| Description: |
Pectolinarin has antioxidant, antiobesity, analgesic, and hepatoprotective activity, it may inhibit eicosanoid formation in inflammatory lesions. |
| Targets: |
COX | NF-kB | PGE |
| In vitro: |
| Food Sci. Biotech., 2015, 24(6):2235-43. | | Assessment of the pectolinarin content and the radical scavenging-linked antiobesity activity of Cirsium setidens Nakai extracts.[Reference: WebLink] | Cirsium setidens Nakai contains bioactive compounds that exert biological activities.
METHODS AND RESULTS:
Method validation for analysis of the pectolinarin content in Cirsium setidens extracts (CSE) and radical scavenging-linked antiobesity activities using 3T3-L1 cells and C57BL/6 mice were performed. The pectolinarin content of CSE was 2.81±0.01 mg/g with a high degree of linearity in calibration curves (R 2=0.9999). CSE exhibited free radical-scavenging activities and a reducing power. CSE and pectolinarin inhibited lipid accumulation during adipogenesis of 3T3-L1 cells via down-regulation of adipogenic transcription factors. CSE supplementation suppressed body weight in C57BL/6 mice fed a high fat diet and reduced plasma total cholesterol, triglyceride, insulin, and glucose levels.
CONCLUSIONS:
Pectolinarin-enriched CSE can be considered as a good source of natural antioxidants and antiobesity ingredients. | | J Cell Biochem . 2019 Sep;120(9):15202-15210. | | Pectolinarin inhibits proliferation, induces apoptosis, and suppresses inflammation in rheumatoid arthritis fibroblast-like synoviocytes by inactivating the phosphatidylinositol 3 kinase/protein kinase B pathway[Pubmed: 31020684] | | Abstract
Rheumatoid arthritis fibroblast-like synoviocytes (RA-FLSs), a pathological hallmark of rheumatoid arthritis (RA), exhibit the characteristics of tumor cells. The extracts of Cirsium japonicum var. ussuriense have been shown to possess antitumor and anti-inflammatory activities. Our study aimed to investigate the effects of pectolinarin, a flavonoid compound isolated from C. japonicum var. ussuriense, on RA. Cell viability was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide assay. Apoptosis was determined by flow cytometry analysis and Western blot analysis of Bax and Bcl-2 levels. Inflammation was assessed by detecting the expressions and secretion of interleukin (IL)-6 and IL-8 using quantitative real-time polymerase chain reaction and enzyme-linked immunosorbent assay, respectively. The production of nitric oxide (NO) and prostaglandin E2 (PGE2) was also measured. The effects of pectolinarin on the phosphatidylinositol 3 kinase (PI3K)/protein kinase B (Akt) pathway were examined by Western blot. We found that pectolinarin significantly inhibited cell viability at 24 and 48 hours in a dose-dependently manner in RA-FLSs. Pectolinarin reduced the apoptotic rate, increased Bax level, and decreased Bcl-2 level in RA-FLSs. Pectolinarin inhibited the messenger RNA expression and secretion of IL-6 and IL-8, as well as the production of PGE2 and NO in RA-FLSs. Furthermore, pectolinarin inactivated the phosphatidylinositol 3 kinase/protein kinase B (PI3K/Akt) pathway in RA-FLSs. Activation of the PI3K/Akt pathway by 740Y-P impaired the effects of pectolinarin on cell viability, apoptosis, and inflammation in RA-FLSs. In conclusion, pectolinarin suppressed cell proliferation and inflammatory response and induced apoptosis in RA-FLSs via inactivation of the PI3K/Akt pathway.
Keywords: apoptosis; inflammation; pectolinarin; rheumatoid arthritis fibroblast-like synoviocytes; the phosphatidylinositol 3 kinase/protein kinase B pathway. |
|
| In vivo: |
| Biol Pharm Bull. 2008 Nov;31(11):2063-7. | | Anti-inflammatory activity of pectolinarigenin and pectolinarin isolated from Cirsium chanroenicum.[Pubmed: 18981574] |
METHODS AND RESULTS:
In order to identify the active anti-inflammatory ingredient(s) in Cirsium chanroenicum (Compositae), its methanol extract and several solvent fractions were prepared; the methanol extract and the ethylacetate fraction inhibited cyclooxygenase-2 (COX-2)-mediated prostaglandin E2 (PGE2) and 5-lipoxygenase (5-LOX)-mediated leukotriene (LT) production in lipopolysaccharide-treated RAW 264.7 cells and A23187-treated rat basophilic leukemia (RBL-1) cells, respectively. Further bioactivity-guided fractionation of the ethylacetate fraction using column chromatography led to the isolation of pectolinarigenin (5,7-dihydroxy-4',6-dimethoxyflavone), along with pectolinarin [pectolinarigenin 7-rhamnosyl-(1-->6)-glucoside]. Pectolinarigenin strongly inhibited COX-2-mediated PGE2 and 5-LOX-mediated LT production at >1 microM, indicating that it is a dual inhibitor of COX-2/5-LOX. However, pectolinarigenin did not affect COX-2 expression or nuclear transcription factor (NF-kappaB) activation. In addition, in vivo studies demonstrated that oral administration of these two compounds at 20-100 mg/kg resulted in similar inhibitory activities against several animal models of inflammation/allergy: arachidonic acid-induced mouse ear edema, carrageenan-induced mouse paw edema and passive cutaneous anaphylaxis.
CONCLUSIONS:
All of these results suggest that pectolinarigenin and pectolinarin possess anti-inflammatory activity and that they may inhibit eicosanoid formation in inflammatory lesions. These activities certainly contribute to the anti-inflammatory mechanism of C. chanroenicum. | | Planta Med. 1998 Mar;64(2):134-7. | | A comparative study of the analgesic and anti-inflammatory activities of pectolinarin isolated from Cirsium subcoriaceum and linarin isolated from Buddleia cordata.[Pubmed: 9525105] |
METHODS AND RESULTS:
The dried aqueous extract of aerial parts of Cirsium subcoriaceum (Asteraceae) and its major flavonoid glycoside, pectolinarin, have been evaluated for analgesic and anti-inflammatory effects in mice and rats, respectively. Both the extract and pectolinarin exerted significant and dose-dependent analgesic and anti-inflammatory activities. Also, the anti-inflammatory activities of an aqueous extract of Buddleia cordata and its principal glycoside linarin were evaluated.
CONCLUSIONS:
The results of pharmacological testing proved that linarin is a better anti-inflammatory agent than pectolinarin and indomethacin. On the other hand, pectolinarin exerted a better analgesic effect than linarin. |
|
Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
