Hemostatic effect and distribution of new rhThrombin formulations in rats.

Recombinant human thrombin (rhThrombin) is a potential hemostatic alternative to bovine and human plasma-derived thrombin. Hemostatic, liver regeneration effect and plasma concentrations of rhThrombin (SCILL) tested in the form of solution and hydrogels (thermo-sensitive poloxamer gel and carbomer gel; hameln rds) were evaluated. In the bleeding model, rhThrombin was applied locally on the bleeding site.

Surface decorated poly(ester-ether-urethane)s nanoparticles: a versatile approach towards clinical translation.

Poly(ester-ether-urethane)s copolymers are a resourceful class of biopolymers for the preparation of nanocarriers for drug delivery applications. However, a simple clinical translation for this synthetic material with biological and quality features is still needed. In this view, poly(ε-caprolactone)-co-poly(ethylene glycol) copolymers were synthesized as semi-bulk pilot (Kg) scale under mild conditions in absence of catalyst, bearing functional termini such as fluorescein tag and anticancer targeting moieties.

Isolation, structure elucidation and biological activity of angucycline antibiotics from an epiphytic yew streptomycete.

In the course of study of epiphytic microorganisms occurring on the surface of roots of Taxus baccata L. a new strain Streptomyces sp. AC113 was isolated.

Encapsulation of anticancer drug and magnetic particles in biodegradable polymer nanospheres.

In this study, we have prepared PLGA (poly-D,L-lactide-co-glycolide) nanospheres loaded with biocompatible magnetic fluid and anticancer drug taxol by a modified nanoprecipitation technique and investigated their magnetic properties. A magnetic fluid, MF-PEG, with a biocompatible layer of polyethylene glycol (PEG), was chosen as a magnetic carrier. The PLGA, whose copolymer ratio of D,L-lactide to glycolide is 85:15, was utilized as a capsulation material.

Antiprotease and antimetastatic activity of ursolic acid isolated from Salvia officinalis.

Proteases play a regulatory role in a variety of pathologies including cancer, pancreatitis, thromboembolic disorders, viral infections and many others. One of the possible strategies how to combat with these pathologies seems to be the use of low molecular inhibitors. Natural products were evaluated in the in vitro antiprotease assay on serine proteases (trypsin, thrombin and urokinase) and on the cysteine protease cathepsin B.

Cytotoxic/antiproliferative effects of new [1,2,4]triazolo[4,3-c] quinazolines in tumor cell lines HeLa and B16.

Quinazolines - 1,3-benzodiazines are biological active compounds, and some of them act as anticancer drugs. We evaluated cytotoxic/antiproliferative activity of new synthetically prepared [1,2,4]triazolo[4,3-c]quinazolines using tumor cell lines HeLa and B16. The in vitro cytotoxic studies of the most active derivative 3-(5-nitro-2-thienyl)-9-chloro-5-morpholin- 4-yl[1,2,4]triazolo[4,3-c]quinazoline (NTCHMTQ) were complemented by cell cycle analysis, and determination of apoptotic DNA fragmentation.

Teratological study of the herbicide 4-chloro-2-methylphenoxyacetic acid in rabbits.

4-Chloro-2-methylphenoxyacetic acid (MCPA) is an aryloxyacetic acid derivative categorised as a plant hormone herbicide. The aim of the study was to evaluate the effect of MCPA on pregnant females and the prenatal development of rabbits. The substance tested was administered orally to pregnant New Zealand White rabbits from day 6 to day 27 of gestation at doses of 5, 10 and 25 mg kg(-1) day(-1).

Antiproliferative activity of berberine in vitro and in vivo.

Berberine, an isoquinoline plant alkaloid acted cytotoxically in vitro on tumour cell lines B16. Its anticancer activity in vivo was studied with the transplanted B16 line in the range of doses from 1 mg/kg to 10 mg/kg. The significant reduction of tumor volume was observed on day 16 at doses of 5 and 10 mg/kg.

Berberine-antiproliferative activity in vitro and induction of apoptosis/necrosis of the U937 and B16 cells.

Berberine, an isoquinoline plant alkaloid, is widely distributed in plants used in the traditional Chinese medicine. It displays a wide range of biological activities and the mechanism of action. Our previous studies of the anticancer activity of berberine against the cancer cell lines HeLa and L1210 were extended to the human tumour U937 cell line and the murine melanoma B16 cell line growing in vitro.

Immunosuppressive effects of vermiculine in vitro and in allotransplantation system in vivo.

Vermiculine, a macrocyclic aglycosidic dilactone isolated from Penicillium vermiculatum, has been shown to have immunomodulatory properties. Here, we tested the effects of vermiculine on selected parameters of cell-mediated immunity in vitro and on skin allograft survival in vivo. Vermiculine inhibited in a dose-dependent manner the proliferation of mouse spleen cells stimulated with Concanavalin A ((Con A), i.

Toxicological evaluation of the new calcium antagonist VULM 993.

The tolerance of the new calcium antagonist VULM 993 was investigated in a series of toxicological studies. The following results were obtained: the maximum tolerated oral dose in acute toxicity was 10,000 mg/kg for mice and 6600 mg/kg for rats, for venous administration it was 26.1 mg/kg in mice and 32.

Efficacy of 6-amino-2-n-pentylthiobenzothiazole on Trichophyton in vitro and in vivo.

In vitro and in vivo antifungal activities of synthetically parepared 6-amino-2-n-pentylthiobenzothiazole (APB) against Trichophyton strains were studied. APB inhibited the growth of 3 Trichophyton strains at 65 micrograms/ml. 2-Mercaptobenzothiazole was not effective at 125 micrograms/ml and ketoconazole inhibited the growth at 20-30 micrograms/ml.

Antifungal activity of a new benzothiazole derivative against Candida in vitro and in vivo.

The antifungal activity of 6-amino-2-n-pentylthiobenzothiazole (APB) against 26 strains of the genus Candida in vitro was studied. Susceptibility of 17 strains was IC(50) View Article and Find Full Text PDF

Vermiculin derivatives. Part 2: Cytotoxic and mutagenic activities of vermiculin derivatives.

The induction of mutations at the HPRT locus and cytotoxicities of 4 vermiculin derivatives 2-4 and 6 were examined in V79 Chinese hamster cells and compared with those of the parent compound vermiculin (1). Derivatives prepared by hydrogenation were less toxic and mutagenic or non toxic and non mutagenic. The substitution at position 13 affected the evaluated biological effects.

Vermiculin derivatives. Part 1: Synthesis of vermiculin derivatives.

Hydrogenation of the macrodiolide antibiotic vermiculin (1) over Adams catalyst afforded [8S, 16S]-8,16-bis(2'-oxopropyl)-1,9- dioxyacyclohexadeca-2,5,10,13-tetrone (2), [8S, 16S]-8,16-bis(2'-oxopropyl)-13-hydroxy-1,9-dioxacyclohexadeca- 2,5,10-trione (3), [8S,16S]-8,16-bis(2' oxopropyl)-1,9- dioxacyclohexadeca-2,5,10-trione (4) together with [7S]-4,9-dioxo-7-(4',9'-dioxodecanoyloxy)decanoic acid (5). Hydrogenation of diolide 1 over Pd/C gave tetrahydrovermiculin (2) only. The prepared compounds showed lower antibacterial and cytotoxic activities than vermiculin (1).

[The in vitro effect of a combination of sulbactam with cephalothin and cefazolin on strains of Escherichia coli and Proteus mirabilis which produce beta lactamase].

The effect of the combination of sulbactam, cephalothin, and cephazolin was studied in vitro on 88 strains of E. coli and 11 strains of P. mirabilis producing beta-lactamases.