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Molecules 2014, 19(4), 5135-5149; doi:10.3390/molecules19045135
Article

The Effect of DA-9701 on 5-Hydroxytryptamine-Induced Contraction of Feline Esophageal Smooth Muscle Cells

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Received: 7 February 2014; in revised form: 8 April 2014 / Accepted: 15 April 2014 / Published: 22 April 2014
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Abstract: Serotonin, or 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter found in blood platelets, the gastrointestinal (GI) tract, and the central nervous system (CNS) of animals and humans. The signaling pathways of 5-hydroxytryptamine (5-HT)-induced contractions in cat esophageal smooth muscle cell (ESMC)s have been identified, but the downstream components of the 5-HT signaling pathway remain unclear. DA-9701 is the standardized extract of the Pharbitis nil Choisy seed (Pharbitidis Semen, Convolvulaceae) and the root of Corydalis yahusuo W.T. Wang (Corydalis Tuber, Papaveraceae). DA-9701 is known to have strong gastroprokinetic effects and a good safety profile. In this study, we investigated the 5-HT signaling pathway at the G-protein level, and we explored the mechanisms by which DA-9701 induces smooth muscle contraction. Freshly isolated smooth muscle cells were harvested from the feline esophagus, and cells were permeabilized to measure their length. 5-HT produced esophageal smooth muscle contractions in a dose-dependent manner. Furthermore, 5-HT produced a relatively long-acting contraction. 5-HT binds to the 5-HT2, 5-HT3 and 5-HT4 receptors to induce smooth muscle contraction in feline ESMCs. These receptors, which are located in esophageal smooth muscle, are coupled to Gαq, Gαo and Gαs. These G proteins activate PLC, which leads to Ca2+/calmodulin-dependent MLCK activation, resulting in MLC20 phosphorylation and cell contraction. Conversely, DA-9701 inhibits 5-HT-induced contraction by inhibiting MLC20 phosphorylation.
Keywords: 5-hydroxytryptamine; feline esophageal smooth muscle; DA-9701; Pharbitidis Semen; Corydalis Tuber; MLC20; phosphorylation 5-hydroxytryptamine; feline esophageal smooth muscle; DA-9701; Pharbitidis Semen; Corydalis Tuber; MLC20; phosphorylation
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Oh, K.H.; Nam, Y.; Jeong, J.H.; Kim, I.K.; Sohn, U.D. The Effect of DA-9701 on 5-Hydroxytryptamine-Induced Contraction of Feline Esophageal Smooth Muscle Cells. Molecules 2014, 19, 5135-5149.

AMA Style

Oh KH, Nam Y, Jeong JH, Kim IK, Sohn UD. The Effect of DA-9701 on 5-Hydroxytryptamine-Induced Contraction of Feline Esophageal Smooth Muscle Cells. Molecules. 2014; 19(4):5135-5149.

Chicago/Turabian Style

Oh, Kyung H.; Nam, Yoonjin; Jeong, Ji H.; Kim, In K.; Sohn, Uy D. 2014. "The Effect of DA-9701 on 5-Hydroxytryptamine-Induced Contraction of Feline Esophageal Smooth Muscle Cells." Molecules 19, no. 4: 5135-5149.



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