New and facile method of preparation of the anti-HIV-1 agent, 1,3-dicaffeoylquinic acid
| Autoři | |
|---|---|
| Rok publikování | 2001 |
| Druh | Článek v odborném periodiku |
| Časopis / Zdroj | Tetrahedron Letters |
| Fakulta / Pracoviště MU | |
| Citace | |
| Obor | Organická chemie |
| Klíčová slova | Antivirals; biologically active compounds; isomerisation; phenolics; tannins |
| Popis | A facile and inexpensive preparation of 1,3-dicaffeoylquinic acid (cynarin) from the leaves Cynara cardunculus L. (Asteraceae) without the use any chromatographic steps is described. The procedure was based on separation of the fraction rich in 1,5-dicaffeoylquinic acid, isomerisation of 1,5-dicaffeoylquinic acid to cynarin and, owing to its higher polarity, the simple isolation of cynarin from the reaction mixture. Cynarin inhibited HIV-1 replication in MT-2 cell culture at nontoxic concentrations similar to other previously tested dicaffeoylquinic acids, which have been recently established as a potent and highly selective class of HIV-1 integrase inhibitors. |
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