Syntheses, Characterization and Anti-HIVActivity of Charge TransferHeteropolycomplexes

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.

Total Synthesis of (±)-Calanolide A and Its Anti-HIV Activity

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.

Anti-HIV-1 Activities of 4 Telomerase Restrictors

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.

Synthesis and Anti-HIV Activity of Trisubstituted (3′R, 4′R)-3′,4′- Di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) Analogs

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.

Therapeutic Potential of Anti-HIV RNA-loaded Exosomes

Highly active antiretroviral therapy（HAART）is used globally and has significantly reduced the morbidity,mortality,and transmission of human immunodeficiency virus（HIV）-related illness.However,the attendant shortcomings such as toxic side effects,necessity of life-long therapy that is expensive, and inefficiency in eradicating latent viral infections have greatly limited the application of HAART.

In Vitro Anti-HIV Activity of a Chinese Fungus Extract

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.

Anti-HIV ELISA试剂间接法与双抗原夹心法的比较

由于艾滋病目前既无疫苗预防又缺乏有效的治疗手段,使艾滋病在全球范围内迅速蔓延,这就使诊断艾滋病的试剂质量水平显得尤为重要.一个好的方法首先要考虑简单、快速、准确.笔者试用国产第三代HIV酶免检测试剂盒,一段时间后,认为其有很大优势,完全能替代目前一直延用的间接法酶免试剂.

Synthesis of 6-sulfamoyl-4-oxoquinoline-3-carboxylic acid derivatives as integrase antagonists with anti-HIV activity

一系列新奇 6-sulfamoyl-4-oxoquinoline-3-carboxylic 酸衍生物为 HIV integrase 抑制活动被综合了并且屏蔽。他们的结构被 ESIMS 证实， 1 H NMR 和 13 C NMR。

Current Status of Targets and Assays for Anti-HIV Drug Screening

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.

Synthesis and anti-HIV-1 activity of the conjugates of gossypol with oligopeptides and D-glucosamine

A series of novel gossypol derivatives were synthesized and screened for their in vitro anti-HIV- 1I activity. The results showed that replacing the aldehyde groups of gossypol with certain oligopeptides and Dglucosamine not only reduced the cytotoxicity of gossypol derivatives but also enhanced their antiviral activity against HIV-1. Interestingly, D-glucosamine derivative of gossypol that lacked the COONa group also exhibited the same potent anti-HIV-1 activity as oligopeptide derivatives with the COONa group. These compounds blocked the entry of HIV-1ⅢB into target cell. which was similar to T20. Furthermore, the molecular docking analysis rationalized their anti-HIV-1 activity. The results also implied that certain oligopeptides and D-glucosamine were important moities to prepare gossypol derivatives as HIV- 1 entry inhibitors besides certain amino acids.

Synthesis and Anti-HIV Activity of a Series of 6-Modified 2＇,3＇-Dideoxyguanosine and 2＇,3＇-Didehydro-2＇,3＇- dideoxyguanosine Analogs

In search of potential 2＇,3＇-dideoxyguanosine （ddG） and 2＇,3＇-didehydro-2＇,3＇-dideoxyguanosine （D4G） prodrugs, a series of 6-modified ddG, D4G analogs were synthesized and evaluated for their anti-HIV activities and cyto- toxities in cell-based assays. All analogs showed low cytotoxieities and some of them displayed benign anti-HIV activities. The active triphosphate forms in vivo, ddGTP and D4TTP, were also synthesized by a novel and facile ＂one-pot＂ method. The recognition of ddGTP and D4TTP by Taq, Therminater DNA polymerase and HIV reverse transcriptase （RT） incorporated in DNA/RNA strands were investigated by a non-radioactivity method and Km were determined.

Anti-HIV lignans from Justicia procumbens

Twenty-one lignans including three new ones(1, 2 and 13) were isolated from Justicia procumbens. The chemical structures of the new lignans were determined by spectroscopic means including 1 D and 2 D NMR analysis. These compounds were evaluated for their cytotoxic and anti-HIV activities. The new secoisolariciresinol dimethyl ether acetate(13) exhibited anti-HIV-1 activity with an IC50 value of 5.27 μmol·L^-1 and a selective index(SI) value of 2.2. The known arylnaphthalene lignan procumbenoside A(3) and diphyllin(8) demonstrated inhibitory activity against HIV-1 with IC50 values of 4.95(SI > 6.2) and 0.38 μmol·L^-1(SI = 5.3), respectively.

Insight into the deamination mechanism of 6-cyclopropylamino guanosine analogs for anti-HIV drug design

Deamination is a crucial step in the transformation of 6-cyclopropylamino guanosine prodrug to its active form. A convenient method using capillary electrophoresis （CE） without sample labeling was developed to analyze the deamination of a series of D-/L-6-cyclopropylamino guanosine analogs by mouse liver homogenate, mouse liver microsome, and adenosine deaminase （ADA）. A two-step process involving a 6-amino guanosine intermediate formed by oxidative N-dealkylation was demonstrated in the metabolism of 6-cyclopropylamino guanosine to 6-hydroxy guanosine. The results indicated that the transformation rates of different prodrugs to the active form varied greatly, which were closely correlated with the configuration of nucleosides and the structure of glycosyl groups. Most importantly, D-form analogs were metabolized much faster than their L-counterparts, thus clearly pointed out that compared to guanine, modification of glycosyl part might be a better choice for the development of L-Kuanosine analogs for the treatment of HIV,

Neamine-heterocycle conjugates as potential anti-HIV agents

A series of neamine-heterocycle conjugates were designed and synthesized. All new compounds displayed more potent inhibitory effect on HIV replication than neamine, among them two compounds displayed stronger anti-HIV activity than neomycin B. The results suggested that it might be a promising approach to modify neamine for the discovery of new anti-HIV agents.

泉州口岸1991-1997年Anti-HIV检测结果报告

本文报告了泉州卫生检疫局从1991—1997年艾滋病的监测结果。7年共检测标本41615份,检出阳性4份,其中2例船员,1例外籍人员,1例外籍人员配偶。对外籍人员及回国人员提出艾滋病的预防措施。

Synthesis and biological evaluation of andrographolide derivatives as potent anti-HIV agents

一系列 Andro 衍生物在 vitro 为他们的 anti-HIV 活动被描述并且评估。化合物 10 并且 16b， TI 是 > 10，在 vitro 举办了某 anti-HIV-1 活动。在那里，加重 10 它是最好的有势力混合物，能为反爱滋病代理人的进一步的开发担任新领先。

非HIV马尔尼菲篮状菌病免疫相关易感因素分析

目的 对HIV阴性的马尔尼菲篮状菌病(TSM)患者的免疫相关易感因素进行分析,以提高临床医师对这一疾病的认识和管理。方法 前瞻性研究本课题组收集的来自广西及国内其他省市2012年至2021年确诊为HIV阴性的TSM患者临床特点,分析其免疫相关易感因素。结果 纳入患者154例,132例检出免疫缺陷。儿童患者以原发性免疫缺陷病为主;成人患者以抗伽马干扰素自身抗体相关的免疫缺陷综合征为主,其余包括合并恶性肿瘤及结缔组织病等基础病。结论TSM可发生于存在不同形式免疫缺陷的非HIV患者,应基于易感因素建立完整的免疫状态评估策略,以改善患者预后。