Copaiba Oil: An Alternative to Development of New Drugs against Leishmaniasis

Leishmaniasis is a neglected disease that is increasing globally at an alarming rate. Glucantime has been the therapy of choice for more than 50 years. A recent study reported the antileishmanial activity of copaiba oil against Leishmania amazonensis. These results led us to investigate morphological and ultrastructural changes in L. amazonensis treated with copaiba oil, using electron microscopy and flow cytometry to assess specific organelles as targets for copaiba oil. In the promastigote and axenic amastigote forms, this copaiba oil caused notable morphological and ultrastructural changes, including extensive mitochondrial damage and denaturation of the plasma membrane. Copaiba oil treatment also induced a decrease in Rh123 fluorescence, suggesting interference with the mitochondrial membrane potential and loss of cell viability with an increase in plasma membrane permeability, as observed by flow cytometry after staining with propidium iodide. In conclusion, copaiba oil could be exploited for the development of new antileishmanial drugs

Atividades antioxidante e antifúngica de extratos e taninos condensados de Stryphnodendron obovatum Benth.

The antioxidant activity of stem-bark extracts from Stryphnodendron obovatum Benth., including fractions and isolated compounds, was evaluated by DPPH in thin-layer chromatography. All the fractions and isolated compounds showed antioxidant activity. Antifungal activity was determined by the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) against the yeasts Candida albicans, Candida parapsilosis, Candida krusei and Candida tropicalis. All extracts (CE, EtOAc and FW), subfractions (F1-F12) and the compounds I, II and III were inactive against the yeasts. Against C. parapsilosis and C. albicans, fractions F13-15 and F20 showed moderate antifungal activity, and fractions F16-19 and F21-22 showed good activity. Chemical isolation of the ethyl-acetate fraction resulted in the identification of three compounds: epigallocatechin, gallocatechin and epigallocatechin-(4;b®;8)-gallocatechin.Atividade antioxidante de extrato, frações, subfrações e substâncias isoladas das cascas de Stryphnodendron obovatum Benth. foi avaliada através da redução do radical 1,1-difenil-2-picrilhidrazila (método DDPH·) em cromatografia em camada delgada. O extrato bruto (CE, acetona:água), as frações acetato de etila (EtOAc) e aquosa (FW), as subfrações (F1-F12) e as substâncias isoladas I, II e III apresentaram a capacidade de reduzir o radical DDPH·. A atividade antifúngica foi determinada pela concentração inibitória mínima (CIM) e concentração fungicida mínima (CFM) frente às amostras de leveduras Candida albicans, Candida parapsilosis, Candida krusei e Candida tropicalis. O extrato bruto (CE), as frações (EtOAC e FW), e os compostos isolados I, II e III, como também as subfrações cromatográficas (F1-F12) foram inativos frente a todas as leveduras testadas. Por outro lado, as subfrações cromatográficas F13-15 e F20 apresentaram atividade antifúngica moderada. Já as subfrações F16-19 e F21-22 mostraram boa atividade antifúngica frente às cepas de C. albicans e C. parapsilosis. As substâncias I, II, e III, isoladas da fração EtOAc por cromatografia e recromatografia em coluna de Sephadex® LH-20, foram identificadas como sendo os monômeros de flavan-3-ol, epigalocatequina e galocatequina, e um dímero, epigalocatequina-(4;b®;8)-galocatequina, respectivamente

Análise por CG-EM do óleo essencial de Calendula officinalis cultivado no Brasil utilizando-se três diferentes processos de extração

Terpenos e aromas voláteis das flores de Calendula officinalis cultivados no sudoeste do Brasil foram isolados por arraste a vapor (SD), dedo frio (HS-CF) e micro extração em fase sólida (HS-SPME) acoplada à espectrometria de massas. As flores secas da C. officinalis contêm 0,1% de óleo essencial e foram identificadas 27 substâncias químicas através do cálculo do índice de Kováts e interpretação dos espectros de massas. As substâncias majoritárias presentes no óleo essencial das flores de C. officinalis, obtido por SD, HS-SPME e HS-CF foram δ-cadinene (22,5; 22,1 e 18,4 %) γ-cadinene (8,9, 25,4 e 24,9 %) e 20.4 % de α-cadinol foi observado apenas na extração por arraste a vapor.Terpenes and aroma volatiles from flowers of Calendula officinalis cultivated in southeastern Brazil were obtained by steam distillation (SD), headspace-cold finger (HS-CF) extraction and headspace solid-phase microextraction (HS-SPME) coupled with gas chromatography and mass spectrometric analysis. The dried flowers contained 0.1% oil. Kovats indices and mass spectra were used to identify 27 individual components in the various volatile fractions. The main components present in the volatile fractions of the C. officinalis flowers, obtained by SD, HS-SPME, and HS-CF, were δ-cadinene (22.5, 22.1, and 18.4 %) and γ-cadinene (8.9, 25.4, and 24.9 %) while 20.4 % of α-cadinol was seen only after SD extraction

Effect of 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[3,4-b]indole-3-carbohydrazide on in vitropoliovirus replication

The effect of the alkaloid, 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[3,4-b]indole-3-carbohydrazide (PMC)on poliovirus (PV) replication cycle in Vero cells was assayed by inhibition of the cytopathic effect (CPE) and inhibition of plaque forming units (PFU). Both methodologies suggested that the mode of action was avoidance of infection progression in the host cell. The compound was able to prevent CPE and PFU formation when the cells were pretreated with PMC for 24 h prior to PV infection. In addition, when the alkaloid was continuously maintained in the infected cultures, the spread of PV to adjacent cells was impaired. The pre-exposure and post-exposure prophylactic applications are possible situations in which an anti-PV drug might be used. Future studies are needed to elucidate the PMC mode of action and verify the feasibility of PMC use of in vivo. No antipicornavirus agent is currently approved for clinical use

n vitro Antileishmanial Activity of Hydroalcoholic Extract, Fractions, and Compounds Isolated from Leaves of Piper ovatum Vahl against Leishmania amazonensis

We assessed the biological activity of a crude extract, a mixture of several fractions, and a pure compound obtained from Piper ovatum Vahl against promastigote and amastigote forms of Leishmania amazonensis. The medicinal plant P. ovatum is used popularly as an anesthetic and anti-inflammatory. This study included the extraction process and bioassay-guided fractionation by the adsorption chromatography and Sephadex LH-20 method. A progressive increase in the antileishmanial effect was observed in the course of fractionation. The 50% inhibitory concentration (IC50) for dichloromethane-ethyl acetate (1:1 v/v) fraction was 2.1 μg/ml and 24 μg/ml; mixture of piperovatine: piperlongumune (2:3) 0.9 μg/ml and 24 μg/ml; piperovatine (1) 9.5 μg/ml and 10 μg/ml; and piperlonguminine (2) 2.5 μg/ml and 9.0 μg/ml, for promastigote and amastigote forms, respectively. Cytotoxicity analysis indicated that these toxic concentrations were much higher for J774G8 macrophages and Vero cells than for the protozoans. The mixture of piperovatine: piperlongumune (2:3) showed important antiprotozoal activity against the amastigote and promastigote forms of L. amazonensis, and it produced morphological changes in promastigotes and amastigotes at 0.9 μg/ml and 24 μg/ml (50% growth inhibition concentration), respectively, including intense cytoplasmic vacuolization, mitochondrial swelling, and mitochondrial damage, as revealed by transmission electron microscopy

Studies on effectiveness of Tanacetum parthenium against Leishmania amazonensis

Summary. We assessed the biological activity of a plant powder, crude extracts, and several fractions obtained from Tanacetum parthenium on Leishmania amazonensis. The medicinal plant T. parthenium is indicated for prevention of migraine headache crises, and several investigations have already demonstrated its anti-inflammatory activity. This study included the extraction process and bioassay-guided fractionation by the adsorption chromatography method. A progressive increase in the antileishmanial effect was observed in the course of the purification process. The plant powder (PTP) had a 50% inhibitory concentration (IC 50 ) at 490 µg/ml, whereas the dichloromethane fraction (DF) showed an IC 50 of 3.6 µg/ml against the growth of promastigote forms after 48 h of culturing. In axenic amastigote forms, the IC 50 of the PTP and DF were 74.8 µg/ml and 2.7 µg/ml, respectively. Cytotoxicity analysis indicated that the toxic concentrations of the PTP, ethyl-acetate crude extract (ECE), and DF were much higher for J774G8 macrophages than for the protozoans. Haemolytic experiments were performed, and the ECE and DF did not cause lysis at concentrations higher than the IC 50 for promastigotes

Operation of a slow rate anaerobic digester treating municipal secondary sludge

This study was designed to evaluate the performance of a slow rate anaerobic digester in treating secondary sewage sludge received from one local municipal wastewater treatment plant. The digester was fed by secondary sewage sludge without any previous thickening. A series of three independent batch experiments was investigated at an operation time of 60 days. The total solids (TS) in the influent sludge contained a percentage of organic matter of 59, 63 and 54%, a concentration of volatile suspended solids (VSS) of 23.7, 29.2 and 27.8 g L-1 and a chemical oxygen demand (COD) of 51.8, 32.9 and 65.7 g L-1 for the three experiments, respectively. The operation of anaerobic digestion was stable, with no noticeable scum or foaming problems. The COD reduction in each experiment reached 29, 21 and 45% in the sludge and 95, 85 and 82% in the supernatant. The microbial indicators were surveyed by sampling the sludge throughout the digester operation and counting the number of bacteria in the sampled sludge. Counted bacteria included the total culturable, the total and fecal coliform groups, Pseudomonas aeruginosa and fecal streptococci. The percentage removal of the indicator bacteria was higher for fecal streptococci (99.9%) than for coliform bacteria (96.3%), which in turn was higher than for P. aeruginosa (95.6%). Parasitological analysis was also performed on multiple sludge samples by determination of protozoa and helminth eggs. Protozoa ( Eimeria and Entamoeba ), helminth eggs ( Ascaris , Trichuris , Toxocara , Hymenolepis ) and mites were detected in the influent sludge, and particularly among the helminth eggs, only Trichuris was detected in the effluent sludge

Chemical constituents of Luehea divaricata Mart. (Tiliaceae)

Chemical studies of the leaves of L. divaricata afforded 3beta-p-hydroxybenzoyl-tormentic acid, a triterpene with an ursene-type skeleton, a mixture whose main compound was an oleanene derivative, the maslinic acid, a C-glycoside flavone, vitexin and glucopyranosylsitosterol. A flavonoid, characterized as (-)-epicatechin, which belongs to the flavan-3-ol class, was isolated from the stem's bark. The structures of the compounds were elucidated by spectroscopic analysis. The antibacterial, antifungal and antiproliferative activities of the crude methanolic extracts of leaves and bark were evaluated and the antibacterial properties of the fractions of the barks were also investigated.834837Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES

Effects of medicinal plant extracts on growth of Leishmania (L.) amazonensis and Trypanosoma cruzi

Este estudo descreve a triagem de extratos obtidos de 19 espécies de plantas usadas na medicina tradicional brasileira para o tratamento de várias doenças. Os extratos foram testados contra formas amastigota axênica e promastigota de Leishmania (L.) amazonensis, e formas epimastigota de Trypanosoma cruzi in vitro na concentração de 100 mg/ml. Baccharis trimera, Cymbopogon citratus, Matricaria chamomilla, Mikania glomerata, Ocimum gratissimum, Piper regnellii, Prunus domestica, Psidium guajava, Sambucus canadensis, Stryphnodendron adstringens, Tanacetum parthenium, e Tanacetum vulgare apresentaram efeito significante contra um ou ambos parasitas, com a porcentagem de inibição de crescimento entre 49,5 e 99%. Os extratos não mostraram efeito citotóxico em hemácias de carneiro. Essas plantas medicinais podem ser fontes alternativas de novos compostos clinicamente ativos contra L. amazonensis e T. cruzi.This study describes the screening of extracts obtained from 19 species of plants used in Brazilian traditional medicine for treatment of a variety of diseases. The extracts were tested against axenic amastigote and promastigote forms of Leishmania (L.) amazonensis, and epimastigote forms of Trypanosoma cruzi in vitro at a concentration of 100 mg/ml. Baccharis trimera, Cymbopogon citratus, Matricaria chamomilla, Mikania glomerata, Ocimum gratissimum, Piper regnellii, Prunus domestica, Psidium guajava, Sambucus canadensis, Stryphnodendron adstringens, Tanacetum parthenium, and Tanacetum vulgare showed significant effects against one or both parasites, with a percentage of growth inhibition between 49.5 and 99%. The extracts showed no cytotoxic effect on sheep erythrocytes. These medicinal plants may be sources of new compounds that are clinically active against L. amazonensis and T. cruzi