Asperolide A, a marine-derived tetranorditerpenoid, induces G2/M arrest in human NCI-H460 lung carcinoma cells, is mediated by p53-p21 stabilization and modulated by Ras/Raf/MEK/ERK signaling pathway.

Here we first demonstrate that asperolide A, a very recently reported marine-derived tetranorditerpenoid, leads to the inhibition of NCI-H460 lung carcinoma cell proliferation by G2/M arrest with the activation of the Ras/Raf/MEK/ERK signaling and p53-dependent p21 pathway. Treatment with 35 µM asperolide A (2 × IC(50)) resulted in a significant increase in the proportion of G2/M phase cells, about a 2.9-fold increase during 48 h. Immunoblot assays demonstrated time-dependent inhibition of G2/M regulatory proteins. Moreover, asperolide A significantly activated MAP kinases (ERK1/2, JNK and p38 MAP kinase) by phosphorylation, and only the inhibition of ERK activation by PD98059 reversed downregulation of G2/M regulatory proteins CDC2, and suppressed upregulation of p21 and p-p53 levels. Transfection of cells with dominant-negative Ras (RasN17) mutant genes up-regulated asperolide A-induced the decrease of cyclin B1 and CDC2, suppressed Raf, ERK activity and p53-p21 expression, and at last, abolished G2/M arrest. This study indicates that asperolide A-induced G2/M arrest in human NCI-H460 lung carcinoma cells relys on the participation of the Ras/Raf/MEK/ERK signaling pathway in p53-p21 stabilization. An in vivo study with asperolide A illustrated a marked inhibition of tumor growth, and little toxcity compared to Cisplatin therapy. Overall, these findings provide potential effectiveness and a theoretical basis for the therapeutic use of asperolide A in the treatment of malignancies.

Asperolides A-C, tetranorlabdane diterpenoids from the marine alga-derived endophytic fungus Aspergillus wentii EN-48.

Bioassay-guided fractionation of the culture extract of Aspergillus wentii EN-48, an endophytic fungus isolated from an unidentified marine brown algal species of the genus Sargassum, led to the isolation of three new tetranorlabdane diterpenoids, asperolides A-C (1-3), and five related derivatives (4-8). The structures of these compounds were established on the basis of spectroscopic interpretation, and compound 1 was confirmed by X-ray crystallographic analysis. The absolute configuration of 1 was determined by application of the modified Mosher's method. An X-ray structure for wentilactone B (6) is also reported. Compounds 1-8 were evaluated for cytotoxic and antibacterial activities.

Triazole and dihydroimidazole alkaloids from the marine sediment-derived fungus Penicillium paneum SD-44.

A novel triazole carboxylic acid, penipanoid A (1), two new quinazolinone alkaloids, penipanoids B (2) and C (3), and a very recently reported quinazolinone derivative (4) were isolated from the marine sediment-derived fungus Penicillium paneum SD-44. Their structures were elucidated by spectroscopic analysis, and the structure for 1 was confirmed by X-ray crystallographic analysis. Compound 1 represents the first example of a triazole derivative from marine sediment-derived fungi, and compound 2 is a rare quinazolinone derivative having a dihydroimidazole ring system. The cytotoxicity of compounds 1 and 4 and the antimicrobial activity of 1-4 were evaluated.

A high-nuclearity complex containing a decanuclear iron(iii)/oxo cage in a football-like structure and rare (R-/S)-hemiacetalate ligands in a butterfly-like format.

A challenge in the field of high nuclearity Fe(iii)/oxo cluster chemistry remains the development of new synthetic methods to such molecules. In this work, the employment of pyridine-2-carboxaldehyde (py-2-al) in high-nuclearity transition-metal cluster chemistry has provided access to an unprecedented decanuclear iron(iii) complex, [Fe10(NO3)7(O)6(OH0.5)2((S)-py-hemi)4((R)-py-hemi)4]·4H2O (1) ((R-/S)-py-hemi = (R-/S)-pyridine-2-carboxaldehyde hemiacetalate). The synthesis, beautiful structure and the physical characterization (thermal gravimetric analysis, X-ray powder diffraction, proton nuclear magnetic resonance, magnetic susceptibility) of complex 1 are described in this contribution. Complex 1 provides a new route to obtain high nuclearity magnetic clusters with beautiful structures.

Degradation of crude oil by indigenous microorganisms supplemented with nutrients.

Different kinds of mineral nutrients(NO3-N, NH4-N and PO4-P) were applied in the simulated oil-polluted seawater for enhancing oil biodegradation in the N/P ratio 10:1 and 20:1. Although indigenous microorganisms have the ability to degrade oil, adding nutrients accelerated biodegradation rates significantly. For the group amended with NO3-N and PO4-P in the ratio 10:1, the reaction rate coefficient was 4 times higher than the natural biodegradation. Chemical and microbiological analysis showed that the optimal N/P ratio in the system is 10:1, and microorganisms tend to utilize nitrate rather than ammonium as N source.