<b>OBJECTIVEb>To study the chemical constituents of Swertia hispidicalyx.

<b>METHODb>The EtOAc part of S. hispidicalyx was chromatographied by various column chromatography methods, and the isolates were identified based on spectroscopic analyses (MS, 1H-and 13C-NMR).

<b>RESULTb>Eleven compounds were isolated from S. hispidicalyx and characterized as 1,3,5,8-tetrahydroxyxanthone (1), 1,5,8-trihydroxy-3-methoxyxanthone (2), gentiolactone (3), swertiamarin (4), 3,4-dihydro-1H,6H,8H-naphtho [1, 2-c:4, 5-c', d'] dipyrano-1,8-dione (5), (+)-syringaresinol (6), trans-coniferyl aldehyde (7), maslinic acid (8), oleanolic acid (9), daucosterol (10), and -sitosterol (11).

<b>CONCLUSIONb>Compounds 1-11 were obtained from S. hispidicalyx for the first time.

Antiviral Agents ; isolation & purification ; pharmacology ; Hepatitis B virus ; drug effects ; Swertia ; chemistry

Fifteen known compounds were isolated from Swertia delavayi by silica gel, Sephadex LH-20 and Rp-18 column chromatographies. Based on extensive spectroscopic analysis (MS, 1H, 13C-NMR), their structures were identified aserythrocentaurin (1), erythrocentaurindimethylacetal (2), sweroside (3), swertiamarin (4), gentiopicroside (5), swertiakoside A (6), 2'-O-acetylswertiamarin (7), 4'-O-[(Z) -coumaroyl] swertiamarin (8), 1,5,8-trihydroxy-3-methoxyxanthone (9), 8-O-β-D-glucopyranosyl-1-hydroxy-2,3, 5-trimethoxyxanthone (10), 8-O-[β-D-xyl- opyranosyl-(1 --> 6)-β-D-glucopyranosyl]-7,8-dihydroxy-3-methoxyxanthone (11), isovitexin (12), β-sitosterol (13), daucosterol (14), and oleanolic acid (15). Among them, ten ones (14, 7-11, 13) were obtained from S. delavayi for the first time. The isolates were evaluated for their anti-HBV activities in HepG 2. 2. 15 cell line in vitro. The results showed that compound 1, 2, 6, 7, 9 and 12 exhibited significant inhibitory activity on HBV DNA replication with IC50 values from 0.05 to 1.46 mmol x L(-1).
Antiviral Agents ; chemistry ; isolation & purification ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Hepatitis B virus ; drug effects ; genetics ; Magnetic Resonance Imaging ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Swertia ; chemistry

<b>OBJECTIVEb>To investigate the anti-HBV constituents in the roots of Euphorbia fischeriana.

<b>METHODb>The compounds were isolated by various chromatographic methods and identified by spectroscopic analysis. Some compounds were tested for the anti-HBV activity.

<b>RESULTb>Eleven compounds were isolated and identified as tirucalla-5,24-dien-3-ol (1), 24-methyltirucalla-5, 24-dien-3-ol (2), euphol (3), butyrospermol (4), 24-methylenecycloartenol (5), cycloartenol (6), jolkinolid E (7) helioscopinolide A (8), isoscopoletion (9), dephnoretin (10), and 3, 3'-di-O-methylellagic acid 4'-O-beta-D-xylopyranoside (11).

<b>CONCLUSIONb>Compounds 1, 2 and 10 were isolated from the genus Euphorbia for the first time. Compounds 3, 4 and 11 were isolated from this species for the first time. Compounds 1, 8, 9 and 11 showed weak anti-HBsAg and anti-HBeAg activity, while compound 10 showed weak anti-HBsAg activity.

Antiviral Agents ; analysis ; isolation & purification ; pharmacology ; Drugs, Chinese Herbal ; analysis ; isolation & purification ; pharmacology ; Euphorbia ; chemistry ; Hepatitis B virus ; drug effects ; Plant Roots ; chemistry

Adolescent ; Adult ; Aged ; DNA Mutational Analysis ; DNA, Viral ; genetics ; Drug Resistance, Viral ; drug effects ; genetics ; Female ; Hepatitis B virus ; drug effects ; genetics ; isolation & purification ; Hepatitis B, Chronic ; genetics ; virology ; Humans ; Male ; Middle Aged ; Young Adult

<b>OBJECTIVEb>To evaluate clinical applicability of a novel technique that can quantify the lamivudine-resistant mutants of hepatitis B virus (HBV) in the serum of patients utilizing gene microarray technology.

<b>METHODSb>The oligonucleotide microarray was designed to detect 3 important mutational positions. Fifty-one patients who were receiving lamivudine therapy were selected as subjects. The oligonucleotide microarray and traditional sequencing were applied to detect the lamivudine resistant mutation, the monitoring lasted for 24 months. Then the clinical result was analyzed and the obtained data were compared between the two methods.

<b>RESULTSb>Lamivudine resistant mutation was detected in 39 percent of the patients during the 2 years period. The results of the oligonucleotide microarray technique was consistent to the results of traditional sequencing in accuracy and the miroarray was more sensitive in detection of the mixed infection.

<b>CONCLUSIONb>Application of the oligonucleotide microarray for quantitative detection of lamivudine-resistant mutation of HBV is feasible.

Antiviral Agents ; therapeutic use ; Drug Resistance, Viral ; Female ; Hepatitis B ; drug therapy ; virology ; Hepatitis B virus ; drug effects ; genetics ; isolation & purification ; Humans ; Lamivudine ; therapeutic use ; Male ; Mutation ; Oligonucleotide Array Sequence Analysis ; methods

<b>OBJECTIVEb>To establish a new method for rapidly selecting anti-hepatitis B virus drugs in clinical therapy.

<b>METHODSb>The full-length hepatitis B virus (HBV) genomes from 8 patients with chronic hepatitis B (CHB) were generated by polymerase chain reaction (PCR). All patients were resistant to lamivudine therapy. Their HBV DNA fragments were inserted into Sap I site of pHY106 eukaryotic expression vector separately. The recombinant plasmids containing 1.1 copies of HBV genome were transfected into Huh7 cell line; the levels of HBsAg, HBeAg and HBV DNA in supernatants of Huh7 cells were measured by ELISA and real-time quantitative PCR, and intracellular HBV replicative intermediates were detected by Southern blot. Antiviral effects of lamivudine and adefovir were evaluated in this vitro system.

<b>RESULTSb>The 8 recombinant plasmids containing a full-length genome of clinical HBV isolates could replicate and be expressed in Huh 7 cells. There were 6 isolates with polymerase YVDD mutations and 2 isolates with polymerase YIDD mutations. Adefovir, but not lamivudine, inhibited the HBV replication and gene expression in vitro. Furthermore, adefovir inhibited HBV replication in these CHB patients.

<b>CONCLUSIONb>The method described here enables a rapid selection of anti-HBV drugs in clinical therapy and is very useful in antiviral therapy for CHB patients.

Adult ; Antiviral Agents ; pharmacology ; Drug Evaluation, Preclinical ; Drug Resistance, Viral ; Female ; Hepatitis B ; virology ; Hepatitis B virus ; drug effects ; genetics ; isolation & purification ; Humans ; Male ; Middle Aged ; Virosomes ; Young Adult

<b>OBJECTIVEb>To analyze the development of liver damage and reactivation of hepatitis B virus (HBV) during the treatment of extremely severe burn injury in HBsAg positive patients, in order to provide reference for prevention and treatment of liver damage in patients with HBV infection after extremely severe burn.

<b>METHODSb>Medical records of 54 HBsAg positive patients after extremely severe burn injury admitted from January 2004 to December 2014 were retrospectively analyzed. Development of liver damage and HBV reactivation of these patients during the treatment were analyzed according to the classification of their gender, results of hepatitis B e antigen (HBeAg) and HBV DNA examinations on admission, and development of sepsis in the process of treatment. Data were processed with chi-square test.

<b>RESULTSb>(1) The incidence of liver damage in the process of treatment of these patients was 85.2% (46/54). Among all the patients, the proportion of liver damage was 35/38 in male, which was significantly higher than that in female (11/16, χ² = 4.867, P<0.05). Liver damage was found in all of 26 patients who were HBeAg positive on admission, 34 patients who were HBV DNA positive on admission, and 36 patients who developed sepsis in the process of treatment; the proportions were significantly higher than those in patients who were HBeAg negative on admission (20/28), patients who were HBV DNA negative on admission (12/20), and patients who did not develop sepsis in the process of treatment (10/18), with χ² values respectively 11.801, 18.384, and 20.574, P values below 0.01. (2) The incidence of HBV reactivation in these patients was 29.6% (16/54). Among all the patients, the proportion of HBV reactivation was 13/38 in male and 3/16 in female, with no statistically significant difference between them (χ² = 0.656, P>0.05). The proportions of HBV reactivation in patients who were HBeAg positive on admission, patients who were HBV DNA positive on admission, and patients who developed sepsis in the process of treatment were respectively 13/26, 16/34, and 15/36, and they were significantly higher than those in patients who were HBeAg negative on admission (3/28), patients who were HBV DNA negative on admission (0/20), and patients who did not develop sepsis in the process of treatment (1/18), with χ² values respectively 9.979, 18.615, and 5.873, P<0.05 or P<0.01.

<b>CONCLUSIONSb>Patients who are HBsAg positive, HBeAg positive, HBV DNA positive on admission, and develop sepsis in the process of treatment of extremely severe burn injury are more likely to develop liver damage and HBV reactivation. It is necessary to dynamically monitor the changes in HBV DNA and liver function, in order to identity the reactivation of virus.

Alanine Transaminase ; blood ; Burns ; complications ; drug therapy ; Chemical and Drug Induced Liver Injury ; DNA, Viral ; Female ; Hepatitis Antibodies ; blood ; Hepatitis B ; drug therapy ; epidemiology ; virology ; Hepatitis B Surface Antigens ; blood ; immunology ; Hepatitis B virus ; drug effects ; immunology ; isolation & purification ; Hepatitis B, Chronic ; blood ; pathology ; virology ; Humans ; Incidence ; Liver ; pathology ; Male ; Retrospective Studies

It has been previously shown that Taraphochlamys affinis possessed anti-hepatitis B virus (HBV) activities. To identify the active ingredients, the total saponins (TSTA) were isolated from T. affinis and the inhibitory effect of TSTA on HBV in the duck HBV model was examined. The results showed that serum levels of DHBV-DNA decreased in all ducks treated with TSTA (1.0 and 2.0 g x kg(-1) x d(-1)) and lamivudine (3TC) (50 mg x kg(-1) x d(-1)) during treatment, but 7 days after the cessation of treatment (p7) with 3TC, the viral replication level returned to the pretreatment baseline. Contrariwise in ducks treated with TSTA, the effect of DHBV DNA inhibition lasted. Compared with model control group,the alanine aminotransferase (ALT), aspartate aminotransferase (AST) and duck hepatitis B surface antigen (DHBsAg) values of 1.0 and 2.0 g x kg(-1) x d(-1)-dose TSTA groups were significantly lower on 7, 14 days after the treatment (d7, d14) and p7, and at p7, the ALT and DHBsAg levels of 2.0 g x kg(-1) x d(-1)-dose TSTA group was significantly lower than that of 3TC group. Furthermore, significant histological improvement was noted in ducklings of TSTA treatment group 7 days after the withdrawal. The study results demonstrate that TSTA possesses potent anti-HBV activity.
Animals ; Antigens, Surface ; blood ; Antiviral Agents ; administration & dosage ; isolation & purification ; pharmacology ; DNA, Viral ; blood ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Hepadnaviridae Infections ; drug therapy ; virology ; Hepatitis B Virus, Duck ; drug effects ; immunology ; Hepatitis, Viral, Animal ; drug therapy ; virology ; Liver ; drug effects ; metabolism ; pathology ; Liver Function Tests ; Saponins ; administration & dosage ; isolation & purification ; pharmacology ; Virus Replication ; drug effects

<b>OBJECTIVEb>To analyze antiviral effects of entecavir in patients with hepatitis B virus-related cirrhosis.

<b>METHODSb>104 patients of hepatitis B virus-related cirrhosis with no previous history of antiviral therapy were treated with entecavir 0.5 mg once daily. 37 patients were taken hepatic histologic examination before and after the treatment.

<b>RESULTSb>Mean reductions of serum HBV DNA was 5.1 log10 96 weeks after the treatment, HBV DNA became undetectable in 98.1% patients, and ALT became normal in 80.7% patients; HBeAg seroconversion occurred in 13.9% of the 72 HBeAg positive patients; 61.5% of these patients were infected with genotype C HBV, and 26.9% were infected with genotype B HBV. The genotype of HBV was not associated with the therapeutical effect. Child-pugh score was associated with the progression of the disease: the proportion of patients with disease progression was highest in Child-Pugh C grade patients and lowest in Child-Pugh A grade patients. The level of the HBV DNA load was positively correlated with Knodell HAI score at the baseline and 96 weeks after the treatment.

<b>CONCLUSIONb>Entecavir treatment results in suppression of HBV replication and delayed progression of fibrosis in patients with hepatitis B virus-related cirrhosis.

Adult ; Alanine Transaminase ; blood ; Antiviral Agents ; therapeutic use ; DNA, Viral ; blood ; Female ; Genotype ; Guanine ; analogs & derivatives ; therapeutic use ; Hepatitis B e Antigens ; blood ; Hepatitis B virus ; drug effects ; genetics ; isolation & purification ; Hepatitis B, Chronic ; complications ; drug therapy ; virology ; Humans ; Liver Cirrhosis ; drug therapy ; etiology ; virology ; Male ; Middle Aged ; Time Factors ; Treatment Outcome ; Virus Replication ; drug effects

BACKGROUND AND AIMS: Telbivudine is an L-nucleoside analogue with potent antiviral activity against hepatitis B virus (HBV). Clinical trials have shown that telbivudine is more potent than lamivudine for suppressing virus. METHODS: A total 101 Korean patients among 1,367 patients who participated in the phase III GLOBE trial were randomized in this study. All 101 HBeAg positive or HBeAg negative patients were assigned to treatment with 600 mg of telbivudine or 100 mg of lamivudine once daily. The primary efficacy endpoint (the "therapeutic response") was defined as suppression of the serum HBV DNA to less than 5 log10 copies/mL coupled with either normalization of the serum alanine aminotransferase level or loss of HBeAg. The secondary endpoints included the histologic response, serum HBV DNA reduction, serum alanine aminotransferase normalization and HBeAg loss for the HBeAg positive patients. This analysis includes the data collected at 52 weeks of treatment. RESULTS: Fifty four of 101 patients were assigned to telbivudine treatment and 47 patients were assigned to lamivudine treatment. At week 52, significantly more patients who were treated with telbivudine than those treated with lamivudine had a therapeutic response (83% vs 62%, respectively, P=0.017), their mean serum HBV DNA levels were more reduced (6.6 vs 5.6 log10 copies/mL, respectively, P=0.027), and they more often achieved PCR-undetectable levels of serum HBV DNA (74% vs 34%, P<0.0001). No virologic resistance to telbivudine was detected (0% vs 18%, respectively, P=0.001). Telbivudine was well tolerated and it had a safety profile comparable to lamivudine. CONCLUSIONS: Patients treated with telbivudine achieved earlier and more profound viral suppression than those treated with lamivudine.
Adolescent ; Adult ; Alanine Transaminase/analysis ; Antiviral Agents/administration & dosage/adverse effects/*therapeutic use ; Drug Resistance, Viral ; Female ; Hepatitis B e Antigens/analysis ; Hepatitis B virus/drug effects/genetics/isolation & purification ; Hepatitis B, Chronic/*drug therapy/virology ; Humans ; Korea ; Lamivudine/administration & dosage/adverse effects/therapeutic use ; Male ; Middle Aged ; Nucleosides/administration & dosage/adverse effects/*therapeutic use ; Pyrimidinones/administration & dosage/adverse effects/*therapeutic use ; Treatment Outcome