E-Notopterol

The title compound (systematic name: 4-{[(2E)-5-hydr­oxy-3,7-dimethylocta-2,6-dien-1-yl]­oxy}-7H-furo[3,2-g][1]benzopyran-7-one), C21H22O5, is a known furan­ocoumarin, which was isolated from the Chinese herbal product Radix seu Rhizoma Notopterygii. The crystal structure shows a weak O—H⋯O hydrogen bond

Identification and characterization of [6]-shogaol from ginger as inhibitor of vascular smooth muscle cell proliferation

Scope Vascular smooth muscle cell (VSMC) proliferation is involved in the pathogenesis of cardiovascular disease, making the identification of new counteracting agents and their mechanisms of action relevant. Ginger and its constituents have been reported to improve cardiovascular health, but no studies exist addressing a potential interference with VSMC proliferation. Methods and results The dichloromethane extract of ginger inhibited VSMC proliferation when monitored by resazurin metabolic conversion (IC50 = 2.5 μg/mL). The examination of major constituents from ginger yielded [6]-shogaol as the most active compound (IC50 = 2.7 μM). In the tested concentration range [6]-shogaol did not exhibit cytotoxicity toward VSMC and did not interfere with endothelial cell proliferation. [6]-shogaol inhibited DNA synthesis and induced accumulation of the VSMC in the G0/G1 cell-cycle phase accompanied with activation of the nuclear factor-erythroid 2-related factor 2 (Nrf2)/HO-1 pathway. Since [6]-shogaol lost its antiproliferative activity in the presence of the heme oxygenase-1 (HO-1) inhibitor tin protoporphyrin IX, HO-1 induction appears to contribute to the antiproliferative effect. Conclusion This study demonstrates for the first time inhibitory potential of ginger constituents on VSMC proliferation. The presented data suggest that [6]-shogaol exerts its antiproliferative effect through accumulation of cells in the G0/G1 cell-cycle phase associated with activation of the Nrf2/HO-1 pathway

Polyyne Hybrid Compounds from Notopterygium incisum with Peroxisome Proliferator-Activated Receptor Gamma Agonistic Effects

[Image: see text] In the search for peroxisome proliferator-activated receptor gamma (PPARγ) active constituents from the roots and rhizomes of Notopterygium incisum, 11 new polyacetylene derivatives (1–11) were isolated. Their structures were elucidated by NMR and HRESIMS as new polyyne hybrid molecules of falcarindiol with sesquiterpenoid or phenylpropanoid moieties, named notoethers A–H (1–8) and notoincisols A–C (9–11), respectively. Notoincisol B (10) and notoincisol C (11) represent two new carbon skeletons. When tested for PPARγ activation in a luciferase reporter assay with HEK-293 cells, notoethers A–C (1–3), notoincisol A (9), and notoincisol B (10) showed promising agonistic activity (EC(50) values of 1.7 to 2.3 μM). In addition, notoincisol A (9) exhibited inhibitory activity on NO production of stimulated RAW 264.7 macrophages

Small molecules and their detection by matrix assisted and matrix free laser desorption ionization.

International audienc

Small molecules and their detection by matrix assisted and matrix free laser desorption ionization.

International audienc

Matrix free laser desorption ionization as a versatile tool for the detection natural products.

International audienc

Matrix free laser desorption ionization as a versatile tool for the detection natural products.

International audienc

Matrix-Free Laser Desorption Ionization Mass Spectrometry as an Efficient Tool for the Rapid Detection of Opiates in Crude Extracts of Papaver somniferum

International audienc

Ostruthin: An Antimycobacterial Coumarin from the Roots of Peucedanum ostruthium

Following a bioassay-guided fractionation, ostruthin (6-geranyl-7-hydroxycoumarin) was isolated from the roots of Peucedanum ostruthium Koch (Apiaceae) as a compound with pronounced in vitro activity against several species of rapidly growing Mycobacteria, namely Mycobacterium abscesus, M. aurum, M. fortuitum, M. phlei and M. smegmatis. Minimum inhibitory concentrations (MIC) ranged between 3.4 to 107.4 μM and were comparable to those of ethambutol and isoniazid. Imperatorin (8-isopent-2-enyloxy-6,7-furanocoumarin) showed no activity at concentrations up to 1.9 mM. Umbelliferone (7-hydroxycoumarin) was only weakly active (MIC = 0.79 mM)