Clerodane Diterpenes from as Allosteric GABA Receptor Modulators.

An EtOAc extract of leaves led to an allosteric potentiation of the GABA signal in a fluorometric imaging plate reader (FLIPR) assay on Chinese hamster ovary (CHO) cells stably expressing GABA receptors with an αβγ subunit composition. The activity was tracked by HPLC-based activity profiling, and four known (, , , and ) and five new clerodane-type diterpenoids (, -, and ) were isolated. Compounds - were obtained from the active time window.

A multicomponent herbal feed additive improves somatic cell counts in dairy cows - a two stage, multicentre, placebo-controlled long-term on-farm trial.

In contrast to natural and historical diets of wild and domesticated ruminants, the diversity of plant species is limited in diets of modern dairy cows. Are "production diseases" linked to this? We conducted a trial to test the effects of a multicomponent herbal feed additive (HFA) on health, performance and fertility traits. A dose-finding study (DF) with 62 cows on 11 commercial farms compared a low (50 g) and a high (100 g) dose of HFA (HFA-50, HFA-100) with a placebo (PL).

A FLIPR Assay for Discovery of GABAA Receptor Modulators of Natural Origin.

A fluorometric imaging plate reader (FLIPR) assay utilizing Chinese hamster ovary (CHO) cells stably transfected with GABA receptors of subunit composition was evaluated and validated for rapid screening of plant extract libraries and efficient localization of active compounds in extracts. Validation was performed with pure compounds and extracts known to contain allosteric GABA receptor modulators. Plants extracts that had been previously reported as active in an assay using oocytes transiently expressing GABA receptors of subunit composition were also active in the FLIPR assay.

A Bufadienolide-Enriched Fraction of Bryophyllum pinnatum Inhibits Human Myometrial Contractility In Vitro.

has been used since the 1970s to prevent premature labour, first in anthroposophic hospitals and, more recently, also in the main Swiss perinatal centres. However, it is not known which compounds in leaves contribute to the tocolytic effect. Here we studied the effects of a flavonoid-enriched fraction, the corresponding flavonoid aglycon mixture, a bufadienolide-enriched fraction, and leaf press juice on human myometrial contractility .

Andrographolide-loaded nanoparticles for brain delivery: Formulation, characterisation and in vitro permeability using hCMEC/D3 cell line.

Andrographolide (AG) is a major diterpenoid of the Asian medicinal plant Andrographis paniculata which has shown exciting pharmacological potential for the treatment of inflammation-related pathologies including neurodegenerative disorders. Conversely, the low bioavailability of AG still represents a limiting factor for its use. To overcome these limitations, AG was loaded into human serum albumin based nanoparticles (HSA NPs) and poly ethylcyanoacrylate nanoparticles (PECA NPs).

The Dual Edema-Preventing Molecular Mechanism of the Crataegus Extract WS 1442 Can Be Assigned to Distinct Phytochemical Fractions.

The hawthorn ( spp.) extract WS 1442 is used against mild forms of chronic heart failure. This disease is associated with endothelial barrier dysfunction and edema formation.

Identification of Plant-derived Alkaloids with Therapeutic Potential for Myotonic Dystrophy Type I.

Myotonic dystrophy type I (DM1) is a disabling neuromuscular disease with no causal treatment available. This disease is caused by expanded CTG trinucleotide repeats in the 3' UTR of the dystrophia myotonica protein kinase gene. On the RNA level, expanded (CUG)n repeats form hairpin structures that sequester splicing factors such as muscleblind-like 1 (MBNL1).