This study identified six novel azaphilones, isochromophilones G-L (1-6), and three novel biosynthetically related congeners (7-9) from Diaporthe sp. SCSIO 41011. The structures and absolute configurations were elucidated through comprehensive spectroscopic analyses combined with experimental and calculated electronic circular dichroism (ECD) spectra. Significantly, three highly oxygenated azaphilones contain an acetyl group at the terminal chain (4) or linear conjugated polyenoid moieties (5 and 6), which occur infrequently in the azaphilone family. Additionally, several compounds demonstrated inhibition of lipopolysaccharide (LPS)-induced nuclear factor kappa-B (NF-κB) activation in RAW 264.7 macrophages at 20 μmol·L^-1. The novel compound (1) effectively inhibited receptor activator of NF-κB ligand (RANKL)-induced osteoclast differentiation without exhibiting cytotoxicity in bone marrow and RAW 264.7 macrophages, indicating its potential as a promising lead compound for osteolytic disease treatment. This research presents the first documented evidence of azaphilone derivatives as inhibitors of RANKL-induced osteoclastogenesis.
Animals ; Mice ; RANK Ligand/genetics* ; RAW 264.7 Cells ; Osteoclasts/metabolism* ; Benzopyrans/isolation & purification* ; Osteogenesis/drug effects* ; Macrophages/metabolism* ; Molecular Structure ; Pigments, Biological/isolation & purification* ; Ascomycota/chemistry* ; NF-kappa B/genetics* ; Cell Differentiation/drug effects*

The diethyl sulfate (DES) mutagenesis was chosen for the mutagenic treatment to Phellinus igniarius, and the relationship of mutagenesis time and death rate was investigated with 0.5% DES. The differences of mycelial growth speed, liquid fermentation mycelia biomass, morphology and pigment classes of secondary metabolites production speed and antioxidant activities of metabolite products were discussed. The study displayed that DES mutagenesis could change mycelial morphology without obvious effect on mycelium growth, and the DES mutagenesis improved antioxidant activities of the active ingredients of P. igniarius and had more antioxidant activity of hypoxia/sugar PC12 nerve cells than that of P. igniarius.
Basidiomycota ; drug effects ; genetics ; growth & development ; metabolism ; Mutagenesis ; Mutagens ; pharmacology ; Mycelium ; drug effects ; genetics ; growth & development ; metabolism ; Pigments, Biological ; analysis ; metabolism ; Secondary Metabolism ; drug effects ; Sulfuric Acid Esters ; pharmacology

No abstract available.
Aged ; Anti-Bacterial Agents/therapeutic use ; Bacteria/metabolism ; Catheter-Related Infections/diagnosis/drug therapy/*microbiology ; Color ; Equipment Design ; Escherichia coli Infections/diagnosis/drug therapy/*microbiology ; Female ; Humans ; Intestines/*microbiology ; Pigments, Biological/metabolism ; Treatment Outcome ; Tryptophan/metabolism ; Urinary Bladder Neoplasms/surgery ; Urinary Catheterization/adverse effects/*instrumentation ; *Urinary Catheters ; *Urinary Diversion ; Urinary Tract Infections/diagnosis/drug therapy/*microbiology ; Urine/chemistry/microbiology

OBJECTIVETo investigate the inhibitory effect of lycium pigment on lipopolysaccharide (LPS)-induced uveitis in rats and its mechanism.

METHODThe rat uveitis model was established by 30-day oral administration of lycium pigment (50, 100, 200 mg x kg(-1)) and footpad injection of LPS. Ocular tissues were collected for a histopathological inspection. The protein, nitric oxide and ADMA in aqueous humor, level of inducible nitric oxide synthase (iNOS) in retina, activities of serum total antioxidant capacity (T-AOC), superoxide dismutase (SOD) and glutathione peroxidase (GSH-PX), and content of malondialdehyde (MDA) were determined by using Western blot, ELISA and biochemical methods.

RESULTAccording to the pathological study, lycium pigment (50, 100, 200 mg x kg(-1)) could notably reduce the inflammatory cell infiltration around corpus ciliare matrix of uveitis rats, and the concentration of protein and nitric oxide, and increased ADMA in aqueous humor. Lycium pigment (100, 200 mg x kg(-1)) could significantly inhibit the expression of iNOS in ocular tissues. In addition, lycium pigment (100, 200 mg x kg(-1)) also decrease the activities of serum T-AOC, SOD, GSH-PX, and the content of lipid peroxide MDA.

CONCLUSIONLycium pigment has the inhibitory effect on LPS-induced uveitis in rats. Its mechanism is related to the regulation of nitric oxide/ADMA pathway and the improvement of oxidation resistance.

Animals ; Glutathione Peroxidase ; genetics ; metabolism ; Humans ; Lipopolysaccharides ; adverse effects ; Lycium ; chemistry ; Male ; Malondialdehyde ; metabolism ; Nitric Oxide Synthase Type II ; genetics ; metabolism ; Pigments, Biological ; administration & dosage ; Plant Extracts ; administration & dosage ; Rats ; Rats, Sprague-Dawley ; Superoxide Dismutase ; genetics ; metabolism ; Uveitis ; chemically induced ; genetics ; metabolism ; prevention & control

Animals ; Embryo, Mammalian ; Humans ; Photoreceptor Cells, Vertebrate ; metabolism ; physiology ; Retinal Ganglion Cells ; metabolism ; physiology ; Retinal Pigments ; metabolism

S-adenosylmethionine-dependent uroporphyrinogen III methyltransferase (SUMT) is a novel red fluorescence indicator. However, the production of SUMT in Escherichia coli is restricted by its relatively low solubility, and little is known about the red fluorescent materials that are associate with SUMT. Two individual SUMT mutations, L166A and L88R/L89G double mutant were produced by site-directed mutagenesis. Both mutants were overexpressed in E. coli and purified by Ni-NTA chromatography. The reddish mixtures isolated from the purified L88R/L89G double mutant were analyzed by UV-visible spectra scanning and mass analysis(MS). The L88R/L89G double mutant has enzymatic activity in vivo, whereas L166A mutant loses the activity. Trimethylpyrrocorphin is identified as the main constituent in the isolated pigments. The purified L88R/L89G mutant increases protein solubility, which is applied potentially as the fluorescent indicator denoting the solubility of protein fusion partner.
Amino Acid Substitution ; Electrophoresis, Polyacrylamide Gel ; Escherichia coli ; genetics ; Fluorescence ; Mass Spectrometry ; Methyltransferases ; chemistry ; genetics ; metabolism ; Molecular Weight ; Mutagenesis, Site-Directed ; methods ; Mutation ; Pigments, Biological ; chemistry ; metabolism ; Plant Proteins ; chemistry ; genetics ; metabolism ; Recombinant Proteins ; chemistry ; metabolism ; Solubility ; Spectrophotometry, Ultraviolet ; Zea mays ; enzymology ; genetics

OBJECTIVETo observe dynamically the effect of drugs for clearing heat and removing dampness (CHRD) on biliary components in rabbits with pigment gallstones (PGS).

METHODSForty rabbits were established into PGS model and randomly divided into 3 groups, the bacterial infection group, the CHRD low-dose group and the CHRD high-dose group. Besides, a normal group was set up with healthy rabbits for control. Changes of total bilirubin (TB), unconjugated bilirubin (UCB), total bile acid (TBA), Ca2+, bacterial and endogenous beta-glucuronidase (beta-Gase) in bile were observed.

RESULTSCHRD drugs significantly decreased the contents of UCB, Ca2+, bacterial and endogenous beta-Gase (P < 0.05), and increased TBA in bile (P < 0.05).

CONCLUSIONCHRD drugs have good effect in reducing the lithogenesis of the pigment gallstones.

Animals ; Bile ; drug effects ; metabolism ; Bile Pigments ; metabolism ; Calcium ; metabolism ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Gallstones ; drug therapy ; metabolism ; pathology ; Glucuronidase ; metabolism ; Male ; Phytotherapy ; Rabbits ; Random Allocation ; Treatment Outcome

OBJECTIVETo obtain the full-length cDNA of a novel gene (named yp05) associated with citrinin production-related genes in Monascus aurantiacus.

METHODSTotal RNA was extracted from mycelium, 3' and 5' cDNA end of yp05 gene was amplified using smart trace cDNA amplification kit, and the full-length cDNA of a novel gene (named yp05) was obtained from the electronic assembly of 3'-RACE and 5'-RACE products.

RESULTSThis yp05 gene was 787 bp including a 597 bp open reading frame (ORF) and encoded a deduced protein with 199 amino acid residues, and the amino acid sequence of this protein was found similar with the sequences of many fungal manganese-superoxide dismutases in the GenBank with the aid of BLASTp. The transcription of yp05 gene in Monascus strains was analyzed with the aid of Northern blotting. The transcription of yp05 gene was only detected in Monascus strains, provided that citrinin was produced.

CONCLUSIONThe transcription of yp05 gene belongs to differential expression genes of citrinin yielded from Monascus and has no correlation with the biosynthesis pathway of red pigments.

Amino Acid Sequence ; Base Sequence ; Blotting, Northern ; Citrinin ; biosynthesis ; Cloning, Molecular ; DNA, Complementary ; chemistry ; Fungal Proteins ; chemistry ; genetics ; Gene Library ; Molecular Sequence Data ; Monascus ; genetics ; metabolism ; Mycelium ; genetics ; metabolism ; Pigments, Biological ; biosynthesis ; RNA, Messenger ; metabolism ; Sequence Alignment ; Sequence Analysis, DNA

OBJECTIVETo investigate the relationship between anatomic abnormalities and malfunction of Oddi sphincter with formation of bile duct pigment gallstone.

METHODSOne hundred and twenty-three patients with a T tube after cholecystectomy and choledochotomy were divided into reflux group and control group by measuring the amounts of radioactivity of (99m)Tc-DTPA in the bile. Among them 53 were selected randomly to undergo choledochoscopic manometry. Basal pressure of Oddi's sphincter (SOBP), amplitude of Oddi's sphincter (SOCA), frequency of contraction (SOF), duration of contraction (SOD), duodenal pressure (DP), common bile duct pressure (CBDP) were scored and analyzed. The level of plasma motilin and serum gastrin of 45 patients and 12 healthy volunteers were measured by radioimmunoassay. The incidence rates of duodenal descending part diverticulum in patients with bile duct pigment stones, patients without alimentary tract diseases, patients with gallbladder polyps, patients with gallbladder stones were studied by means of barium meal examination. The incidence rates of intraduodenal peri-ampullary diverticulum in patients with primary bile duct pigment stones, patients with bile duct stone and gallbladder stones, patients with bile duct stones originating from the gallbladder, patients with inflammation and stricture of the extremity of bile duct and papilla, patients with cancer of the extremity of bile duct and papilla, patients with post-cholecystectomy syndrome were detected by duodenoscope.

RESULTSOf the patients, 44 were detected with duodenal-biliary reflux (35.8%). SOBP, SOCA and CBDP in the reflux group were much lower than those in control group (P < 0.001). The level of serum gastrin and plasma motilin of the reflux group were much lower than those of control group (P < 0.01). Positive correlation was found between level of motilin and SOBP while level of gastrin was positively correlated with SOBP and CBDP. The incidence of duodenal diverticulum in patients with bile duct pigment stone was 36.62%, which was higher than that of the other 3 groups. The incidence rate of intraduodenal peri-ampullary diverticulum in patients with primary bile duct pigment stone was higher than that of patients with inflammation and stricture of the extremity of bile duct and papilla, patients with cancer of the extremity of bile duct and papilla and patients with bile duct stones originating from the gallbladder.

CONCLUSIONSThe patients with bile duct pigment stone have apparent duodenal-biliary reflux and infection of the bile duct. The state of structure and function of Oddi's sphincter is correlated significantly with bile duct pigment stone. The anatomic abnormalities and malfunction of Oddi's sphincter played an important role in the formation of bile duct pigment stone.

Adult ; Aged ; Aged, 80 and over ; Bile Pigments ; metabolism ; Cholelithiasis ; metabolism ; pathology ; physiopathology ; Female ; Gastrins ; blood ; Humans ; Male ; Middle Aged ; Motilin ; blood ; Pressure ; Radioimmunoassay ; Retrospective Studies ; Sphincter of Oddi ; pathology ; physiopathology

OBJECTIVETo elvaulate the antioxidant activity of the pigment of Lycium ruthenicum.

METHODThe antioxidant activities were measured by the effects of the reducing ability, scavenging DPPH. H2O2-induced hemolysis of mice erythrocyte, serum resistance of reactive oxygen species, content of MDA in liver tissue, and swelling effect of mitochondria in liver tissue.

RESULTThe pigment of L. ruthenicum could scaveng DPPH* remarkably with IC50 0.164 mg x mL(-1), inhibitte hemolysis of mice erythrocyte evidently with IC50 0.112 mg x mL(-1). The resistant of reactive oxygen species was enhanced by the tested substances, simultanously. The concentration of MDA of peroxidation of lipid in mice liver could be reduced, and the swelling of mice liver mitochondria alse be restrained.

CONCLUSIONThe pigment of L. ruthenicum has antioxidant activity in tested concentration.

Animals ; Antioxidants ; pharmacology ; Biphenyl Compounds ; metabolism ; Erythrocytes ; drug effects ; Free Radical Scavengers ; pharmacology ; Hemolysis ; drug effects ; Hydrazines ; metabolism ; Lipid Peroxidation ; drug effects ; Liver ; metabolism ; Lycium ; chemistry ; Malondialdehyde ; metabolism ; Mice ; Mitochondria, Liver ; pathology ; Mitochondrial Swelling ; drug effects ; Phenols ; isolation & purification ; pharmacology ; Picrates ; Pigments, Biological ; isolation & purification ; pharmacology ; Plants, Medicinal ; chemistry ; Reactive Oxygen Species