Isolation, structural identification of secondary metabolites from Pseudomonas aeruginosa HBD-12 with antibacterial and antitumor activities / 生物工程学报

To screen strains with antibacterial and antitumor activity, pregnenolone was used as the sole carbon source for screening bacteria from soil. Based on bacteriostatic activity assay, Pseudomonas aeruginosa HBD-12 was found to be effectively inhibiting the growth of Escherichia coli, Bacillus thuringiensis, Penicillium digitatum and Penicillium italicum, and its fermentation broth was separated and purified using column chromatography. Then, structure of the obtained monomeric compounds was analyzed by spectrum analysis, and their antitumor activity was measured using HTRF kinase detection kit. The isolated monomeric compounds 1-hydroxy-9,10-phenanthroline and 3-hydroxy-9,10-dihydrophenanthroline had significant antitumor activity. At 20 μg/mL, 1-hydroxy-9,10-phenanthroline and 3-hydroxy-9,10-dihydrophenanthroline inhibited 78.39±2.29% and 60.34±8.35% Aurora kinase A, respectively. Therefore, the secondary metabolites of Pseudomonas aeruginosa HBD-12 have the potential to develop antibacterial and antitumor drugs.

Study on in vitro Bacteriostatic Activity of the Extracts from Miao Medicine Polygonum runcinatum / 中国药房

OBJECTIVE:To study in vitro bacteriostatic activity of the extracts from Miao medicine Polygonum runcinatum. METHODS:Using chloramphenicol and fluconazole as positive control,the inhibitory effects of water extract,95％ ethanol extract and its ethyl acetate and n-butanol fraction on 9 kinds of strains were determined by cup plate method, such as Staphylococcus aureus,Escherichia coli,Shigella flexneri,Salmonella typhi,Bacillus subtilis,Pseudomonas aeruginosa,type B Hemolytic streptococcus,Candida albicans and Cryptococcus neoformans. The parts with bacteriostatic activity and trial strains sensitive to drug were screened. Micro-broth dilution method and agar culture medium plate method were used to determine MIC and MBC of 95％ ethanol extract and its fractions of P. runcinatum to sensitive strains. RESULTS:The water extract of P. runcinatum almost had no inhibitory effect. 95％ ethanol extract showed different degrees of bacteriostatic activity to strains;bacteriostatic effects of it to 6 kinds of bacteria as S. typhi was better than that of type B H. streptococcus and 2 kinds of fungus. The ethyl acetate and n-butanol fraction of 95％ ethanol extracts showed good bacteriostatic effect and the ethyl acetate fraction had stronger effect,while all the fractions of 95％ ethanol extracts showed no inhibitory effect on fungus. MIC and MBC of 95％ethanol extract to above 6 kinds of bacteria were 6.25-12.5 and 12.5-25 mg/mL,respectively;MIC and MBC of ethyl acetate fraction were 3.13-6.25, 6.25-12.5 mg/mL; MIC and MBC of n-butanol fraction were 6.25-12.5, 12.5-25 mg/mL. CONCLUSIONS:95％ ethanol extract,ethyl acetate and n-butanol fractions of Miao medicine P. runcinatum have obvious in vitro bacteriostatic activity to 6 common bacterias as S. typhi.

Synthesis of β-Cyclodextrin-N-vinyl-2-pyrrolidone Water-SolubleCopolymer and Its Adsorption of Hydrophobic Drugs / 分析化学

β-Cyclodextrin-N-vinyl-2-pyrrolidone (CDM-NVP) copolymer was prepared by free radical chain reaction of N-vinyl-2-pyrrolidone (NVP) and β-CD maleate (CDM) with γ-ray as initiator.The synthesis conditions of CDM-NVP polymer were as follows: mass ratio of CDM to NVP was 1∶0.7 (CDM 3.6 g and NVP 2.52 g), irradiation dosage was 4 kGy, and DMF aqueous solution (50%, V/V) was set at 20 mL.Under the synthesis conditions, the yield of CDM-NVP was 84% and the weight-average molecular weight was 20 kD.The natamycin (NM) and carbendazim (MBC) could form stable inclusion complexes with CDM-NVP copolymer, and the solubility and fungicidal activity of the complexes were investigated.The stability constant of NM·CDM-NVP and MBC·CDM-NVP complexes at 303 K were 12, 988.54 L/mol and 865.94 L/mol, respectively.The complexes were characterized using phase solubility diagrams, nuclear magnetic resonance (NMR) spectra and ultraviolet (UV) spectra.The analysis of the biological activities of these two complexes indicated that they possessed enhancing fungicidal activities compared to NM and MBC alone.

Isolation, identification and structural characterization of secondary metabolites from amarine sponge-derived rare actinobacterium Dermacoccus sp. X4 / 生物工程学报

We isolated and identified the symbiotic and adnascent microorganisms from an unidentified sponge collected from 10-meter-deep seawater of the Paracel Islands in China. A total of 16 strains were obtained and identified. Through bacteriostatic activity assay, one of the strains, Dermacoccus sp. X4, was found to effectively inhibit the growth of Staphylococcus aureus. Subsequently, its secondary metabolites were purified by silica gel partition, octadecylsilane (ODS) reverse phase, Sephadex™LH-20 size exclusion, and C18 reverse phase chromatography. Using liquid chromatography, mass spectrometry, and nuclear magnetic resonance, three of the purified compounds were structurally characterized to be one 3-(4-hydroxybenzyl) hexahydropyrrolo [1,2-a]pyrazine-1,4-dione and two indole acid glycerides. This is the first report about indole acid glyceride isolated from microbial secondary metabolites, enriching marine drug candidate resources.

Study on bacteriostatic activity and stability of pine bark Oligomeric Proantho Cyanidins / 中国生化药物杂志

Objective To study the bacteriostatic activity and stability of pine bark Oligomeric Proantho Cyanidins. Methods By the K-B disk diffusion method, spoilage bacteria as experiment strains, to study the inhibition effects of the pine bark Oligomeric Proantho Cyanidins and the antimicrobial stability under certain temperature, pH, and UV exposure time. Results Pine bark Oligomeric Proantho Cyanidins had significant inhibitory effect on Gram positive bacteria (Staphylococcus aureus and Bacillus Sukatilis), which had better inhibition effects in the media neutral, but temperature and UV had little influence on the antimicrobial effects. The minimum inhibitory concentration (MIC) of pine bark Oligomeric Proantho Cyanidins against Staphylococcus aureus and Bacillus Sukatilis were 12.5 and 6.25 mg/mL, respective. However, on Gram negative bacteria(Escherichia coli and Pseudomonas aeruginosa) there was no obvious inhibition effects. Conclusion The pine bark Oligomeric Proantho Cyanidins has significant inhibitory effect on Gram positive bacteria, the inhibitory effect is stronger in the range of pH 6-7 , and the temperature and UV had a little effect on its antibacterial action, which means that the antibacterial action of pine bark Oligomeric Proantho Cyanidins had good stability.

Purification and characterization of structural and functional properties of two lectins from a marine sponge Spheciospongia vesparia.

The purification, structural and functional characterization of two different lectins (named Svl-1 and Svl-2) has been reported from the marine sponge Spheciospongia vesparia. Purification procedure includes ammonium sulfate precipitation, combined with chromatography including Octyl-Sepharose-(NH4)SO4 hydrophobic column and DEAE-Toyopearl anion-exchange column using a high performance liquid chromatography. The similarities in function, specificity for saccharides, molecular weight, amino acid content and the N-terminal sequence of two lectins suggest that these proteins are isolectins. Amino acid composition and fluorescence analyses reveal that they contain an intrachain disulfide bridge, which might contribute to their high thermal stability. Furthermore, the purified lectins exhibit antibacterial activity against the gram-negative bacteria Pseudomonas aeruginosa and E. coli, indicating that they may be involved in a recognition strategy and may play a role in the defense response function of the sponge. This is the first report on the isolation of lectins from the S. vesparia. The purified lectins represent a potential possible candidate for future application in the recognition or treatment of cancer cells.

In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates

Antihistaminics are widely used for various indications during microbial infection. Hence, this paper investigates the antimicrobial activities of 10 antihistaminics belonging to both old and new generations using multiresistant Gram-positive and Gram-negative clinical isolates. The bacteriostatic activity of antihistaminics was investigated by determining their MIC both by broth and agar dilution techniques against 29 bacterial strains. Azelastine, cyproheptadine, mequitazine and promethazine were the most active among the tested drugs. Diphenhydramine and cetirizine possessed weaker activity whereas doxylamine, fexofenadine and loratadine were inactive even at the highest tested concentration (1 mg/ml). The MIC of meclozine could not be determined as it precipitated with the used culture media. The MBC values of antihistaminics were almost identical to the corresponding MIC values. The bactericidal activity of antihistaminics was also studied by the viable count technique in sterile saline solution. Evident killing effects were exerted by mequitazine, meclozine, azelastine and cyproheptadine. Moreover, the dynamics of bactericidal activity of azelastine were studied by the viable count technique in nutrient broth. This activity was found to be concentration-dependant. This effect was reduced on increasing the inoculum size while it was increased on raising the pH. The post-antimicrobial effect of 100 fg/ml azelastine was also determined and reached up to 3.36 h.

Difusão de microrganismos, inibição do crescimento e atividade biocida do cianoacrilato super bonder / Diffusion, growth Inhibition and biocide activity of the super bonder cyanoacrylate

Os objetivos do presente trabalho foram avaliar se o Super Bonder" apresenta algum risco de veiculação de microorganismos em humanos e se possui alguma atividade bactericida ou bacteriostática para cocos gram-positivo. Foi testada a esterilidade de dez tubas do adesivo nos meios de cultivo BHI, agar sangue, agar Sabouraud com cloranfenicol e Mycosel. A provável ação bactericida ou bacteriostática do adesivo Super Bonder"', in vitro, foi verificada utilizando cepas de Staphylococcus aureus e staphylococcus epidermidir, semeadas em meio de cultura agar sangue e agar Mueller-Hinton. Nao foi observado crescimento de microrganismos nos meios de cultura contendo somente gotas de Super Bonder"'. No agar sangue, observou-se ausência de beta-hemólise e de crescimento bacteriano nas áreas de sobreposição do adesivo. Em agarMueller-Hinton, houve rarefação de colônias ao redor das gotas do cianoacrilato.Os dados deste trabalho mostram que a cola de cianoacrilato Super Bonder"' parece ser livre de contaminação por microrganismos e apresenta possfvel atividade bacteriostatica in vitro.

The purposes of the present study were to verify the human's risk of the Super Bondet microorganisms' diffusion and the probably biocide or bacteriostatic adhesive's activity for gram-positive cocci. The sterility of ten tubes of the adhesive was tested in BHI culture tube and blood-agar, agar-Sabouraud with cloranfenicol and Mycosel culture plates. The biocide or bacteriostatic activity of the Super Bondet adhesive, in vitro, was verified using cultures of Staphylococcus aureus and staphylococcus epidermidis,seeded on blood-agar and agar-Mueller-Hinton culture plates. No microorganisms' growth was observed in the culture plates containing only drops of the Super Bondet. In agar-Mueller-Hinton, zones with reduced number of colonies were noticed around the cyanoacrylate's drops. In blood-agar, absence of haemolysis-beta and bacterial growth were observed in the covered areas of the adhesive. According to the results of this investigation, the Super Bondet cyanoacrylate is free of microorganisms' diffusion and probably inhibits in vitro the bacterial growth.

Atractylodes lancea and Its Geo-Varieties / 中草药

The geo-herbalism of Cangzhu, Atractylodes lancea (Thunb.) DC. , was studied for itsstrict quality control. Samples of typical and representative populations of geo-herbal and non-geo herbalorigin were collected, examined and cultivated through field work. Volatile oils from samples of varioushabitats were determined by GC/MS, and their respective bacteriostatic minimum inhibitory concentration(MIC)determined. Results of the study showed that both the size of capitulum and cleft on the leaves var-ied greatly even in species of the same population. The main components in their volatile oil also variedgreatly with Maocangzhu (MCZ) contains atractylone (29.54%) and atractylodin (17.82%); that of Nan-cangzhu (NCZ) contains hinesol (61.86%) and β-eudesmol (19.79%), and Baicangzhu (BCZ) cantains βeudesmol or mixture of β-eudesmol and atractylone (over 30%). Volatile oils of speciaes from Luotina,Taibai, and Huanglong showed potent bacteriostatic activity against Streptococcus hemolyticus (SH), com-parable to penicillin or streptomycin. In conclusion, A. lancea is a polymorphic complex greatly influencedby geographic environment and a reasonable proposal is to name them by geo-herbal names such as: MCZas A. lancea var. maoshanensis Hu et Feng; NCZ as A. lancea subsp. luotianensis Hu et Feng; and BCZ asA. lancea var. chinensis (Bunge) Kitam other than independent species as A. chinensis Bunge. It was in-correct to say that MCZ has no atractylone in its volatile oil and therefore differs from A. macrocephalaKoidz. (Baizhu). Inhibitory activity of the volatile oils against SH and Pseudomonas aeruginosa (PA) arealso quite different due to the habitats and imply that the rhizome from Luotian may be used to cure infec-tion diseases caused by SH and PA besides their traditional uses.

Pharmacodynamic of Guanhuang Ganmao Capsule / 中成药

AIM: To study the pharmacodynamics of Guanhuang Ganmao Capsule. METHODS: Antiviral effect of Guanhuang Ganmao Capsule was investigated by infecting chicken embryo with N_1H_1; its antipyretic action was evaluated with rabbit pyrogentic test induced by bacterial endotoxin; anti-inflammation by rats swelling test with injection of 1% agar and mice abdominal capillary permeability test with dimethylbanzene; the antitussive activities were investigated through testing cough times induced by ammonium hydroxide and sulfur dioxide in mice; the expectorant activities of it were studied by testing the amount of phlegm secreted in mice; The antibacterial effects in vivo were evaluated in mice with induced systematic infection. RESULTS: Guanhuang Ganmao Capsules had obvious antiviral action, antipyretic action, anti-inflammation and antitussive action. It took expectorant effect. The capsules markedly reduced death rate of staphylococcus aureus infection in mice. CONCLUSION: Guanhuang Ganmao Capsules possess antiviral; antipyretic; antitussive and expectorant effects as well as anti-inflammation