26 / 29
Page 87
conferenceseries
.com
Volume 8
Medicinal Chemistry
ISSN: 2161-0444
Medicinal Chemistry 2018
June 14-15, 2018
June 14-15, 2018 | Barcelona, Spain
10
th
World Congress on
Medicinal Chemistry and Drug Design
Drug discovery from edible plants based on GLP-1R disease target
Rong-Jie Chein, Chebolu Naga Sesha Sai Pavan Kumar, Shih-Che Lin, Nai-Pin Lin, Klim King, Yu-Hong Cheng
and
Gao-Huei Chen
Academia Sinica, Taiwan
T
he glucagon-like peptide-1 receptor (GLP-1R) is expressed in many tissues and has been implicated in diverse physiological
functions, such as energy homeostasis and cognition. GLP-1 analogs are approved for treatment of type 2 diabetes and
are undergoing clinical trials for other disorders, including neurodegenerative diseases. GLP-1 analog therapies maintain
chronically high plasma levels of the analog and can lead to loss of spatiotemporal control of GLP-1R activation. To avoid
adverse effects associated with current therapies, we characterized positive modulators of GLP-1R signaling. We screened
extracts from edible plants using an intracellular cAMP biosensor and GLP-1R endocytosis assays. Galanal B and a new
compound (N55) were isolated from Hedychium coronarium (HC) and Trigonella foenum-graecum (fenugreek) respectively
as active principles for modulating glucagon-like-peptide-1 GLP-1 activity. The first total syntheses of both natural products
and their analogue were finished for structure elucidation and SAR study. These findings identify a new class of modulators of
GLP-1R signaling and suggest that GLP-1 is a viable target for drug discovery.
rjchein@chem.sinica.edu.twMed chem (Los Angeles) 2018, Volume 8
DOI: 10.4172/2161-0444-C1-040