Mechanism of action of Coumermycin A1.

Important note: Information in this article was accurate in 1994. The state of the art may have changed since the publication date.

Mechanism of action of Coumermycin A1.

Annu Conf Australas Soc HIV Med. 1993 Oct 28-30;5:102 (poster no. 54). Unique Identifier : AIDSLINE ASHM5/94348915
Jardine D; Locarnini S; Tachedjian G; Birch C; Virology Dept., Fairfield Hospital, Victoria.

Abstract: AIM: To investigate the mechanism of action of Coumermycin A1 against HIV. METHODS: We investigated the in vitro anti HIV activity of coumermycin A1 in acutely infected PBLs, T-cell lines (MT-2) and macrophages and in chronically infected cells (H9-HTLVIIIB and macrophages). Several in vitro assays, such as reverse transcription and CD4/gp120-interaction, were used in an attempt to elucidate the specific mechanism of action of the drug in the acutely infected lines. In addition a Coumermycin resistant isolate was generated by passage of the virus in increasing concentrations of the drug. RESULTS: Coumermycin A1 was active in cells acutely infected with HIV, with complete inhibition of the virus at 5 micrograms/ml. No inhibition of viral replication was observed in chronically infected cells. In vitro assays failed to locate the target of coumermycin in the replication cycle of HIV. Coumermycin resistant strains of HIV have been generated. CONCLUSION: Because Coumermycin inhibits HIV replication in acute but not chronic infections suggests that its target is at or before integration. However in vitro assays targeting attachment, penetration and reverse transcription have ruled out these processes as targets.

Keywords: Antibiotics/PHARMACOLOGY Cell Line Coumarins/PHARMACOLOGY Human HIV/*DRUG EFFECTS In Vitro Macrophages/MICROBIOLOGY T-Lymphocytes/MICROBIOLOGY Virus Integration/DRUG EFFECTS Virus Replication/*DRUG EFFECTS ABSTRACT
941230
M94C4312

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