New Types of Germacranolides from Austroliabum candidum1.

The investigation of AUSTROLIABUM CANDIDUM afforded, in addition to several known sesquiterpene lactones, four new ones, including three germacranolides with an ether bridge, as well as an unusual glucoside. The structures were elucidated by spectroscopic methods.     

Development of analytical methods for hydrochloride salts of cardiocyclide,a new Russian class III antiarrhythmic

Cardiocyclide, a new Russian class III antiarrhythmic agent, was developed at the State V. V. Zakusov Science Research Institute Pharmacology, Russian Academy of Medical Sciences. The aims of the present work were to study the physicochemical properties of the hydrochloride salt of this agent (N¹-(3-diethylaminopropyl)-N¹-(p-nitrobenzoyl)aminoacetic acid N,N-dicyclohexylamide HCl) and to develop an analytical method for this compound. IR, ¹H NMR, and UV spectra were obtained for cardiocyclide; its solubility was studied; its melting temperature, weight loss on drying and the transparency, color, and pH of its solutions were determined. The purity of material containing compound I was determined by thin-layer chromatography; quantitative cardiocyclide contents were estimated by non-aqueous titration. __________ Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 41, No. 8, pp. 42–45, August, 2007.     

Development of three parallel cytochrome P450 enzyme affinity detection systems coupled on-line to gradient high-performance liquid chromatography.

A high resolution screening (HRS) technology is described, in which gradient high-performance liquid chromatography (HPLC) is connected on-line to three parallel placed bioaffinity detection systems containing mammalian cytochromes P450 (P450s). The three so-called enzyme affinity detection (EAD) systems contained, respectively, liver microsomes from rats induced by beta-naphthoflavone (CYP1A activity), phenobarbital (CYP2B activity), and dexamethasone (CYP3A activity). Each P450-EAD system was optimized for enzyme, substrate, and organic modifier (isopropyl alcohol, methanol, and acetonitrile) in flow injection analysis mode. Characteristic P450 ligands were used to validate the P450-EAD systems. IC(50) values of the ligands were measured and found to be similar to those obtained with conventional microtiter plate reader assays. Detection limits (n = 3; signal-to-noise ratio = 3) of potent inhibitors ranged from 1 to 3 pmol for CYP1A activity, 4 to 17 pmol for CYP2B activity, and 4 to 15 pmol for CYP3A activity. The three optimized P450-EAD systems were subsequently coupled to gradient HPLC and used to screen compound mixtures for individual ligands. Finally, to increase analysis efficiency, a HRS system was constructed in which all three P450-EAD systems were coupled on-line and in parallel to gradient HPLC. The triple parallelized P450-EAD system was shown to enable rapid profiling of individual components in complex mixtures for inhibitory activity to three different P450s.     

Erosive gastropathy not associated with duodenal ulcer]

There was a study of 422 in-patient subjects of the therapeutic profile. Endoscopy enabled to discover mucous coat erosions of the antral part of the stomach associated with Helicobacter pylori and absence of ulcer in the anamnesis in 8.7% of them (more frequently in women). As many as 81% of such patients belonged to patients with the ischemic heart disease. Erosive gastropathy is accompanied by the activity of the chronic inflammation response in the duodenum mucous coat that is most evident in IHD patients.     

Surgical treatment of extensive hemangiomas of the liver

The results of treatment of 7 patients with extensive hepatic hemangiomas are analysed. In 6 patients the diagnosis was established before the operation. The liver was resected in 4 patients. One patients with malignant degeneration of the hemangioma was inoperable, in another the hemangioma was not removed because of his old age, and still in another because the process had spread. The authors conclude that in large hemangiomas of the liver in young and middle-aged patients resection of the organ is indicated, especially if there is a destruction cavity and a rapid growth of hemangioma. The operation is not indicated in capillary, surface hemangiomas of a small size, old age of the patient, extension of the process in to the main vascular structures of the other hepatic lobe.     

Use of heparin in the prevention of thrombotic complications in aged oncologic patients

A method for the prevention of thrombotic complications with heparin was developed during examination of 30 elderly and old-aged patients who underwent operation for gastric carcinoma. It was established that the therapeutic activity of heparin in plasma is maintained for 6 hours after a single subcutaneous injection of 5,000 u. Four injections of this dose of heparin ensures its continuous therapeutic activity for 24 hours in elderly oncological patients. Heparin prevention in a daily dose of 20,000 u is safe from the standpoint of hemorrhagic complications. Under clinical conditions, control of plasma heparin activity may be accomplished by means of activated partial thromboplastin time.