Effects of caffeoylquinic acid derivatives and C-flavonoid from Lychnophora ericoides on in vitro inflammatory mediator production.

In this study we aimed at evaluating the effect of the major polar constituents of the medicinal plant Lychnophora ericoides on the production of inflammatory mediators produced by LPS-stimulated U-937 cells. The 6,8-di-C-beta-glucosylapigenin (vicenin-2) presented no effect on tumor necrosis factor (TNF)-alpha production, but inhibited, in a dose-dependent manner, the production of prostaglandin (PG) E2 without altering the expression of cyclooxygenase (COX)-2 protein. 3,5-Dicaffeoylquinic acid and 4,5-dicaffeoylquinic acid, at lower concentrations, had small but significant effects on reducing PGE2 levels; at higher doses these compounds stimulated PGE2 and also TNF-alpha production by the cells. All the caffeoylquinic acid derivatives, in a dose-dependent fashion, were able to inhibit monocyte chemoattractant protein-3 synthesis/release, with 4,5-DCQ being the most potent at the highest tested concentration. These results add important information on the effects of plant natural polyphenols, namely vicenin-2 and caffeoylquinic acid derivatives, on the production of inflammatory mediators by cultured cells.

A new high-performance liquid chromatography assay for the determination of sesquiterpene lactone 15-deoxygoyazensolide in rat plasma.

A simple, rapid and sensitive high-performance liquid chromatography method was developed for the analysis of the sesquiterpene lactone 15-deoxygoyazensolide (LAC15-D) in rat plasma samples. The chromatographic separation was achieved on a LiChrospher RP18 column using methanol:water (50:50, v/v) containing 0.6% acetic acid as mobile phase, at a flow rate of 0.7 mL min(-1). UV detection was carried out at 270 nm. Phenytoin was used as internal standard. Prior to the analysis, the rat plasma samples were submitted to liquid-liquid extraction with dichloromethane. The mean absolute recoveries were 73% with R.S.D. values lower than 3.5. The method was linear over the 6.0-2000 ng mL(-1) concentration range and the quantification limit was 6.0 ng mL(-1). Within-day and between-day assay precision and accuracy were studied at three concentration levels (15, 300 and 480 ng mL(-1)) and were lower than 15%. The validated method was used to measure the plasmatic concentration of LAC15-D in rats that received a single intraperitoneal dose of 30 mg kg(-1).

Evaluation of the anti-inflammatory, analgesic and antipyretic activities of the natural polyphenol chlorogenic acid.

Phenolic compounds are numerous and ubiquitous in the plant kingdom, being particularly present in health-promoting foods. Epidemiological evidences suggest that the consumption of polyphenol-rich foods reduces the incidence of cancer, coronary heart disease and inflammation. Chlorogenic acid (CGA) is one of the most abundant polyphenol compounds in human diet. Data obtained from in vivo and in vitro experiments show that CGA mostly presents antioxidant and anti-carcinogenic activities. However, the effects of CGA on the inflammatory reaction and on the related pain and fever processes have been explored less so far. Therefore, this study was designed to evaluate the anti-inflammatory, antinociceptive and antipyretic activities of CGA in rats. In comparison to control, CGA at doses 50 and 100 mg/kg inhibited carrageenin-induced paw edema beginning at the 2nd hour of the experimental procedure. Furthermore, at doses 50 and 100 mg/kg CGA also inhibited the number of flinches in the late phase of formalin-induced pain test. Such activities may be derived from the inhibitory action of CGA in the peripheral synthesis/release of inflammatory mediators involved in these responses. On the other hand, even at the highest tested dose (200 mg/kg), CGA did not inhibit the febrile response induced by lipopolysaccharide (LPS) in rats. Additional experiments are necessary in order to clarify the true target for the anti-inflammatory and analgesic effects of CGA.

Analgesic activity of di-caffeoylquinic acids from roots of Lychnophora ericoides (Arnica da serra).

The Brazilian medicinal plant Lychnophora ericoides Mart. (Asteraceae) has been used in traditional medicine to treat wounds, pain and inflammation. As part of our continuing investigation of this commercial phytomedicine, we focused on the polar fractions of the plant, since it is employed as alcoholic and hydroalcoholic preparations. The analgesic bioguided fractionation of the root polar extract yielded 3,5-di-O-[E]-caffeoylquinic acid, 4,5-di-O-[E]-caffeoylquinic acid and 3,4,5-tri-O-[E]-caffeoylquinic acid. The n-butanol fraction and the di-caffeoylquinic acids showed significant analgesic activity in the acetic acid-induced mouse writhing test at low but not at high doses. These findings support, at least in part, the validity of the use of Lychnophora ericoides roots in traditional medicine.