Fungal metabolites, asterric acid derivatives inhibit vascular endothelial growth factor (VEGF)-induced tube formation of HUVECs.

In the search for new naturally occurring anti-angiogenic compounds, we found that a culture broth of an unidentified fungal strain B90911 exerted inhibitory activity on capillary-like tube formation of human umbilical vein endothelial cells (HUVEC) in vitro. Four active compounds were isolated by bioassay-guided separation and their structures were identified to be sulochrin (1), methyl asterric acid (2), and two new asterric acid derivatives, 3-chloroasterric acid (3), and 3,5-dichloroasterric acid (4) by spectroscopic analyses. These compounds significantly inhibited the VEGF-induced tube formation of HUVEC, suggesting that asterric derivatives could be useful for further study as anti-angiogenic agents.

Two new furanoditerpenes from Saururus chinenesis and their effects on the activation of peroxisome proliferator-activated receptor gamma.

Two new acyclic furanoditerpene compounds, saurufuran A (1) and B (2), were obtained from the root of Saururus chinensis, and their structures were elucidated by means of 1D and 2D NMR spectroscopic analyses. Saurufuran A (1) is effective on the activation of peroxisome proliferator-activated receptor gamma (PPARgamma) with an EC(50) value of 16.7 microM; however, saurufuran B (2), with an EC(50) value of >100 microM, weakly activated the PPARgamma.

Furanoligularenone, an eremophilane from Ligularia fischeri, inhibits the LPS-induced production of nitric oxide and prostaglandin E2 in macrophage RAW264.7 cells.

Furanoligularenone (1), a known eremophilane, was identified from Ligularia fischeri (Compositae) together with 3-oxo-8alpha-hydroxy-10alphaH-eremophila-1,7(11)-dien-12,8beta-olide (2) and 3-oxo-8alpha-methoxy-10alphaH-eremophila-1,7(11)-dien-12,8beta-olide (3), by its potent inhibition of LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production in RAW 264.7 cells. Compound 1 also suppressed the expression of iNOS and COX-2 mRNA and protein in a dose-dependent manner.

Antiinflammatory constituents of Celastrus orbiculatus inhibit the NF-kappaB activation and NO production.

Two new sesquiterpene esters, 1beta,8beta-diacetoxyl-6alpha,9alpha-difuroyloxydihydro-beta-agarofuran (1) and 1beta-acetoxyl-2beta,6alpha,9alpha-trifuroyloxydihydro-beta-agarofuran (2), together with four known sesquiterpene esters (3-6), celastrol (7), and celaphanol A (8) were isolated from the roots of Celastrus orbiculatus in a search for inhibitors of NF-kappaB activation and nitric oxide production. Compound 7 was the most active, while compounds 1, 2, 4, and 8 showed moderate inhibition in both NF-kappaB activation and nitric oxide production.