Biotransformation of total coumarins of Radix Glehniae by Lecanicillium attenuatum W-1-9.

The biotransformation of total coumarins of Radix Glehniae by Lecanicillium attenuatum W-1-9 yielded three new products, lecaniside A (1), lecaniside B (2), and lecaniside C (3). The chemical structures of these metabolites were elucidated based on extensive spectral data, including 2D NMR and HRMS. The hydrogenation, dealkylation, glycosylation, and O-methylation reactions of these metabolites were observed in the present study. In the in vitro assays, compound 1 displayed a little PTP1B inhibitory activity.

Tanshinone IIA reduces the risk of Alzheimer's disease by inhibiting iNOS, MMP­2 and NF­κBp65 transcription and translation in the temporal lobes of rat models of Alzheimer's disease.

Tanshinone IIA (Tan IIA), one of the major active constituents of the medicinal herb Salvia miltiorrhiza, has been reported to possess neuroprotective effects against the pathological features of Alzheimer's disease (AD), but the molecular mechanism underlying this effect remains unclear. To examine the effect of Tan IIA on AD, as well as the underlying molecular mechanisms, in vivo animal experiments and in vitro molecular biology investigations were employed in the present study. Firstly, a rat model of AD was successfully established by direct injection of the amyloid beta protein (Aß) and then these rats were administered an interventional treatment of Tan IIA. The learning and memory ability of rats was evaluated in four groups (Control, Sham, AD and Tan IIA) utilizing a Morris water maze test. Quantitative (q)PCR was employed to detect the mRNA expression of inducible nitric oxide synthase (iNOS), matrix metalloproteinase­2 (MMP­2) and nuclear transcription factor kappa (NF­κBp65) in temporal lobe tissues and protein expression was determined with western blot analysis. In addition, association analyses between iNOS, MMP­2 and NF­κBp65 at a transcriptional and translational level were performed utilizing Spearman's correlation analysis. In the present study, the results revealed that rats in the AD group demonstrated significant disruptions in learning and memory ability, and the symptoms were evidently reduced by Tan IIA. Furthermore, the upregulation of iNOS, MMP­2 and NF­κBp65 at a transcriptional and translational level in AD rats was distinctly inhibited by Tan IIA. Therefore, it was concluded that iNOS, MMP­2 and NF­κBp65 are involved in AD development, and Tan IIA may reduce AD risk by inhibiting transcription and translation of these genes. Furthermore, the positive correlation of iNOS and MMP­2 with NF­κBp65, respectively, provides evidence supporting the hypothesis that Tan IIA reduces AD risk by inhibiting iNOS and MMP­2 at a transcriptional and translational level through the NF­κB pathway. In summary, Tan IIA is an effective neuroprotective agent for AD therapy, and iNOS, MMP­2 and NF­κBp65 may be the potential molecular targets for manipulating this effect therapeutically.

Traditional Chinese medicine--sea urchin.

The sea urchin is an ancient, common, seafloor-dwelling marine invertebrate that belongs to the phylum Echinodermata. There are multiple species of sea urchin with resources that are widely distributed in China, where they were used in ancient times as Traditional Chinese Medicine for treating a variety of diseases. At present, it is known that the shell, spine and gonad of the sea urchin have many medicinal values determined through modern research. In this paper, we summarized the major chemical constituents and medicinal value of the sea urchin.

A new aromatic glycoside from Glehnia littoralis.

A new aromatic glycoside (1) was isolated from the roots of Glehnia littoralis Fr. Schmidtex Miq. Its structure was elucidated as vanillic acid 1-O-[ß-D-apiofuranosyl-(1 → 6)-ß-D-glucopyranoside] ester mainly by analysing the NMR and MS spectral data. In the in vitro assays, compound 1 displayed some TNF-α secretion inhibitory activity.

ß-D-Glucosyl-(1-4)-α-L-thevetosides of 17ß-digitoxigenin from seeds of Cerbera manghas L. induces apoptosis in human hepatocellular carcinoma HepG2 cells.

ß-D-Glucosyl-(1-4)-α-L-thevetosides of 17ß-digitoxigenin (GHSC-73) is a cardiac glycoside isolated from the seeds of Cerbera manghas L. GHSC-73 reduced viability of HepG2 cells in a time- and dose-dependent manner without decreasing the viability of Chang human liver cells and Swiss albino 3T3 fibroblasts, induced efficiently stimulated apoptosis in HepG2 cells as evidenced by DNA fragmentation, annexin V/PI binding assay and DAPI staining. This apoptotic process was accompanied by the activation of the effector caspase-3, the loss of mitochondrial membrane potential (ΔΨ(m)) and translocation of AIF from the mitochondrion to the nucleus in HepG2 cells. In addition, a broad-spectrum caspase inhibitor (z-VAD-fmk) tested in this experiment partially prevent HepG2 cells from GHSC-73-induced cell death, but did not affect translocation of AIF from the mitochondrion to the nucleus after GHSC-73 treatment. Our results firstly show that GHSC-73 inhibits the growth of HepG2 cells through caspase-dependent and -independent apoptosis pathways.

Description of a sulfitobacter strain and its extracellular cyclodipeptides.

A marine bacterium M44 was separated from 30 m deep seawater in the East China Sea (26° 28.3' N 122° 29.0' E) in 2006. 16S rDNA gene sequence comparison showed that the strain M44 was a member of the genus Sulfitobacter and highly similar to KMM 3554(T). A series of experiments demonstrated that this strain M44 had many distinctive characteristics: its cells were gram-negative and mesophilic; its colonies were slightly yellowish, round, convex, and smooth; and it could grow at 10-28°C, pH 6.0-10.0, and in the presence of 0-12.5% (w/v) NaCl; the optimum growth conditions were 25°C and pH 7.0, and the optimum Na(+) concentration was 2.5%. In addition, strain M44 contained 18 : 1 ω7c, 11 methyl 18 : 1 ω7c and 16 : 0 fatty acids as major fatty acids, and the genomic DNA G+C content was 58.04 mol%. According to our results of the secondary metabolites, six cyclodipeptides were isolated from the strain M44, which were Cyclo (Val-Leu), Cyclo (Phe-Val), Cyclo (Phe-Leu), Cyclo (Leu-Ile), Cyclo (Phe-Ile), and Cyclo (Trp-Pro). It is the first study of secondary metabolites isolated from this genus.

A preliminary study of the microbial resources and their biological activities of the East china sea.

East China Sea is one of the four sea areas in China, which possesses peculiar ecological environment and many kinds of living creatures, especially the microorganisms. We established the East China Sea microorganism library (during 2006-2010) for the first time, which stored about 30000 strains that covered most kinds of the species. In this paper, 395 pure strains of East China Sea microorganism library which belong to 33 different genera were mainly introduced. Sulfitobacter, Halomonas, Bacillus, Pseudoalteromonas, and Idiomarina were the most dominant species. On the large-scale biological activity screening of the 395 strains, 100 strains possess different biological activities based on different screening models, of which 11.4% strains have antibacterial activities, 15.9% have cytotoxicity activities, and 6.1% have antioxidation activities. Besides, the secondary metabolites of 6 strains with strong biological activities were studied systematically; diketopiperazines and macrocyclic lactones are the active secondary metabolites. The species and the biological activity of microorganisms diversity, the abundant structure type of the secondary metabolites, and their bioactivities all indicate that East China Sea is a potent marine microorganisms-derived developing resource for drug discovery.

Neriifolin from seeds of Cerbera manghas L. induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells.

The effects of neriifolin, a cardiac glycoside from Cerbera manghas L. on various end-points of oncologic relevance (cell growth, cell cycle regulation, and apoptosis in HepG2 cells) were investigated. Neriifolin reduced viability of HepG2 cells, induced S and G2/M phase arrests of the cell cycle, and stimulated apoptosis of HepG2 cells. Stimulation of HepG2 cells with neriifolin induced activation of caspase-3, -8, and -9, and up-regulated expression of Fas and FasL proteins. Based on these results, neriifolin could be considered a candidate for the treatment of hepatocellular carcinoma.

Iridoid glycosides from Saprosma ternatum.

Three new iridoid glycosides, epiasperuloside (1), epipaederosidic acid (2), and epipaederoside (3), together with 7 known compounds, were isolated from the 85% ethanol extract of the leaves of Saprosma ternatum Hook. f. Their structures were determined by application of spectroscopic (NMR, MS) and chemical methodologies. The antioxidant activity was evaluated for all isolates in terms of both DPPH and ABTS bioassays. Epiasperuloside (1) showed some antioxidant activity.

Superoxide radicals scavenging and xanthine oxidase inhibitory activity of magnesium lithospermate B from Salvia miltiorrhiza.

In this study we investigated the superoxide radicals scavenging effect and xanthine oxidase inhibitory activity by magnesium lithospermate B, which was originally isolated from the roots of Salvia miltiorrhiza (also named Danshen or Dansham), an important herb in Oriental medicine. Superoxide radicals were generated both in beta-NADH/PMS system and xanthine/ xanthine oxidase system. Magnesium lithospermate B significantly inhibited the reduction of NBT induced by superoxide radicals with an IC(50) of 29.8 microg/mL and 4.06 microg/mL respectively in the two systems. Further study suggested that magnesium lithospermate B can directly inhibit xanthine oxidase and exhibits competitive inhibition. Magnesium lithospermate B was also found to have the hypouricemic activity in vivo against potassium oxonate-induced hyperuricaemia in mice. After oral administration of magnesium lithospermate B at doses of 10, 20 and 30 mg/kg, there was a significant decrease in the serum urate level when compared to the hyperuricemia control. In addition, magnesium lithospermate B significantly protected HL-60 cells from superoxide radicals-induced apoptosis in the xanthine/ xanthine oxidase reactions. This study provided evidence that magnesium lithospermate B exhibits direct superoxide radicals scavenging and xanthine oxidase inhibitory activity.