Acetylace 7-hydroxy skupiny dibenzocyklooktadienových lignanů zvyšuje inhibici P-glykoproteinu
| Title in English | Acetylation of 7-hydroxygroup of dibenzocyclooktadiene lignans increases inhibition of P-glycoprotein |
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| Authors | |
| Year of publication | 2021 |
| Type | Conference abstract |
| MU Faculty or unit | |
| Citation | |
| Description | We prepared 3 new acetyl derivatives of dibenzocyclooctadiene lignans, which inhibited the activity of P-glycoproteins more effectively than the original lignans with an unesterified 7-hydroxy group. Acetylation of the 7-hydroxy group almost eliminated the negative effect of the 7-hydroxy group on P-glycoprotein inhibition. We have shown that the activity of lignans increases with their hydrophobicity, which can be explained by the action of P-glycoprotein inhibitors in the hydrophobic cell membrane. The study of the effect of the hydrophobicity of lignans on their ability to inhibit P-glycoprotein led to the conclusion that the significant increase in the activity of the two acetyl derivatives is also due to the specific effect of the acetyl group. |
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