Sialidase inhibitory activity of diarylnonanoid and neolignan compounds extracted from the seeds of Myristica fragrans. Issue 14 (15th July 2017)

• Record Type: Journal Article
• Authors: Park, Ji-Young; Hwan Lim, Su; Ram Kim, Bo; Jae Jeong, Hyung; Kwon, Hyung-Jun; Song, Gyu-Yong; Bae Ryu, Young; Song Lee, Woo
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 14(2017)
• Page Start: 3060
• Page End: 3064
• Publication Date: 2017-07-15
• Subjects: Sialidase -- NanA -- NanB -- Myristica fragrans -- Malabaricone C; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.05.055
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: Twelve compounds with sialidase inhibitory potency were extracted from M. fragrans. Malabaricone C showed the maximal inhibitory activity against NanA, NanB, and NanC. Natural diarylnonanoids and lignans are useful against bacterial infection. Abstract: Sialidases are key virulence factors that remove sialic acid from host cell surface glycans, thus unmasking receptors to facilitate bacterial adherence and colonization. In this study, we report the isolation and characterization of novel inhibitors of the Streptococcus pneumoniae sialidases NanA, NanB, and NanC from Myristica fragrans seeds. Of the isolated compounds (1 –12 ), malabaricone C showed the most pneumococcal sialidases inhibition (IC50 of 0.3 μM for NanA, 3.6 μM for NanB, and 2.9 μM for NanC). These results suggested that malabaricone C and neolignans could be potential agents for combating S. pneumoniae infection agents.