Modulation of Gut Microbiota, and Morphometry, Blood Profiles and performance of Broiler Chickens Supplemented with Piper aduncum, Morinda citrifolia, and Artocarpus altilis leaves Ethanolic Extracts.

Bioactive plants such as P. aduncum, M. citrifolia, and A. altilis might improve intestinal health as an alternative to antibiotic growth promoters. The objective of this study was to determine the effect of the ethanolic extracts (EEs) of these plants on the intestinal health of broiler chickens. Cobb 500 chickens (n = 352) were distributed into eight treatments with four replicates and 11 chickens each. T1 received a base diet, and T2 received a base diet with 0.005% zinc bacitracin. T3, T5, and T7 were supplemented with 0.005% of P. aduncum, M. citrifolia, and A. altilis EE in the diet while T4, T6, and T8 with 0.01% of the extract. The EEs were supplemented with drinking water from 1 to 26 days of age. The following parameters were evaluated: hematological profiles at 28 days of age, blood metabolites profiles at 14, 21, and 28 days; Escherichia coli, Staphylococcus aureus, and Lactobacillus sp. abundance in the ileum mucosa and content at 21 and 28 days, and histomorphometry of the duodenum, jejunum, and ileum mucosa at 14, 21, and 28 d. Final weight (FW), weight gain (WG), feed intake (FI), and feed conversion rate (FCR) were evaluated at seven, 21, and 33 days of age. M. citrifolia and A. altilis EE at 0.01% increased blood glucose levels at 21 and 28 days of age, respectively, and P. aduncum and M. citrifolia EE at 0.01% increased triglycerides at 28 days of age; in addition, this EE did not have any effect on the AST and ALT profiles. The depths of the Lieberkühn crypts and the villi length to the crypt's depth ratio increased with age on supplementation with 0.01% M. citrifolia and A. altilis EE at 21 days of age (p < 0.05). In addition, the depth of the crypts increased at 28 days of age (p < 0.05) in chickens supplemented with 0.01% A. altilis EE. The 0.01% M. citrifolia EE in diet decreased in the Staphylococcus aureus population in the ileal microbiota (p < 0.05). The FW and WG during the fattening and in the three stages overall increased, and the FCR decreased; however, the FI and the carcass yield did not change in the broiler chickens supplemented with 0.01% M. citrifolia EE (p < 0.05). Conclusively, the M. citrifolia EE at 0.01% of the diet improved intestinal health and thus the performance indices of the broiler chickens and did not have a detrimental effect on any of the parameters evaluated, so it is postulated as a potential alternative to AGP in poultry.

Synergism in Two-Component Insecticides with Dillapiole against Fall Armyworm.

The fall armyworm (Spodoptera frugiperda), a polyphagous insect pest, is a major threat to food production, rapidly spreading through all the tropical areas in the world. Resistance has developed to the control protocols used so far (pyrethroids, organophosphorus, and genetically modified plants), and alternative strategies must be found. The bioactivity in essential oils is usually associated with the major constituents, but synergistic interactions among the constituents (even minor ones) can improve the levels of activity considerably. Herein, we tested the insecticidal activity of several constituents of the essential oil from Piper aduncum, an Amazonian Piperaceae, both separately and as binary mixtures, through their application on the dorsal side of the larva pronotum. Dillapiole proved to be, isolated, the most active compound in this oil (LD50 = 0.35 ppm). In binary mixtures, a strong synergistic effect was observed for the pairs of dillapiole with ß-caryophyllene (LD50 = 0.03 ppm), methyl eugenol (LD50 = 0.05 ppm), and α-humulene (LD50 = 0.05 ppm). In some cases, however, antagonism was recorded, as for dillapiole + ß-pinene (LD50 = 0.44 ppm). The use of binary mixtures of essential oil constituents as low-environmental-toxicity insecticides allows a fine tuning of the insecticidal activity, and the exploitation of synergy effects.

Development, validation and application of a gas chromatography method for the determination of dillapiole from Piper aduncum essential oil in skin permeation samples.

The essential oil extracted from the leaves of Piper aduncum has antifungal, insecticidal and antibacterial activity. Studies with its main compound, dillapiole (DIL) revealed antibacterial and anti-inflammatory potential. Despite all this bioactivity, there is no updated report on the development and validation of analytical and bioanalytical methodology to quantify DIL in skin samples. A selective, precise, accurate and adequate method for the determination of DIL in solutions, porcine ear skin samples and receptor fluid was developed and validated by headspace extraction-gas chromatography with flame ionization detection (HS-GC-FID). HS-GC-FID was applied to determine DIL in Franz cell permeation and retention studies using porcine ear skin samples. In the HS-GC-FID method, matrix-related interferences were not observed at the peak of the DIL retention time. The results showed a high recovery (>97%) after the extraction procedure, allowing the quantification of DIL in complex matrices. In vitro permeation/retention for DIL showed cumulative amounts permeated in the order: receptor fluid (21.98 ± 1.19 µg/cm2 ) > epidermis (15.40 ± 1.20 µg/cm2 ) > dermis (9.52 ± 1.13 µg/cm2 ). HS-GC-FID was successfully validated and the results point to DIL transdermal permeation and to the potential to develop pharmaceutical formulations for skin delivery to treat inflammation or infections.

Piper aduncum Essential Oil Rich in Dillapiole: Development of Hydrogel-Thickened Nanoemulsion and Nanostructured Lipid Carrier Intended for Skin Delivery.

The essential oil extracted from the leaves of Piper aduncum, an aromatic plant from the Amazon region, is rich in dillapiole and presents anti-inflammatory activity. In this study, nanoemulsions (NE) and nanostructured lipid carriers (NLC), which are biocompatible nanostructured systems of a lipid nature, were prepared by high-pressure homogenization for the yet unexplored skin delivery of dillapiole. The addition of hydroxyethylcellulose produced hydrogel-thickened NE or NLC in view to improving the viscosity and skin adherence of the nanoformulations. Formulations were characterized with respect to dillapiole content, droplet size, polydispersity index, zeta potential, morphology, rheological behavior, bioadhesion, skin permeation profile, and in vitro irritancy (HET-CAM). The formulations developed presented spherical, homogeneous nanometric particle size (around 130 nm), narrow polydispersity index (<0.3), and negative zeta potential (around −40 mV). Dillapiole content was slightly lower in NLC compared to NE since the production process involves heating. The hydrogels containing nanocarriers showed pseudoplastic behavior with bioadhesive characteristics. The developed formulations exhibited a controlled release profile, dillapiole delivery up to the dermis, the layer of interest for anti-inflammatory potential, and low irritant potential in the chorioallantoic membrane (HET-CAM). Both hydrogels-thickened NE and NLC seemed to be promising formulations for skin delivery of Piper aduncum essential oil.

Piper aduncum L. (matico) utilizado como tratamiento para el daño pulmonar y Covid-19

Resumen El objetivo principal fue conocer las propiedades antimicrobianas del Piper aduncum L. (matico) para el tratamiento de prevención del Covid-19. El aceite esencial, como los extractos de las hojas y la corteza son muy valiosos como agente cicatrizante, antibacterianos y antifúngico. De esta manera los componentes los flavonoides presentes en el aceite esencial de Piper aduncum L. (matico) fortifican la conectividad de los tejidos mediante la inhibición de algunas de las enzimas que pueden hidrolizar el proteoglicano y la malla proteica, lo cual podría aumentar el efecto antibacteriano al obstaculizar la difusión de la infección al tejido, su actividad antibacterial frente a Staphylococus aureus y Echerichia coli; obteniéndose como resultado que los metabolitos secundarios como flavonoides, compuestos fenólicos, esteroides y alcaloides cuentan con acción antibacterial. La planta del Piper aduncum L. (matico) es un buen cicatrizante y antifúngico se está comercializando como producto farmacéutico en gel. La conclusión que el aceite esencial de Piper aduncum L. (matico) no ayuda a prevenir ni mucho menos a eliminar el nuevo coronavirus y su composición química del matico solo ayuda a prevenir algunas de los síntomas del Covid 19.

Abstract The main objective was to know the antimicrobial properties of Piper aduncum L. (matico) for the prevention treatment of Covid-19. The essential oil, like the extracts of the leaves and the bark, are very valuable as a healing agent, antibacterial and antifungal. In this way, the flavonoid components present in the essential oil of Piper aduncum L. (matico) fortify the connectivity of the tissues by inhibiting some of the enzymes that can hydrolyze the proteoglycan and the protein mesh, which could increase the effect antibacterial by hindering the spread of the infection to the tissue, its antibacterial activity against Staphylococus aureus and Echerichia coli; As a result, secondary metabolites such as flavonoids, phenolic compounds, steroids and alkaloids have antibacterial action. The Piper aduncum L. (matico) plant is a good healing and antifungal agent. It is being marketed as a pharmaceutical gel product. The conclusion that the essential oil of Piper aduncum L. (matico) does not help prevent, much less eliminate the new coronavirus and its chemical composition of the matico only helps prevent some of the symptoms of Covid 19.

Resumo El principal objetivo fue conocer las propiedades antimicrobianas de Piper aduncum L. (matico) para el tratamiento preventivo de Covid-19. El aceite esencial, al igual que los extractos de las hojas y la corteza, son muy valiosos como agente curativo, antibacteriano y antifúngico. De esta forma, los componentes flavonoides presentes en el aceite esencial de Piper aduncum L. (matico) fortalecen la conectividad de los tejidos al inhibir algunas de las enzimas que pueden hidrolizar el proteoglicano y la malla proteica, lo que podría incrementar el efecto antibacteriano al obstaculizar la propagación de la infección al tejido, su actividad antibacteriana contra Staphylococus aureus y Echerichia coli; Como resultado, los metabolitos secundarios como flavonoides, compuestos fenólicos, esteroides y alcaloides tienen acción antibacteriana. La planta Piper aduncum L. (matico) es un buen agente curativo y antifúngico. Se comercializa como un producto farmacéutico en gel. La conclusión de que el aceite esencial de Piper aduncum L. (matico) no ayuda a prevenir, mucho menos eliminar el nuevo coronavirus y su composición química del matico solo ayuda a prevenir algunos de los síntomas de Covid 19.

Piper aduncum essential oil: a promising insecticide, acaricide and antiparasitic. A review.

Several studies have assessed the potential of essential oils as substitutes for synthetic pesticides, in order to counter insect resistance to commercial pesticides. Piper aduncum L. is a very common shrub in the Amazon Rainforest and in other subtropical areas. The objective of this review was to analyse the existing information on P. aduncum essential oil as a raw material for new bioproducts for sustainable pest disease management. With this review, we collected and critically analysed 59 papers, representing all the studies that aimed to evaluate the essential oil properties of this species as an insecticide, acaricide and antiparasitic. The chemical composition differs depending on the origin, although phenylpropanoid dillapiole is the most cited component, followed by myristicin, 1,8-cineole and ß-ocimene. Between the acaricidal, antiparasitic and synergistic activities, the insecticidal effects are highly promising, with optimal results against the malaria vector Aedes aegypti, with an LC50 that ranges between 57 and 200µg/mL. Acaricidal activity has mainly been reported against Tetranychus urticae, showing an LC50 that ranges between 5.83 and 7.17µg/mL. Antiparasitic activity has predominately been found on Leishmania amazonensis, and antipromastigote activity has been found to be between 23.8 and 25.9µg/mL. Concerning the synergistic effect between dillapiole and synthetic insecticides, four studies on Spodoptera frugiperda found promising results with cypermethrin. In this review, we highlighted the potential of P. aduncum essential oil as a biopesticide, also focusing on the lack of information about applied research. We also provide suggestions for future investigations.

TITLE: L'huile essentielle de Piper aduncum: un insecticide, acaricide et antiparasitaire prometteur. Une synthèse. ABSTRACT: Plusieurs études ont abordé le potentiel des huiles essentielles comme substitut aux pesticides de synthèse, afin de lutter contre la résistance des insectes aux pesticides commerciaux. Piper aduncum L. est un arbuste très commun dans la forêt amazonienne et dans d'autres zones subtropicales. L'objectif de ce travail est d'analyser les informations existantes sur l'huile essentielle de P. aduncum comme matière première de nouveaux bioproduits pour une gestion durable des maladies nuisibles. Dans cette synthèse, nous avons collecté et analysé de manière critique 59 articles, représentant toutes les études qui visaient à prouver les propriétés des huiles essentielles de cette espèce en tant qu'insecticide, acaricide et antiparasitaire. La composition chimique diffère selon la provenance, bien que le phénylpropanoïde dillapiole soit le composant le plus cité, suivi de la myristicine, du 1,8-cinéole et du ß-ocimène. À côté des activités acaricide, antiparasitaire et de synergie avec les autres composants, les effets insecticides sont les plus prometteurs, avec des résultats optimaux contre le vecteur du paludisme Aedes aegypti, avec une CL50 comprise entre 57 et 200µg/mL. Une activité acaricide a été principalement rapportée contre Tetranychus urticae avec une CL50 comprise entre 5,83 et 7,17µg/mL. L'activité antiparasitaire a été montrée principalement sur Leishmania amazonensis et l'activité antipromastigote s'est avérée être comprise entre 23,8 et 25,9µg/mL. Concernant l'effet synergique entre le dillapiole et les insecticides synthétiques, quatre études sur Spodoptera frugiperda ont mis l'accent sur des résultats prometteurs avec la cyperméthrine. Avec cette étude, nous avons mis en évidence le potentiel de l'huile essentielle de P. aduncum en tant que biopesticide, en insistant sur le manque d'informations de la recherche appliquée et sur certaines propositions pour de futures recherches.

Acaricidal activity of binary blends of essential oils and selected constituents against Tetranychus urticae in laboratory/greenhouse experiments and the impact on Neoseiulus californicus.

The aim of this study was to test the effectiveness of essential oils form Piper aduncum, Melaleuca leucadendra and Schinus terebinthifolius and their blends by fumigation and residual contact on Tetranychus urticae and its natural enemy, Neoseiulus californicus. Bioassays were performed in a greenhouse with the best blend of the oils and compared to the individual oils and Vertimec® (positive control). The main constituents identified by GC-MS were dillapiole, (E)-nerolidol and limonene in the oils from P. aduncum (76.5%), M. leucadendra (87.3%) and S. terebinthifolius (unripe/ripe fruits, 42.5/34.1%). The P. aduncum and M. leucadendra oils were the most toxic to the pest. Among the blends, the greatest toxicity to T. urticae occurred by residual contact with the M. leucadendra + S. terebinthifolius ripe fruit blend (50/50). The evaluation of the effects on N. californicus showed the compatibility of the oils and blends with the predator mite for use in the integrated management of T. urticae. ß-Caryophyllene was the most toxic, independent of the method used. Based on toxicities of 11 oil constituents, the structure-activity relationship of these compounds is also discussed. This study showed that the acaricidal effect of the Piper, Melaleuca and Schinus oils can easily be increased by the binary combination of these oils. The binary blend between the oils of the Melaleuca leaves and ripe Schinus fruit in the greenhouse was effective at controlling the mite after 72 h, exhibiting the same level of toxicity as that found for the positive control (Vertimec 18 EC).

Antioxidant and Cytoprotective Effect of Piper aduncum L. against Sodium Fluoride (NaF)-Induced Toxicity in Albino Mice.

Piper aduncum, commonly known as matico, is a plant that grows in the mountainous and coastal regions of Peru, and is studied for its antimicrobial properties and various ethnopharmacological uses. The main objective of this study was to determine the cytoprotective and antioxidant effects of the methanolic extract of Piper aduncum leaves in Mus musculus previously administered with sodium fluoride (NaF) using the Micronucleus test and the Comet assay. The extract was administrated orally in four different concentrations: 150, 300, 600, and 1200 mg/Kg for ten days. At the 11th day, a single dose of NaF was administrated via intraperitoneal at 20 mg/Kg. The genotoxicity study was performed with mice from the strain BALB/c, using the Micronucleus test on bone marrow and the Comet assay on peripheral blood according to OECD guidelines 474 and 489, respectively. The statistical analysis was performed by median analysis with ANOVA. Significant differences were found in Micronucleus frequency between the highest concentrations of Piper aduncum and NaF. The Comet assay showed significant reduction of NaF-induced damage on erythrocytes depending on the different concentrations of the extract which were evaluated in this study. It is concluded that the methanolic extract of P. aduncum leaves has cytoprotective and antioxidant activity against sodium fluoride.

Encapsulation of Piper aduncum and Piper hispidinervum essential oils in gelatin nanoparticles: a possible sustainable control tool of Aedes aegypti, Tetranychus urticae and Cerataphis lataniae.

BACKGROUND: The encapsulated essential oils (EOs) of Piper aduncum L. and Piper hispidinervum C. DC. in gelatin nanoparticles were evaluated against Aedes aegypti Linn., Tetranychus urticae Koch and Cerataphis lataniae Boisd. RESULTS: Encapsulation efficiency of the EOs was measured for absolute concentrations of 500 µg mL-1 (79.2 and 72.7%) and 1000 µg mL-1 (84.5 and 82.2%). The loaded nanoparticles were nearly spherical and well dispersed. The nanoparticles loaded with P. hispidinervum EO had an average size of 100 ± 2 nm, while the nanoparticles containing P. aduncum EO ranged from 175 ± 4 to 220 ± 4 nm. According to zeta potential analysis, the nanoparticles loaded with P. hispidinervum and P. aduncum EOs presented values around -43.5 ± 3 and -37.5 ± 2 mV respectively. The controlled release of EOs was described by the anomalous mechanism of Korsmeyer-Peppas. Both encapsulated EOs reached lethal dosages within 24 h of exposure and total mortality of the tested pests. CONCLUSION: The present work successfully developed gelatin-based nanoparticles that served as carriers for the EOs of P. aduncum and P. hispidinervum to be applied as a sustainable control tool of A. aegypti, T. urticae and C. lataniae. The developed loaded nanoparticles presented high encapsulation efficiency and EO concentration release higher than lethal dosages. This indicates that it is feasible to use gelatin-based nanoparticles loaded with P. aduncum and P. hispidinervum EOs to control the tested pests. © 2018 Society of Chemical Industry.

Fixatives Increase the Efficacy of Gel Formulations containing Piper aduncum Linnaeus (Piperales: Piperaceae) Essential Oil as Repellent / Jurnal Sains Kesihatan Malaysia

@#Piper aduncum essential oil exhibit repellency activity and has a potential to be use as an alternative for synthetic repellent such as N,N-diethyl-3- methylbenzamide, (DEET). However, the volatility properties of the essential oil decrease their persistence as a topical repellent. Study has shown that formulation of the essential oil with some fixatives may increase their effectiveness. Therefore, this study was conduct to evaluate the effectiveness of gel formulation containing P. aduncum essential oil with two fixative; vanillin and paraffin oil. Gel formulations containing P. aduncum essential oil with 5% and 10% vanillin and 6% paraffin oil was prepared and tested against Aedes aegypti in laboratory using Standards and Industrial Research Institute of Malaysia (SIRIM) bioassay method. After 240 minute post-application, formulation containing 5% and 10% vanillin was able to provide >70% repellency percentage against mosquito while formulation containing 6% paraffin oil gives <30% repellency percentage. As conclusion, P. aduncum based repellent gel containing 5% and 10% vanillin was able to prolong the effect of P. aduncum essential oil as repellent against dengue vector in laboratory.

Essential Oil from Piper aduncum: Chemical Analysis, Antimicrobial Assessment, and Literature Review.

Background: The challenge in antimicrobial chemotherapy is to find safe and selective agents with potency that will not be compromised by previously developed resistance. Terrestrial plants could provide new leads to antibacterial, antifungal, or antiprotozoal activity. Methods: The essential oil (EO) of Piper aduncum L. (Piperaceae) from Cuba was analyzed by gas chromatography-mass spectrometry (GC-MS). A cluster analysis of P. aduncum EO compositions reported in the literature was carried out. The EO was screened against a panel of microorganisms (bacteria, fungi, parasitic protozoa) as well as for cytotoxicity against human cells. In addition, a review of scientific literature and a bibliometric study was also conducted. Results: A total of 90 compounds were identified in the EO, of which camphor (17.1%), viridiflorol (14.5%), and piperitone (23.7%) were the main components. The cluster analysis revealed at least nine different chemotypes. The EO did not show notable activity against bacteria or fungi, but was active against parasitic protozoa. Conclusions: The results from this study indicate P. aduncum from Cuba is a unique chemotype, support the importance of P. aduncum EOs as medicines, and demonstrate the promise of Cuban P. aduncum EO as a chemotherapeutic agent against parasitic protozoal infections.

Nerolidol, the main constituent of Piper aduncum essential oil, has anti-Leishmania braziliensis activity.

Leishmania (Viannia) braziliensis is a protozoan that causes mucocutaneous leishmaniasis, which is an infectious disease that affects more than 12 million people worldwide. The available treatment is limited, has side-effects or is inefficient. In a search for alternative compounds of natural origin, we tested the microbicidal activity of Piper aduncum essential oil (PaEO) on this parasite. Our data showed that PaEO had an inhibitory effect on the growth of L. braziliensis promastigotes with an IC50/24 h=77·9 µg mL-1. The main constituent (nerolidol: 25·22%) presented a similar inhibitory effect (IC50/24 h = 74·3 µg mL-1). Ultrastructural observation of nerolidol-treated parasites by scanning and transmission electron microscopies revealed cell shrinkage and morphological alterations in the mitochondrion, nuclear chromatin and flagellar pocket. Flow cytometry analysis showed a reduction in the cell size, loss of mitochondrial membrane potential, phosphatidylserine exposure and DNA degradation, which when associated with the morphological changes indicated that nerolidol induced incidental cell death in the L. braziliensis promastigotes. The results presented here indicate that nerolidol derivatives are promising compounds for further evaluation against Leishmania parasites.

Linalool, a Piper aduncum essential oil component, has selective activity against Trypanosoma cruzi trypomastigote forms at 4°C

BACKGROUND Recent studies showed that essential oils from different pepper species (Piper spp.) have promising leishmanicidal and trypanocidal activities. OBJECTIVES In search for natural compounds against Trypanosoma cruzi, different forms of the parasite were incubated for 24 h at 28ºC or 4ºC with Piper aduncum essential oil (PaEO) or its main constituents linalool and nerolidol. METHODS PaEO chemical composition was obtained by GC-MS. Drug activity assays were based on cell counting, MTT data or infection index values. The effect of PaEO on the T. cruzi cell cycle and mitochondrial membrane potential was evaluated by flow cytometry. FINDINGS PaEO was effective against cell-derived (IC50/24 h: 2.8 μg/mL) and metacyclic (IC50/24 h: 12.1 μg/mL) trypomastigotes, as well as intracellular amastigotes (IC50/24 h: 9 μg/mL). At 4ºC - the temperature of red blood cells (RBCs) storage in blood banks - cell-derived trypomastigotes were more sensitive to PaEO (IC50/24 h = 3.8 μg/mL) than to gentian violet (IC50/24 h = 24.7 mg/mL). Cytotoxicity assays using Vero cells (37ºC) and RBCs (4ºC) showed that PaEO has increased selectivity for cell-derived trypomastigotes. Flow cytometry analysis showed that PaEO does not affect the cell cycle of T. cruzi epimastigotes, but decreases their mitochondrial membrane potential. GC-MS data identified nerolidol and linalool as major components of PaEO, and linalool had trypanocidal effect (IC50/24 h: 306 ng/mL) at 4ºC. MAIN CONCLUSION The trypanocidal effect of PaEO is likely due to the presence of linalool, which may represent an interesting candidate for use in the treatment of potentially contaminated RBCs bags at low temperature.

The formulation of the essential oil of Piper aduncum Linnaeus (Piperales: Piperaceae) increases its efficacy as an insect repellent.

The essential oil (EO) of Piper aduncum Linnaeus, known as 'sireh lada' to locals Malaysian, has the potential to be used as an alternative to synthetic insect repellents such as N,N-diethyl-meta-toluamide. However, the EO's efficacy as a repellent decreases after application due to the high volatility of its active ingredients. A number of studies have showed that optimizing the formulation of plant-based EOs can improve their efficacy as repellents. The present study sought to evaluate the effectiveness of 10% P. aduncum EO in ethanol and in three different semisolid formulations: ointment, cream and gel. These formulations were tested on Aedes aegypti under laboratory conditions. Each formulation was applied to the subject's hands, which were then inserted into a cage containing 25 nulliparous A. aegypti. The number of mosquitoes landing on or biting each subject's hand was recorded, and the repellency percentage, landing/biting percentage and protection time for each of the formulations were compared. There were no statistically significant differences between the semisolid EO formulations with regards to the repellency percentage and the landing/biting percentage at 4 h post-application. All three semisolid EO formulations were able to repel >65% of the A. aegypti at 4 h post-application. The EO ointment formulation provided a protection time (182.5 ± 16.01 min) that was statistically significantly longer than that associated with the EO gel formulation (97.5 ± 14.93 min). Meanwhile, the EO cream formulation provided a protection time of 162.5 ± 6.29 min. As the EO cream and ointment formulations displayed better repellent properties than the EO gel formulation, they appear to be the most promising P. aduncum EO formulations to be developed and commercialized as alternatives to synthetic repellents.

Factor de protección solar del extracto hidroalcohólico de hojas de piper aduncum "matico" / Sun protection factor of hydroalcoholic extract of piper leaves aduncum "matico"

El presente trabajo tiene como principal objetivo determinar el factor de protección solar del extracto hidroalcohólico de las hojas de Piper aduncum "matico". Para poder analizar la capacidad fotoprotectora, se recolectó las hojas de Piper aduncum "matico" del jardín botánico de plantas medicinales "Rosa Elena de los Ríos Martínez" de la Facultad de Farmacia y Bioquímica, Universidad Nacional de Trujillo (UNT) por el método de herborización, el extracto se obtuvo por el método de Soxhlet usando como solvente etanol de 70°GL hasta agotamiento de la droga. Se determinó la concentración del extracto mediante el peso del extracto seco/ml de extracto, encontrándose un valor de 0,0155 mg /ml. Las diez muestras de extracto se analizaron en el espectrofotómetro midiéndose las absorbancias por triplicado en la región de la radiación UVB (290-320 nm), principal responsable por los foto-daños cutáneos, según la metodología de comprobación de FPS in vitro descrita por Sayre y por Mansur et al. Quienes en base al efecto eritemogénico (EE) y la intensidad de la radiación (I) calculan el factor de protección solar in vitro. Se concluye que el Factor de Protección Solar promedio de las muestras es 9,32.

Efecto del gel de extracto etanólico de hojas de Piper aduncum en la inflamación inducida en Rattus rattus var. norvegicus / Effect of the ethanolic extract gel of Piper aduncum leaves on the inflammation induced in Rattus rattus var. norvegicus

La inflamación es un proceso tisular que se produce ante una lesión, ya sea debido a bacterias, traumatismos, sustancias químicas, calor o cualquier otro fenómeno. Existen medicamentos que se emplean para aliviar los procesos inflamatorios, los cuales deben ser cuidadosamente valorados, ya que producen una gran variedad de efectos secundarios. Entre los efectos secundarios producidos destacan la patología digestiva, y de forma más reciente se determinó un aumento en la probabilidad de ataque cardiaco o derrame cerebral. Debido a que los efectos secundarios de los medicamentos son difíciles de dilucidar, la medicina tradicional continúa siendo una opción importante. Piper aduncum es una planta a la que se le atribuyen propiedades medicinales, tales como antiséptica y cicatrizante de heridas. Es por ello que el presente trabajo tuvo como objetivo determinar el efecto del gel de extracto etanólico de hojas de Piper aduncum, en la inflamación inducida en Rattus rattus var. norvegicus. Se formaron 5 grupos (Grupo control, grupo patrón y 3 grupos expuestos al gel de extracto etanólico de hojas de Piper aduncum al 1%, 2% y 4%) de 12 especímenes y se indujo inflamación inyectando 1 mL de solución de carragenina al 1% en la zona subplantar de la pata posterior derecha, aplicando posteriormente vía tópica los geles preparados con el extracto etanólico de hojas de Piper aduncum a los grupos problema, empleándose un fármaco (diclofenaco gel) de comparación en el grupo patrón. El gel del extracto etanólico de hojas de Piper aduncum presentó efecto antiinflamatorio, a las concentraciones de 1%, 2% y 4%, en la inflamación inducida en Rattus rattus var. norvegicus. Asimismo, se determinó que no existe diferencia estadísticamente significativa entre el efecto antiinflamatorio de los grupos y del grupo patrón. El efecto antiinflamatorio podría explicarse debido a la concentración de flavonoides presentes en las hojas de Piper aduncum.

Cardamonin, a schistosomicidal chalcone from Piper aduncum L. (Piperaceae) that inhibits Schistosoma mansoni ATP diphosphohydrolase.

BACKGROUND: Schistosomiasis is one of the world's major public health problems, and praziquantel (PZQ) is the only available drug to treat this neglected disease with an urgent demand for new drugs. Recent studies indicated that extracts from Piper aduncum L. (Piperaceae) are active against adult worms of Schistosoma mansoni, the major etiological agent of human schistosomiasis. PURPOSE: We investigated the in vitro schistosomicidal activity of cardamonin, a chalcone isolated from the crude extract of P. aduncum. Also, this present work describes, for the first time, the S. mansoni ATP diphosphohydrolase inhibitory activity of cardamonin, as well as, its molecular docking with S. mansoni ATPDase1, in order to investigate its mode of inhibition. METHODS: In vitro schistosomicidal assays and confocal laser scanning microscopy were used to evaluate the effects of cardamonin on adult schistosomes. Cell viability was measured by MTT assay, and the S. mansoni ATPase activity was determined spectrophotometrically. Identification of the cardamonin binding site and its interactions on S. mansoni ATPDase1 were made by molecular docking experiments. RESULTS: A bioguided fractionation of the crude extract of P. aduncum was carried out, leading to identification of cardamonin as the active compound, along with pinocembrin and uvangoletin. Cardamonin (25, 50, and 100 µM) caused 100% mortality, tegumental alterations, and reduction of oviposition and motor activity of all adult worms of S. mansoni, without affecting mammalian cells. Confocal laser scanning microscopy showed tegumental morphological alterations and changes on the numbers of tubercles of S. mansoni worms in a dose-dependent manner. Cardamonin also inhibited S. mansoni ATP diphosphohydrolase (IC50 of 23.54 µM). Molecular docking studies revealed that cardamonin interacts with the Nucleotide-Binding of SmATPDase 1. The nature of SmATPDase 1-cardamonin interactions is mainly hydrophobic and hydrogen bonding. CONCLUSION: This report provides evidence for the in vitro schistosomicidal activity of cardamonin and demonstrated, for the first time, that this chalcone is highly effective in inhibiting S. mansoni ATP diphosphohydrolase, opening the route to further studies of chalcones as prototypes for new S. mansoni ATP diphosphohydrolase inhibitors.

Antibacterial activity of the Piper aduncum oil and dillapiole, its main constituent, against multidrug-resistant strains / Actividad antibacteriana del aceite de Piper aduncum y dillapiole, su componente principal, frente a cepas resistentes a múltiples fármacos

The study aimed to evaluate the bactericidal activity of oil essential and dillapiole from P. aduncum against standard and multidrug-resistant strains of Staphylococcus spp. The oil showed antimicrobial action against these strains, but better results were obtained for the standards strains of S. epidermidis and S. aureus, with MIC of 250 and 500 ug/mL, respectively. Dillapiolle was less effective than the oil against the same standard and multi-drug resistant strains (MIC =1000 ug/mL). However, when dillapiolle was tested in combination with myristicin, another component of the oil, it increased its bactericidal activity and showed a synergistic action...

El objetivo del estudio fue evaluar la actividad bactericida de los aceites esenciales y dillapiole de P. aduncum contra cepas estándar y multirresistentes de Staphylococcus spp. El aceite mostró acción antimicrobiana frente a estas cepas, pero se obtuvo mejores resultados para las cepas de S. epidermidis y S. aureus, con MIC de 250 y 500 ug/ml, respectivamente. Dillapiolle fue menos eficaz que el aceite contra cepas estándar y multirresistentes (MIC = 1000 ug/ml). Sin embargo, cuando dillapiolle fue probado en combinación con la miristicina, otro componente del aceite, que aumentó su actividad bactericida y mostró una acción sinérgica...

Antileishmanial activity evaluation of adunchalcone, a new prenylated dihydrochalcone from Piper aduncum L.

Bioactivity-guided fractionation of EtOH extract from the leaves of Piper aduncum L. (Piperaceae) afforded a new dihydrochalcone, named adunchalcone. Its structure was elucidated on the basis of their spectroscopic data, primarily NMR and MS. Adunchalcone was evaluated against promastigote forms of Leishmania (L.) amazonensis, L. (V.) braziliensis, L. (V.) shawi, and L. (L.) chagasi and displayed 50% effective concentrations (EC50) of 11.03, 26.70, and 11.26 µM, as well as selective indexes of 4.86, 2.01, 4.76 and 0.50, respectively. This compound was also tested against intracellular forms of L. (L.) amazonensis, displaying weak activity, in comparison to reference drug amphotericin B. However, despite reduced effect of adunchalcone against amastigotes of L. (L.) amazonensis, this work opens the perspective to use this particular molecule as a scaffold for the design of novel and selective drug candidates for neglected diseases, mainly leishmaniasis.

Efecto antitumoral in vitro del aceite esencial de Piper aduncum L. (matico) y su toxicidad oral en ratones / Piper aduncum L. (matico) essential oil in vitro antitumoral effect and oral toxicity in mice

Introducción: Piper aduncum (matico) es una especie utilizada por sus propiedades medicinales en desórdenes gastrointestinales y genitourinarios. Objetivos: Evaluar el efecto antitumoral del aceite esencial de Piper aduncum (matico) in vitro en siete líneas celulares tumorales humanas y determinar la toxicidad oral en ratones. Diseño: Experimental. Institución: Facultad de Medicina, Universidad Nacional Mayor de San Marcos, Lima, Perú. Material biológico: Líneas celulares tumorales humanas H460, DU-145, ME-180, K562, HT-29, MCF 7, M14, K562; fibroblastos normales de ratón 3T3 y ratones albinos machos Balb/C53. Intervenciones: Las líneas celulares fueron expuestas a cuatro concentraciones del aceite esencial de P. aduncum y 5-fluorouracilo (5-FU). Para la toxicidad oral se utilizó ratones albinos machos Balb C/53 de 40 días post destete, a cinco dosis de tratamiento, evaluándose el número de muertes en cada dosis. Principales medidas de los resultados: Porcentaje de inhibición del crecimiento celular (IC50), dosis letal 50 (DL50). Resultados: El aceite esencial mostró IC50 mayor a 250 ug/mL para las líneas celulares M-14 (r = -0,99; p < 0,01), DU-145 (r = 0,99; p < 0,01), ME-180 (r = -0,99; p < 0,01). Para líneas celulares tumorales H460 (r = -0,99; p < 0,01), MCF-7 (r = -0,99; p < 0,01), K562 (r = -0,99; p < 0,01), HT-29 (r = -0,99; p < 0,01), los niveles de IC50 estuvieron entre 20 ug/mL y 250 ug/mL. DL50 > 2 000 mg/kg. Conclusiones: El aceite esencial de P. aduncum no presentó efecto antitumoral in vitro para las siete líneas celulares tumorales humanas y no fue tóxico.

Introduction: Piper aduncum (matìco) is a medicinal plant used for gastrointestinal and genitourinary disorders. Objectives: To determine the in vitro antitumoral effect of Piper aduncum (matico) essential oil on seven human tumoral cell lines and its oral toxicity in mice. Design: Experimental. Setting: Faculty of Medicine, Universidad Nacional Mayor de San Marcos, Lima, Peru. Biologic material: Human tumoral cell lines HT-29, H-460, MCF-7, M-14, ME-180, DU-145, K-562; and 3T3 fibroblasts and male 40 days post weaning Balb C/53 mice. Interventions: The cell lines HT-29, H-460, MCF-7, M-14, ME-180, DU-145, K-562, and 3T3 were exposed to four different concentrations of Piper aduncum essential oil, and to different 5-fluorouracil concentrations used as a positive control. Cell lines growth inhibition (IC50) was determined using linear regression analysis and DL50 by the number of deaths with each dose. Main outcome measures: Antitumor effect. Results: Piper aduncum essential oil showed cytotoxic activity at IC50 levels > 250 ug/mL on cell lines M-14 (r = -0.99; p < 0.01), DU-145 (r = -0.99; p < 0.01), ME-180 (r = -0.99; p < 0.01). IC50 was between 20 ug/mL and 250 ug/mL on cell lines H-460 (r = -0.99; p < 0.01), MCF-7, (r = -0.99; p < 0.01), K562 (r = -0.99; p < 0.01), HT-29 (r = -0.99; p < 0.01). DL50 was > 2 000 mg/kg. Conclusions: P. aduncum essential oil did not show antitumoral effect on seven human tumoral cell lines and it was non toxic.