linarin and Disease-Models--Animal

Osteoarthritis (OA) is one of the most common degenerative diseases, ultimately leading to long-term joint pain and severe articular malformation. Controlling local chronic inflammation is a crucial strategy for delaying OA development. Linarin is a natural flavonoid glycoside that is widely available in Compositae, Chrysanthemum indicum and Dendrocalamus and processes protective effects in several animal models. The purpose of our work was to study the protective effect of Linarin for OA. Cellular experiments data showed that Linarin suppressed lipopolysaccharide (LPS)-caused the overproduction of nitric oxide (NO), prostaglandin E2 (PGE2), interleukin-6 (IL-6) and tumour necrosis factor-alpha (TNF-α) in chondrocyte. In addition, LPS-stimulated expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide nitrate (iNOS) was decreased by Linarin pre-treatment. Together, Linarin prevented the catabiosis of extracellular matrix caused by LPS. For mechanism, Linarin inhibited the formation of Toll-like receptor 4 (TLR4) / myeloid differentiation protein-2 (MD-2) dipolymer complex and subsequently intervened NF-κB activation. Our mouse DMM model further clarified the protection of Linarin

Topics: Animals; Chondrocytes; Cyclooxygenase 2; Dinoprostone; Disease Models, Animal; Extracellular Matrix; Glycosides; Humans; Interleukin-6; Lipopolysaccharides; Lymphocyte Antigen 96; Menisci, Tibial; Mice; NF-kappa B; Nitric Oxide; Nitric Oxide Synthase Type II; Osteoarthritis; Toll-Like Receptor 4; Tumor Necrosis Factor-alpha

Topics: Administration, Oral; Animals; Chemical and Drug Induced Liver Injury; Chromatography, Liquid; Disease Models, Animal; Galactosamine; Glycosides; Liver; Male; Plasma; Rats; Spectrometry, Mass, Electrospray Ionization; Tandem Mass Spectrometry; Tissue Distribution

To assess protective effects of micronized purified flavonoid fraction (MPFF) on microcirculation in an original chronic model of hind limb venous hypertension with low blood flow in small animals.. Vein ligatures were performed on male hamsters, as follows: A-right femoral vein; A + B-right femoral vein and its right branch; A + C-right femoral vein and its left branch; A + B + C-right femoral and its right and left branches; D-external right iliac vein. In sham operated groups, similar vascular dissections were performed without ligatures. Superficial (epigastric) and central (jugular) venous pressure evaluations were made during a 10 week period. Hamsters subjected to A + B + C and D ligatures were selected for leukocyte rolling and sticking, functional capillary density (FCD), and venular and arteriolar diameter observations. D ligature was selected to evaluate pharmacological treatment efficacy. MPFF (100 mg/kg), concomitant active flavonoids of MPFF (diosmetin, hesperidin, linarin, and isorhoifolin) (10 mg/kg), diosmin (100 mg/kg) or drug vehicle were administered orally during 2 weeks before vein ligature and 6 weeks thereafter.. A, A + B and A + C models maintained venous return through collaterals. From the 2. MPFF was more effective than diosmin in improving all microvascular variables. The superiority of MPFF over diosmin alone can be explained by the synergistic beneficial effects of the association between diosmin and active flavonoids of MPFF.

Topics: Animals; Capillary Permeability; Cricetinae; Diosmin; Disease Models, Animal; Drug Evaluation, Preclinical; Flavonoids; Glycosides; Hesperidin; Hypertension; Iliac Vein; Male; Microcirculation; Reperfusion Injury

The flowers or leaves of Chrysanthemum boreale (Compositae) have been traditionally used as herb tea to reduce anxiety, insomnia, and stress. Sedative and anticonvulsant activities were evaluated in mice using pentobarbital-induced sleeping assay and pentylenetetrazole (PTZ)-induced convulsion assay. The flower extract exhibited more potent activities than the extracts of the leaves and stems, and chromatographic isolation yielded the five compounds acacetin, linarin, acacetin 7-O-β-D-glucopyranosyl-(1 → 2)[α-L-rhamnopyranosyl-(1 → 6)]-β-D-glucopyranoside, chlorogenic acid, and 3,5-di-O-caffeoylquinic acid. These compounds were simultaneously analyzed by HPLC, and the method was validated. The contents of linarin, which were shown to be most abundant in C. boreale, were observed in the order of leaf (11.93 mg/g) > flower (8.50 mg/g) > stem (5.60 mg/g). Linarin and its aglycone, acacetin, exhibited sedative and anticonvulsant activities in the present in vivo assays. It can be considered that linarin is one of the active compounds effective against anxiety, insomnia, and stress, with acacetin as its active moiety.

Topics: Animals; Anticonvulsants; Anxiety; Chromatography, High Pressure Liquid; Chrysanthemum; Disease Models, Animal; Flavones; Flowers; Glycosides; Hypnotics and Sedatives; Male; Mice; Mice, Inbred ICR; Molecular Structure; Plant Leaves; Plant Stems; Reflex, Righting; Seizures