Bufadienolides from Helleborus foetidus and their cytotoxic properties on MCF-7 breast cancer cells.

Twelve bufadienolides and six 19-norbufadienolides were isolated from the aerial parts of Helleborus foetidus. They consist of aglycons and glucosides and include nine previously undescribed compounds and a compound reported for the first time as a genuine natural product. Their structures were established by extensive spectroscopic analysis and the structure and absolute configuration of two previously unreported 3,4-epoxy derivatives were confirmed by single crystal X-ray diffraction analysis.

Extract Ze 440: Diterpene and Triterpene's Interactions with Dopamine D2 Receptor.

Pre-clinical studies suggest that extracts prepared from the fruits of (VAC) interact with dopamine D2 receptors, leading to reduced prolactin secretion. In previous experiments, dopaminergic activity was mostly evaluated using radioligand binding assays or via the inhibition of prolactin release from rat pituitary cells. Diterpenes featuring a clerodadienol scaffold were identified as major active compounds, but no conclusive data regarding their potency and intrinsic activity are available.

Highly oxygenated antiplasmodial and non-hemolytic Δ stigmastane-type steroids from the twigs of Vernonia amygdalina Delile.

Chemical investigations of a methanolic extract of the twigs of Vernonia amygdalina Delile (Asteraceae) resulted in the isolation and identification of three previously undescribed highly oxygenated Δ stigmastane-type steroids namely vernonins U-W (1-3) along with six known compounds (4-9). The structural characterization of all the isolated compounds has been conducted via comprehensive 1D and 2D-NMR spectroscopy as well as HRMS. The seven steroidal derivatives 1-7 were evaluated for their antiplasmodial activity against the chloroquine-resistant strain P.

Biosynthesis of the bacterial antibiotic 3,7-dihydroxytropolone through enzymatic salvaging of catabolic shunt products.

The non-benzenoid aromatic tropone ring is a structural motif of numerous microbial and plant natural products with potent bioactivities. In bacteria, tropone biosynthesis involves early steps of the widespread CoA-dependent phenylacetic acid (paa) catabolon, from which a shunt product is sequestered and surprisingly further utilized as a universal precursor for structurally and functionally diverse tropone derivatives such as tropodithietic acid or (hydroxy)tropolones. Here, we elucidate the biosynthesis of the antibiotic 3,7-dihydroxytropolone in Actinobacteria by pathway reconstitution using paa catabolic enzymes as well as dedicated downstream tailoring enzymes, including a thioesterase (TrlF) and two flavoprotein monooxygenases (TrlCD and TrlE).

Assay for evaluation of proarrhythmic effects of herbal products: Case study with 12 preparations.

Guidelines for preclinical drug development reduce the occurrence of arrhythmia-related side effects. Besides ample evidence for the presence of arrhythmogenic substances in plants, there is no consensus on a research strategy for the evaluation of proarrhythmic effects of herbal products. Here, we propose a cardiac safety assay for the detection of proarrhythmic effects of plant extracts based on the experimental approaches described in the Comprehensive Proarrhythmia Assay (CiPA).

Phytochemical Comparison of Medicinal Cannabis Extracts and Study of Their CYP-Mediated Interactions with Coumarinic Oral Anticoagulants.

Introduction: Treatment with cannabis extracts for a variety of diseases has gained popularity. However, differences in herb-drug interaction potential of extracts from different plant sources are poorly understood. In this study, we provide a characterization of cannabis extracts prepared from four cannabis chemotypes and an in vitro assessment of their Cytochrome P450 (CYP)-mediated herb-drug interaction profiles.

A Dimerosesquiterpene and Sesquiterpene Lactones from Inhibiting Oncogenic PI3K/AKT Signaling in Melanoma Cells.

A library of more than 2500 plant extracts was screened for activity on oncogenic signaling in melanoma cells. The ethyl acetate extract from the aerial parts of displayed pronounced inhibition of the PI3K/AKT pathway. Active compounds were tracked with the aid of HPLC-based activity profiling, and altogether 21 active compounds were isolated, including one novel dimerosequiterpenoid (), one new disesquiterpenoid (), three new guaianolides (-), 12 known sesquiterpenoids (-), and four known flavonoids (-).

Flavonoids from Ericameria nauseosa inhibiting PI3K/AKT pathway in human melanoma cells.

The PI3K/AKT and MAPK/ERK pathways are frequently mutated in metastatic melanoma. In a screen of over 2500 plant extracts, the dichloromethane extract of Ericameria nauseosa significantly inhibited oncogenic activity of AKT in MM121224 human melanoma cells. This extract was analyzed by analytical HPLC, and the column effluent was fractionated and tested for activity to generate the so-called HPLC-based activity profile.

A Compliance-Reactance Framework for Evaluating Human-Robot Interaction.

When do we follow requests and recommendations and which ones do we choose not to comply with? This publication combines definitions of compliance and reactance as behaviours and as affective processes in one model for application to human-robot interaction. The framework comprises three steps: human perception, comprehension, and selection of an action following a cue given by a robot. The paper outlines the application of the model in different study settings such as controlled experiments that allow for the assessment of cognition as well as observational field studies that lack this possibility.

Combining Activity Profiling with Advanced Annotation to Accelerate the Discovery of Natural Products Targeting Oncogenic Signaling in Melanoma.

The discovery of bioactive natural products remains a time-consuming and challenging task. The ability to link high-confidence metabolite annotations in crude extracts with activity would be highly beneficial to the drug discovery process. To address this challenge, HPLC-based activity profiling and advanced UHPLC-HRMS/MS metabolite profiling for annotation were combined to leverage the information obtained from both approaches on a crude extract scaled down to the submilligram level.

Phytotherapy in Integrative Oncology-An Update of Promising Treatment Options.

Modern phytotherapy is part of today's conventional evidence-based medicine and the use of phytopharmaceuticals in integrative oncology is becoming increasingly popular. Approximately 40% of users of such phytopharmaceuticals are tumour patients. The present review provides an overview of the most important plants and nature-based compounds used in integrative oncology and illustrates their pharmacological potential in preclinical and clinical settings.

High-Content Screening Pipeline for Natural Products Targeting Oncogenic Signaling in Melanoma.

The incidence of melanoma, the most fatal dermatological cancer, has dramatically increased over the last few decades. Modern targeted therapy with kinase inhibitors induces potent clinical responses, but drug resistance quickly develops. Combination therapy improves treatment outcomes.

Immunosuppressant flavonoids from Scutellaria baicalensis.

Some plants used in Traditional Chinese Medicine serve as treatment for disease states where a suppression of the cellular immune response is desired. However, the compounds responsible for the immunosuppressant effects of these plants are not necessarily known. The immunosuppressant compounds in the roots of Scutellaria baicalensis, one of the most promising plants identified in a previous screening, were tracked by HPLC activity profiling and concomitant on-line spectroscopic analysis.

Design of a hesitant movement gesture for mobile robots.

In previous experiments, a back-off movement was introduced as a motion strategy of robots to facilitate the order of passage at bottlenecks in human-robot spatial interaction. In this article we take a closer look at the appropriate application of motion parameters that make the backward movement legible. Related works in distance perception, size-speed illusions, and viewpoint-based legibility considerations suggest a relationship between the size of the robot and the observer's perspective on the expected execution of this movement.

Compounds from : Immunosuppressant Activity and Absolute Configurations.

In a screening of an extract library from plants used in Traditional Chinese Medicine the MeOH extract of inhibited proliferation of human primary T cells with an IC of 25.8 μg/mL. Activity in the extract was tracked by HPLC activity profiling, and a total of 15 compounds were characterized.

Boswellia carteri extract and 3-O-acetyl-alpha-boswellic acid suppress T cell function.

Resins from various Boswellia species have a long track record in different cultures as a treatment for inflammatory diseases. This study was designed to provide evidence for the anti-inflammatory capacity and medicinal use of Boswellia carteri (Burseraceae). A dichloromethane (DCM) extract of B.

Immunosuppressive Activity of Extract and Isolated Compounds.

The need for novel drugs for the treatment of autoimmune diseases is high, since available pharmaceuticals often have substantial side effects and limited efficacy. Natural products are a good starting point in the development of immunosuppressive leads. Since enhanced T cell proliferation is a common feature of autoimmune diseases, we investigated the T cell proliferation inhibitory potential of an extract library of plants used in traditional Chinese medicine.

Antibacterial and ATP Synthesis Modulating Compounds from .

A surface extract of the aerial parts of afforded a nor-sesterterpenoid () and eight new sesterterpenoids (-̵), along with five known sesterterpenoids, five labdane and one abietane diterpenoid, one sesquiterpenoid, and four flavonoids. The structures of the new compounds were established by 1D and 2D NMR spectroscopy, HRESIMS, and VCD data and Mosher's esters analysis. The antimicrobial activity of compounds was evaluated against 30 human pathogens including 27 clinical strains and three isolates of marine origin for their possible implications on human health.

European medicinal mushrooms: Do they have potential for modern medicine? - An update.

Background: The application of mushrooms for health purposes has a long tradition and is very common in Asian countries. This trend is also becoming increasingly popular in the western hemisphere. However, mushrooms from European tradition are being treated in a restrained manner despite having significant potential as drugs or as sources of pure bioactive substances.

Sesquiterpene Lactones from Artemisia argyi: Absolute Configuration and Immunosuppressant Activity.

A library of extracts from plants used in Chinese Traditional Medicine was screened for inhibition of T lymphocyte proliferation. An ethyl acetate extract from aerial parts of Artemisia argyi showed promising activity and was submitted to HPLC-based activity profiling to track the active compounds. From the most active time window, three guaianolides (1, 2, and 5) and two seco-tanapartholides (3 and 4) were identified and, in a less active time window, five new sesquiterpene lactones (8-11, 17), along with six known sesquiterpene lactones and two known flavonoids.

A one-stage cultivation process for lipid- and carbohydrate-rich biomass of Scenedesmus obtusiusculus based on artificial and natural water sources.

A one-stage cultivation process of the microalgae Scenedesmus obtusiusculus with medium based on natural water sources was developed to enhance lipids and carbohydrates. A medium based on artificial sea water, Baltic Sea water and river water with optimized nutrient concentrations compared to the standard BG-11 for nitrate (-75%), phosphate and iron (-90%) was used for cultivation. Although nitrate exhaustion over cultivation resulted in nitrate limitation, growth of the microalgae was not reduced.

The ring opening reaction of 1,3-dithiol-2-one systems is fully reversible.

The deprotection of a common precursor moiety in dithiolene chemistry was discovered to be fully reversible, which, besides being relevant for researchers working in very different fields with these non-innocent ligand systems, may even have an impact on CO2 housekeeping, as the deprotected ligand acts as an efficient trap.