A single 400 mg oral dose of gatifloxacin was given to each of nine healthy male volunteers and the concentrations of the drug in plasma, cantharidine-induced inflammatory fluid and urine were measured over the following 24 h. The mean peak concentration in plasma of 4. 1 mg/L was attained at a mean time of 1.8 h post dose. The mean peak concentration in inflammatory fluid was 3.6 mg/L and was ...

To characterize the role of hen eggs used for analyzing the insect Mylabris phalerata a traditional Chinese medicine for curing liver cancer, egg white was separated from the whole egg and added to M. phalerata. The volatile compounds found in egg white when added to M. phalerata and therefore in M. phalerata itself were analyzed by GC. Cantharidin was detected both in egg white added to M. pha...

Cantharidin is a natural compound of novel structure with ideal insecticidal activity. However, the relationship of structure to insecticidal activity of cantharidin and its derivatives has not been ever clarified. To explore what determines the insecticidal activity structurally of cantharidin-related compounds, two series target compounds 6 and 7 were synthesized by replacing the anhydride ri...

Serine/threonine protein phosphatase 5 (PP5) is a promising novel target for anticancer therapies. This work aims to uncover the key interactions at the atomic level between PP5 and three inhibitors (cantharidin, norcantharidin and endothall). We found that, unlike previous report, Arg 100 contributes less to PP5-inhibitor binding, and the residues His 69, Asn 128, His 129, Arg 225, His 252 and...

It has been suggested that the rol genes of Agrobacterium rhizogenes could play an essential role in the activation of secondary metabolite production in plant transformed cultures. This study investigated whether the content of anthraquinone phytoalexins was changed in callus cultures of Rubia cordifolia transgenic for the 35S-rolB and 35S-rolC genes in comparison with a non-transformed callus...

Three major families in the order Coleoptera have been found to produce vesicant toxins, Meloidae (true blister beetles) and Oedemeridae (false blister beetles) produce cantharidin and Staphylinidae (rove beetles) produce paederin. Some of the most important distribution, biological and ecological aspects of these beetle families had been studied because of their products cause human dermatitis...

The pharmacokinetics and penetration into a cantharidine-induced inflammatory exudate of meropenem was studied in six volunteers following a single 1-g intravenous dose. Concentrations in plasma, urine, and the inflammatory exudate were determined by a microbiological assay. The mean elimination half-life of meropenem in plasma was 1.1 h, with the concentration in plasma declining from a mean o...

A 400-mg dose of the trifluorinated quinolone Ro 23-6240 was administered orally to each of six healthy male volunteers, after which the concentrations of this agent in serum and cantharidin-induced inflammatory fluid were measured. Absorption was rapid, with a mean peak level in serum of 6.1 micrograms/ml, which was attained 0.71 h after administration. The elimination half-life in serum was 1...

PURPOSE Mammalian cells at mitosis contain chromatin in compacted form and are hypersensitive to ionizing radiation. Previous research had shown some chemicals that induce chromatin compaction within interphase cells act as radiosensitizers. Of these agents, cantharidin (LS-1), which is an inhibitor of protein phosphatases 1 (PP1) and 2A (PP2A), showed good radiosensitizing activity at non-toxi...