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ARS Home » Southeast Area » Oxford, Mississippi » Natural Products Utilization Research » Research » Publications at this Location » Publication #364044
Research Project: Discovery and Development of Natural Products for Pharmaceutical and Agrochemical Applications II

Location: Natural Products Utilization Research

Title: Synthesis and anti-inflammatory activities of Phloroglucinol-based derivatives

Author
item LI, NING - University Of Mississippi
item KHAN, SHABANA - University Of Mississippi
item QUI, SHI - University Of Mississippi
item LI, XING-CONG - University Of Mississippi

Submitted to: Molecules
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 12/3/2018
Publication Date: 12/7/2018
Publication URL: http://handle.nal.usda.gov/10113/6471202
Citation: Li, N., Khan, S.I., Qui, S., Li, X. 2018. Synthesis and anti-inflammatory activities of Phloroglucinol-based derivatives. Molecules. 23(12):3232-3240. https://doi.org/10.3390/molecules23123232.
DOI: https://doi.org/10.3390/molecules23123232

Interpretive Summary: Both natural and synthetic phlorogluinol derivatives possess potent biological activities. In an effort to identify synthetically available phloroglucinol-based anti-inflammatory compounds, monoacyl-, diacyl-, dimeric acyl-, alkylated monoacyl-, and the nitrogen-containing alkylated monoacylphloroglucinols were synthesized and evaluated for inhibitory activities against the inflammatory mediators such as inducible nitric oxide synthase (iNOS) and nuclear factor kappaB (NF-kB). The diacylphloroglucinol compound 2 and the alkylated monoacylphloroglucinol compound 4 are dual inhibitors of iNOS and NF-kB and may serve as leads for the synthesis of more potent anti-inflammatory compounds for future drug discovery.

Technical Abstract: The natural product phloroglucinol-based derivatives representing monoacyl-, diacyl-, dimeric acyl-, alkylated monoacyl-, and the nitrogen-containing alkylated monoacylphloroglucinols were synthesized and evaluated for inhibitory activities against the inflammatory mediators such as inducible nitric oxide synthase (iNOS) and nuclear factor kappaB (NF-kB). The diacylphloroglucinol compound 2 and the alkylated acylphloroglucinol compound 4 inhibited iNOS with IC50 values of 19.0 and 19.5 µM, respectively, and NF-kB with IC50 values of 34.0 and 37.5 µM, respectively. These compounds may serve as leads for the synthesis of more potent anti-inflammatory compounds for future drug discovery.