Effects of Inonotus hispidus Extracts and Compounds on Human Immunocompetent Cells.

Inonotus hispidus is used as a traditional medicine in China. Previous investigations revealed promising immunomodulatory activity of fruit body extracts of I. hispidus. Bioactivity-guided fractionation showed that hispolon and hispidin were active substances.In this study, we analysed the effects of I. hispidus extract and selected constituents on different types of human immune cells and investigated the potential of I. hispidus extract as a medicinal mushroom. The influence of I. hispidus extract on activity and maturation of human T cells, purified natural killer cells, and dendritic cells was analysed using cytometric-based surface marker expression. The cell division characteristics of the activated T cells were assessed by membrane permeable dye, and the function of natural killer cells was investigated by a degranulation CD107a assay. Apoptosis induction was assessed by surface staining of phosphatidylserine, and camptothecin and cyclosporine A were used individually as controls. Phytochemical analysis, using TLC chromatograms and HPLC analysis, was conducted to characterise the I. hispidus extract. I. hispidus extract increased the activation and diminished the proliferation of activated human T cells in the presence of apoptosis. Natural killer cell activity and function were dose-dependently increased. Surface marker expression of dendritic cells demonstrated that I. hispidus extract has the potential to induce maturation. TLC and HPLC analyses showed that the extract contained hispidin and hispolon. Investigations using hispidin and hispolon demonstrated similar, albeit noncongruent, results with extracts on measured parameters.The results indicate that extracts from I. hispidus and their constituents, hispidin and hispolon, interfere with the function of multiple immune cells, thus providing a rationale for their potential as a medicinal mushroom.

Inhibition of DNA-Topoisomerase I by Acylated Triterpene Saponins from Pittosporum angustifolium Lodd.

Previous phytochemical investigation of the leaves and seeds of Pittosporum angustifolium Lodd. led to the isolation and structural elucidation of polyphenols and triterpene saponins. Evaluation for cytotoxicity of isolated saponins revealed that the predominant structural feature for a cytotoxic activity are acyl substituents at the oleanane aglycon backbone. The present work reports the results of a screening of 10 selected acylated saponins for their potential to inhibit the human DNA-topoisomerase I, giving rise to IC50 values in a range of 2.8-46.5 µM. To clarify the mode of observed cytotoxic action and, moreover, to distinguish from a pure surfactant effect which is commonly accompanied with saponins, these results indicate an involvement of the topoisomerase I and its role as a possible target structure for a cytotoxic activity. In addition, computational predictions of the fitting of saponins to the topoisomerase I-DNA complex, indicate a similar binding mode to that of clinically used topoisomerase I inhibitors. Ten acylated triterpene saponins from Pittosporum angustifolium were investigated for their potential to inhibit the human DNA-topoisomerase I and computational predictions of the fitting of saponins to the topoisomerase I-DNA complex were carried out.

Cytotoxic saponins from the seeds of Pittosporum angustifolium.

Three new acylated R1-barrigenol triterpene glycosides, 1-3, were isolated from the seeds of Pittosporum angustifolium Lodd. together with four known glycosides, 4-7, containing R1- and A1-barrigenol backbones. On the basis of spectroscopic, spectrometric, and chemical analyses the novel compounds were named pittangretosides N-P and established as 21beta-acetoxy-22alpha-angeloyloxy- (1), 21beta-acetoxy-22alpha-(2-acetoxy-2-methylbutyroyloxy)- (2), and 21beta-(2-methylbutyroyloxy)-22alpha-acetoxy-3beta-[beta-D-glucopyranosyl- (1 --> 2)]-[alpha-L-arabinopyranosyl-(1 --> 3)]-[alpha-L-arabinofuranosyl-(1 --> 4)]-beta-D-glucuronopyranosyloxyolean-12-ene-15alpha, 6alpha, 28-triol (3). Evaluation of the in vitro cytotoxicity against three tumour cell lines and one non-tumourigenic cell line revealed antiproliferative effects with IC50 values in a range of 1.74-34.1 microM.

Triterpene glycosides from the leaves of Pittosporum angustifolium.

Phytochemical investigation of the leaves of Pittosporum angustifolium resulted in the isolation and structural elucidation of nine new triterpene saponins, named pittangretosides A-I (1-9), together with a known compound (10). Mainly by NMR and HRESIMS experiments, eight compounds were identified as A1-barrigenol glycosides (1-7, 10), whereas two compounds exhibited an unusual 17,22-seco-backbone of oleanolic acid (8, 9). All compounds were evaluated for their in vitro cytotoxicities against human urinary bladder carcinoma cells (5637). Only compounds with an angeloyl-residue at C-22 of the aglycone (1-4 and 10) showed antiproliferative effects with IC50 values of 4.1, 5.2, 2.1, 17.9, and 2.4 µM, respectively.

[Druggists of Aalst during the 18th century]. / Apothekers te Aalst in de 18de eeuw.

Our previous research and the recent edition of the regesta of the scabinal records of the city of Aalst (Alost, Occidental Flanders Province, Belgium), gave us the opportunity to write here for the very first time a prosopography of the apothecaries of that city during the 18th century. Additional information about medical doctors and surgeons are also included.

[Apothecaries, doctors and surgeons, members of the guild Sint-Joris at Aalst between 1488 and 1574]. / Apothekers, geneesheren en chirurgijns, leden van de schuttersgilde Sint-Joris te Aalst tussen 1488 en 1574.

The register of the members of St George's cross-bow Guild of the city of Aalst (Alost) in Flanders includes three names of apothecaries: Bertelmeeux vande Putte from Ghent (1523), magister Gérard Boyengenye of Antwerp (1538) and magister Jean Jolybois (1550) of Alost itself. The last two apothecaries were until now not noticed.

[Migration of pharmacists in Belgium from the 13th through 18th centuries]. / Mobiliteit en migratie van de apotheker in Vlaanderen en Brabant van de 13de tot de 18de eeuw.

The municipal records are important sources for the migration and mobility of the apothecaries from the 13th to the 18th century. They prove that immigration from Italy and France, formerly regarded as the first factor for the presence in our country of pharmacists, was minimal. Only two Italian and two French pharmacists from 1377 unto 1500 could be traced. The second thesis concerning the evolution of the profession, the so called mercer theory, is on the other hand very important. Mobility is here a really substantial component because of the apprentice years. The 18th century represents a growing settlement in small locations. The emigration of the 16th century were occasioned by religious and political factors.