1,4-Naphthoquinone Motif in the Synthesis of New Thiopyrano[2,3-d]thiazoles as Potential Biologically Active Compounds.

A series of 11-substituted 3,5,10,11-tetrahydro-2H-benzo[6,7]thiochromeno[2,3-d][1,3]thiazole-2,5,10-triones were obtained via hetero-Diels-Alder reaction of 5-alkyl/arylallylidene/-4-thioxo-2-thiazolidinones and 1,4-naphthoquinones. The structures of newly synthesized compounds were established by spectral data and a single-crystal X-ray diffraction analysis. According to U.S. NCI protocols, compounds 3.5 and 3.6 were screened for their anticancer activity; 11-Phenethyl-3,11-dihydro-2H-benzo[6,7]thiochromeno[2,3-d]thiazole-2,5,10-trione (3.6) showed pronounced cytotoxic effect on leukemia (Jurkat, THP-1), epidermoid (KB3-1, KBC-1), and colon (HCT116wt, HCT116 p53-/-) cell lines. The cytotoxic action of 3.6 on p53-deficient colon carcinoma cells was two times weaker than on HCT116wt, and it may be an interesting feature of the mechanism action.

Actual prospects of using some types of larch growing in Kazakhstan in medicine.

Local plants can save natural resources and be used as a source of biologically active compounds, which can be high-quality, effective, and safe ingredients for pharmacological or chemical industries. Therefore, this study aimed to investigate the properties of two medicinal plants - the fine-scaled larch (Lárix Kaémpferi) and Siberian larch (Lárix Sibirica), which are growing in the Republic of Kazakhstan. We compared the two types of larches according to botanical affiliation and species description. We studied the alcoholic extracts from Lárix Kaémpferi and Lárix Sibirica to determine their physical and chemical properties. The data on the chemical composition of extractive compounds were generalized and systematized. The authenticity of Lárix Kaémpferi and Lárix Sibirica was established by external, anatomical, and diagnostic signs in microscopic examination and qualitative reactions. Specific indicators and their norms for raw materials were identified. This is the standard for both types of larch and determines their quality. We experimented with grinding fineness for studied materials and tested the impurities and moisture content of raw materials, total ash, and ash insoluble in a 10% hydrochloric acid solution. Determination of heavy metals and radionuclides was also considered. The quality specifications were developed based on the standardization of fine-scaled larch and Siberian larch.

Determination of the Chemical Composition and Antimicrobial Activity of Lavatera thuringiaca L. Medicinal Herb Material Extracted under Subcritical Conditions by the Liquid Carbon Dioxide Method.

This article presents the composition of the components of Lavatera thuringiaca L. (Malvaceae Juss. family), which has a certain antibacterial effect. The plant collection was carried out in the Shamalgan gorge of Mountain Range of the Trans-Ili Alatau in the territory of the Karasay district of the Almaty region, in the flowering phase. A CO2 extract of the aboveground part of the medicinal plant Lavatera thuringiaca L. was obtained under subcritical conditions and, for the first time, studied for its component composition and antimicrobial activity. Determination of the chemical composition of the extract was carried out by gas chromatography/mass spectrometry (GC/MS). To identify the obtained mass spectra, we used the Wiley 7th edition and the NIST'02 data library. To determine the antimicrobial and antifungal activity, standard test strains of microorganisms were used: Staphylococcus aureus ATCC 6538-P, Escherichia coli ATCC 8739, Pseudomonas aeruginosa ATCC 9027, Candida albicans ATCC 10231, Streptococcus pneumonia ATCC 660, Klebsiella pneumoniae ATCC 700603, Staphylococcus haemolyticus, and Staphylococcus saprophyticus. In the composition of thick CO2 Lavatera thuringiaca L. extract, the content of 31 components was proven: spathulenol 6.97%, pulegone 5 08%, cis-ß-farnesene 7.63%, verbenone 1.93%, α-bisabolol oxide B 9.65%, bisabolol oxide A 8.26%, α-bisabolol 1.36%, linolenic acid, ethyl ether 3.15%, phytol 2.49%, herniarin 5.61%, linolenic acid 9.38%, linoleic acid 6.95%, myristic acid 2.33%, and elaidic acid 2.57%. Antimicrobial activity studies have shown that the CO2 extract of Lavatera thuringiaca L. has a pronounced effect against clinically significant microorganisms: Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Streptococcus pneumonia, Klebsiella pneumoniae, Staphylococcus haemolyticus, and Staphylococcus saprophyticus. During testing, the method of serial dilutions proved that the extract of Lavatera thuringiaca L. has a bactericidal effect on Staphylococcus aureus at a concentration of 0.83 µg/µl, on Escherichia coli at a concentration of 3.33 µg/µl, on Pseudomonas aeruginosa at a concentration of 0.83 µg/µl, on Streptococcus pneumoniae at a concentration of 1.67 µg/µl, on a clinical isolate of Staphylococcus haemolyticus at a concentration of 26.65 µg/µl, on Staphylococcus saprophyticus at a concentration of 6.67 µg/µl, and against Klebsiella pneumoniae at a concentration of 13.36 µg/µl. The test result showed that the extract also has fungicidal activity against the test culture of Candida albicans at a concentration of 0.21 µg/µl. At tests, the disc diffusion method proved that the extract has antimicrobial activity with high values of the growth suppression zone exceeding 15 mm. The zones of growth retardation of the test strains were 19.33 ± 1.15 for Staphylococcus aureus; 17.33 ± 3.21 for Escherichia coli; 15.67 ± 0.57 for Pseudomonas aeruginosa; 20.0 ± 1.0 for Streptococcus pneumoniae; 16.0 ± 2.64 for Klebsiella pneumoniae; 15.0 ± 1.0 for Staphylococcus saprophyticus, and 22.0 ± 1.73 for Candida albicans. In relation to the clinical isolate of Staphylococcus haemolyticus, the extract has a bacteriostatic effect.