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In the peresent work, new aluminium complex from a Schiff base ligand was synthesized and characterized. The Schiff base ligand was derived from the condensation of 5-bromo-2-hydroxybenzaldehyde with 8-aminoquinoline. The synthesized compounds were characterized by elemental analyses, FTIR, and UV-Vis spectroscopy. Alumina nanomaterials were synthesized via thermal decomposition technique using aluminum Schiff base complex. The properties of the obtained nano alumina was studied by FTIR spectra. To investigate the phase formation, powder X-ray diffraction technique was used. Rietveld refinement using powder XRD confirms structure model determined by X-ray diffraction. SEM micrographs were used to investigate the morphology of the obtained material. Anticancer activity of these compounds on MKN-45 and LS174T cancer cell-lines was investigated by MTT assay. All compounds showed anticancer activity and have a very good inhibitory effect on the growth of cells. The cell viability decreased with the increasing concentrations of all compounds. Based on the results, it was found that the proliferation rate of cancer cells decreased after treatment with the compounds in a dose dependent way.

After dietary exposure, residues of multiple pesticides will enter human body and cause the potential health risk, which is always worse than that caused by single pesticide. The proliferation inhibition toxicity of abamectin, acetamiprid, carbendazim, chlorothalonil, chlorpyrifos, cyhalothrin, prochloraz and triazophos on HepG2 hepatocytes was determined by the classical MTT colorimetry. The result showed that the effects of different pesticide combinations on the survival rate of HepG2 cells were different after 24 h exposure. The combined toxicity of pesticide mixtures (comprised of two components, three components, four components, five components and six components) demonstrated two types of concentration-response curves towards proliferation inhibition HepG2 cells with the increase of pesticide concentrations. One type was a S type trend, with the increase of the concentration of pesticides, the cell survival rate first rapidly decreased, then slowly decreased. The followings are examples of this type: binary combination (carbendazim + cyhalothrin) at concentration of 0-10.00 mg/L, ternary combination (carbendazim + abamectin + cyhalothrin) at concentration of 0-24.12 mg/L, quaternary combination (triazophos + cyhalothrin + carbendazim + abamectin) at concentration of 0- 47.46 mg/L and five-component (chlorpyrifos + abamectin + acetamiprid + cyhalothrin + triazophos) at concentration of 0-62.80 mg/L. The other type was a linear trend, cell survival linearly decreased with the increase of the concentration of pesticides. The followings are examples of this type: binary combination (carbendazim + chlorothalonil) at concentration of 0-8.46 mg/L, ternary combination (chlorpyrifos + acetamiprid + carbendazim) at concentration of 0-39.97 mg/L, quaternary combined (carbendazim + cyhalothrin + chlorothalonil + abamectin) at concentration of 0-25.92 mg/L, and sixcomponent (acetamiprid + chlorpyrifos + triazophos + carbendazim + cyhalothrin + abamectin) at concentration of 0-57.48 mg/L. In this study, different combinations of pesticides showed different types of inhibition to the proliferation of human liver cancer cells, which provided a basis for the mechanism research and cumulative risk assessment of pesticide residues in the future. [ABSTRACT FROM AUTHOR]

Background and objective Screening of small-cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC) cell lines with gemcitabine hydrochloride (GEM) and cisplatin (CDDP) related to drug sensitivity gene might clarify the action mechanism of anti-cancer drugs and provide a new clue for overcoming drug resistance and the development of new anti-cancer drugs, and also provide theoretical basis for the clinical treatment of individual. Methods The drug sensitivity of CDDP and GEM in 4 SCLC cell lines and 6 NSCLC cell lines was determined using MTT colorimetric assay, while the cDNA macroarray was applied to detect the gene expression state related to drug sensitivity of 10 lung cancer cell line in 1 291, and the correlation between the two was analysized. Results There were 6 genes showing significant positive correlation (r≥0.632, P < 0.05) with GEM sensitivity; 45 genes positively related to CDDP; another 41 genes related to both GEM and CDDP (r≥± 0.4). Lung cancer with GEM and CDDP sensitivity of two types of drugs significantly related genes were Metallothinein (Signal transduction molecules), Cathepsin B (Organization protease B) and TIMP1 (Growth factor); the GEM, CDDP sensitivity associated genes of lung cancer cell lines mainly distributed in Metallothinein, Cathepsin B, growth factor TIMP1 categories. Conclusion There existed drug-related sensitive genes of GEM, CDDP in SCLC and NSCLC cell lines; of these genes, Metallothinein, Cathepsin B and TIMP1 genes presented a significant positive correlation with GEM drug sensitivity, a significant negative correlation with CDDP drug sensitivity.

A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives 5a – 5l , 7a – 7e and 9 have been synthesised and screened for in vitro antimycobacterial activity against Mycobacterium smegmatis MC-155. In addition these compounds have also been screened for cytotoxic activity against cancer cell lines HT-29, MDA-MB-231 by MTT colorimetric assay. The compounds are well characterized by spectral analysis viz. 1 H NMR, 13 C NMR, FT-IR, mass and HRMS. Screening results indicate that compounds 5g , 7a possess good antitubercular activity with MIC value 65.74 and 40.86, respectively, compounds 5g , 7a , 7b , 7d , 7e and 9 displayed promising cytotoxic activity against the cell lines tested. 5g and 7a stand out to be potent antimycobacterial and anticancer agents among the tested series. Further the title compounds were also tested on human normal cells HEK293T and are found to be safer with lesser cytotoxicity. It is interesting to observe that compound 5g has come out to be safer, potent anticancer and antimycobacterial agent. [ABSTRACT FROM AUTHOR]

Background To investigate the relationship between P-glycoprotein (Pgp), glutathione S-transferase π (GST-π) and topoisomerase II (Topo II) expression and human gastric cancer chemoresistance in vitro. Methods Primary single-cell suspensions were prepared from fresh specimens of primary gastric cancer and exposed to hydroxycamptothecin (HCPT), cisplatin (CDDP), 5-fluorouracil (5- FU), adriamycin (ADM) and mitomycin (MMC) for 48 h. Cell metabolic activity and rate of inhibition were evaluated using tetrazolium (MTT) assay. Pgp, GST-π and Topo II expression was determined in gastric carcinoma tissue samples using immunohistochemistry. Results Chemosensitivity of the gastric cancer cells varied; the rates of inhibition of cells exposed to HCPT, CDDP and 5-FU were significantly higher than that of cells exposed to ADM and MMC (p < 0.05). Gastric cancer cells with Pgp expression were resistant to ADM and HCPT (p = 0.008 and p = 0.011, respectively). Cells resistant to 5-FU, CDDP and MMC had significantly higher GST-π expression (p < 0.05). Topo II expression was significantly lower in cells resistant to HCPT, ADM and MMC (p < 0.05). Pgp and GST-π expression may contribute to primary resistance of gastric cancer cells to some chemotherapeutic drugs, while Topo II expression may indicate HCPT, ADM and MMC sensitivity. Conclusions Pgp, GST-π and Topo II detection and the MTT assay could be used as predictors in chemotherapeutic drug administration and for identifying drug resistance in gastric carcinoma. [ABSTRACT FROM AUTHOR]

Abstract: Jerdonitin is a P-II class snake venom metalloproteinase comprising metalloproteinase and disintegrin domains. In this study, we established a high-level expression system in Pichia pastoris and developed a purification strategy for the recombinant Jerdonitin. This recombinant Jerdonitin degraded fibrinogen at a level of activity comparable with its wild type. The effects of recombinant Jerdonitin on inhibiting ADP-induced human platelet aggregation were in a dose-dependent manner with an IC50 of 248nM. In addition, we reported here that Jerdonitin can significantly inhibit the growth of several cell lines, including human liver cancer cells (Bel7402), human leukemia cells (K562) and human gastric carcinoma cells (BGC823). This study offers recombinant Jerdonitin that will be valuable for further functional and structural studies of Jerdonitin. [Copyright &y& Elsevier]

Abstract: Cryopreserved human cardiac valve allografts could suffer lethal damages if the temperature is elevated during cryostorage. This work describes the functional and morphological alterations suffered by human cardiac valve allografts after a gradual increment of the cryostorage temperature from −147°C to −47°C due to a technical failure. Three experimental groups of human pulmonary and aortic allografts were compared: fresh, cryopreserved (−147°C) and cryopreserved with temperature changes from −147°C up to −47°C and back to −147°C. Fibroblast functionality was studied to asses the degree of valvular damages. Collagen network was also analyzed with bright light field and polarized microscopy; an immunohistochemistry for procollagen I was performed and the MTT colorimetric assay was used to evaluate fibroblast mitochondrial enzymatic activity. Porcine heart grafts valves were used to set the MTT colorimetric assay. With bright light field microscopy, disorganized collagen network was seen together with interstitial edema in cryopreserved groups. Polarized microscopy showed that fresh allografts had abundant collagen type I and III, cryopreserved group had less amount of collagen type I and in allografts that suffered cryopreservation temperature elevation collagen type I synthesis could not been demonstrated. Procollagen I was present in fibroblast cytoplasm of fresh group, but it was diminished in cryopreserved group and was absent in the group that suffered temperature elevation. Temperature changes during the cryopreservation period of human cardiac valve allografts induced fibroblast activity reduction. When the cryopreservation temperature is elevated during cryostorage, fibroblasts lost their functionality and the allografts may be not suitable for transplant. [Copyright &y& Elsevier]

The objective of this study is to propose a more accurate and faster MTT [3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyl tetrazolium bromide] colorimetric assay (MCA) for quantitative measurement of polypeptide bacteriocins in solutions with nisin as an example. After an initial incubation of nisin and indicator bacterium Micrococcus luteus NCIB 8166 in tubes, MTT was added for another incubation period. After that, nisin was quantified by estimating the number of viable bacteria based on measuring the amount of purple formazan produced by cleavage of yellow tetrazolium salt MTT. Then MCA was compared to a standard agar diffusion assay (ADA). The results suggested a high correlation coefficient ( r 2=0.975±0.004) between optical density (OD) and the inhibitory effect of nisin on a bacterial strain Micrococcus luteus NCIB 8166 at a range of 0.125∼32 IU/ml. The MCA described in this study was very quick. Quantification of nisin took only 7∼8 h and the detection limit was at the level of 0.125 IU/ml when compared to 12 IU/ml and 24∼28 h for ADA. The MCA provides an accurate and rapid method for quantification of nisin in solutions and is expected to be used for quantification of other antimicrobial substances. [ABSTRACT FROM AUTHOR]

To investigate the feasibility of chemosensitivity testing of antitumor drugs by flow cytometry in clinical applications so as to provide experimental and theoretical basis for the establishment of a novel antitumor drugs sensitivity testing and the screening of particular antitumor drugs. Detect the apoptosis rate of 12 cases of Molt-4 cell line, 57 cases of fresh clinical gastrointestinal tumor cells by Sub-G1 and Annexin V assay of flow cytometry under the effects of antitumor drugs at different times and the outcomes were compared with the ones of the MTT (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide) assay. The lethality of drugs on Molt-4 cell, clinical gastrointestinal tumor cells had a positive correlation with the acting time of antidrugs by employing Annexin V, Sub-G1 and MTT assay. Drug-incurring maximum lethality of Annexin V assay was higher than MTT colorimetric assay, that of Sub-G1 was lower than MTT assay, the virtual times of Annexin V and Sub-G1 assay were obviously earlier than that of MTT colorimetric assay. Annexin V and Sub-G1 assay of flow cytometry can be taken as potent protocols testing anti-tumor drug chemosensitivity. Annexin V assay is featured by more sensitive, concise, reliable compared with the classical chemosensitivity testing assay of MTT colorimetric assay and it possesses clinical applied value. [ABSTRACT FROM AUTHOR]

Abstract: Anthocyanidins, the aglycones of anthocyanins, impart brilliant colors in many fruits and vegetables. The widespread consumption of diets rich in anthocyanin and anthocyanidins prompted us to determine their inhibitory effects on human cancer cell proliferation. Five anthocyanidins, cyanidin (1), delphinidin (2), pelargonidin (3), petunidin (4) and malvidin (5), and four anthocyanins, cyanidin-3-glucoside, cyanidin-3-galactoside, delphinidin-3-galactoside and pelargonidin-3-galactoside were tested for cell proliferation inhibitory activity against human cancer cell lines, AGS (stomach), HCT-116 (colon), MCF-7 (breast), NCI H460 (lung), and SF-268 (Central Nervous System, CNS) at 12.5–200 μg/mL concentrations. The viability of cells after exposure to anthocyanins and anthocyanidins was determined by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) colorimetric methods. The anthocyanins assayed did not inhibit cell proliferation of cell lines tested at 200 μg/mL. However, anthocyanidins showed cell proliferation inhibitory activity. Malvidin inhibited AGS, HCT-116, NCI-H460, MCF-7 and SF-268 cell growth by 69, 75.7, 67.7, 74.7 and 40.5%, respectively, at 200 μg/mL. Similarly, pelargonidin inhibited AGS, HCT-116, NCI H460, MCF-7 and SF-268 cell growth by 64, 63, 62, 63 and 34%, respectively, at 200 μg/mL. At 200 μg/mL, cyanidin, delphinidin and petunidin inhibited the breast cancer cell growth by 47, 66 and 53%, respectively. This is the first report of tumor cell proliferation inhibitory activity by anthocyanidins. [Copyright &y& Elsevier]