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*

Response surface methodology (RSM) was used to optimizing the ultrasonic-assisted extraction technology of pigment from Coreopsis tinctoria. The results showed that the flavonoids were the main constituents of the pigment Based on single factor experiments, a four-factor-level experiment design were developed by box-benhnhen central composite design method with causal factors of ultrasonic temperature, ultrasonic time, ratio of liquid to raw material, the concentrations of ethanol in solvent and the extract absorbance value for the response. The interactive effects of four crucial technological parameters were assessed by response surface methodology (RSM). The optimum ultrasonic-assisted extraction conditions were as follow: ultrasonic temperature was 70 °C, ultrasonic time was 60 min, the concentrations of ethanol in solvent was 72.25% and the ratio of liquid to raw material was 32.05:1 mL . g-1. Under the optimum extraction technology conditions, the absorbance value was 0. 936. The conditidns are suitable for the extraction process regression analysis and parameter optimization.
Coreopsis ; chemistry ; Ethanol ; Flavonoids ; isolation & purification ; Pigments, Biological ; isolation & purification ; Plant Extracts ; isolation & purification ; Plants, Medicinal ; Regression Analysis ; Solvents ; Temperature ; Time Factors ; Ultrasonics

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

OBJECTIVEThis study is to investigate the effect of tea polyphenols and tea pigments on telomerase activity of human liver cancer cell line, HepG2 cells.

METHODSTRAP-PCR-ELISA was applied to investigate the telomerase activity.

RESULTSTelomerase was positive in tea polyphenols treated groups, tea pigments treated groups and blank control group. Telomerase activities (A(450 approximately 690) values) were 1.56 and 1.46 in 50 mg/L and 100 mg/L tea polyphenols-treated groups, 1.55 and 1.49 in 50 mg/L and 100 mg/L tea pigments-treated groups, respectively. The results showed that telomerase activity was significantly inhibited by tea polyphenols and tea pigments treatment as compared with the blank control group (A(450 approximately 690) = 2.11).

CONCLUSIONSTea polyphenols and tea pigments could significantly inhibit telomerase activity of HepG2 cells, and telomerase activity may be a useful biomarker for cancer chemoprevention.

Biomarkers, Tumor ; metabolism ; Carcinoma, Hepatocellular ; enzymology ; pathology ; Flavonoids ; isolation & purification ; pharmacology ; Humans ; Liver Neoplasms ; enzymology ; pathology ; Phenols ; isolation & purification ; pharmacology ; Pigments, Biological ; isolation & purification ; pharmacology ; Polyphenols ; Tea ; chemistry ; Telomerase ; metabolism ; Tumor Cells, Cultured