Tat-P combined with GAPR1 releases Beclin1 to promote autophagy and improve Bronchopulmonary dysplasia model.

Long-term exposure to hyperoxia can leading to the bronchopulmonary dysplasia (BPD). The progression of BPD is primarily driven by the apoptosis of alveolar epithelial cells, and the regulation of autophagy has an impact on apoptosis. This study aims to investigate the therapeutic potential and underlying mechanism of an autophagy-promoting peptide (Tat-P) in ameliorating BPD. In vitro experiments demonstrated that Tat-P promoted autophagy and partially prevented apoptosis caused by exposure to hyperoxia. Further investigation into the mechanism revealed that Tat-P competitively binds to GAPR1, displacing the Beclin1 protein and thereby inhibiting the apoptosis. In vivo experiments conducted on Sprague-Dawley pups exposed to high oxygen levels demonstrated that Tat-P promoted autophagy and reduced apoptosis in lung tissues and ameliorated BPD-related phenotypes. Our findings elucidate the underlying mechanisms and effects of Tat-P in enhancing autophagy and preventing apoptosis. This study presents an approach for the prevention and treatment of BPD.

Diaporine, a novel endophyte-derived regulator of macrophage differentiation.

Diaporine (1), an unprecedented symmetric polyketide, was characterized from the endophytic fungus. The structure was determined by extensive spectroscopic analyses. Diaporine can inhibit significantly the differentiation of macrophages and has potential to induce conversion from the M2 to the M1 phenotype, in addition to regulation of the TLR4-MAPK signal pathway and PPARγ activity.

Polyketides from the plant endophytic fungus Cladosporium sp. IFB3lp-2.

Chemical study of the ethyl acetate extract of the plant endophytic fungus Cladosporium sp. (strain no. IFB3lp-2) yielded three new polyketides (1-3), together with nine known compounds. All of the structures were elucidated on the basis of spectroscopic methods. The isolated compounds were screened for their cytotoxic, antiviral, and acetyl cholinesterase inhibitory activities. Regretfully, no compounds showed any significant activity in these assays.

Effects of Rhynchophylline on relaxation and contraction of the bladder detrusor in rats.

AIM: The aim of this study was to observe the effects of Rhynchophylline (Rhy) on the relaxation and contraction of rat bladder detrusor and urodynamics and determine the changes in the tension of isolated rat bladder muscle strips. MATERIALS AND METHODS: Rats were randomly divided into four groups: sham-operated, overactive bladder (OAB) model, Rhy-treated, and the control group. Sections of urodynamic testing and electrophysiological OAB indicators of detrusor were measured. The effect of tension on the isolated rat bladder detrusor muscle strips was determined; activators and antagonists of calcium-activated potassium ion channels were detected in vitro using the tension method. The contraction of detrusor muscle strips and the antagonism of acetylcholine due to changes in muscle contraction were observed. RESULTS: The Rhy-treated group significantly decreased the maximum bladder capacity, bladder filling pressure, leak point pressure, contraction frequency, motility index (p < 0.05). The affinity index of Rhy was 4.53 ± 0.22. However, 1 µmol/L to 2 µmol/L Rhy shifts CaCl2 cumulative dose-response curves to the right in a non-parallel manner, showing a non-competitive antagonism. Rhy inhibits detrusor contraction by blocking L-type calcium channels and activating big-conductance calcium-activated potassium channels. A low concentration of Rhy can inhibit muscle contraction caused by intracellular calcium. CONCLUSIONS: Rhy plays an important role in OAB treatment and decreases effectively on sections of urodynamic testing and electrophysiological OAB indicators of detrusor.

Sesquiterpenoids from the mangrove-derived endophytic fungus Diaporthe sp.

A new sesquiterpenoid, diaporol A (1), possessing a unique tricyclic lactone framework, eight new drimane sesquiterpenoids, diaporols B-I (2-9), and the known compounds 10 and 11 were isolated from a culture of the mangrove-derived endophyte Diaporthe sp. The absolute configurations of 1-5 were determined by low-temperature (100 K) single-crystal X-ray diffraction with Cu Kα radiation. The compounds were evaluated for cytotoxic activity; however, no compound showed significant cytotoxicity against the tested cell lines at a concentration of 20 µM.

Precursor-directed fungal generation of novel halogenated chaetoglobosins with more preferable immunosuppressive action.

Precursor-fed cultivation of endophytic Chaetomium globosum 1C51 afforded nine novel "unnatural" halogenated chaetoglobosins including those with more preferable immunosuppressive activity.