2.High Selective Synthesis of 11?-hydroxycanrenone by Biotransformation
Rong-Sheng TAO ; Hai-Feng HU ; Xiao-Dun LI ; Bao-Quan ZHU ;
Microbiology 1992;0(02):-
Canrenone is an important intermediate for the synthesis of eplerenone,a cardiovascular drug.C_ 11 ?-hydroxylation of canrenone is the key reaction,which can be done by microbial transformation.Rhizopus sp.SIPI-0602,kept in our lab,could high selectively transform canrenone to a compound named SIPI-11.By determining and analyzing the MS,UV,NMR etc.spectra of compound SIPI-11,its chemical structure was elucidated to be 11?-hydroxycanrenone.The study on flask transformation technology showed that the transformation ratio exceeded 90% when the substrate concentration was not more than 6g/L.
3.Clinical efficacy of Paroxetine combined with mid-frequency electrical pulse acupoint stimulation for premature ejaculation.
Tao LI ; Yan TAN ; Zi-ping XIE ; Wan-rong WANG ; Shu-hong WANG ; Hai OUYANG ; Zhao-peng KANG ; Sheng XIE
National Journal of Andrology 2015;21(10):921-924
OBJECTIVETo investigate the clinical value of Paroxetine combined with mid-frequency electrical pulse acupoint stimulation (EPAS) in the treatment of premature ejaculation (PE).
METHODSTotally 69 PE patients were equally assigned to receive oral Paroxetine 20 mg/d, mid-frequency EPAS, or oral Paroxetine 10 mg/d combined with mid-frequency EPAS (P + EPAS) , all for 8 weeks. We obtained the intravaginal ejaculation latency time (IELT) and Chinese Index of Premature Ejaculation (CIPE-5) scores of the patients before and after treatment, and compared adverse reactions among the three groups of patients.
RESULTSOne patient of the Paroxetine group gave up treatment because of abdominal pain and nausea. Compared with the baseline, the patients in the Paroxetine, EPAS, and P + EPAS groups all showed markedly increased IELT ([0.92 ± 0.11] vs [4.07 ± 0.11] min, P < 0.01; [0.92 ± 0.12] VS [2.78 ± 0.17] min P < 0.05; [0.91 ± 0.09] vs [5.31 ± 0.13], P < 0.01) and decreased CIPE-5 scores (12.5 ± 3.0 vs 22.0 ± 2.1, P < 0.01; 12.8 ± 2.9 vs 19.5 ± 1.9, P > 0.05; 13.1 ± 2.8 vs 25.2 ± 2.1, P 0.01), with statistically significant differences between the P + EPAS group and the other two (P < 0.05). The total effectiveness rate was 95.7% in the P + EPAS group, remarkably higher than in the Paroxetine (72.7%, P < 0.05) and the EPAS group (47.8, P < 0.01).
CONCLUSIONOral Paroxetine combined with mid-frequency EPAS has a higher safety and efficacy than either Paroxetine or EPAS alone in the treatment of PE.
Acupuncture Points ; Aged ; Combined Modality Therapy ; methods ; Ejaculation ; Electroacupuncture ; methods ; Humans ; Male ; Paroxetine ; therapeutic use ; Premature Ejaculation ; therapy ; Serotonin Uptake Inhibitors ; therapeutic use ; Treatment Outcome
4.Cytotoxicity of epigallocatechin-3-gallate to LNCaP cells in the presence of Cu2+.
Hai-ning YU ; Sheng-rong SHEN ; Yao-kang XIONG
Journal of Zhejiang University. Science. B 2005;6(2):125-131
Epigallocatechin-3-gallate (EGCG) has shown remarkably anti-cancer activity, with its bioactivity being related to reactive conditions, such as pH and metal ions. The present study investigated the degradation of EGCG and its effect on prostate cancer cell in the presence of Cu2+. EGCG was incubated with prostate cancer cells, LNCaP, pretreated with or without Cu2+. EGCG in F-12 medium was quantified using HPLC and the viability of cells was assessed by gel electrophoresis, flow cytometry, and electron microscope. The results of HPLC showed that EGCG degraded completely within 12 h in F-12 medium with or without Cu2+. Gel electrophoresis and flow cytometry did not detect apoptosis of LNCaP cells when they were incubated with EGCG. Electron microscopy examination revealed that EGCG-Cu2+ complex led to damage of cytoplasm membrane in LNCaP cells. It was speculated that not EGCG, but its oxide and complex with Cu2+, are the bioactive components responsible for its cytotoxicity to LNCaP prostate cancer cells.
Anticarcinogenic Agents
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administration & dosage
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Apoptosis
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drug effects
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Catechin
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administration & dosage
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analogs & derivatives
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Cell Line, Tumor
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Cell Proliferation
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drug effects
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Cell Survival
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drug effects
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Copper
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administration & dosage
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metabolism
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Dose-Response Relationship, Drug
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Drug Combinations
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Humans
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Male
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Prostatic Neoplasms
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drug therapy
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pathology
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physiopathology
5.Cerebral magnetic resonance imaging characteristics of eclampsia:an analysis of 15 cases
En WANG ; Wei-Hai XU ; Qin HUANG ; Jing-Rong DING ; Xiao-Ping JIN ; Ze-Ying CHAI ; Ling SUN ; Sheng XU ;
Chinese Journal of Neurology 2000;0(05):-
Objective To investigate cerebral MRI characteristics of patients with eclampsia. Methods A retrospective study was conducted on 15 cases of eclampsia and items reviewed cover all data concerning clinical features,cerebral MRI findings and results of follow-up survey.Results All of these patients had clinical symptoms of.blurred vision,headache,seizure,hypertension,proteinuria and edema of lower extremity.As for the characteristics of imaging,13 cases had only abnormal symmetric signals in parieto-occipital lobes,frontal lobe and basal ganglia were involved in 2 cases,and temporal lobe was involved in 1 case.The signals of lesions in DWI were isointense or hypointense,however they were hyperintense in ADC map.Two cases had hyperintense signals in DWI.All the patients recovered well,and all brain lesions disappeared during follow up.Conclusion The most important imaging of eclampsia is vasogenic edema with a good prognosis.
6.Effects of different time parameters on hypercholesterolemia treated with mild moxibustion.
Hai-Hui XING ; Ling-Ling WANG ; Jian-Bin ZHANG ; Hai-Rong SHENG
Chinese Acupuncture & Moxibustion 2010;30(11):937-940
OBJECTIVETo probe into the relevance between the parameters of mild moxibustion (persistent time, interval time, treatment session) and the efficacy, as well as the optimum treatment program of mild moxibustion in hypercholesterolemia.
METHODSThe patients with hypercholesterolemia were selected as the observation objects. Mild moxibustion was applied to Shenque (CV 8) and Zusanli (ST 36). The total cholesterol (TC) was taken as the index. The orthogonal experimental design was adopted for paired combination of 3 factors (persistent time, interval time and treatment session) that affected TC reducing in mild moxibustion. Moreover, the changes in blood lipid were observed to choose the optimum treatment program.
RESULTSThe importance of the factors of mild moxibustion that induced TC reducing in the patients with hypercholesterolemia was interval time > treatment session > persistent time. The effect of 10 min moxibustion on each point was better than that of 5 min moxibustion. The effect of once moxibustion every other day was better than that of once every day; and the effect of 6-week treatment was better than that of 12-week treatment.
CONCLUSIONThe interval time of mild moxibustion is the chief factor of the efficacy on hypercholesterolemia. The optimum treatment program is mild moxibustion, 10 min on each point, once every other day and lasting 6 weeks.
Adult ; Aged ; Cholesterol ; blood ; Female ; Humans ; Hypercholesterolemia ; blood ; therapy ; Male ; Middle Aged ; Moxibustion ; Time Factors ; Treatment Outcome
7.Study on antipyretic effect of Reduning injection on lipopolysaccharide-induced fever rats.
Lu-Ping TANG ; Rong-Rong HE ; Yi-Fang LI ; Hai-Bo LI ; Xin-Sheng YAO ; Kurihara HIROSHI ; Wei XIAO
China Journal of Chinese Materia Medica 2013;38(14):2374-2377
To observe the antipyretic effect of Reduning injection (RDN) on lipopolysaccharide (LPS)-induced fever rats and its impact on centric fever medium. Rats were randomly divided into the blank control group, the model group, the Metamizole group, and high and low-dose RDN groups. Except for the blank control group, all of the rats were injected intraperitoneally with LPS (80 microg x kg(-1)) to observe their body temperature changes. The double-antibody sandwich ELSIA method was adopted to determine cAMP content in hypothalamus and MPO in lung tissues of fever peak rats. The high-dose RDN group can obviously reduce the temperature rise in fever rats, and cAMP and MPO content in hypothalamus. RDN showed significant antipyretic effect, which may be related with the reduction of cAMP content in hypothalamus and MPO in lung tissues.
Animals
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Antipyretics
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pharmacology
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Drugs, Chinese Herbal
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pharmacology
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Fever
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chemically induced
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drug therapy
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Lipopolysaccharides
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Male
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Plants, Medicinal
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Random Allocation
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Rats
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Rats, Sprague-Dawley
8.n-MSP detection of p16 gene demethylation and transcription in human multiple myeloma U266 cell line induced by arsenic trioxide.
Hai-Ying FU ; Jian-Zhen SHENG ; Song-Fei SHENG ; Hua-Rong ZHOU
Journal of Experimental Hematology 2007;15(1):79-85
The study was purposed to investigate the effect of arsenic trioxide (As(2)O(3))- induced p16 gene demethylation by a sensitive and specific PCR-based method (nested-methylation specific PCR, n-MSP) and DNA sequencing for rapid analysis of the promoter demethylation status, and to explore the possible mechanism of the p16 gene demethylation in human multiple myeloma U266 cells induced by As(2)O(3). The methylation status of the p16 gene in U266 cell line before and after treatment with As(2)O(3) was detected by the nested-methylation specific PCR and DNA sequencing, the mRNA of p16, DNA methyltransferase (DNMT 1, DNMT3A and 3B) gene were determined by RT-PCR, and the induced growth inhibition of U266 cell was assayed by growth curve, MTT and CFU; the DNA content of U266 cells was analyzed by flow cytometry after being exposed to As(2)O(3). The results showed that (1) all cytosines in CpG dinucleotides in untreated U266 cell not were changed, while all cytosines in treated U266 cells with As(2)O(3) had been converted to thymidine. (2) p16 gene was not expressed in U266 cell line after methylation. As compared with the beta-actin, the expression of U266 cell p16 gene mRNA was increased to (0.22 +/- 0.10), (0.59 +/- 0.11), (0.68 +/- 0.09) after exposed to 0.5 micromol/L, 1.0 micromol/L and 2.0 micromol/L As(2)O(3) for 72 hours respectively. (3) As(2)O(3) could significantly down-regulate DNA methyltransferase 1 (DNMT 1), DNMT3A and DNMT3B gene at mRNA level in a dose-dependent manner. (4) U266 cells line grew slowly and arrested at G(0) - G(1) phase after treatment with three different concentrations of As(2)O(3). It is concluded that As(2)O(3) can activate and up-regulate the expression of p16 gene which inhibits the proliferation of U266 cell through inducing the G(0) - G(1) arrest by demethylation or/and by inhibiting DNMT 1, DNMT3A and 3B gene.
Antineoplastic Agents
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pharmacology
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Arsenicals
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pharmacology
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Base Sequence
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Cell Line, Tumor
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Cyclin-Dependent Kinase Inhibitor p16
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biosynthesis
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genetics
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DNA (Cytosine-5-)-Methyltransferase 1
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DNA (Cytosine-5-)-Methyltransferases
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biosynthesis
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genetics
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DNA Methylation
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drug effects
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Genes, p16
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Humans
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Molecular Sequence Data
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Multiple Myeloma
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genetics
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metabolism
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pathology
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Oxides
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pharmacology
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Polymerase Chain Reaction
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methods
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Promoter Regions, Genetic
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genetics
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RNA, Messenger
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biosynthesis
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genetics
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Transcription, Genetic
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drug effects
9.Report on the surveillance results of endemic fluorosis in Qinghai Province in 2007
Sheng-ying, WEI ; Ping, DING ; Sheng-rong, DING ; Hai-yan, ZHANG ; Shu-bang, LI ; Xiu-li, ZHANG ; Wen-gui, CHEN ; Qing, LU ; You-fu, LI
Chinese Journal of Endemiology 2008;27(6):671-672
Objective To investigate the fulfillment of improved water measures for endemic fluomsis and to find out the trend of prevalence in Qinghai Province in order to provide scientific basis and technical support for the government to formulate control strategies for endemic fluorosis.Methods Usage and management of reforming water facilities in Huzhu County were generally surveyed.Yanya Village,Caijiabu Town,Huzhu County was chosen as the surveillance spot.The household drinking water was surveyed.The dental fluorosis and urine fluoride content of children aged 8-12 years and adult above 16 years were examined.Skeletal fluorosis of adult was checked.The fluomsis content in drinking water and urine was determined with F-ion selective electrode method.The dental fluowsis was examined with Dean index.Skeletal fluorosis was diagnosed according to eountry standard(GB 16396-1996.WS 192-1999).Results The rate of water-improving was 60%(36/60)in Huzhu County.The mean of fluoride content in drinking water Was 1.25 mg/L The prevalence rate of dental fluorosis of children aged 8-12 years was 90.20%(46/51);that of adult was 88.89%(48/54).The dental fluorosis index of children was 1.77,that of adult was 2.95.The prevalence rate of skeletal fluorosis was 98.15% indicated by clinical data,18.87% by X-ray.The ufine fluorosis content of children was 2.27 mg/L,that of adult was 2.00 mg/L.Conclusion The disease condition of endemic fluorosis in Qinshai is serious,defluofidation is slow in effect.
10.The impact of early rapid virological response on the outcomes of hepatitis B associated acute on chronic liver failure during antiviral treatment.
Li CHEN ; Cai-xia ZHENG ; Ming-hua LIN ; Qiao-rong GAN ; Rong-sheng LIN ; Hai-bing GAO ; Jian-rong HUANG ; Chen PAN
Chinese Journal of Hepatology 2011;19(10):734-737
OBJECTIVETo investigate the impact of early rapid virological response on the outcomes of hepatitis B associated acute on chronic liver failure during antiviral treatment.
METHODS106 acute on chronic liver failure patients in our hospital from January 2008 to July 2010 were enrolled in present study retrospectively. Besides internal medicine therapy, all patients received lamivudine (100 mg/d) or entecavir (0.5 mg/d) treatment. The profile of liver biochemistry, prothrombin time activity and viral load were detected at baseline and week 4, respectively. The patients were divided into HBV DNA negative group and HBV DNA positive group according to the viral load at week 4. The clinical features and treatment outcomes were compared between groups. Frequency variables were compared by x2 test or Fisher's exact test. Continuous variables were compared using independent samples T-test. The factors that impact on the treatment outcomes were determined using stepwise multivariate logistic regression analysis.
RESULTSAt the week 4, the TBil and PTA in HBV DNA positive group [(261.6+/-205.6)mumol/L and 44.7%+/-19.7%, respectively] were significantly different from those in HBV DNA negative group [(160.1+/-173.4) mumol/L and 56.8%+/-23.1%, respectively] ( t = 2.190 and -2.077, respectively, P less than 0.05). The non-effective rate of HBVDNA positive group (50%, 9/18) was significantly higher than that of HBV DNA negative group (14.8%, 13/88) (x2 = 9.235, P less than 0.01). By using stepwise multivariate logistic regression analysis, the disease stage and HBV DNA undetectable at week 4 were the independent factor. The OR values of disease stage and HBV DNA undetectable were 6.559 and 0.209, respectively, and 95% CI was 2.316~18.576 and 0.058~0.747, respectively.
CONCLUSIONThe rapid suppression of viral load by nucleotide analogue may improve the efficacy of hepatitis B associated acute on chronic liver failure treatment. The early rapid virological response within first 4 weeks may contribute to the prediction of the treatment outcomes.
Adult ; Antiviral Agents ; therapeutic use ; DNA, Viral ; blood ; End Stage Liver Disease ; drug therapy ; virology ; Female ; Hepatitis B ; drug therapy ; Humans ; Liver Failure, Acute ; drug therapy ; virology ; Male ; Middle Aged ; Prognosis ; Retrospective Studies ; Treatment Outcome ; Viral Load