Pectolinarin

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.

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.

Biol Pharm Bull. 2008 Apr;31(4):760-4.

Pectolinarin and Pectolinarigenin of Cirsium setidens Prevent the Hepatic Injury in Rats Caused by D-Galactosamine via an Antioxidant Mechanism.[Pubmed: 18379079]

To identify the hepatoprotective component from the leaves of Cirsium setidens (Compositae), the methanolic extract was divided into two fractions, chloroform and butanol fractions, and their hepatoprotective efficacy was evaluated in a rat model of hepatic injury caused by D-galactosamine (GalN).
METHODS AND RESULTS:
Hepatoprotective activity was measured by the activity of serum aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), and lactate dehydrogenase (LDH). Glutathione metabolism was measured via biochemical parameters such as glutathione (GSH), glutathione reductase (GR), gamma-glutamylcysteine synthetase (GCS), glutathione S-transferase (GST), and superoxide dismutase (SOD) levels. We subjected the butanol fraction, which had higher activity, to column chromatography to yield Pectolinarin, which was further hydrolyzed to yield pectolinarigenin. Administration (10, 20 mg/kg, p.o.) of the main flavonoid glycoside component, Pectolinarin, and its aglycone, pectolinarigenin, for 2 weeks significantly decreased the activity levels of AST, ALT, ALP and LDH, indicating that the two compounds have hepatoprotective activity. Pectolinarin and pectolinarigenin also increased activity levels of GSH, GR, GCS, and GST, as well as SOD. The significant effect was only seen in SOD activity.
CONCLUSIONS:
This suggests that the two components exhibit hepatoprotective activity mainly via SOD antioxidant mechanism.