Different topical hemostatic materials are used to achieve effective hemostasis. High hemostatic activity, biocompatibility, bioresorbability, and easy manipulation are to be expected in such a ...developed product. In the surgical world with these specific requirements, finding a proper hemostatic agent is very difficult. The study compared several materials of various construction properties, which were assessed for structural and related properties by morphological analyses and assessed in vivo for their efficiency and behaviour using a model of rat partial nephrectomy. New sodium salt of carboxymethyl cellulose (CMC) sponge with the lowest porosity and free swell absorptive capacity contained the highest amount of hydroxyl and carboxyl groups. Results revealed that this CMC material in the form of a bioresorbable sponge may ensure the necessary hemostatic effects, while also providing a positive influence on the reaction of the local tissue. The CMC material also needed significantly less time to achieve hemostasis (
p
< 0.001). Moreover, the sponge reached satisfactory results in the histopathological evaluation with the lowest destruction score and favorable healing reaction. This modified product proved itself to be a promising bioresorbable hemostat, which, according to its design, matches with its surgical applications. In general, the obtained data elucidated the dependency of the total effect on its structure and composition.
Graphic abstract
The experiment aimed to determine the effect of 50% (LS50) or 100% (LS100) substitution of lupin protein (variety Zulika) for soybean protein in feed mixtures intended for the nutrition of broiler ...chickens, on muscular fat quality (composition of fatty acids). There were established three groups of chickens for fattening with 80 individuals each (control group C and experimental groups). After the 34-day fattening period chicken breast and thigh muscles were analysed to find out the fatty acid composition. Lupin protein-based diets had a positive effect on the muscle quality of fattened chickens due to changes in fatty acid composition, compared to soya protein-based diets. The feeding of lupin-based diets to broiler chickens resulted in the reduction of saturated fatty acids (P ≤ 0.05) by 14% in LS50 group and 17% in LS100 group and increase of unsaturated fatty acids (P ≤ 0.05) by 58% in LS50 group and 90% in LS100 group in muscle fat. The results clearly confirm that lupin-based diet increases the dietary value of chicken meat as one of the most important protein sources in human nutrition.
The aim of the experiment was to determine how the content of lupin meal in the diet for commercial laying hens would affect the quality of fat in the egg yolk. A total of 210 Isa Brown laying hens ...was divided into three groups: the control group C (fed a mixture containing only soybean meal as a source of protein) and two experimental groups: EN 50% (fed a mixture containing 50% of soybean meal and 50% of white lupin seed meal, Zulika variety) and EN 100% (fed a mixture containing only white lupin seed meal as a source of protein). The results of the experiment using lupin seed meal in the feed mixture as a 50% and 100% replacement of extracted soybean meal confirmed the positive effect of lupin-based diets on egg yolk fat composition. Although the diets did not affect the fat content of the egg yolk, some other changes in the quality of the egg yolk were demonstrated during laying. These changes in egg yolk fat were characterized by a decrease (P ≤ 0.05) of saturated fatty acids (SFA), an increase (P ≤ 0.05) of monounsaturated fatty acids (MUFA), but only in some of them (C17:1 – heptadecenoic acid; C20:1n9 – eicosenoic acid and C22:1n9 – erucic acid) and, what is important, by a significant (P ≤ 0.05) increase of polyunsaturated fatty acids (PUFA) from the n-6 group (C18:2n6 – linoleic acid and C20:2n-6 – eicosadienoic acid) and n-3 group (C18:3n3 – α-linolenic acid; C20:5n3 – eicosapentaenoid acid and C22:5n3 – docosapentaenoic acid). From these results it is evident that using lupin meal in the feed mixtures for commercial laying hens increases the nutritional value and health benefit of the egg through the improvement of the levels of saturated and unsaturated fatty acids.
We report in vitro and in vivo anti-inflammatory activities of a series of copper(II)-lawsone complexes of the general composition Cu(Law)2(LN)x(H2O)(2-x)·yH2O; where HLaw = ...2-hydroxy-1,4-naphthoquinone, x = 1 when LN = pyridine (1) and 2-aminopyridine (3) and x = 2 when LN = imidazole (2), 3-aminopyridine (4), 4-aminopyridine (5), 3-hydroxypyridine (6), and 3,5-dimethylpyrazole (7). The compounds were thoroughly characterized by physical techniques, including single crystal X-ray analysis of complex 2. Some of the complexes showed the ability to suppress significantly the activation of nuclear factor κB (NF-κB) both by lipopolysaccharide (LPS) and TNF-alpha (complexes 3-7 at 100 nM level) in the similar manner as the reference drug prednisone (at 1 μM level). On the other hand, all the complexes 1-7 decreased significantly the levels of the secreted TNF-alpha after the LPS activation of THP-1 cells, thus showing the anti-inflammatory potential via both NF-κB moderation and by other mechanisms, such as influence on TNF-alpha transcription and/or translation and/or secretion. In addition, a strong intracellular pro-oxidative effect of all the complexes has been found at 100 nM dose in vitro. The ability to suppress the inflammatory response, caused by the subcutaneous application of λ-carrageenan, has been determined by in vivo testing in hind-paw edema model on rats. The most active complexes 1-3 (applied in a dose corresponding to 40 μmol Cu/kg), diminished the formation of edema simalarly as the reference drug indomethacine (applied in 10 mg/kg dose). The overall effect of the complexes, dominantly 1-3, shows similarity to anti-inflammatory drug benoxaprofen, known to induce intracellular pro-oxidative effects.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, SIK, UILJ, UKNU, UL, UM, UPUK
This work presents a deeper pharmacological evaluation of two formerly prepared and characterized, and highly in vitro cytotoxic platinum(II) oxalato complexes Pt(ox)(L
1
)
2
(
1
) and Pt(ox)(L
2
)
...2
(
2
), containing the derivatives of cyclin-dependent kinase inhibitor (CDKi) seliciclib ((
R
)-roscovitine, CYC202) coordinating as
N
-donor carrier ligands, i.e., 2-(1-ethyl-2-hydroxyethylamino)-
N
6-(4-methoxybenzyl)-9-isopropyladenine (L
1
) and 2-chloro-
N
6-(2,4-dimethoxybenzyl)-9-isopropyladenine (L
2
). The positive results of in vitro cytotoxicity screening on human cancer cell lines (HeLa, HOS, A2780, A2780R, G361 and MCF7 with IC
50
at low micromolar levels) published previously, motivated us to perform extended preclinical in vitro experiments to reveal the mechanisms associated with the induction of cancer cell death. In addition, the in vivo antitumor activity was evaluated using the mouse lymphocytic leukaemia L1210 model. The obtained results revealed that complex
1
exceeds the antitumor effect of cisplatin (as for the extension of life-span of mice) and shows far less adverse effects as compared to reference drug cisplatin. The in vitro and ex vivo studies of cellular effects and molecular mechanisms of cell death induction showed that the mechanism of action of complex
1
is essentially different from that of cisplatin. The obtained results showed a possible way how to obtain antitumor active platinum(II) oxalato complexes with better therapeutic profile than contemporary used platinum-based therapeutics.
The gold(I) complexes of the general formula Au(L n )(PPh3)·xH2O (1–8; n = 1–8 and x = 0–1.5), where L n stands for a deprotonated form of the benzyl-substituted derivatives of 6-benzylaminopurine, ...were prepared, thoroughly characterized (elemental analyses, FT-IR, Raman and multinuclear NMR spectroscopy, ESI+ mass spectrometry, conductivity, DFT calculations), and studied for their in vitro cytotoxicity and in vitro and in vivo anti-inflammatory effects on LPS-activated macrophages (derived from THP-1 cell line) and using the carrageenan-induced hind paw edema model on rats. The obtained results indicate that the representative complexes (1, 3, 6) exhibit a strong ability to reduce the production of pro-inflammatory cytokines TNF-α, IL-1β and HMGB1 without influence on the secretion of anti-inflammatory cytokine IL-1RA in the LPS-activated macrophages. The complexes also significantly influence the formation of edema, caused by the intraplantar application of polysaccharide λ-carrageenan to rats in vivo. All the tested complexes showed similar or better biological effects as compared with Auranofin, but contrary to Auranofin they were found to be less cytotoxic in vitro. The obtained results clearly indicate that the gold(I) complexes behave as very effective anti-inflammatory agents and could prove to be useful for the treatment of difficult to treat inflammatory diseases such as rheumatoid arthritis.
Morusin is a prenylated flavonoid isolated from the root bark of Morus alba. Many studies have shown the ability of flavonoids to act as anti-inflammatory agents. The aim of this study was to ...evaluate the effect of morusin on experimentally colitis induced by 2,4,6-trinitrobenzensulfonic acid in Wistar rats and to compare it with sulfasalazine, a drug conventionally used in the treatment of inflammatory bowel disease. Morusin was administered by gavage at doses of 12.5, 25, or 50 mg/kg/day for five days. The colonic tissue was evaluated macroscopically, histologically, and by performing immunodetection and zymographic analysis to determine the levels of antioxidant enzymes superoxide dismutase (SOD) and catalase (CAT), interleukin (IL)-1β, and transforming growth factor (TGF)-β1 and the activities of matrix metalloproteinases (MMP) 2 and 9. The tissue damage scores were significantly reduced with increasing dose of morusin, however efficacy was not demonstrated at the highest dose. At the dose of 12.5 mg/kg, morusin exerted therapeutic effectivity similar to that of sulfasalazine (50 mg/kg). This was associated with significant reduction of TGF-β1 levels and MMP2 and MMP9 activities, and slight reduction of IL-1β. Our results suggest that morusin possesses therapeutic potential for the treatment of chronic inflammatory diseases.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, SIK, UILJ, UKNU, UL, UM, UPUK
The in vitro antitumour activity studies on a panel of human cancer cell lines (A549, HeLa, G-361, A2780, and A2780R) and the combined in vivo and ex vivo antitumour testing on the L1210 lymphocytic ...leukaemia model were performed on the cis-PtCl2(naza)2 complexes (1-3) involving the 7-azaindole derivatives (naza). The platinum(II) complexes showed significantly higher in vitro cytotoxic effects on cell-based models, as compared with cisplatin, and showed the ability to avoid the acquired resistance of the A2780R cell line to cisplatin. The in vivo testing of the complexes (applied at the same dose as cisplatin) revealed their positive effect on the reduction of cancerous tissues volume, even if it is lower than that of cisplatin, however, they also showed less serious adverse effects on the healthy tissues and the health status of the treated mice. The results of ex vivo assays revealed that the complexes 1-3 were able to modulate the levels of active forms of caspases 3 and 8, and the transcription factor p53, and thus activate the intrinsic (mitochondrial) pathway of apoptosis. The pharmacological observations were supported by both the histological and immunohistochemical evaluation of isolated cancerous tissues. The applicability of the prepared complexes and their fate in biological systems, characterized by the hydrolytic stability and the thermodynamic aspects of the interactions with cysteine, reduced glutathione, and human serum albumin were studied by the mass spectrometry and isothermal titration calorimetric experiments.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, SIK, UILJ, UKNU, UL, UM, UPUK
The achievement of rapid hemostasis represents a long-term trend in hemostatic research. Specifically, composite materials are now the focus of attention, based on the given issues and required ...properties. In urology, different materials are used to achieve fast and effective hemostasis. Additionally, it is desirable to exert a positive influence on local tissue reaction. In this study, three nonwoven textiles prepared by a wet spinning method and based on a combination of hyaluronic acid with either oxidized cellulose or carboxymethyl cellulose, along with the addition of etamsylate, were introduced and assessed in vivo using the rat partial nephrectomy model. A significantly shorter time to hemostasis in seconds (
< 0.05), was attributed to the effect of the carboxymethyl cellulose material. The addition of etamsylate did not noticeably contribute to further hemostasis, but its application strengthened the structure and therefore significantly improved the effect on local changes, while also facilitating any manipulation by the surgeons. Specifically, the hyaluronic acid supported the tissue healing and regeneration, and ensured the favorable results of the histological analysis. Moreover, the prepared textiles proved their bioresorbability after a three-day period. In brief, the fabrics yielded favorable hemostatic activity, bioresorbability, non-irritability, and had a beneficial effect on the tissue repair.
Morus alba L. is used in traditional Chinese medicine for the treatment of various diseases, including bacterial infections and inflammation. As a rich source of phenolic compounds, the plant is an ...object of many phytochemical and pharmacological studies.
The aim of the study was to isolate and evaluate possible parallel antiviral, antibacterial, and anti-inflammatory activities of phenolic mulberry compounds.
Extensive chromatographic separation of mulberry root bark extract and in vitro biological screening of 26 constituents identified promising candidates for further pharmacological research. Selected compounds were screened for anti-infective and anti-inflammatory activities. Antiviral activity was determined by the plaque number reduction assay and by the titer reduction assay, antibacterial using broth microdilution method, and anti-inflammatory activity using COX Colorimetric inhibitor screening assay kit. One compound was evaluated in vivo in carrageenan-induced paw-edema in mice.
Five prenylated compounds 1, 2, 8, 9, and 11, together with a simple phenolic ester 13, exhibited inhibitory activity against the replication of herpes simplex virus 1 (HSV-1) or herpes simplex virus 2 (HSV-2), with IC50 values ranging from 0.64 to 1.93 μg/mL, and EC50 values 0.93 and 1.61 μg/mL. Molecular docking studies demonstrated the effects of the active compounds by targeting HSV-1 DNA polymerase and HSV-2 protease. In antibacterial assay, compounds 1, 4, 11, and 17 diminished the growth of all of the Gram-positive strains tested, with MIC values of 1–16 μg/mL. The anti-inflammatory ability of several compounds to inhibit cyclooxygenase 2 (COX-2) was tested in vitro, and compound 16 displayed greater activity than the indomethacin, positive control. Mulberrofuran B (11) showed anti-inflammatory activity in vivo against carrageenan-induced paw-edema in mice.
Experimental investigation showed promising antiviral, antibacterial, and/or anti-inflammatory activities of the phenolic mulberry constituents, often with multiple inhibitory effects that might be used as a potential source of new medicine.
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