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)

A number of nucleoside 5'-phosphonates and nucleoside 5'-methylphosphonates were synthesised, to study their ability to inhibit reproduction of HIV-1. Three compounds, 5'-hydrogen phosphonates of 3'-azido-2',3'-dideoxythymidine (AZT-HP, IVc), 3'-fluoro-2',3'-dideoxythymidine (FLT-HP, IVa) and 2',3'-dideoxyadenosine (ddA-HP, I), exhibit potent anti-HIV-1 activity with selectivity indices similar to or better of those of their parent nucleosides.
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PMID:[New 5'-phosphonates, modified through the nucleoside sugar residue, as inhibitors of HIV replication]. 140 17

In February 1991, a 30-year old single, Chinese male, who had not has sexual intercourse with another man but did have it with a woman while in another country 12 months earlier, sought medical care at Tan Tock Seng Hospital in Singapore. He had a productive cough for 3 months, lost 5 kg over 4 months, and had been gasping for breath for 3 days. Upon admission, he had a low grade fever and breathed very rapidly while resting. The apical segment of the right lower lobe of the lung had a 3 x 2 cm cavity which was filling with exudate. A sputum smear did not indicate acid fast bacilli in 2 of 3 samples and blood cultures did not yield aerobic or anaerobic bacteria. The Western blot test revealed HIV antibodies. The absolute CD4 lymphocyte count stood at 80/cu mm compared with more than 500/cm mm in healthy individuals. Physicians used a bronchoscope to do bronchoalveolar lavage (BAL) and transbronchial lung biopsy (TBLB), both of which disclosed cysts of Pneumocystis carinii. Treatment first consisted of trimethoprim/sulfamethoxazole for 7 days and antituberculosis chemotherapy for 2 weeks until the physicians realized he had Pneumocystis carinii. They switched the treatment to iv pentamidine isethionate because he still had a fever after 7 days. This treatment was successful. Physicians then administered Zidovudine (AZT) and aerosolized pentamidine each month. As of mid-1992 he was still healthy. In addition to the BAL/TBLB results indicating Pneumocystis carinii and excluding tuberculosis, other features excluding tuberculosis were a Mantoux reading of O, absence of hilar and/or mediastinal lymphadenopathy, response to pentamidine isethionate, and sputum and blood cultures that did not indicate Mycobacterium species.
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PMID:A case of cavitating pneumonia in AIDS. 141 78

We report the case of a woman who was found to be HIV positive after a sexual assault, in the absence of other risk factors for HIV infection. This observation and the report of one similar case support the view that HIV may be transmitted to a victim of a single sexual assault. We believe that all victims of rape should be offered a test for HIV and offered counselling. In addition to the current recommendations, the semen obtained should be tested for HIV antibodies by Western blot analysis. In the absence of clear data on safety and efficacy, we should recommend neither routine application of virucidal agents nor systematic Zidovudine (AZT) prophylaxis.
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PMID:HIV infection and rape. 141 36

The historical antisyphilis drug oxyphenarsine has been tested for antiviral activity and for cytotoxicity to characterize it as a potential therapy for treatment of HIV infections. These data show that the compound demonstrates marginal antiviral activity against the HTLV-IIIB strain of HIV-1, two clinical isolates of HIV-1 (one sensitive to AZT and one resistant), and the MS strain of HIV-2. However, treatment with concentrations of oxyphenarsine showing optimal anti-HIV activity resulted in significant cytotoxicity. The drug's selectivity index was not significantly improved when tested against H9 cells chronically infected with the HTLV-IIIB strain of HIV-1. Thus, despite a previous report suggesting significant antiviral activity and low cytotoxicity for oxyphenarsine, the data presented here do not provide support for further development of this drug as an anti-HIV agent.
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PMID:Characterization of oxyphenarsine as a potential antiviral agent for AIDS. 145 17

The goal of our study was to evaluate the incidence of heart involvement in AIDS patients during various stages of the disease. Between January 1988 to September 1991, we conducted a prospective study in 114 anti-HIV positive patients. The patients, whose mean age (+/- SD) was 34.6 +/- 5.4 years (range 20 to 54), were divided into three groups: anti-HIV positive asymptomatic (n = 31; 27%), AIDS related complex (ARC) group IV-A (n = 11; 10%), and AIDS subgroups IV-C1 (n = 62; 54%) and IV-D (n = 10; 9%). Overall, 84 patients (74%) were i.v. drug abusers, 24 (21%) were homosexuals, and six (5%) were partners at risk. Zidovudine (AZT) was administered to 94 patients (82%). Opportunistic infections and/or secondary malignancies were detected in 72 patients (63%). Electrocardiographic changes were of little clinical relevance. Of 72 AIDS patients, 47 (65.2%) presented a cardiac involvement: 12 subjects (16.6%) were affected by a dilated cardiomyopathy, 13 (18%) by pericardial effusion, three (4.1%) by mitral valve prolapse, four (5.5%) by myocarditis, five (6.9%) by valvular bacterial endocarditis, and 10 (13.8%) by alterations of left ventricle regional contractility. During a mean follow-up period of 44 months, 29 AIDS patients (40.2%) died. Death was attributed to a cardiac event in four patients; autopsy could be performed in 24 of the 29 patients who died. Our results demonstrate that heart involvement is present in 45.6% of HIV-infected patients, but only in the end-stage of the disease (AIDS) and it is presumably due to opportunistic infections and/or secondary malignancies.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Heart involvement in AIDS: a prospective study during various stages of the disease. 146 34

Inhibition of HIV-1- or HIV-2-induced cytopathicity and (Moloney) murine sarcoma virus (MSV)-induced cell transformation by amino acid and amino alcohol adducts of either 3'-azido-2',3'-dideoxythymidine 5'-monophosphate (AZTMP) or 5'-hydrogenphosphonate (AZTHP) were investigated. Both types of nucleotide adducts inhibited replication of HIV-1 and HIV-2 in MT-4 cells at a 1.5- to 3-fold higher EC50 (50% effective concentration) than AZT; and, also, selectivity indexes of these adducts were approximately 1.5 to 3-fold lower than that of AZT. The activity of the AZTMP and AZTHP adducts against MSV-induced transformation of C3H/3T3 cells was equal to or only slightly inferior than that of AZT, but their toxicity was 10-fold lower, so that their selectivity indexes were 2- to 7-fold higher. The nature of the aminoacyl component of the adducts significantly influence the antiretroviral activity of the test compounds.
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PMID:[Adducts of 3'-azido-2,3'-dideoxythymidine 5'-phosphate or 5'-phosphonate as inhibitors of cytopathic effect and transformation of cells under the influence of retroviruses in cell culture]. 147 Jan 77

Tachyplesin and polyphemusin are antimicrobial peptides recently isolated from the hemocytes of horseshoe crabs (Tachypleus tridentatus and Limulus polyphemus). We synthesized them and their analogs and examined their antiviral activity against human immunodeficiency virus (HIV) type 1 in vitro. The infection of human T cells with the virus was markedly inhibited by some of them at low concentrations. In this structure-activity study, we found that [Tyr5,12, Lys7]-polyphemusin II, which was designated as T22, had extremely high anti-HIV activity. Its 50% inhibitory concentration (EC50) was 0.008 micrograms/ml, while its 50% cytotoxic concentration (CC50) was 54 micrograms/ml and these values were comparable to those of AZT. This result indicates that T22 would be a potential candidate for the therapy of HIV infection.
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PMID:A novel anti-HIV synthetic peptide, T-22 ([Tyr5,12,Lys7]-polyphemusin II). 147 56

A sensitive assay was developed for in vitro evaluation of anti-HIV agents in monocyte-macrophage cells (M/M) (a crucial target of HIV in the body). Monocyte-macrophage cells are usually poorly sensitive to the cytopathic effect induced by HIV. However, when fresh adherent monocyte-macrophage cells are cultured at relatively high density in the presence of macrophage-colony stimulating factor (M-CSF), they undergo cytolysis and die in 2-3 weeks. HIV-mediated cell-killing can thus be assessed with a method based on the reduction of the yellow colored 3-(4-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) by metabolically active cells to a blue formazan, which can be measured spectrophotometrically. HIV-mediated cytopathic effect of M-CSF-exposed monocyte-macrophage cells was consistently achieved in all experiments performed under the conditions described herein. Anti-HIV activity of zidovudine (AZT) was also comparatively evaluated in M-CSF- and normal monocyte-macrophage cells both using the MTT assay and by measuring HIV-p24 antigen production in supernatants of monocyte-macrophage cells cultures, and similar results obtained with both methods. These results support the use of this colorimetric assay for broad screening of anti-HIV agents in monocyte-macrophage cells.
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PMID:A tetrazolium-based colorimetric assay for quantification of HIV-1-induced cytopathogenicity in monocyte-macrophages exposed to macrophage-colony-stimulating factor. 147 34

Building on the Weibull distribution, we develop a modeled time-varying density function of the incubation time between exposure to HIV infection and full-blown AIDS. This approach leads to a series of cohort-specific density functions that take into account the increasing impact of new therapies such as zidovudine (AZT). The resulting modeled density functions are studied in detail, particularly with regard to their modes and medians. The mode is sensitive to changes in the period incubation time distribution, with even a possibility of a bimodal distribution for certain combinations of the parameters that determine the rate at which the period median incubation time changes. An important substantive result is that when a period median incubation period slowly increases to some leveling off value, say m(xc), then it is surprisingly early on that cohorts of infected individuals have a median incubation period very close to that ultimate value m(xc).
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PMID:A modeled time-varying density function for the incubation period of AIDS. 148 77

Granulocyte-macrophage colony-stimulating factor (GMCSF) is a hematopoietic protein that has been studied both in vitro and in vivo in human immunodeficiency virus (HIV) infection. Since both HIV infection primarily and zidovudine (formerly AZT) treatment secondarily may result in neutropenia, administration of GMCSF to persons with HIV infection is generating considerable interest. Despite in vitro studies demonstrating that the agent may stimulate HIV replication, in the presence of zidovudine a synergistic inhibition of replication occurs. Early clinical studies in patients with the acquired immunodeficiency syndrome indicate that GMCSF can raise neutrophil counts with or without concurrent zidovudine treatment. The long-term safety and tolerance of the combination has to be established.
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PMID:Granulocyte-macrophage colony-stimulating factor and zidovudine in the treatment of neutropenia and human immunodeficiency virus infection. 149 10


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