Pre-clinical development as microbicide of zinc tetra-ascorbo-camphorate, a novel terpenoid derivative: Potent in vitro inhibitory activity against both R5- and X4-tropic HIV-1 strains without significant in vivo mucosal toxicity

AIDS Research and Therapy

Volumn 5, Issue , 2008, Pages

  Saïdi, Héla ^a   Jenabian, Mohammad Ali ^a   Gombert, Bernard ^b   Charpentier, Charlotte ^a   Mannarini, Aurèle ^b   Bélec, Laurent ^a  

^a HÔPITAL EUROPÉEN GEORGES POMPIDOU   (France)

^b MGB Pharma   (France)

Author keywords

[No Author keywords available]

Indexed keywords

CARBON 14; ENFUVIRTIDE; MICROBICIDE; TERPENOID DERIVATIVE; ZINC TETRAASCORBOCAMPHORATE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIVIRAL ACTIVITY; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DENDRITIC CELL; DRUG DOSE COMPARISON; DRUG MEGADOSE; DRUG POTENCY; DRUG SAFETY; FEMALE; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; IN VITRO STUDY; IN VIVO STUDY; LOW DRUG DOSE; MACROPHAGE; NONHUMAN; PRIORITY JOURNAL; RABBIT; T LYMPHOCYTE; TARGET CELL; VAGINAL PRURITUS; VIRUS INHIBITION; VIRUS STRAIN; VIRUS TRANSMISSION;

EID: 45549085361     PISSN: 17426405     EISSN: None     Source Type: Journal    
DOI: 10.1186/1742-6405-5-10     Document Type: Article

References (30)

1. Türmen T Gender and HIV/AIDS Int J Gynaecol Obstet 2003, 82(3):411-8. 10.1016/S0020-7292(03)00202-9 14499987
2. Pool R Hart G Green G Harrison S Nyanzi S Whitworth J Men's attitudes to condoms and female controlled means of protection against HIV and STDs in south-western Uganda Cult Health Sex 2000, 2(2):197-211. 10.1080/ 136910500300804 12295882
3. Lee-Huang S Huang PL Huang PL Bourinbaiar AS Chen HC Kung HF Inhibition of the integrase of human immunodeficiency virus (HIV) type 1 by anti-HIV plant proteins MAP30 and GAP31 Proc Natl Acad Sci USA 1995, 92:8818-22. 41058 7568024 10.1073/pnas.92.19.8818
4. Mlinaric A Kreft S Umek A Strukelj B Screening of selected plant extracts for in vitro inhibitory activity on HIV-1 reverse transcriptase (HIV-1 RT) Pharmazie 2000, 55:75-7. 10683878
5. Yu D Morris-Natschke SL Lee KH New developments in natural products-based anti-AIDS research Med Res Rev 2007, 27:108-32. 10.1002/ med.20075 16888749
6. Alakurtti S Makela T Koskimies S Yli-Kauhaluoma J Pharmacological properties of the ubiquitous natural product betulin Eur J Pharm Sci 2006. 29:1-13. 10.1016/j.ejps.2006.04.006 16716572
7. Yogeeswari P Sriram D Betulinic acid and its derivatives: A review on their biological properties Curr Med Chem 2005, 12:657-66. 15790304
8. Tsuda H Okamoto H Elimination of metabolic cooperation by glycyrrhetinic acid, an anti-tumor promoter, in cultured Chinese hamster cells Carcinogenesis 2005, 7(11):1805-7. 10.1093/carcin/7.11.1805 3533303
9. Cichewicz RH Kouzi SA Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection Med Res Rev 2004, 24:90-114. 10.1002/med.10053 14595673
10. Huang L Chen CH Molecular targets of anti-HIV-1 triterpenes Curr Drug Targets Infect Disord 2002, 2(1):33-6. 10.2174/1568005024605936 12462151
11. Chomont N Hocini H Gody JC Bouhlal H Becquart P Krief-Bouillet C Kazatchkine M Bélec L Neutralizing monoclonal antibodies to human immunodeficiency virus type 1 do not inhibit viral transcytosis through mucosal epithelial cells Virology 2008, 20;370(2):246-54. 10.1016/ j.virol.2007.09.006
12. Legoff J Bouhlal H Grésenguet G Weiss H Khonde N Hocini H Désiré N Si-Mohamed A de Dieu Longo J Chemin C Frost E Pépin J Malkin JE Mayaud P Bélec L Real-time PCR quantification of genital shedding of herpes simplex virus (HSV) and human immunodeficiency virus (HIV) in women coinfected with HSV and HIV J Clin Microbiol 2006, 44(2):42. 1351957 16390945 10.1128/ JCM.44.2.423-432.2006
13. Saïdi H Magri G Carbonneil C Nasreddine N Réquena M Bélec L IFN-gamma-activated monocytes weakly produce HIV-1 but induce the recruitment of HIV-sensitive T cells and enhance the viral production by these recruited T cells J Leukoc Biol 2007, 81(3):642-53. 10.1189/jlb.0406278 16971466
14. Saïdi H Nasreddine N Jenabian MA Lecerf M Schols D Krief C Balzarini J Bélec L Differential in vitro inhibitory activity against HIV-1 of alpha-(1-3)- and alpha-(1-6)-D-mannose specific plant lectins: Implication for microbicide development J Transl Med 2007, 5:28. 1904181 17565674 10.1186/1479-5876-5-28
15. Laurendeau I Bahuau M Vodovar N Larramendy C Olivi M Bieche I Vidaud M Vidaud D TaqMan PCR-based gene dosage assay for predictive testing in individuals from a cancer family with INK4 locus haploinsufficiency Clin Chem 1999, 45:982-6. 10388473
16. Eckstein P Jackson MC Millman N Sobrero AJ Comparison of vaginal tolerance tests of spermicidal preparations in rabbits and monkeys J Reprod Fertil 1969, 20(1):85-93. 4982533
17. Haywood AM Virus receptors: Binding, adhesion strengthening, and changes in viral structure J Virol 1994, 68:1-5. 236257 8254718
18. Hladik F Sakchalathorn P Ballweber L Lentz G Fialkow M Eschenbach D McElrath MJ Initial events in establishing vaginal entry and infection by human immunodeficiency virus type-1 Immunity 2007, 26(2):257-70. 1885958 17306567 10.1016/j.immuni.2007.01.007
19. Miller CJ Shattock RJ Target cells in vaginal HIV transmission Microbes Infect 2003, 5(1):59-67. 10.1016/S1286-4579(02)00056-4 12593974
20. Schnittman SM Lane HC Greenhouse J Justement JS Baseler M Fauci AS Preferential infection of CD4+ memory T cells by human immunodeficiency virus type 1: Evidence for a role in the selective T-cell functional defects observed in infected individuals Proc Natl Acad Sci USA 1990, 87:6058-62. 54471 2385584 10.1073/pnas.87.16.6058
21. Lard-Whiteford SL Matecka D O'Rear JJ Yuen IS Litterst C Reichelderfer P Recommendations for the nonclinical development of topical microbicides for prevention of HIV transmission: An update J Acquir Immune Defic Syndr 2004, 36:541-52. 10.1097/00126334-200405010-00001 15097296
22. Geijtenbeek TB Kwon DS Torensma R van Vliet SJ van Duijnhoven GC Middel J Cornelissen IL Nottet HS KewalRamani VN Littman DR Figdor CG van Kooyk Y DC-SIGN, a dendritic cell-specific HIV-1-binding protein that enhances trans-infection of T cells Cell 2000, 100:587-97. 10.1016/ S0092-8674(00)80694-7 10721995
23. Turville SG Vermeire K Balzarini J Schols D Sugar-binding proteins potently inhibit dendritic cell human immunodeficiency virus type 1 (HIV-1) infection and dendritic-cell-directed HIV-1 transfer J Virol 2005, 79:13519-27. 1262561 16227272 10.1128/JVI.79.21.13519-13527.2005
24. Burleigh L Lozach PY Schiffer C Staropoli I Pezo V Porrot F Canque B Virelizier JL Arenzana-Seisdedos F Amara A Infection of dendritic cells (DCs), not DC-SIGN-mediated internalization of human immunodeficiency virus, is required for long-term transfer of virus to T cells J Virol 2006, 80(6):2949-57. 1395470 16501104 10.1128/JVI.80.6.2949-2957.2006
25. Polsky B Baron PA Gold JW Smith JL Jensen RH Armstrong D In vitro inactivation of HIV-1 by contraceptive sponge containing nonoxynol-9 Lancet 1988, 1:1456. 10.1016/S0140-6736(88)92261-1 2898603
26. Van Damme L Ramjee G Alary M Vuylsteke B Chandeying V Rees H Sirivongrangson P Mukenge-Tshibaka L Ettiegne-Traore V Uaheowitchai C Karim SS Masse B Perriens J Laga M Effectiveness of COL-1492, a nonoxynol-9 vaginal gel, on HIV-1 transmission in female sex workers: A randomised controlled trial Lancet 2002, 360:971-7. 10.1016/ S0140-6736(02)11079-8 12383665
27. D'Cruz OJ Uckun FM Intravaginal toxicity studies of a gel-microemulsion formulation of spermicidal vanadocenes in rabbits Toxicol Appl Pharmacol 2001, 170(2):104-12. 10.1006/taap.2000.9089 11162774
28. Fichorova RN Guiding the vaginal microbicide trials with biomarkers of inflammation J Acquir Immune Defic Syndr 2004, 37(Suppl 3):S184-93. 16419271
29. Kish-Catalone TM Lu W Gallo RC DeVico AL Preclinical evaluation of synthetic -2 RANTES as a candidate vaginal microbicide to target CCR5 Antimicrob Agents Chemother 2006, 50:1497-509. 1426989 16569870 10.1128/ AAC.50.4.1497-1509.2006
30. Mauck C Rosenberg Z Van Damme L International Working Group on Microbicides Recommendations for the clinical development of topical microbicides: An update AIDS 2001, 4;15(7):857-68. 10.1097/ 00002030-200105040-00006