alexa Phospholipid-based Prodrugs For The Treatment Of IBD: Drug Targeting Strategy
ISSN: 2161-0444

Medicinal Chemistry
Open Access

Like us on:
OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations

700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

Share This Page

Additional Info

Loading Please wait..

6th World Congress on Medicinal Chemistry and Drug Design
June 07-08, 2017 Milan, Italy

Shimon Ben-Shabat, Arik Dahan, Ellen M Zimmerman and Aaron Aponick
Ben-Gurion University of the Negev, Israel
University of Florida, USA
ScientificTracks Abstracts: Med Chem (Los Angeles)
DOI: 10.4172/2161-0444-C1-030
Phospholipase A2 (PLA2) expression/activity is significantly elevated in inflamed intestinal tissue in inflammatory bowel disease (IBD), Crohn’s disease and ulcerative colitis. PLA2 hydrolyses the sn-2 fatty acyl bond of phospholipids (PL) liberating a fattyacid and a lysophospholipid. By replacing the sn-2 positioned fatty-acid with a drug, PLA2 may be exploited as a prodrug activating enzyme, liberating the free drug from the PL-complex. Therefore, orally delivered PL-based prodrugs will release the free drug at the inflamed sites, effectively targeting the regions of intestinal inflammation. We have utilized a modern computational approach to simulate the PLA2-mediated activation using the candidate drug, and to predict the most appropriate linker length. We have synthesized PL-diclofenac conjugates and shown in-vitro activation of these synthesized conjugates by isolated bee venom PLA2 and conditioned medium from inflamed Caco-2 cell line. We showed that depending on the linker length between the PL and diclofenac, PLA2 could be exploited as the activating enzyme in-vitro, liberating the free diclofenac from the PL complex. We have compared the computational calculations to our experimental data, and obtained excellent correlation between the in-silico predictions and the in-vitro experiments. The proposed research may significantly improve drug therapy in IBD patients, enabling higher efficacy and lower toxicity profiles.

Shimon Ben-Shabat has his expertise in Bio-organic and Medicinal Chemistry combining the following areas: Design and synthesis (structure-activity relationship), drug delivery approaches (pro-drugs), targeting and mechanistic studies and bio-analytical studies. His work centers on the relationships between chemistry and biological activity, including evaluation on different disease models.

Email: [email protected]

image PDF   |   image HTML
Peer Reviewed Journals
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri, Food, Aqua and Veterinary Science Journals

Dr. Krish

[email protected]

1-702-714-7001 Extn: 9040

Clinical and Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals


[email protected]

1-702-714-7001Extn: 9042

Chemical Engineering and Chemistry Journals

Gabriel Shaw

[email protected]

1-702-714-7001 Extn: 9040

Earth & Environmental Sciences

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

General Science and Health care Journals

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics and Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001 Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Informatics Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Material Sciences Journals

Rachle Green

m[email protected]

1-702-714-7001Extn: 9039

Mathematics and Physics Journals

Jim Willison

[email protected]

1-702-714-7001 Extn: 9042

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001 Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

John Behannon

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

[email protected]

1-702-714-7001 Extn: 9042

© 2008-2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version