In the search for potential antiobese agents from natural sources, this study investigated the effects of betulinic acid (BA), a pentacyclic triterpene from Clusia nemorosa L. (Clusiaceae), in mice on a high-fat diet (HFD). Adult male Swiss mice (n = 8) treated or not with BA (50 mg/L, in drinking water) were fed a HFD during 15 weeks. Mice treated with BA and fed a HFD showed significantly (P < 0.05) decreased body weights, abdominal fat accumulation, blood glucose, plasma triglycerides, and total cholesterol relative to their respective controls fed no BA. Additionally, BA treatment, while significantly elevating the plasma hormone levels of insulin and leptin, decreased the level of ghrelin. However, it caused a greater decrease in plasma amylase activity than the lipase. These findings suggest that BA has an antiobese potential through modulation of fat and carbohydrate metabolism, and it may be a suitable lead compound in the treatment of obesity.

We have evaluated the in-vitro and in-vivo antitumour activity of physalin B and physalin D isolated from the aerial parts of Physalis angulata. In-vitro, both compounds displayed considerable cytotoxicity against several cancer cell lines, showing IC50 values in the range of 0.58 to 15.18 microg mL(-1) for physalin B, and 0.28 to 2.43 microg mL(-1) for physalin D. The antitumour activity of both compounds was confirmed in-vivo using mice bearing sarcoma 180 tumour cells. The in-vivo antitumour activity was related to the inhibition of tumour proliferation, as observed by the reduction of Ki67 staining in tumours of treated animals. Histopathological examination of the kidney and liver showed that both organs were affected by physalin treatment, but in a reversible manner. These compounds were probably responsible for the previously described antitumour activity of ethanol extracts of P. angulata, and their identification and characterization presented here could explain the ethnopharmacological use of this species in the treatment of cancer.

Many authors have already emphasized that phytochemicals from spices have biological applications. Piperlonguminine is a known alkaloid amide from peppers, including Piper divaricatum. The aim of this study was to investigate the in vitro and in vivo antitumor effects of piperlonguminine in experimental models. In order to evaluate the toxicological aspects related to piperlonguminine treatment, hematological, biochemical, histopathological and morphological analyses of treated animals were performed. Piperlonguminine did not show any significant in vitro cytotoxic effect at experimental exposure levels, but showed an in vivo antitumor effect. After 7 days of treatment, the inhibition rates were 38.71% and 40.68% at doses of 25 mg kg(-1) and 50 mg kg(-1), respectively. The histopathological analysis suggests that the liver and kidney were only weakly affected by piperlonguminine treatment. Neither the enzymatic activity of transaminases (AST and ALT) nor the urea levels were significantly altered. In the hematological analysis, all parameters analysed remained constant after piperlonguminine treatment. In conclusion, these data reinforce the anticancer potential of spice components.

Phytochemical analysis of the leaves of Acnistus arborescens (Solanaceae) resulted in the isolation of two new epimeric withaphysalins (17S,20R,22R)-5beta,6beta: 18,20-diepoxy-4beta,18-dihydroxy-1-oxowitha-24-enolide (2, 18R and 18S), together with the known withaphysalin F (1, 18R and 18S). Their structures were established by spectroscopic methods, including 2D NMR data and comparison with literature data. Compounds 1 and 2 dis-played potent cytotoxic activities against several cancer cell lines with IC50 values in the range of 0.20 to 1.46 microg/mL for 1 and 0.89 to 8.08 microg/mL for 2. The strong cytotoxicity presented by 1 suggests that in this series of compounds, the 2,3-unsaturated ketone moiety is an important pharmacophoric unit. The cytotoxic activity seemed to be related to DNA synthesis inhibition, as revealed by the reduction of 5-bromo-2'-deoxyuridine incorporation after 24 hours of incubation on leukemic cells.

The anti-inflammatory effect of physalin E, a seco-steroid isolated from Physalis angulata L. was evaluated on acute and chronic models of dermatitis induced by 12-O-tetradecanoyl-phorbol-13-acetate (TPA) and oxazolone, respectively, in mouse ear. The changes in ear edema/thickness, production of pro-inflammatory cytokines (TNF-alpha and IFN-gamma), myeloperoxidase (MPO) activity, and histological and immunohistochemical findings were analysed, as indicators of dermal inflammation. Similar to dexamethasone, topically applied Physalin E (0.125; 0.25 and 0.5 mg/ear) potently inhibited the TPA and oxazolone-induced dermatitis, leading to substantial reductions in ear edema/thickness, pro-inflammatory cytokines, and MPO activity. These effects were reversed by mifepristone, a steroid antagonist and confirmed by immunohistochemical and histopathological analysis. The data suggest that physalin E may be a potent and topically effective anti-inflammatory agent useful to treat the acute and chronic skin inflammatory conditions.

Croton regelianus Muell. Arg., popularly known as 'velame-de-cheiro', is a native plant from the Northeast of Brazil used in folk medicine to treat diseases of different kinds, including malignant tumors. In this study, the in vitro and in vivo antitumor effects of the essential oil from the leaves of C. regelianus and ascaridole, one of the main constituents, were investigated. In vitro, the essential oil and ascaridole displayed cytotoxicity, showing IC(50) values in the range of 22.2 to 48.0 microg/ml in HL-60 and SF-295 cell lines for the essential oil, and 6.3 to 18.4 microg/ml in HL-60 and HCT-8 cells lines for ascaridole, respectively. The in vivo study, using sarcoma 180 as a tumor model, demonstrated inhibition rates of 28.1 and 31.8% for essential oil, at the 50 and 100 mg/kg, while ascaridole inhibition rates were 33.9% at 10 mg/kg and 33.3% at 20-mg/kg doses. Histopathological examination showed that the organs were only weakly affected by the treatment. In conclusion, ascaridole has an interesting antitumor activity in sarcoma 180 murine model, probably related to the described cytotoxic activity, and, moreover, its presence in the essential oil from the leaves of C. regelianus could explain, at least in part, the ethnopharmacological use of this plant in the treatment of cancer.

No abstract

Um novo sesquiterpeno, nomeado trichotomol e compostos conhecidos como cordiacromo C, α-cadinol, ácido oleanólico, oncocalyxona A, β-sitosterol, glicosídeo do β-sitosterol, alantoína e sacarose foram isolados a partir do extrato etanólico do cerne de Cordia trichotoma. Suas estruturas foram determinadas por análises espectroscópicas e comparação com dados publicados para compostos estruturalmente relacionados.A new sesquiterpene, named trichotomol, and known compounds cordiachrome C, α-cadinol, oleanolic acid, oncocalyxone A, β-sitosterol, β-sitosterol-β-D-glucoside, allantoin and sucrose were isolated from the heart wood ethanol extract of Cordia trichotoma. Their structures were assigned unambiguously by spectroscopic analyses and comparison with the published data for structurally related compounds.