Development of vaginal microbicides for the prevention of heterosexual transmission of HIV

Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology

Volumn 11, Issue 3, 1996, Pages 211-221

  Pauwels, Rudi ^a,b   De Clercq, Erik ^a  

^a REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

^b TIBOTEC BVBA   (Belgium)

Author keywords

Antiviral agents; Sexual transmission; Vaginal microbicides; Virucidal agents

Indexed keywords

ANTIVIRUS AGENT; CHLORHEXIDINE; NONOXINOL 9; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ANTIMICROBIAL ACTIVITY; ARTICLE; DISEASE SEVERITY; DISEASE TRANSMISSION; HETEROSEXUALITY; HUMAN; PRIORITY JOURNAL; SEXUAL TRANSMISSION; SEXUALLY TRANSMITTED DISEASE; VIRUS REPLICATION;

EID: 0030008132     PISSN: 10779450     EISSN: None     Source Type: Journal    
DOI: 10.1097/00042560-199603010-00001     Document Type: Article

References (70)

1. De Clercq E. Antiviral agents: characteristic activity spectrum depending on the molecular target they interact with. In: Maramorosch K, Murphy FA, Shatkin AJ, eds. Advances in virus research, vol. 42. Orlando: Academic Press, 1993:1-55.
2. Nkowane BM. Prevalence and incidence of HIV infection in Africa: a review of data published in 1990. AIDS 1991;5:s7-16.
3. Levy JA. Pathogenesis of human immunodeficiency virus infection. Microbiol Rev 1993;57:183-289.
4. Wolff H, Anderson DJ, Immunohistologic characterization and quantitation of leukocyte subpopulations in human semen. Fertil Steril 1988;49:497-504.
5. Pearce-Pratt R, Philips DM. Studies of adhesion of lymphocyte cells: implications for sexual transmission of human immunodeficiency virus. Biol Reprod 1993;48:431-45.
6. Feldblum PJ, Rosenberg MJ. Spermicides and sexually transmitted diseases: new perspectives. NC Med J 1986;47:569-72.
7. Alexander NJ. Sexual transmission of human immunodeficiency virus: virus entry into the male and female genital tract. Fertil Steril 1990;54:1-18.
8. Niruthisard S, Roddy RE, Chutivongse S. The effects of frequent nonoxynol-9 use on the vaginal and cervical mucosa. Sex Transm Dis 1991;18:176-9.
9. Roddy RE, Cordero M, Fortney JA. A dosing study of non-oxynol-9 and genital irritation. Int J STD AIDS 1993;4:165-70.
10. Kreiss J, Ngugi E, Holmes K, Guinan ME, Stone KM, Peterson HB. Efficacy of nonoxynol-9 contraceptive sponge use in preventing heterosexual acquisition of HIV in Nairobi prostitutes. JAMA 1991;268:477-82.
11. Montefiori DC, Robinson WE, Modliszewski A, Mitchell WM. Effective inactivation of human immunodeficiency virus with chlorhexidine antiseptics containing detergents and alcohol. J Hosp Infect 1990;15:279-82.
12. Yamaguchi Y, Semmel M, Stanislawski L, Strosberg AD, Stanislawski M. Virucidal effects of glucose oxidase and peroxidase or their protein conjugates on human immunodeficiency virus type 1. Antimicrob Agents Chemother 1993;37:26-31.
13. Lavie G, Valentine F, Levin B, et al. Studies of the mechanisms of action of the antiretroviral agents hypericin and pseudohypericin. Prod Natl Acad Sci USA 1989;86:5963-7.
14. Schinazi RF, Chu CK, Babu JR, et al. Anthraquinones as a new class of antiviral agents against human immunodeficiency virus. Antiviral Res 1990;13:265-72.
15. Andersen DO, Weber ND, Wood SG, Hughes BG, Murray BK, North JA. In vitro virucidal activity of selected anthraquinones and anthraquinone derivatives. Antiviral Res 1991;16:185-96.
16. Tang J, Colacino JM, Larsen SH, Spitzer W. Virucidal activity of hypericin against enveloped and non-enveloped DNA and RNA viruses. Antiviral Res 1990;13:313-26.
17. Hudson JB, Lopez-Bazzocchi I, Towers GHN. Antiviral activities of hypericin. Antiviral Res 1991;15:101-12.
18. 60 fullerene. Antimicrob Agents Chemeter 1993;37:1707-10.
19. De Somer P, De Clercq E, Billiau A, Schonne E, Claesen M. Antiviral activity of polyacrylic and polymethacrylic acids. I. Mode of action in vitro. J Virol 1968;2:878-85.
20. De Somer P, De Clercq E, Billiau A, Schonne E, Claesen M. Antiviral activity of polyacrylic and polymethacrylic acids. II. Mode of action in vivo. J Virol 1968;2:886-93.
21. Pauwels R, Andries K, Desmyter J, et al. Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives. Nature 1990;343:470-4.
22. Baba M, Pauwels R, Balzarini J, Arnout J, Desmyter J, De Clercq E. Mechanism of inhibitory effect of dextran sulfate and heparin on the replication of human immunodeficiency virus in vitro. Proc Natl Acad Sci USA 1988;85:6132-6.
23. + cells. Science 1988;240:646-9.
24. + cells. J Acquir Immune Defic Syndr 1989;2:10-5.
25. Schols D, Pauwels R, Desmyter J, De Clercq E. Dextran sulfate and other polyanionic anti-HIV compounds specifically interact with the viral gp120 glycoprotein expressed by T-cells persistently infected with HIV-1. Virology 1990;175:556-61.
26. Schols D, De Clercq E, Balzarini J, et al. Sulphated polymers are potent and selective inhibitors of various enveloped viruses, including herpes simplex virus, cytomegalovirus, vesicular stomatitis virus, respiratory syncytial virus, and toga-, arena- and retroviruses. Antiviral Chem Chemother 1990;1:233-40.
27. Callahan LN, Phelan M, Mallinson M, Norcross MA. Dextran sulfate blocks antibody binding to the principal neutralizing domain of human immunodeficiency virus type 1 without interfering with gp120-CD4 interactions. J Virol 1991;65:1543-50.
28. Baba M, Schols D, Pauwels R, Nakashima H, De Clercq E. Sulfated polysaccharides as potent inhibitors of HIV-induced syncytium formation: a new strategy towards AIDS chemotherapy. J Acquir Immune Defic Syndr 1990;3:493-9.
29. Ueno R, Kuno S. Dextran sulfate, a potent anti-HIV agent in vitro having synergism with zidovudine. Lancet 1987;1:1379.
30. Ito M, Baba M, Sato A, Pauwels R, De Clercq E, Shigeta S. Inhibitory effect of dextran sulfate and heparin on the replication of human immunodeficiency virus (HIV) in vitro. Antiviral Res 1987;7:361-7.
31. Baba M, Nakajima M, Schols D, Pauwels R, Balzarini J, De Clercq E. Pentosan polysulfate, a sulfated oligosaccharide, is a potent and selective anti-HIV agent in vitro. Antiviral Res 1988;9:335-43.
32. Witvrouw M, Baba M, Balzarini J, Pauwels R, De Clercq E. Establishment of a bioassay to determine serum levels of dextran sulfate and pentosan polysulfate, two potent inhibitors of human immunodeficiency virus. J Acquir Immune Defic Syndr 1990;3:343-7.
33. Yoshida O, Nakashima H, Yoshida T, et al. Sulfation-of the immunomodulating polysaccharide lentinan: a novel strategy for antivirals to human immunodeficiency virus (HIV). Biochem Pharmacol 1988;37:2887-91.
34. Ito M, Baba M, Hirabayashi K, et al. In vitro activity of mannan sulfate, a novel sulfated polysaccharide, against human immunodeficiency virus type 1 and other enveloped viruses. Eur J Clin Microbiol Infect Dis 1989;8:171-3.
35. Jurkiewicz E, Panse P, Jentsch KD, Hartmann H, Hunsmann G. In vitro anti-HIV-1 activity of chondroitin poly sulphate. AIDS 1989;3:423-7.
36. Baba M, De Clercq E, Schols D, et al. Novel sulfated polysaccharides: dissociation of anti-human immunodeficiency virus activity from antithrombin activity. J Infect Dis 1990;161:208-13.
37. Kaneko Y, Yoshida O, Nakagawa R, et al. Inhibition of HIV-1 infectivity with curdlan sulfate in vitro. Biochem Pharmacol 1990;39:793-7.
38. Yoshida T, Hatanaka K, Uryu T, et al. Synthesis and structural analysis of curdlan sulfate with a potent inhibitory effect in vitro of AIDS virus infection. Macromolecules 1990;23:3117-22.
39. Weiler BE, Schröder HC, Stefanovich V, et al. Sulphoevernan, a polyanionic polysaccharide, and the naricissus lectin potently inhibit human immunodeficiency virus infection by binding to viral envelope protein. J Gen Virol 1990;71:1957-63.
40. Ito M, Baba M, Shigeta S, et al. Potent and selective activity of dextrin sulphate against human immunodeficiency virus type 1 in vitro. Antiviral Chem Chemother 1991;2:41-4.
41. Schols D, De Clercq E, Witvrouw M, et al. Sulphated cyclodextrins are potent anti-HIV agents acting synergistically with 2′,3′-dideoxynucleoside analogues. Antiviral Chem Chemother 1991;2:45-53.
42. Sosa MA, Fazely F, Koch JA, Vercelotti SV, Ruprecht RM. N-Carboxymethylchitosan-N,O-sulfate as an anti-HIV-1 agent. Biochem Biophys Res Commun 1991;174:489-96.
43. Handa A, Hoshino H, Nakajima K, et al. Inhibition of infection with human immunodeficiency virus type 1 by sulfated gangliosides. Biochem Biophys Res Commun 1991;175:1-9.
44. Witvrouw M, Schols D, Andrei G, et al. Antiviral activity of low-MW dextran sulphate (derived from dextran MW 1000) compared to dextran sulphate samples of higher MW. Antiviral Chem Chemother 1991;2:171-9.
45. Baba M, Schols D, De Clercq E, et al. Novel sulfated polymers as highly potent and selective inhibitors of human immunodeficiency virus (HIV) replication and giant cell formation. Antimicrob Agents Chemother 1990;34:134-8.
46. De Clercq E. Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses. Cancer Lett 1979;8:9-22.
47. Mitsuya H, Popovic M, Yarchoan R, Matsushita RC, Gallo RC, Broder S. Suramin protection of T-cells in vitro against infectivity and cytopathic effect of HTLV-III. Science 1984;226:172-4.
48. Broder S, Yarchoan R, Collins JM, et al. Effects of suramin on HTLV-III/LAV infection presenting as Kaposi's sarcoma or AIDS-related complex: clinical pharmacology and suppression of virus replication in vivo Lancet 1985;2:627-30.
49. Busch W, Brodt R, Ganser A, Helma EB, Stille W. Suramin treatment for AIDS. Lancet 1985;2:1247.
50. Cheson EA, Levine AM, Mildvan D. Suramin therapy in AIDS and related disorders. Report of the US Suramin working group. JAMA 1987;258:1347-51.
51. Mohan P, Singh R, Wepsiec J, Gonzalez I, Sun DK, Sarin PS. Inhibition of HIV replication, by naphthalenemonosulfonic acid derivatives and a bis naphthalenedisulfonic acid compound. Life Sci 1990;47:993-9.
52. Mohan P, Singh R, Baba M. Potential anti-AIDS agents. Synthesis and antiviral activity of naphthalenesulfonic acid derivatives against HIV-1 and HIV-2. J Med Chem 1991;34:212-7.
53. Balzarini J, Mitsuya H, De Clercq E, Broder S. Aurintricarboxylic acid and Evans Blue represent two different classes of anionic compounds which selectively inhibit the cytopathogenicity of human T-cell lymphotropic virus type III/lymphadenopathy-associated virus. Biochem Biophys Res Commun 1986;136:64-71.
54. Cushman M, Wang P, Chang SH, et al. Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogues: direct correlation of antiviral potency with molecular weight. J Med Chem 1991;34:329-37.
55. Cushman M, Wang P, Stowell JG, Schols D, De Clercq E. Structural investigation and anti-HIV activities of high molecular weight ATA polymers. J Org Chem 1992;57:7241-8.
56. Schols D, Baba M, Pauwels R, Desmyter J, De Clercq E. Specific interaction of aurintricarboxylic acid with the human immunodeficiency virus/CD4 cell receptor. Proc Natl Acad Sci USA 1989;86:3322-6.
57. Cushman M, Kanamathareddy S, De Clercq E, Schols D, Goldman ME, Bowen JA. Synthesis and anti-HIV activities of low molecular weight aurintricarboxylic acid fragments and related compounds. J Med Chem 1991;34:337-42.
58. Jansen RW, Molema G, Pauwels R, Schols D, De Clercq E, Meijer DKF. Potent in vitro anti-human immunodeficiency virus-1 activity of modified human serum albumins. Mol Pharmacol 1991;39:818-23.
59. Jansen RW, Pauwels R, Schols D, De Clercq E, Meijer DKF. Novel, negatively charged human serum albumins display potent and selective in vitro anti-human immunodeficiency virus type 1 activity. Mol Pharmacol 1993;44:1003-7.
60. Hill CL, Hartnup M, Faraj M, et al. Polyoxometalates as inorganic anti-HIV-1 compounds. Structure-activity relationships. In Diasio RB, Sommadossi J-P, eds. Advances in Chemotherapy of AIDS. New York: Pergamom Press, 1990;33-41.
61. Yamamoto N, Schols D, De Clercq E, et al. Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents. Mol Pharmacol 1992;42:1109-17.
62. Mayaux J-F, Bousseau A, Pauwels R, et al. Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells. Proc Natl Acad Sci USA 1994;91:3564-8.
63. De Clercq E, Yamamoto N, Pauwels R, et al. Potent and selective inhibition of human immunodeficiency virus (HIV)-l and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event. Proc Natl Acad Sci USA 1992;89:5286-90.
64. De Clercq E, Yamamoto N, Pauwels R, et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam JM3100. Antimicrob Agents Chemother 1994;38:668-74.
65. De Clercq E. HIV-1-specific RT inhibitors: highly selective inhibitors of human immunodeficiency virus type 1 that are specifically targeted at the viral reverse transcriptase. Med Res Rev 1993;13:229-58.
66. Baba M, Shigeta S, Tanaka H, et al. Highly potent and selective inhibition of HIV-1 replication by 6-phenylthioruracil derivatives. Antiviral Res 1992;17:245-64.
67. Merluzzi VJ, Hargrave KD, Labadia M, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science 1990;250:1411-3.
68. Goldman ME, Nunberg JH, O'Brien JA, et al. Pyridinone derivatives: specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity. Proc Natl Acad Sci USA 1991;88:6863-7.
69. Romero DL, Busso M, Tan C-K, et al. Nonnucleoside reverse transcriptase inhibitors that potently and specifically block human immunodeficiency virus type 1 replication. Proc Natl Acad Sci USA 1991;88:8806-10.
70. Pauwels R, Andries K, Debyser Z, et al. Potent and highly selective HIV-1 inhibition by a new series of α-anilino phenylacetamide (α-APA) derivatives targeted at HIV-1 reverse transcriptase. Proc Natl Acad Sci USA 1993;90:1711-5.