Our previous report showed that polyacetylene compound, 1-Heptadecene-11, 13-diyne-8, 9, 10-triol (PA) from the root of Cirsium japonicum var. ussuriense has anti-inflammatory activity. In this study we investigated the role of the PA as inhibitor of caspase-1, which converts prointerleukin-1β (proIL-1β) to active IL-1β and is activated by inflammasome involved in the inflammatory process. We tested the effect of PA on the production of pro-inflammatory cytokines, IL-1β in murine macrophage cell line, RAW264.7. PA inhibited lipopolysaccharide (LPS)-induced IL-1β production by macrophages at a dose dependent manner. PA also suppressed the activation of caspase-1. The mRNA level of ASC (apoptosis-associated spec-like protein containing a CARD), an important adaptor protein of inflammasome, was decreased in the PA treated group. Therefore our results suggest that the anti-inflammatory effect of PA is due to inhibit the caspase-1 activation.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3509166 | PMC |
http://dx.doi.org/10.4110/in.2012.12.5.213 | DOI Listing |
Nat Prod Res
January 2025
College of Pharmacy, Chungbuk National University, Cheongju, Korea.
Phytochemical investigation of the roots of yielded a new phenylpropanoid, adenophoride () and a new polyacetylene, adenylene () along with four phenylpropanoids and a polyacetylene. The structures were determined by spectroscopic analysis including NMR, MS, UV and IR. Among the isolated compounds, phenylpropanoids including a new compound showed mild α-glucosidase inhibitory activities.
View Article and Find Full Text PDFNat Prod Res
January 2025
Chongqing Key Laboratory of New Drug Screening from Traditional Chinese Medicine, Integrative Science Center of Germplasm Creation in Western China (Chongqing) Science City, SWU-TAAHC Medicinal Plant Joint R&D Centre, College of Pharmaceutical Sciences, Southwest University, Chongqing, P. R. China.
Two new polyacetylenes, (5,12)-14-hydroxytetradeca-5,12-dien-8,10-diyn-1-yl 3-methylbut-2-enoate () and 5, 1'-(6,12)-1-hydroxytetradeca-6,12-dien-8,10-diyn-5-yl 2-methylbutanoate (), together with two known ones, (2,8)-12--methylbutyryltetradeca-2,8-diene-4,6-diyne-1,14-diol (), and ()-5-[5-(but-3-en-1-yn-1-yl)thiophen-2-yl]pent-2-en-4-yn-1-yl acetate () were isolated from the ethyl acetate extract of the roots of by various chromatographic methods, such as normal phase silica gel column, MPLC, and semi-preparative HPLC. Their structures were identified by kinds of spectroscopic methods including 1D NMR, 2D NMR, IR, UV, HR-ESI-MS, and ECD. Compound exhibited cytotoxic activities in HepG2 and Huh7 cells with IC values of 20.
View Article and Find Full Text PDFMolecules
December 2024
Department of Chemistry, William & Mary, Williamsburg, VA 23185, USA.
The development of new antibiotics with unique mechanisms of action is paramount to combating the growing threat of antibiotic resistance. Recently, based on inspiration from natural products, an asymmetrical polyacetylene core structure was examined for its bioactivity and found to have differential specificity for different bacterial species based on the substituents around the conjugated alkyne. This research further probes the structural requirements for bioactivity through a systematic synthesis and investigation of new compounds with variable carbon chain length, alkynyl subunits, and alcohol substitution.
View Article and Find Full Text PDFMolecules
December 2024
Graduate School of Pharmaceutical Sciences, College of Pharmacy, Ewha Womans University, Seoul 03760, Republic of Korea.
Leveille is a traditional medicine used to treat migraine headache and dysmenorrhea. In this study, three polyacetylenes, methyl (10,9,16)-16-acetoxy-9-hydroxyoctadeca-10,17-dien-12,14-diynoate (), methyl (10,9,16)-9,16-dihydroxyoctadeca-10-en-12,14-diynoate (), and methyl (10,9,16)-9,16-dihydroxyoctadeca-10,17-dien-12,14-diynoate (), were isolated from the aerial parts of . , together with seven known compounds (-).
View Article and Find Full Text PDFJ Nat Med
January 2025
College of Pharmacy, Chungnam National University, Daejeon, 34134, Republic of Korea.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!