Anti-HIV-1 activity of the Iboga alkaloid congener 18- methoxycoronaridine.

Le centre de recherche sur l'ibogaïne de l' "Albany Medical College" a développé un alcaloïde synthétique le 18-MC (18-methoxycoronaridine).
Il semble présenter les mêmes propriétés anti-addictives que l'ibogaïne, sans en avoir les effets hallucinogènes.
Or, d''après PubMed, cette molécule d' ibogaïne synthétique aurait des propriétés antirétrovirales et inhiberait l'infection à HIV-1.

- Article en anglais:

· Silva EM,
· Cirne-Santos CC,
· Frugulhetti IC,
· Galvao-Castro B,
· Saraiva EM,
· Kuehne ME,
· Bou-Habib DC.

Laboratorio Avancado de Saude Publica, Centro de Pesquisas Goncalo Moniz, Salvador, BA, Brazil.

The Iboga alkaloid congener 18-methoxycoronaridine (18-MC) exhibits in vitro leishmanicidal and in vivo anti-addiction properties. In this paper, we describe that 18-MC inhibits HIV-1 infection in human peripheral blood mononuclear cells (PBMCs) and monocyte-derived macrophages. We found that 18-MC inhibits the replication of
primary isolates of HIV-1 in a dose-dependent manner, regardless of the preferentialchemokine receptor usage of the isolates, at non-cell-toxic concentrations.

The antiretroviral activity of 18-MC resulted in EC (50) values of 22.5 +/- 4.7 microM and 23 +/- 4.5 microM for R5 and X4 isolates, respectively, in PBMCs, and a therapeutic index (TI) of 14.5. Similar findings were observed for inhibition of HIV-1 replication in
macrophages: EC (50) equal to 12.8 +/- 5 microM and 9.5 +/- 3 microM for an R5 virus after 14 and 21 days of infection, respectively, with TI equal to 25.6 and 34.5.
18-MC moderately inhibits the HIV-1 enzyme reverse transcriptase (IC (50) = 69.4 microM), which at least partially explains its antiretroviral activity.

PMID: 15386189 [PubMed - indexed for MEDLINE]