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Yoo, Dong-Jin,Park, Hyung-Du,Kim, Ae-Rhan,Rho, Young S.,Shim, Sang-Chul Korean Chemical Society 2002 Bulletin of the Korean Chemical Society Vol.23 No.9
The model compounds, 8-methoxypsoralen-CH2O(CH2)n-adenine (MOPCH2OCnAd, n=2, 3, 5, 6, 8, and 10) in which 5 position of 8-methoxypsoralen (8-MOP) is linked by various lengths of polymethylene bridge to N9 of adenine. UV absorption spectra are identical with the sum of MOPCH2OC3 and adenine absorption spectra. Solvent effects on the UV absorption and fluorescence emission spectra indicate that the lowest excited singlet state is the $(\pi${\rightarrow}$\pi*)$ state. The spectral characteristics of the fluorescence of MOPCH2OCnAd are strongly dependent upon the nature of the solvents. The fluorescence emission spectra in aprotic solvents are broad and structureless due to the excimer formation through the folded conformation accelerated by hydrophobic ${\pi}-{\pi}$ stacking interaction. Increasing polarity of the protic solvents leads to higher population of unfolded conformation stabilized through favorable solvation and H-bonding, and consequently to an increase in the fluorescence intensity, fluorescence lifetime, and a shift of fluorescence maximum to longer wavelengths. The decay characteristics of the fluorescence in polar protic solvents shows two exponential decays with the lifetimes of 0.6-0.8 and 1.6-1.9 ns in 5% ethanol/water, while MOPCH2OC3 shows 0.5 and 1.7 ns fluorescence lifetimes. The long-lived component of fluorescence can be attributed to the relaxed species (i.e., the species for which the solvent reorientation (or relaxation) has occurred), while the short-lived components can be associated with the unrelaxed, or only partially relaxed, species.
Synthesis of Psoralen Derivatives and Their Blocking Effect of hKv1.5 Channel
Eun, Jae-Soon,Kim, Kwang-Sik,Kim, Han-Na,Park, Seon-Ah,Ma, Tian-Ze,Lee, Kyung-A,Kim, Dae-Keun,Kim, Hyung-Kyo,Kim, In-Su,Jung, Young-Hoon,Zee, Ok-Pyo,Yoo, Dong-Jin,Kwak, Yong-Geun 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
Previously, we found that a furocoumarin derivative, psoralen (7H-furo[3,2-g][1 ]benzopyran-7-one), blocked a human Kv1.5 potassium channel (hKv1.5) and has a potential antiarrhythmic effect. In the present study, to develop more potent hKv1.5 blockers or antiarrhythmic drugs, we synthesized ten psoralen derivatives and examined their blocking effects or hKv1.5 stably expressed in Ltk cells. Among the newly synthesized psoralen derivatives, three derivatives (Compounds 5,9 and 10) showed the open channel-blocking effect. Compound 9 among them was the most potent In blocking hKv1.5. We found that compound 9, one of the psoralen derivatives, inhibited the hKv1.5 current in a concentration-, use- and voltage-dependent manner with an IC$_{50}$ value of 27.4 ${\pm}$ 5.1 nM at +60 mV. Compound 9 accelerated the inactivation kinetics of the hKv1.5 channel, slowed the deactivation kinetics of hKv1.5 current resulting in a tail crossover phenomenon. Compound 9 inhibited hKv1.5 current in a use-dependent manner. These results indicate that compound 9, one of psoralen derivatives, acts on hKv1.5 channel as an open charnel blocker and is much more potent than psoralen in blocking hKv1.5 channel. If further studios were done, compound 9 might be an ideal antiarrhythmic drug for atrial fibrillation.
Synthesis of Psoralen Derivatives and Their Blocking Effect of hKv1.5 Channel
은재순,김광식,김한나,박선아,Tian-Ze Ma,이경아,김대근,김형교,김인수,정영훈,지옥표,유동진,곽용근 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
Previously, we found that a furocoumarin derivative, psoralen (7H-furo[3,2-g][1]benzopyran-7- one), blocked a human Kv1.5 potassium channel (hKv1.5) and has a potential antiarrhythmic effect. In the present study, to develop more potent hKv1.5 blockers or antiarrhythmic drugs, we synthesized ten psoralen derivatives and examined their blocking effects on hKv1.5 stably expressed in Ltk- cells. Among the newly synthesized psoralen derivatives, three derivatives (Compounds 5, 9 and 10) showed the open channel-blocking effect. Compound 9 among them was the most potent in blocking hKv1.5. We found that compound 9, one of the psoralen derivatives, inhibited the hKv1.5 current in a concentration-, use- and voltage-dependent manner with an IC50 value of 27.4 ± 5.1 nM at +60 mV. Compound 9 accelerated the inactivation kinetics of the hKv1.5 channel, slowed the deactivation kinetics of hKv1.5 current resulting in a tail crossover phenomenon. Compound 9 inhibited hKv1.5 current in a use-dependent manner. These results indicate that compound 9, one of psoralen derivatives, acts on hKv1.5 channel as an open channel blocker and is much more potent than psoralen in blocking hKv1.5 channel. If further studies were done, compound 9 might be an ideal antiarrhythmic drug for atrial fibrillation.