Studies on Bignoniaceae: Newbouldiosides D - F, Minor Phenylethanoid Glycosides from Newbouldia laevis, and New Flavonoids from Markhamia zanzibarica and Spathodea campanulata.

Continued examination of the stem bark of afforded three minor phenylethanoid glycosides, designated as newbouldiosides D - F. Their structures were elucidated by spectroscopic methods as -(3,4-dihydroxyphenyl)ethyl 5--syringoyl---apiofuranosyloxy-(1 → 2)--[-L-rhamnopyranosyl-(1 → 3)]-6--E-sinapoyl--D-glucopyranoside, -(3,4-dihydroxyphenyl)ethyl -D-apiofuranosyloxy-(1 → 2)--[-L-rhamnopyranosyl-(1 → 3)]-6--E-sinapoyl--D-glucopyranoside, and -(3,4-dihydroxyphenyl)ethyl -D-apiofuranosyloxy-(1 → 2)---L-rhamnopyranosyl-(1 → 2)-6--E-sinapoyl---glucopyranoside, respectively. These metabolites are the first members possessing a sinapoyl structural element.

Different Inhibitory Potencies of Oseltamivir Carboxylate, Zanamivir, and Several Tannins on Bacterial and Viral Neuraminidases as Assessed in a Cell-Free Fluorescence-Based Enzyme Inhibition Assay.

Neuraminidaseis a key enzyme in the life cycle of influenza viruses and is present in some bacterial pathogens. We here assess the inhibitory potency of plant tannins versus clinically used inhibitors on both a viral and a bacterial model neuraminidase by applying the 2'-(4-methylumbelliferyl)-α-d--acetylneuraminic acid (MUNANA)-based activity assay. A range of flavan-3-ols, ellagitannins and chemically defined proanthocyanidin fractions was evaluated in comparison to oseltamivir carboxylate and zanamivir for their inhibitory activities against viral influenza A (H1N1) and bacterial neuraminidase (VCNA).

Trans-Resveratrol Induces Apoptosis through ROS-Triggered Mitochondria-Dependent Pathways in A549 Human Lung Adenocarcinoma Epithelial Cells.

Resveratrol has been shown to be a potential chemopreventive and anticancer agent, inducing apoptosis in a variety of cancer cells. The present study was performed to evaluate the effect of resveratrol on A549 human lung adenocarcinoma epithelial cells. 3-(4,5-Dimethylthiazol-2-Yl)-2,5-diphenyltetrazolium bromide evaluation demonstrated that the exposure of cells to increasing concentrations of resveratrol (0-175 µM) for 24 h resulted in a decrease in cell viability (IC50 85.

A chemically defined 2,3-trans procyanidin fraction from willow bark causes redox-sensitive endothelium-dependent relaxation in porcine coronary arteries.

Extracts of the bark of willow species (Salix spp.) are popular herbal remedies to relieve fever and inflammation. The effects are attributed to salicin and structurally related phenolic metabolites, while polyphenols including procyanidins are suggested to contribute to the overall effect of willow bark.

2,3-cis-procyanidins elicit endothelium-dependent relaxation in porcine coronary arteries via activation of the PI3/Akt kinase signaling pathway.

Polyphenols including procyanidins have been reported to reduce the risk of cardiovascular diseases. However, polyphenolic extracts represent complex mixtures, and detailed information on their chemical composition is commonly lacking. The aim of this study was to investigate the potential of a highly purified and chemically defined 2,3-cis-procyanidin sample (di- to hexameric [4β,8]-linked oligomers) from Nelia meyeri to relax coronary arteries and to get insight into the underlying mechanisms.

High sensitivity of Giardia duodenalis to tetrahydrolipstatin (orlistat) in vitro.

Giardiasis, a gastrointestinal disease caused by Giardia duodenalis, is currently treated mainly with nitroimidazoles, primarily metronidazole (MTZ). Treatment failure rates of up to 20 percent reflect the compelling need for alternative treatment options. Here, we investigated whether orlistat, a drug approved to treat obesity, represents a potential therapeutic agent against giardiasis.

In vitro antileishmanial activity of resveratrol originates from its cytotoxic potential against host cells.

In addition to a range of beneficial pharmacological activities, resveratrol is recently reported to have potential antileishmanial activities in vitro. The present study was conducted to evaluate the effect of resveratrol on promastigotes and amastigotes of transgenic Leishmania major expressing green fluorescent protein in comparison with its direct cytotoxic effects on host cells (bone marrow-derived and J774-G8 macrophages, respectively). As assessed by FACS analysis, resveratrol showed moderate antipromastigote activity at <35 µg/mL (153.

Antimicrobial, Antiviral and Immunomodulatory Activity Studies of Pelargonium sidoides (EPs 7630) in the Context of Health Promotion.

Pelargonium species contribute significantly to the health care of a large population in the Southern African region, as part of a long-standing medical system intimately linked to traditional healing practices. Most notably, extracts of the roots of P. sidoides have commonly been applied for the treatment of dysentery and diarrhoea but only occasionally for respiratory complaints.

Structure/antileishmanial activity relationship study of naphthoquinones and dependency of the mode of action on the substitution patterns.

A series of naphthoquinones was tested for activity against both extracellular promastigote and intracellular amastigote Leishmania major GFP in vitro. In parallel, the compounds were evaluated for cytotoxic effects against bone marrow-derived macrophages (BMM Φ) as a mammalian host cell control. Most of the compounds noticeably inhibited the growth of extracellular parasites (IC (50) 0.

Anti-infective activities of Pelargonium sidoides (EPS® 7630): effects of induced NO production on Leishmania major in infected macrophages and antiviral effects as assessed in a fibroblast-virus protection assay.

EPs® 7630 is an aqueous-ethanolic extract of the roots of Pelargonium sidoides, employed in the treatment of upper respiratory tract infections. Its anti-infective activity is supposed to be associated with the activation of the nonspecific immune system. Using Leishmania major GFP-infected murine BMMΦ, the NO production of EPs® 7630-activated macrophages was correlated with the reduction of the GFP signal measured at single cell levels using flow cytometry.

Anti-adhesive activities of flavan-3-ols and proanthocyanidins in the interaction of group A-streptococci and human epithelial cells.

Bacterial adhesion to epithelial cells is a key step in infections, allowing subsequent colonization, invasion and internalization of pathogens into tissues. Anti-adhesive agents are therefore potential prophylactic tools against bacterial infections. The range of anti-adhesive compounds is largely confined to carbohydrate analogues.

Evaluation of an aqueous-ethanolic extract from Pelargonium sidoides (EPs® 7630) for its activity against group A-streptococci adhesion to human HEp-2 epithelial cells.

Aim Of The Study: The root extract of Pelargonium sidoides DC (Geraniaceae), EPs® 7630, is currently used to treat respiratory tract infections. The therapeutic benefits are largely related to the modulation of the non-specific immune system. The present study was designed to investigate the anti-adhesive activity of this herbal medicine with Streptococcus pyogenes as model microorganism and to identify the underlying biologically active principle.

Anti-infective mode of action of EPs 7630 at the molecular level.

Clinical trials have shown that EPs 7630, an aqueous ethanolic extract from the roots of Pelargonium sidoides, is an efficacious treatment for respiratory tract infections. A large body of in vitro studies has provided evidence for an anti-infective principle associated with activation of the non-specific immune system. However, the mode of action at the cellular and molecular level is still insufficiently defined.

Intracellular parasite kill: flow cytometry and NO detection for rapid discrimination between anti-leishmanial activity and macrophage activation.

Transgenic Leishmania expressing fluorescent reporter proteins such as green fluorescent protein (GFP) have opened the way for a flow cytometry (FACS)-based method to assess the killing of Leishmania parasites inside their macrophage host. Compared with counting parasites in microscopic preparations, the assessment of anti-leishmanial effects by FACS analysis promises both strict objectivity and significant reduction of labour-per-sample while scanning thousands of cells within seconds. Compared with other semi-automated methods based on host cell lysis and biochemical quantification of released parasites, the procedure is more direct and simple, reducing handling artefacts.

Aqueous ethanolic extract of the roots of Pelargonium sidoides--new scientific evidence for an old anti-infective phytopharmaceutical.

Among the PELARGONIUM-based herbal remedies that are widely used in traditional medical systems in the Southern African region is a highly valued root medicine (commonly termed UMCKALOABO) of initially unknown botanical origin for the treatment of infectious conditions of the respiratory tract including tuberculosis. Nowadays, a modern aqueous-ethanolic formulation of the roots of Pelargonium sidoides (EPs 7630), developed from this traditional medicine, is successfully employed for the treatment of bronchitis. The article summarizes the fascinating story of this herbal medicine including its way to Europe, identification of the botanical origin, and provides background information of the many profound anti-infectious actions and clinical studies.

Stimulus (polyphenol, IFN-gamma, LPS)-dependent nitric oxide production and antileishmanial effects in RAW 264.7 macrophages.

The effects of interferon (IFN-gamma), lipopolysaccharide (LPS), and some polyphenols as individual stimuli, as well as in various combinations on NO production in non-infected and infected macrophage-like RAW 264.7 cells were investigated, with emphasis on the NO/parasite kill relationship. In non-infected and in Leishmania parasitized cells, gallic acid significantly inhibited the IFN-gamma and LPS-induced NO detected in the supernatant.

An ellagitannin, n-butyl gallate, two aryltetralin lignans, and an unprecedented diterpene ester from Pelargonium reniforme.

The structural diversity of the metabolic pool of Pelargonium reniforme was extended by the characterization of the 1C4-glucose based ellagitannin pelargoniin E, gallic acid n-butyl ester, (-)-4,4',9'-trihydroxy-3',5'-dimethoxy-2,7'-cyclolignan 9-O-beta-glucopyranoside and reniformin, a diterpene ester comprised of a diterpene acid with an uncommon -(CH2)(2)- bridging element linked to 2-(4-hydroxyphenyl)ethansulfonic acid. These metabolites were associated with the known (alpha,beta)-3,4-di-O-galloyl-glucopyranoside, 4,6-dihydroxy-2beta-glucopyranosyloxyacetophenone, 1-O-galloylglycerol, 6'-O-galloylsalidroside and (+)-isolariciresinol-9'-O-beta-glucopyranoside. All structures were established on the basis of spectroscopic methods.

[Pelargonium sidoides-extract (EPs 7630): registration confirms efficacy and safety].

For centuries the roots of Pelargonium sidoides DC have been used in South African ethno-medicine for the treatment of respiratory diseases. In Germany, a medicinal product containing a special extract of this substance is among the group of self-medication products most widely bought at chemist's shops. In December 2005, the Federal Institute for Drugs and Medical Devices (BfArM, Bonn) approved a new license for its use as a drug.

In vitro evaluation of antibacterial and immunomodulatory activities of Pelargonium reniforme, Pelargonium sidoides and the related herbal drug preparation EPs 7630.

The importance of Pelargonium species, most notably Pelargonium reniforme and Pelargonium sidoides, in traditional medicine in the Southern African region is well documented. Nowadays, a modern aqueous-ethanolic formulation of the roots of P. sidoides (EPs) 7630) is successfully employed for the treatment of ear, nose and throat disorders as well as respiratory tract infections.

Fascinating metabolic pools of Pelargonium sidoides and Pelargonium reniforme, traditional and phytomedicinal sources of the herbal medicine Umckaloabo.

The metabolic pools of Pelargonium sidoides DC and Pelargonium reniforme CURT, associated with the origin of the herbal medicine Umckaloabo, exhibit remarkable diversity and complexity. They comprise a variety of phenolic and polyphenolic compounds, a notable wealth of highly oxygenated simple coumarins and a number of miscellaneous uncommon metabolites. Noteworthy, the roots of both species express conspicuously distinct coumarin variations that facilitate their identification.

Newbouldiosides A-C, phenylethanoid glycosides from the stem bark of Newbouldia laevis.

From the stem bark of Newbouldia laevis three phenylethanoid glycosides, designated as newbouldioside A-C, were isolated together with a sodium salt of analogue B and the known compounds, verbascoside, 5-hydroxydehydro-iso-alpha-lapachone, 3,8-dihydroxydehydro-iso-alpha-lapachone, apigenin and luteolin. The structures of the phenylethanoid glycosides were elucidated by spectroscopic methods as beta-(3,4-dihydroxyphenyl)ethyl 5-O-syringoyl-beta-D-apiofuranosyloxy-(1-->2)-O-[alpha-L-rhamnopyranosyl-(1-->3)]-beta-D-glucopyranoside, ss-(3,4-dihydroxyphenyl)ethyl 5-O-syringoyl-beta-D-apiofuranosyloxy-(1-->2)-O-[alpha-L-rhamnopyranosyl-(1-->3)]-6-O-E-feruloyl-beta-D-glucopyranoside, and beta-(3,4-dihydroxyphenyl)ethyl 3-O-E-feruloyl-beta-D-apiofuranosyloxy-(1-->2)-O-alpha-L-rhamnopyranosyl-(1-->2)-6-O-E-sinapoyl-beta-D-glucopyranoside, respectively.

Antileishmanial activity and immune modulatory effects of tannins and related compounds on Leishmania parasitised RAW 264.7 cells.

The antileishmanial and immunomodulatory potencies of a total of 67 tannins and structurally related compounds were evaluated in terms of extra- and intra-cellular leishmanicidal effects and macrophage activation for release of nitric oxide (NO), tumour necrosis factor (TNF) and interferon (IFN)-like activities. Their effects on macrophage functions were further assessed by expression analysis (iNOS, IFN-alpha, IFN-gamma, TNF-alpha, IL-1, IL-10, IL-12, IL-18). With few exceptions, e.