Synthesis of norlignans and in vitro inhibitory activity of antigen-induced degranulation

Eonjeong Park; Yoon Jung Yang; Aejin Kim; Jong Hwan Kwak; Young Hoon Jung; Se Chan Kang; In Su Kim

doi:10.1016/j.bmcl.2012.04.033

Synthesis of norlignans and in vitro inhibitory activity of antigen-induced degranulation

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3653-5. doi: 10.1016/j.bmcl.2012.04.033. Epub 2012 Apr 13.

Authors

Eonjeong Park¹, Yoon Jung Yang, Aejin Kim, Jong Hwan Kwak, Young Hoon Jung, Se Chan Kang, In Su Kim

Affiliation

¹ College of Pharmacy, Kyung Hee University, Seoul, Republic of Korea.

PMID: 22543029
DOI: 10.1016/j.bmcl.2012.04.033

Abstract

The synthesis and biological evaluation of a series of novel norlignans are described. Norlignans were evaluated for their inhibitory activity on the release of β-hexosaminidase, a marker of degranulation, from RBL-2H3 cells induced by the IgE-antigen complex. The results showed that norlignans 4c and 4e potently inhibited degranulation, with IC(50) values of 18.3 and 17.9 μM, respectively.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antigen-Antibody Complex / immunology*
Basophils / physiology
Cell Degranulation / drug effects*
Cell Line, Tumor
Immunoglobulin E / chemistry
Immunoglobulin E / metabolism
Lignans / chemical synthesis
Lignans / chemistry*
Lignans / pharmacology
Rats
Structure-Activity Relationship
beta-N-Acetylhexosaminidases / metabolism

Substances

Antigen-Antibody Complex
Lignans
Immunoglobulin E
beta-N-Acetylhexosaminidases