cm−2 and 3.70 μg cm−2 in 24 h and 48 h, respectively. The LC50 of inhibition of the maturation of eggs into adults was 0.10 μg cm−2 and the LC90 0.68 μg cm−2. Based on the results obtained, it is possible to conclude that the both SAEO and EG have in vitro pulicidal activity as well as acting as inhibitors of the maturation of eggs into adults of the flea C. felis felis.

Petroselinum crispum var. neapolitanum Danert (Apiaceae) (PC), popularly known as parsley, is an herb native to the Mediterranean region widely cultivated around the world for culinary and ethnomedicinal purposes. The herb is traditionally used in various parts of the world to treat arterial hypertension, hemorrhoid, nose bleeding, hyperlipidemia, and pain, among other indications. The aim of this study was to evaluate the antithrombotic activity of an aqueous extract PC in rats. Aerial parts of a flat-leaf variety of parsley were extracted by decoction. In vivo thrombosis in rat models as well as ex vivo assays were used in the evaluation of PC antithrombotic effects. Intravenous administration of PC (25 mg/kg.b.w), 5 min before thrombosis induction, reduced the venous thrombus formation by 98.2%, while oral administration (125 mg/kg.b.w) impaired it by 76.2%. In the arterial thrombosis model, the oral administration of PC at 15 or 25 mg/kg.b.w, 60 min before thrombosis induction, increased the carotid artery occlusion time by 150% (37.0 ± 6.44 min) and 240% (more than 60 min), respectively. A HPLC-DAD-MS/MS profile of PC extract used in this study was provided. Apiin showed to be the most abundant phenolic compound in the extract. It also revealed the presence of many coumaric acid derivatives. Our results indicate that PC is a potential candidate for the development of a phytotherapeutic drug in the treatment of thromboembolic diseases and provide a detailed chemical profile useful for controlling PC extract production in view of phytotherapy., Graphical abstract Image 1

According to the World Health Organization (WHO), in the next 20 years there will be 24 million deaths from cardiovascular diseases (CVDs). Current spending on antithrombotic treatment is extremely high. An estimated 17.7 million people died from CVDs in 2015, representing 31% of all global deaths. Of these deaths, an estimated 7.4 million were due to coronary heart disease and 6.7 million were due to strokes. Patent information has been used to study technological trends, new technological potential, as well as decision making in research and development. As an strategic approach to promote research and development (R&D) and to evaluate innovation trends, patent applications can be monitored via patents database. The International Patent Classification (IPC) provides a hierarchical system of language independent symbols for the classification of patents, in a patents database, according to the different areas of technology to which they pertain. To get an overview of the patents focusing on natural products acting as antithrombotic agents, a search strategy was constructed based on keywords, the IPC, and a combination thereof. The aim of this study was to carry out an extensive patent search, using an open (or free) patents database, to collect information on several natural products used as antithrombotic agents, including medicinal plants, vegetables, fruits, spices, edible mushrooms, etc., and their mode of action. The technical aspects covered in this chapter include bioactive plant extracts or herbal formulations with antiplatelet and anticoagulant activities.

Plant extracts and essential oils have been showing potential for use as acaricides. Rhipicephalus sanguineus, the brown tick, mainly parasitizes dogs and is responsible for pathogens transmission. The insecticidal and acaricidal activity of the essential oil (EO) of Syzygium aromaticum and eugenol have already been reported, however the activity against R. sanguineus is lacked. To evaluate the acaricidal activity of S. aromaticum EO and eugenol against larvae of R. sanguineus, in vitro assays were performed using the larval immersion test. Bioassays were performed in duplicate, within the concentration range of 0.078 to 40 mg.mL-1. Mortality assessment was performed after 24 hours. Mortality above 90% was achieved through using the EO and eugenol at concentrations greater than 5 and 10 mg.mL-1, respectively. The LC50 values of 1.4 and 3.3 mg.mL-1 for eugenol and S. aromaticum EO, respectively, while the LC90 values found for eugenol and S. aromaticum EO were, respectively, 6.4 and 6.7 mg.mL-1 were calculated. These compounds present activity against R. sanguineus larvae and demonstrate potential for use as acaricides., Extratos vegetais e óleos essenciais têm apresentado potencial para uso como acaricidas. Rhipicephalus sanguineus, o carrapato marrom, parasita principalmente cães, sendo responsável pela transmissão de patógenos. O óleo essencial (OE) de Syzygium aromaticum e o eugenol já tiveram atividade inseticida e acaricida relatada, porém faltam ensaios que relatem atividade contra R. sanguineus. Com o objetivo de avaliar atividade carrapaticida de OE de S. aromaticum e eugenol frente a larvas de R. sanguineus, foram realizados ensaios in vitro por meio de Teste de Imersão Larval. Os bioensaios foram realizados em duplicata, na faixa de concentração de 0,078 a 40 mg.mL-1. A avaliação da mortalidade foi realizada após 24 horas. Mortalidade acima de 90% foi alcançada para o OE e o eugenol em concentrações superiores a 5 e 10 mg.mL-1, respectivamente. Valores de CL50 de 1,4 e 3,3 mg.mL-1 para eugenol e OE de S. aromaticum, respectivamente, enquanto os valores de CL90 encontrados para eugenol e óleo essencial de S. aromaticum foram, respectivamente, de 6,4 e 6,7 mg.mL-1. Os compostos têm atividade contra larvas de R. sanguineus e demonstram potencial para uso como acaricida.

SUMMARYExtracts and essential oils from plants are important natural sources of pesticides. These compounds are considered an alternative to control ectoparasites of veterinary importance. Schinus molle, an endemic species of Brazil, produces a high level of essential oil and several other compounds. The aim of this work was to determinate the chemical composition of extracts and essential oils of S. molle and further to evaluate the activity against eggs and adults of Ctenocephalides felis felis, a predominant flea that infests dogs and cats in Brazil. In an in vitro assay, the non-polar (n-hexane) extract showed 100% efficacy (800 µg cm−2; LD50 = 524·80 µg cm−2) at 24 and 48 h. Its major compound was lupenone (50·25%). Essential oils from fruits and leaves were evaluated, and had 100% efficacy against adult fleas at 800 µg cm−2 (LD50 = 353·95 µg cm−2) and at 50 µg cm−2 (LD50 = 12·02 µg cm−2), respectively. On the other hand, the essential oil from fruits and leaves was not active against flea eggs. This is the first study that reports the insecticidal effects of essential oils and extracts obtained from Schinus molle against Ctenocephalides felis felis.

This study identified two phenolic compounds in Schinus terebinthifolius Raddi fruits: naringenin (first report in this species) and gallic acid. Their structures were elucidated by nuclear magnetic resonance (NMR) data (1H-, 13C-NMR) and a high-performance liquid chromatography (HPLC) technique. A high content of phenolics (659.21 mg of gallic acid equivalents/g of sample—Folin-Ciocalteau method) and total flavonoids (140.69 mg of rutin equivalents/g of sample—aluminum chloride method) were quantified in S. terebinthifolius, as well as high antioxidant activity (77.47%—2,2-diphenyl-1-picrylhydrazyl, DPPH method). The antihypertensive activity related to its phenolic content was investigated. After intravenous infusion in Wistar rats, these phenolics significantly reduced (p < 0.05) the systolic, median, and diastolic arterial pressures of individuals. The rotarod test was performed to determine the mechanism of action of the sample vasorelaxant effect. It was found that its action exceeded that of the positive control used (diazepam). This confirmed the vasodilatory activity exerted by S. terebinthifolius fruits is related to the phenolic compounds present in the plant, which are potent antioxidants and inhibit oxidative stress, mainly in the central nervous system.

The Lippia alba essential oil has been used for the preparation of cosmetics, which makes important the search for a plant that presents chemical and sensorial properties with greater stability under varying environmental conditions. In this context, the objective of this work was to identify genotypes of L. alba that are stable regarding to essential oil profile in two seasons. For this purpose, we extracted by hydrodistillation and analyzed by GC-FID and GC–MS the essential oils eight L. alba genotypes from plants collected in the summer and winter, to estimate the variation of the metabolites between and within genotypes. Afterwards, the data on geranial and neral concentrations were submitted to analysis of variance (ANOVA) and testing of the means. Then the metabolites data were submitted to the t-test at 5% probability, to compare the two seasons and submitted to cluster analysis by UPGMA. We formulated an index to assess the chemical profile stability according to the genotype, called the Genotype Chemical Profile Stability Index (GCPSI), based on the production of the metabolites between the seasons. All told, 63 metabolites were identified in the essential oil of the genotypes, of which 31 were listed and used as the data for calculating GCPSI. The environment (season) had a stronger influence on the number of metabolites than the total quality of the essential oil. Citral and its isomers geranial and neral were stable during the seasons. In general, the essential oil chemical profile was grouped according to the season. The lowest estimated GCPSI was 84.00% (genotype UFRRJ ECB011) and the highest was 95.40% (UFRRJ ECB005). Of the genotypes evaluated, UFRRJ ECB005 was the most chemically stable. Therefore, we recommend that it be studied regarding its productive potential.

Background: Simira grazielae P. is widely found at Brazil. S. grazielae have been used to treat pain and inflammation in the Northeast of Brazil. Objective: This study investigated the mechanisms of the extract and partitions using pharmacological techniques in mice. Materials and Methods: Male Swiss mice (20–22 g) were used in models of pain (acetic acid-induced abdominal writhing, formalin, and tail-flick tests) and inflammation (edema paw and air pouch tests) as well as in model for the evaluation of motor activity (open field test). Furthermore, we evaluate the probable action mechanism of S. grazielae using naloxone, L-nitro-arginine methyl ester, L-arginine, glibenclamide, atropine, 4-chloro-DL-phenylalanine, and ondansetron in tail-flick test. The cytokines production was also evaluated. The methanolic extract from the S. grazielae and its partitions were administered orally at doses of 10–100 mg/kg. Results: Methanolic extract from the wood of S. grazielae (SGM) and its partitions showed antinociceptive properties in models of acute pain (SGM and ethyl acetate partition [SGMAc]) as well as in models of inflammation (dichloromethane partition [SGMD]). Prior administration of ondansetron and naloxone reduced the antinociceptive effect of SGMAc. SGMD reduced the production of tumor necrosis factor-α (TNF-α) induced by carrageenan. Conclusion: The results show that the anti-inflammatory activity showed by SGMD involves to reduction of the TNF-α, and the antinociceptive activity showed by SGMAc has relation to participation of the serotoninergic receptors and opioid system. These evidence justify the popular therapeutic use of this species in the control of pain and inflammation. Abbreviations Used: PCPA: 4-chloro-DL-phenylalanine, SGM: Methanolic extract of Simira grazielae, SGMAc: Ethyl acetate partition, SGMD: Dichloromethane partition, SGMH: Hexane partition, SGMB: Butanol partition, SGMR: Residual partition, 5-HT: Serotonin, TNF-α: Tumor necrosis factor-α, n-C6H14: Hexane, CH2Cl2: Dichloromethane, EtOAc: Ethyl acetate, BuOH: Butanol, TLC: Thin-layer chromatography, HPLC: High-performance liquid chromatography, DAD: Diode array detector, COX-2: Cyclooxygenase-2, PGE2: Prostaglandin E2, eNOS: Endothelial nitric oxide synthase, NO: Nitric oxide, TRPA 1: Transient receptor potential cation, LT: Latency time, IBL: Increase in baseline, BL: Baseline.

Plant-derived natural products remain an important source of biologically active substances for cancer treatment. The evaluation of the genus Cecropia for cytotoxic activity is still poorly investigated, particularly the specie Cecropia catharinensis, whose study is reported here. This study reports the phytochemical composition of the leaves of C. catharinensis as well as the in vitro evaluation of cell growth inhibition by the crude methanolic extract (CME) and two semi-purified fractions (CME1 and CME2) against three human tumor cell lines: breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and melanoma (A375-C5). The crude methanolic extract CME was obtained by exhaustive extraction of the dried leaves of C. catarinensis . The less polar fraction CME1 was obtained from CME by its treatment with dichloromethane and ethyl acetate. The polar fraction CME2 corresponded to the insoluble residue obtained in the referred treatment. The effects of the crude extract and the two semi-purified fractions were evaluated on the growth of human tumor cell lines according to the procedure adopted by the National Cancer Institute (NCI, USA) in the “ In vitro Anticancer Drug Discovery Screen”. Results were expressed as GI 50 (?g.mL -1 ) values by means ± SD of at least three independent experiments performed in duplicate. CME inhibited the growth of the three human tumor cell lines used in this biological assay. The fraction CME1 was not only active against the panel of cancer cells but also presented the highest inhibitory activity among the three tested samples. The fraction CME2 showed moderate activity against MCF-7 and NCI-H460 cells and was inactive towards A375-C5 cells. These results indicate that Cecropia catarinensis can be considered as a potential source of cytotoxic compounds. To the best of our knowledge, there has been no report on the cytotoxic activity for Cecropia catarinensis . DOI: 10.5935/1984-6835.20160002

Cardiovascular diseases are responsible for the largest number of deaths among humans worldwide, including heart attacks, strokes, and thrombosis. The treatment of thrombosis is generally through the administration of anticoagulant and/or antiplatelet drugs, which have some clinical limitations. Plants synthesize a wide variety of bioactive metabolites in response to different stimuli. This review focuses on a number of molecules of vegetal origin belonging to different chemical classes, with significant anticoagulant and antiplatelet effects. Their promising antithrombotic profile confirms the potential of natural products as a source of lead molecules for drug development in the prevention and treatment of thrombosis.

Essential oils extracted from Schinus molle L. and Schinus terebinthifolius Raddi, Anacardiaceae, leaves and fruit hydrodistillation, as well as, their chemical composition and extraction kinetic were evaluated. For this proposal, 6 h extraction and aliquots collected at sequencing different times (0.5, 1, 2, 4 and 6 h) were carried out allowing calculating accumulated content (% w/w) and verifying essential oil chemical profile. β-caryophyllene (35.2%), α-pinene (28.1%) and germacrene D (15.5%) represent S. terebinthifolius dried leaves essential oil major components, as well as, α-pinene (44.9%), germacrene D (17.6%) and β-pinene (15.1%) in the fruit. Cubenol (27.1%), caryophyllene oxide (15.3%) and spathulenol (12.4%) represent S. molle dried leaves essential oil major components, and β-pinene (36.3%) α-pinene (20.3%), germacrene D (12.1%) and spathulenol in the fruit. Essential oil extraction kinetics showed a hyperbolic distribution; monoterpene content presented exponential decay in time function and sesquiterpene showed exponential growth. Faster monoterpene extraction than the sesquiterpene extraction was observed, however, both presented increasing exponential distribution. Keywords: Essential oil, Hydrodistillation, Terpenes, Schinus genus, Anacardicaceae

Passiflora caerulea L., P. alata Curtis and P. incarnata L. (synonym for P. edulis Sims), are the most popular representatives of the Passiflora genus in South America. In recent years, a growing attention is paid to the biological activity and phytochemical profiles of crude extracts from various species of Passiflora in worldwide. The aim of this study was to evaluate and to compare of anti-leukemic activity of the dry crude extracts from leaves of three Passiflora species from greenhouse of Poland in two human acute lymphoblastic leukemia cell lines: CCRF-CEM and its multidrug resistant variant. Two systems of liquid chromatography in order to assessment of phytochemical composition of extracts were applied. Extracts of P. alata and P. incarnata showed the potent inhibitory activity against human acute lymphoblastic leukemia CCRF-CEM, while P. caerulea not showed activity (or activity was poor). Despite similarities in quality phytochemical profile of extracts from P. caerulea and P. incarnata, differences in quantity of chemical compounds may determine their various pharmacological potency. For the activity of P. alata extract the highest content of terpenoids and a lack of flavones C-glycosides are believed to be crucial. Summarizing, the crude extract from P. alata leaves may be considered as a substance for complementary therapy for cancer patients. Keywords: Passion flower, HPLC-ESI-MSn/UPLC-PDA, Flavones C-glycosides, Terpenoids, Anti-leukemic activity

From the aqueous extract (Pc) of Petroselinum crispum (Mill) flat leaves specimens were isolated and identified the flavonoids apigenin (1), apigenin-7- O-glucoside or cosmosiin (2), apigenin-7- O-apiosyl-(1→2)- O-glucoside or apiin (3) and the coumarin 2″,3″-dihydroxy-furanocoumarin or oxypeucedanin hydrate (4). The inhibitory activity toward clotting formation and platelet aggregation was assessed for Pc flavonoids (1) and (2), and the coumarin (4). Pc showed no inhibition on clotting activity when compared with the control. On the other hand, a strong antiplatelet aggregation activity was observed for Pc (IC50 = 1.81 mg/mL), apigenin (IC50 = 0.036 mg/mL) and cosmosiin (IC50 = 0.18 mg/mL). In all cases ADP was used as inductor of platelet aggregation. Our results showed that Pc, apigenin and cosmosiin interfere on haemostasis inhibiting platelet aggregation. To the best of our knowledge this is the first report for the cosmosiin antiplatelet aggregation in vitro activity.