Novel Natural Oximes and Oxime Esters with a Vibralactone Backbone from the Basidiomycete Boreostereum vibrans.

A variety of novel natural products with significant bioactivities are produced by the basidiomycete Boreostereum vibrans. In the present study, we describe 16 novel natural oximes and oxime esters with a vibralactone backbone, vibralactoximes, which were isolated from the scale-up fermentation broth of B. vibrans. Their structures were determined through extensive spectroscopic analyses. These compounds represent the first oxime esters from nature. The hypothetical biosynthetic pathway of these compounds was also proposed. Seven compounds exhibited significant pancreatic lipase inhibitory activity, while ten compounds exhibited cytotoxicities against five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW480), with IC50 values comparable with those of cisplatin.

Chemical constituents from fruiting bodies of Basidiomycete Perenniporia subacida.

Four new aromatic abietane diterpenoids and two new benzene derivatives, namely perenacidins A-F (1-6), have been isolated from the fruiting bodies of Basidiomycete Perenniporia subacida. The structures were elucidated by means of extensive spectroscopic methods and computational ECD method. The antifungal activities against Canidia albicans and the cytotoxic activities against four cancer cell lines (including K-562, A-549, SMMC-7721, MCF-7) were evaluated in vitro.

Structure-Based Optimization and Biological Evaluation of Pancreatic Lipase Inhibitors as Novel Potential Antiobesity Agents.

The unusual fused ß-lactone vibralactone was isolated from cultures of the basidiomycete Boreostereum vibrans and has been shown to significantly inhibit pancreatic lipase. In this study, a structure-based lead optimization of vibralactone resulted in three series of 104 analogs, among which compound C1 exhibited the most potent inhibition of pancreatic lipase, with an IC50 value of 14 nM. This activity is more than 3000-fold higher than that of vibralactone. The effect of compound C1 on obesity was investigated using high-fat diet (HFD)-induced C57BL/6 J obese mice. Treatment with compound C1 at a dose of 100 mg/kg significantly decreased HFD-induced obesity, primarily through the improvement of metabolic parameters, such as triglyceride levels.

Triterpenoids from the spores of Ganoderma lucidum.

Recently a series of triterpenoids were isolated from ganoderma spores and have drawn the attention of chemists and pharmacists. The aim of this review is to summarize the triterpenoids and their bioactivities of ganoderma spores. The chemical and biological literatures of ganoderma spores dealing with the structural analysis and bioactivity assay were selected. Triterpenoids isolated from ganoderma spores showed significantly anti-HIV-1 protease, anti-tumor, and anti-complement activities. Triterpenoids are the main active constituents of ganoderma spores and show various bioactivities for its medicinal use. In addition, biological activities of ganoderma spores still need further assessment before they can be accepted not only by the traditional Asian medicine community, but also by western science and medicine.