Rosy Caniato

Hyperforin Inhibits Cancer Invasion and Metastasis

Hyperforin (Hyp), the major lipophilic constituent of St. John’s wort, was assayed as a stable dicyclohexylammonium salt (Hyp-DCHA) for cytotoxicity and inhibition of matrix proteinases, tumor invasion, and metastasis. Hyp-DCHA triggered apoptosis-associated cytotoxic effect in both murine (C-26, B16-LU8, and TRAMP-C1) and human (HT-1080 and SK-N-BE) tumor cells; its effect varied, with B16-LU8, HT-1080, and C-26 the most sensitive (IC50 = 5 to 8 μmol/L). At these concentrations, a marked and progressive decline of growth was observed in HT-1080 cells, whereas untransformed endothelial cells were only marginally affected. Hyp-DCHA inhibited in a dose-dependent and noncompetitive manner various proteinases instrumental to extracellular matrix degradation; the activity of leukocyte elastase was inhibited the most (IC50 = 3 μmol/L), followed by cathepsin G and urokinase-type plasminogen activator, whereas that of the matrix metalloproteinases (MMPs) 2 and 9 showed an IC50 > 100 μmol/L. Nevertheless, inhibition of extracellular signal-regulated kinase 1/2 constitutive activity and reduction of MMP-2 and MMP-9 secretion was triggered by 0.5 μmol/L Hyp-DCHA to various degrees in different cell lines, the most in C-26. Inhibition of C-26 and HT-1080 cell chemoinvasion (80 and 54%, respectively) through reconstituted basement membrane was observed at these doses. Finally, in mice that received i.v. injections of C-26 or B16-LU8 cells, daily i.p. administration of Hyp-DCHA—without reaching tumor-cytotoxic blood levels—remarkably reduced inflammatory infiltration, neovascularization, lung weight (−48%), and size of experimental metastases with C-26 (−38%) and number of lung metastases with B16-LU8 (−22%), with preservation of apparently healthy and active behavior. These observations qualify Hyp-DCHA as an interesting lead compound to prevent and contrast cancer spread and metastatic growth.

Anthocyanins and xanthones in the calli and regenerated shoots of Hypericum perforatum var. angustifolium (sin. Fröhlich) Borkh.

The present paper reports on the production of anthocyanins and xanthones in different in vitro systems of Hypericum perforatum var. angustifolium (sin. Fröhlich) Borkh. Undifferentiated calli and regenerated shoots at different developmental stages were analyzed by applying an extractive and an analytical procedure capable of detecting and quantifying anthocyanins. The findings revealed, for the first time, the co-presence of hypericins and anthocyanins in shoots at initial and more developed stages of H. perforatum var. angustifolium L. Moreover, a high production of xanthones was found in the undifferentiated calli.

In vivo and in vitro production of alkaloids by Haplophyllum patavinum.

A protocol for shoot induction from callus of Haplophyllum patavinum was established. Two known furoquinoline (skimmianine and haplopine), and three quinolone (edulinine, ribalinine and isoplatydesmine) alkaloids were isolated for the first time from plant material, callus and shoot cultures of this species. The structures of these compounds have been characterised on the basis of spectroscopic evidence.

Fucoxanthin from Undaria pinnatifida: Photostability and Coextractive Effects

Fucoxanthin is one of the most abundant carotenoids and possesses a number of beneficial medicinal qualities which include its anti-oxidant, anti-obesity and anti-cancer properties. In this study, the photostability of fucoxanthin in extracts with different chemical profiles was studied. The extracts were obtained from Undaria pinnatifida, a seaweed rich in this carotenoid, using conventional liquid solvent extraction procedures and the QuEChERS method. All the extracts contained all-trans-fucoxanthin as the major compound. Conventional procedures produced a fucoxanthin purity of lower than 50%, whereas after liquid-liquid partition, PSA cleanup, and PSA and GCB cleanup (QuEChERS method) fucoxanthin purity increased to 70%, 86%, and 94%, respectively. Although in the acetone extract the initial content of fucoxanthin was the highest, results demonstrate that coextractives play an important role in enhancing the rate of photodegradation. After light exposure, the conventional extracts lost around 90% of the initial fucoxanthin content. On the other hand, the extracts obtained by the QuEChERS method showed significantly higher light stability than the conventional extracts. These results suggest that the QuEChERS method could be used and further improved to obtain more purified and stable extracts for fucoxanthin from U. pinnatifida.

Production of coumarin compounds by Haplophyllum patavinum in vivo and in vitro

Abstract Native plants, calli and suspension cultures of Haplophyllum patavinum were found to produce several coumarin compounds, eight of which were identified as umbelliferone, scopoletin, 7-isoprenyloxycoumarin, umbelliprenin, osthenol, columbianetin, angelicin and psoralen. Umbelliferone, angelicin and psoralen were found both in plant organs and in tissue cultures, scopoletin and umbelliprenin only in vivo , osthenol, 7-isoprenyloxycoumarin and columbianetin only in vitro conditions. The coumarin production in vitro was strongly affected by the cell strain. The co-occurrence of the linear and the angular furanocoumarins, psoralen and angelicin, had never been previously reported in the genus Haplophyllum .

Production of lignans by Haplophyllum Patavinum in vivo and in vitro

Three known arylnaphthalene lignans (justicidin B, diphyllin and tuberculatin), and one dibenzylbutyrolactone (arctigenin) were isolated from native plants, callus and suspension cultures of Haplophyllum patavinum. The present paper represents the first report on arylnaphthalene lignan production by in vitro cultures; in vitro, the biogenetic potential is strictly dependent on the cell strain.

Naphthoquinone Contents of Cultivated Drosera Species Drosera binata, D. binata var. dichotoma, and D. capensis

AbstractThe naphthoquinone contents of greenhouse cultivated Australian and South-African Drosera species (D. binata, D. binata var. dichotoma and D. capensis) have been investigated with regard to the plant organ, propagation method and plant development stage. Comparative analyses have been carried out on native populations of D. rotundifolia L., European species of pharmaceutical interest. D. binata and mostly D. binata var. dichotoma represent good natural sources of plumbagin, the only quinone occurring in these Australian species, otherwise D. capensis must be regarded as an interesting natural source of 7-methyljuglone, the only naphthoquinone ubiquitously occurring in all the plant organs.

Somatic embryogenesis and shoot regeneration from leaf derived callus of Hypericum perforatum var. angustifolium (sin. Fröhlich) Borkh

Abstract The development of in vitro regeneration systems for Hypericum perforatum var. angustifolium (sin. Fröhlich) Borkh, a medicinal plant used for treating neurological disorders, is described. For the first time in this variety, somatic embryogenesis and shoot regeneration were induced from leaf-derived callus. Well-formed plantlets were obtained through both shoot regeneration and somatic embryogenesis, with separate morphogenetic programmes. Proembryogenic masses were obtained in liquid MS and B5 media supplemented with 5.8 μM 2,4-D, 1.34 μM NAA, and 1.16 μM Kin; after being transferred onto hormone-free medium, they formed whitish and spherical structures that subsequently developed into the heart and torpedo stages.  On MS agarized medium containing thidiazuron (TDZ) at different concentrations (3, 6, 9, 12 μM) combined with 2 μM IBA, only shoot regeneration, and not somatic embryogenesis, was obtained. The mean number of shoots increased significantly when the concentration of TDZ was 3 μM.

Botanical Identification of Powdered Plant Drugs. Verbascum Flowers

AbstractCommercial powdered samples of Verbascum flowers and slightly broken and powdered samples obtained from previously authenticated plant material (flowers of Verbascum thapsus L. subsp. thapsus) were examined by SEM. For the powdered drug, the most valuable diagnostic characters are the 3-colporoidate prolate pollen grains with reticulate exine and the co-occurrence of smooth branched and of warty-striated non-branched trichomes. Contamination of a commercial powdered sample of Verbascum flowers with plant material not belonging to a Verbascum species (most probably flowers of a Composite), was observed.