Antinociceptive, anti-inflammatory and acute toxicity effects of Zhumeria majdae extracts in mice and rats

Antinociceptive and anti-inflammatory effects and acute toxicity of aqueous infusion and ethanolic maceration extracts of the aerial parts of Zhumeria majdae were studied in mice and rats. Antinociceptive activity was determined using hot-plate and writhing tests. The effect of the extracts against acute inflammation was studied by acetic acid increased vascular permeability and xylene-induced ear edema in mice. The activity of the extracts against chronic inflammation was assessed using the cotton pellet test in rats. LD50 values of the infusion and maceration extracts were 3.09 g/kg body wt., and 3.94 g/kg body wt., respectively. Phytochemical screening of the extracts indicated the presence of flavonoids and tannins. In the hot-plate test, the intraperitoneal injection of both extracts showed significant and dose-dependent antinociceptive activity in mice. Naloxone, an opioid antagonist, on pretreatment inhibited the antinociceptive activity of the extracts. The extracts exhibited antinociceptive activity against acetic acid-induced writhing, which was partially blocked by naloxone. Both extracts showed significant effect against acute inflammation induced by acetic acid in mice. In the chronic inflammation test, efficacy of the extracts was similar to that of baclofen and dexamethasone in rats. It is concluded that the aqueous infusion and ethanolic maceration extract of the aerial parts of Zhumeria majdae have antinociceptive effects and this may be mediated by opioid receptors. The extracts also showed anti-inflammatory effects against acute and chronic inflammation.     

Antimicrobial activities of 2-arylthio-N-alkylmaleimides

Summary A variety of 2-arylthio-N-alkylmaleimides were prepared, and their antimicrobial activities were examined. Almost all of these compounds exhibited antibacterial activity against Gram-positive bacteria such asBacillus subtilis andStaphylococcus aureus. Some compounds such as 2-(halogeno-phenyl)-thio-N-methylmaleimides (4, 5, 6, 8 and 10) and 2-(2-carbamoylphenyl)thio-N-methylmaleimide(35) exhibited antibacterial activity againstEscherichia coli. All compounds tested were inactive againstPseudomonas aeruginosa except 2-(2-carbamoylphenyl)thio-N-methylmaleimide(35) which was marginally active. Activities against Gram-positive bacteria were not due to the effect of the substituent on the benzene ring, except in the instances 2-carboxy, 2-carbomethoxy, 2-amino groups and alkyl chains, however, activities against Gram-negative bacteria were due to phenylthio and the alkyl substituents. Some of 2-arylthio-N-alkylmaleimides were examined for their antifungal activities using eight strains of fungi, and they showed activity against these.     

Active substances against trypomastigote forms of Trypanosoma cruzi and microorganisms are produced in sequence by Talaromyces flavus

The conditions for the sequential production of antibiotic activity by Talaromyces flavus were determined. The highest level of activity against Trypanosoma cruzi was obtained from the aqueous extract of the Czapeck's fermentative culture after 48 hours, with lysis of 97.58% of the trypomastigote forms of Trypanosoma cruzi (red blood cells remained normal). The antimicrobial activity was detected in the extracts of fermentative cultures from different media just after 144 hours of incubation. Maximum activities against Micrococcus luteus, Staphylococcus aureus and Candida albicans were present in chloroform, butanolic and water extracts, in this order, when Talaromyces flavus was cultivated at pH 5.0. The minimal inhibitory concentration (MIC) of extracts of Takeuchi's cultures were determined.     

Ribonuclease,deoxyribonuclease, and antiviral activity of <Emphasis Type="Italic">Escherichia coli</Emphasis>-expressed <Emphasis Type="Italic">Bougainvillea xbuttiana</Emphasis> antiviral protein 1

A full-length cDNA encoding ribosome-inactivating/antiviral protein from the leaves of Bougainvillea xbuttiana was recently isolated. The coding region of cDNA was cloned and expressed in Escherichia coli, and the protein product was designated as BBAP1 (Bougainvillea xbuttiana antiviral protein 1). BBAP1 showed ribonuclease activity against Torula yeast RNA. It also exhibited depurination activity against supercoiled pBlueScript SK+ plasmid DNA in a concentration dependent manner, and was found to convert nicked circular DNA into linear form only at higher concentration. On bioassay, BBAP1 exhibited antiviral activity against sunnhemp rosette virus infecting Cyamopsis tetragonoloba leaves in which 95% inhibition of local lesion formation was observed.     

Synthesis and biological activity of dialkylphosphocholines

A series of dialkylphosphocholines were prepared and evaluated for their biological activity. The antiprotozoal activity was determined against Acanthamoeba lugdunensis. Compound 15 exhibited excellent trophocidal activity. None of the tested dialkylphosphocholines exhibited better fungicidal activity against Candida albicans than miltefosine. The antineoplastic activity was determined against HeLa. The most cytotoxic was compound 10, which was more active against tumor cells as against normal cells.     

Antimicrobial evaluation of coumarins and flavonoids from the stems of Daphne gnidium L.

The antimicrobial activity of stems methanol extract from Daphne gnidium L. collected from Sardinia (Italy) was evaluated against 6 strains of standard and clinical isolated gram (+/-) bacteria. The antimicrobial effect on two strains of fungi was also tested. The extract in toto exhibited antibacterial activity against Bacillus lentus and Escherichia coli, but was inactive against fungi. Four coumarins (daphnetin, daphnin, acetylumbelliferone, daphnoretin) and seven flavonoids (luteolin, orientin, isoorientin, apigenin-7-O-glucoside, genkwanin, 5-O-beta-D-primeverosyl genkwanine, 2,5,7,4'-tetrahydroxyisoflavanol) present in the plant extract were also investigated against the same strains of bacteria and fungi assayed for the crude extract. The most active compounds were daphnetin, genkwanin, and 2,5,7,4'-tetrahydroxyisoflavanol.     

Synthesis and evaluation of bioactive naphthoquinones from the Brazilian medicinal plant, Tabebuia avellanedae

A series of naphthoquinones based on the naphtho[2,3-b]furan-4,9-dione skeleton such as (−)-5-hydroxy-2-(1′-hydoxyethyl)naphtho[2,3-b]furan-4,9-dione (1) and its positional isomer, (−)-8-hydroxy-2-(1′-hydoxyethyl)naphtho[2,3-b]furan-4,9-dione (2), which are secondary metabolites found in the inner bark of Tabebuia avellanedae, were stereoselectively synthesized and their biological activities were evaluated in conjunction with those of their corresponding enantiomers. Compound 1 exhibited potent antiproliferative effect against several human tumor cell lines, but its effect against some human normal cell lines was much lower than that of mitomycin. On the other hand, its enantiomer (R)-1 was less active toward the above tumor cell lines than 1. The antiproliferative effect of 2 against all tumor cell lines was significantly reduced. These results indicated the presence of the phenolic hydroxy group at C-5 is of great important for increasing antiproliferative effect. In addition, 1 also showed higher cancer chemopreventive activity than 2, while there were no significant differences between 1 and 2 in antimicrobial activity. Both compounds displayed modest antifungal and antibacterial activity (Gram-positive bacteria), whereas they were inactive against Gram-negative bacteria.     

Antibacterial activity of the leaf essential oil of <Emphasis Type="Italic">Blumea mollis</Emphasis> (D. Don) Merr.

The antibacterial activity of the leaf essential oil of Blumea mollis was assayed against 14 clinically isolated bacterial strains on Muller–Hinton Agar medium and Muller–Hinton Agar medium with 5% sheep blood. The essential oil had promising antibacterial activity against all the bacterial strains tested. The highest mean zone of inhibition and lowest values of minimum inhibitory concentration were recorded against methicillin-resistant Staphylococcus aureus followed by beta hemolytic Streptococcus pyogenes. The Gram-positive bacteria were more sensitive than Gram-negative bacteria. Among the bacterial strains tested, Psudomonas aeruginosa was resistant to the essential oil. The results of the present study suggest that the essential oil of B. mollis is one of the new medicinal resources as an antibacterial agent against the bacterial strains tested.     

Screening Antimicrobial Activities of Basic Protein Fractions from Dry and Germinated Wheat Seeds

Two small cationic peptide fractions (5 kDa) were isolated from dry and germinated seeds of wheat, named WAP and GWAP, respectively. The antifungal and antibacterial activities of the peptides were analyzed using disk diffusion and turbidity measurement assays. The peptides in vitro exhibited effective antifungal activity against four plant pathogenic fungi at minimum concentration of 15 g(protein) cm^–3. Their antimicrobial activity was negatively affected by the presence of 5 mM CaCl₂. The peptides were less effective against Gram-negative bacterium Erwinia carotovora subsp. carotovora, but they demonstrated inhibitory activity against Gram-positive bacterium Clavibacter michiganensis subsp. sepedonicus. The antimicrobial activity of GWAP was more effective than WAP.     

Physiological activities of a β-glucan produced by Panebacillus polymyxa

In vitro bioactivities of a beta-glucan produced by Panebacillus polymyxa JB115 were investigated. Nitric oxide production by RAW 264.7 macrophage cells pre-treated with beta-glucan JB115 (from 0.1 to 1 mg ml(-1)) was significantly increased, compared to that in untreated cells (P < 0.001). The beta-glucan JB115 increased superoxide radical-scavenging activity by 66% at 1 mg ml(-1). It also suppressed hyaluronidase (32%) and collagenase (33%) activities and, additionally, displayed antitumor activity, blocking the growth of Sarcoma 180 cells in a concentration-dependent manner. The immune-stimulatory, antioxidant, collagenase inhibitory and hyaluronidase inhibitory effects of the beta-glucan support its potential role in the prevention of bacterial disease against fish and in the protection of skin against aging.     

Investigation of the cyt gene in Bacillus thuringiensis and the biological activities of Bt isolates from the soil of China

The presence of cyt genes was investigated in 80 type strains of Bacillus thuringiensis and 143 isolates obtained from soil samples of China by PCR amplification using two pairs of primers for the cyt1 and cyt2 genes. Three type strains of serotypes H11ac, H14 and H36, eight isolates belonging to H3, H14, H18 and H21, and one isolate of unknown serotype harbored cyt genes. We also tested the cytolytic activity for mammal cells, the hemolytic activity for sheep erythrocytes and insecticidal activity against mosquitoes of five isolates that contained cyt genes but did not belong to B. thuringiensis serovar israelensis. The protein profiles of the five isolates were different from those of the type strains of B. thuringiensis serovar israelensis, and among the five isolates, only Y-5 showed mosquitocidal activity against larvae of Culex quinquefasciatus. All five of the isolates exhibited hemolytic activity, but only three could cause the cell death of A549 cells. The cytopathological changes induced by NX-4 in some A549 cells were characterized with cell-ballooning.     

In vitro antibacterial activity of laboratory grown culture of Spirulina platensis

The hexane, ethyl acetate, dichloromethane, methanol extracts and spent media (extracellular substances) were tested in vitro for their antibacterial activity for which one Gram-positive bacterium (Staphylococcus aureus) and four Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, and Klebsiella pneumoniae) were used as test organisms. The methanol extract showed more potent activity than other organic extracts, spent medium of the culture exhibited little activity against E. coli only. No inhibitory effect was found against Klebsiella pneumoniae.The broth microdilution assay gave minimum inhibitory concentrations (MIC) values ranging from 1 to 512 μg/ml. The MIC of methanol extract against S. aureus and E. coli were 128 μg/ml and 256 μg/ml, respectively.     

Antimicrobial, antioxidant, and antiviral activities of Retama raetam (Forssk.) Webb flowers growing in Tunisia

Antimicrobial, antioxidant, and antiviral activities of flower extracts of Retama raetam Forssk. Webb (Fabaceae) were screened both from standard and isolated Gram-positive and Gram-negative bacteria by solid medium technique. Oxacillin, Amoxicillin, Ticarcillin, Cefotaxim, and Amphotericin were used as the control agents. The antiviral activity was evaluated against human cytomegalovirus (HCMV) strain AD-169 (ATCC Ref. VR 538) and coxsackie B virus type 3 (CoxB-3) using a cytopathic effect (CPE) reduction assay. The antioxidant activity was evaluated using two tests: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free-radical scavenging and the ammonium thiocyanate methods. All extracts were characterized quantitatively for the presence of polyphenols, flavonoids, and tannins. Of the extracts tested, butanol and ethyl acetate extracts showed important antibacterial activity against Gram-positive and Gram-negative bacteria but only moderate antifungal activity. Methanol extract exhibited moderate antiviral activity against HCMV with IC₅₀ of 250 μg/ml. Ethyl acetate, chloroform, and methanol fractions were found to cause significant free-radical-scavenging effects in both assays. These results may suggest that R. raetam flowers could be used as a natural preservative ingredient in the food and/or pharmaceutical industries.     

Pharmacological and toxicological activity of Heterophyllaea pustulata anthraquinone extracts

Benzenic extracts from both stems and leaves of Heterophyllaea pustulata showed the most significant activity in vivo in the Brine Shrimp Lethally Test (BST), relative to others of different polarity. They were therefore selected for in vitro antimicrobial activity studies. Bacteriostatic activity against Micrococcus luteus ATCC 9341 was detected, selectively inhibiting both oxacillin-sensitive and -resistant Staphylococcus aureus, among several gram-positive and gram-negative bacterial species tested. Antifungal activity against important opportunist microorganisms and against those involved in superficial mycosis, all from nosocomial origin was also detected. A chemical screening revealed the presence of anthraquinones as major compounds. Among them, we identified damnacanthal, rubiadin, 2-hydroxy-3-methyl anthraquinone, soranjidiol, rubiadin-1-methyl ether, and damnacanthol in the benzenic stem extract. The benzenic leaf extract shows a similar chemical composition, except for damnacanthal, damnacanthol, soranjidiol-1-methyl ether, and 3 anthraquinones whose structures have not yet been elucidated. Acute toxicity studies revealed a low toxicity in mice for the anthraquinonic extracts, as measured in the LD50 value (123 mg/kg body wt. i.v.), and death was not observed at doses of up to 4000 mg/kg body wt. s.c.     

Nematicidal activity of <Emphasis Type="Italic">Paecilomyces</Emphasis> spp. and isolation of a novel active compound

Many species of Paecilomyces are entomogenous fungi and several are efficacious toward nematodes. To study the potential of Paecilomyces species in controlling nematodes, fungal extracts of 40 Paecilomyces spp. were evaluated for their nematicidal activity against Bursaphelenchus xylophilus and Panagrellus redivivus. The extracts of six Paecilomyces spp. exhibited the nematicidal activity against P. redivivus, and 11 species exhibited the nematicidal activity against B. xylophilus. The methanol extract of strain 1.01761 incubating on Czapek solid medium killed more than 95% P. redivivus in 24 h at 5 mg/ml, and the filtrate of strain 1.01788 cultured in Sabouraud’s broth medium resulted in 90% mortality of B. xylophilus in 24 h at 5 mg/ml. A novel nematicidal compound 4-(4′-carboxy-2′-ethyl-hydroxypentyl)-5,6-dihydro-6-methylcyclobuta[b]pyridine-3,6-dicarboxylic acid, was isolated from Paecilomyces sp. YMF1.01761. The LD₅₀ value of the compound within 24 h against P. redivivus was 50.86 mg/L, against Meloidogyne incognita was 47.1 mg/L, and against B. xylophilus was 167.7 mg/L.     

Antiviral and antimicrobial activities of three sesquiterpene lactones from Centaurea solstitialis L. ssp. solstitialis

Three sesquiterpene lactones (centaurepensin=chlorohyssopifolin A, chlorojanerin and 13-acetyl solstitialin A) isolated from the aerial parts of Centaurea solstitialis L. ssp. solstitialis (Asteraceae) were investigated for antimicrobial and antiviral activities. For the antimicrobial activity assessment, both standard and isolated strains of Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, Staphylococcus aureus, Candida albicans and C. parapsilosis were employed by the microdilution method. Herpes simplex type-1, a DNA virus, and Parainfluenza, an RNA virus, were employed for the determination of the antiviral activity of these three sesquiterpene lactones using Vero cell lines. Ampicilline, ofloxocine, ketoconazole, fluconazole, acyclovir and oseltamivir were used as the reference drugs. 13-Acetyl solstitialin A displayed remarkable antibacterial activity against isolated strains of E. faecalis at 1 μg/ml concentration, which was close to the effective concentrations of ampicillin. The same compound also showed significant activity against the DNA virus, being as potent as the reference compound acyclovir at maximum and minimum concentrations of 16–<0.00006 μg/ml. This is the first report showing that 13-acetyl solstitialin A possesses significant antiviral activity.     

Composition and biological activities of essential oils from Limnophila geoffrayi Bonati

Essential oils from the dried aerial parts of Limnophila geoffrayi Bonati were obtained by water-distillation. d-Pulegone (27.14%), perillaldehyde (19.13%) and limonene (9.00%) were characterized as the major constituents using gas chromatography-mass spectrometry analysis. The antimicrobial activities of the essential oils and their major components were evaluated against microorganisms encountered normally in contaminated cosmetic products, using the agar- and broth-dilution methods. Their insecticidal activities against the Oriental fruit fly Bactrocera dorsalis (Hendel) were tested using a bioassay with impregnated filter paper. The results showed that the essential oils possessed high antimicrobial activity, with minimum inhibitory concentrations ranging from 0.03 to 0.2% per unit volume (v/v). Strong insecticidal activity as a fumigant was also observed at an oil dose of 5 μl/disc, with a 94% mortality. Perillaldehyde was the most active compound among the main components of these essential oils.     

Antibacterial efficacy of Withania somnifera (ashwagandha) an indigenous medicinal plant against experimental murine salmonellosis

In the present study, we evaluated the antibacterial activity of ashwagandha [Withania somnifera L. Dunal (Solanaceae; root and leaves)], an Indian traditional medicinal plant against pathogenic bacteria. Both aqueous as well as alcoholic extracts of the plant (root as well as leaves) were found to possess strong antibacterial activity against a range of bacteria, as revealed by in vitro Agar Well Diffusion Method. The methanolic extract was further subfractionated using various solvents and the butanolic sub-fraction was found to possess maximum inhibitory activity against a spectrum of bacteria including Salmonella typhimurium. Moreover, in contrast to the synthetic antibiotic (viz. chloramphenicol), these extracts did not induce lysis on incubation with human erythrocytes, advocating their safety to the living cells. Finally, the antibacterial efficacy of the extracts isolated from plant (both root and leaves) was determined against experimental salmonellosis in Balb/C mice. Oral administration of the aqueous extracts successfully obliterated salmonella infection in Balb/C mice as revealed by increased survival rate as well as less bacterial load in various vital organs of the treated animals.     

Antibacterial, antifungal, and antiviral activities of the lipophylic extracts of Pistacia vera

In the present study, antibacterial, antifungal, and antiviral properties of 15 lipohylic extracts obtained from different parts (leaf, branch, stem, kernel, shell skins, seeds) of Pistacia vera were screened against both standard and the isolated strains of Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, Staphylococcus aureus, Candida albicans and C. parapsilosis by microdilution method. Both Herpes simplex (DNA) and Parainfluenza viruses (RNA) were used for the determination of antiviral activity of the P. vera extracts by using Vero cell line. Ampicilline, ofloxocine, ketoconazole, fluconazole, acyclovir and oseltamivir were used as the control agents. The extracts showed little antibacterial activity between the range of 128-256 microg/ml concentrations whereas they had noticeable antifungal activity at the same concentrations. Kernel and seed extracts showed significant antiviral activity compared to the rest of the extracts as well as the controls.     

Synthesis and evaluation of N-alkyl-beta-D-glucosylamines on the growth of two wood fungi, Coriolus versicolor and Poria placenta

Various glucosylamines were synthesized from glucose and different alkyl amine compounds. These amino compounds are beta-d-glucopyranosylamine (GPA), N-ethyl-beta-d-glucopyranosylamine (EtGPA), N-butyl-beta-d-glucopyranosylamine (BuGPA), N-hexyl-beta-d-glucopyranosylamine (HeGPA), N-octyl-beta-d-glucopyranosylamine (OcGPA), N-dodecyl-beta-d-glucopyranosylamine (DoGPA), N-(2-hydroxyethyl)-beta-d-glucopyranosylamine (HEtGPA) and N,N-di(2-hydroxyethyl)-beta-d-glucopyranosylamine (DHEtGPA). They were tested for their antifungal activity against the growth of Coriolus versicolor and Poria placenta. An improvement of the antifungal activity with the increase of alkyl chain length was observed. DoGPA exhibited the best antifungal activity against both strains. It completely inhibited the fungal growth at 0.01x10(-3)molmL(-1) and 0.0075x10(-3)molmL(-1) for C. versicolor and P. placenta, respectively. For other glucosylamines higher concentrations were needed for complete inhibition of fungi.