Geranyl phenyl ethers from Illicium micranthum and their anti-HBV activity / 中国天然药物

Fourteen new geranyl phenyl ethers (1-14) along with three known compounds (15-17) were isolated from Illicium micranthum, and their structures were elucidated by comprehensive spectroscopic methods. Illimicranins A-H (1-8) were characterized as geranyl vanillin ethers, while 9 and 10 were dimethyl acetal derivatives. Illimicranins I and J (11 and 12) were rare geranyl isoeugenol ethers. Illimicranins K and L (13 and 14) represented the first example of geranyl guaiacylacetone ether and geranyl zingerone ether, respectively. Compounds 1, 2 and 15 exhibited anti-HBV (hepatitis B virus) activity against HBsAg (hepatitis B surface antigen) and HBeAg (hepatitis B e antigen) secretion, and HBV DNA replication.

Serological prevalence of hepatitis B virus (HBV) in Mardan district, Khyber Pakhtunkhwa, Pakistan / Prevalência sorológica do vírus da hepatite B (HBV) no distrito de Mardan, Khyber Pakhtunkhwa, Paquistão

Hepatitis B virus infection is perilous among the five types of Hepatitis, as it remains clinically asymptomatic. The present study draws up-to-date prevalence of Hepatitis B virus (HBV) in the general population of Mardan, Khyber Pakhtunkhwa Pakistan. The blood samples from 4803 individuals including 2399 male and 2404 females were investigated. All the suspected samples were analyzed for hepatitis B surface antigen using Immuno-chromatographic test (ICT), Enzyme-linked immunosorbent assay (ELISA), and followed by Reverse transcription-polymerase chain reaction (RT-PCR). Results showed that 312 (13.00%) out of 2399 individuals contained antibodies in their blood against HBV, while among the different age groups, the highest incidences of HBV antibodies were found in the age of 21-30 groups (10.73%). Furthermore, the ICT positive samples were screened by nested polymerase chain reaction to detect the existence of active HBV-DNA. It was observed that 169 (7.04%) out of (2399) male of the total population (4803) tested was positive. On the other hand, the female 463 (19.25%) possessed antibodies in their blood against HBV. Accumulatively, our results showed a higher percentage of HBV prevalence in males than females in the age group 21-30 years. The total HCV infected in Mardan general population was recorded at 5.7% comprising both male and female.

A infecção pelo vírus da hepatite B é perigosa entre os cinco tipos de hepatite, pois permanece clinicamente assintomática. O presente estudo traça a prevalência atualizada do vírus da hepatite B (HBV) na população geral de Mardan, Khyber Pakhtunkhwa, no Paquistão. Amostras de sangue de 4.803 indivíduos, incluindo 2.399 homens e 2.404 mulheres, foram investigadas. Todas as amostras suspeitas foram analisadas para o antígeno de superfície da hepatite B usando teste imunocromatográfico (ICT), enzyme-linked immunosorbent assay (ELISA), seguido por transcrição reversa-reação em cadeia da polimerase (RT-PCR). Os resultados mostraram que 312 (13,00%) de 2.399 indivíduos continham anticorpos no sangue contra o VHB, enquanto, entre as diferentes faixas etárias, as maiores incidências de anticorpos VHB foram encontradas nos grupos de 21 a 30 anos (10,73%). Além disso, amostras positivas para ICT foram rastreadas por reação em cadeia da polimerase aninhada para detectar a existência de HBV-DNA ativo. Observou-se que 169 (7,04%) de 2.399 homens do total da população (4803) testados foram positivos. Por outro lado, 463 mulheres (19,25%) possuíam anticorpos no sangue contra VHB. Acumulativamente, nossos resultados mostraram uma porcentagem maior de prevalência de HBV em homens do que em mulheres na faixa etária de 21 a 30 anos. O total de HCV infectados na população geral de Mardan foi registrado em 5,7%, incluindo homens e mulheres.

Serological prevalence of hepatitis B virus (HBV) in Mardan district, Khyber Pakhtunkhwa, Pakistan

Abstract Hepatitis B virus infection is perilous among the five types of Hepatitis, as it remains clinically asymptomatic. The present study draws up-to-date prevalence of Hepatitis B virus (HBV) in the general population of Mardan, Khyber Pakhtunkhwa Pakistan. The blood samples from 4803 individuals including 2399 male and 2404 females were investigated. All the suspected samples were analyzed for hepatitis B surface antigen using Immuno-chromatographic test (ICT), Enzyme-linked immunosorbent assay (ELISA), and followed by Reverse transcription-polymerase chain reaction (RT-PCR). Results showed that 312 (13.00%) out of 2399 individuals contained antibodies in their blood against HBV, while among the different age groups, the highest incidences of HBV antibodies were found in the age of 21-30 groups (10.73%). Furthermore, the ICT positive samples were screened by nested polymerase chain reaction to detect the existence of active HBV-DNA. It was observed that 169 (7.04%) out of (2399) male of the total population (4803) tested was positive. On the other hand, the female 463 (19.25%) possessed antibodies in their blood against HBV. Accumulatively, our results showed a higher percentage of HBV prevalence in males than females in the age group 21-30 years. The total HCV infected in Mardan general population was recorded at 5.7% comprising both male and female.

Resumo A infecção pelo vírus da hepatite B é perigosa entre os cinco tipos de hepatite, pois permanece clinicamente assintomática. O presente estudo traça a prevalência atualizada do vírus da hepatite B (HBV) na população geral de Mardan, Khyber Pakhtunkhwa, no Paquistão. Amostras de sangue de 4.803 indivíduos, incluindo 2.399 homens e 2.404 mulheres, foram investigadas. Todas as amostras suspeitas foram analisadas para o antígeno de superfície da hepatite B usando teste imunocromatográfico (ICT), enzyme-linked immunosorbent assay (ELISA), seguido por transcrição reversa-reação em cadeia da polimerase (RT-PCR). Os resultados mostraram que 312 (13,00%) de 2.399 indivíduos continham anticorpos no sangue contra o VHB, enquanto, entre as diferentes faixas etárias, as maiores incidências de anticorpos VHB foram encontradas nos grupos de 21 a 30 anos (10,73%). Além disso, amostras positivas para ICT foram rastreadas por reação em cadeia da polimerase aninhada para detectar a existência de HBV-DNA ativo. Observou-se que 169 (7,04%) de 2.399 homens do total da população (4803) testados foram positivos. Por outro lado, 463 mulheres (19,25%) possuíam anticorpos no sangue contra VHB. Acumulativamente, nossos resultados mostraram uma porcentagem maior de prevalência de HBV em homens do que em mulheres na faixa etária de 21 a 30 anos. O total de HCV infectados na população geral de Mardan foi registrado em 5,7%, incluindo homens e mulheres.

Serological prevalence of hepatitis B virus (HBV) in Mardan district, Khyber Pakhtunkhwa, Pakistan / Prevalência sorológica do vírus da hepatite B (HBV) no distrito de Mardan, Khyber Pakhtunkhwa, Paquistão

Hepatitis B virus infection is perilous among the five types of Hepatitis, as it remains clinically asymptomatic. The present study draws up-to-date prevalence of Hepatitis B virus (HBV) in the general population of Mardan, Khyber Pakhtunkhwa Pakistan. The blood samples from 4803 individuals including 2399 male and 2404 females were investigated. All the suspected samples were analyzed for hepatitis B surface antigen using Immuno-chromatographic test (ICT), Enzyme-linked immunosorbent assay (ELISA), and followed by Reverse transcription-polymerase chain reaction (RT-PCR). Results showed that 312 (13.00%) out of 2399 individuals contained antibodies in their blood against HBV, while among the different age groups, the highest incidences of HBV antibodies were found in the age of 21-30 groups (10.73%). Furthermore, the ICT positive samples were screened by nested polymerase chain reaction to detect the existence of active HBV-DNA. It was observed that 169 (7.04%) out of (2399) male of the total population (4803) tested was positive. On the other hand, the female 463 (19.25%) possessed antibodies in their blood against HBV. Accumulatively, our results showed a higher percentage of HBV prevalence in males than females in the age group 21-30 years. The total HCV infected in Mardan general population was recorded at 5.7% comprising both male and female.

A infecção pelo vírus da hepatite B é perigosa entre os cinco tipos de hepatite, pois permanece clinicamente assintomática. O presente estudo traça a prevalência atualizada do vírus da hepatite B (HBV) na população geral de Mardan, Khyber Pakhtunkhwa, no Paquistão. Amostras de sangue de 4.803 indivíduos, incluindo 2.399 homens e 2.404 mulheres, foram investigadas. Todas as amostras suspeitas foram analisadas para o antígeno de superfície da hepatite B usando teste imunocromatográfico (ICT), enzyme-linked immunosorbent assay (ELISA), seguido por transcrição reversa-reação em cadeia da polimerase (RT-PCR). Os resultados mostraram que 312 (13,00%) de 2.399 indivíduos continham anticorpos no sangue contra o VHB, enquanto, entre as diferentes faixas etárias, as maiores incidências de anticorpos VHB foram encontradas nos grupos de 21 a 30 anos (10,73%). Além disso, amostras positivas para ICT foram rastreadas por reação em cadeia da polimerase aninhada para detectar a existência de HBV-DNA ativo. Observou-se que 169 (7,04%) de 2.399 homens do total da população (4803) testados foram positivos. Por outro lado, 463 mulheres (19,25%) possuíam anticorpos no sangue contra VHB. Acumulativamente, nossos resultados mostraram uma porcentagem maior de prevalência de HBV em homens do que em mulheres na faixa etária de 21 a 30 anos. O total de HCV infectados na população geral de Mardan foi registrado em 5,7%, incluindo homens e mulheres.

Advances in HBV capsid protein assembly modulators / 中国药理学通报

Hepatitis B virus (HBV) belongs to the Hepadnaviridae family. HBV infection may lead to acute and chronic hepatitis, which has become a global health issue. HBV capsid protein assembly modulators play an important role in multiple stages of HBV replication, such as encapsidation of pgRNA and synthesis of HBV DNA, thus becoming a new hotspot in the research and development of hepatitis B drugs. This paper reviews the research progress of HBV capsid protein assembly modulators.

Chemical constituents from Pogonatherum crinitum and their in vitro anti-HBV activities / 中成药

AIM To study the chemical constituents from Pogonatherum crinitum (Thunb.) Kunthand and their in vitro anti-HBV activities.METHODS The ethyl acetate and n-butanol fractions of 70％ ethanol extract from P.crinitum were isolated and purified by AB-8 macroporous resin,silica column and Sephadex LH-20,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The in vitro anti-HBV activities of the isolated compounds were tested in the model of HepG2.2.15 cells.RESULTS Eight compounds were isolated and identified as 6,8,4'-trihydroxy-7,3'-dimethoxyisoflavone (1),quercetin-7,4'-dimethylester-5-O-β-D-glucopyranoside (2),8-(1-(3,4-dihydroxyphenyl) ethyl) quercetin (3),chrysoeiml-7-O-α-L-rhamnopyranosyl-(1 → 2)-β-D-glucopyranoside (4),kaempferol-3-O-(2",3"-di-O-E-p-cou-maroyl)-α-L-rhamnopyranoside (5),1,3,7-trihydroxyxanthone-2-C-β-D-glucopyra-noside (6),luteolin-6-C-β-D-boivinopyranoside (7),luteolin-6-C-β-D-glucopyranoside (8).Compounds 3,5,7,8 had certain inhibitory effects on HBsAg with the IC50 values of 96.6,127.1,72.4 and 54.5 μg/mL.Compounds 7,8 had certain inhibitory effects on HBeAg with the IC50 values of 81.0,61.3 μg/mL.CONCLUSION Compounds 1-6 are isolated from genus Pogonatherum for the first time,compounds 3、5、7、8 have certain in vitro anti-HBV activities.

Research on the varieties, characteristics of new anti-HBV drugs and related clinical trials / 中华临床感染病杂志

HBV infection is a major public health threat around the world.At present, clinical anti-HBV drugs,including nucleoside/nucleotide analogues (NAs) and PegIFNα, can only directly or indirectly inhibit viral replication rather than viral elimination.In recent years, medical researchers and pharmaceutical enterprises are extensively researching and developing new drugs for treatment of HBV, and a variety of drugs have entered the stage of clinical trials.This article reviews the research progress on characteristics,safety and clinical trials,as well as the development trends of several currently available anti-HBV drugs, focusing on the target points and life cycle of HBV.

Design, virtual screening, synthesis and anti-hepatitis B virus of oxime derivatives / 药学学报

A series of new oxime and oxime ethers compounds were designed and virtually screened with target using the Molecular Operating Environment (MOE) software. Twelve unreported compounds including 4 oximes and 8 oxime ethers were synthesized with benzene, toluene, methoxybenzene and chlorobenzene as initial raw materials. Structures of compounds were elucidated by 1H NMR, 13C NMR and MS. The results of bioactive screening showed that a part of compounds displayed obviously anti-HBV activities. Inhibitory activities of compounds 4B-2 in secretion of HBsAg and HBeAg were IC50 HBsAg=81.15 μmol·L-1, SIHBsAg=9.20 and IC50 HBeAg=90.66 μmol·L-1, SIHBeAg8.24, respectively. Preliminary structure-activity relationship study shows that methyl oxime ethers displayed better anti-HBV activities than the oximes.

Synthesis and anti-HBV activity evaluation of Matijin-Su derivatives with aromatic heterocycles / 中国药科大学学报

@#Hepatitis B virus(HBV)-infected hepatitis is one of the most common infectious disease worldwide. To find novel effective anti-HBV agents, a series of Matijin-Su(MTS)derivatives with aromatic heterocycles were synthesized and evaluated for their anti- HBV activities in HepG2 2. 2. 15 cells. Among them, compounds 7a(IC50=2. 94 μmol/L)and 9a(IC50=2. 21 μmol/L)exhibited more potent inhibitory activity against the replication of HBV DNA in HepG2 2. 2. 15 cells than that of lead compound MTS(IC50=11. 16 μmol/L). Notably, both 7a and 9a displayed a high selective index(SI)of 146. 39 and > 250, respectively, which were also much higher than that of MTS(SI=10. 78). Therefore, compounds 7a and 9a may be promising anti-HBV agents with safety profile for HBV infection.

Research on the determination of molecular weight distribution of anti-HBV placenta transfer factor injection / 中国生化药物杂志

Objective To establish the molecular weight distribution of anti-HBV placenta transfer factor injection (PSTF) by electrophoresis, HPLC and MS.Methods Using the methods of SDS-PAGE, HPSEC, MALDI-TOF-MS to test the molecular of PSTF.Results The Molecular was 8000 Da by SDS-PAGE.There were 5026.67,6783.44,7496.42,8736.55 Da components in PSTF by HPSEC.The main component molecular was 2972 Da and the maximum molecular component was 8194 Da.Conclusion HPSEC is simple and rapid to determine the maximum component molecular of PSTF.

Curative effect of anti-HBV treatment in advanced schistosomiasis patients with ascites and HBV infection / 中国血吸虫病防治杂志

Objective To improve the curative effect of advanced schistosomiasis patients with ascites and HBV infection. Methods A total of 27 advanced schistosomiasis patients with ascites and HBV infection were selected as a trial group and giv?en with anti?HBV treatment and 31 corresponding patients were as the controls and did not received anti?HBV treatment from February 2003 to December 2012. Results The incidence of ascites recurrence spontaneous peritonitis hepatic encephalopa?thy hepatorenal syndrome upper gastrointestinal bleeding and primary liver cancer in the trial group were significantly lower than those in the control group. The detection indexes of liver function renal function and prothrombin time in the trial group were superior to those in the control group. The mortality in the treatment group was also significantly lower than that in the con?trol group. Conclusion The anti?HBV treatment in the advanced schistosomiasis patients with ascites and HBV infection can obviously improve their physical conditions the survival rate and their life qualities.

A new sesquiterpene lactone from the fruits of Illicium henryi / 中国天然药物

AIM@#To study the chemical constituents of the fruits of Illicium henryi.@*METHOD@#Chromatographic separations on silica gel, Sephadex LH-20 gel and MCI gel were used to isolate the compounds. The structures were elucidated based on extensive spectroscopic data analyses.@*RESULTS@#Seven compounds were obtained and their structures were identified as 10-benzoyl-cycloparvifloralone (1), cycloparvifloralone (2), 2α-hydroxycycloparviforalone (3), henrylactone B (4), merrillianone (5), henrylactone C (6) and 7, 14-ortholactone- 3-hydroxyfloridanolide (7).@*CONCLUSION@#Compound 1 is a new sesquiterpene lactone. The tested compounds showed weak anti-HBV activities on HBV surface antigen (HBsAg) secretion and HBV e antigen (HBeAg) secretion using Hep G2.2.15 cell line.

Anti-hepatitis virus constituents from Corydalis saxicola / 中草药

Objective To study the anti-HBV constituents from Corydalis saxola. Methods The constituents were repeatedly purified by column chromatography and were identified on the basis of spectral analysis and comparison of their spectral data with those previously reported. Compounds isolated in large amounts were assayed against HBV. Results Sixteen compounds were identified to be dihydrosanguinarine (1), d-corydaline (2), cavidine (3), stylopine (4), 6-acetonyl-5, 6-dihydrosanguinarine (5), dihydrochelerythrine (6), tetrahydropalmatine (7), adlumidine (8), (-)-salutaridine (9), palmatine (10), protopine (11), berberine (12), coptisine (13), thalifaurine (14), dehydroapocavidine (15), and (+)-magnoflorine (16). Compounds 5, 6, 8-11, 13, and 16 with high amounts were chosen to detect anti-HBV activities. Compounds 5 and 8 were moderately active, compounds 11 and 16 showed weak inhibitory effects, while compound 6 exihibited the most potent activity against HBsAg and HBeAg secretions in HepG 2.2.15 cell line, followed by compound 9. Conclusion Compounds 1, 4-6, 8, 9, 13, 14, and 16 are isolated from C. saxicola for the first time. Compound 10 is the main constituent and compound 6 exihibits the most potent activity against HBV.

Perfil sorológico dos marcadores de hepatite B em profissionais acadêmicos da área da saúde / Serologic profile of hepatitis B markers in professionals academics of the area of the health

O objetivo deste estudo foi avaliar a presença de marcadores sorológicos para hepatite B em profissionais acadêmicos da área da saúde, assim como a situação vacinal destes acadêmicos. Participaram da pesquisa 50 profissionais acadêmicos da área da saúde. As amostras foram identificadas e estocadas até a realização dos testes. Realizou-se através de ensaio imunoenzimático a detecção dos seguintes marcadores HBsAg, anti HBc e anti HBs. Os dados analisados mostraram que 28% foram reagentes para o HBsAg e 72% não reagentes. Quanto ao anti HBc, 98% foram não reagentes e 2% mostraram reagentes. Em relação ao anti HBs, 48% mostraram positividade enquanto 52% foram não regentes. Observou-se qua a grande maioria dos acad~emicos foi vacinada (80%), e 20% nunca receberam a vacina. A imunogênese anti HBs (+) completou-se em 57, 5% dos vacinados, entretanto 42,5% dos participantes que foram vacinados apresentaram anti HBs (-). Baseados nestes resultados, conclui-se que a campanha de vacinação e implantação de medidas profiláticas devem ser intensificadas, bem como a realização de triagem sorológica para hepatite B dos profissionais da área da saúde para confirmação da imunização, visando à prevenção e controle da infecção pelo HBV nestes profissionais.

Tea Polyphenols Exerts Anti-hepatitis B Virus Effects in a Stably HBV-transfected Cell Line / 华中科技大学学报（医学）（英德文版）

In this study,the anti-HBV effects of tea polyphenols (TP) were examined.After cells were exposed to TP for 3,6,9 days,amounts of HBsAg,HBeAg and HBV-DNA released into the supernatant of the cultured HepG2 2.2.15 cells were detected.TP,to some extent,inhibited the secre-tion of HBsAg and strongly suppressed the secretion of HBeAg in a dose-dependent (P<0.01) and time-dependent manner,with 50% maximal inhibitory concentration (IC50) value being 7.34 μg/mL on the 9th day,but the time-dependence was not significant (P=0.051).Expression of HBV-DNA in the supernatant of the cell culture also was significantly decreased in a dose-dependent fashion (P<0.01).The IC50 of TP in inhibiting HBV DNA was 2.54 μg/mL.It concluded that TP possessed potential anti-HBV effects and may be used as a treatment alternative for HBV infection.

Anti-Hepatitis B Virus Drugs in Clinical and Preclinical Development / 中国病毒学·英文版

Up to date, there are two types of drugs approved to treat hepatitis B: interferons and nucleos (t) ide analogues. However, the therapies are limited in the clinical context because of the negative side effects of interferon-α and the development of substantial viral resistance to nucleos (t) idic inhibitors. Therefore, new drugs with novel structures and mechanisms are needed. In this article, the drugs approved by FDA or the European Commission for treating chronic hepatitis B virus infection, as well as those under clinical trials, and several compounds in preclinical studies are reviewed. Additionally, some potential targets and strategies to combat chronic hepatitis B virus infection are discussed.

Cloning, Eukaryotic Expression of Human ISG20 and Preliminary Study on the Effect of Its Anti-HBV / 华中科技大学学报（医学）（英德文版）

Human ISG20 gene was cloned and the effect of its anti-HBV was primarily studied. The ISG20 gene was amplified from HeLa cells by RT-PCR and recombinant vector expressing ISG20 was constructed by genetic engineering. The overexpression of ISG20 in HepG2 cells was detected by Western blot and the levels of secretion of HBs antigen and HBe antigen tested by ELISA. The results showed that: (1) Sequence of ISG20 cloned was consistent to that published in Genebank; (2) Recombinant vector expressing ISG20 could be expressed in HepG2 cells by transfection; (3) The overexpression of ISG20 protein could reduce the levels of the secretion of HBs antigen and HBe an-tigen in transfected HepG2 cells. It was suggested that the overexpression of recombinant ISG20 in culture cells could reduce the synthesis of HBV proteins.

Efficacy of the intervention with anti-HBV immunoglobulin and hepatitis B vaccination within 24 hours after birth for neonates in Hanoi

Background: Previous studies showed that B hepatitis prevalence in Vietnam was very high and the rate of mother-to-child transmission was range from 44.7% to 45.2%. Objectives: Study on the efficacies of the interventional methods with anti-HBV immunoglobulin and hepatitis B vaccination within 24 hours after birth for neonates in Hanoi. Subjects and method: This interventional study was carried out on 163 neonates of positive-HBsAg mothers who were admitted to Hanoi Obstetrical Hospital from 6/2005 to 3/2007. These neonates received anti-HBV immunoglobulin and hepatitis B vaccination within 24 hours after birth, then were followed up for 11 to 18 months. Results: Among these 163 neonates that received interventions, there were 135 neonates that underwent HBsAg tests after 11 to 18 months. The results showed that only one newborn baby had positive HBsAg (0.74%) and 134 neonates with non-HBV (99.26%). 81.5% of neonates had hepatitis B surface antibody that can protect against HBV. Conclusion: Early interventions with anti-HBV immunoglobulin and HBV vaccination were effective in preventing HBV for neonates of positive-HBsAg mothers.

The Therapeutic Effect of Anti-HBV Placenta Transfer Factor Injection on liver Cirrhosis Resulting from Chronic Hepatitis B / 医学研究杂志

Objective To observe the therapeutic effect of anti-HBV placenta transfer factor injection to liver cirrhosis.Methods 193 cases of liver cirrhosis resulting from chronic hepatitis B are administrated anti-HBV placenta transfer factor.The main clinical symptoms and signs(weakness,hepatalgia,hepatosplenomegaly),the biochemical markers such as liver function(ALT,AST,serum total protein,albumin,total bilirubin,A/G),blood routine,fibrosis markers(HA、LN、PⅢP、PIVP),and serum protein electrophoresis before and after 24 weeks treatment were analysed.Results The main clinical symptoms and signs,liver function,blood routine,fibrosis markers,serum protein electrophoresis were significantly improved after 24 weeks of treatment.(P

The inhibitory effect of oxymatrine on hepatitis B virus in vitro / 中华消化杂志

Objective To study the inhibitory effect of oxymatrine on hepatitis B virus(HBV) in vitro. Methods Microparticle enzyme immunoassay, bDNA signal amplification assay was used for determining secrected HBsAg/HBeAg in the culture medium, HBV DNA from core particles in the cytoplasm and MTT colorimetric assay was used to assay the oxymatrine cytotoxity. Results The inhibitory rates of HBsAg and HBeAg were 40.57% and 48.27% by oxymatrine at the concentration of 2 000 ?g/ml. At 100～2 000 ?g/ml, it can remarkably decrease the level of viral core associated HBV DNA in the cytoplasm. No significant toxicity was shown in such concentrations. Conclusion Oxymatrine has a potential anti HBV activity in vitro.