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The present study evaluates the phytochemical content and biological activities of eight Clerodendrum paniculatum leaf extracts obtained using four solvents of varying polarity and two extraction methods. GC-HRMS analysis of the hexane extract predicted presence of phytol, 22-tritetracontanone, and 6,9,12-octadecatrienoic acid, phenyl methyl ester, (ZZZ)-as major compounds, and ethyl acetate extract was predicted to contain phytol. LC-HRMS analysis of methanolic extract exhibited the presence of 8',10'-dihydroxydihydroergotamine, Khayanthone, Galactonic acid, Calotropin, and 26,26,26,27,27,27-hexafluoro-1alpha,24-dihydroxy vitamin D3 as significant fractions. Ethyl acetate extract showed significant antimicrobial activity in-vitro. Methanolic extracts possess the highest radical scavenging activity (up to 87%) and antidiabetic activity (up to 49%) at 1 mg/mL concentration. Methanolic extracts from maceration and the Soxhlet method showed better cytotoxicity against breast and oral cancer cell lines, while the aqueous extract from maceration demonstrated better cytotoxicity against lung cancer cell lines. Methanolic extracts containing tannins, flavonoids, alkaloids, quinones, glycosides, terpenoids, diterpenoids, and phytosterols demonstrated significant bioactivity. [ABSTRACT FROM AUTHOR]

The aim of the study was to examine the immunomodulatory effect of crude Chelidonium majus L ethanolic extract on ex vivo harvested peripheral blood mononuclear cells (PBMNCs). PBMNCs were isolated by density gradient centrifugation. The PBMNC cytotoxicity assay was performed with HeLa tumor cells as target cells. MTT assay was used to estimate the proliferation effect of extract and cytotoxic efficiency of treated PBMNCs. Flow cytometric analysis was used for immunophenotyping. Treatment induced moderate proliferative response, perturbation in PBMNC ratios, and the emergence of some unconventional subpopulations. The percentage ratio of double positive CD4+ and CD8+ T lymphocytes and monocytes, ratio of T and B lymphocytes expressing CD14, and percentage of NK cells expressing CD57 increased after treatment, indicating activation of PBMNC subpopulations. Cytotoxic activity against HeLa cells was enhanced. Activation of PBMNCs and enhancement of their cytotoxic effect toward HeLa cells indicate the immunostimulatory effect of Ch. majus ethanolic extract. [ABSTRACT FROM AUTHOR]

Synthetic 3 D extracellular matrix (ECM) have been used to evaluate cell behavior in vitro. However, how cells and the growth factors interact with the ECM is still not fully understood. The objective of the present work is to evaluate in vitro L929 mouse fibroblasts in contact with Poly(vinyl alcohol) (PVA) hydrogel added with the growth factors: fibroblast (FGF), transforming-β1 (TGF-ß1), vascular endothelial (VEGF), insulin-like (IGF), and epidermal (EGF). The cytotoxicity assay showed that the maximum concentration of PVA hydrogel per well must be 10 vol%. When the factors EGF and FGF were added to the wells individually, it was possible to increase the concentration of PVA hydrogel to 15.04% and 18.81%, respectively, without interfering with the level of cytotoxicity. The IGF and the TGF-β1, when individually incorporated into the PVA hydrogel, affected negatively the cell viability (7.04% and 7.89%, respectively) compared to the other. The smallest allowable concentration occurred when all the factors were incorporated together with the PVA hydrogel (3,6%). Statistical significance (p < 0.05) was obtained between PVA + FGF, PVA + TGF, and PVA + EGF and their controls. [ABSTRACT FROM AUTHOR]

Cistus incanus L. (hairy rockrose) is a medicinal plant which belongs to the Cistaceae family and the Cistus genus, with a well established position in traditional medicine of the Mediterranean basin and the Middle East. It was the aim of this study to compare antibacterial activity of the phenolics derived from fourteen C. incanus samples of different origin (Turkey, Albania, Greece, and an unknown geographical location) obtained as herbal teas from a local market of diet supplements. This activity was assessed with the use of thin-layer chromatography-direct bioautography (TLC-DB) applied to crude extracts against the Gram negative naturally luminescent marine bacterium Aliivibrio fischeri and the Gram positive soil bacterium Bacillus subtilis as the test microorganisms. It was established that in spite of different origin of the investigated herbal samples, in qualitative terms their antibacterial activity was closely comparable and more strongly pronounced against the Gram positive than the Gram negative bacterium. Crude extract originating from one herbal specimen labelled A3 (sample no. 3 from Albania) underwent selective multi-step extraction of the phenolics, dividing them into six fractions (I to VI) that expectedly contain flavonoid aglycons, free phenolic acids, non-polar flavonoid glycosides, polar flavonoid glycosides, and phenolic acids obtained through the acidic and basic hydrolysis from the respective glycosides. Antibacterial activity of each A3 fraction was then assessed with the use of the same TLC-DB approach and it was established that the strongest effect was exerted by fractions I and II (flavonoid aglycons and free phenolic acids). Moreover, cytotoxic assay was performed for the crude C. incanus extracts against the human colon adenocarcinoma cells and a moderate yet well measurable cytotoxic effect was observed with all investigated C. incanus samples. In analogy to antibacterial activity, also in this case cytotoxic potential of all investigated crude C. incanus extracts was similar. [ABSTRACT FROM AUTHOR]

To solve the high viscosity of bisphenol A glycerolate dimethacrylate (Bis-GMA), its derivate Ac-Bis-GMA substituting acetyl groups for hydroxyl groups was synthesised by the esterification reaction and mixed with tri(ethylene glycol) dimethacrylate (TEGDMA) as polymer matrix to fabricate dental resin restorative composites. To improve the degree of conversion (DC), polymerization shrinkage (PS) and wear resistance of resin-based composite (RBC) 58-12 filled with commercial microsize and nanosize (M/N) SiO2 particles, bimodal silica nanostructures consisting of SiO2 nanoparticles (NPs) and SiO2 nanoclusters (NCs) were introduced as inorganic fillers. Resin composites with different mass ratios of silanized SiO2 NPs and SiO2 NCs were fabricated under the light polymerisation, and the effect of filler compositions on these two properties, wear resistance (wear volume and worn surface morphology), and cytotoxicity assay of resin composites was investigated in this work. The results suggested that resin composites reinforced with bimodal silica nanostructures at the optimum ratio presented the improved performance, especially for RBC 35-35 (SiO2 NPs:SiO2 NCs = 35:35, wt/wt), which resulted in 16% enhancement in DC and 19% reduction of PS, the smoother and flatter worn surface after 10 000 wear cycles, as well as the excellent cytocompatibility, compared with those of RBC 58-12.This effective and facile way might provide a new sight to develop dental resin restorative composites for clinical application. [ABSTRACT FROM AUTHOR]

Context: Skin cancer has turned into global epidemic leading to higher incidences among cancer stricken population. Objective: The aim of the present investigation is to evaluate the anticancer potential and intracellular uptake of a novel nanovesicular formulation of 5-FU. Materials and methods: Detailed intracellular uptake study in conjunction with estimation of intracellular reactive oxygen species was done using skin melanoma cell lines (A375) along with cytotoxicity studies. To further obtain the mechanistic insights into inhibition of tumor cell proliferation, cell-cycle arrest studies were conducted. The preclinical anticancer activity was carried out employing in vivo DMBA-croton oil-induced skin cancer model in mice. Results and discussion: Significant reduction in the number of papillomas was observed in skin cancer-bearing mice on treatment with nanovesicular formulation (51.4 ± 3.2%) in comparison with marketed formulation (21.3 ± 2.1%) of 5-FU. Tumor volume was found to be reduced to 46.3 ± 3.5% with prepared formulation, whereas the marketed formulation-treated group showed the reduction of 18.6 ± 1.8% in comparison with the control (untreated) group. Conclusion: The results of present study demonstrated that nanovesicular formulation of 5-FU possessed the enhanced anticancer activity which could be attributed to better intracellular uptake, cellular retention, and sustained release of drug. [ABSTRACT FROM AUTHOR]

Two new compounds 5-[4′-(4″-hydroxybenzyl)-3′-hydroxybenzyloxymethyl]-furan-2-carbaldehyde (1) and 5-[4′-(4″-hydroxybenzyl)-3′-hydroxybenzyl]-furan-2-carbal-dehyde (2), together with two known 5-(4-hydroxbenzyloxymethyl)-furan-2-carbaldehyde] (3) and 5-(hydroxymethyl)-2-furaldehyde (4), were isolated from the rhizome ofGastrodia elata. Their structures were elucidated by spectroscopic analysis and comparison of their spectral data with those reported previously. All compounds exhibited weak or no cytotoxicity against human colon carcinoma cell line (HT-29) and human chronic myelogenous leukemia cell line (K-562). [ABSTRACT FROM AUTHOR]

Established cell lines are utilized extensively to study tumor biology and preclinical therapeutic development. However, they may not accurately recapitulate the heterogeneity of their corresponding primary disease. B-cell tumor cells are especially difficult to maintain under conventional culture conditions, limiting access to samples that faithfully represent this disease for preclinical studies. Here, we used primary canine diffuse large B-cell lymphoma to establish a culture system that reliably supports the growth of these cells. CD40 ligand, either expressed by feeder cells or provided as a soluble two-trimeric form, was sufficient to support primary lymphoma cells in vitro. The tumor cells retained their original phenotype, clonality and known karyotypic abnormalities after extended expansion in culture. Finally, we illustrate the utility of the feeder cell-free culture system for comparable assessment of cytotoxicity using dog and human B-cell malignancies. We conclude that this system has broad applications for in vitro preclinical development for B-cell malignancies. [ABSTRACT FROM AUTHOR]