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.

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.

Three withaphysalins, rel-(17S,20R,22R)-5 beta,6 beta:18,20-diepoxy-4 beta-hydroxy-1,18-dioxowitha-2,24-dienolide(withaphysalin M) (1), rel-(17S,20R,22R)-5 beta,6 beta:18,20-diepoxy-4 beta-hydroxy-18-ethoxy-1-oxowitha-2,24-dienolide (withaphysalin F ethyl ether, withaphysalin O) (2), and rel-(17S,20R,22R)-5 beta,6 beta:18,20-diepoxy-4 beta-hydroxy-1,18-dioxowitha-24-enolide (withaphysalin N) (3), were isolated from the leaves of Acnistus arborescens. The structures were deduced from 1D ((1)H NMR, (13)C NMR, DEPT-(13)C NMR) and 2D (COSY, HMQC, HMBC) NMR analysis and the relative stereochemical assignments based on 1D NOESY correlations and analysis of coupling constants. Compounds 1 and 2 displayed potent cytotoxic activity against a panel of human cancer cell lines.

No abstract

Physalins D (1), B (2), F (3), 5α-ethoxy-6β-hydroxy-5,6-dihydrophysalin B (4) and E (5), all isolated from Physalis angulata L. extracts, were tested for cytotoxic activity using a panel of tumor cell lines and sea urchin eggs. In general, the most active compounds were 1 and 3, followed by 2 and 4. Compound 4a obtained by the hydrogenation of 4 was weaker than all the others in tumor cells and possessed no activity in sea urchin eggs. Compound 5 had no activity in tumor cells and exhibited activity in sea urchin eggs only in the third cleavage and blastulae. The present data suggest that the cytotoxic effect of physalins is probably determined by the combination of the conjugated cyclohexanone moiety and the presence of an oxygen located at both C-5 and C-6.

Duas novas ceramidas N-(4-hidroxifeniletil)octacosamida (1) e rel-(2S,3S,4R,16E)-2-[(2'R)-2'-hidroxinonadecanoilamino]-heneicosadec-16-eno-1,3,4-triol (2) foram isoladas do extrato etanólico de Acnistus arborescens. As estruturas foram elucidadas por métodos espectroscópicos (experimentos de RMN 1D e 2D, EMAR com ionização por electrospray, EM e IV). (2) were isolated from the EtOH extract of Acnistus arborescens. The structures were elucidated by spectroscopic (1D and 2D NMR experiments, HR-ESI-MS, LR-MS and IR) methods. Two new ceramides, N-(4-hydroxyphenethyl)octacosamide (1) and rel-(2S,3S,4R,16E)-2-

No abstract