Each of Keggin type heteropolytungstosilicic and heteropolytungstogermanic acids reacted with 8-quinolinol, p-aminodimethylaniline and pyridine, respectively, yielding six charge trans- fer heteropolycomplexes (CTHPC...Each of Keggin type heteropolytungstosilicic and heteropolytungstogermanic acids reacted with 8-quinolinol, p-aminodimethylaniline and pyridine, respectively, yielding six charge trans- fer heteropolycomplexes (CTHPCs), which were purified and characterized by elemental analy- sis, IR, UV and 183W NMR. The anti-HIV-1 activities of CTHPCs were evaluated by ELISA of HIV-P24 antigen. The toxicity against MT-4 cells was measured by MTT. The results show that median inhibitory concentration (IC50) for each CTHPC to inhibit HIV-P24 antigen in cell culture was lower than 5 μg/mL, while median toxicity concentration (IC50) against MT-4 cells was higher than 268 μg/mL. The following mechanisms might be considered for their anti-HIV- 1 activity, namely, (1) inhibiting the penetration of HIV- 1 virus into target cells for it can blockade CD4 receptor of MT-4 cells and (2) inhibition of syncytium formation.展开更多
A series of novel 6-sulfamoyl-4-oxoquinoline-3-carboxylic acids derivatives have been synthesized and screened for HIV integrase inhibition activity. Their structures were confirmed by ESI-MS, ^1H NMR and ^13C NMR. 2...A series of novel 6-sulfamoyl-4-oxoquinoline-3-carboxylic acids derivatives have been synthesized and screened for HIV integrase inhibition activity. Their structures were confirmed by ESI-MS, ^1H NMR and ^13C NMR. 2009 Li Ming Hu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.展开更多
Anti-HIV agent (±)-calanolide A has been synthesized by a four-step approach startingfrom phloroglucinol, including the Pechmann reaction, Friedel-Crafts acylation, cyclization,chromenylation and Luche reduction.
HIV/AIDS is one of the most serious public health challenges globally. Despite the great efforts that are being devoted to prevent,treat and to better understand the disease,it is one of the main causes of morbidity a...HIV/AIDS is one of the most serious public health challenges globally. Despite the great efforts that are being devoted to prevent,treat and to better understand the disease,it is one of the main causes of morbidity and mortality worldwide. Currently,there are 30 drugs or combinations of drugs approved by FDA. Because of the side-effects,price and drug resistance,it is essential to discover new targets,to develop new technology and to find new anti-HIV drugs. This review summarizes the major targets and assays currently used in anti-HIV drug screening.展开更多
Objective To investigate the inhibitory effect of the mycelium extract from a Chinese fungus （MI） on HIV-I and its mode of action. Methods Several in vitro methods including time of action, time of addition and PCR ...Objective To investigate the inhibitory effect of the mycelium extract from a Chinese fungus （MI） on HIV-I and its mode of action. Methods Several in vitro methods including time of action, time of addition and PCR were used to test the mode of action of M 1. Results M 1 inhibited acute HIV infection in vitro and was effective when it was added 12 h after infection. PCR analysis of infected cells demonstrated that MI delayed the appearance of late product of reverse transcription and HIV was blocked before its RNA expression. Conclusion The target of M 1 is post-integration of proviral DNA.展开更多
To further explore the potential of DCK analogs as anti-HIV drug candidates, ten new tri-substituted （3＇R,4＇R）-3＇,4＇-di-O-（S）-camphanoyl-（＋）-cis-khellactone （DCK） derivatives （4-13） were designed, synth...To further explore the potential of DCK analogs as anti-HIV drug candidates, ten new tri-substituted （3＇R,4＇R）-3＇,4＇-di-O-（S）-camphanoyl-（＋）-cis-khellactone （DCK） derivatives （4-13） were designed, synthesized, and evaluated against HIV replication in MT4 cells and H9 lympho- cytes.展开更多
MTT Cell Proliferation Assay was used to optimize the concentration of Telomerase Restrictors（TRs） with minimum toxicity to the selected cells. FACSort flow cytometer and Innotest P24 HIV（Human immtmodeficiency Vi...MTT Cell Proliferation Assay was used to optimize the concentration of Telomerase Restrictors（TRs） with minimum toxicity to the selected cells. FACSort flow cytometer and Innotest P24 HIV（Human immtmodeficiency Virus） antigen mAb ELISA Kit were used to investigate the anti-HIV-1 activities of TRs. The results showed that TRs had low cytotoxicity to the PBMC （Peripheral Blood mononuclear cells） and CEM/GFP if the concentration of TRs was at 50μmol/L or below, and the supernatant from PBMC pretreated with SHIV and TR1-001 /TR1-002 could not infect the PBMC, while can infect the C8166 with reduced infectivity, which suggested that the TRs may be one of the novel resources for screening anti-HIV-1 agents.展开更多
Introduction: Human immunodeficiency virus (HIV) infection is a public health problem of concern. Anti-retroviral therapy (ART) is associated with multiple side effects. This study aimed at identifying the different h...Introduction: Human immunodeficiency virus (HIV) infection is a public health problem of concern. Anti-retroviral therapy (ART) is associated with multiple side effects. This study aimed at identifying the different hepatic manifestations of antiretroviral therapy and the responsible molecules. Patients and Methods: This was an eight months period prospective descriptive study, from January 1st to August 31st, 2015, conducted in the Department of Gastroenterology and Internal Medicine at the Brazzaville University Teaching Hospital. Study participants were treatment-na?ve HIV patients who were initiated on ART treatment during the study period. Patients with liver disease, liver cytolysis prior to initiation of therapy, and those with alternative therapy that may cause hepatotoxicity were excluded. The sample size was 110 patients. Results: The age was ranging from 25 to 70 years with a mean age of 47.5 ± 7.5 years. During the six months of follow-up, the alarming hepatic signs were observed in 26.36% of cases (n = 29) in the 3rd month of treatment. There was no observed alarming sign in the 6th month of follow-up. The cytolytic pattern was observed in 54.55% of cases (n = 60) in the 3rd month. The cholestatic pattern was observed in 6.36% of cases (n = 7) in the 3rd month. Triple therapy combination of Zidovudine, Lamivudine and Nevirapine (AZT + 3TC + NVP) was the most used in 57.27% (n = 63) with a statistically significant p value to the occurrence of cytolytic pattern (p Conclusion: Drug induced liver toxicity occurs in a significant number of patients starting ART. The prevalence of hepatic events was high at the third month of treatment and the triple therapy of Zidovudine, Lamivudine and Nevirapine (AZT + 3TC + NVP) was the most incriminated.展开更多
PLHIV have decreased economic productivity both due to direct and indirect causes. Data from developed countries have shown that at the societal level, high costs ART are offset by increased productivity. We hypothesi...PLHIV have decreased economic productivity both due to direct and indirect causes. Data from developed countries have shown that at the societal level, high costs ART are offset by increased productivity. We hypothesized that post-ART the SES would improve regardless of the baseline SES and will be sustained over time. Our objective was to perform a comprehensive SES evaluation pre/post ART initiation using an ambispective cohort study design. We used Indian household-specific SES validated tool, with score of 76 being affluent, along with clinical, ART adherence data at median of 6 and 18 months post ART, and compared using paired t-tests. Among 140 persons started on ART, with a median follow up of 22 months, 118 had Pre-ART SES data, of these: 57% were women;median age was 38 years;67% were married;89 (78%) had heterosexual sex as HIV risk;40 (34%) had major OI and/or TB at presentation. Reported self-occupation was: skilled labourers 41 (35%);12 (10%) unskilled labourers;27 (23%) housewives;26 (22%) pro-fessionals/blue collar job;1 student, 10 unemployed. The median pre-post ART CD4 cell counts were: 187 and 454 cells/cumm (P < 0.01);median body weight pre-post ART was 54 and 57 kg (P < 0.01);97% of the participants were 100% adherent. The mean Pre-ART total SES score was 37.06 (+/-10.2);and Post-ART SES score 40.62 (+10.1 P < 0.001) and these results were sustained over time and remained significant even when only monthly income was considered. Our data show a significant impact of ART on SES in a sustained manner in a developing world setting, which has policy level implications.展开更多
合成了Keggin结构钨硅、钨锗、钨磷、钨砷两电子及四电子稀土钐盐杂多蓝，铈量滴定及元素分析方法确定了化合物的还原电子数及化学组成，采用 IR，UV－Vis，183 W NMR和ESR等对其结构进行了表征．在人T淋巴细胞 MT－4内，对合成的化合...合成了Keggin结构钨硅、钨锗、钨磷、钨砷两电子及四电子稀土钐盐杂多蓝，铈量滴定及元素分析方法确定了化合物的还原电子数及化学组成，采用 IR，UV－Vis，183 W NMR和ESR等对其结构进行了表征．在人T淋巴细胞 MT－4内，对合成的化合物进行了系统的抗艾滋病毒（HIV-1）活性及毒性测定．发现Keggin结构钨硅、钨锗四电子稀土钐盐杂多蓝具有较强的抗HIV-1活性，其中钨锗酸钐四电子杂多蓝（代号HPBR－2）具有较高的治疗指数．展开更多
文摘Each of Keggin type heteropolytungstosilicic and heteropolytungstogermanic acids reacted with 8-quinolinol, p-aminodimethylaniline and pyridine, respectively, yielding six charge trans- fer heteropolycomplexes (CTHPCs), which were purified and characterized by elemental analy- sis, IR, UV and 183W NMR. The anti-HIV-1 activities of CTHPCs were evaluated by ELISA of HIV-P24 antigen. The toxicity against MT-4 cells was measured by MTT. The results show that median inhibitory concentration (IC50) for each CTHPC to inhibit HIV-P24 antigen in cell culture was lower than 5 μg/mL, while median toxicity concentration (IC50) against MT-4 cells was higher than 268 μg/mL. The following mechanisms might be considered for their anti-HIV- 1 activity, namely, (1) inhibiting the penetration of HIV- 1 virus into target cells for it can blockade CD4 receptor of MT-4 cells and (2) inhibition of syncytium formation.
基金the financial supports of the National Basic Research Program(No.2009CB930200)the Fund from Beijing City Education Committee(No.KM200610005029)Funding Project for Academic Human Resources Development in Institutions of Higher Learning Under the Jurisdiction of Beijing Municipality.
文摘A series of novel 6-sulfamoyl-4-oxoquinoline-3-carboxylic acids derivatives have been synthesized and screened for HIV integrase inhibition activity. Their structures were confirmed by ESI-MS, ^1H NMR and ^13C NMR. 2009 Li Ming Hu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
文摘Anti-HIV agent (±)-calanolide A has been synthesized by a four-step approach startingfrom phloroglucinol, including the Pechmann reaction, Friedel-Crafts acylation, cyclization,chromenylation and Luche reduction.
文摘HIV/AIDS is one of the most serious public health challenges globally. Despite the great efforts that are being devoted to prevent,treat and to better understand the disease,it is one of the main causes of morbidity and mortality worldwide. Currently,there are 30 drugs or combinations of drugs approved by FDA. Because of the side-effects,price and drug resistance,it is essential to discover new targets,to develop new technology and to find new anti-HIV drugs. This review summarizes the major targets and assays currently used in anti-HIV drug screening.
基金This project was supported by National Medicine Science Foundation during the 10th-five year plan period (2001BA705B01) and Chinese National Science Fund for Outstanding Youths (30325047).
文摘Objective To investigate the inhibitory effect of the mycelium extract from a Chinese fungus （MI） on HIV-I and its mode of action. Methods Several in vitro methods including time of action, time of addition and PCR were used to test the mode of action of M 1. Results M 1 inhibited acute HIV infection in vitro and was effective when it was added 12 h after infection. PCR analysis of infected cells demonstrated that MI delayed the appearance of late product of reverse transcription and HIV was blocked before its RNA expression. Conclusion The target of M 1 is post-integration of proviral DNA.
文摘To further explore the potential of DCK analogs as anti-HIV drug candidates, ten new tri-substituted （3＇R,4＇R）-3＇,4＇-di-O-（S）-camphanoyl-（＋）-cis-khellactone （DCK） derivatives （4-13） were designed, synthesized, and evaluated against HIV replication in MT4 cells and H9 lympho- cytes.
基金Supported by China Scholarship Counsil(CSC) and Wuhan Chenguang Program of Wuhan City (2003002016-24)
文摘MTT Cell Proliferation Assay was used to optimize the concentration of Telomerase Restrictors（TRs） with minimum toxicity to the selected cells. FACSort flow cytometer and Innotest P24 HIV（Human immtmodeficiency Virus） antigen mAb ELISA Kit were used to investigate the anti-HIV-1 activities of TRs. The results showed that TRs had low cytotoxicity to the PBMC （Peripheral Blood mononuclear cells） and CEM/GFP if the concentration of TRs was at 50μmol/L or below, and the supernatant from PBMC pretreated with SHIV and TR1-001 /TR1-002 could not infect the PBMC, while can infect the C8166 with reduced infectivity, which suggested that the TRs may be one of the novel resources for screening anti-HIV-1 agents.
文摘Introduction: Human immunodeficiency virus (HIV) infection is a public health problem of concern. Anti-retroviral therapy (ART) is associated with multiple side effects. This study aimed at identifying the different hepatic manifestations of antiretroviral therapy and the responsible molecules. Patients and Methods: This was an eight months period prospective descriptive study, from January 1st to August 31st, 2015, conducted in the Department of Gastroenterology and Internal Medicine at the Brazzaville University Teaching Hospital. Study participants were treatment-na?ve HIV patients who were initiated on ART treatment during the study period. Patients with liver disease, liver cytolysis prior to initiation of therapy, and those with alternative therapy that may cause hepatotoxicity were excluded. The sample size was 110 patients. Results: The age was ranging from 25 to 70 years with a mean age of 47.5 ± 7.5 years. During the six months of follow-up, the alarming hepatic signs were observed in 26.36% of cases (n = 29) in the 3rd month of treatment. There was no observed alarming sign in the 6th month of follow-up. The cytolytic pattern was observed in 54.55% of cases (n = 60) in the 3rd month. The cholestatic pattern was observed in 6.36% of cases (n = 7) in the 3rd month. Triple therapy combination of Zidovudine, Lamivudine and Nevirapine (AZT + 3TC + NVP) was the most used in 57.27% (n = 63) with a statistically significant p value to the occurrence of cytolytic pattern (p Conclusion: Drug induced liver toxicity occurs in a significant number of patients starting ART. The prevalence of hepatic events was high at the third month of treatment and the triple therapy of Zidovudine, Lamivudine and Nevirapine (AZT + 3TC + NVP) was the most incriminated.
文摘PLHIV have decreased economic productivity both due to direct and indirect causes. Data from developed countries have shown that at the societal level, high costs ART are offset by increased productivity. We hypothesized that post-ART the SES would improve regardless of the baseline SES and will be sustained over time. Our objective was to perform a comprehensive SES evaluation pre/post ART initiation using an ambispective cohort study design. We used Indian household-specific SES validated tool, with score of 76 being affluent, along with clinical, ART adherence data at median of 6 and 18 months post ART, and compared using paired t-tests. Among 140 persons started on ART, with a median follow up of 22 months, 118 had Pre-ART SES data, of these: 57% were women;median age was 38 years;67% were married;89 (78%) had heterosexual sex as HIV risk;40 (34%) had major OI and/or TB at presentation. Reported self-occupation was: skilled labourers 41 (35%);12 (10%) unskilled labourers;27 (23%) housewives;26 (22%) pro-fessionals/blue collar job;1 student, 10 unemployed. The median pre-post ART CD4 cell counts were: 187 and 454 cells/cumm (P < 0.01);median body weight pre-post ART was 54 and 57 kg (P < 0.01);97% of the participants were 100% adherent. The mean Pre-ART total SES score was 37.06 (+/-10.2);and Post-ART SES score 40.62 (+10.1 P < 0.001) and these results were sustained over time and remained significant even when only monthly income was considered. Our data show a significant impact of ART on SES in a sustained manner in a developing world setting, which has policy level implications.
文摘合成了Keggin结构钨硅、钨锗、钨磷、钨砷两电子及四电子稀土钐盐杂多蓝，铈量滴定及元素分析方法确定了化合物的还原电子数及化学组成，采用 IR，UV－Vis，183 W NMR和ESR等对其结构进行了表征．在人T淋巴细胞 MT－4内，对合成的化合物进行了系统的抗艾滋病毒（HIV-1）活性及毒性测定．发现Keggin结构钨硅、钨锗四电子稀土钐盐杂多蓝具有较强的抗HIV-1活性，其中钨锗酸钐四电子杂多蓝（代号HPBR－2）具有较高的治疗指数．
