Four new dialkylphosphonate derivatives 2–5 were prepared for the first time from the guaiane-type sesquiterpene lactone estafiatin (1), which was isolated from the aerial part of Achillea nobilis. Their structures were elucidated using PMR, 13C NMR, two-dimensional 1H–1H COSY, 13C–1H COLOC, and 31P–1H spectroscopy. The estafiatin phosphorylation reaction was highly chemo- and stereoselective. The antimicrobial activity of the prepared derivatives was studied.
Investigations aimed at the development of a combined wound-healing preparation on a hydrophilic ointment base have been carried out. Copolymers of acrylic acid and its derivatives with a new divinyl monomer, β-vinyloxyethylamide of acrylic acid, are proposed as the bases. It is established that these ointment bases exhibit sufficiently high osmotic activity. Polymer-based complexes including the ethereal oil of smooth wormwood and the proteolytic enzyme protosubtilin showed pronounced antibacterial and wound-healing activity.
Проведено исследование по разработке комбинированного ранозаживляющего средства на гидрофильной мазевой основе. В качестве основы предложены сополимеры акриловой кислоты и ее производных с новым дивиниловым мономером - β-винилоксиэтил- амидом акриловой кислоты. Установлено, что исследуемые мазевые основы имеют достаточную осмотическую активность, а полимерные комплексы, включающие эфирное масло полыни гладкой и протеолитический фермент протосубтилин, показали выраженную антибактериальную и ранозаживляющую активности.
The spermicidal action of a Saussurea salsa (Pall.) Spreng. (SS) extract has been demonstrated by in vivo and in vitro tests in comparison to the reference preparation (Pharmatex). The SS extract in therapeutic concentrations did not produce significant irritating action on mucous membranes and had no negative influence on the normal genital microflora.
The spermicidal action of a Saussurea salsa (Pall.) Spreng . (SS) extract has been demonstrated by in vivo and in vitro tests in comparison to the reference pharmathex preparation. The SS extract in therapeutic concentrations did not produce significant irritating action on mucous membranes and had no negative influence on the normal genital microflora.
The antiparasitic properties of Saussurea salsa (Pall.) Spreng. extract and cynaropicrin have been studied on a model of opisthorchosis. The tested substances produced a dose-dependent therapeutic effect, which was comparable with that of the reference antihelminthic drug praziquantel.
The antiparasitic properties of the Saussurea salsa (Pall.) Spreng. extract and its cynaropicrin fraction have been studied on a model of opisthorchosis in golden hamsters. The tested substances produced a dose-dependent therapeutic effect comparable with that of the reference antihelminthic drug biltricide (praziquantel).
: The sesquiterpene lactone arglabin, as well as its derivative 11,13-Dihydro-13-dimethylaminoarglabin hydrochloride, exhibit antiexudative and antiproliferative properties on the models of acute aseptic inflammation caused by formalin, carrageenan, and histamine, and on the model of proliferative inflammation accompanying cotton-pellet granuloma.
Essential oils are complex mixtures of various organic compounds, most of which possess an isoprenoid structure. Data in the literature are indicative of the high biological activity of essential oils, which makes possible the use of these substances in medicine and pharmacology [1, 2]. The chemical and pharmacological properties of an essential oil isolated from wormwood species Artemisia glabella Kar. et Kir. have been thoroughly studied within the framework of investigations aimed at the complex use of these species, which are employed as a raw material for the drug arglabin [3] developed at the Institute of Phytochemistry (Karaganda). Recently [4], more than 70 compounds were identified in the essential oil from Artemisia glabella (EOAG) studied by a gas chromatography (GC) technique using a capillary column with nonpolar methyl silicon immobile phase and a flame-ionization detector. The main chemical components of the characteristic chemical composition of EOAG are 1,8-cineole (12%), linalool (8%), 4-terpineol (6.5%), -terpineol (5%), and sabinol derivatives (5%). These substances were also found in the essential oils isolated from medicinal plants of some other genuses. At the same time EOAG contains a series of genetically related compounds including para-cymene, cuminaldehyde, cuminyl alcohol and acetate, -thujene, sabinene, sabinene hydrate, sabinol and related esters with a homologous series of fatty acids, -pinene, myrtenal, and verbenone. The purpose of this study was to identify the essential oil isolated from Artemisia glabella Kar. et Kir. and characterize EOAG with respect to biological activity.
Reaction of pinostrobin with hydroxylamine and hydrazine formed the corresponding oxime and hydrazone with retention of the γ-pyrone ring. The structures of the modified pinostrobin derivatives were established using PMR, 13C NMR, mass spectrometry, and X-ray analysis of pinostrobin oxime. Experiments in vivo revealed high hepatoprotective activity for pinostrobin oxime.