Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0019693 (HIV)
 170,526 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Various polyoxometalates proved inhibitory to the replication of a number of enveloped DNA and RNA viruses, i.e., herpesviruses (herpes simplex and cytomegalo), togaviruses (Sindbis), paramyxoviruses (respiratory syncytial), rhabdoviruses (vesicular stomatitis), arenaviruses (Junin and Tacaribe), and retroviruses [human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2), simian immunodeficiency virus, and murine sarcoma virus]. The most potent compounds, i.e., JM1590 [K13[Ce(SiW11O39)2]. 26H2O] and JM2766 [K6[BGa(H2O)W11O39]. 15H2O], inhibited HIV-1 and simian immunodeficiency virus at concentrations as low as 0.008-0.8 microM. The polyoxometalates also inhibited giant cell formation in co-cultures of HIV-infected HUT-78 cells and uninfected MOLT-4 cells. Studies designed to unravel the mechanism of action of these compounds revealed that they inhibit the reverse transcriptase activity associated with HIV. The polyoxometalates also proved inhibitory to the binding of HIV-1 virions to the cells. From "time of addition" experiments, whereby the polyoxometalates were added at different times after virus infection, their mechanism of anti-HIV action could be attributed to inhibition of virus-cell binding. There was a good correlation (r = 0.84) between the inhibitory effects of the compounds on HIV-1-induced cytopathicity and their inhibitory effects on syncytium formation and a close correlation (r = 0.902) between their inhibitory effects on syncytium formation and their interaction with gp120, whereas there was no correlation between their anti-HIV-1 activity and their inhibitory effects on HIV-1 reverse transcriptase. In flow cytometric studies, the compounds did not interfere with the binding of OKT4A/Leu-3a monoclonal antibody to the CD4 receptor of uninfected cells, but they inhibited binding of anti-gp120 monoclonal antibody to HIV-1-infected cells. Thus, the binding of the polyoxometalates to the viral envelope glycoprotein gp120 is responsible for their anti-HIV activity.
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PMID:Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents. 128 64

India has launched a liberalization of its economy with restructuring, privatization, and increased imports in order to achieve higher economic performance. This drive also affected the pharmaceutical industry and drug distribution, but in a negative manner. In the 1980s there were 9000 drug manufacturers that together produced up to 60,000 different preparations. In 1992, only 20,000 drugs were produced. The Voluntary Health Organization of India (VHAI) has fought for 10 years for a rational policy on medicines to halt the production of worthless or outright harmful products. For instance, anabolic steroids are sold as nutritional supplements to children, and the banned clioquinol is regularly used against diarrhea despite an international boycott. In recent years unscrupulous manufacturers have sold contaminated water as glucose for infusion bags and anti-D-immunoglobulin which was contaminated with HIV-infected blood. In northern India, a criminal organization bought up used cannulas from hospitals and repacked them for resale as new supplies. While a new medicine policy is formulated, there is a serious shortage of life-saving drugs such as insulin and rifampicin. In the last years, prices have exploded as some products have become six times more expensive. The whole national health system has undergone cost cuts to comply with an ultimatum from the World Bank and the International Monetary Fund; otherwise, sorely needed dollar loans would not be forthcoming. Funds for fighting tuberculosis and malaria have been trimmed, although AIDS and family planning budgets have been increased. One-fourth of the state health expenditures go to combat AIDS, since about 1 million people are infected with HIV. The pharmaceutical industry has also been embroiled in a patent protection wrangle with American drug exporters who claim that Retrovir or AZT (developed by Burroughs Wellcome) was pirated by the Cipla firm, whereas Cipla countered that it was ferreted out from scientific journals.
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PMID:[India: an expensive and dangerous drug]. 130 Jun 63

HIV infection develops not only to AIDS, but it is also a leading risk factor for the development of many other infectious diseases due to the depletion of T lymphocytes such as the interrelated prevalence of tuberculosis (TB) and AIDS. Surveillance conducted in the 1988-1989 in the US and other recent studies found a serious epidemiological relation. Thailand has an endemic disease, melioidosis, caused by P. pseudomallei living in environmental soil and water. The disease takes various clinical types; localized, systemic, acute, subacute, chronic, and inapparent; presenting symptoms undistinguishable from many other infectious diseases. Pulmonary melioidosis shows a clinical feature similar to lung tuberculosis which occurs more easily in the individuals of impaired immunity, such as diabetes patients. According to available literatures, one case of recurrent melioidosis has been reported in Thailand as a complication of AIDS. The patient was a German homosexual male who had been living in the country for more than 10 years and showed a fatal course with interstitial pneumonitis. Ubon Ratchathani province, Thailand, is an area endemic for both TB and melioidosis, as well as a major supplier of laborers to Bangkok. A preliminary survey was conducted for the prevalence of HIV infections in pulmonary TB and melioidosis patients in Ubon Ratchathani province. TB was found to be prevalent in the province to a greater extent than in most other provinces and melioidosis is endemic. Four individuals were found to be HIV-seropositive amid a total 551 suspected and culture-positive cases of pulmonary TB, while no HIV-seropositive case was found among 121 melioidosis patients. In view of the rapidly expanding HIV-infections in Thailand, careful attention will have to be given to the future epidemiological status of HIV infection in TB patients.
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PMID:A preliminary survey for human immunodeficient virus (HIV) infections in tuberculosis and melioidosis patients in Ubon Ratchathani, Thailand. 130 71

The synthesis of a novel series of lipophilic prodrug derivatives of the anti-HIV drugs 2',3'-dideoxycytidine (ddC, 1) and 3'-fluoro-ddC (2), involving N4-substitution with (N,N-dialkylamino)methylene side chains, is described. The increase in the partition coefficients for the prodrug series, compared to those of the parent drugs 1 and 2, ranged from 1.5- to 122-fold and from 1.6- to 175-fold, respectively. At pH 7.4, 37 degrees C, the hydrolytic t1/2 values ranged from 2 to 52 h, the diisopropyl derivatives (3d and 4d) being most stable in the series. 3d and 4d were greater than or equal to 4-fold and 1.7-fold more soluble in water than 1 and 2, respectively. The in vitro antiretroviral activities of 3d, 4a, and 4d were evaluated; the results indicate efficient prodrug-to-drug conversion under the assay conditions. The results of this investigation demonstrate that it is indeed feasible to chemically modify certain nucleoside analogues with inferior solubility properties to simultaneously achieve significantly enhanced lipid and water solubility.
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PMID:Highly water-soluble lipophilic prodrugs of the anti-HIV nucleoside analogue 2',3'-dideoxycytidine and its 3'-fluoro derivative. 131 21

Direct condensation of 2-deoxy-D-ribose (1) with mercaptans using the P4O10/H2O/Bu3N reagent in chloroform resulted in coupling at C-3 to give the anomeric mixtures of the corresponding pentopyranoses 2 and pentofuranoses 3. After acetylation with acetic anhydride in dry pyridine of these 3-alkylthio pentofuranoses, coupling with the nucleobases uracil, thymine, and cytosine in accordance with the Friedel-Crafts catalyzed silyl Hilbert-Johnson method yielded the acetylated D-erythro nucleosides 7 as anomeric mixtures, separable only by means of chromatography either before or after deprotection with ammonia. The nucleosides 8a-e were devoid of any activity against HSV-1 and HIV-1.
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PMID:Synthesis of 3'-alkylthio-2',3'-dideoxy nucleosides with potential anti-HIV activity from 2-deoxy-D-ribose, using a phosphorus pentoxide reagent. 133 47

Bangkok, the capital of Thailand, is a large city of about six million people. According to the rapid growth of economy, Bangkok faces to the problems of urbanization and industrialization. Non-communicable disease such as cardiovascular diseases, cancers are the leading causes of death. There is a trend of increasing air pollution in the congested areas and industrialized zones, with the increase over the ambient air quality standard involving suspended particulate matter. Other public health problems include the sanitation of restaurants, the quality of drinking water and coloring agents in food, drug addiction especially in young males. Poor hygiene in drug injection is one of the major causes of HIV transmission. AIDS, originally our imported disease, needs urgent prevention by health education and counseling. Improvements in government and non-government health care resources are still needed. A good cooperative city health plan serves a practical purpose, especially for the solution of the air and water pollution in Bangkok. However, pilot operational research on nutrition, health and environment in relation to city health planning needs to be discussed further for more effective implementation.
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PMID:Nutrition and the environmental situation in Bangkok. 134 57

The synthesis, chemistry, biochemistry, and anti-HIV activity of a series of 1-(2,3-dideoxy-2-fluoro-beta-D-threopentofuranosyl)pyrimidines have been studied in an attempt to find useful anti-AIDS drugs. Synthesis is carried out via a 2,3-dideoxyribose intermediate which facilitates the preparation of analogues by removing the sugar 3'-hydroxyl group prior to, rather than after, condensation with a uracil or cytosine aglycon. The 2'-F-dd-uridine analogues 7a-d (with H, F, Cl, and CH3 substitution in the 5-position) as well as the 4-deoxy compound (12b) are nonprotective to ATH8 or CEM cells infected with HIV-1. In the corresponding cytidine series, the 5-chloro analogue (11) is inactive. However, 2'-fluoro-2',3'-dideoxyarabinosylcytosine, 10a, and its 5-fluoro analogue, 10b, are both active. While neither compounds is a potent as ddC or 5-F-ddC (2b), 10b gives complete protection against the cytopathic effects of HIV in both host cell lines. 2'-Fluoro substitution confers increased chemical and enzymatic stability on dideoxynucleosides. Even though dideoxy pyrimidine nucleosides are inherently more stable than the corresponding purine analogues toward acid-catalyzed cleavage of the glycosidic bond, 2'-fluoro substitution (10a) still increases stabilization relative to ddC (2b). No detectable deamination by partially purified cytidine deaminase is observed with the 2'-fluoro compounds 10a, 10b, or 11 under conditions which rapidly deaminate cytidine. A small amount of 2'-F-dd-ara-U (7a) is formed from 10a in monkey plasma after greater than 24 h of exposure. The octanol-water partition coefficients for the dideoxynucleosides in this study indicate their hydrophilic character, with log P values varying from -0.28 to -1.18.
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PMID:Chemistry and anti-HIV properties of 2'-fluoro-2',3'-dideoxyarabinofuranosylpyrimidines. 135 45

Some types of reused dental equipment, especially handpieces and their attachments for drilling and cleaning teeth, might be responsible for cross-contamination if patient material were to lodge temporarily in difficult-to-disinfect internal mechanisms. This possibility is worrisome with respect to transmission of hepatitis B and human immunodeficiency viruses (HBV, HIV). Previous cross-contamination studies have relied on laboratory experiments with bacteria or dye tracers. To assess possible risk more thoroughly, we tested 30 new prophylaxis angles and 12 new high-speed handpieces to see whether they would take up and expel contaminants in laboratory and clinical trials. In treatments of three patients, including two infected with HIV, human-specific DNA (beta-globin, HLA DQ alpha) and HIV proviral DNA were detected inside or coming back from the devices. Similarly, when handpieces were operated in contact with blood pooled from HBV-infected patients, HBV DNA was detected in samples taken from inside the equipment and from their attached air/water hoses. When we used bacteriophage phi X174 as a model virus in laboratory tests, many infective viral particles were recovered from internal mechanisms of handpieces, their connecting air/water hoses, and from water spray expelled when the equipment was reused. We recommend that reused high-speed, air-driven handpieces and prophylaxis angles should be cleaned and heat-treated between patients. Further studies are needed to determine ways of eliminating the risks associated with exhaust hoses and air/water input lines.
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PMID:Cross-contamination potential with dental equipment. 809 83

The active principle of EP3, a fraction from an extract of the culture medium of Lentinus edodes mycelia (LEM), which activates murine macrophages, causes proliferation of bone marrow cells, and inhibit the replication of Human Immunodeficiency Virus in vitro, was characterized as a water-solubilized lignin. The detailed structural feature of this water-solubilized lignin was investigated and shown to be a highly condensed and polycarboxylated lignin which is denatured and solubilized by Lentinus edodes from bagasse. The water-solubilized lignin itself was confirmed to have both immunological activities and the antiviral activity.
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PMID:Structural characterization of the immunoactive and antiviral water-solubilized lignin in an extract of the culture medium of Lentinus edodes mycelia (LEM). 136 12

The cesium and tetramethylammonium (TMA) salts of polyoxotungstate anions with covalently attached organosilyl groups of formula [(RSi)2O]SiW11O39(4-), where R = CH2CH2COCH3, (CH2)3CN, and CH==CH2 (1-R, cesium salt, unless otherwise noted) have been prepared, purified, and spectroscopically characterized. The water solubility (25 degrees C) of these 10 new compounds ranges from 0.14 mM to 2.16 mM. All appear to be stable in aqueous media over a period of several hours as assessed by 1H NMR. The activities (EC50) of the new compounds against human immunodeficiency virus in primary human lymphocytes range from 3.3 microM to 39.0 microM. Their toxicities (IC50) are all greater than 100 microM. The inhibition constants of the new compounds against purified virion-derived HIV-1 reverse transcriptase are in the 1-10 microM range.
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PMID:Synthesis, characterization, and anti-human immunodeficiency virus activity of water-soluble salts of polyoxotungstate anions with covalently attached organic groups. 137 90


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