Pharmaceutical Chemistry Journal最新文献

Material devoted to the peculiarities of plant extract microencapsulation used for the development and production of drugs and active substances with pharmacological activity is reviewed. The advantages of some microencapsulation methods of plant extracts are shown: emulsification (dispersion), coacervation, ionic gelation, spray and freeze drying, solvent evaporation, extrusion, fluidized bed microencapsulation. The parameters for choosing an encapsulation method for plant extracts were determined. Possible prospects for microencapsulation technology of plant extracts were described. Domestic and foreign literature sources in the public domain were analyzed using the electronic databases PubMed, e-Library, and CyberLeninka and Google Scholar search engine.

Changes in the quantitative content and specific activity of hyaluronidase enzyme after ultrasonic treatment of solutions of bovhyaluronidase azoximer were studied. Solutions of the finished dosage form of bovhyaluronidase azoximer (Longidase^® lyophilizate for preparation of solution for injection, 3000 IE) and bovhyaluronidase azoximer drug substance (Longidase^® substance-lyophilizate) were studied. The aim of the study was to determine the effect of ultrasound (US) on the stability of bovhyaluronidase azoximer determined from the measured quantitative content and enzymatic activity of the substance in solution. US at a radiation intensity of 61.4 W/L during treatment in an ultrasonic bath did not significantly affect the quantitative content of the bovhyaluronidase azoximer drug substance in solution, while the decrease in the enzymatic activity of the active substance in Longidase solution after 20 and 30 min of ultrasonic treatment was statistically significant. At the same time, the enzymatic activity of the active substance determined by a biochemical method differed significantly (residual activity from 99.70% to 59.27%) depending on the design features of the nebulizers and the nebulization time after nebulization of the bovhyaluronidase azoximer solution in mesh nebulizers from various manufacturers. Nebulization times of min were least associated with the risk of significant loss of stability of bovhyaluronidase azoximer.

Features of using the generalized Harrington desirability function for the selection of a binder and lubricant for GML-1 (N-benzyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide) tablets are considered. The factors affecting the characteristics of the finished dosage form are evaluated. Model formulations with different qualitative and quantitative compositions of disintegrant and lubricant excipients were developed. Their pharmaceutical and technological properties were studied. The factors having the greatest impact on indicators such as the mass loss on drying, strength, disintegration, and solubility of the tablets were identified. The type and amount of disintegrant and lubricant in the tablet that could produce a dosage form with the optimal pharmaceutical and technological characteristics were determined.

The effect of the eluent composition (type and concentration of the organic and acid components) on the retention times and selectivity of the separation of some standard samples of phenylpropanoids under reversed- phase HPLC conditions is studied. Ethanol, being a nontoxic solvent, exhibited good characteristics as an eluent for the separation of this group of substances. A mobile phase containing ethanol and organic acids could be recommended as an extractant for studies of plant raw material containing phenylpropanoids.

Literature data on the use of virtual reality in various fields of activity and the prospects for development and possible limitations of the spread of this technology in the Russian Federation and around the world are analyzed and summarized. The relevance of introducing virtual reality technology into Russian pharmaceutical education at various levels of professional training of specialists for the industry is considered.

Anticancer peptides are among the most important bioactive peptides found in animal sources. The modulation of the molecular process of apoptosis via the genes involved in the signaling pathway is now being studied for cancer treatment. In this study, the anticancer properties of peptide HL-10 extracted from scorpion venom by regulating the apoptosis signaling pathway were investigated. In the present study, the anticancer activity of the HL-10 peptide against the HeLa cancer cell line was assessed using the cytotoxicity assay. The real-time PCR method was used to analyse the expression levels of Bax, p53, caspase-3, PTEN, and Akt genes. The cytotoxicity assay demonstrated that the IC₅₀ value of the HL-10 peptide was 40 μM. The results also showed that the treatment of Hela cells with HL-10 led to an increase in the expression of Bax, p53, caspase-3, and PTEN genes, while it resulted in a significant decrease in the expression level of the Akt gene in a dose-dependent manner (p.05). The flow cytometry analysis also revealed a high number of cells in the secondary apoptotic stage. According to changes in the expression of genes implicated in the apoptosis pathway, the HL-10 peptide appears to play a role in the activation of the intrinsic apoptosis pathway. However, additional research in molecular dimensions and clinical studies is needed. It is suggested to confirm the effectiveness of HL-10 peptide in cancer treatment.

A dimeric dipeptide mimetic based on the β-turn of the 4^th loop of neurotrophin-3, bis-(N-monosuccinyl-L-asparaginyl-L-asparagine)hexamethylenediamide (GTS-301LL), was recently designed and synthesized by us. GTS-301, like the full-length neurotrophin, activated TrkC and TrkB receptors and exhibited neuroprotective activity on HT22 cells under oxidative stress conditions in the concentration range 10^–5 – 10^–12 M and antidepressant-like activity in the forced swimming test in mice (10 – 40 mg/kg, intraperitoneally). The stereospecificity of the pharmacological effects of GTS-301LL was revealed by synthesizing the LD, DL, and DD stereoisomers of GTS-301LL and studying their neuroprotective and antidepressant-like properties under the same conditions as for GTS-301LL. Both activities were found to disappear on going from the LL to the DL and DD stereoisomers and were retained on going to the LD stereoisomer. Thus, the stereospecificity of the neuroprotective and antidepressant-like activities of the dipeptide mimetic of neurotrophin-3 GTS-301LL at the N-terminal asparagine residue was proven, which indicated the key role of that amino-acid residue in the interaction with the receptor.

Asteriscus graveolens (Asteraceae) is a medicinal herb, used in Algeria to treat diabetes, hypertension, pain, fever, inflammation and gastrointestinal diseases. Doxorubicin (DOX) is an antibiotic antineoplastic drug used to treat many types of cancers; unfortunately, its antitumor activity links toxic effects to several organs including the heart, liver and testis. The appropriate mechanism of its organotoxicity is linked to free reactive oxygen species (ROS) generation and oxidative stress induction. In this study, the antioxidant and protective role of A. graveolens and vitamin E (Vit E) against DOX-induced hepatic and testicular toxicity was assessed. Thirty-five rats were distributed equally into five groups and orally administered with n-butanol extract of A. graveolens (75 mg/kg bw) or Vit E (100 mg/kg bw) for 10 days in the absence or presence of a single intraperitoneal injection of DOX (15 mg/kg bw). The results revealed that DOX toxicity induced a significant elevation in the liver serum marker enzymes and lipid profile levels (cholesterol, triglycerides and LDL). In addition, DOX-induced hepatic and testicular oxidative injury was indicated due to a significant increase of malondialdehyde levels along with a noticeable reduction of the antioxidant system. A. graveolens and Vit E treatment might improve the biochemical and histopathological changes induced by DOX. A. graveolens has antioxidant and hypolipidemic properties and it can reduce DOX-induced oxidative damage in the liver and testis. A. graveolens showed a similar protective effect of Vit E against DOX damage due to the presence of an abundant amount of phenolics such as flavonoids. This protection is mediated by their direct free-radical scavenging activity and their ability to prevent DOX depletion of the hepato-testicular antioxidant defense systems.

The extraction and isolation of biomolecules were carried out from the active fractions of Muntingia calabura which exhibited stronger antibacterial activity. Among all the extracts, methanol and ethyl acetate extracts of M. calabura stem bark showed strong antimicrobial activity. Bioassay guided fractionation of methanol and ethyl acetate extracts acquired from the hardwood stem of M. calabura was done using silica gel column chromatography (100 – 200 mesh) to identify the active fractions and to eliminate the non-active fractions. Hexane and ethyl acetate were used as eluent in different ratios. 5,8-Dihydroxy-6,7,4^′-trimethoxy flavones, 6,4^′-dihydroxy-3^′-propen chalcone, 7-(alloxy)-2-phenyl-4H-chromen-4-one, 7-hydroxy-4-oxo-2-phenyl-4Hchromen-8-carbaldehyde were isolated and identified as flavonols. The structures were established from IR, ¹H NMR, ¹³C NMR, and mass spectral data.

Russian and foreign pharmacopoeias require at least two stages in the manufacturing process of medicinal products based on animal serum-plasma to provide at least a 4-log decrease in the concentration of extraneous viruses to minimize the risk of viral contamination in the corresponding intermediates after each stage. The enzymolysis and thermal denaturation stages involved in the production of drugs based on equine blood plasma were validated for reduction of model enveloped viruses in influenza (RNA-containing) and smallpox vaccine (DNA-containing). Both stages were shown to provide the required level of inactivation of these model viruses in the corresponding drug intermediates, significantly minimizing the risk of their contamination with enveloped viruses.