3/31/2023 0 Comments Find all x in r4 that are mappedMacrocyclic lactones are used as drugs in the treatment of cancers of the breast, ovary, testes, and pancreas. Antitumor properties are demonstrated by macrocyclic lactones and numerous bicyclic compounds with a multi-membered ring fused with the α-methylene-γ-butyrolactone ring. The most representative examples are: tavulin, dentin A, tanachin, isolated from Tanacetum argyrophyllum, or Nocardia, showing activity against Staphylococcus aureus, Escherichia coli, and Bacillus subtilis ATCC 6633. ![]() Antimicrobial properties are also demonstrated by α-methylene-γ-butyrolactones condensed with a 10-membered ring. From the lithographic data, it is known only that bacteriostatic properties are exhibited by substances in which the lactone moiety is present in a small ring, e.g., xanthatin, a bicyclic lactone isolated from Xanthium pensylvanicum and Xanthium strumarium, which is active against Staphylococcus aureus, including MRSA-resistant methicillin strains. ![]() The knowledge on antimicrobial properties of lactones is still fragmentary, therefore, there is a need to clarify their role. A good representative of seven-membered ring δ-lactone is 6-phenyl tetrahydro pyran-2-one of structure D ( Figure 1). This colorless liquid compound, miscible with water and several organic solvents, is produced in large quantities in chemical industry as an important polymer caprolactam precursor. Important representative of ε-lactones is ε-Caprolactone C. Coumarins are also used as inhibitors of plant, bacterial, and fungal growth. The most important properties of coumarin and its derivatives include anti-cancer, antiviral, anti-allergic, anti-inflammatory, and anti-thrombotic properties. coli R1–R4, which have a complete LPS core region composed of the outer and inner core. It does not have LPS, unlike the analyzed mutants of E. Under certain conditions, the colon rod is pathogenic for humans, mainly causing diseases of the digestive and urinary systems. In the intestine, this symbiotic bacterium plays a useful role by participating in the breakdown of food and also contributing to the production of B and K vitamins. It is part of the physiological bacterial flora of the human colon and other warm-blooded animals. It is a Gram-negative relatively anaerobic bacterium belonging to the Enterobacteriaceae family. coli belongs to the model organisms among bacteria because its structure, genetics, and metabolism are well known and used in genetic studies. One of the typical lactones is coumarin and its derivatives, which have a broad antibacterial effect, causing damage to the bacterial cell membrane, e.g., in E. The observed results are of particular importance in the case of increasing bacterial resistance to various drugs and antibiotics, especially in nosocomial infections and neoplasms, and in the era of a microbial pandemic. ![]() Their chemical and biological activity is related to coumarin derivatives and the corresponding δ-lactone groups in the structure of the substituent. The presented research clearly shows that lactone derivatives can be potential candidates as substitutes for drugs, e.g., the analyzed antibiotics. ![]() The analyzed damage values were compared with the modification with appropriate antibiotics: ciprofloxacin, bleomycin, and cloxacillin. Moreover, oxidative damage of bacterial DNA isolated from bacteria after modification with newly synthesized compounds after application of the repair enzyme Fpg glycosylase was analyzed. In the presented studies, on the basis of the conducted MIC and MBC tests, it was shown that the antibacterial (toxic) activity of lactones depends on their structure and the length of the bacterial LPS in the membrane of specific strains. Particular emphasis was placed on the selection of the structure of lactones with the highest biological activity, especially those with fluorine in their structure as a substituent in terms of action on bacterial lipopolysaccharide (LPS) in the model strains of Escherichia coli K12 (without LPS in its structure) and R2–R4 (LPS of different lengths in its structure). A preliminary study of δ-lactone derivatives as new potential candidates for antibacterial drugs was conducted. In recent years, among this group of compounds, new biologically active substances have been searched by modifying the main (leading) structure with new analogs with stronger or different responses that may have a toxic effect on the cells of pathogenic bacteria and constitute an alternative to commonly used antibiotics. They are characterized by antibacterial, antiviral, anti-inflammatory, and anti-cancer properties. Lactones are among the well-known organic substances with a specific taste and smell.
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