Dynamics of clinical and morphological parameters in patients with peptic ulcer in the combined laser therapy

The eff ectiveness of the use of a therapeutic complex based on the combined eff ects of intragastric low-intensity and transcutaneous infrared laser therapy in the antiulcer drug therapy of 60 patients with gastric ulcer and duodenal ulcer was studied. In all 30 patients of the main group, after a course of combined laser exposure, the regression of the morphological picture of the activity of the infl ammatory process with epithelialization of the ulcer defect and positive dynamics of the clinical manifestations of the disease within 10 days of treatment was noted. Meanwhile, in the patients of the control group (n = 30), the positive dynamics of similar parameters in the same period was achieved in 70 % of patients against the background of basic drug therapy.

Gastroprotective Activity of the Total Flavones from Abelmoschus manihot (L.) Medic Flowers

Background. Abelmoschus manihot (L.) Medic flower is a medicinal plant for the treatment of diseases in China. The present study was carried out to scientifically validate the gastroprotective activity and clarify the possible mechanism of the total flavones from Abelmoschus manihot (L.) Medic flowers (TFA). Methods. Gastric ulcer was induced in mice by oral administration of ethanol. The gastroprotective activity of TFA was evaluated by the gastric ulcer index and histological examinations. The gastric tissue was collected in the form of homogenate. The level of malondialdehyde (MDA) and glutathione (GSH), the activity of superoxide dismutase (SOD), and protein content were measured. Western blotting for the expression of Bax, Bcl-2, TNF-α, and NF-κB(p65) was also carried out. The effect of TFA was compared with that of standard antiulcer drug omeprazole (100 mg/kg). Results. This gastroprotective effect of TFA could be attributed to the increase in the activity of SOD and GSH and decrease in the levels of MDA and also decrease in the levels of Bax, TNF-α, and NF-κB(p65) expressions and increase in the Bcl-2 expression level. Conclusion. The findings of this study demonstrated that TFA could significantly attenuate ethanol-induced gastric injury via antioxidative, anti-inflammatory, and antiapoptotic effects.

Phosphonate reagents and building blocks in the synthesis of bioactive compounds, natural products and medicines

This account outlines the results obtained in the author’s laboratory on the application of phosphonates in the synthesis of various classes of biologically active cyclopentenones and cyclopentanones. In the first place two general methods for the synthesis of mono-, 1,2- and 1,4-dicarbonyl compounds are presented. The first is based on the use of α-phosphoryl sulfides in conjunction with the Horner reaction while in the second method the oxygenation reaction of α-phosphonate carbanion is a key step. The utility of these two approaches to 1,4-diketones as precursors of cyclopentenones was exemplified by the synthesis of dihydrojasmone and (Z)-jasmone. The use of simple phosphonates, α-phosphoryl sulfides and β- and γ-ketophosphonates as starting reagents in the synthesis of cyclopentanoid antibiotics (methylenomycin B, racemic desepoxy-4,5-didehydromethylenomycin, enantiomeric sarkomycins) is presented. The synthesis and reactivity of achiral 3-(phosphorylmethyl)cyclopent-2-enone and chiral diastereoisomeric camphor protected 3-(phosphorylmethyl)-4,5-dihydroxycyclopent-2-enones as building blocks is discussed as a platform for developing a new access to a variety of bioactive cyclopentenones. The utility and value of achiral phosphonate building block is demonstrated by the synthesis of racemic and enantiopure prostaglandin B1 methyl esters and enantiomeric phytoprostanes B1 type I and II. The range of biologically active compounds prepared from chiral diastereoisomeric cyclopentenone phosphonates is wider. Herein the total syntheses of the following target compounds are presented: enantiomeric isoterreins, natural (−)-neplanocin A and its unnatural (+)-enantiomer, anticancer prostaglandin analogues (enantiomers of TEI-9826, NEPP-11, iso-NEPP-11). The design and synthesis of racemic and four enantiopure stereoisomers of an antiulcer drug rosaprostol is also described.

A new and expeditious synthesis of all enantiomerically pure stereoisomers of rosaprostol, an antiulcer drug

Four enantiomerically pure stereoisomers of rosaprostol (1), an antiulcer drug, were efficiently synthesized from the enantiomers of 2-(dimethoxyphosphoryl)-3-hexylcyclopentanone (3) as chiral substrates. The latter were obtained by resolution of racemic 3 with (+)-(R)-1-(1-naphthyl)ethylamine. The conversion of (+)-3 into rosaprostol stereoisomer (−)-1a was accomplished in four steps in 56% overall yield. According to the same protocol, the second stereoisomer (+)-1c was obtained from (−)-3 in 55% overall yield. A slightly improved procedure of the last two steps of the transformation of (+)-3 into (−)-1a allowed an increase in the overall yield to 64%. The remaining two stereoisomers, (−)-1b and (+)-1d, were obtained from (−)-1a and (+)-1c in 71 and 68% yield, respectively, by a two-reaction sequence, in which a Mitsunobu inversion of configuration at C-5 was the key step.