Novel Fluoroquinolones With Pinane Moiety: Synthesis and Antimicrobial Activity.

Here, we report a synthesis of fluoroquinolones carrying a monoterpene moiety at the C7 position of aromatic structure. The minimal inhibitory concentrations of fluoroquinolone fused with trans-3-hydroxy-cis-myrtanylamine 18 against Staphylococcus aureus (MSSA isolates) were two- to eightfold lower compared to moxifloxacin, although fourfold higher against MRSA isolates. The fluoroquinolone fused with (-)-nopylamine 16 was four- to eightfold less active on MSSA compared to moxifloxacin, while had similar activity on MRSA.

Mechanisms of action of fungal polysaccharides and their therapeutic effect.

Background: The purpose of this article is to discuss the relationship between the therapeutic bioactivity of basidial fungal polysaccharides (BFPs) BFPs and their structural characteristics and conformational features, as well as to characterize the mechanisms of action of BFPs in diseases of various origins.

Methods: The review was conducted using the PubMed (Medline), Scopus, Web of Science and the Russian Science Citation Index databases. 8645 records were identified, of which 5250 were studies (86 were randomized controlled trials).

The Influence of Polysaccharide Fractions of the Lion's Mane Medicinal Mushroom Hericium erinaceus (Agaricomycetes) on the Immunomodulatory and Antioxidant Activity of Neutrophils Exposed to Stress of Different Durations.

Polysaccharide fractions from the mycelium of the lion's mane medicinal mushroom Hericium erinaceus BP 16, cultivated on sterile grain substrates (barley, oats, wheat, rice, rye), were isolated and characterized. One percent solutions were prepared from the resulting fractions, mixed with blood, which was then subjected to cold stress at a temperature of 6°C for 3, 5 and 7 d. It has been shown that the fraction of H.

Cryoprotective Effect of Pectin Tanacetan from L.

We researched the ability of tanacetan pectin from inflorescences of common tansy L. to change the osmolarity and freezing point of water in solutions of cryoprotectants: glycerol-3.5%, dimethyl sulfoxide (DMSO)-10%, dimethylacetamide-10% (DMAC), and 1.

The use of pectins as part of a cryoprotective solution for long-term storage of human platelet concentrates.

Background: Pectins have unique properties and great potential to become an indispensable component of cryoprotective environment for platelet freezing.

Objective: To investigate the possibility of including pectins (apple pectin AU-701, tanacetan) into the composition of a cryoprotective solution for platelets during low-temperature storage.

Materials And Methods: Samples of platelet concentrates (PC) were frozen under the protection of complex solutions and stored in an electric freezer at -80 degree C for 1 and 6 months.

Synthesis of Trifluoromethylated Monoterpene Amino Alcohols.

For the first time, monoterpene trifluoromethylated β-hydroxy-benzyl--oximes were synthesized in 81-95% yields by nucleophilic addition of the Ruppert-Prakash reagent (TMSCF) to the corresponding β-keto-benzyl--oximes based on (+)-nopinone, (-)-verbanone and (+)-camphoroquinone. Trifluoromethylation has been determined to entirely proceed chemo- and stereoselective at the C=O rather than C=N bond. Trifluoromethylated benzyl--oximes were reduced to the corresponding α-trifluoromethyl-β-amino alcohols in 82-88% yields.

Synthesis and Biological Activity of Unsymmetrical Monoterpenylhetaryl Disulfides.

New unsymmetrical monoterpenylhetaryl disulfides based on heterocyclic disulfides and monoterpene thiols were synthesized for the first time in 48-88% yields. Hydrolysis of disulfides with fragments of methyl esters of 2-mercaptonicotinic acid was carried out in 73-95% yields. The obtained compounds were evaluated for antioxidant, antibacterial, antifungal activity, cytotoxicity and mutagenicity.

Synthesis and Oxidative Transformations of New Chiral Pinane-Type γ-Ketothiols: Stereochemical Features of Reactions.

Chiral γ-ketothiols, thioacetates, thiobenzoate, disulfides, sulfones, thiosulfonates, and sulfonic acids were obtained from β-pinene for the first time. New compounds open up prospects for the synthesis of other polyfunctional compounds combining a biologically active pinane fragment with various pharmacophore groups. It was shown that the syntheses of sulfanyl and sulfonyl derivatives based on 2-norpinanone are characterized by high stereoselectivity in comparison with similar reactions of pinocarvone.

Apple Pectin as a New Component for Cryopreservation of Nucleated Cells.

This study explored the ability of apple pectin AU-701 to change the freezing point of water in cryoprotectant solutions with different penetrating abilities using glycerol, dimethyl sulfoxide (DMSO), 1,2-propanediol (1,2-PD), dimethyl acetamide (DMAC), hydroxyethyl starch (HES), hexamethylenebistetraoxyethylurea (or substance A-378), and in biological fluid (human venous blood). An effective interaction was used to protect human blood leukocytes at ultrafreezer temperature (-80°C). Apple pectin affects the freezing temperature of water in different ways and it depends on the medium in which it is dissolved, as it either slows down the freezing process (in glycerol) or accelerates it (venous blood).

Antimicrobial and Antifungal Activities of Terpene-Derived Palladium Complexes.

In an era of multidrug-resistant bacterial infections overshadowed by a lack of innovation in the antimicrobial drug development pipeline, there has been a resurgence in multidisciplinary approaches aimed at tackling this global health problem. One such approach is to use metal complexes as a framework for new antimicrobials. Indeed, in this context, bismuth-, silver- and gold-derived compounds in particular have displayed demonstrable antimicrobial activity.