A fast and validated supercritical fluid chromatography method for the quantitative determination of major lactones in Piper methysticum, a plant used against nervous anxiety, stress, and restlessness, was developed. The baseline separation of dihydrokavain, demethoxyyangonin, kavain, yangonin, dihydromethysticin, and methysticin was possible in less than 4 min on an Aquity UPC2 BEH 1.7 µm colu...

The central role of protein kinase C (PK-C) in cellular signal transduction has established it as an important therapeutic target for cancer and other diseases. We have developed a series of 4,4-disubstituted-gamma-butyrolactones, which contain a constrained glycerol backbone (DAG-lactones) and behave as potent and selective activating ligands of PK-C with affinities that approach those of the ...

The genus Anthemis L., assigned by Bremer (1994) to the tribe Anthemideae (subtribe Anthemidinae) of the Asteraceae, comprises ca. 210 species. The Anthemidinae consist of the genus Anthemis with provisional addition of the monotypic genus NanantheaDC (Bremer, 1994). Anthemis wiedemanniana Fisch. & C.A. Mey. (section Cota) is an endemic species distributed in the Mediterranean, the Middle and t...

The pharmacology of macrocyclic lactones is varied, with many beneficial effects in treating disease processes. FK-506, rapamycin and ascomycin have been utilized as immunosuppressant agents. Ivermectin is typically used to treat parasitic worm infections in mammals. Another immunosuppressant, cyclosporin A, is a cyclic oligotide that has similar immunosuppressant properties to those exerted by...

There is rapidly mounting evidence that intracellular proteases in bacteria are compelling targets for antibacterial drugs. Multiple reports suggest that the human pathogen Mycobacterium tuberculosis and other actinobacteria may be particularly sensitive to small molecules that perturb the activities of self-compartmentalized peptidases, which catalyze intracellular protein turnover as componen...

Feverfew is a traditional herbal remedy for a wide range of medical conditions, including migraine and arthritis1−4. The plant contains a large number of natural products, but the active principles probably include one or more of the sesquiterpene lactones known to be present, including parthenolide (Figure 1)5−6. Feverfew can be taken in a variety of forms, including the raw leaf or tablets or...

Bacteria use small secreted chemicals or peptides as auto-inducers to coordinately regulate gene expression within a population in a process called quorum sensing. Quorum sensing controls several important functions in different bacterial species, including the production of virulence factors and biofilm formation in Pseudomonas aeruginosa and bioluminescence in Vibrio fischeri. Many gram-negat...

We report an unusual face selective reduction of the exocyclic double bond in the α-methylene-γ-butyrolactone motif of spiro-oxindole systems. The spiro-oxindoles were assembled by an indium metal mediated Barbier-type reaction followed by an acid catalyzed lactonization.

The complex formed from Pd(CH(3)CN)(4)(BF(4))(2) and (R,R)-MeDUPHOS is a highly enantioselective catalyst for the asymmetric conjugate addition of aryltriethylsiloxanes to a variety of unsaturated ketones, lactones and lactams.

A facile synthesis of a 5,7,5-fused ring system that is present in thapsigargins belonging to a novel family of sesquiterpene lactones, guainanolides, using domino enyne-RCM is reported here.