3T3 Cell Lines Research Articles

Enhancing the Bioconversion of Azelaic Acid to Its Derivatives by Response Surface Methodology.

Azelaic acid (AzA) and its derivatives have been known to be effective in the treatment of acne and various cutaneous hyperpigmentary disorders. The esterification of azelaic acid with lauryl alcohol (LA) to produce dilaurylazelate using immobilized lipase B from Candida antarctica (Novozym 435) is reported. Response surface methodology was selected to optimize the reaction conditions. A well-fitting quadratic polynomial regression model for the acid conversion was established with regards to several parameters, including reaction time and temperature, enzyme amount, and substrate molar ratios. The regression equation obtained by the central composite design of RSM predicted that the optimal reaction conditions included a reaction time of 360 min, 0.14 g of enzyme, a reaction temperature of 46 °C, and a molar ratio of substrates of 1:4.1. The results from the model were in good agreement with the experimental data and were within the experimental range (R2 of 0.9732).The inhibition zone can be seen at dilaurylazelate ester with diameter 9.0±0.1 mm activities against Staphylococcus epidermidis S273. The normal fibroblasts cell line (3T3) was used to assess the cytotoxicity activity of AzA and AzA derivative, which is dilaurylazelate ester. The comparison of the IC50 (50% inhibition of cell viability) value for AzA and AzA derivative was demonstrated. The IC50 value for AzA was 85.28 μg/mL, whereas the IC50 value for AzA derivative was more than 100 μg/mL. The 3T3 cell was still able to survive without any sign of toxicity from the AzA derivative; thus, it was proven to be non-toxic in this MTT assay when compared with AzA.

The effect of urinary Foley catheter substrate material on the antimicrobial potential of calixerene-based molecules.

This study was to investigate the antimicrobial activity of a modified calixarene polymer bound to a silicone substrate in the presence of pathogens associated with catheter infections, Escherichia coli and Proteus mirabilis. The molecule and its constituent parts were studied bound and unbound to silicone substrates to ascertain growth effects. Minimum inhibitory and bactericidal concentrations were determined against E.coli and P. mirabilis. Biofilm growth was studied by immersing silicone discs seeded with either P. mirabilis or E.coli in artificial urine. Biofilms were assessed at 3, 7 and 10days. The coated material reduced bacterial cell density compared to the uncoated samples. Direct and indirect toxicity tests were conducted with a fibroblast cell line (3T3); coated and noncoated silicone samples were seeded with cells (1×104 /cm2 ) and incubated for 72h. Hoechst propidium iodide staining identified delayed toxic effect from the coated and noncoated material leachate in all but the platinum-cured medical-grade silicone, which showed no evident toxicity. The calixerene polymer was determined to be the active part of the coating. Biofilm formation was dramatically reduced in the coated platinum-cured medical-grade silicone samples, but cell viability was reduced on the clinical-grade silicones regardless of coating in contrast to cells seeded on the platinum-cured medical-grade silicone. A delayed toxic response was evident to the extract of the coated and noncoated clinical-grade samples, indicating that the toxic effect is due to the underlying substrate. This study has established that the immobilized molecule enhances the antibacterial and antifouling properties of silicone, without toxicity. It also clearly demonstrates that regardless of coating efficacy, the substrate material has the capacity to disrupt its potency and change the nature of the material coating.

Evaluation of cytotoxic effects and acute and chronic toxicity of aqueous extract of the seeds of Calycotome villosa (Poiret) Link (subsp. intermedia) in rodents.

The present investigation was carried out to evaluate the safety of an aqueous extract of the seeds of Calycotome villosa (Poiret) Link (subsp. intermedia) by determining its cytotoxicity and potential toxicity after acute and sub-chronic administration in rodents. Cytotoxic activity was tested in cancer and non-cancer cell lines HeLa, Mel-5, HL-60 and 3T3. Acute toxicity tests were carried out in mice by a single oral administration of Calycotome seed-extract (0 - 12 g/kg) as well as intraperitoneal doses of 0 - 5 g/kg. Sub-chronic studies were conducted in Wistar rats by administration of oral daily doses for up to 90 days. Changes in body and vital organ weights, mortality, haematology, clinical biochemistry and histologic morphology were evaluated. The lyophilized aqueous extract of C. villosa exhibited a low cytotoxicity in all cell lines tested with an IC50 > 100 µg/ml. In the acute study in mice, intra-peritoneal administration caused dose-dependent adverse effects and mortality with an LD50 of 4.06 ± 0.01 g/kg. In the chronic tests, neither mortality nor visible signs of lethality was seen in rats. Even AST and ALT were not affected while a significant decrease in serum glucose levels, at 300 and 600 mg/kg was detected. Histopathological examination of the kidney and liver did not show any alteration or inflammation at the end of treatment. In conclusion, the aqueous extract of C. villosa seed appeared to be non-toxic and did not produce mortality or clinically significant changes in the haematological and biochemical parameters in rats.

Biological contour, molecular docking and antiproliferative studies of DNA targeted histidine based transition metal(II) complexes: Invention and its depiction

A novel series of histidine derived transition metal complexes were synthesized and characterized by multispectral techniques such as UV‐Vis., FT IR, EPR, NMR, ESI‐mass analysis and other physico‐chemical methods like elemental analysis, molar conductivity, magnetic susceptibility. The synthesized compounds were attempted for their biological prospective. The biological studies involved are DNA interaction (binding and damage), antimicrobial, antioxidant, antiproliferative and molecular docking. DNA interaction studies were carried out with the help of UV‐Vis absorption titration, viscosity measurement and cyclic voltammetric techniques which revealed that the synthesized compounds could interact with CT‐DNA through intercalative binding mode. A gel electrophoresis assay demonstrated the ability of complexes to cleave the supercoiled pUC18 DNA. The antioxidant property shows that the metal complexes have preferable ability to scavenge hydroxyl radical than the ligand. Moreover, the antimicrobial assay indicates that these complexes are good antimicrobial agents against various pathogens. Furthermore, the in vitro antiproliferative activities of the complexes were examined on HeLa, Hep G2 and NIH 3 T3 cell lines using an MTT assay. The morphological changes were investigated using Hoechst 33258 staining apoptosis assay. In addition, molecular docking studies were executed to considerate the nature of binding of the synthesized complexes with protein and DNA.

Antiproliferative and antiapoptotic effect of thymoquinone on cancer cells in vitro.

Nigella sativa oil and thymoquinone were comparatively tested in vitro for their effects on human cancer cell lines (glioma,T98; prostate, LnCaP) as well as mouse embryonic fibroblastcelllines (3T3), and for the induction of apoptosis. Individual cell lines were treated with thymoquinone and N. sativa oil for 24 and 48 hr. Survival rate with MTT, apoptosis with flow cytometry and caspase-9 mRNA enzyme levels with RT-PCR were determined in vitro. Application of respective concentrations of N. sativa oil (excluding 100 μg/mL for 48 hr) did not change the number of tested cell lines, however, treatment with thymoquinone reduced the number of all cells significantly. Thymoquinone also exerted its apoptosis inducing effect through the activation of caspase-9. Differing with the type of cancer cells, thymoquinone posseses a strong contentration and time dependent survival reducing effect on cancer cells via apoptosis (Fig. 6, Ref. 22). Text in PDF www.elis.sk.

Anti-inflammatory and anti-melanogenic effects of major leaf components of Alpinia zerumbet var. excelsa

Background: The leaves of Alpinia zerumbet var. excelsa (alpinia) are used to prepare traditional food items and folk medicines. Objective: This study was designed with a view to explore the anti-inflammatory and anti-melanogenic potentials of major components of alpinia leaves. Materials and Methods: Anti-inflammatory effects of leaf-derived compounds were primarily assessed with protein denaturation and proteinase assay. Their inhibitory effects on nitrite accumulation and prostaglandin E2 (PGE2) production in lipopolysaccharide-induced RAW 264.7 cells were also evaluated. For anti-melanogenic assays, all the compounds were tested on α-melanocyte-stimulating hormone-stimulated B16F10 cells and on mushroom tyrosinase in vitro. Their cytotoxicity was evaluated using fibroblast cell line 3T3 L-1 and brine shrimps. Results: Five compounds, 5,6-dehydrokawain, dihydro-5,6-dehydrokawain, (E)-5-methoxy-8-(4-methoxy-2-oxo-2H-pyran-6-yl)-7-phenyl-1-styryl-2-oxabicyclo[4.2.0]oct-4-en-3-one (AS-2), kaempferol 3-O-β-D-glucuronide (KOG), and quercetin 3-O-β-D-glucuronide (QOG) were purified from the leaves. Of which, AS-2 and QOG were purified for the first time. All compounds significantly inhibited albumin denaturation and proteinase activity. AS-2, KOG, and QOG remarkably inhibited nitric oxide formation with IC50 values of 8.2, 13.3, and 12.6 μM, respectively, in RAW 264.7 cells. They also inhibited PGE2 production with IC50 values 19.8-23.7 μM. They showed anti-melanogenic effects reducing tyrosinase activity (IC50 values 29.6-112.5 μM) and melanin formation (IC50 values 30.8–164.4 μM) in B16F10 cells, and inhibiting mushroom tyrosinase (IC50 values 61.5-456.4 μg/ml). Conclusion: Taken together, major components of alpinia leaf could be utilized as a potent herbal drug and food supplement with therapeutic prospects against inflammatory disorders and hyperpigmentation. Abbreviations used: HPLC: High performance liquid chromatography; DK: 5,6-dehydrokawain; DDK: Dihydro-5,6-dehydrokawain; AS-2: (E)-5-methoxy-8-(4-methoxy-2-oxo-2H-pyran-6-yl)-7-phenyl-1-styryl-2-oxabicyclo[4.2.0]oct-4-en-3-one; KOG: Kaempferol 3-O-β-D-glucuronide; QOG: Quercetin 3-O-β-D-glucuronide; PGE2: Prostaglandin E2; PAK1: RAC/CDC42-activated kinase 1; UV: Ultra violet; α-MSH: α-Melanocyte-stimulating hormone; COX-2: Cyclooxygenase-2; iNOS: Inducible Nitric Oxide Synthase; PDGF: Platelet Derived Growth Factor; MITF: Microphthalmia-Associated Transcription Factor; TRP: Tyrosinase Related Protein; ATCC: American Type Culture Collection; DMEM: Dulbecco's Modified Eagle Medium; FBS: Fetal bovine serum; CS: Newborn calf serum; MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide; DMSO: Dimethyl sulfoxide; NO: Nitric oxide; LPS: Lipopolysaccharide; DMRT: Duncan's multiple range test; SPSS: Statistical Package for the Social Sciences.

Aminoquinoline Schiff Bases as Non-Acidic, Non-Steroidal, Anti-Inflammatory Agents

Inflammation is common localized condition which makes body reddened and swollen due to some injury or any infection. The commonly available drugs i. e. diclofenac, ibuprofen etc. in market against inflammation bear acid group which cause severe stomach disturbance in their prolong use. Thus, such issues required significant attention in term of introducing acid free new anti-inflammatory agents with enhance efficacy. In the present study, we screened a series of eighteen aminoquinoline Schiff bases for their anti-inflammatory activity. These compounds were tested for their inhibitory effect on intracellular reactive oxygen species (ROS) produced from phagocytes isolated from human whole blood. Among the synthetic analogs, (E)-4-((quinolin-5-ylimino)methyl)benzene-1,2,3-triol (5), (E)-1-(2,4-dimethoxyphenyl)-N-(quinolin-5-yl)methanimine (6), (E)-2,6-dimethoxy-4-((quinolin-5-ylimino)methyl)phenol (7), and (E)-4-((quinolin-3-ylimino)methyl)benzene-1,2,3-triol (15) were found to exhibit potent activity with IC50 values of 1.9 ± 0.9, 2.7 ± 0.5, 1.4 ± 0.1, and 2.4 ± 0.1 μg/mL, respectively. Ibuprofen with IC50 value of 2.5 ± 0.6 μg/mL has been used standard in this assay. Cytotoxicity of these compounds was also tested against rat fibroblast cell line (3T3 cell line). The synthetic aminoquinoline Schiff bases were found to be non-toxic in cellular model except trihydroxy derivative 5. The active compounds can serve as potential leads for new anti-inflammatory drugs.

Gadolinium-Doped Gallic Acid-Zinc/Aluminium-Layered Double Hydroxide/Gold Theranostic Nanoparticles for a Bimodal Magnetic Resonance Imaging and Drug Delivery System.

We have developed gadolinium-based theranostic nanoparticles for co-delivery of drug and magnetic resonance imaging (MRI) contrast agent using Zn/Al-layered double hydroxide as the nanocarrier platform, a naturally occurring phenolic compound, gallic acid (GA) as therapeutic agent, and Gd(NO3)3 as diagnostic agent. Gold nanoparticles (AuNPs) were grown on the system to support the contrast for MRI imaging. The nanoparticles were characterized using techniques such as Hi-TEM, XRD, ICP-ES. Kinetic release study of the GA from the nanoparticles showed about 70% of GA was released over a period of 72 h. The in vitro cell viability test for the nanoparticles showed relatively low toxicity to human cell lines (3T3) and improved toxicity on cancerous cell lines (HepG2). A preliminary contrast property test of the nanoparticles, tested on a 3 Tesla MRI machine at various concentrations of GAGZAu and water (as a reference) indicates that the nanoparticles have a promising dual diagnostic and therapeutic features to further develop a better future for clinical remedy for cancer treatment.

Structure and intracellular antioxidant activity of pectic polysaccharide from acerola (Malpighia emarginata)

Malpighia emarginata is a tropical fruit plant, found naturally in the Caribbean islands and South America that produces an edible fruit known as acerola or Barbados Cherry. Its polysaccharides were obtained by aqueous extraction, subjected to a freezing and thawing process and ultrafiltration. A homogeneous fraction (ACWS-01E) was analyzed by sugar composition, HPSEC, methylation and NMR spectroscopy analyses. The results showed an arabinan-rich pectic polysaccharide, with 6.1×104g/mol and formed mainly by a high methyl esterified (DM=86%) homogalacturonan and branched arabinan. This latter is anchored in type I rhamnogalacturonan regions. The main chain of arabinan consisted of (1→5)-linked α-Araf, branched only at O-3. The potential ACWS-01E intracellular antioxidant activity against H2O2-induced oxidative stress in murine fibroblast cell line (3T3) was determined by DCFH-DA assay. The treatment with ACWS-01E significantly reduced H2O2-induced cytotoxic effect and the levels of reactive oxygen species (ROS). These findings suggested that ACWS-01E protected and improved NIH 3T3 cell viability from H2O2-induced toxicity by decreasing intracellular levels of ROS.

One-Pot Aqueous Synthesization of Near-Infrared Quantum Dots for Bioimaging and Photodynamic Therapy of Gliomas.

As the early detection and total destruction of gliomas are essential for longer survival, we attempted to synthesize a quantum dot (QD) that is capable of recognizing glioma cells for imaging and photodynamic therapy. Using a one-pot aqueous approach, near infrared-emitting CdTe was produced. After detection of its physicochemical characteriistics, it was conjugated with RGD. The emission images were observed with confocal microscopy. To test its toxicity, CdTe-RGD at various concentrations was separately added to a human glioma cell line (U251) and a mouse embryo fibroblast cell line (3T3) (control) for incubation in dark conditions. To test its photodynamic effect, the U251 and 3T3 cells were then irradiated for 5-60 min, using a 632.8-nm laser. This QD (Φ = 3.75 nm, photoluminescence (PL) peak wavelength = 700 nm, photoluminescence quantum yield (PLQY) = 20 %), was a spherical crystal with excellent monodispersity. Under a confocal microscope, U251 cells were visualized, but not the 3T3 cells. In dark conditions, the survival rates of both U251 and 3T3 cells were above 85 %. After laser irradiation, the survival rate of U251 cells decreased to 37 ± 1.6 % as the irradiation time and the CdTe-RGD concentration were increased. With good physicochemical characteriistics and low toxicity, this QD-RGD has broad prospects for use in the biomedical imaging and photodynamic therapy of gliomas.

Cytotoxicity of Etch-and-Rinse, Self-Etch, and Universal Dental Adhesive Systems in Fibroblast Cell Line 3T3.

The aim of this study was to evaluate in fibroblast cultures the direct cytotoxic effects of etch-and-rinse, self-etch, and universal adhesive systems. The sterile glass cover slips (n = 3) were then immersed in culture medium to obtain the eluates for the experimental groups: (1) Adper™ Single Bond 2; (2) Ambar; (3) Adper™ Scotchbond™ Multi-Purpose; (4) Scotchbond™ Universal; (5) Ambar Universal; and (6) OptiBond All-In-One. As a negative control, sterile glass cover slips were immersed in culture medium only. After 24 h, the eluate obtained was applied on fibroblast culture. Cell viability and cell morphology were evaluated by MTT assay and SEM, respectively. Data were analyzed by Kruskal–Wallis and Mann–Whitney tests (α = 0.05). All adhesive systems except universal reduced cell viability in 3T3 cells to between 26.04% and 56.57%, and Scotchbond Universal and Ambar Universal reduced cell viability to 2.13% and 3.57%, respectively, when compared to the negative control. Cytoplasmic membrane shrinkage and cell-free areas with residual membrane fragments from dead cells were observed. In conclusion, improvements in universal adhesive system formulations and their mechanisms of action are not accompanied by increased toxicity compared with those in other systems, warranting commitment to the use of these dentin-pulp complexes.

Cell division cycle 7-kinase inhibitor PHA-767491 hydrochloride suppresses glioblastoma growth and invasiveness.

BackgroundGenomic instability is a hallmark of cancer cells, and this cellular phenomenon can emerge as a result of replicative stress. It is possible to take advantage of replicative stress, and enhance it in a targeted way to fight cancer cells. One of such strategies involves targeting the cell division cycle 7-related protein kinase (CDC7), a protein with key roles in regulation of initiation of DNA replication. CDC7 overexpression is present in different cancers, and small molecule inhibitors of the CDC7 have well-documented anti-tumor effects. Here, we aimed to test the potential of CDC7 inhibition as a new strategy for glioblastoma treatment.MethodsPHA-767491 hydrochloride was used as the CDC7 inhibitor. Two glioblastoma cell lines (U87-MG and U251-MG) and a control cell line (3T3) were used to characterize the effects of CDC7 inhibition. The effect of CDC7 inhibition on cell viability, cell proliferation, apoptosis, migration, and invasion were analyzed. In addition, real-time PCR arrays were used to identify the differentially expressed genes in response to CDC7 inhibition.ResultsOur results showed that CDC7 inhibition reduces glioblastoma cell viability, suppresses cell proliferation, and triggers apoptosis in glioblastoma cell lines. In addition, we determined that CDC7 inhibition also suppresses glioblastoma cell migration and invasion. To identify molecular targets of CDC7 inhibition, we used real-time PCR arrays, which showed dysregulation of several mRNAs and miRNAs.ConclusionsTaken together, our findings suggest that CDC7 inhibition is a promising strategy for treatment of glioblastoma.Electronic supplementary materialThe online version of this article (doi:10.1186/s12935-016-0364-8) contains supplementary material, which is available to authorized users.

Cytotoxic cardiac glycosides from the fruit (pods) of Adenium obesum (Forssk.) Roem. & Schult

Phytochemical investigation of methanolic extract of Adenium obesum led to the isolation of 42 (1–42) compounds belongs to cardiac glycosides, triterpenoids and steroids. The chemical structures of isolated compounds were elucidated by spectral techniques UV, IR, NMR and FAB MS. The cardiac glycosides were tested against three human cell lines, 3T3 (normal cells), HeLa (Human cervical cancer cell lines) and PC-3 (Human prostate cancer cell lines). The cardiac glycoside, honghelin (4), obeside B (5) and obeside C (6) showed significant effects against cell lines Hela, 3T3 and PC-3 compared to standard drug doxorubicin. Compounds 4, 5 and 6 exhibited very low IC50 (μM) against the PC3 human cell line. 4 and 6 also showed least IC50 against the HeLa human cell lines as compared to the standard drug doxorubicin whereas these three compounds showed effect on 3T3 cell line with high IC50 values compared to drug cycloheximide.

A magnetic-dependent protein corona of tailor-made superparamagnetic iron oxides alters their biological behaviors

In recent years, it is becoming increasingly evident that once nanoparticles come into contact with biological fluids, a protein corona surely forms and critically affects the biological behaviors of nanoparticles. Herein, we investigate whether the formation of protein corona on the surface of superparamagnetic iron oxides (SPIOs) is influenced by static magnetic field. Under static magnetic field, there is no obvious variation in the total amount of protein adsorption, but the proportion of adsorbed proteins significantly changes. Noticeably, certain proteins including apolipoproteins, complement system proteins and acute phase proteins, increase in the protein corona of SPIOs in the magnetic field. More importantly, the magnetic-dependent protein corona of SPIOs enhances the cellular uptake of SPIOs into the normal cell line (3T3 cells) and tumor cell line (HepG2 cells), due to increased adsorption of apolipoprotein. In addition, SPIOs with the magnetic-dependent protein corona cause high cytotoxicity to 3T3 cells and HepG2 cells. This work discloses that superparamagnetism as a key feature of SPIOs affects the composition of protein corona to a large extent, which further alters the biological behaviors of SPIOs.

A new 5-alkylresorcinol glucoside derivative from Cybianthus magnus

One new 5-alkylresorcinol glucoside (1) was isolated from leaves of Cybianthus magnus, along with 12 known compounds, isolated from four plants belonging to Myrsinaceae family (2, 3 isolated from C. magnus; 4–7, 10 and 11 isolated from Myrsine latifolia; 4, 8 and 9 isolated from Myrsine sessiflora; 6, 7, 10, 12 and 13 isolated from Myrsine congesta). Their structures were determined on the basis of spectroscopic analysis and by comparison of their spectral data with those reported in the literature. So far, only nine 5-alkylresorcinol glucosides were isolated from leaves of Grevillea robusta. Since resorcinols are known to exhibit strong cytotoxic activity, compounds 1 and 2 were tested against cell lines 3T3, H460, DU145 and MCF-7 for cytotoxicity in vitro and compounds 3–13 were tested for their antileishmanial activity. Compound 2 displayed a strong cytotoxic activity with IC50 values ranging between 22 and 100 μM for all tested cell lines. Compounds 3–13 were not active against Leishmania amazonensis amastigotes.

P192. Small hairpin RNA against PMP22 is effective in vitro but fails to improve the phenotype of a CMT1A rat model in vivo

CMT1A is the most common form of hereditary neuropathies, accounting for about 30–40% of all patients. A causative treatment is not available as of yet. CMT1A is based on a duplication of the gene PMP22. Thus, lowering PMP22 expression represents a promising avenue for treatment studies. In this pilot study, we used plasmid-vector encoded shRNA against PMP22 for posttranscriptional silencing of PMP22 in vitro and in vivo. Cell lines 3T3, HEK 293, and MSC80 (Schwann cell-derived) were used to test the effects of PMP22-shRNA in vitro. In vitro assays confirmed knockdown of PMP22 mRNA and protein by PMP22-shRNA. The CMT1A rat model carrying a PMP22-transgene (CPMP rats) were injected with PMP22-shRNA in vivo. Concecutively, we were able to detect the construct in the peripheral nerves by PCR for up to 7 days after injection. However, shRNA injections did not significantly knock-down PMP22 mRNA or protein in peripheral nerves. Functional and behavioral tests as well as nerve conduction studies did not show significant improvements in PMP22-shRNA versus scramble-shRNA or NaCl treated rats. In conclusion, the shRNA constructs in this study were effective in reducing PMP22 in vitro, but not in vivo with the treatment protocol used. Likewise, a functional benefit could not be achieved (Fig. 1).

Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2.

Due to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design of ATP-competitive inhibitors of human CK2. In the present study, we prepared twenty-one indeno[1,2-b]indole derivatives, all of which were tested in vitro on human CK2. The indenoindolones 5a and 5b inhibited human CK2 with an IC50 of 0.17 and 0.61 µM, respectively. The indeno[1,2-b]indoloquinone 7a also showed inhibitory activity on CK2 at a submicromolar range (IC50 = 0.43 µM). Additionally, a large number of indenoindole derivatives was evaluated for their cytotoxic activities against the cell lines 3T3, WI-38, HEK293T and MEF.

Synthesis of phenyl thiazole hydrazones and their activity against glycation of proteins

Phenyl thiazole hydrazone derivatives 1–21 have been synthesized and screened for their in vitro antiglycation activity. Hydrazones 1–21 displayed assorted antiglycation activities having IC50 values in the range of 187.61 ± 1.12–886.98 ± 5.29 µM as compared to standard rutin (IC50 = 269.07 ± 3.79 µM). Compounds 5 (IC50 = 187.61 ± 1.12 µM), 3 (IC50 = 191.92 ± 3.08 µM), 4 (IC50 = 193.77 ± 3.06 µM), 6 (IC50 = 217.90 ± 2.48 µM), 15 (IC50 = 221.98 ± 2.34 µM), 2 (IC50 = 226.59 ± 1.19 µM), 21 (IC50 = 229.67 ± 1.95 µM), 18 (IC50 = 231.09 ± 0.38 µM), 12 (IC50 = 242.94 ± 2.05 µM), and 1 (IC50 = 264.22 ± 5.60 µM), respectively, showed excellent antiglycation activities superior to standard rutin. Compound 17 (IC50 = 269.94 ± 1.11 µM) demonstrated a comparable activity to the standard. Compounds 7, 8, 9, 10, 11, 13, 14, and 16 exhibited weaker activities than standard. However, compounds 19 and 20 showed no activity. When evaluated for cytotoxicity against rat fibroblast cell line (3T3 cell line), all compounds were found to be non-toxic in cellular model.

Experimental self-etching HEMA-free adhesive systems: cytotoxicity and degree of conversion.

The aim of this study was to evaluate the effect of replacing 2-hydroxyethyl methacrylate (HEMA) by methacrylate surfactant monomers on the cytotoxicity and degree of conversion of two-step self-etching dentin adhesive systems. Five HEMA-free adhesive systems were tested: Bis-EMA 10, Bis-EMA 30, PEG400, PEG400UDMA, PEG1000, and a HEMA group was used as positive control. The cytotoxicity of the experimental primers, with different monomer concentrations (2 or 20wt%), and bond resins, containing 25wt% surfactant, was assessed using murine fibroblast cell line 3T3 and the tetrazolium assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT)). The degree of conversion of the bond resins was analyzed using Fourier transform infrared spectroscopy. The data were submitted to statistical analysis using level of significance set at P<0.05. The PEG 1000 group obtained higher cell viability in comparison with HEMA in the 2% primer. The cell survival rate using 20% primer showed that PEG1000 and BIS-EMA 10 were less cytotoxic than HEMA. With regard to the eluate from bond resin, the data showed that the groups BIS-EMA 10, BIS-EMA 30 and PEG400UDMA were less cytotoxic than HEMA. No statistically significant difference was found among degrees of conversion of the experimental groups and HEMA. PEG 1000, BIS-EMA 10 and 30 monomers showed the biological potential for use in new adhesive system formulations since they showed lower cytotoxicity and similar degree of conversion when compared with the HEMA-containing group.

Antiglycation activity of quinoline derivatives- a new therapeutic class for the management of type 2 diabetes complications.

We report here a new class of compounds, quinoline derivatives, as potential inhibitors of in vitro bovine serum albumin-methylglyoxal glycation. Among compounds 1-19, compound 14 was found to be the most active analog with IC₅₀ of 282.98 ± 8.4 µM. Compounds 12 (IC₅₀ = 661.78 ± 8.7 µM) and 15 (IC₅₀ = 629.43 ± 7.85 7 µM) were also identified as modest inhibitors, in comparison to the standard inhibitor, rutin (IC₅₀ = 294.50 ± 1.5 µM). When evaluated for antioxidant activity through in vitro DPPH radical scavenging assay, compounds 3 (IC₅₀ = 2.19 ± 0.27 µM), 6 (IC₅₀ = 7.35 ± 2.27 µM), 11 (IC₅₀ = 8.96 ± 0.56 µM), and 12 (IC₅₀ = 10.11 ± 2.03 µM), and 15 (IC₅₀ = 7.01 ± 3.87 µM) were found to be more active than the standard i.e. gallic acid (IC₅₀ = 23.34 ± 0.43 µM). These compounds were also evaluated for cytotoxicity against rat fibroblast cell line (3T3 cell line). All compounds were found to be non-toxic in cellular model. This study identifies quinoline derivatives as a new class of inhibitors of protein glycation in vitro, along with antioxidant and non-toxic nature. These properties make them interesting leads for further studies as potential anti-diabetic agents.