Antifungal activity of Terminalia australis.

Dichloromethane, methanol and aqueous extracts of the aerial parts of Terminalia australis were evaluated for their antifungal activity. The methanol and aqueous extracts were found to be effective against the tested Aspergillus and Candida strains.

Identification of phenolic compounds in Equisetum giganteum by LC-ESI-MS/MS and a new approach to total flavonoid quantification.

Equisetum giganteum L., commonly called "giant horsetail", is an endemic species of Latin America. Its aerial parts have been widely used in ethnomedicine as a diuretic and in herbal medicine and food supplements as a raw material. The phenolic composition of E. giganteum stems was studied by liquid chromatography coupled to diode array detection (LC-DAD) and liquid chromatography coupled to electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS), which identified caffeic acid derivatives, flavonoids and styrylpyrones. The most abundant glycosilated flavonoids in this sample were kaempferol derivatives. Other rare phenolic components, namely, quercetin-3-O-(caffeoyl)-glucoside and 3-hydroxyhispidin-3,4'-di-O-glucoside, were reported for first time in the Equisetum genus. An LC-UV method for the simultaneous quantification of flavonoid aglycones in E. giganteum obtained after hydrolysis was developed and validated. The method exhibited excellent linearity for all analytes, with regression coefficients above 0.998, LOD ≥ 0.043µg mL(-1), LOQ ≥ 0.158 µg mL(-1) and recovery rates of 96.89-103.33% and 98.22-102.49% for quercetin and kaempferol, respectively. The relative standard deviation for the intra- and inter-day precision was ≤ 3.75%. The hydrolysis process was optimized by central composite rotational design and response surface analysis. The second-order response models for the aglycones contents were as follows: quercetin (µg g(-1))=24.8102+55.2823 × HCl+0.776997 × Time-7.23852 × HCl(2)-7.46528E-04 × Time(2)-0.229167 × HCl × Time; kaempferol (µg g(-1))=-9.66755+974.822 × HCl+11.8059 × Time-130.612 × HCl(2)-0.0125694×Time(2) -3.22917 × HCl × Time, with estimated optimal conditions of 1.18 M HCl and 205 min of hydrolysis. The results obtained with these new methods were compared to those from a spectrophotometric assay used to determine the total flavonoids in the Equisetum arvense monograph (Horsetail, British Pharmacopoeia 2011). For all four species analyzed (E. giganteum, E. arvense, E. hyemale and E. bogotense), the calculated aglycone content was higher using the optimized hydrolysis conditions. Additionally, the LC method was more appropriate and specific for quantitative analysis.

Anti-inflammatory activity of berenjenol and related compounds.

Berenjenol (1), isolated from Oxandra cf. xylopioides (Annonaceae), was tested on two different experimental models of inflammation. The compound showed anti-inflammatory activity in the test of acute mouse ear edema induced by TPA (54% inhibition, 1 micromol/ear) as well as in the test of subchronic inflammation induced by repeated application of TPA (57% inhibition, 7x1 micromol/ear). Moreover, while it reduced the expression of both COX-2 (65% inhibition at 50 microM) and iNOS (80% inhibition at 50 microM), it was not active against TNF-alpha and IL-1 beta in murine macrophages (RAW 264.7) stimulated with LPS. Structural modification of 1 gave two derivatives, berenjenol acetate (2) and 3-oxo-berenjenol (3). Of these, the latter had a high degree of activity in the acute test (66% inhibition, 1.1 micromol/ear), whereas the former showed no enhanced pharmacological properties. Interestingly, the original compound exhibited higher activity than either of its derivatives in the subchronic model. We thus concluded that whereas 3-oxidation of 1 (compound 3), but not 3-acetylation (2), increases the activity in the acute model of inflammation, structural modification of 1 does not enhance the compound's effects in the subchronic model.

Anti-inflammatory activity of Heterotheca subaxillaris var. latifolia (Buckley) Gandhi & R.D. Thomas, Asteraceae

The anti-inflammatory activity of the petroleum ether, dichloromethane and methanol extracts from Heterotheca subaxillaris var. latifolia were assayed using 12-O-tetradecanoyl phorbol acetate (TPA) induced ear edema test in mice and carrageenan-induced paw edema test in rats. The dichloromethane extract showed a significant anti-inflammatory activity (91 percent of inhibition) in TPA-induced ear edema test (topical administration at 1 mg/ear). No effects were seen on carragenan-induced edema. Bio-guided fractionation deal to the isolation of the major flavonoids santin, pectolinaringenin, 3,6-dimethoxy-5,7,4'-trihydroxyflavone and hispidulin present in the active fractions.

A atividade antiinflamatória de extratos éter petróleo, diclorometânico e metanólico de Heterotheca subaxillaris var. latifolia, foi testada pelo método de edema induzido pelo 12-O-tetradecanoil phorbol acetato (TPA) na orelha do camundongos e pelo método do edema de pata induzido por carragenina em ratos. O extrato diclorometânico mostrou atividade antiinflamatória significativa (91 por cento inibição) no edema de orelha induzido por TPA (administração tópica de 1 mg/orelha). Não houve efeitos significativos no teste do edema induzido pela carragenina. O fracionamento bioguiado das frações ativas levou ao isolamento dos flavonoides majoritários santina, pectolinaringenina, 3,6-dimetoxi-5, 7,4 '-trihidroxiflavona e hispidulina.