[Antiaggregation activity of arachidonic acid conjugates with neurotropic peptides proglyprol and semax].

The influence two original derivatives of a therapeutically important peptide, bearing arachidonic acid residue with semax and proglyprol, upon platelet aggregation have been studied in vitro. It is established that both derivatives, in contrast to the parent peptide, possess moderate anti-aggregant properties and produce a dose-dependent decrease in the interplatelet interaction induced by ADP, epinephrine, and arachidonic acid within the concentration range of 0.018 - 1.8 mM. This activity was more pronounced for arachidonoylsemax in comparison with arachidonoylproglyprol.

[Possibilities of remaxol in prevention of toxic hepatitis during chemotherapy for cancer patients].

The effectiveness of planning polychemotherapy (PCT) for cancer patients depends on the functional state of the liver. The use of remaxol was studied in 100 patients with advanced forms of cancer (including breast cancer) in a preventive mode in comparison with the control group (100 patients, essentiale group of 40 patients) and in the process of PCT. Remaxol, compared with the control group, allowed reducing the frequency of drug hepatotoxicity by 30 +/- 3.7% and by 6.5 +/- 2.9% in comparison with the group of patients who received essentiale.

[Use of Reamberin for the prevention of adverse effects of combined antineoplastic agents in stage III-IV ovarian cancer during induction treatment].

Ovary cancer treatment often presents clinical promlems due to frequent occurence of late diagnostics (III-IV stages), severe treatment complications in patients with ascitis and tumor intoxication. Reamberin can be used as supportive therapy aimed at decrease of intoxication, which is one of the main hindrances for antitumor therapy. In the current study reamberin was used in 89 stage III-IV (FIGO) ovary cancer patients with ascitis, age 42 to 79, CP or CAP chemotherapy recipients after prior cytoreductive surgery. The occurrence of hematological complications (grade 1-2 anemia and neutropenia) and cardiac dysfunctions in the study group was much lower, than in the control group. This difference is statistically valid (p < 0.01 and p < 0.05). The patients receiving reamberin prior to chemotherapy or during chemotherapy rarely (in 3.7% of cases) displayed raised creatinine values. In the control group grade 1-3 renal impairment was observed in 41.4% cases, in 12 cases the therapy had to be ceased. This difference between the groups is statistically valid (p < 0.001). Patients receiving reamberin displayed more rapid rate of CA-125 tumor marker serum concentration decrease. Therefore, reamberin is an effective drug for prevention of chemotherapy side effects and alleviation of intoxication allowing the more rigid chemotherapy schedule without an increase in toxicity.

[Influence of new 1,3,4-thiadiazines on platelet aggregation in vitro and ex vivo].

The influence of new original 1,3,4-thiadiazines on the human platelet aggregation in vitro was studied. All substances inhibited the platelet aggregation induced by both ADP and arachidonic acid. 1,3,4-Thiadiazines L-19, H-30 and L-37 were the most effective inhibitors. Effect of the intravenous injection of L-19 in various doses on platelet aggregation and some parameters of plasmatic hemostasis were studied ex vivo.

[Antiaggregant properties of new 1,3,4-thiadiazine derivatives].

A series of new 1,3,4-thiadiazine derivatives have been synthesized and their effect on the human platelet aggregation in vitro has been studied. All the tested substances inhibit the human platelet aggregation induced by ADP and arachidonic acid in a broad concentration range. The most active 1,3,4-thiadiazines (L-19, L-28 and L-31) effectively inhibit platelet aggregation at concentrations within 0.01-1 mM.

[Effect of RGD-containing peptides on platelet aggregation].

The influence of new synthetic peptides ARGDS-NH2 and RGD-dFK (synthesized by the fermentative method) and VPNLRGDLQVLA (a fragment of the foot-and-mouth virus's surface peptide) on the ADP-induced human platelet aggregation in vitro was studied. All peptides were found to inhibit the human platelet aggregation, but the synthetic peptides (ARGDS-NH2 and RGD-dFK) showed the most pronounced effect. Significant decrease in the platelet aggregation was observed at their concentrations within 0.1-10 mM. ARGDS-NH2 and RGD-dFK inhibited the platelet aggregation stronger than the reference drug pentoxifylline at equivalent concentrations.

[Effect of the new antimigraine drug serotonin receptor antagonist tropoxin on platelet aggregation].

The effect of the new antimigraine drug tropoxin - the serotonin receptor (5-HT2) antagonist - on the human platelet aggregation in vitro induced by ADP (1 x 10(-5) M) and epinephrine (2.5 x 10(-6) M) was studied. Tropoxin reliably inhibited the ADP-induced platelet aggregation in a concentration range of 0.01 - 7 mg/ml. A significant inhibition effect with respect to the epinephrine-induced platelet aggregation was observed in a drug concentration range of 2 - 7 mg/ml, although a reliable antiaggregant activity was also observed below 2 mg/ml. A bolus administration of tropoxin (10 mg/kg) in rabbits decreased the ADP-induced platelet aggregation ex vivo by a factor of 1.2 - 1.4. The effect appeared 45 min after treatment and was observed during subsequent 30 min.