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1.
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi ; 34(5): 469-474, 2022 Oct 21.
Article in Chinese | MEDLINE | ID: mdl-36464260

ABSTRACT

OBJECTIVE: To investigate the changing trends in the prevalence of schistosomiasis in Anhui Province from 2004 to 2020, so as to provide the evidence for formulating the schistosomiasis elimination strategy in the province. METHODS: The epidemiological data of schistosomiasis in Anhui Province from 2004 to 2020 were collected, and the trends in the endemic status of schistosomiasis were analyzed using a Joinpoint regression model. The trends in the prevalence of Schistosoma japonicum infections in humans, bovines and Oncomelania hupensis were measured in Anhui Province from 2004 to 2020 using average annual percent change (AAPC), and the correlations among the changing trends in the prevalence of S. japonicum infections in humans, bovines and O. hupensis snail status were evaluated using Pearson correlation analysis. RESULTS: The prevalence of S.japonicum human infections continued to decline in Anhui Province from 2004 to 2020, with an annual mean decline of 14.8% [AAPC = -14.8%, 95% confidential interval (CI): (-18.9%, -10.5%), P < 0.01]. The prevalence of S. japonicum infections continued to decline in bovines in Anhui Province from 2004 to 2015 [AAPC = -31.3%, 95%CI: (-35.1%, -27.2%), P < 0.01], and was 0 for 5 successive years from 2016 to 2020. During the period from 2004 to 2020, there was an annual mean decline of 0.7% in areas of snail habitats [AAPC = -0.7%, 95%CI: (-1.2%, 0.3%), P < 0.05] and an annual mean decline of 9.2% in the density of living snails [AAPC = -9.2%, 95%CI: (-18.3%, 1.0%), P = 0.08] in Anhui Province from 2004 to 2020, and an annual mean decline of 35.6% was found in the density of S. japonicum-infected snails [AAPC = -35.6%, 95%CI: (-49.2%, -18.3%), P < 0.01] from 2004 to 2012, with no infected snails detected in Anhui Province from 2013 to 2020. There were significant correlations in the prevalence of S. japonicum infections between humans and bovines (r = 0.959, P < 0.01), between the prevalence of S. japonicum human infections and the density of S. japonicum-infected snails (r = 0.823, P < 0.01) and between the prevalence of S. japonicum infections in bovines and the density of S. japonicum-infected snails (r = 0.902, P < 0.01). CONCLUSIONS: The prevalence of S. japonicum infections appeared a decline in humans, bovines and O. hupensis in Anhui Province from 2004 to 2020, and significant correlations were found among the changing trends in the prevalence of S. japonicum human infections, the prevalence of S. japonicum bovine infections and the density of S. japonicum-infected O. hupensis snails. Because of a minor decline in the area of snail habitats and widespread distribution of O. hupensis, however, there is still a risk of schistosomiasis transmission, and precision control for schistosomiasis remains to be reinforced in Anhui Province.


Subject(s)
Gastropoda , Schistosomiasis japonica , Schistosomiasis , Humans , Animals , Cattle , Prevalence , Schistosomiasis/epidemiology , Schistosomiasis/veterinary , Schistosomiasis japonica/epidemiology , Schistosomiasis japonica/veterinary , Regression Analysis
2.
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi ; 34(3): 252-258, 2022 Jun 24.
Article in Chinese | MEDLINE | ID: mdl-35896488

ABSTRACT

OBJECTIVE: To analyze the spatial-temporal distribution characteristics of Oncomelania hupensis snails in Anhui Province from 2011 to 2020, to provide insights into precision control of O. hupensis snails in Anhui Province. METHODS: O. hupensis snail distribution data were collected in Anhui Province from 2011 to 2020 and descriptively analyzed, including actual area of snail habitats, area of emerging snail habitats and area of Schistosoma japonicum-infected snails. The actual area of snail habitats and area of emerging snail habitats were subjected to spatial autocorrelation analysis, hotspot analysis, standard deviation ellipse analysis and space-time scanning analysis, and the clusters of snail distribution and settings at high risk of snail spread were identified in Anhui Province from 2011 to 2020. RESULTS: The actual area of snail habitats gradually decreased in Anhui Province from 2011 to 2020. The actual area of snail habitats were 26 238.85 hm2 in Anhui Province in 2020, which were mainly distributed in marshland and lake regions. There was a large fluctuation in the area of emerging snail habitats in Anhui Province during the period from 2011 to 2020, with the largest area seen in 2016 (1 287.65 hm2), and 1.96 hm2 emerging infected snail habitats were detected in Guichi District, Chizhou City in 2020. Spatial autocorrelation and hotspot analyses showed spatial clusters in the distribution of actual areas of snail habitats in Anhui Province from 2011 to 2020 (Z = 3.00 to 3.43, all P values < 0.01), and the hotspots were mainly concentrated in the marshland and lake regions and distributed along the south side of the Yangtze River, while the cold spots were mainly concentrated in the mountainous regions of southern Anhui Province. There were no overall spatial clusters in the distribution of areas of emerging snail habitats (Z = -2.20 to 1.71, all P values > 0.05), and a scattered distribution was found in local regions. Standard deviation ellipse analysis showed relatively stable distributions of the actual areas of snail habitats in Anhui Province from 2011 to 2020, which was consistent with the flow direction of the Yangtze River, and the focus of the distribution of areas of emerging snail habitats shifted from the lower reaches to upper reaches of Anhui section of the Yangtze River. Space-time scanning analysis identified two high-value clusters in the distribution of actual areas of snail habitats in lower and middle reaches of Anhui section of the Yangtze River from 2011 to 2020, and two high-value clusters in the distribution of areas of emerging snail habitats were identified in mountainous and hilly regions. CONCLUSIONS: There were spatial clusters in the distribution of O. hupensis snails in Anhui Province from 2011 to 2020, which appeared a tendency of aggregation towards the south side and upper reaches of the Yangtze River; however, the spread of O. hupensis snails could not be neglected in mountainous and hilly regions. Monitoring of emerging snail habitats should be reinforced in mountainous and hilly regions and along the Yangtze River basin.


Subject(s)
Gastropoda , Schistosoma japonicum , Animals , China/epidemiology , Ecosystem , Lakes , Rivers
3.
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi ; 34(6): 622-625, 2022 Aug 30.
Article in Chinese | MEDLINE | ID: mdl-36642903

ABSTRACT

OBJECTIVE: To investigate the prevalence of Schistosoma japonicum infection in wild mice in Shitai County, Anhui Province, so as to provide insights into precise control of the source of S. japonicum infections. METHODS: Wild mice were captured using the trapping method for three successive nights at snail-infested settings from Jitan Village of Jitan Township, and Shiquan Village and Xibai Village of Dingxiang Township, Shitai County, Anhui Province in June and October, 2018. All trapped wild mice were sacrificed and liver and mesenteric vein specimens were collected for detection of S. japonicum eggs using microscopy, while the fecal samples in mouse intestines were collected for identification of S. japonicum infections using Kato-Katz technique. In addition, the population density of trapped wild mice was estimated and the prevalence of S. japonicum infection was calculated in trapped wild mice. RESULTS: A total of 376 wild mice were trapped from three villages in Shitai County. The population density of trapped wild mice was 9.1% (376/4 124), and the prevalence of S. japonicum infection was 24.2% (91/376) in trapped wild mice. The highest prevalence of S. japonicum infection was detected in Shiquan Village of Dingxiang Township (30.1%), and the lowest prevalence was seen in Xibai Village of Dingxiang Township; however, there was no significant difference in the prevalence of S. japonicum infection in trapped wild mice among three villages (χ2= 4.111, P > 0.05). In addition, there was no significant difference in the prevalence of S. japonicum infection in wild mice captured between on June (26.8%, 34/127) and October (22.9%, 57/249) (χ2 = 0.690, P = 0.406). The trapped wild mice included 6 species, including Rattus norvegicus, Niviventer niviventer, R. losea, Apodemus agrarius, Mus musculus and N. coning, and the two highest prevalence of S. japonicum infection was detected in R. losea (34.9%, 22/63) and R. norvegicus (31.2%, 44/141). CONCLUSIONS: The prevalence of S. japonicum infections is high in wild mice in Shitai County, and there is a natural focus of schistosomiasis transmission in Shitai County.


Subject(s)
Schistosoma japonicum , Schistosomiasis japonica , Schistosomiasis , Animals , Mice , Rats , Schistosomiasis japonica/epidemiology , Schistosomiasis japonica/veterinary , Prevalence , Schistosomiasis/prevention & control , Liver , Snails , China/epidemiology
4.
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi ; 32(3): 301-303, 2020 Apr 29.
Article in Chinese | MEDLINE | ID: mdl-32468795

ABSTRACT

OBJECTIVE: To analyze the endemic situation of schistosomiasis in national surveillance sites of Anhui Province from 2015 to 2018, so as to provide scientific evidence for schistosomiasis control and prevention in Anhui Province. METHODS: According to the National Schistosomiasis Surveillance Programme (2014 version), a total of 51 national schistosomiasis surveillance sites were assigned in Anhui Province in 2015, and Schistosoma japonicum infections in humans and livestock and snail distribution were monitored from 2015 to 2018. RESULTS: A total of 89 638 local residents and 42 609 mobile populations received serological screening of schistosomiasis in 51 national surveillance sites of Anhui Province from 2015 to 2018, and the sero-prevalence of S. japonicum infections was 1.41% to 3.69% in local residents and 0.84% to 2.13% in mobile populations, respectively. There were 5 egg-positive local residents and 1 egg-positive mobile populations detected in 2015, with occupations of farmers and fishermen. There were 6 405 livestock detected for S. japonicum infections, and no egg-positives were identified. Among an area of 12 661 hm2 surveyed in the national schistosomiasis surveillance sites of Anhui Province from 2015 to 2018, the areas of snail habitats were 2 461.27 to 2 628.96 hm2, andthemeandensityoflivingsnailswas 0.3757 to 0.4330 snails/0.1 m2, with no S. japonicum infections identified in snails. CONCLUSIONS: The endemic situation of schistosomiasis is at a low level in Anhui Province; however, the risk of schistosomiasis transmission remains in local regions of the province. The construction of the surveillance-responsesystemshouldbereinforcedtoconsolidatetheachievementsofschistosomiasis control in Anhui Province.


Subject(s)
Schistosomiasis , Animal Distribution , Animals , China/epidemiology , Ecosystem , Endemic Diseases/statistics & numerical data , Humans , Livestock/parasitology , Population Surveillance , Prevalence , Schistosomiasis/epidemiology , Schistosomiasis/prevention & control , Snails/parasitology , Snails/physiology
5.
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi ; 32(2): 140-147, 2020 Mar 26.
Article in Chinese | MEDLINE | ID: mdl-32458602

ABSTRACT

OBJECTIVE: To investigate the spatiotemporal distribution of Oncomelania hupensis snails and infected snails in the endemic areas of schistosomiasis in Anhui Province. METHODS: Based on the snail survey data in Anhui Province in 2016, the distribution of snails and infected snails were analyzed, and the spatial distribution of snails and spatial cluster patterns of infected snails were investigated in snail habitats in Anhui Province from 1950 to 2016. RESULTS: A total of 22 757 snail habitats and 5 004 infected snail habitats were identified in Anhui Province from 1950 to 2016, which appeared single-peak and double-peak patterns, with an inflection point seen in 1970. There were 141 000 hm2 historically accumulative snail habitats, 88.08% of which were firstly identified from 1950 to 1979, and totally 114 500 hm2 snail habitats were eradicated, 77.17% of which were eradicated from 1970 to 1999. There were 4 830 snail habitats identified until 2016, in which 1 051 were once detected with infected snails. In addition, 78.12% of current snail habitats had been present for over 40 years, and infected snails had been eliminated in 65.75% of the infected snail habitats within 10 years. There was a spatial autocorrelation of the living snail density in current snail habitats in Anhui Province (Moran's I = 0.196, Z = 139.63, P < 0.001), and local hotspot analysis showed spatial clusters of living snails density in snail habitats, with high-value clusters in south of the Yangtze River and low-value clusters in north of the Yangtze River. The 21 high-value clusters of living snail density with statistical significance were distributed along the Yangtze River basin and its branches. Spatiotemporal scan analysis revealed spatiotemporal clusters of infected snails in 4 current snail habitats. CONCLUSIONS: The current snail habitats have been present for a long period of time, and snails are difficult to be eliminated by chemical treatment alone, which requires the combination of environment improvements. There are spatial clusters of living snail density in current snail habitats in Anhui Province. The epidemic factors and risk of human and animal infections still remain in some clusters of historical infected snail habitats revealed by spatiotemporal scan analysis, which should be consid- ered as the key target areas for snail control in Anhui Province.


Subject(s)
Ecosystem , Gastropoda , Animals , China/epidemiology , Gastropoda/physiology , Humans , Rivers , Schistosomiasis/epidemiology , Schistosomiasis/parasitology , Spatio-Temporal Analysis
6.
Article in Chinese | MEDLINE | ID: mdl-32306680

ABSTRACT

Objective: To investigate the CT features of lung injury induced by paraquat poisoning and its relationship with prognosis, and to provide reference for the judgment of the condition and prognosis of paraquat poisoning. Methods: 146 cases of paraquat poisoning patients were treated in the Third People's Hospital of Xuzhou City from January 2013 to April 2016. The cases were divided into mild group, moderate-severe group and fulminant group according to the concentration of paraquat in urine. The clinical data and CT imaging findings were analyzed and reconstructed in three-dimensional reconstruction. The extent of the lesion was observed and the relationship between CT and prognosis was explored. Results: Paraquat lung injury has many manifestations on CT images, and it's performance can be intersecting at the same time. Early lesions lighter cases, late CT imaging lesions can be completely absorbed or residual fibrosis, the prognosis was good; the early lesion was pulmonary consolidation, pleural effusion cases, the late CT image was usually pleural thickening and bronchiectasis, the prognosis was relatively good; early lesions were large patches of ground glass opacity cases, finally, pulmonary fibrosis was common, the mortality rate of 56.57%. There were significant differences in the extent of lung injury between different groups (P<0.001) , and the difference in mortality was statistically significant when the lung injury was different (P<0.001) . Multivariate stepwise Logistic regression analysis showed that ground-glass opacity (OR value=2.013) , interstitial lung fibrosis (OR=3.779) and mediastinal emphysema (OR=33.118) were risk factors for death of lung injury caused by paraquat poisoning (P<0.05) . Conclusion: There were many manifestations on CT images of paraquat lung injury, and the manifestations of paraquat lung injury can be intersecting at the same time. The pulmonary manifestations and outcomes of different paraquat types were different. The CT manifestations of lung injury in paraquat poisoning were mainly exudative changes at early stage, and can be gradually absorbed or evolved into interstitial changes at later stage. The cumulative damage range can be used as a reference for evaluating the prognosis. Ground-glass opacity, interstitial pulmonary fibrosis and mediastinal emphysema are the risk factors for death of lung injury caused by paraquat poisoning.


Subject(s)
Acute Lung Injury/diagnostic imaging , Paraquat/poisoning , Acute Lung Injury/chemically induced , Humans , Lung/diagnostic imaging , Lung/pathology , Prognosis , Tomography, X-Ray Computed
7.
Zhongguo Xue Xi Chong Bing Fang Zhi Za Zhi ; 31(6): 635-637, 2019 Oct 23.
Article in Chinese | MEDLINE | ID: mdl-32064808

ABSTRACT

OBJECTIVE: To analyze the endemic situation of schistosomiasis in Wuhu City from 2009 to 2018, so as to provide evidence for adjusting and developing the control strategy. METHODS: The data regarding the endemic situation were retrospectively collected and analyzed in Wuhu City from 2009 to 2018. RESULTS: The prevalence of human Schistosoma japonicum infections reduced from 0.450% in 2009 to 0.035% in 2018 in Wuhu City, and a reduction rate of 92.22% (χ2 = 1 6128.307, P < 0.01), and the prevalence of S. japonicum infections decreased from 0.483% in 2009 to 0 in 2018 (χ2 = 27.570, P < 0.01) in livestock. The area of snail habitats increased from 1 501.07 hm2 in 2009 to 4 408.62 hm2 in 2018, with an increase of 193.70%. No infected snails were found in Wuhu City since 2012, and no egg positives were detected in humans and livestock since 2016. CONCLUSIONS: Currently, the endemic situation of schistosomiasis is at a low level in Wuhu City; however, there are still factors affecting schistosomiasis transmission. In the future, the integrated strategy with emphasis on the control of infectious source and the surveillance-response system should be intensified to consolidate the achievements of schistosomiasis control.


Subject(s)
Schistosomiasis japonica , Animals , China/epidemiology , Humans , Livestock , Retrospective Studies , Schistosoma/physiology , Schistosomiasis japonica/epidemiology , Schistosomiasis japonica/prevention & control , Schistosomiasis japonica/transmission
8.
Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi ; 34(11): 839-840, 2016 Nov 20.
Article in Chinese | MEDLINE | ID: mdl-28043273

ABSTRACT

Objective: To observe the effect of early intervention and intermittent application of bi level positive air-way pressure ventilation (BiPAP) in patients with pneumoconiosis combined with chronic respiratory failure. Methods: Will meet the diagnostic criteria of pneumoconiosis in GBZ70-2009< >, the blood gas analysis in patients with chronic type II re-spiratory failure in 62 cases were randomly divided into rehabilitation treatment group 32 cases, control group of 30 cases. Pa-tients in the observation group were treated by on-invasive ventilation, while the control group were treated by the convention-al treatment. The data such as arterial blood gas、pulmonary function、the grade about dyspnea and echocardiography was col-lected from the both group before the beginning of the treatment and after the three months. Results: the PaO2 level、FEV1.0、FEV1.0%、the grade of dyspnea and the Right Ventricular Ejection Fractions were not significantly different between the experi-mental group and the control before the start of the treatment (P>0.05) . After the three month treatment, the PaO2 level of the observation was significantly lower the control (P<0.05) . The data about FEV1.0、FEV1.0% and the Right Ventricular Ejection Fractions were higher than the control group (P<0.05) . Conclusion: Non-invasive ventilation has exactly effect in the treat-ment of the pneumoconiosis patients with Chronic Respiratory Failure. It can improve the function of the heart and lung and ease the pain of patients.


Subject(s)
Noninvasive Ventilation , Pneumoconiosis/therapy , Respiratory Insufficiency/therapy , Blood Gas Analysis , Humans , Lung , Pneumoconiosis/complications , Positive-Pressure Respiration , Respiratory Insufficiency/etiology
9.
Curr Med Chem ; 18(26): 4012-8, 2011.
Article in English | MEDLINE | ID: mdl-21824090

ABSTRACT

Aberrant activation of the signal transducer and activator of transcription (STAT) 3 occurs in many human tumors. Constitutive STAT3 activity induces specific target genes that stimulate cell proliferation, prevent apoptosis, promote angiogenesis and facilitate tumor immune evasion. Thus, STAT3 is an attractive molecular target for the development of novel cancer therapeutics. Targeting and disruption of oncogenic STAT3 signaling may theoretically be accomplished through various approaches, involving direct and indirect strategies. Small molecular weight compounds have been used for this purpose. This review is intended to be full coverage of the small molecular inhibitors to develop direct STAT3 as a target for cancer therapy and will provide a discussion on the inhibitory modalities developed to date. At present, we retrieved related small molecular inhibitors experimental research papers about STAT3 as a cancer therapy target, the rationale to pursue the protein for the discovery and development of novel anticancer strategies and agents.


Subject(s)
Neoplasms/drug therapy , STAT3 Transcription Factor/antagonists & inhibitors , Signal Transduction/drug effects , Animals , Cell Line, Tumor , Gene Expression Regulation, Neoplastic/drug effects , Humans , Mice , Molecular Targeted Therapy , Neoplasms/therapy , STAT3 Transcription Factor/chemistry , STAT3 Transcription Factor/genetics , STAT3 Transcription Factor/metabolism , Signal Transduction/physiology , Small Molecule Libraries/chemistry , Small Molecule Libraries/pharmacology
10.
Mol Reprod Dev ; 59(3): 314-21, 2001 Jul.
Article in English | MEDLINE | ID: mdl-11424217

ABSTRACT

The nonchromatin structure or nuclear matrix in developing spermatogenic cells of the rat was studied using a biochemical fractionation in concert with resinless section electron microscopy. Observations demonstrated that the nuclear matrix of spermatogenic cells consisted of a three-dimensional network of filaments of variable thicknesses. In spermatogonia and spermatocytes the nuclear matrix consisted of relatively thin filaments, while that of round spermatids consisted of a thicker interconnecting network of filament. In elongating spermatids, the interior of the nuclear matrix consisted of a network of dense filaments bounded by a peripheral lamina. The protein composition of the nuclear matrix in spermatogenic cells was examined by high-resolution two-dimensional gel electrophoresis and correlated with morphological changes characteristic of each stage. The results showed that the proteins of nuclear matrix changed in a cell stage-specific manner. These stage-specific changes corresponded to the major transitions of chromatin structure and function during spermatogenesis. Furthermore, immunocytochemical and immunoblotting analysis of DNA topoisomerase II (topo II) revealed that this enzyme exhibited stage-specific variations and was associated with the nuclear matrix. These results suggest that the nuclear matrix in spermatogenic cells may be involved in mediating DNA modifications and maintaining nuclear organization during spermatogenesis. Mol. Reprod. Dev. 59:314-321, 2001.


Subject(s)
Nuclear Matrix/ultrastructure , Spermatogenesis , Spermatozoa/ultrastructure , Testis/cytology , Animals , Antigens, Nuclear , Cell Fractionation , DNA Topoisomerases, Type II/metabolism , Electrophoresis, Gel, Two-Dimensional , Histocytological Preparation Techniques/methods , Immunoblotting , Male , Microscopy, Immunoelectron , Nuclear Matrix/chemistry , Nuclear Proteins/analysis , Rats , Spermatids/chemistry , Spermatids/enzymology , Spermatids/ultrastructure , Spermatocytes/chemistry , Spermatocytes/enzymology , Spermatocytes/ultrastructure , Spermatogonia/chemistry , Spermatogonia/enzymology , Spermatogonia/ultrastructure , Spermatozoa/chemistry , Spermatozoa/enzymology , Testis/enzymology
11.
Article in Chinese | MEDLINE | ID: mdl-12571934

ABSTRACT

OBJECTIVE: To verify the efficacy of abendazole emulsion, a new formulation of abendazole, in treatment of human cystic echinococcosis. METHODS: 212 patients with liver cystic echinococcosis were treated orally with albendazole emulsion at a daily dose of 10 mg/kg or 12.5 mg/kg for 3 to 12 months or over one year. The therapeutic efficacy was mainly evaluated by image feature examined with B ultrasound examination, a short-term efficacy at the completion of treatment and a long-term efficacy followed-up for 1-4 years. RESULTS: In 212 patients treated with albendazole emulsion at a daily dose of 10 mg/kg and 12.5 mg/kg, the average cure rate, improved rate and the rate of no avail were 74.5%, 99.1% and 0.9% respectively after termination of the treatment, and the average long-term rates were 83.1%, 89.3% and 0.6% respectively. Recurrence occurred in 18 patients(10.2%). The results indicated that the best efficacy was seen in patients treated with albendazole 12.5 mg/kg daily for 9 months. Better response was also found when the recurrent patients were re-treated with albendazole. CONCLUSION: The efficacy of albendazole emulsion on patients with liver cystic echinococcosis is much better than that of albendazole tablet or capsule and mebendazole. Meanwhile, the efficacy of albendazole emulsion is stable with less adverse effects. The results suggest that albendazole emulsion could be the drug of choice for treatment of cystic hydatid disease.


Subject(s)
Albendazole/therapeutic use , Anthelmintics/therapeutic use , Echinococcosis, Hepatic/drug therapy , Albendazole/administration & dosage , Anthelmintics/administration & dosage , Emulsions , Female , Follow-Up Studies , Humans , Male , Treatment Outcome
12.
Appl Environ Microbiol ; 57(8): 2164-70, 1991 Aug.
Article in English | MEDLINE | ID: mdl-1662930

ABSTRACT

The interaction of the peptide antibiotic nisin with liposomes has been studied. The effect of this interaction was analyzed on the membrane potential (inside negative) and the pH gradient (inside alkaline) in liposomes made from Escherichia coli phosphatidylethanolamine and egg phosphatidylcholine (9:1, wt/wt). The membrane potential and pH gradient were generated by artificial ion gradients or by the oxidation of ascorbate, N,N,N',N'-tetramethyl-p-phenylenediamine, and cytochrome c by the beef heart cytochrome c oxidase incorporated in the liposomal membranes. Nisin dissipated the membrane potential and the pH gradient in both types of liposomes and inhibited oxygen consumption by cytochrome c oxidase in proteoliposomes. The dissipation of the proton motive force in proteoliposomes was only to a minor extent due to a decrease of the oxidase activity by nisin. The results in these model systems show that a membrane potential and/or a pH gradient across the membrane enhances the activity of nisin. Nisin incorporates into the membrane and makes the membrane permeable for ions. As a result, both the membrane potential and pH gradient are dissipated. The activity of nisin was found to be influenced by the phospholipid composition of the liposomal membrane.


Subject(s)
Electron Transport Complex IV/metabolism , Liposomes/metabolism , Nisin/pharmacology , Proteolipids/metabolism , Animals , Cattle , Escherichia coli , Hydrogen-Ion Concentration/drug effects , Kinetics , Membrane Potentials/drug effects , Models, Biological , Phosphatidylcholines , Phosphatidylethanolamines
13.
Yao Xue Xue Bao ; 26(12): 895-901, 1991.
Article in Chinese | MEDLINE | ID: mdl-1823988

ABSTRACT

2-Chloro-6-methoxy-8-nitroquinoline was reacted with substituted benzyl alcohols (or sodium methanol) and then brominated to give 2-substituted benzyloxy-6-methoxy- and 2,6-dimethoxy-5-bromo-8-nitroquinolines (compounds 5-8 in Table 1). These products were condensed with substituted phenols to form corresponding 5-substituted phenoxy compounds (9-19 in Tables 1 and 2) which were subsequently reduced to afford 2-substituted benzyloxy-6-methoxy- and 2,6-dimethoxy-5-substituted phenoxy-8-aminoquinolines (20-28, 47 and 48 in Tables 3 and 6). Condensation with 4-bromophthalimidopentane yielded corresponding 8-(4-phthalimido-1-methylbutyl)aminoquinolines (29-37, 49 and 50 in Tables 4 and 6) which were subsequently treated with hydrazine hydrate to give 2-substituted benzyloxy-6-methoxy- and 2,6-dimethoxy-5-substituted phenoxy-8-(4-amino-1-methylbutyl)amino-quinolines, compounds III and IV (38-46, 51 and 52 in Tables 5 and 6), the analogues of primaquine. Compounds III and IV were tested against Plasmodium yoenii in mice infected with sporozoites. The parasitaemia of 80% and 90% of tested mice was negative at an oral single dose of 100 mg/kg of compounds 39 and 45, respectively. The results of further studies on compound 45 showed that the parasitaemia of 80% of mice was negative at a single dose of 20 mg/kg, and the acute toxicity in mice was less than that of primaquine.


Subject(s)
Antimalarials/chemical synthesis , Malaria/drug therapy , Plasmodium yoelii/drug effects , Primaquine/analogs & derivatives , Primaquine/chemical synthesis , Animals , Antimalarials/pharmacology , Mice , Molecular Structure , Primaquine/pharmacology
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