NDLI: Ginsenoside Rb1, a novel activator of the TMEM16A chloride channel, augments the contraction of guinea pig ileum

Content Provider	Springer Nature Link
Author	Guo, Shuai Chen, Yafei Pang, Chunli Wang, Xuzhao Qi, Jinlong Mo, Li Zhang, Hailin An, Hailong Zhan, Yong
Copyright Year	2017
Abstract	Calcium-activated chloride channels (CaCCs) play important roles in many physiological processes, and the molecular basis of CaCCs has been identified as TMEM16A in many cell types. It is well established that TMEM16A is a drug target in many diseases, including cystic fibrosis, hypertension, asthma, and various tumors. Therefore, identifying potent and specific modulators of the TMEM16A channel is crucial. In this study, we identified the first natural activator of TMEM16A from traditional Chinese medicine and explored its mechanism. Our data showed that Ginsenoside Rb1 (GRb1) can activate TMEM16A directly from the intracellular side in a dose-dependent manner at an EC50 of 38.4 ± 2.14 μM. GRb1 specifically activated TMEM16A/B, but not the other previously proposed CaCC mediators such as CFTR and bestrophin. Moreover, GRb1 promoted proliferation of CHO cells stably expressing TMEM16A, in a concentration-dependent manner. Finally, we showed that GRb1 increased the amplitude and frequency of contractions in an isolated guinea pig ileum assay in vivo. In summary, GRb1 can be considered a lead compound for the development of novel drugs for the treatment of diseases caused by TMEM16A dysfunction.
Starting Page	681
Ending Page	692
Page Count	12
File Format	PDF
ISSN	00316768
Journal	Pflügers Archiv
Volume Number	469
Issue Number	5-6
e-ISSN	14322013
Language	English
Publisher	Springer Berlin Heidelberg
Publisher Date	2017-01-25
Publisher Place	Berlin, Heidelberg
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Ginsenoside Rb1 Activator CaCCs/TMEM16A Electrophysiology Ileum contraction Human Physiology Molecular Medicine Neurosciences Cell Biology Receptors
Content Type	Text
Resource Type	Article
Subject	Physiology Physiology (medical) Clinical Biochemistry

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Determining the parameters of concentration-response relationship for histamine on the isolated portion of guinea pig stomach and guinea pig right atrium

Characterization of the effects of Cl− channel modulators on TMEM16A and bestrophin-1 Ca2+ activated Cl− channels

Relaxation of epicardial strains after volume changes in the isolated guinea pig left ventricle

The reversible displacement of the passive diastolic p-V curve in the isolated guinea pig left ventricle

Expression of anoctamins in retinal pigment epithelium (RPE)

Endothelin augments unitary calcium channel currents on the smooth muscle cell membrane of guinea-pig portal vein.

Cl− channels in smooth muscle cells

The relative potencies of some agonists at M2 muscarinic receptors in guinea-pig ileum, atria and bronchi.

Theaflavin binds to a druggable pocket of TMEM16A channel and inhibits lung adenocarcinoma cell viability.

Ginsenoside Rb1, a novel activator of the TMEM16A chloride channel, augments the contraction of guinea pig ileum

Similar Documents

Determining the parameters of concentration-response relationship for histamine on the isolated portion of guinea pig stomach and guinea pig right atrium

Characterization of the effects of Cl− channel modulators on TMEM16A and bestrophin-1 Ca2+ activated Cl− channels

Relaxation of epicardial strains after volume changes in the isolated guinea pig left ventricle

The reversible displacement of the passive diastolic p-V curve in the isolated guinea pig left ventricle

Expression of anoctamins in retinal pigment epithelium (RPE)

Endothelin augments unitary calcium channel currents on the smooth muscle cell membrane of guinea-pig portal vein.

Cl− channels in smooth muscle cells

The relative potencies of some agonists at M2 muscarinic receptors in guinea-pig ileum, atria and bronchi.

Theaflavin binds to a druggable pocket of TMEM16A channel and inhibits lung adenocarcinoma cell viability.

Ginsenoside Rb1, a novel activator of the TMEM16A chloride channel, augments the contraction of guinea pig ileum