Potencialidade acaricida sobre Rhipicephalus (Boophilus) microplus e estudo fitoquímico de Piper aduncum L. (Piperaceae), Palicourea marcgravii St. Hil (Rubiaceae) e Derris negrensis Benth (Fabaceae)

O carrapato Rhipicephalus (Boophilus) microplus é um ectoparasita que causa prejuízos econômicos à pecuária brasileira. Neste trabalho foi avaliada a potencialidade de extratos de Palicourea marcgravii e Derris negrensis e de extratos e óleo essencial de Piper aducum para o controle de R. microplus. Extratos de folhas de P. aduncum e P. marcgravii e caules de D. negrensis foram preparados com os solventes hexano, acetato de etila e etanol. Avaliou-se a atividade dos extratos sobre carrapatos adultos nas concentrações de 5, 25, 50, 75 e 100mg/ml, a fim de verificar a mortalidade e reprodução dos ácaros, observando-se que entre os extratos das três espécies avaliadas, o que apresentou maior potencial acaricida foi o extrato acetato de etila de P. marcgravii, o qual ocasionou taxas de mortalidade de fêmeas ingurgitadas entre 24 e 78%, estimando CL50 = 30,08 mg/ml; inibiu 100% da oviposição, estimando CI50 = 5,79 mg/ml. Avaliou-se, também, o efeito dos extratos das três plantas nas concentrações de 1,5, 10, 15 e 20mg/ml sobre larvas de R. microplus, verificando-se que o extrato acetato de etila de P. marcgravii foi o mais eficiente induzindo taxas de mortalidade que variaram de 30,32 a 95,11%, estimando CL50 = 2,46 mg/ml. A ação do óleo essencial de P. aduncum foi avaliada também em larvas, induzindo a mortalidade total das mesmas em todas as concentrações avaliadas. O óleo essencial foi analisado por Cromatografia Gasosa (CG) e Cromatografia Gasosa acoplada a Espectro de Massas (CG/EM) apresentando o dilapiol como composto majoritário(94,84%). Os extratos de D. negrensis não estimaram CL50 para fêmeas ingurgitadas e larvas de R. microplus. Estes resultados indicam a potencialidade acaricida dos extratos de P. marcgravii e do óleo essencial de P. aduncum, podendo ser uma alternativa de controle contra essa espécie de carrapato.The tick Rhipicephalus (Boophilus) microplus is an ectoparasite that cause economic losses to brazilian livestock. In this work, it was evaluated the toxicity of Palicourea marcgravii and Derris negrensis extracts and Piper aduncum extracts and essential oil for R. microplus. Extract of leaves of P. aduncum and P. marcgravii and stems of D. negrensis were prepared with hexane, ethyl acetate and ethanol solvents. The extracts activity was evaluated on adult ticks at concentrations of 5, 25, 50, 75 and 100 mg/ml, in order to verify mortality and reproduction of the acarids, being observed that among the extracts of three species evaluated, one that showed higher acaricidal potential was the ethyl acetate extract of P. marcgravii, which caused mortality rates of engorged female between 24 and 78%, estimating CL50 = 30,08 mg/ml; it have inhibited 100% of the oviposition, estimating CI50 = 5,79 mg/ml. It was evaluated too the extracts effect of the three plants at concentrations of 1, 5, 10, 15 and 20 mg/ml on R. microplus larvae, verifying that the P. marcgravii ethyl extract was more efficient inducing mortality rates that ranged from 30,32 to 95,11%, estimating CL50 = 2,46 mg/ml. The action of P. aduncum essential oil was evaluated on larvae too, inducing the total mortality of the same ones in all concentrations evaluated. The essential oil was analyzed by Gas Chromatography (GC) and Gas Chromatography coupled Mass Spectrum (GC/MS) showing dilapiol as the major compound (94,84%). The D. negrensis extracts didn t estimate CL50 for engorged female and larvae of R. microplus. These results indicate the acaricidal potential of the P. marcgravii extracts and P. aduncum essential oil, and could be an alternative of control against that tick species

Isolation and Identification of Bioactive Secondary Metabolites

The health benefits of food, plants, fruits, and seaweeds stem from the biological activities of their constituents—namely, secondary metabolites. The study of secondary metabolites and their potential to treat and/or prevent a number of diseases has become a research topic of growing interest for biologists, pharmacists, and chemists. Notably, in order to propose a compound as a potential new drug with pharmacological effects, the chemical structure of this compound and its biological activity against a given target must be well established. The Special Issue, “Isolation and Identification of Bioactive Secondary Metabolites”, considers species beyond their nutritional value and identifies instances of wider and more efficient use, thereby contributing to a more sustainable management of natural resources. The fifteen articles published in this Special Issue reflect the latest research trends, and consider the isolation, identification, and assessment of the beneficial effects of secondary metabolites from both edible and inedible species. Thus, these contributions collectively demonstrate that these compounds, and their plants of origin, should be valued beyond their nutritional benefits

Estudos agronômicos e fitoquímicos de Piper hispidinervum C.DC. e Piper aduncum L. para produção de safrol e dilapiol.

A família Piperaceae é reconhecida como aromática sendo o gênero Piper o mais representativo desta família. Das mais de 700 espécies deste gênero, destacam-se a Piper hispidinervum C.DC. (pimenta longa) e a Piper aduncum L. (pimenta-demacaco) como produtoras de safrol e dilapiol respectivamente, compostos usados na indústria de cosméticos, perfumaria e no controle de pragas e doenças de interesse agropecuário. A P. hispidinervum poderá substituir a planta originalmente fornecedora de safrol no Brasil, a canela sassafrás. Essas espécies se encontram em processo de domesticação e estudos sobre seu cultivo são escassos. Objetivando a produção de óleo essencial com alto teor de safrol e dilapiol, nas condições edafoclimáticas do litoral paranaense, e contribuir para o conhecimento da diversidade de Piper sp em remanescente de Floresta Atlântica no município de Morretes/PR, foram identificadas as seguintes espécies locais: P. aduncum L., P. cernuum Vell., P. dilatatum Rich, P. gaudichaudianum Kunth, P. glabratum Kunth, P. lindbergii C. DC., P. solmsianum C. DC. e P. umbellatum L. Estas oito espécies representam 34% das 23 reportadas de ocorrência no Paraná. De novembro de 2007 a junho de 2009, no mesmo município, dois experimentos foram conduzidos, ambos em blocos casualizados, em esquema fatorial. No primeiro, com a espécie P. hispidinervum, combinaram-se espaçamentos (0,5; 1,0 e 1,5 m) entre plantas e épocas de corte (9, 12 e 15 meses após o plantio). As melhores épocas de colheita foram aos 12 ou 15 meses num espaçamento de 0,50 x 0,50 m entre plantas. Nestas condições de manejo, obtém-se uma produtividade acima de 94 litros de OE por hectare, com teor mínimo de safrol de 91%. No segundo, com a espécie P. aduncum, no espaçamento 1,0 x 1,0 m, combinaram-se épocas de corte (9, 12, 15 e 18 meses após o plantio) e procedências do Acre e Paraná. A procedência Acre apresenta um rendimento maior de OE na massa seca quando comparada à do Paraná. A melhor época de colheita para a P. aduncum, procedência Acre, é aos 18 meses, com produtividade estimada de 83 litros de OE por hectare e teor médio de dilapiol de 78%. A presença majoritária do dilapiol no OE da procedência Acre e a ausência na procedência Paraná caracterizam quimiotipos distintos. Conclui-se pelos estudos agronômicos e fitoquímicos das espécies P. hispidinervum e P. aduncum que a produção de safrol e dilapiol é tecnicamente viável, desde que em condições fisiográficas específicas, a exemplo do município de Morretes/PR.Tese (Doutorado em Produção Vegetal) - Departamento de Fitotecnia e Fitossanitarismo, Universidade Federal do Paraná, Curitiba. Orientador: Luiz Antonio Biasi

Estudo fitoquímico e biológico da Piper solmsianum C.DC. variedade solmsianum (Piperaceae)

Tese (doutorado) - Universidade Federal de Santa Catarina, Centro de Ciências Físicas e Matemáticas. Programa de Pós-Graduação em Química.O presente trabalho envolveu processos de extração, isolamento, purificação e identificação dos constituintes químicos das folhas de outono da Piper solmsianum. Da fração hexânica foram isoladas três neolignanas benzofurânicas denominadas de euponatenóide-3, eupomatenóide-5 e conocarpano. Da fração diclorometano foi isolado o conocarpano. Na fração acetato de etila foram detectados as flavonas 7- metoxi-apigenina (genkwanina) e a orientina e duas flavanonas hesperidina e iluteolina-7-rutinosídeo. O conocarpano foi submetido a reações de metilação, benzoilação e acetilação e obteve-se os derivados: conocarpano metilado, conocarpano benzoilado e conocarpano acetilado, os quais foram avaliados quanto ao potencial analgésico e observou-se que o conocarpano cetilado foi mais ativo que os demais. Por reações de dimerização oxidativa do isoeugenol obteve-se dois análogos ao conocarpanp o a-di-isoeugenol e o diidrodiisoeugenol, os quais demonstra

From ethnomedicine to pharmaceutical biology through Cooperation projects: a cultural and research bridge between Africa and Amazonia

BACKGROUND: This research has its background in Cooperation and Development projects, organized and sponsored by University of Ferrara. In this context, four Amazonian essential oils (i.e. Ocimum micranthum, Cimbopogon citratus, Curcuma longa, Zingiber officinale) and Rwandese avocado oil (Persea americana) extracted both by hexane maceration (HM) and supercritical fluid extraction (SFE), have been explored for their chemical and biological properties, with the target to employ these derivates as formulations (blended essential oils). AIMS: The research has been focused on: o checking best and easy handling extraction technology to transfer to Developing Countries (essential oils and avocado fixed oil); o chracterizing phytochemically these natural derived products o confirming safety and assaying biological activities; o suggesting an easy handling formulation which could give economic relapses to Developing Counties

Chemical transformation and phytochemical studies of bioactive constituents from extract of callistemon citrinus (curtis) skeels

Callistemon citrinus belongs to the family Myrtaceae and exhibits therapeutic activities. The aerial parts of this plant are used to treat different ailments, among them are parasitic infections. The leaves, flowers and stems of Callistemon citrinus were subjected to hydrodistillation. The oils collected were studied by GC-MS analysis for the essential constituents. The overall phenolic content of the leaves oil, radical scavenging, antibacterial action and antioxidant activities of the essential oils of Callistemon citrinus were determined using standard methods, with free radical DPPH or ABTS as reference antioxidants. Chemical transformation of the components was examined for a whole year. A relationship between the chemical change in the volatile oil constituents, antioxidant capacity, percentage yield of the oil of Callistemon citrinus and fluctuation in season has been established. Active phytochemicals present in both ethyl acetate and methanolic extracts of Callistemon citrinus were determined spectrophotometrically. The antimicrobial properties, time of kill, and antioxidant activity of the extracts were explored. The bioactive components were characterized by high level of fatty acids. Squalene, a triterpenoid synthesized in human liver was obtained in the two extracts at varying amounts. The ethyl acetate extract demonstrated strong activity against P. aeruginosa ACC (28.7 ± 1.2 mm), Listeria ACC (26.0 ± 2.0 mm) and Escherichia coli ATCC 35150 (24.0 ± 3.5 mm). Qualitative phytochemical screening revealed the presence of alkaloids, glycosides, saponins, steroids and triterpenoids, fats and oils, flavonoids, phenols and tannins in them. In the quantitative phytochemical determination (total tannin, total flavonoids and flavonols, total phenolic and total antioxidant capacity) were carried out. The minimum time needed to kill the tested bacterial strains totally ranged from 15 to 24 hours. The aqueous extracts used for biosynthesis of nanoparticles were obtained from the fresh aerial parts of the plant. The biosynthesized gold and silver nanoparticles (AuNPs and AgNPs) of the aqueous extracts of the seed, flower and leaf of the plant, which are active as reducing and capping agents, were characterized using UV-VIS spectrophotometry, XRD, SEM, EDS, TEM, and FT IR. The XRD analysis revealed that the AgNPs were crystalline and the TEM showed that the shapes were spherical with an average size of 29 nm. For AuNPs, an average particle size of about 37 nm was confirmed by the TEM while the morphology and composition of the AuNPs were ascertained by SEM and EDS micrographs; uneven spherical shaped nanoparticles were established by the SEM. Both SEM and EDS demonstrated triangular shaped materials made up of silver and oxygen only. Absorption spectra confirmed by UV-VIS signify the dispersed nature of the synthesized nanoparticles with absorption band observed at 280 nm for the leaf AgNPs. FT IR had absorption bands at about 1700 cm-1 establishing the C=O stretching due to the amide bond while the FT IR for the AuNPs showed an absorption peak at 230 cm-1 confirming the presence of gold nanoparticles. The phytochemical investigation, isolation and characterization of the bioactive compounds of various organic crude extracts like hexane, dichloromethane, methanol and ethyl acetate were as well carried out, and the compounds responsible for their medicinal actions were determined. The results from different experiments revealed that the leaves and flowers of Callistemon citrinus possessed phenolic compounds and cyclic ethers with a variety of pharmacological action. The ethyl acetate and methanol crude extracts were found to possess broad spectrum of antimicrobial activities and pharmaceutically essential bioactive components with striking antioxidant capacities that may be used in the synthesis of novel drugs for the management of different ailments. The AuNPs and AgNPs synthesized from the seed, flower and leaf extracts of Callistemon citrinus where found to have prominent antimalarial, antiplasmodial, and antibacterial activities. The biosynthesized nanoparticles inhibit all the bacterial strains used and they were not cytotoxic to Hela cells, confirming their prospect for use as an excellent source for naturally occurring drugs against malaria, cell cytotoxicity, trypanosomes, and microbial infection. Similarly the crude organic extracts and the fractions derived from them exhibited high antimalarial and antitrypanosomal activities, but they were toxic to Hela cells. This is an indication that they will not be safe for use as targeted drugs for mammalian organism

The potential role of Peperomia pellucida (l.) Kunth in ameliorating hyperglycaemic and glycation-induced inflammation in human retinal pigment epithelial cell line (ARPE-19)

Diabetic retinopathy (DR) is a microvascular complication that causes blindness. DR management is costly and accompanied with adverse effects. Peperomia pellucida (L.) Kunth is traditionally used for inflammation, but its effects on DR remain unexplored. This study aimed to elucidate the regulatory mechanism of P. pellucida against high glucose and glycation induced stress in human retinal pigment epithelial cell line (ARPE-19). P. pellucida was macerated with methanol, and fractionated with hexane, chloroform, ethyl acetate, n-butanol and water. Semi-quantitative colorimetric assays indicated that the ethyl acetate plant fraction demonstrated potent antioxidant, anti-inflammatory and anti-glycation activities, alongside significant (p<0.05) higher α-amylase and α-glucosidase inhibitory activities when compared to the standard anti-diabetic drug, acarbose. Both ethyl acetate fraction and crude methanolic plant extract significantly (p<0.05) restored the ARPE-19 cell viability under high glucose and glycation stress. High glucose and glycation induced the nuclear factor kappa B (NF-κB) p65 and signal transducer and activator of transcription 3 (STAT3) signalling pathways with significant (p<0.05) increase of gene (1.22-31.30 folds) and protein (1.39-7.79 folds) expression for angiogenic and inflammatory markers, including interleukin 8 (IL-8), matrix metalloproteinase 2, monocyte chemoattractant protein 1, receptor for AGE, and vascular endothelial growth factor in ARPE-19, as determined via reverse transcription real-time polymerase chain reaction and western blot. Conversely, the gene and protein (0.12-0.56 folds) expression of glutathione peroxidase were significantly reduced due to the suppression of peroxisome proliferator-activated receptor gamma (PPAR-γ). P. pellucida did not alter the biomarkers’ gene and protein expression under normal glucose condition except for IL-8 (0.75-0.89 folds). Although in vivo brine shrimp toxicity analysis revealed that crude methanolic extract and ethyl acetate fraction were mildly toxic, in vitro cell viability findings showed that they were non-cytotoxic towards ARPE-19. Dillapiole, 2,4,5-trimethoxystyrene, β-caryophyllene, β-santalene, methyl 9-octadecenoic acid and methyl pheophorbide-a were among the predominant phytochemicals identified in the crude methanolic extract via spectroscopic and spectrometric techniques. Notably, methyl pheophorbide-a was identified for the first time in P. pellucida. The current findings support P. pellucida as an alternative therapeutic source to mitigate high glucose and glycation-induced stress in DR by regulating the NF-κB p65, PPAR-γ and STAT3 signalling pathways