[Determination of the binding constants of four anti-HIV-1 active compounds with bovine serum albumin by capillary zone electrophoresis].
The binding constants (Kb) of four novel anti-HIV-1 active compounds with bovine serum albumin (BSA) were determined by capillary zone electrophoresis (CZE) with UV detection under condition of phosphate buffer (pH 8.0, 50 mmol/L) at 15 kV running voltage. These molecules were synthesized by computer-simulated design with the property of inhibiting the binding of HIV-1 Tat protein to trans-activation response region (TAR) RNA required for HIV-1 transcription and blocking the HIV replication cycle. The results showed that with the addition of different concentrations of BSA into the buffer solution, the binding constants of four active compounds (IG3, iso-C3, C3, MC3) with BSA could be measured by the change of migration time. The experimental values of Kb were 1.07 x 10(4), 1.34 x 10(4), 8.51 x 10(3) and 9.45 x 10(3) L/mol, respectively. It is an easy and simple method to estimate the interaction of small molecules with biomacromolecules with 1:1 molar binding ratio.
Ding
Li
L
College of Chemistry, Peking University, Beijing 100871, China.
Zhang
Xin-Xiang
XX
Chang
Wenbao
W
Lin
Wei
W
Yang
Ming
M
D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry*; D002417:Cattle; D019075:Electrophoresis, Capillary / Q000379:methods; D015497:HIV-1 / Q000187:drug effects*; D011485:Protein Binding; D012710:Serum Albumin, Bovine / Q000737:chemistry*; D013056:Spectrophotometry, Ultraviolet
D019380:Anti-HIV Agents; D012710:Serum Albumin, Bovine