Indigofera oblongifolia leaf extract regulates spleen macrophage response during Plasmodium chabaudi infection

Malaria is a major health problem that still affects numerous countries. The current study aimed to identify the role of Indigofera oblongifolia leaf extract in regulating mouse spleen macrophages during the progression of Plasmodium chabaudi infection. Three doses of the leaf extract (100, 200, and 300 mg/kg) were administered to mice inoculated with P. chabaudi infected erythrocytes. The weight of the infected mice improved after the treatment with I. oblongifolia. The infection causes disorganization of macrophage distribution in the spleen. After the mice had been treated with the leaf extract, the macrophages appeared to be reorganized in the white and red pulp areas. In addition, the I. oblongifolia leaf extract (IOLE) significantly increased the total antioxidant capacity of the mice spleens infected with P. chabaudi. The phagocytic activity of spleen macrophages was increased in the infected group as indicated by the significant decrease in the number of fluorescent particles in the spleen sections. This number increased in the mice spleens after treatment with IOLE. Based on these results, it is suggested that IOLE regulate macrophage response of the spleen during the blood stage of malaria in mice.     

胆汁分离细菌种类及主要分离菌株耐药性分析

目的了解2000年至2008年临床胆汁普通培养分离细菌的种类,并分析主要分离菌株的耐药性。方法回顾性分析近9年710例胆囊炎和胆囊结石患者胆汁普通培养分离细菌的分布情况及耐药率;用微量稀释法进行药物敏感性测定。结果710例患者胆汁培养共分离出细菌435株,检出率为61.27%,前5位分别为大肠埃希菌、肠球菌、假单胞菌、肺炎克雷伯菌和凝固酶阴性葡萄球菌。革兰阴性杆菌对亚胺培南、阿米卡星的耐药率均低于10%,对常用青霉素类和头孢菌素类抗生素耐药率超过50%。结论胆汁分离细菌以肠道细菌为主,阿米卡星可以作为经验治疗的首选药物。     

Anthelmintic potency of Rumex crispus L. extracts against Caenorhabditis elegans and non-targeted identification of the bioactive compounds

Traditional healers and ethnoveterinary therapists use several medicinal plants, such as Rumex crispus L., to treat endoparasite infections. R. crispus has been established by researchers to be effective agasint a few parasitic worms. In this study, we evaluated the potency of R. crispus extracts on the model organism, Caenorhabditis elegans and the bioactive compounds of the extracts were also identified. The solvent extracts of R. crispus were tested against C. elegans for up to 72 h. The effect of the extracts on C. elegans was examined using light microscopy (LM) and scanning electron microscopy (SEM). LM and SEM analysis showed damage on the body wall, reduced body and slight modifications of the nematode organs. The lethality test reveals a significant reduction in the viability of the nematode with the water extract of leaf (LF-WAE), among others, having the strongest potency against the nematode, with 83% lethality. Anlysis done with Fourier-transform infrared spectroscopy (FTIR) spectra reveals various characteristic vibration bands and fingerprint bands at 3400–600 cm⁻¹, identifying phenols, organic acids, aromatics, amines, among others in the plant. The compounds were identified with liquid chromatography-mass spectrometry (LC-MS), under the categories of flavonoids, steroidal alkaloids and proanthocyanidin. In conclusion, this study confirmed that R. crispus has anthelmintic potential, using standardised C. elegans models as a tool and suggests that there could be novel compounds yet to be explored in the studied plant that could be of great benefit to livestock and humans.Keyword: Caenorhabditis elegans, Gastrointestinal infections, Anthelmintic drug, Bioactive compounds, Phytochemical, Ethnoveterinary therapists     

Evaluation of the in vitro activity of dermaseptin 01, a cationic antimicrobial peptide, against Schistosoma mansoni

Schistosomiasis is a neglected tropical disease that remains a considerable public health problem worldwide. Since the mainstay of schistosomiasis control is chemotherapy with a single drug, praziquantel, drug resistance is a concern. Here, we examined the in vitro effects of dermaseptin 01 (DS 01), an antimicrobial peptide found in the skin secretion of frogs of the genus Phyllomedusa, on Schistosoma mansoni adult worms. DS 01 at a concentration of 100 μg/ml reduced the worm motor activity and caused the death of all worms within 48 h in RPMI 1640 medium. At the highest sublethal concentration of antimicrobial peptide (75 μg/ml), a 100% reduction in egg output of paired female worms was observed. Additionally, DS 01 induced morphological alterations on the tegument of S. mansoni, and a quantitative analysis carried out by confocal microscopy revealed extensive destruction of the tubercles in a dose-dependent manner over the concentration range of 50-200 μg/ml. It was the first time that an anthelmintic activity towards schistosomes has been reported for a dermaseptin.     

Synthesis and antimicrobial activity of cysteine-free coprisin nonapeptides

Coprisin is a 43-mer defensin-like peptide from the dung beetle, Copris tripartitus. CopA3 (LLCIALRKK-NH₂), a 9-mer peptide containing a single free cysteine residue at position 3 of its sequence, was derived from the α-helical region of coprisin and exhibits potent antibacterial and anti-inflammatory activities. The single cysteine implies a tendency for dimerization; however, it remains unknown whether this cysteine residue is indispensible for CopA3’s antimicrobial activity. To address this issue, in the present study we synthesized eight cysteine-substituted monomeric CopA3 analogs and two dimeric analogs, CopA3 (Dimer) and CopIK (Dimer), and evaluated their antimicrobial effects against bacteria and fungi, as well as their hemolytic activity toward human erythrocytes. Under physiological conditions, CopA3 (Mono) exhibits a 6/4 (monomer/dimer) molar ratio in HPLC area percent, indicating that its effects on bacterial strains likely reflect a CopA3 (Mono)/CopA3 (Dimer) mixture. We also report the identification of CopW, a new cysteine-free nonapeptide derived from CopA3 that has potent antimicrobial activity with virtually no hemolytic activity. Apparently, the cysteine residue in CopA3 is not essential for its antimicrobial function. Notably, CopW also exhibited significant synergistic activity with ampicillin and showed more potent antifungal activity than either wild-type coprisin or melittin.     

Biodiversity of endophytic fungi in different leaf ages of Calotropis procera and their antimicrobial activity

Calotropis procera has many important medicinal properties with proven pharmacological potential. Some of these properties may be mediated by its fungal endophytes. This study analyzed, for the first time, the community of endophytic fungi of C. procera outside its region of origin. A total of 156 fungal isolates distributed across 19 taxa were obtained from 468 fragments of C. procera leaves at different stages of maturation. The rate of endophyte colonization increased with the leaf age/development. The dominant species of endophytic fungi of C. procera introduced in Northeast Brazil were different from those found in studies on the same species and other species of the same genus in native regions. The dominant endophyte was Phaeoramularia calotropidis (63.5 %), followed by Guignardia bidwellii (21.1 %). Six isolates of endophytic fungi showed antimicrobial activity against human pathogenic micro-organisms and one plant pathogenic fungus. The antibacterial activity was more intense than the antifungal activity. The endophytic Curvularia pallescens (URM 6048) stood out inhibited Gram-positive bacteria, Staphylococcus aureus, Streptococcus pyogenes, the plant pathogenic fungus Colletotrichum dematium. Ecological and biotechnological aspects of endophytic mycota are discussed.     

Assessment of the antimicrobial activity of the lipoidal and pigment extracts of Punica granatum L. leaves

Punica granatum L. is one of the famous and old species belonging to Family Punicaceae. The lipoidal and natural pigment extracts of the pomegranate were screened for their antimicrobial activity against nine different microbial pathogens. Three different doses of each extract (50, 100 and 150?μl) at three different contact times (15, 30 and 60?min) were examined. Results can be cleared that, all tested microbial pathogens were inhibited by 150?μl of both extracts at 60?min. Furthermore, the removal efficiency of n-hexane extract was powerful than the pigment extract. Also, the quantitative evaluation of the pigments in the leaves was performed using spectroscopical and HPLC analyses, carotenoids and chlorophylls content of P. granatum L. leaves were spectroscopically determined (mg/g) as 6.7?±?0.214 and 4.9?±?0.251, respectively. Chlorophyll a and b were 2.33?±?0.014 and 1.51?±?0.023, respectively. HPLC analysis of lutein and β-carotene were investigated as 3.652 and 1.915?mg/g. GC/MS analysis of the saponifiable and unsaponifiable fraction of n-hexane extract was carried out and α-amyrin acetate, ergosterol, and α-tocopherol were isolated, purified and identified using different spectroscopical methods. Toxicity assessment demonstrated their high biocompatibility since no toxic effect was recorded.     

Anthelmintic,anticoccidial and antioxidant activity of Salvadora persica root extracts

Human infection with parasites is still one of the big problems worldwide. Medicinal plants succeeded to overcome a variety of protozoan and helminthic parasites. In this study, Salvadora persica root extracts (SE) were used to treat helminthosis and coccideosis. Three doses were used (200, 100 and 50 mg/ml) to study the anthelmintic activity of S. persica. Allolobophora caliginosa was used as a model worm. Also, Albendazole was used as a reference drug. In order to study the anticoccideal activity of SE, a group of mice were infected with Eimeria papillata sporulated oocysts. Experimental mice were treated with SE (300 mg/Kg) for 5 days. The extract was able to decrease the number of meronts and gamonts of the parasite in jejunum. Also, it regulates the level of glutathione and malondialdehyde and the activity of catalase as well. We conclude that S. persica possesses a powerful Anthelmintic, anticoccidial and antioxidant activity.     

In vitro antimicrobial activity of propolis and synergism between propolis and antimicrobial drugs

The aim of this study was to investigate antimicrobial properties of ethanolic extract of 13 propolis (EEP) samples from different regions of Serbia against 39 microorganisms (14 resistant or multiresistant to antibiotics), and to determine synergistic activity between antimicrobials and propolis. Antimicrobial activity of propolis samples was evaluated by agar diffusion and agar dilution method. The synergistic action of propolis with antimicrobial drugs was assayed by the disc diffusion method on agar containing subinhibitory concentrations of propolis. Obtained results indicate that EEP, irrespectively of microbial resistance to antibiotics, showed significant antimicrobial activities against Gram-positive bacteria (MIC 0.078%–1.25% of EEP) and yeasts (0.16%–1.25%), while Gram-negative bacteria were less susceptible (1.25&%ndash;>5%). Enterococcus faecalis was the most resistant Gram-positive bacterium, Salmonella spp. the most resistant Gram-negative bacteria, and Candida albicans the most resistant yeast. EEP showed synergism with selected antibiotics, and displayed ability to enhance the activities of antifungals. The shown antimicrobial potential of propolis alone or in combination with certain antibiotics and antifungals is of potential medical interest.     

Optimal methods for evaluating antimicrobial activities from plant extracts

The search for antimicrobial agents from plants has been a growing interest in the last few decades. However, results generated from many of these studies cannot be directly compared due to the absence of standardization in particular antimicrobial methods employed. The need for established methods with consistent results for the evaluation of antimicrobial activities from plant extracts has been proposed by many researchers. Nevertheless, there are still many studies reported in the literature describing different methodologies. The aim of this study was to find optimal methods to give consistent quantitative antimicrobial results for studying plant extracts. Three different agar-based assays (pour plate disc diffusion (PPDD), streak plate disc diffusion (SPDD) and well-in agar (WA)) and one broth-based (turbidometric (TB)) assay were used in this study. Extracts from two plant species (Duabanga grandiflora and Acalypha wilkesiana) were tested on two bacterial species, namely Escherichia coli and Staphylococcus aureus. Amongst the agar-based assays, PPDD produced the most reproducible results. TB was able to show the inhibitory effects of the test samples on the growth kinetic of the bacteria including plant extracts with low polarity. We propose that both agar- (i.e PPDD) and broth-based assays should be employed when assessing the antimicrobial activity of plant crude extracts.     

Synthesis and antimicrobial activity of meso-substituted polymethine cyanine dyes

The condensation reaction of equivalent amounts of 2-cyanomethyl benzooxazole or its derivatives with variously substituted aromatic aldehydes gave 2-cyano-styryl benzooxazole or its derivatives. The subsequent reaction of the 2-cyano-styryl benzooxazoles with 2(4)-methyl substituted heterocyclic quaternary salts afforded meso-substituted styryl-2(4)-polymethine cyanines. The condensation reaction of 2-cyanomethyl benzooxazole or its derivatives with alpha-nitroso-beta-naphthol followed by reaction with 2(4)-methyl substituted heterocyclic quaternary salts gave meso-substituted aza-2(4)-polymethine cyanines. The reaction of 2-cyanomethyl benzooxazole or its derivatives with N-methyl heterocyclic quaternary salts followed by the reaction with 2-methylquinolinium methiodide afforded the corresponding meso-substituted trimethine cyanine dyes. Elemental analyses, visible absorption, IR, (1)H NMR spectroscopy, and mass spectra established the structures of these compounds. The relationship between the structure and properties of these dyes has been studied and the solvatochromic behavior of some selected cyanine dyes in organic solvents is discussed. Finally, the antimicrobial activity of selected novel dyes was investigated in vitro using a wide spectrum of microbial strains.     

Plasmodium chabaudi-infected mice spleen response to synthesized silver nanoparticles from Indigofera oblongifolia extract

Malaria is a worldwide serious-threatening infectious disease caused by Plasmodium and the parasite resistance to antimalarial drugs has confirmed a significant obstacle to novel therapeutic antimalarial drugs. In this article, we assessed the antioxidant and anti-inflammatory activity of nanoparticles prepared from Indigofera oblongifolia extract (AgNPs) against the infection with Plasmodium chabaudi caused in mice spleen. AgNPs could significantly suppress the parasitaemia caused by the parasite to approximately 98% on day 7 postinfection with P. chabaudi and could improve the histopathological induced spleen damage. Also, AgNPs were able to increase the capsule thickness of the infected mice spleen. In addition, the AgNPs functioned as an antioxidant agent that affects the change in glutathione, nitric oxide and catalase levels in the spleen. Moreover spleen IL1β, IL-6 and TNF-α-mRNA expression was regulated by AgNPs administration to the infected mice. These results indicated the anti-oxidant and the anti-inflammatory protective role of AgNPs against P. chabaudi-induced spleen injury.     

Membrane-active antimicrobial peptides and human placental lysosomal extracts are highly active against mycobacteria

Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis, manifests discreet strategies to subvert host immune responses, which enable the pathogen to survive and multiply inside the macrophages. This problem is further worsened by the emergence of multidrug resistant mycobacterial strains, which make most of the anti-tuberculous drugs ineffective. It is thus imperative to search for and design better therapeutic strategies, including employment of new antibiotics. Recently, naturally produced antimicrobial molecules such as enzymes, peptides and their synthetic analogs have emerged as compounds with potentially significant therapeutical applications. Although, many antimicrobial peptides have been identified only very few of them have been tested against mycobacteria. A major limitation in using peptides as therapeutics is their sensitivity to enzymatic degradation or inactivity under certain physiological conditions such as relatively high salt concentration. Here, we show that NK-2, a peptide representing the cationic core region of the lymphocytic effector protein NK-lysin, and Ci-MAM-A24, a synthetic salt-tolerant peptide derived from immune cells of Ciona intestinalis, efficiently kill Mycobacterium smegmatis and Mycobacterium bovis-BCG. In addition, NK-2 and Ci-MAM-A24 showed a synergistic killing effect against M. smegmatis, no cytotoxic effect on mouse macrophages at bactericidal concentrations, and were even found to kill mycobacteria residing inside the macrophages. We also show that human placental lysosomal contents exert potent killing effect against mycobacteria under acidic and reducing growth conditions. Electron microscopic studies demonstrate that the lysosomal extract disintegrate bacterial cell membrane resulting in killing of mycobacteria.     

Peroxidase-like activity and antimicrobial properties of curcumin-inorganic hybrid nanostructure

For the first time in this study, curcumin was utilized as an organic component reacting with Cu (II) ion (Cu²⁺) as an inorganic component for fabrication of curcumin based Cu hybrid nanostructure (Cu-hNs). We also systematically examined the catalytic effect towards guaiacol and antimicrobial activities of Cu-hNs towards fish pathogen bacteria. For the characterization of Cu-hNs, Scanning Electron Microscopy (SEM), Energy Dispersive X-ray spectroscopy (EDX) and Fourier transform infrared spectrometry (FT-IR) analysis were used. We claimed that hydroxyl group might react with Cu²⁺ in phosphate solution (PO₄^-3) to form Cu-hNs. However, more uniform and spherical Cu-hNs were not seen owing to absence of more reactive functional groups like amine and carboxyl groups on structure of curcumin. In addition to our findings, synthesis of Cu-hNs were carried out in the various pH values to evaluate the effect of pHs on formation of Cu-hNs. The Cu-hNs exhibited remarkable catalytic activity throught the Fenton reaction in the presence of hydrogen peroxide (H₂O₂) and effective antimicrobial activities against Gram-positive/negative fish pathogen bacteria. In this study, cheap and efficient synthesis of nanoflowers (NFs) using plant extracts is proposed for biomedical applications rather than expensive molecules such as amino acids and DNA.     

Characterization and antimicrobial activity of the bioactive metabolites in streptomycete isolates

Twenty different streptomycete isolates were obtained from soils of southeast Serbia. Five isolates identified as Streptomyces hygroscopicus (SH100, SH101, SH102, SH103, and SH104) showed strong activity against Botrytis cinerea, a parasite found in domestic vines. These isolates were extensively studied for their in vitro antimicrobial activity against Gram-positive bacteria, Gram-negative bacteria, yeasts and fungi, and also antiviral activity against Herpes simplex. The results indicated that the obtained isolates were highly active against Botrytis cinerea, Candida albicans, and Herpes simplex, with an inhibition zone at ≥31 mm. The structure of the bioactive components was determined using elemental analysis, as well as UV/VIS, FTIR, and TLC.     

Screening of plant extracts for antimicrobial activity against bacteria and yeasts with dermatological relevance

There is cumulative resistance against antibiotics of many bacteria. Therefore, the development of new antiseptics and antimicrobial agents for the treatment of skin infections is of increasing interest. We have screened six plant extracts and isolated compounds for antimicrobial effects on bacteria and yeasts with dermatological relevance. The following plant extracts have been tested: Gentiana lutea, Harpagophytum procumbens, Boswellia serrata (dry extracts), Usnea barbata, Rosmarinus officinalis and Salvia officinalis (supercritical carbon dioxide [CO2] extracts). Additionally, the following characteristic plant substances were tested: usnic acid, carnosol, carnosic acid, ursolic acid, oleanolic acid, harpagoside, boswellic acid and gentiopicroside. The extracts and compounds were tested against 29 aerobic and anaerobic bacteria and yeasts in the agar dilution test. U. barbata-extract and usnic acid were the most active compounds, especially in anaerobic bacteria. Usnea CO2-extract effectively inhibited the growth of several Gram-positive bacteria like Staphylococcus aureus (including methicillin-resistant strains - MRSA), Propionibacterium acnes and Corynebacterium species. Growth of the dimorphic yeast Malassezia furfur was also inhibited by Usnea-extract. Besides the Usnea-extract, Rosmarinus-, Salvia-, Boswellia- and Harpagophytum-extracts proved to be effective against a panel of bacteria. It is concluded that due to their antimicrobial effects some of the plant extracts may be used for the topical treatment of skin disorders like acne vulgaris and seborrhoic eczema.     

Synthesis and antimicrobial activity of some new hydrazone-bridged thiazole-pyrrole derivatives

In this work, we synthesized fourteen different compounds which contain hydrazone bridged thiazole and pyrrole rings. For this purpose, pyrrole-2-carboxaldehydes were reacted directly with thiosemicarbazide in ethanol and then obtained thiosemicarbazones were condensed with α-bromoacetophenone derivatives (Hantzsch reaction) to give 1-substituted pyrrole-2-carboxaldehyde [4-(4-substituted phenyl)-1,3-thiazol-2-yl] hydrazones. The structures of the obtained compounds were elucidated by using IR, ¹H-NMR and FAB⁺-MS spectral data and elemental analyses results. All of the compounds were screened for their antibacterial and antifungal activities against twelve different microorganisms by using microbroth dilution method. Ketoconazole and chloramphenicol were used as standard drugs. All of the compounds showed good activity against Staphylococcus aureus and Enterococcus faecalis.     

Truncated antimicrobial peptides from marine organisms retain anticancer activity and antibacterial activity against multidrug-resistant Staphylococcus aureus

Antimicrobial peptides (AMPs) were recently determined to be potential candidates for treating drug-resistant bacterial infections. The aim of this study was to develop shorter AMP fragments that combine maximal bactericidal effect with minimal synthesis cost. We first synthesized a series of truncated forms of AMPs (anti-lipopolysaccharide factor from shrimp, epinecidin from grouper, and pardaxin from Pardachirus marmoratus). The minimum inhibitory concentrations (MICs) of modified AMPs against ten bacterial species were determined. We also examined the synergy between peptide and non-peptide antibiotics. In addition, we measured the inhibitory rate of cancer cells treated with AMPs by MTS assay. We found that two modified antibacterial peptides (epinecidin-8 and pardaxin-6) had a broad range of action against both gram-positive and gram-negative bacteria. Furthermore, epinecidin and pardaxin were demonstrated to have high antibacterial and anticancer activities, and both AMPs resulted in a significant synergistic improvement in the potencies of streptomycin and kanamycin against methicillin-resistant Staphylococcus aureus. Neither AMP induced significant hemolysis at their MICs. In addition, both AMPs inhibited human epithelial carcinoma (HeLa) and fibrosarcoma (HT-1080) cell growth. The functions of these truncated AMPs were similar to those of their full-length equivalents. In conclusion, we have successfully identified shorter, inexpensive fragments with maximal bactericidal activity. This study also provides an excellent basis for the investigation of potential synergies between peptide and non-peptide antibiotics, for a broad range of antimicrobial and anticancer activities.     

Synthesis and antimicrobial activity of imidazole and pyridine appended cholestane-based conjugates

A series of 3α-amino-5α-cholestane and 3α,7α-diamino-5α-cholestane derivatives containing imidazole and pyridine rings were synthesized by simple and effective reductive amination, and their in vitro activities against a range of Gram-positive and Gram-negative strains were evaluated. Most of the compound exhibited enhanced activity against MRSA pathogen. 3α,7α-Di(pyridylmethyl)amino-5α-cholestane 10 showed the highest potency in these series toward the Gram-positive bacteria, Staphylococcus epidermidis 887E, with the lowest MIC value of 1 μg/mL.     

The activity of antimicrobial peptide S-thanatin is independent on multidrug-resistant spectrum of bacteria

In this study, the activity of S-thanatin (an analog of antimicrobial peptide derived from thanatin) against different bacterial pathogens frequently which can cause therapeutic problems was tested. The result showed minimal inhibitory concentrations (MICs) of S-thanatin against all isolates of the Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Enterobacter aerogenes, Klebsiella ornithinolytica and Klebsiella oxytoca were in the range of 4-16 μg/ml, no matter which antibiotic the bacterial was resistant or susceptible, while almost all MICs to Gram-positive bacterial were >128 μg/ml except Enterococcus faecium. S-thanatin was more effective toward Gram-negative strains, especially for Enterobacter and Klebsiella. The MICs of S-thanatin were no significantly different in the same species regardless of antibiotic sensitive or -resistant isolates to single or multiple antibiotic (P > 0.05). Likewise, no notable difference could be observed between E. coli, K. pneumoniae, E. cloacae, E. aerogenes, K. ornithinolytica which were sensitive to S-thanatin (P > 0.05). It was implied that the antimicrobial activity of S-thanatin was independent on multi-drug resistance spectrum of bacteria.