RESUMO
To overcome the disadvantages of chemical and physical methods, phyto-fabricated nanoparticles attained great attention due to their multifarious applications. Here we successfully demonstrated Papaver somniferum L. mediated green synthesis of lead oxide (PbO) and iron oxide (Fe2O3) nanoparticles. Characterization of nanoparticles involved techniques including X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and energy dispersive X-ray (EDX) associated with scanning electron microscopy (SEM). XRD analysis confirmed the phase identification and crystalline nature. FTIR analysis confirmed the capping of nanoparticles by plants' phytochemicals. SEM revealed morphological features of PbO and Fe2O3 with size of nanoparticles being 23⯱â¯11â¯nm and 38⯱â¯13â¯nm, respectively. The elemental composition of the nanoparticles was confirmed by EDX. Both bacterial and fungal isolates showed susceptibility towards PbO and Fe2O3 NPs. Both the NPs also showed considerable total antioxidant potential, free radical scavenging potential and reducing power. Insignificant level of α-amylase for both NPs was observed. Fe2O3 NPs showed superior biocompatibility with human RBCs as compared to PbO whereas PbO showed more potent anti-cancer activity as compared to Fe2O3 NPs. Overall our study concluded that both NPs played vital role in multiple biological assays however, extensive research focused on cytotoxic evaluation of NPs in-vivo is required.
Assuntos
Compostos Férricos/química , Chumbo/química , Nanopartículas Metálicas/química , Óxidos/química , Papaver/metabolismo , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Avaliação Pré-Clínica de Medicamentos , Estabilidade de Medicamentos , Eritrócitos/efeitos dos fármacos , Hemolíticos/química , Hemolíticos/farmacologia , Células Hep G2 , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Nanopartículas Metálicas/uso terapêutico , Papaver/química , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismoRESUMO
The present investigation was undertaken to evaluate the antibacterial, antifungal and hemolytic activities of organic and aqueous fractions of Fumaria indica, Dicliptera bupleuroides and Curcuma zedoaria. The methanolic extracts of the plants were dissolved in the water (distilled) separately and then partitioned with the n-hexane, CHCl3, EtOAc and n-BuOH sequentially. Antibacterial activity was checked against Escherichia coli, Pasturella multocida, Bacillus subtilis and Staphylococcus aureus by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. It was revealed that aqueous fraction of F. indica showed very good antibacterial activity against P. multocida with zone of inhibition 26mm and MIC of 98µg/mL. Its CHCl3 and n-BuOH fractions also displayed good results. Its CHCl3 fraction showed good antifungal activity against G. lucidum with zone of inhibition 24mm and MIC of 115µg/mL. Other polar fractions of F. indica showed good activity against somefungal strains. The CHCl3 and EtOAc fractions of D. bupleuroides displayed good antibacterial activity against some bacterial strains. Its EtOAc fraction showed good antifungal activity only against G. lucidum. The CHCl3 fraction of C. zedoaria showed good activity against all studied bacterial strains, while its EtOAc and n-BuOH fractions displayed good results against some bacterial strains. None of the fractions of C. zedoaria displayed antifungal activity against the under test strains. All the studied fractions of three plants showed very less toxicity except n-hexane fraction of D. bupleuroides which showed 79% toxicity.
Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Hemolíticos/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Acanthaceae/química , Antibacterianos/química , Antifúngicos/química , Curcuma/química , Avaliação Pré-Clínica de Medicamentos , Fumaria/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hemólise/efeitos dos fármacos , Hemolíticos/química , Humanos , Testes de Sensibilidade Microbiana , Extratos Vegetais/químicaRESUMO
In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and their α-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1H-NMR, 13C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield. In comparison to typical acarbose (IC50 = 37.38±0.12µM), all synthesized compounds showed potent activity with IC50 values between 31.26±0.11 to 396.25±0.18µM. The most potent compounds 6, 8 and 11 showed IC50 values within the range of 31.26±0.11 to 37.48±0.12µM. Compounds 7, 10, 12 and 13 showed IC50 values within the range of 65.23±0.12 to 154.87±0.16µM, while compounds 4, 5 and 9 showed moderate inhibition with IC50 values 286.56±0.16 to 396.25±0.18µM. Structure-activity relationship (SAR) studies, suggests that electron withdrawing groups played a crucial role in enhancing α-glucosidase inhibitory effects of title compounds. In addition, results of the hemolytic and antihemolytic activity studies indicated that compound 13 possessed moderate levels of hemolytic and highest anti- hemolytic activity while 8 showed low anti- hemolytic and high hemolytic activity.
Assuntos
Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Hemolíticos/química , Hemolíticos/farmacologia , Pirazóis/síntese química , Cristalografia por Raios X , Avaliação Pré-Clínica de Medicamentos , Hemólise/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Pirazóis/química , Pirazóis/farmacologia , Espectrofotometria Infravermelho , Relação Estrutura-AtividadeRESUMO
The saponins, as components of tea seed meal, are undesirable hemolytic components and should be degraded for reducing their hemolytic activity in order to be used in animal feed. In this study, ß-glucuronidase was verified to be a potent hydrolase of tea seed saponins to reduce their hemolytic activity and a ß-glucuronidase-producing Lactobacillus crustorum strain was screened from raw bovine milk. Next, solid-state fermentation with the isolated L. crustorum and a Bacillus subtilis natto strain, which can produce cellulase and hence improve the fermentation performance of tea seed meal, was carried out for detoxification of tea seed meal. The 50% hemolytic dosage (HD50) value of tea seed saponins was increased from 6.69 to 27.43 µg mL-1. The results of LC-MS analysis showed that the percentage of saponin aglycones increased from 30.95 to 84.25% after the fermentation. According to the roles of sugar moieties in hemolytic activity, and the enzymatic hydrolysis characteristics of ß-glucuronidase, the degradation of tea seed saponins from glucosides to aglycones may contribute to the reduction of hemolytic activity. Therefore, tea seed meal may be used as animal feed after fermentation with the tested saponin-degrading microbial strains.
Assuntos
Bacillus subtilis/metabolismo , Camellia/química , Hemolíticos/metabolismo , Lactobacillus/metabolismo , Extratos Vegetais/metabolismo , Saponinas/metabolismo , Sementes/microbiologia , Ração Animal/análise , Ração Animal/microbiologia , Animais , Camellia/microbiologia , Bovinos , Cromatografia Líquida de Alta Pressão , Fermentação , Hemolíticos/química , Espectrometria de Massas , Extratos Vegetais/química , Saponinas/química , Sementes/químicaRESUMO
BACKGROUND: Saponins isolated from a number of plants possess a broad spectrum of biological and pharmacological activities by using in vitro and in vivo bioassays. The recent investigations and findings in biological activity studies of saponins have mostly focused on immunomodulatory, hemolytic and cytotoxic properties. HYPOTHESIS/PURPOSE: Considering the great potential of saponins as bioactive agents, we investigated the cytotoxic, hemolytic and immunomodulatory activities of nineteen triterpenoid saponins from the aerial parts of eight Cephalaria species from Turkey. STUDY DESIGN: The isolated oleanane type saponins from Cephalaria species were tested for their hemolytic, cytotoxic and immunomodulatory activities through anin vitro cell based assay systems. METHODS: HeLa, A549, and a normal cell line HEK293 were used for testing cytotoxicity using MTT method. Immunomodulatory activity was performed in stimulated whole blood cells by PMA plus ionomycin. Hemolytic activity was assessed on human erythrocytes. RESULTS: Aristatoside C (3) and davisianoside B (16) displayed significant inhibitory effects on cancerous A549 and HeLa cells, and non-cancerous HEK293 cells with IC50 values of 3.52 ± 0.11, 35.69 ± 0.50, 8.96 ± 0.62 µM and 4.08 ± 0.06, 11.74 ± 0.82, 20.43 ± 3.21 µM, respectively. Thirteen saponins out of the nineteen tested increased IL-1ß concentrations considerably, while six compounds changed IL-2 or IFN-γ levels slightly. Almost all of the saponins showed noticeable hemolysis in human erythrocyte cells based on the sugar units. CONCLUSION: In this study, almost all saponins with oleanolic acid as aglycones exhibited significant hemolysis, monodesmosidic saponins with hederagenin as aglycone were the most active compounds against lung cancer cells with greater activity than standard commercial chemotherapy drug doxorubicin and some of the hederagenin type saponins induced remarkable IL-1ß secretion.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Dipsacaceae/química , Hemolíticos/farmacologia , Fatores Imunológicos/farmacologia , Saponinas/farmacologia , Antineoplásicos Fitogênicos/química , Avaliação Pré-Clínica de Medicamentos/métodos , Ensaios de Seleção de Medicamentos Antitumorais , Células HEK293 , Células HeLa , Hemólise/efeitos dos fármacos , Hemolíticos/química , Humanos , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/química , Saponinas/química , Triterpenos/química , Triterpenos/farmacologia , TurquiaRESUMO
In efforts to find new antimicrobial peptides (AMPs), we studied the skin secretion of the endemic Colombian frog Dendropsophus columbianus belonging to a genus that has not been investigated previously. From HPLC-fractionated secretion, we identified one peptide with slightly antibacterial activity. Its peptide sequence showed no sequence similarity to current annotated peptides. We named this novel peptide dendropsophin 1 (Dc1). Afterward, two analogues were designed (Dc1.1 and Dc1.2) to improve the cationic and amphipathic features. Then, their antiproliferative and cytotoxic properties were evaluated against several pathogens including bacteria, fungi, protozoa and also mammalian cells. Dc1 and its two analogues exhibited moderate antibacterial activities and no hemolytic and cytotoxic effects on mammalian cells. Analogue Dc1.2 showed slightly improved antibacterial properties. Their secondary structures were characterised using CD spectroscopy and Dc1.2 displayed a higher α-helix content and thermal stability compared to Dc1 and Dc1.1 in hydrophobic experimental conditions.
Assuntos
Antibacterianos/farmacologia , Peptídeos Catiônicos Antimicrobianos/química , Peptídeos Catiônicos Antimicrobianos/farmacologia , Anuros , Pele/metabolismo , Animais , Antibacterianos/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Colômbia , Avaliação Pré-Clínica de Medicamentos/métodos , Hemólise/efeitos dos fármacos , Hemolíticos/química , Hemolíticos/farmacologia , Humanos , Interações Hidrofóbicas e Hidrofílicas , Masculino , Testes de Sensibilidade Microbiana , Estabilidade Proteica , Estrutura Secundária de Proteína , Ratos , Homologia de Sequência de Aminoácidos , Trypanosoma/efeitos dos fármacosRESUMO
New efficient antifungal agents are urgently needed to treat drug-resistant fungal infections. Here, we designed and synthesized a series of cationic xanthone amphiphilics as antifungal agents from natural α-mangostin to combat fungal resistance. The attachment of cationic residues on the xanthone scaffold of α-mangostin resulted in interesting antifungal agents with a novel mode of action. Two lead compounds (1 and 2) showed potent antifungal activity against a wide range of fungal pathogens, including drug-resistant Candida albicans, Aspergillus, and Fusarium strains and low cytotoxicity and hemolytic activity against mammalian cells. Both compounds can kill fungus rapidly by directly disrupting fungal cell membranes and avoid developing drug resistance. Additionally, compound 1 exhibited potent in vivo antifungal activity in the murine model of fungal keratitis. To our knowledge, membrane-targeting xanthone-based antifungals have not been reported previously. These results demonstrated that compounds 1 and 2 may be promising candidates for treating drug-resistant fungal infections.
Assuntos
Antifúngicos/química , Antifúngicos/farmacologia , Farmacorresistência Fúngica/efeitos dos fármacos , Xantonas/química , Animais , Antifúngicos/síntese química , Aspergillus/efeitos dos fármacos , Candida/efeitos dos fármacos , Linhagem Celular , Avaliação Pré-Clínica de Medicamentos/métodos , Fibroblastos/efeitos dos fármacos , Fusarium/efeitos dos fármacos , Hemolíticos/química , Hemolíticos/farmacologia , Humanos , Concentração Inibidora 50 , Ceratite/tratamento farmacológico , Ceratite/microbiologia , Camundongos Endogâmicos C57BL , Testes de Sensibilidade Microbiana , Relação Estrutura-AtividadeRESUMO
BACKGROUND: The continuous emergence of multi-drug-resistant bacteria drastically reduces the efficacy of antibiotic armory and, consequently, increases the frequency of therapeutic failure. The discovery of new antibacterial drugs is an urgent need. The present study reports the antibacterial and antioxidant activities of the methanol extract, fractions and iridoids from Canthium subcordatum, a plant traditionally used as antidiabetic, anti-inflammatory, and antimicrobial. METHODS: Broth microdilution assay was used to determine minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) of extracts and iridoids against Staphylococcus aureus, Vibrio cholerae and Shigella flexneri. Antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and gallic acid equivalent antioxidant capacity (GAEAC) assays. The samples were also tested for their cytotoxicity against human red blood cells (RBC). RESULTS: The methanol extract, hexane, ethyl acetate and iso-butanol fractions from C. subcordatum fruits displayed different degrees of antioxidant (EC50 = 62.83-70.17 µg/ml; GAEAC = 45.63-58.23 µg/ml) and antibacterial (MIC = 128-512 µg/ml) activities. Canthiumoside 1(1) and linearin (7) were the most active antioxidant (EC50 = 1.12-2.03 µg/ml; GAEAC = 79.82-92.35 µg/ml) and antibacterial (MIC = 8-64 µg/ml) compounds while the most sensitive bacterium was Staphylococcus aureus. The tested samples were non-toxic to normal cells. CONCLUSION: Our results demonstrated that compounds 1 and 7 were potent antibacterial agents and DPPH/ABTS·+ radical scavengers, so they warrant further investigation.
Assuntos
Iridoides/farmacologia , Extratos Vegetais/farmacologia , Rubiaceae/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Células Sanguíneas/efeitos dos fármacos , Frutas/química , Hemolíticos/química , Hemolíticos/isolamento & purificação , Hemolíticos/farmacologia , Humanos , Iridoides/química , Iridoides/isolamento & purificação , Testes de Sensibilidade Microbiana , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificaçãoRESUMO
BACKGROUND: One of the major challenges limiting the development of gene therapy is an absence of efficient and safe gene carriers. Among the nonviral gene delivery methods, lipofection is considered as one of the most promising. In the present study, a set of cationic polyprenyl derivatives [trimethylpolyprenylammonium iodides (PTAI)] with different lengths of polyprenyl chains (from 7, 8 and 11 to 15 isoprene units) was suggested as a component of efficient DNA vehicles. METHODS: Optimization studies were conducted for PTAI in combination with co-lipid dioleoylphosphatidylethanolamine on DU145 human prostate cancer cells using: size and zeta potential measurements, confocal microscopy, the fluorescein diacetate/ethidium bromide test, cell counting, time-lapse monitoring of cell movement, gap junctional intercellular coupling analysis, antimicrobial activity assay and a red blood cell hemolysis test. RESULTS: The results obtained show that the lipofecting activity of PTAI allows effective transfection of plasmid DNA complexed in negatively-charged lipoplexes of 200-500 nm size into cells without significant side effects on cell physiology (viability, proliferation, morphology, migration and gap junctional intercellular coupling). Moreover, PTAI-based vehicles exhibit a potent bactericidal activity against Staphylococcus aureus and Escherichia coli. The developed anionic lipoplexes are safe towards human red blood cell membranes, which are not disrupted in their presence. CONCLUSIONS: The developed carriers constitute a group of promising lipofecting agents of a new type that can be utilized as effective lipofecting agents in vitro and they are also an encouraging basis for in vivo applications.
Assuntos
Compostos de Amônio/toxicidade , Terpenos/toxicidade , Transfecção , Compostos de Amônio/química , Ânions , Antibacterianos/química , Antibacterianos/toxicidade , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Escherichia coli , Terapia Genética , Hemolíticos/química , Hemolíticos/toxicidade , Humanos , Lipossomos , Tamanho da Partícula , Staphylococcus aureus , Terpenos/químicaRESUMO
A strategy is introduced for enhancing the cellular selectivity of Amphotericin B (AmB) and other classes of membrane-disrupting agents. This strategy involves attaching the agent to a molecular umbrella to minimize the disruptive power of aggregated forms. Based on this approach, AmB has been coupled to a molecular umbrella derived from one spermidine and two cholic acid molecules and found to have antifungal activities approaching that of the native drug. However, in sharp contrast to AmB, the hemolytic activity and the cytotoxcity of this conjugate toward HEK293 T cells have been dramatically reduced.
Assuntos
Anfotericina B/química , Anfotericina B/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Anfotericina B/efeitos adversos , Animais , Ácido Cólico/química , Avaliação Pré-Clínica de Medicamentos/métodos , Eritrócitos/efeitos dos fármacos , Células HEK293/efeitos dos fármacos , Hemolíticos/química , Hemolíticos/farmacologia , Humanos , Espermidina/química , Relação Estrutura-AtividadeRESUMO
Hymenaea courbaril var courbaril seed xyloglucan was efficiently extracted with 0.1M NaCl, followed by ethanol precipitation (yield=72±5% w/w). Its amorphous structure was identified by the pattern of X-ray diffraction. The monosaccharide composition was determined by GC/MS analysis of the alditol acetates and showed the occurrence of glucose:xylose:galactose:arabinose (40:34:20:6). One-(1D) and two-dimensional-(2D) NMR spectra confirmed a central backbone composed by 4-linked ß-glucose units partially branched at position 6 with non-reducing terminal units of α-xylose or ß-galactose-(1â2)-α-xylose disaccharides. The xyloglucan solution was evaluated by dynamic light scattering and presents a polydisperse and practically neutral profile, and at 0.5 and 1.0% (w/v) the solutions behave as a viscoelastic fluid. The polysaccharide did not show significant antibacterial or hemolytic activities. Overall our results indicate that xyloglucan from H. courbaril is a promising polysaccharide for food and pharmaceutical industries.
Assuntos
Glucanos/química , Hymenaea/química , Extratos Vegetais/química , Sementes/química , Xilanos/química , Antibacterianos/química , Antibacterianos/farmacologia , Cromatografia em Gel , Glucanos/farmacologia , Hemolíticos/química , Hemolíticos/farmacologia , Metilação , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Extratos Vegetais/farmacologia , Reologia , Difração de Raios X , Xilanos/farmacologiaRESUMO
The contention and treatment of Mycobacterium tuberculosis and other bacteria that cause infectious diseases require the use of new type of antibiotics. Pandinin 2 (Pin2) is a scorpion venom antimicrobial peptide highly hemolytic that has a central proline residue. This residue forms a structural "kink" linked to its pore-forming activity towards human erythrocytes. In this work, the residue Pro14 of Pin2 was both substituted and flanked using glycine residues (P14G and P14GPG) based on the low hemolytic activities of antimicrobial peptides with structural motifs Gly and GlyProGly such as magainin 2 and ponericin G1, respectively. The two Pin2 variants showed antimicrobial activity against E. coli, S. aureus, and M. tuberculosis. However, Pin2 [GPG] was less hemolytic (30%) than that of Pin2 [G] variant. In addition, based on the primary structure of Pin2 [G] and Pin2 [GPG], two short peptide variants were designed and chemically synthesized keeping attention to their physicochemical properties such as hydrophobicity and propensity to adopt alpha-helical conformations. The aim to design these two short antimicrobial peptides was to avoid the drawback cost associated to the synthesis of peptides with large sequences. The short Pin2 variants named Pin2 [14] and Pin2 [17] showed antibiotic activity against E. coli and M. tuberculosis. Besides, Pin2 [14] presented only 25% of hemolysis toward human erythrocytes at concentrations as high as 100 µM, while the peptide Pin2 [17] did not show any hemolytic effect at the same concentration. Furthermore, these short antimicrobial peptides had better activity at molar concentrations against multidrug resistance M. tuberculosis than that of the conventional antibiotics ethambutol, isoniazid and rifampicin. Therefore, Pin2 [14] and Pin2 [17] have the potential to be used as an alternative antibiotics and anti-tuberculosis agents with reduced hemolytic effects.
Assuntos
Antibacterianos/farmacologia , Hemolíticos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Peptídeos/química , Peptídeos/síntese química , Engenharia de Proteínas/métodos , Antibacterianos/química , Linhagem Celular , Dicroísmo Circular , Avaliação Pré-Clínica de Medicamentos , Escherichia coli , Hemólise/efeitos dos fármacos , Hemolíticos/química , Humanos , Mycobacterium tuberculosis/química , Conformação Proteica , Análise de Regressão , Staphylococcus aureusRESUMO
We report on the screening for biological activities of organic extracts from seven strains that represent four varieties of the fungus Aureobasidium pullulans, that is A. pullulans var. melanogenum, A. pullulans var. pullulans, A. pullulans var. subglaciale and A. pullulans var. namibiae. We monitored haemolysis, cytotoxicity, antioxidant capacity and growth inhibition against three bacterial species. The haemolytic activity of A. pullulans var. pullulans EXF-150 strain was due to five different haemolytically active fractions. Extracts from all of the other varieties contained at least one haemolytically active fraction. Short-term exposure of cell lines to these haemolytically active organic extracts resulted in more than 95% cytotoxicity. Strong antioxidant capacity, corresponding to 163.88 µg ascorbic acid equivalent per gram of total solid, was measured in the organic extract of the strain EXF-3382, obtained from A. pullulans var. melanogenum, isolated from the deep sea. Organic extracts from selected varieties of A. pullulans exhibited weak antibacterial activities.
Assuntos
Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Ascomicetos/química , Citotoxinas/isolamento & purificação , Citotoxinas/farmacologia , Hemolíticos/isolamento & purificação , Hemolíticos/farmacologia , Antibacterianos/química , Antioxidantes/química , Compostos de Bifenilo/farmacologia , Citotoxinas/química , Ecossistema , Glucanos , Hemolíticos/química , Biologia Marinha , Testes de Sensibilidade Microbiana , Oceanos e Mares , Picratos/farmacologia , Extratos Vegetais/farmacologiaRESUMO
Reactive oxygen species (ROS) can lead to haemolysis and eventually to diseases such as thalassemia and sickle cell anaemia. Their action can be counteracted by the antihaemolytic activity of therapeutic agents. The aim of our study was to identify plants that most efficiently counteract ROS-caused haemolysis. From ten plants known for their antioxidant activity (Orobanche orientalis G. Beck, Cucumis melo L., Albizzia julibrissin Durazz, Galium verum L., Scutellaria tournefortii Benth, Crocus caspius Fischer & Meyer, Sambucus ebulus L., Danae racemosa L., Rubus fruticsos L., and Artemisia absinthium L.) we prepared 30 extracts using three extraction methods (percolation, Soxhlet, and ultrasound-assisted extraction) to see whether the extraction method affects antihaemolytic efficiency, and one extraction method (polyphenol extraction) to see how much of this action is phenol-related. Extract antihaemolytic activity was determined in mice red blood cells and compared to that of vitamin C as a known antioxidant. Nine of our extracts were more potent than vitamin C, of which G. verum (aerial parts/percolation) and S. tournefortii (aerial parts/polyphenol) extracts were the most potent, with an IC50 of 1.32 and 2.08 µg mL⻹, respectively. Haemolysis inhibition depended on extract concentration and the method of extraction. These plants could provide accessible sources of natural antioxidants to the pharmaceutical industry.
Assuntos
Eritrócitos/efeitos dos fármacos , Hemólise/efeitos dos fármacos , Hemolíticos/farmacologia , Extratos Vegetais/farmacologia , Animais , Antioxidantes/farmacologia , Ácido Ascórbico/farmacologia , Hemolíticos/química , Irã (Geográfico) , Masculino , Camundongos , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Espécies Reativas de OxigênioRESUMO
It is essential to study the phytochemical constituents and toxicological properties of seagrasses when considering their food applications. Aqueous methanolic extracts of six seagrasses were evaluated for their antibacterial, cytotoxic (brine shrimp leathality assay) and haemolytic activity. Thin layer chromatography (TLC) and phytochemical analysis were used to compare the phytochemical profiles of six seagrasses. Among the six seagrasses examined, Halodule pinifolia and Cymodocea rotundata showed predominant growth inhibitory activity against all the tested human pathogens. Cytotoxicity of seagrass extracts against nauplii of Artemia salina revealed that Syringodium isoetifolium exhibited lesser toxicity with LC(50) value of 699.096 µg/ml. Of all the seagrasses tested, H. pinifolia recorded the minimum haemolytic activity of 2.07±0.63% at 1000 µg/ml concentration. Phytochemical analysis showed the presence of common plant chemical constituents which varied with respect to species. The present findings suggest the possible pharmacological applications of selected seagrasses that can be used as food ingredients.
Assuntos
Antibacterianos/farmacologia , Citotoxinas/farmacologia , Hemolíticos/farmacologia , Magnoliopsida/química , Extratos Vegetais/farmacologia , Animais , Antibacterianos/química , Artemia/efeitos dos fármacos , Bactérias/efeitos dos fármacos , Bioensaio , Células Sanguíneas/efeitos dos fármacos , Cromatografia em Camada Fina , Citotoxinas/química , Hemolíticos/química , Humanos , Índia , Dose Letal Mediana , Testes de Sensibilidade Microbiana , Extratos Vegetais/químicaRESUMO
Moon jellyfish (Aurelia aurita) tentacle extract was studied for its anticoagulant activity in vitro. The Jellyfish Tentacle Extract (JFTE) showed very strong fibrinogenolytic activity by cleaving Aα and Bß chain of fibrinogen molecule. The fibrinogenolytic activity was found to be stronger than some snake venom derived anticoagulants. JFTE also completely liquefied fibrin clots in 24 h. JFTE was found to contain both high and low molecular weight proteins/peptides. The fibrinogenolysis appears to be caused by high molecular weight fractions of the extract. It has been also noted that PMSF significantly reduced fibrinogenolytic activity and heating totally abolished it. Autolytic degradation of the high molecular weight protein was also noted. Autolysis slowed down, but did not abolish the fibrinogenolytic activity of the extract.
Assuntos
Anticoagulantes/química , Fibrinogênio/química , Fibrinolíticos/química , Hemolíticos/química , Cifozoários/química , Extratos de Tecidos/química , Animais , Impedância Elétrica , Eletroforese em Gel de Poliacrilamida , Humanos , Índia , Peso Molecular , Agregação Plaquetária/efeitos dos fármacosRESUMO
A series of 46 compounds derived from esculentoside A and its aglycone were synthesized and characterized. The effect of these compounds on lipopolysaccharide (LPS)-induced NO production, haemolytic activity, and cell viability was evaluated. Structure-activity relationship was established by comparing the derivatives of esculentoside A with its aglycone derivatives. Both the aglycone and its derivatives showed higher inhibitory effects on LPS-induced NO production, and lower haemolytic activities than esculentoside A and its derivatives.
Assuntos
Hemolíticos/química , Hemolíticos/farmacologia , Óxido Nítrico/biossíntese , Ácido Oleanólico/análogos & derivados , Saponinas/química , Saponinas/síntese química , Saponinas/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Eritrócitos/efeitos dos fármacos , Concentração Inibidora 50 , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Ácido Oleanólico/síntese química , Ácido Oleanólico/química , Ácido Oleanólico/farmacologia , Phytolacca/química , Coelhos , Relação Estrutura-AtividadeRESUMO
Lariciresinol is an enterolignan precursor isolated from the herb Sambucus williamsii, a folk medicinal plant used for its therapeutic properties. In this study, the antifungal properties and mode of action of lariciresinol were investigated. Lariciresinol displays potent antifungal properties against several human pathogenic fungal strains without hemolytic effects on human erythrocytes. To understand the antifungal mechanism of action of lariciresinol, the membrane interactions of lariciresinol were examined. Fluorescence analysis using the membrane probe 3,3'-diethylthio-dicarbocyanine iodide (DiSC(3)-5) and 1,6-diphenyl-1,3,5-hexatriene (DPH), as well as a flow cytometric analysis with propidium iodide (PI), a membrane-impermeable dye, indicated that lariciresinol was associated with lipid bilayers and induced membrane permeabilization. Therefore, the present study suggests that lariciresinol possesses fungicidal activities by disrupting the fungal plasma membrane and therapeutic potential as a novel antifungal agent for the treatment of fungal infectious diseases in humans.
Assuntos
Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Membrana Celular/efeitos dos fármacos , Furanos/farmacologia , Lignanas/farmacologia , Sambucus/química , Antifúngicos/química , Antifúngicos/isolamento & purificação , Benzotiazóis/química , Carbocianinas/química , Células Cultivadas , Difenilexatrieno/química , Eritrócitos/efeitos dos fármacos , Citometria de Fluxo , Corantes Fluorescentes/química , Furanos/química , Furanos/isolamento & purificação , Hemólise , Hemolíticos/química , Hemolíticos/isolamento & purificação , Hemolíticos/farmacologia , Humanos , Lignanas/química , Lignanas/isolamento & purificação , Propídio/químicaRESUMO
The genus Symplocos has been reviewed for its chemical constituents and biological activities including traditional importance of some common species. The plants of this genus contain terpenoids, flavonoids, lignans, phenols, steroids, alkaloids, and iridoids. Terpenoids are the major constituents within the genus Symplocos and most of them exhibit antiproliferative effects. Some phenolic glycoside derivatives showed inhibitory activity against snake-venom phosphodiesterase I and human nucleotide pyrophosphatase phosphodiesterase I. The members of genus Symplocos are well known for their traditional uses in the treatment of various diseases like leprosy, gynecological disorders, ulcers, leucorrhea, menorrhagia, malaria, and tumefaction. The aim of the present paper is to review the comprehensive knowledge of the plants of this genus including the traditional uses, chemistry, and pharmacology.
Assuntos
Magnoliopsida/química , Plantas Medicinais/química , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antidiarreicos/química , Antidiarreicos/isolamento & purificação , Antidiarreicos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Fármacos do Sistema Nervoso Central/química , Fármacos do Sistema Nervoso Central/isolamento & purificação , Fármacos do Sistema Nervoso Central/farmacologia , Quimotripsina/antagonistas & inibidores , Feminino , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Glicosídeos/química , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Hemolíticos/química , Hemolíticos/isolamento & purificação , Hemolíticos/farmacologia , Humanos , Iridoides/química , Iridoides/isolamento & purificação , Iridoides/farmacologia , Lignanas/química , Lignanas/isolamento & purificação , Lignanas/farmacologia , Estrutura Molecular , Parassimpatolíticos/química , Parassimpatolíticos/isolamento & purificação , Parassimpatolíticos/farmacologia , Inibidores de Fosfodiesterase/química , Inibidores de Fosfodiesterase/isolamento & purificação , Inibidores de Fosfodiesterase/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidoresRESUMO
We report on screening tests of 66 extracts obtained from 35 marine sponge species from the Caribbean Sea (Curaçao) and from eight species from the Great Barrier Reef (Lizard Island). Extracts were prepared in aqueous and organic solvents and were tested for hemolytic, hemagglutinating, antibacterial and anti-acetylcholinesterase (AChE) activities, as well as their ability to inhibit or activate cell protein phosphatase 1 (PP1). The most interesting activities were obtained from extracts of Ircinia felix, Pandaros acanthifolium, Topsentia ophiraphidites, Verongula rigida and Neofibularia nolitangere. Aqueous and organic extracts of I. felix and V. rigida showed strong antibacterial activity. Topsentia aqueous and some organic extracts were strongly hemolytic, as were all organic extracts from I. felix. The strongest hemolytic activity was observed in aqueous extracts from P. acanthifolium. Organic extracts of N. nolitangere and I. felix inhibited PP1. The aqueous extract from Myrmekioderma styx possessed the strongest hemagglutinating activity, whilst AChE inhibiting activity was found only in a few sponges and was generally weak, except in the methanolic extract of T. ophiraphidites.