casticin and Inflammation

This short review provides an update of the anticancer and anti-inflammatory properties of casticin from Vitex species. Casticin is a polymethylflavone with three rings, an orthocatechol moiety, a double bond, two hydroxyl groups and four methoxyl groups. Casticin has been isolated from various tissues of plants in the Vitex genus: fruits and leaves of V. trifolia, aerial parts and seeds of V. agnus-castus and leaves of V. negundo. Studies have reported the antiproliferative and apoptotic activities of casticin from Vitex species. The compound is effective against many cancer cell lines via different molecular mechanisms. Studies have also affirmed the anti-inflammatory properties of casticin, with several molecular mechanisms identified. Other pharmacological properties include anti-asthmatic, tracheospasmolytic, analgesic, antihyperprolactinemia, immunomodulatory, opioidergic, oestrogenic, anti-angiogenic, antiglioma, lung injury protection, rheumatoid arthritis amelioration and liver fibrosis attenuation activities. Clinical trials and commercial use of the casticin-rich fruit extract of V. agnus-castus among women with premenstrual syndrome were briefly discussed.

Topics: Animals; Anti-Inflammatory Agents; Flavonoids; Humans; Inflammation; Neoplasms; Plant Extracts; Vitex

Casticin, an active compound isolated from Vitex rotundifolia L., was reported to possess anti-inflammatory activity. However, the effect of casticin on inflammatory response in human osteoarthritis (OA) chondrocytes remains unclear. In the current study, we examined the anti-inflammatory effects of casticin on chondrocytes exposed to interleukin-1β (IL-1β). Our results demonstrated that casticin treatment significantly improved cell viability in chondrocytes exposed to IL-1β. Casticin significantly inhibited IL-1β-induced NO and PGE2 production, and iNOS and COX-2 expression in human OA chondrocytes. It also suppressed the levels of TNF-α and IL-6, as well as decreased production of MMP-3, MMP-13, ADAMTS-4 and ADAMTS-5 in IL-1β-stimulated chondrocytes. Furthermore, casticin prevented IL-1β-induced NF-κB activation in chondrocytes. Taken together, these findings showed that casticin attenuates inflammatory responses in chondrocytes stimulated with IL-1β, possibly through the NF-κB signaling pathway. Thus, casticin may serve as a potential anti-inflammatory agent in the treatment of OA.

Topics: ADAMTS Proteins; Cell Survival; Chondrocytes; Cyclooxygenase 2; Cytoprotection; Dinoprostone; Flavonoids; Gene Expression Regulation, Enzymologic; Humans; Inflammation; Interleukin-1beta; Interleukin-6; Matrix Metalloproteinases; Nitric Oxide; Nitric Oxide Synthase Type II; Osteoarthritis; Signal Transduction; Transcription Factor RelA; Tumor Necrosis Factor-alpha

The aim of our experiments was to investigate the anti-inflammatory properties of casticin and chrysosplenol D, two flavonoids present in Artemisia annua L.. Topical inflammation was induced in ICR mice using croton oil. Mice were then treated with casticin or chrysosplenol D. Cutaneous histological changes and edema were assessed. ICR mice were intragastrically administrated with casticin or chrysosplenol D followed by intraperitoneal injection of lipopolysaccharide (LPS). Mouse Raw264.7 macrophage cells were incubated with casticin or chrysosplenol D. Intracellular phosphorylation was detected, and migration was assessed by trans-well assay. HT-29/NFκB-luc cells were incubated with casticin or chrysosplenol D in the presence or absence of LPS, and NF-κB activation was quantified.. In mice, administration of casticin (0.5, 1 and 1.5μmol/cm(2)) and chrysosplenol D (1 and 1.5μmol/cm(2)) inhibited croton oil-induced ear edema (casticin: 29.39-64.95%; chrysosplenol D: 37.76-65.89%, all P<0.05) in a manner similar to indomethacin (0.5, 1 and 1.5μmol/cm(2); 55.63-84.58%). Casticin (0.07, 0.13 and 0.27mmol/kg) and chrysosplenol D (0.07, 0.14 and 0.28mmol/kg) protected against LPS-induced systemic inflammatory response syndrome (SIRS) in mice (all P<0.05), in a manner similar to dexamethasone (0.03mmol/kg). Casticin and chrysosplenol D suppressed LPS-induced release of IL-1 beta, IL-6 and MCP-1, inhibited cell migration, and reduced LPS-induced IκB and c-JUN phosphorylation in Raw264.7 cells. JNK inhibitor SP600125 blocked the inhibitory effect of chrysosplenol D on cytokine release.. The flavonoids casticin and chrysosplenol D from A. annua L. inhibited inflammation in vitro and in vivo.

Topics: Animals; Artemisia annua; Dermatitis; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Edema; Flavones; Flavonoids; HT29 Cells; Human Umbilical Vein Endothelial Cells; Humans; Inflammation; Male; Mice; Mice, Inbred ICR

To investigate the anti-inflammatory effect of casticin of Fructus Viticis.. Observations were made on the anti-inflammatory effect of casticin in the models of acute inflammation in vivo.. Casticin inhibited significantly xylene-induced mouse ear edema, egg albumen-induced rat paw edema and acetic acid-induced mouse vascular permeability.. Casticin has significant anti-inflammatory effect on acute inflammation, which is probably related to the inhibition of the inflammation factors. Casticin is the effective constituent contributing to the anti-inflammatory effect of Fructus Viticis.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Capillary Permeability; Edema; Flavonoids; Inflammation; Mice; Mice, Inbred ICR; Rats; Rats, Sprague-Dawley