Anti-inflammatory Fatty Acid Derivatives From Mangrove-derived Actinomycetes Streptomyces sp.

Mangrove-derived actinomycetes are prolific chemical sources of complex and novel natural products, providing an excellent chance for new drug discovery. The chemical investigation of the mangrove-derived Streptomyces sundarbansensis 06037, led to the discovery of two previously undescribed enone fatty acids (1-2), one new phenylpropionate derivate (3), along with the isolation of the ten known components (4-13). Those chemical structures of isolates were elucidated on the basis of the analysis of diverse spectroscopic data.

Specialized Metabolites from the Husks of Rice Oryza Sativa L. and their Biological Activities.

Rice (Oryza sativa L.) husk harbors a substantial proportion of biological metabolites, as one of the most plentiful agriculture by-products in rice milling process, rice husk remains poorly utilized. As a continuing search for potential bioactive molecules from the husk of rice, a totally of twelve components (1-12), including six sterol ferulates (1-6), one flavonoid (7), one dipeptide (8), and four phenylpropanoid derivatives (9-12) were obtained.

α-Glucosidase inhibitors from the husks of rice Oryza sativa L.

Rice husk is one of the most plentiful agriculture by-products in rice producing areas, which harbors a substantial proportion of biological metabolites, however, it has not been well studied. As an attempt to utilize it as a productive manner, phytochemical investigation on rice husk has performed and led to the isolation of three undescribed (1, 2, and 7), along with twelve known components (3-6, and 8-15). Those chemical structures were elucidated based on massive spectroscopic methods.

Secondary Metabolites from the Fresh Leaves of Pinus yunnanensis Franch.

Fifteen metabolites, including two flavonols (1-2), three lignans (3-5), and ten diterpenoids (6-15), were isolated from the leaves of Pinus yunnanensis. Among them, flavanonol (1) were identified as undescribed flavonol derivative with natural rarely B-ring fission lactone. Massive spectroscopic methods, the DP4+ probabilities and CD/ECD calculations were applied to establish the structure of component 1.

[Spatial-temporal dynamics of grassland NPP and its driving factors in the Loess Plateau, China].

We estimated grassland NPP using CASA model in the Loess Plateau during 2000-2015 and further analyzed the spatiotemporal dynamics, stability and persistence of grassland NPP. The driving factors of grassland NPP were analyzed from four aspects, i.e.

Antibacterial anthraquinone dimers from marine derived fungus Aspergillus sp.

As a continue investigation of the bioactive secondary metabolites from marine derived fungi, two new anthraquinone dimers (1, 2), along with three known anthraquinones (3-5) and two known xanthones (6, 7) were isolated from the marine-derived fungus Aspergillus versicolor. Their structures, including the absolute configurations, were elucidated by NMR, HRMS, and comparison with reported ones. Among them, compounds 1 and 2 were identified as anthraquinone dimers which dimerized by a rare C-O-C ether linkage, and both of them showed selective antibacterial activity against Gram-positive Staphylococcus aureus; whilst compound 6 exhibited moderate cytotoxicity against human cancer cell lines.

Pyocyanin Inhibits Chlamydia Infection by Disabling Infectivity of the Elementary Body and Disrupting Intracellular Growth.

The obligate intracellular bacterium is a widespread human pathogen that causes serious problems, including (but not limited to) infertility and blindness. Our search for novel antichlamydial metabolites from marine-derived microorganisms led to the isolation of pyocyanin, a small compound from Pyocyanin is an effective antichlamydial for all three spp. tested.

Activated production of silent metabolites from marine-derived fungus Penicillium citrinum.

As an attempt to utilize of rare earth elements as a novel method to activate the silent genes in fungus, the marine-derived fungus Penicillium citrinum was cultured under ordinary laboratory fermentation conditions in the presence of scandium chloride (ScCl, 50 μM), and chemical investigation led to the isolation and characterization of three new peptide derivatives (1-3), along with four known pyrrolidine alkaloids (4-7). Those structures were elucidated by spectroscopic data interpretation, as well as chemical reactions. Comparative metabolic profiling of the culture extracts (with/without scandium chloride) indicated that compounds 1-3 scarcely detected in the absence of ScCl.

Biotransformation of 20()-panaxatriol by the fungus Link AS 3.3950.

Microbial transformation of 20()-panaxatriol by the fungus Link AS 3.3950 was performed. Four new (-), along with two previously reported metabolites ( and ), were obtained.

Synthesis of the ABC Tricyclic System of Daphnicyclidin A.

A substrate-stereocontrolled synthesis of the ABC tricyclic system of daphnicyclidin A is developed. The key reactions include an efficient tandem N-allylation-S2' reaction to assemble 2,3,4-cis trisubstituent pyrrolidine ring C and two intramolecular Horner-Wadsworth-Emmons reactions to construct cycloheptanone ring A and piperidine ring B.

Antichlamydial Dimeric Indole Derivatives from Marine Actinomycete Rubrobacter radiotolerans.

Chlamydiae are widely distributed pathogens of human populations, which can lead to serious reproductive and other health problems. In our search for novel antichlamydial metabolites from marine derived-microorganisms, one new () and two known () dimeric indole derivatives were isolated from the sponge-derived actinomycete . The chemical structures of these metabolites were elucidated by NMR spectroscopic data as well as CD calculations.

Antituberculosis compounds from a deep-sea-derived fungus Aspergillus sp. SCSIO Ind09F01.

Eleven diketopiperazine and fumiquinazoline alkaloids (1-11) together with a tetracyclic triterpenoid helvolic acid (12) were obtained from the cultures of a deep-sea derived fungus Aspergillus sp. SCSIO Ind09F01. The structures of these compounds (1-12) were determined mainly by the extensive NMR, ESIMS spectra data and by comparison with previously described compounds.

Acetylcholinesterase inhibitory dimeric indole derivatives from the marine actinomycetes Rubrobacter radiotolerans.

Investigation of the bioactive secondary metabolites of the marine actinomycetes Rubrobacter radiotolerans led to the isolation and characterization of two naturally rare dimeric indole derivatives (1 and 2). The structures of these new compounds were elucidated by spectroscopic data interpretation, and the absolute configurations were assigned by CD calculations. The acetylcholinesterase (AchE) inhibitory activity of compounds 1 and 2 was evaluated, both of which showed moderate activity with IC50 values of 11.

Epimeric methylsulfinyladenosine derivatives from the marine ascidian Herdmania momus.

Investigation of the secondary metabolites of the ascidian Herdmania momus led to the isolation and characterization of four new nucleoside derivatives (1-4). Structural studies showed that these derivatives represent a series of rare methylsulfinyladenosine derivatives of interconvertible transesterification isomers and/or sulfinyl epimers. The antiviral activities of these rare nucleosides were evaluated against a series of human pathogenic viruses.

PPAR-γ agonistic metabolites from the ascidian Herdmania momus.

Seven new amino acid derivatives (1-4 and 6-8) were isolated from MeOH extracts of the marine ascidian Herdmania momus. Planar structures were established on the basis of NMR, IR, and MS spectroscopic analyses. Absolute configurations of these compounds were derived from specific rotation and CD analysis.

A new cyclic tetrapeptide from the jellyfish-derived fungus Phoma sp.

A new cyclic tetrapeptide (1), along with known congeners (2, 3), was isolated from the fungus Phoma sp. derived from the giant jellyfish Nemopilema nomurai. The absolute configuration of 1 was determined using the modified Mosher's method and Marfey's method.

Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists.

On the basis of a marine fungal phthalide (paecilocin A) skeleton, we synthesized 20 analogs and evaluated them for peroxisome proliferator-activated receptor gamma (PPAR-γ) binding and activation. Among these analogs, 6 and 7 had significant PPAR-γ binding activity, and 7 showed further PPAR-γ activation in rat liver Ac2F cells. In docking simulation, 7 formed H bonds with key amino acid residues of the PPAR-γ binding domain, and the overall positioning was similar to rosiglitazone.

Removal of hepatocellular carcinoma extending into the right atrium with extracorporeal circulation.

Hepatocellular carcinoma with tumor thrombus extending into the right atrium is rare and has an extremely poor prognosis. Surgery was once regarded as a contraindication, then as a palliative method to prevent emergencies such as pulmonary embolism or heart failure. With advances of imaging techniques, hepatectomy and widespread use of extracorporeal circulation, conventional viewpoint has gradually changed.

Cytotoxic cytochalasins from the endozoic fungus Phoma sp. of the giant jellyfish Nemopilema nomurai.

Four new cytochalasin derivatives (1-4), together with cytochalasin B (5), were isolated from the fungus Phoma sp. obtained from the giant jellyfish Nemopilema nomurai. The planar structure and relative stereochemistry were established by analysis of 1D and 2D NMR data.

Anti-inflammatory amino acid derivatives from the ascidian Herdmania momus.

Four new amino acid derivatives, herdmanines A-D (1-4), were isolated from the marine ascidian Herdmania momus. Herdmanines A-C contain the unusual D-form of arginine. Compounds 3 and 4 had a moderate suppressive effect on the production of NO, with IC₅₀ values of 96 and 9 μM, respectively.

Antibacterial polyketides from the jellyfish-derived fungus Paecilomyces variotii.

Four new polyketides (1-4) were isolated from the fungus Paecilomyces variotii, which was derived from the jellyfish Nemopilema nomurai. The planar structures and relative configurations of these polyketides were elucidated on the basis of spectroscopic analyses, including 2D NMR experiments. The compounds showed inhibitory activity against pathogenic bacteria including methicillin-resistant Staphylococcus aureus 3089 and multi-drug-resistant Vibrio parahemolyticus 7001 with MIC values in the range 5-40 μg/mL.

Oxygenated hexylitaconates from a marine sponge-derived fungus Penicillium sp.

In the course of our search for bioactive metabolites from marine organisms, new hexylitaconic acid derivatives (1-4), along with (3S)-hexylitaconic acid (5), were isolated from a sponge-derived fungus Penicillium sp. Based on the NMR and MS data, the structures of compounds 1-4 were defined as α,β-dicarboxylic acid derivatives, such as hexylitaconic acid and tensyuic acids which were previously reported as metabolite of Aspergillus niger, Penicillium striatisporum, or Apiospora montagnei. The isolated compounds were evaluated for cytotoxicity against a panel of five human solid tumor cell lines, and for anti-inflammatory activity gauged by their inhibitory effects on the production of major pro-inflammatory mediators (nitric oxide (NO), interleukin (IL)-6, tumor necrosis factor (TNF)-α, and IL-1β) in murine macrophage cells.

An optimized assay for transcription factor NF-kappaB with dsDNA-coupled microplate.

To develop an EMSA-free assay approach for analyzing the sequence-specific DNA-binding proteins (DBPs), an easy cost-effective dsDNA-coupled plate (dcPlate) was developed in our lab for this purpose. In this paper, the assay conditions of such dcPlate were fully optimized for detecting an important transcription factor, NF-kappaB. The optimized parameters of dcPlate for assay of NF-kappaB were as follows: immobilized DNA probe at the concentration of 25 pmol/100 microL-well, incubation time of 90 min for NF-kappaB binding to dcPlate, primary and secondary antibody concentration of 0.

Assay of DNA-binding proteins with a dsDNA-coupled plate.

Objectives: This paper fabricated a cost-effective dsDNA-coupled plate (dcPlate) and applied it to measure the abundance and DNA-binding activity of a DNA-binding protein (DBP).

Design And Methods: The dcPlate was manufactured by covalently immobilizing an amino-modified oligonucleotide in wells of the plate coated with N-oxysuccinimide esters. The dcPlate was applied to measure the abundance of DNA-binding activity of a DBP in the same four steps, including protein incubation, primary antibody binding, enzyme-linked secondary antibody binding, and colorimetric development.