Water soluble skin secretions of six common Chinese amphibians were studied for their biological and enzymatic activities.The skin secretions of Tylototriton verrucosus,Bombina maxima ,and Bufo andrewsi were f...Water soluble skin secretions of six common Chinese amphibians were studied for their biological and enzymatic activities.The skin secretions of Tylototriton verrucosus,Bombina maxima ,and Bufo andrewsi were found toxic to mice with the intraperitoneal LD 50 of 11 5?mg/kg,18 8?mg/kg,and 264?mg/kg,respectively.No acute lethal toxicities were observed for the skin secretions of Rana nigromaculata,Rana guentheri and Rana limnocharis in a dose up to 500?mg/kg.The lethal toxicities of the skin secretions of T verrucosus and B maxima to mice are in the same grade as those of Viperidae snake venoms.The toxic components in T verrucosus and B maxima skin secretions are the proteins with molecular weights ranging from 3 to 60?kDa.All the skin secretions had both proteolytic activity and trypsin inhibitory activity.The skin secretions from T verrucosus , B maxima and B andrewsi also displayed wide spectrum antimicrobial activity.On the other hand,the skin secretions from B andrewsi and B maxima showed cytotoxicity on human cancer cells.All the six samples had not significant effects on mammalian blood coagulation system.Phospholipase A 2 activity was only found in the skin secretions of T verrucosus .None of these skin secretions showed acetylcholine esterase activity.展开更多
Twenty-two nitrate nonutilizing (nit) mutants were recovered from five wild-type isolates of Fusarium graminearum and fifty nit mutants were recovered from three JS399-19-resistant mutants of F. graminearum cultured...Twenty-two nitrate nonutilizing (nit) mutants were recovered from five wild-type isolates of Fusarium graminearum and fifty nit mutants were recovered from three JS399-19-resistant mutants of F. graminearum cultured on MMC medium. Some biological properties were compared between nit mutants and their parental isolates. The results showed that there were no significant differences in growth rate, cultural characters or pathogenicity between JS399-19-resistant nit mutants and their parental isolates. But the conidial production and the sexual reproduction ability changed to some extent. There was no cross resistance toward chlorate and JS399-19 in F. graminearum and the resistance could be stable through 20-time subcultures. Therefore, the nit could be used as a genetic marker for studying the genetics of JS399-19 resistance in E graminearum, which was used to study JS399-19 resistance transferability in hyphal fusion. Resistance in JS399-19 could not be transferred by hyphal fusion or could be transferred with low chance between two compatible isolates, which would delay the development of JS399-19 resistance in the field.展开更多
The effect of seed oil of Korean pine (Pinus koraiensis) on the rats' blood-fat and its anti-ageing function was stud-ied for appraising the efficacy of the seed oil of Korean pine. Sixty experimental rats were ra...The effect of seed oil of Korean pine (Pinus koraiensis) on the rats' blood-fat and its anti-ageing function was stud-ied for appraising the efficacy of the seed oil of Korean pine. Sixty experimental rats were randomly divided into 5 groups (half males and half females in each group) as normal control group, high fat diet control group, and three groups (Group 1 Group 2, Group 3) that were fed with feedstuff with the contents of the seed oil of 2.0g/(kgd-1), 4.0g/(kgd-1) and 8.0g/(kgd-1), respec-tively. The indexes such as superoxide dismutase (SOD), glutathione peroxidase (GSH-PX) and anti-oxidation capacity (AOC) were measured by Reagent Kit method. It was found that the seed oil of the Korean pine could reduce the content of triglyc-eride and improve SOD as well as GSH-PX activity in serum. These indexes of the rats in Group 2 fed with Korean pine seed oil of 4.0 g/(kgd-1) reached the significant level and those of rats in Group 3 fed with the seed oil of 8.0 g/(kgd-1) reached the extremely significant level. The results indicated the seed oil of Korean pine had function of regulating the level of blood-fat and anti-ageing.展开更多
Aster souliei Franch, (Compositae) is a. herbaceous plant distributed innorth China. It has been used in folk medicine as antipyretic, detoxicant, expectorant andantitussive. In an effort to find biologically active c...Aster souliei Franch, (Compositae) is a. herbaceous plant distributed innorth China. It has been used in folk medicine as antipyretic, detoxicant, expectorant andantitussive. In an effort to find biologically active components from Chinese medicinal plants ' ,we have examined the aerial parts of this herb, leading to the isolation of a clerodane-typediterpene, 18, 19-dihydroxy-5α, 10β-neo-cleroda-3, 13 (l4)-dien-16, 15-butenolide (1). In thispaper we report the structural elucidation, and the antitumor and antibacterial activities of thiscompound. It was found that 1 possesses moderate cytotoxicity against human leukemia cells (HL-60)and activity against microorganisms.展开更多
In peanuts, a mechanism of resistance to fungal infection is reported on the synthesis of stilbene phytoalexins, which are antibiotic, low molecular weight metabolites. The phytoalexin-associated response of different...In peanuts, a mechanism of resistance to fungal infection is reported on the synthesis of stilbene phytoalexins, which are antibiotic, low molecular weight metabolites. The phytoalexin-associated response of different peanut varieties to the inoculation with A. flavus has not been investigated and might be useful for breed- ing resistant peanut cultivars. In this study, peanut varieties resistant or susceptible to aflatoxin accumulation caused by A. flavus were selected to compare the synthe- sis differences of the four main stilbenes (resveratrol, ε-viniferin, 6-viniferin and pterostilbene) and the activities of their resistant enzymes (PAL, POD, PPO), and explore the relationship between stilbene synthesis and resistance to aflatoxin accu- mulation. The results indicated that the synthesis speed of stilbenes was related to the resistance to aflatoxin accumulation in peanuts seeds. The total content of the four stilbenes reached the highest value of 47.37 μg/g in the resistant cultivars (Qian huasheng 3) after inoculation by A. flavus (54 times of the control) on the 3nd day, while the total content of stilbenes in susceptible cultivars (Huayu 22) was 5.5 μg/g. The content of stilbenes and the activities of their resistant enzymes from the resistant cultivars were both higher than from the susceptible one. The four peanut varieties with relative higher stilbene contents and lower disease index and aflatoxin content were selected by using the stilbene content. Very significant negative corre- lation, with correlation coefficients (r) of -0.789, -0.851 and -0.850, was observed between the stilbene content with disease index, the content of aflatoxin B1 and the total content of aflatoxins, respectively. Therefore, the study suggested that the total content of stilbene compounds might serve as an important chemical index in peanut seeds after inoculation with A. flavus on the 3nd day, during screening and breeding of peanut varieties resistant to aflatoxin accumulation.展开更多
Aim To synthesize 4″-carbamate derivatives of erythromycin and test their antibacterial activities in vitro. Methods New erythromycin antibacterial agents containing 4″-carbamate group were designed and synthesized ...Aim To synthesize 4″-carbamate derivatives of erythromycin and test their antibacterial activities in vitro. Methods New erythromycin antibacterial agents containing 4″-carbamate group were designed and synthesized from azithromycin via protection, aminoformylation, amination and deprotection. Their antibacterial activities against Staphylococcus aureus strains were tested. Results Nine compounds were synthesized. Their structures were confirmed by MS, IR, ~ 1 H NMR and ~ 13 C NMR, and the synthetic conditi...展开更多
Chemical studies on nine Salvia species yielded various polyphenolic acids. Eleven of them were depsides of R (+) β (3,4 dihydroxyphenyl) lactic acid and a caffeic acid derivative or caffeic acid dimer. Except th...Chemical studies on nine Salvia species yielded various polyphenolic acids. Eleven of them were depsides of R (+) β (3,4 dihydroxyphenyl) lactic acid and a caffeic acid derivative or caffeic acid dimer. Except the two known depsides, rosmarinic acid and lithospermic acid, this type of depsides has not been isolated from other plant materials before, so they were named salvianolic acid A, B, C, D, E, H, I, J and isosalvianolic acid C. Salvianolic acid F, G and przewalskinic acid A were new polyphenolic acids. Pharmacological studies of these polyphenolic acids showed potent antioxidant activities. The effects of these components in protecting against brain and heart damage have been studied.展开更多
[Objective] This study aimed to compare the contents of total alkaloids in different solvent extracts from climbing groundsel herb produced in Guizhou Province and their antibacterial activity. [Method] The content of...[Objective] This study aimed to compare the contents of total alkaloids in different solvent extracts from climbing groundsel herb produced in Guizhou Province and their antibacterial activity. [Method] The content of total alkaloids was measured by UV spectrophotometry, and Oxford cups were used to investigate the antibacterial activity of each solvent extract. [Result] There was a good linear correlation between the absorbance measured by the UV spectrophotometer and the content of total al- kaloids within the concentration of 0.011 0-0.054 8 mg/ml at 207 nm, and the re- gression equation was Y=23.654X+0.021, R=0. 999 7 and the average recovery rate was 99.2%. The contents of total alkaloids in 60% ethanol extract, 95% ethanol and water ethanol were 38.71, 52.25 and 60.50 mg/g, respectively. The 60% ethanol ex- tract had strong antibacterial activity against Streptococcus pneumoniae, Staphylo- coccus aureus and Escherichia coil; the water extractive had stronger antibacterial activity against Escherichia colr, 95% ethanol extract had weak antibacterial activity, with no inhibition of Pseudomonas aeruginosa. [Conclusion] This method is accurate, simple, with good repeatability, which can be used for the determination of alkaloids content of the climbing groundsel herb; there is no positive correlation between the content of total alkaloids in different solvent extracts of climbing groundsel herb and their antibacterial activity.展开更多
A series of 2 (E) (4 hydroxy 3 methoxybenzylidene) 5 (N substituted ami nomethyl) cyclopentanones was synthesized and evaluated for the anti inflammatory activity. All of the target compounds were confirmed ...A series of 2 (E) (4 hydroxy 3 methoxybenzylidene) 5 (N substituted ami nomethyl) cyclopentanones was synthesized and evaluated for the anti inflammatory activity. All of the target compounds were confirmed by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several compounds exerted appreciable inhibitory effect on xylene induced ear edema in mice and that alteration of the substituents of anilines had significant influence in anti inflammatory potency.展开更多
Infection is a major potential complication in the clinical treatment of bone injuries. Magnesium (Mg)-based composites are biodegradable and antibacterial biomaterials that have been employed to reduce infection foll...Infection is a major potential complication in the clinical treatment of bone injuries. Magnesium (Mg)-based composites are biodegradable and antibacterial biomaterials that have been employed to reduce infection following surgical implants. The aim of present study was to synthesize and in-vitro characterize Mg-based scaffolds containing silver for bone tissue engineering. Porous Mg-based scaffolds with four silver concentrations (i.e., 0, 0.5 wt.%, 1 wt.%, and 2 wt.%), denoted by Mg?Ca?Mn-Zn-xAg (MCMZ?xAg)(where x is the silver concentration), were fabricated by the space holder technique. The effects of silver concentration on pore architecture, mechanical properties, bioactivity, and zone of bacterial inhibition were investigated in-vitro. X-ray diffractometry (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and fluorescence microscopy were utilized to characterize the obtained scaffolds. In-vitro corrosion test results indicated that the MCMZ scaffolds with lower silver content were more resistant to corrosion than those enriched with higher amounts of silver. Examination of the antibacterial activity showed that the MCMZ?Ag scaffolds exhibited superb potential with respect to suppressing the growth of Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus), in the inhibition zone around the MCMZ?Ag scaffolds, with increasing in the amount of incorporated silver;however, higher amounts of silver increased the cytotoxicity. Taken together, the results of this study demonstrate that the porous 0.5 wt.% Ag-containing scaffolds with interconnected pores, adequate mechanical properties, antibacterial activity, and cell adhesion are promising with respect to the repair and substitution of damaged and diseased bones.展开更多
Application of high-speed centrifugation and high-performance liquid chro- matography to separation and purification obtained a new type of natural antibacteri- al substance from Escherichia co/i cell. Against Staphy/...Application of high-speed centrifugation and high-performance liquid chro- matography to separation and purification obtained a new type of natural antibacteri- al substance from Escherichia co/i cell. Against Staphy/ococcus aureus, Escherichia coli, Pasteurella multocida, Streptococcus, Pseudomonas, solanacearum the minimal inhibitory concentration (MIC) was 2.5, 5, 0.625 iJg/ml, 0.625 and 1.25 g/ml, the minimum bactericidal concentration (MBC) was 5, 5, 1.25, 2.5, 2.5 g/ml, respectively. Composition identification of chemical method and mass spectrometry shows that the antibacterial active substance alkaloids; and the safety evaluation on the model plant Arabidopsis shows that the antibacterial active substance had no inhibitory and adverse effects on the growth and development of plants. The experimental results show that the antibacterial active substance is a broad-spectrum, high efficiency, safe antibacterial natural product, with the prospect of development and utilization of alternative antibiotics.展开更多
Antimicrobial activity of organic and aqueous extracts from fruits, leaves and roots of Tribulus terrestris L., an Iraqi medicinal plant used as urinary anti-infective in folk medicine, was examined against I l specie...Antimicrobial activity of organic and aqueous extracts from fruits, leaves and roots of Tribulus terrestris L., an Iraqi medicinal plant used as urinary anti-infective in folk medicine, was examined against I l species of pathogenic and non-pathogenic microorganisms: Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Corynebacterium diphtheriae, Escherichia coli, Proteus vulgaris, Serratia marcescens, Salmonella typhimurium, Klebsiella pneumoniae, Pseudomonas aeruginosa and Candida albicans using microdilution method in 96 multiwell microtiter plates. All the extracts from the different parts of the plant showed antimicrobial activity against most tested microorganisms. The most active extract against both Gram-negative and Gram-positive bacteria was ethanol extract from the fruits with a minimal inhibitory concentration (MIC) value of 0.15 mg/ml against B. subtilis, B. cereus, P. vulgaris and C. diphtheriae. In addition, the same extract from the same plant part demonstrated the strongest antifungal activity against C. albicans with an MIC value of 0.15 mg/ml.展开更多
Healthy sporophytes of two gametophyte mutants of Laminariajaponica with different heat resistances: kelp 901 (901, with comparatively stronger heat-resistance) and Rongcheng No. I (RC, sensitive to heat stress),...Healthy sporophytes of two gametophyte mutants of Laminariajaponica with different heat resistances: kelp 901 (901, with comparatively stronger heat-resistance) and Rongcheng No. I (RC, sensitive to heat stress), were respectively collected during October to December 2002 from Yantai and Rongcheng Sea Farm in the Shandong Peninsula of China. The contents of some biochemical materials and antioxidant capacity were analyzed under controlled laboratory conditions to identify if there is any relation between the overall antioxidant capacity and the heat-resistance in L. japonica and to understand possible mechanism of heat-resistance. Results show that: (1) the overall antioxidant capacity in healthy sporophyte of 901, such as vitamin E, polyphenol, and ascorbic acid contents and the enzymatic activity of SOD, POD, CAT, Gpx, PPO, and PAL, were not always higher than that of RC under controlled laboratory conditions, and no significance (P〉0.05) was shown in total antioxidant capacity (T-AOC) in 901 and RC. Result suggested that the difference in antioxidant capacity was not a decisive factor for different heat-resistances in L. japonica; (2) the simultaneous assay on isozymes was carried out using vertical polyacrylamide gel electrophoresis (PAGE). Considerable differences in peroxide (PRX), malate dehydrogenase (MDH), malic enzyme (ME), polyphenol oxidase (PPO) and glutamate dehydrogenase (GDH) were obtained in 901 and RC from either the band number, relative mobility (Rf), or staining intensity, and ME could be used as an indicator to distinguish healthy sporophyte of 901 and RC under controlled laboratory conditions.展开更多
[Objective] The aim was to study effect of Chaetomium globosum ND35 on plant growth and preliminary study of its biocontrol efficacy, and provide basis for popularization and application of this strain.[ Method] With ...[Objective] The aim was to study effect of Chaetomium globosum ND35 on plant growth and preliminary study of its biocontrol efficacy, and provide basis for popularization and application of this strain.[ Method] With endophytic fungus C. globosum ND35 as a tested strain, effect of C. globosumND35 on plant growth and its biocontrol on five plant diseases were investigated in the greenhouse and field,[Result]The results showed that ND35 promoted growth of lateral root and diameter of breast height of poplar. ND35 can induce poplar to resist Poplar Valsa Canker caused by Valsa sordida and Poplar Rust caused by Melampsora puplicola. ND35 was also able to induce tomato and bean to resist Botrytis cinera. Biocontrol of Bean Stem Rot Rhizoctonia by ND35 was effective as well. [Conclusion] Induced systemic resistance by endophytic C. globosum ND35 plays an important role in biocontrol of plant diseases.展开更多
Trichomoniasis is the most common, sexually transmitted infection. It is caused by the flagellated protozoan parasite Trichomonas vaginalis. Symptoms include vaginitis and infections have been associated with preterm ...Trichomoniasis is the most common, sexually transmitted infection. It is caused by the flagellated protozoan parasite Trichomonas vaginalis. Symptoms include vaginitis and infections have been associated with preterm delivery, low birth weight and increased infant mortality, as well as predisposing to HIV/AIDS and cervical cancer. Trichomoniasis has the highest prevalence and incidence of any sexually transmitted infection. The 5-nitroimidazole drugs, of which metronidazole is the most prescribed, are the only approved,effective drugs to treat trichomoniasis. Resistance against metronidazole is frequently reported and crossresistance among the family of 5-nitroimidazole drugs is common, leaving no alternative for treatment, with some cases remaining unresolved. The mechanism of metronidazole resistance in T. vaginalis from treatment failures is not well understood, unlike resistance which is developed in the laboratory under increasing metronidazole pressure. In the latter situation, hydrogenosomal function which is involved in activation of the prodrug, metronidazole, is down-regulated. Reversion to sensitivity is incomplete after removal of drug pressure in the highly resistant parasites while clinically resistant strains, so far analysed, maintain their resistance levels in the absence of drug pressure. Although anaerobic resistance has been regarded as a laboratory induced phenomenon, it clearly has been demonstrated in clinical isolates. Pursuit of both approaches will allow dissection of the underlying mechanisms. Many alternative drugs and treatments have been tested in vivo in cases of refractory trichomoniasis, as well as in vitro with some successes including the broad spectrum anti-parasitic drug nitazoxanide. Drug resistance incidence in T. vaginalis appears to be on the increase and improved surveillance of treatment failures is urged.展开更多
文摘Water soluble skin secretions of six common Chinese amphibians were studied for their biological and enzymatic activities.The skin secretions of Tylototriton verrucosus,Bombina maxima ,and Bufo andrewsi were found toxic to mice with the intraperitoneal LD 50 of 11 5?mg/kg,18 8?mg/kg,and 264?mg/kg,respectively.No acute lethal toxicities were observed for the skin secretions of Rana nigromaculata,Rana guentheri and Rana limnocharis in a dose up to 500?mg/kg.The lethal toxicities of the skin secretions of T verrucosus and B maxima to mice are in the same grade as those of Viperidae snake venoms.The toxic components in T verrucosus and B maxima skin secretions are the proteins with molecular weights ranging from 3 to 60?kDa.All the skin secretions had both proteolytic activity and trypsin inhibitory activity.The skin secretions from T verrucosus , B maxima and B andrewsi also displayed wide spectrum antimicrobial activity.On the other hand,the skin secretions from B andrewsi and B maxima showed cytotoxicity on human cancer cells.All the six samples had not significant effects on mammalian blood coagulation system.Phospholipase A 2 activity was only found in the skin secretions of T verrucosus .None of these skin secretions showed acetylcholine esterase activity.
基金This work was supported by the State "973" Programs from the Ministry of Science and Technology of China (No. 2006CB101900)Technology and the Project (No. 20050307028)+3 种基金from the Ministry of Education of China, the National Natural Science Foundation of China (No. 30671048 & No. 30671384)Jiangsu Provincial Program for Tackling Key Problems of Science and Technology (No. BG2006328)the Key Technology R & D program from the Ministry of Science and Technology of China (No. 2006BAE01A04-08)the state "863" programs from the Ministry of Science and Technology of China (No. 2006AA10A211).
文摘Twenty-two nitrate nonutilizing (nit) mutants were recovered from five wild-type isolates of Fusarium graminearum and fifty nit mutants were recovered from three JS399-19-resistant mutants of F. graminearum cultured on MMC medium. Some biological properties were compared between nit mutants and their parental isolates. The results showed that there were no significant differences in growth rate, cultural characters or pathogenicity between JS399-19-resistant nit mutants and their parental isolates. But the conidial production and the sexual reproduction ability changed to some extent. There was no cross resistance toward chlorate and JS399-19 in F. graminearum and the resistance could be stable through 20-time subcultures. Therefore, the nit could be used as a genetic marker for studying the genetics of JS399-19 resistance in E graminearum, which was used to study JS399-19 resistance transferability in hyphal fusion. Resistance in JS399-19 could not be transferred by hyphal fusion or could be transferred with low chance between two compatible isolates, which would delay the development of JS399-19 resistance in the field.
文摘The effect of seed oil of Korean pine (Pinus koraiensis) on the rats' blood-fat and its anti-ageing function was stud-ied for appraising the efficacy of the seed oil of Korean pine. Sixty experimental rats were randomly divided into 5 groups (half males and half females in each group) as normal control group, high fat diet control group, and three groups (Group 1 Group 2, Group 3) that were fed with feedstuff with the contents of the seed oil of 2.0g/(kgd-1), 4.0g/(kgd-1) and 8.0g/(kgd-1), respec-tively. The indexes such as superoxide dismutase (SOD), glutathione peroxidase (GSH-PX) and anti-oxidation capacity (AOC) were measured by Reagent Kit method. It was found that the seed oil of the Korean pine could reduce the content of triglyc-eride and improve SOD as well as GSH-PX activity in serum. These indexes of the rats in Group 2 fed with Korean pine seed oil of 4.0 g/(kgd-1) reached the significant level and those of rats in Group 3 fed with the seed oil of 8.0 g/(kgd-1) reached the extremely significant level. The results indicated the seed oil of Korean pine had function of regulating the level of blood-fat and anti-ageing.
文摘Aster souliei Franch, (Compositae) is a. herbaceous plant distributed innorth China. It has been used in folk medicine as antipyretic, detoxicant, expectorant andantitussive. In an effort to find biologically active components from Chinese medicinal plants ' ,we have examined the aerial parts of this herb, leading to the isolation of a clerodane-typediterpene, 18, 19-dihydroxy-5α, 10β-neo-cleroda-3, 13 (l4)-dien-16, 15-butenolide (1). In thispaper we report the structural elucidation, and the antitumor and antibacterial activities of thiscompound. It was found that 1 possesses moderate cytotoxicity against human leukemia cells (HL-60)and activity against microorganisms.
基金Supported by Natural Science Foundation of Hainan Province(809034)National Nonprofit Institute Research Grant of CATAS-TCGRI(1630032012025)~~
文摘In peanuts, a mechanism of resistance to fungal infection is reported on the synthesis of stilbene phytoalexins, which are antibiotic, low molecular weight metabolites. The phytoalexin-associated response of different peanut varieties to the inoculation with A. flavus has not been investigated and might be useful for breed- ing resistant peanut cultivars. In this study, peanut varieties resistant or susceptible to aflatoxin accumulation caused by A. flavus were selected to compare the synthe- sis differences of the four main stilbenes (resveratrol, ε-viniferin, 6-viniferin and pterostilbene) and the activities of their resistant enzymes (PAL, POD, PPO), and explore the relationship between stilbene synthesis and resistance to aflatoxin accu- mulation. The results indicated that the synthesis speed of stilbenes was related to the resistance to aflatoxin accumulation in peanuts seeds. The total content of the four stilbenes reached the highest value of 47.37 μg/g in the resistant cultivars (Qian huasheng 3) after inoculation by A. flavus (54 times of the control) on the 3nd day, while the total content of stilbenes in susceptible cultivars (Huayu 22) was 5.5 μg/g. The content of stilbenes and the activities of their resistant enzymes from the resistant cultivars were both higher than from the susceptible one. The four peanut varieties with relative higher stilbene contents and lower disease index and aflatoxin content were selected by using the stilbene content. Very significant negative corre- lation, with correlation coefficients (r) of -0.789, -0.851 and -0.850, was observed between the stilbene content with disease index, the content of aflatoxin B1 and the total content of aflatoxins, respectively. Therefore, the study suggested that the total content of stilbene compounds might serve as an important chemical index in peanut seeds after inoculation with A. flavus on the 3nd day, during screening and breeding of peanut varieties resistant to aflatoxin accumulation.
基金The Project Sponsored by the Foundation for Doctors, Jinan University, No.B0511
文摘Aim To synthesize 4″-carbamate derivatives of erythromycin and test their antibacterial activities in vitro. Methods New erythromycin antibacterial agents containing 4″-carbamate group were designed and synthesized from azithromycin via protection, aminoformylation, amination and deprotection. Their antibacterial activities against Staphylococcus aureus strains were tested. Results Nine compounds were synthesized. Their structures were confirmed by MS, IR, ~ 1 H NMR and ~ 13 C NMR, and the synthetic conditi...
文摘Chemical studies on nine Salvia species yielded various polyphenolic acids. Eleven of them were depsides of R (+) β (3,4 dihydroxyphenyl) lactic acid and a caffeic acid derivative or caffeic acid dimer. Except the two known depsides, rosmarinic acid and lithospermic acid, this type of depsides has not been isolated from other plant materials before, so they were named salvianolic acid A, B, C, D, E, H, I, J and isosalvianolic acid C. Salvianolic acid F, G and przewalskinic acid A were new polyphenolic acids. Pharmacological studies of these polyphenolic acids showed potent antioxidant activities. The effects of these components in protecting against brain and heart damage have been studied.
基金Supported by the Clinical Scientific Research Capacity Construction Program for Country-level Hospitals of Department of Health,Guizhou Province(gzwxky2011-1-022)~~
文摘[Objective] This study aimed to compare the contents of total alkaloids in different solvent extracts from climbing groundsel herb produced in Guizhou Province and their antibacterial activity. [Method] The content of total alkaloids was measured by UV spectrophotometry, and Oxford cups were used to investigate the antibacterial activity of each solvent extract. [Result] There was a good linear correlation between the absorbance measured by the UV spectrophotometer and the content of total al- kaloids within the concentration of 0.011 0-0.054 8 mg/ml at 207 nm, and the re- gression equation was Y=23.654X+0.021, R=0. 999 7 and the average recovery rate was 99.2%. The contents of total alkaloids in 60% ethanol extract, 95% ethanol and water ethanol were 38.71, 52.25 and 60.50 mg/g, respectively. The 60% ethanol ex- tract had strong antibacterial activity against Streptococcus pneumoniae, Staphylo- coccus aureus and Escherichia coil; the water extractive had stronger antibacterial activity against Escherichia colr, 95% ethanol extract had weak antibacterial activity, with no inhibition of Pseudomonas aeruginosa. [Conclusion] This method is accurate, simple, with good repeatability, which can be used for the determination of alkaloids content of the climbing groundsel herb; there is no positive correlation between the content of total alkaloids in different solvent extracts of climbing groundsel herb and their antibacterial activity.
文摘A series of 2 (E) (4 hydroxy 3 methoxybenzylidene) 5 (N substituted ami nomethyl) cyclopentanones was synthesized and evaluated for the anti inflammatory activity. All of the target compounds were confirmed by spectral analysis and elemental analysis. Preliminary pharmacological tests showed that several compounds exerted appreciable inhibitory effect on xylene induced ear edema in mice and that alteration of the substituents of anilines had significant influence in anti inflammatory potency.
基金partial financial support to this research from the Saskatchewan Health Research Foundation (SHRF)
文摘Infection is a major potential complication in the clinical treatment of bone injuries. Magnesium (Mg)-based composites are biodegradable and antibacterial biomaterials that have been employed to reduce infection following surgical implants. The aim of present study was to synthesize and in-vitro characterize Mg-based scaffolds containing silver for bone tissue engineering. Porous Mg-based scaffolds with four silver concentrations (i.e., 0, 0.5 wt.%, 1 wt.%, and 2 wt.%), denoted by Mg?Ca?Mn-Zn-xAg (MCMZ?xAg)(where x is the silver concentration), were fabricated by the space holder technique. The effects of silver concentration on pore architecture, mechanical properties, bioactivity, and zone of bacterial inhibition were investigated in-vitro. X-ray diffractometry (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and fluorescence microscopy were utilized to characterize the obtained scaffolds. In-vitro corrosion test results indicated that the MCMZ scaffolds with lower silver content were more resistant to corrosion than those enriched with higher amounts of silver. Examination of the antibacterial activity showed that the MCMZ?Ag scaffolds exhibited superb potential with respect to suppressing the growth of Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus), in the inhibition zone around the MCMZ?Ag scaffolds, with increasing in the amount of incorporated silver;however, higher amounts of silver increased the cytotoxicity. Taken together, the results of this study demonstrate that the porous 0.5 wt.% Ag-containing scaffolds with interconnected pores, adequate mechanical properties, antibacterial activity, and cell adhesion are promising with respect to the repair and substitution of damaged and diseased bones.
基金Supported by Guangdong Scientific and Technological Bureau(2012B020401012)~~
文摘Application of high-speed centrifugation and high-performance liquid chro- matography to separation and purification obtained a new type of natural antibacteri- al substance from Escherichia co/i cell. Against Staphy/ococcus aureus, Escherichia coli, Pasteurella multocida, Streptococcus, Pseudomonas, solanacearum the minimal inhibitory concentration (MIC) was 2.5, 5, 0.625 iJg/ml, 0.625 and 1.25 g/ml, the minimum bactericidal concentration (MBC) was 5, 5, 1.25, 2.5, 2.5 g/ml, respectively. Composition identification of chemical method and mass spectrometry shows that the antibacterial active substance alkaloids; and the safety evaluation on the model plant Arabidopsis shows that the antibacterial active substance had no inhibitory and adverse effects on the growth and development of plants. The experimental results show that the antibacterial active substance is a broad-spectrum, high efficiency, safe antibacterial natural product, with the prospect of development and utilization of alternative antibiotics.
文摘Antimicrobial activity of organic and aqueous extracts from fruits, leaves and roots of Tribulus terrestris L., an Iraqi medicinal plant used as urinary anti-infective in folk medicine, was examined against I l species of pathogenic and non-pathogenic microorganisms: Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Corynebacterium diphtheriae, Escherichia coli, Proteus vulgaris, Serratia marcescens, Salmonella typhimurium, Klebsiella pneumoniae, Pseudomonas aeruginosa and Candida albicans using microdilution method in 96 multiwell microtiter plates. All the extracts from the different parts of the plant showed antimicrobial activity against most tested microorganisms. The most active extract against both Gram-negative and Gram-positive bacteria was ethanol extract from the fruits with a minimal inhibitory concentration (MIC) value of 0.15 mg/ml against B. subtilis, B. cereus, P. vulgaris and C. diphtheriae. In addition, the same extract from the same plant part demonstrated the strongest antifungal activity against C. albicans with an MIC value of 0.15 mg/ml.
基金Supported by the National Hi-Tech Research Program (863 Program, No. 2004AA639770)the National Natural Science Foundation of China (No.30270258)Program for New Century Excellent Talents in University (NCET-05-0597).
文摘Healthy sporophytes of two gametophyte mutants of Laminariajaponica with different heat resistances: kelp 901 (901, with comparatively stronger heat-resistance) and Rongcheng No. I (RC, sensitive to heat stress), were respectively collected during October to December 2002 from Yantai and Rongcheng Sea Farm in the Shandong Peninsula of China. The contents of some biochemical materials and antioxidant capacity were analyzed under controlled laboratory conditions to identify if there is any relation between the overall antioxidant capacity and the heat-resistance in L. japonica and to understand possible mechanism of heat-resistance. Results show that: (1) the overall antioxidant capacity in healthy sporophyte of 901, such as vitamin E, polyphenol, and ascorbic acid contents and the enzymatic activity of SOD, POD, CAT, Gpx, PPO, and PAL, were not always higher than that of RC under controlled laboratory conditions, and no significance (P〉0.05) was shown in total antioxidant capacity (T-AOC) in 901 and RC. Result suggested that the difference in antioxidant capacity was not a decisive factor for different heat-resistances in L. japonica; (2) the simultaneous assay on isozymes was carried out using vertical polyacrylamide gel electrophoresis (PAGE). Considerable differences in peroxide (PRX), malate dehydrogenase (MDH), malic enzyme (ME), polyphenol oxidase (PPO) and glutamate dehydrogenase (GDH) were obtained in 901 and RC from either the band number, relative mobility (Rf), or staining intensity, and ME could be used as an indicator to distinguish healthy sporophyte of 901 and RC under controlled laboratory conditions.
基金Supported by National Natural Science Foundation of China(30872024,30571498)Students Research Training (SRT) of Shandong Agricultural University (0802024)~~
文摘[Objective] The aim was to study effect of Chaetomium globosum ND35 on plant growth and preliminary study of its biocontrol efficacy, and provide basis for popularization and application of this strain.[ Method] With endophytic fungus C. globosum ND35 as a tested strain, effect of C. globosumND35 on plant growth and its biocontrol on five plant diseases were investigated in the greenhouse and field,[Result]The results showed that ND35 promoted growth of lateral root and diameter of breast height of poplar. ND35 can induce poplar to resist Poplar Valsa Canker caused by Valsa sordida and Poplar Rust caused by Melampsora puplicola. ND35 was also able to induce tomato and bean to resist Botrytis cinera. Biocontrol of Bean Stem Rot Rhizoctonia by ND35 was effective as well. [Conclusion] Induced systemic resistance by endophytic C. globosum ND35 plays an important role in biocontrol of plant diseases.
文摘Trichomoniasis is the most common, sexually transmitted infection. It is caused by the flagellated protozoan parasite Trichomonas vaginalis. Symptoms include vaginitis and infections have been associated with preterm delivery, low birth weight and increased infant mortality, as well as predisposing to HIV/AIDS and cervical cancer. Trichomoniasis has the highest prevalence and incidence of any sexually transmitted infection. The 5-nitroimidazole drugs, of which metronidazole is the most prescribed, are the only approved,effective drugs to treat trichomoniasis. Resistance against metronidazole is frequently reported and crossresistance among the family of 5-nitroimidazole drugs is common, leaving no alternative for treatment, with some cases remaining unresolved. The mechanism of metronidazole resistance in T. vaginalis from treatment failures is not well understood, unlike resistance which is developed in the laboratory under increasing metronidazole pressure. In the latter situation, hydrogenosomal function which is involved in activation of the prodrug, metronidazole, is down-regulated. Reversion to sensitivity is incomplete after removal of drug pressure in the highly resistant parasites while clinically resistant strains, so far analysed, maintain their resistance levels in the absence of drug pressure. Although anaerobic resistance has been regarded as a laboratory induced phenomenon, it clearly has been demonstrated in clinical isolates. Pursuit of both approaches will allow dissection of the underlying mechanisms. Many alternative drugs and treatments have been tested in vivo in cases of refractory trichomoniasis, as well as in vitro with some successes including the broad spectrum anti-parasitic drug nitazoxanide. Drug resistance incidence in T. vaginalis appears to be on the increase and improved surveillance of treatment failures is urged.