OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detect...OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.展开更多
The exotic Sonneratia apetala in Leizhou Peninsula, has shown outstanding fast-growing ability in restored mangrove forests, at the middle and high tide intertidal zone, with year-round fresh water input from drainage...The exotic Sonneratia apetala in Leizhou Peninsula, has shown outstanding fast-growing ability in restored mangrove forests, at the middle and high tide intertidal zone, with year-round fresh water input from drainage. By setting plot and selecting standard tree, investigation and measurement on height growth, diameter growth, biomass, productivity, and so on, were made in a S. apetala plantation at age of six at Lanbei, Fucheng, Leizhou Peninsula in May 2001. The investigating results showed that the mean annual height growth of plantation was 2.03 m and mean annual growth of diameter at breast height (DBH) was 2.35 cm. There exists a significant correlation between the diameter at ground surface (DGS) and DBH. The average biomass of a single standard tree in dry weight was 95.647 kg/m2. A ratio of above-ground biomass to under-ground biomass was 1.60. The stand biomass of unit area was 22.955 kg/m2, singletree wood volume was 88.23 dm3, and the annual wood volume productivity (PA) of the same year was 0.407. The forest energy accumulation was 424.851 MJ/m2, with annual solar energy fixing rate of 40.68 ×10-7%. It is concluded that S. apetala species had characteristics of outstanding high biomass accumulation and could be used as coastal planting tree species in southern China.展开更多
Leizhou Peninsula, located at southem end of mailand China, has 9 284.3 ha mangrove distributed more than 100 sites along its inlets and open coastlines. This paper presents the surveys on mangrove area in Leizhou Pen...Leizhou Peninsula, located at southem end of mailand China, has 9 284.3 ha mangrove distributed more than 100 sites along its inlets and open coastlines. This paper presents the surveys on mangrove area in Leizhou Peninsula during 2000 and 2008, especially the survey in the eight major mangrove areas in 2002. The flora recorded in mangrove systems includes 69 large algea species, 13 native true mangrove species, nine native semi-mangrove species, and another seven intoduced true mangrove species with Sonneratia apetala as the quickest growing exotic mangrove species dominatant in the mangrove plantations, and more than 100 land flora species, consisting of 17 main mangrove associations. The plant biodiversity habitats remained mainly small patches and diverse, and were becoming worse under the intensive disturbance of human acitivities and coastal pollutions, which decreased the value of mangrove coasts as the important sites for flying-by migrating birds in Leizhou Peninsula. The effective mangrove conservation measures should be implemented.展开更多
[Objective] The aim was to isolate a prodigiosin producing strain and study its pigment fractions.[Method] Red pigment-producing bacteria was identified by physiological and biochemical characteristics after isolation...[Objective] The aim was to isolate a prodigiosin producing strain and study its pigment fractions.[Method] Red pigment-producing bacteria was identified by physiological and biochemical characteristics after isolation in plate.By using column chromatography and thin-layer chromatography,pigment fractions were separated and purified from the extractives of the strain after fermentation in flask,and then pigment fractions were analyzed via UV-Vis and LC/MS.[Result] A red pigment-producing Serratia marcescens strain NS-17 sampled from soil of Nanchang was isolated and identified.2 pigment fractions showing similar UV-Vis and LC/MS characters were separated and purified,the characters of fraction 1 were identical to those of prodigiosin,while fraction 2 showed a special UV-Vis absorption spectrum that had not been reported.[Conclusion] A prodigiosin-producing Serratia marcescens strain NS-17 and its 2 pigment fractions were isolated.展开更多
AIM: The mucoprotective agents, sofalcone and polaprezinc have anti-Helicobacter pylori ( H pylori)activities. We determined the therapeutic effects of sofalcone and polaprezinc when combined with rabeprazole,amoxicil...AIM: The mucoprotective agents, sofalcone and polaprezinc have anti-Helicobacter pylori ( H pylori)activities. We determined the therapeutic effects of sofalcone and polaprezinc when combined with rabeprazole,amoxicillin and clarithromycin for Helicobacter pylori infection.METHODS: One hundred and sixty-five consecutive outpatients with peptic ulcer and H pylori infection were randomly assigned to one of the following three groups and medicated for 7 d. Group A: triple therapy with rabeprazole (10 mg twice daily), clarithromycin (200 mg twice daily) and amoxicillin (750 mg twice daily). Group B: sofalcone (100 mg thrice daily) plus the triple therapy.Group C: polaprezinc (150 mg twice daily) plus the triple therapy. Eradication was considered successful if 13C-urea breath test was negative at least 4 wk after cessation of eradication regimens or successive famotidine in the cases of active peptic ulcer.RESULTS: On intention-to-treat basis, H pyloricure wasachieved in 43 of 55 (78.2%) patients, 47 of 54 (87.0%)and 45 of 56 (80.4%) for the groups A, B and Crespectively. Using per protocol analysis, the eradication rates were 81.1% (43/53), 94.0% (47/50) and 84.9% (45/53) respectively. There was a significant difference in the cure rates between group A and B. Adverse events occurred in 10, 12 and 11 patients, from groups A, B and C respectively, but the events were generally mild.CONCLUSION: The addition of sofalcone, but not polaprezinc, significantly increased the cure rate of H pylori infection when combined with the rabeprazole-amoxicillinclarithromycin regimen.展开更多
Numerical study was performed to evaluate the characteristics of combined heat transfer of radiation, conduction and convection in indirect near infrared ray （N/R） heating chamber. The effects of important design pa...Numerical study was performed to evaluate the characteristics of combined heat transfer of radiation, conduction and convection in indirect near infrared ray （N/R） heating chamber. The effects of important design parameters such as the shape of heat absorbing cylinder and heat releasing fin on the pressure drop and heat transfer coefficient were analyzed with different Reynolds numbers. The Reynolds numbers were varied from 103 to 3x106, which was defined based on the hydraulic diameter of the heat absorbing cylinder. Analyses were performed to obtain the inner and outer flow and the temperature distributions in the heat absorbing cylinder and the rates of radiation heat transfer and convection heat transfer. As the Reynolds number increases, the convection heat transfer rate is increased while the radiation heat transfer rate is decreased. The average convection heat transfer rate follows a power rule of the Reynolds number. Addition of three-dimensional heat releasing fin to the outside of the heat absorbing cylinder enhances the convection heat transfer.展开更多
This paper focuses on semantic knowl- edge acquisition from blogs with the proposed tag- topic model. The model extends the Latent Dirichlet Allocation （LDA） model by adding a tag layer be- tween the document and th...This paper focuses on semantic knowl- edge acquisition from blogs with the proposed tag- topic model. The model extends the Latent Dirichlet Allocation （LDA） model by adding a tag layer be- tween the document and the topic. Each document is represented by a mixture of tags; each tag is as- sociated with a multinomial distribution over topics and each topic is associated with a multinomial dis- trNution over words. After parameter estimation, the tags are used to descrNe the underlying topics. Thus the latent semantic knowledge within the top- ics could be represented explicitly. The tags are treated as concepts, and the top-N words from the top topics are selected as related words of the con- cepts. Then PMI-IR is employed to compute the re- latedness between each tag-word pair and noisy words with low correlation removed to improve the quality of the semantic knowledge. Experiment re- sults show that the proposed method can effectively capture semantic knowledge, especially the polyse- me and synonym.展开更多
文摘OBJECTIVE The inhibitory effect of active ingredients of Tripterygium wilfordii Hook.F.(TWHF)(celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine)on human carboxylester⁃ase 1(CES1)and CES2 was detected to investigate the herb-drug interactions(HDIs)of TWHF.METHODS Human liver microsomes catalysed hydrolysis of 2-(2-benzoyl-3-methoxyphenyl)benzothi⁃azole(BMBT)and fluorescein diacetate(FD)were used as the probe reaction to phenotype the activity of CES1 and CES2,respectively.The residual activities of CES1 and CES2 were detected by ultrahigh performance liquid chromatography(UPLC)after intervention with celastrol,triptolide,triptonide,wilforlide A,wilforgine and wilforine(100μmol·L^(-1)).Kinetics analysis,involving half inhibitory concentra⁃tion(IC_(50)),inhibition type and kinetic parameter(Ki),and in vitro-in vivo extrapolation(IVIVE),was carried out to predict the HDIs between these compounds and CES-metabolizing drugs.Molecular docking was performed to analyze the ligand-enzyme interaction.RESULTS Out of the six main con⁃stituents of TWHF,only celastrol exhibited strong inhibition towards both CES1 and CES2,with the inhibitory rates of 97.45%(P<0.05)and 95.62%(P<0.05),respectively.The IC_(50)was 9.95 and 4.02 mol·L^(-1),respectively,and the types of inhibition were all non-competitive inhibition.Based on the kinetics analysis,the Ki values were calculated to be 5.10 and 10.55μmol·L^(-1)for the inhibition of celastrol on CES1 and CES2,respectively.IVIVE indicated that celastrol might disturb the metabolic hydrolysis of clinical drugs in vivo by inhibiting CES1.Molecular docking results showed that hydrogen bonds and hydrophobic contacts contributed to the interaction of celastrol and CESs.CONCLUSION The inhibitory effect of celastrol on CES1 and CES2 might cause HDIs with clinical drugs hydrolysed by CESs.
基金The paper was supported by the project of integrated mangrove management and coastal protection(IMMCP) in Leizhou Peninsula Guangdong Province.
文摘The exotic Sonneratia apetala in Leizhou Peninsula, has shown outstanding fast-growing ability in restored mangrove forests, at the middle and high tide intertidal zone, with year-round fresh water input from drainage. By setting plot and selecting standard tree, investigation and measurement on height growth, diameter growth, biomass, productivity, and so on, were made in a S. apetala plantation at age of six at Lanbei, Fucheng, Leizhou Peninsula in May 2001. The investigating results showed that the mean annual height growth of plantation was 2.03 m and mean annual growth of diameter at breast height (DBH) was 2.35 cm. There exists a significant correlation between the diameter at ground surface (DGS) and DBH. The average biomass of a single standard tree in dry weight was 95.647 kg/m2. A ratio of above-ground biomass to under-ground biomass was 1.60. The stand biomass of unit area was 22.955 kg/m2, singletree wood volume was 88.23 dm3, and the annual wood volume productivity (PA) of the same year was 0.407. The forest energy accumulation was 424.851 MJ/m2, with annual solar energy fixing rate of 40.68 ×10-7%. It is concluded that S. apetala species had characteristics of outstanding high biomass accumulation and could be used as coastal planting tree species in southern China.
文摘Leizhou Peninsula, located at southem end of mailand China, has 9 284.3 ha mangrove distributed more than 100 sites along its inlets and open coastlines. This paper presents the surveys on mangrove area in Leizhou Peninsula during 2000 and 2008, especially the survey in the eight major mangrove areas in 2002. The flora recorded in mangrove systems includes 69 large algea species, 13 native true mangrove species, nine native semi-mangrove species, and another seven intoduced true mangrove species with Sonneratia apetala as the quickest growing exotic mangrove species dominatant in the mangrove plantations, and more than 100 land flora species, consisting of 17 main mangrove associations. The plant biodiversity habitats remained mainly small patches and diverse, and were becoming worse under the intensive disturbance of human acitivities and coastal pollutions, which decreased the value of mangrove coasts as the important sites for flying-by migrating birds in Leizhou Peninsula. The effective mangrove conservation measures should be implemented.
文摘[Objective] The aim was to isolate a prodigiosin producing strain and study its pigment fractions.[Method] Red pigment-producing bacteria was identified by physiological and biochemical characteristics after isolation in plate.By using column chromatography and thin-layer chromatography,pigment fractions were separated and purified from the extractives of the strain after fermentation in flask,and then pigment fractions were analyzed via UV-Vis and LC/MS.[Result] A red pigment-producing Serratia marcescens strain NS-17 sampled from soil of Nanchang was isolated and identified.2 pigment fractions showing similar UV-Vis and LC/MS characters were separated and purified,the characters of fraction 1 were identical to those of prodigiosin,while fraction 2 showed a special UV-Vis absorption spectrum that had not been reported.[Conclusion] A prodigiosin-producing Serratia marcescens strain NS-17 and its 2 pigment fractions were isolated.
文摘AIM: The mucoprotective agents, sofalcone and polaprezinc have anti-Helicobacter pylori ( H pylori)activities. We determined the therapeutic effects of sofalcone and polaprezinc when combined with rabeprazole,amoxicillin and clarithromycin for Helicobacter pylori infection.METHODS: One hundred and sixty-five consecutive outpatients with peptic ulcer and H pylori infection were randomly assigned to one of the following three groups and medicated for 7 d. Group A: triple therapy with rabeprazole (10 mg twice daily), clarithromycin (200 mg twice daily) and amoxicillin (750 mg twice daily). Group B: sofalcone (100 mg thrice daily) plus the triple therapy.Group C: polaprezinc (150 mg twice daily) plus the triple therapy. Eradication was considered successful if 13C-urea breath test was negative at least 4 wk after cessation of eradication regimens or successive famotidine in the cases of active peptic ulcer.RESULTS: On intention-to-treat basis, H pyloricure wasachieved in 43 of 55 (78.2%) patients, 47 of 54 (87.0%)and 45 of 56 (80.4%) for the groups A, B and Crespectively. Using per protocol analysis, the eradication rates were 81.1% (43/53), 94.0% (47/50) and 84.9% (45/53) respectively. There was a significant difference in the cure rates between group A and B. Adverse events occurred in 10, 12 and 11 patients, from groups A, B and C respectively, but the events were generally mild.CONCLUSION: The addition of sofalcone, but not polaprezinc, significantly increased the cure rate of H pylori infection when combined with the rabeprazole-amoxicillinclarithromycin regimen.
基金supported by the Second Stage of Brain Korea 21 Projects
文摘Numerical study was performed to evaluate the characteristics of combined heat transfer of radiation, conduction and convection in indirect near infrared ray （N/R） heating chamber. The effects of important design parameters such as the shape of heat absorbing cylinder and heat releasing fin on the pressure drop and heat transfer coefficient were analyzed with different Reynolds numbers. The Reynolds numbers were varied from 103 to 3x106, which was defined based on the hydraulic diameter of the heat absorbing cylinder. Analyses were performed to obtain the inner and outer flow and the temperature distributions in the heat absorbing cylinder and the rates of radiation heat transfer and convection heat transfer. As the Reynolds number increases, the convection heat transfer rate is increased while the radiation heat transfer rate is decreased. The average convection heat transfer rate follows a power rule of the Reynolds number. Addition of three-dimensional heat releasing fin to the outside of the heat absorbing cylinder enhances the convection heat transfer.
基金supported by the National Natural Science Foundation of China under Grants No.90920005,No.61003192the Key Project of Philosophy and Social Sciences Research,Ministry of Education under Grant No.08JZD0032+3 种基金the Program of Introducing Talents of Discipline to Universities under Grant No.B07042the Natural Science Foundation of Hubei Province under Grants No.2011CDA034,No.2009CDB145Chenguang Program of Wuhan Municipality under Grant No.201050231067the selfdetermined research funds of CCNU from the colleges' basic research and operation of MOE under Grants No.CCNU10A02009,No.CCNU10C01005
文摘This paper focuses on semantic knowl- edge acquisition from blogs with the proposed tag- topic model. The model extends the Latent Dirichlet Allocation （LDA） model by adding a tag layer be- tween the document and the topic. Each document is represented by a mixture of tags; each tag is as- sociated with a multinomial distribution over topics and each topic is associated with a multinomial dis- trNution over words. After parameter estimation, the tags are used to descrNe the underlying topics. Thus the latent semantic knowledge within the top- ics could be represented explicitly. The tags are treated as concepts, and the top-N words from the top topics are selected as related words of the con- cepts. Then PMI-IR is employed to compute the re- latedness between each tag-word pair and noisy words with low correlation removed to improve the quality of the semantic knowledge. Experiment re- sults show that the proposed method can effectively capture semantic knowledge, especially the polyse- me and synonym.
