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Quercetin Inhibits 5-HT3A Receptor-Mediated Ion Current by Interacting with Pretransmembrane DomainⅠ
Byung-Hwan Lee(이병환),Sang-Min Jung(정상민),Jun-Ho Lee(이준호),Jong-Hoon Kim(김종훈),In-Soo Yoon(윤인수),Joon-Hee Lee(이준희),Sun-Hye Choi(최선혜),Sang-Mok Lee(이상목),YeSun Han(한예선),Hyun-Dong Paik(백동현),Seung-Yeol Nah(나승열) 한국생물공학회 2005 한국생물공학회 학술대회 Vol.2005 No.10
Lee, Byung-Hwan,Jeong, Sang-Min,Jung, Sang-Min,Lee, Jun-Ho,Kim, Jong-Hoon,Yoon, In-Soo,Lee, Joon-Hee,Choi, Sun-Hye,Lee, Sang-Mok,Chang, Choon-Gon,Kim, Hyung-Chun,Han, YeSun,Paik, Hyun-Dong,Kim, Yangme Korean Society for Molecular Biology 2005 Molecules and cells Vol.20 No.1
<P>The flavonoid, quercetin, is a low molecular weight substance found in apple, tomato and other fruit. Besides its antioxidative effect, quercetin, like other flavonoids, has a wide range of neuropharmacological actions including analgesia, and motility, sleep, anticonvulsant, sedative and anxiolytic effects. In the present study, we investigated its effect on mouse 5-hydroxytryptamine type 3 (5-HT3A) receptor channel activity, which is involved in pain transmission, analgesia, vomiting, and mood disorders. The 5-HT3A receptor was expressed in Xenopus oocytes, and the current was measured with the two-electrode voltage clamp technique. In oocytes injected with 5-HT3A receptor cRNA, quercetin inhibited the 5-HT-induced inward peak current (I(5-HT)) with an IC50 of 64.7 +/- 2.2 microM. Inhibition was competitive and voltage-independent. Point mutations of pre-transmembrane domain 1 (pre-TM1) such as R222T and R222A, but not R222D, R222E and R222K, abolished inhibition, indicating that quercetin interacts with the pre-TM1 of the 5-HT3A receptor.</P>
Seung-Yeol Nah,Byung-Hwan Lee,Sang-MIn Jung,Jun-Ho Lee,Jong-Hoon Kim,In-Soo Yoon,Joon-Hee Lee,Sun-Hye Choi,Sang-Mok Lee,Choon-Gon Chang,Hyung-Chun Kim,YeSun Han,백현동,김양미 한국분자세포생물학회 2005 Molecules and cells Vol.20 No.1
The flavonoid, quercetin, is a low molecular weight substance found in apple, tomato and other fruit. Besides its antioxidative effect, quercetin, like other flavonoids, has a wide range of neuropharmacological actions including analgesia, and motility, sleep, anticonvulsant, sedative and anxiolytic effects. In the present study, we investigated its effect on mouse 5-hydroxytryptamine type 3 (5-HT3A) receptor channel activity, which is involved in pain transmission, analgesia, vomiting, and mood disorders. The 5-HT3A receptor was expressed in Xenopus oocytes, and the current was measured with the two-electrode voltage clamp technique. In oocytes injected with 5-HT3A receptor cRNA, quercetin inhibited the 5-HT-induced inward peak current (I5-HT) with an IC50 of 64.7 ± 2.2 μM. Inhibition was competitive and voltage-independent. Point mutations of pretransmembrane domain 1 (pre-TM1) such as R222T and R222A, but not R222D, R222E and R222K, abolished inhibition, indicating that quercetin interacts with the pre-TM1 of the 5-HT3A receptor.