The Pharmacokinetics of Fucoidan after Topical Application to Rats

Fucoidan, a fucose-rich polysaccharide from brown algae, has been used for transdermal formulations targeting inflammatory skin conditions, for the treatment of thrombosis, vascular permeability diseases, subcutaneous wounds, and burns. However, the pharmacokinetics of fucoidan after topical application has not been described. In this study, an ointment (OF) containing 15% fucoidan was topically applied to rats at the doses of 50–150 mg/g. The anti-Xa activity was selected as the biomarker, and the amidolytic assay method was validated and applied for pharmacokinetic studies of fucoidan. Fucoidan in OF penetrated the skin and distributed into the skin, striated muscle, and plasma with AUC0–48 = 0.94 μg·h/g, 2.22 μg·h/g, and 1.92 µg·h/mL, respectively. The longest half-life for fucoidan was observed in plasma, then in striated muscle and skin. It was found that the pharmacokinetics of fucoidan after topical OF application was linear, in the range of 50–150 mg/kg. No accumulation of fucoidan in plasma was observed after repeated topical applications of 100 mg/kg during five days. Our results support the rationality of topical application of formulations with fucoidan

The Pharmacokinetics of Fucoidan after Topical Application to Rats

Fucoidan, a fucose-rich polysaccharide from brown algae, has been used for transdermal formulations targeting inflammatory skin conditions, for the treatment of thrombosis, vascular permeability diseases, subcutaneous wounds, and burns. However, the pharmacokinetics of fucoidan after topical application has not been described. In this study, an ointment (OF) containing 15% fucoidan was topically applied to rats at the doses of 50–150 mg/g. The anti-Xa activity was selected as the biomarker, and the amidolytic assay method was validated and applied for pharmacokinetic studies of fucoidan. Fucoidan in OF penetrated the skin and distributed into the skin, striated muscle, and plasma with AUC0–48 = 0.94 μg·h/g, 2.22 μg·h/g, and 1.92 µg·h/mL, respectively. The longest half-life for fucoidan was observed in plasma, then in striated muscle and skin. It was found that the pharmacokinetics of fucoidan after topical OF application was linear, in the range of 50–150 mg/kg. No accumulation of fucoidan in plasma was observed after repeated topical applications of 100 mg/kg during five days. Our results support the rationality of topical application of formulations with fucoidan

Characterization tests of the Nb₃Sn calbe-in-conduit conductors for Se.C.R.E.T.S.

Two Nb3Sn cable-in-conduit conductors have been procured for Se.C.R.E.T.S. (Segregated Copper Ratio Experiment on Transient Stability). The two conductors are identical in the fractional cross sections. The only difference is the location of the copper stabilizer, included either as segregated copper wires or as copper shell in the superconducting strands. A number of characterization tests, on individual strands and cabled conductors, have been carried out to establish a solid data base for the assessment of the results in the main experiment

Se.C.R.E.T.S.: A stability experiment on the role of segregated copper in Nb/sub 3/Sn cable-in-conduit conductors

In Se.C.R.E.T.S. (Segregated Copper Ratio Transient Stability), the stability performance under transverse field transient is compared for two Nb/sub 3/Sn cable-in-conduit conductors which differ only because of the different distribution of the stabilizing copper, either included in the Nb/sub 3/Sn strand cross section or segregated as bundled copper wires. If the segregated copper is found to be effective for stability purposes, the copper fraction in the Nb/sub 3/Sn strands can be substantially reduced, with dramatic cost advantage for the high field fusion magnets. The experiment is assembled in the SULTAN facility at CRPP, with 11 T background field and superimposed transverse pulsed field to generate the transient disturbance. The layout of the conductor, the winding sample and the assembly procedure are described. The instrumentation and the test program are planned to provide results to be easily extrapolated to the ITER conductors

Chemical Profiling and Bioactivity of Body Wall Lipids from Strongylocentrotus droebachiensis

The lipids from gonads and polyhydroxynaphthoquinone pigments from body walls of sea urchins are intensively studied. However, little is known about the body wall (BW) lipids. Ethanol extract (55 degrees C) contained about equal amounts of saturated (SaFA) and monounsaturated fatty acids (MUFA) representing 60% of total fatty acids, with myristic, palmitic and eicosenoic acids as major SaFAs and MUFAs, respectively. Non-methylene-interrupted dienes (13%) were composed of eicosadienoic and docosadienoic acids. Long-chain polyunsaturated fatty acids (LC-PUFA) included two main components, n6 arachidonic and n3 eicosapentaenoic acids, even with equal concentrations (15 mu g/mg) and a balanced n6/n3 PUFA ratio (0.86). The UPLC-ELSD analysis showed that a great majority of the lipids (80%) in the ethanolic extract were phosphatidylcholine (60 mu g/mg) and phosphatidylethanolamine (40 mu g/mg), while the proportion of neutral lipids remained lower than 20%. In addition, alkoxyglycerol derivativeschimyl, selachyl, and batyl alcoholswere quantified. We have assumed that the mechanism of action of body wall lipids in the present study is via the inhibition of MAPK p38, COX-1, and COX-2. Our findings open the prospective to utilize this lipid fraction as a source for the development of drugs with anti-inflammatory activity.Peer reviewe

Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats

Fucus vesiculosus L., known as bladderwrack, belongs to the brown seaweeds, which are widely distributed throughout northern Russia, Atlantic shores of Europe, the Baltic Sea, Greenland, the Azores, the Canary Islands, and shores of the Pacific Ocean. Fucoidan is a major fucose-rich sulfated polysaccharide found in Fucus (F.) vesiculosus. The pharmacokinetic profiling of active compounds is essential for drug development and approval. The aim of the study was to evaluate the pharmacokinetics and tissue distribution of fucoidan in rats after a single-dose oral administration. Fucoidan was isolated from F. vesiculosus. The method of measuring anti-activated factor X (anti-Xa) activity by amidolytic assay was used to analyze the plasma and tissue concentrations of fucoidan. The tissue distribution of fucoidan after intragastric administration to the rats was characterized, and it exhibited considerable heterogeneity. Fucoidan preferentially accumulates in the kidneys (AUC(0-t) = 10.74 mu g.h/g; C-max = 1.23 mu g/g after 5 h), spleen (AUC(0-t) = 6.89 mu g.h/g; C-max = 0.78 mu g/g after 3 h), and liver (AUC(0-t) = 3.26 mu g.h/g; C-max = 0.53 mu g/g after 2 h) and shows a relatively long absorption time and extended circulation in the blood, with a mean residence time (MRT) = 6.79 h. The outcome of this study provides additional scientific data for traditional use of fucoidan-containing plants and offers tangible support for the continued development of new effective pharmaceuticals using fucoidan.Peer reviewe

THE INFLUENCE OF THE DIFFERENT FACTORS ON THE GROWTH OF THE GINSENG BIOMASS AND THE DEVELOPMENT OF THE SMALL-WASTE TECHNOLOGY OF THE READY MEDICINAL MEANS FROM IT

The influence of the low temperatures on the growth and content of the panaxosides and carbohydrates in the culture of the ginseng tissue has been studied. It has been established, that the triterene glycosides play the role of the trigger in the mechanism of the adaptation reaction. The method of growing the biomass of the ginseng on the not expensive nutrient medium without adding the kinetine, has been improved. The optimum technology of the potion Bioginseng and small-waste technology of the original high-effective inspecific enterosorbent Panasorb from the ginseng biomass short have been developedAvailable from VNTIC / VNTIC - Scientific & Technical Information Centre of RussiaSIGLERURussian Federatio

Medicinal plants from the 14^th edition of the Russian Pharmacopoeia, recent updates

Ethnopharmacological relevance: Herbal medicine in Russia has a long history starting with handwritten herbalist manuscripts from the Middle Ages to the officinal Pharmacopoeia of the 21st century. The “herbophilious” Russian population has accumulated a lot of knowledge about the beneficial effects of local medicinal plants. Yet, for a long time, Russian traditional and officinal herbal medicine was not well known to the international audience. In our previous comprehensive review, we discussed the pharmacological effects of specific plants included in the 11 edition of the Pharmacopoeia of the USSR, which was also for a while used in Russia. The 14 edition of the Russian Federation's State Pharmacopoeia was implemented in 2018. Aim of the review: The aims of the present review are: (i) to trace the evolution of medicinal plant handling from handwritten herbalist manuscripts to Pharmacopoeias; (ii) to describe the modern situation with regulatory documents for herbal medicinal products and their updated classification; (iii) to summarize and discuss the pharmacology, safety, and clinical data for new plants, which are included in the new edition of the Pharmacopoeia. Methods: New medicinal plants included in the 14th edition of the Russian Federation's State Pharmacopoeia were selected. We carefully searched the scientific literature for data related to traditional use, pharmacological, clinical application, and safety. The information was collected from local libraries in Saint-Petersburg, the online databases E-library.ru, Scopus, Web of Science, and the search engine Google scholar. Results: Investigating the evolution of all medicinal plants referred to in the Russian Pharmacopoeias led us to the identification of ten medicinal plants that were present in all editions of civilian Russian Pharmacopoeias starting from 1778. In the 14 edition of the modern Russian Pharmacopoeia, medicinal plants are described in 107 monographs. Altogether, 25 new monographs were included in the 14 edition, and one monograph was excluded in comparison to the 11 edition. Some of the included plants are not endemic to Russia and do not have a history of traditional use, or on the other hand, are widely used in Western medicine. For 15 plants, we described the specificity of their application in Russian traditional medicine along with the claimed dosages and indications in officinal medicine. The pharmacology, safety, and clinical data are summarized and assessed for nine plants, underlining their therapeutic potential and significance for global phytopharmacotherapy. Conclusions: In this review, we highlight the therapeutical potential of new plants included in the modern edition of the Russian Pharmacopoeia. We hope that these plants will play an imperative role in drug development and will have a priority for future detailed research. th th th th t