The structural (FTIR,XRD, and XPS) and biological studies of thermosensitive chitosan chloride gels with β‐glycerophosphate disodium

In this article, the properties of thermosensitive chitosan hydrogels (structural and biological) prepared using chitosan chloride and β‐glycerophosphate are presented. The porous structure of the gels was observed with a scanning electron microscopy (SEM). Rheological and other structural and morphological investigations were carried out by infrared spectroscopy and X‐ray photoelectron spectroscopy. Crystallinity of the gel was determined by X‐ray diffraction analysis. Biocompatibility of the chitosan gels was investigated by contact with bone cells (line Saos‐2) for 7 and 21 days. The cells were encapsulated and seeded onto the gel. A live/dead test showed no cytotoxic reaction. The structure of the gels, before and after the cell culture, was tested using SEM (including ESEM), to select the most suitable method of preparation and reliable visualization of the gel with cells. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135, 46459.     

Influence of microstructural characteristics on corrosion behavior of Mg–5Sn–3In alloy in Hank's solution

The microstructural observation, the mass loss test, potentiodynamic polarization measurements and corrosion morphology examinations were conducted to study the influence of microstructural characteristics on corrosion behavior of Mg–5Sn–3In alloys in Hank's solution after extrusion. The results show that the corrosion rate of the as-cast alloy is similar to that of as-extruded alloy; however, the local corrosion susceptibility is greatly weakened in the as-extruded alloy, especially in the extrusion direction. The relatively uniform corrosion morphology of the as-extruded alloy is attributed to refined Mg₂Sn particles, uniform distribution of Mg₂Sn particles and favorable crystal orientation. Meanwhile, the cytotoxicity tests confirm that the Mg–5Sn–3In alloy exhibits cytotoxicity of Grade 0–1 for NIH3T3 cells, suggesting an acceptable cytotoxicity of this alloy in the vitro assay.     

Chiral platinum(II) metallointercalators with potent in vitro cytotoxic activity

Four platinum(II) metallointercalating complexes of 1,10-phenanthroline (phen) with the chiral ancillary ligands trans-R,R- and trans-S,S-1,2-diaminocyclohexane (R,R- and S,S-dach, respectively), and N,N'-dimethyl-R,R- and N,N'-dimethyl-S,S-1,2-diaminocyclohexane (Me(2)-R,R-dach and Me(2)-S,S-dach, respectively) have been synthesised and characterised. The crystal structure of [Pt(Me(2)-S,S-dach)(phen)](ClO(4))(2)1.5 H(2)O (C(20)H(26)Cl(2)N(4)O(9.5)Pt) has been determined; orthorhombic, space group P2(1)2(1)2(1)(No. 19), a=23.194(8), b=25.131(9), c=8.522(3) A. In vitro cytotoxic assays (IC(50)) in the human bladder cancer cell line 5637 and in the murine leukemia L1210 cell line revealed that [Pt(S,S-dach)(phen)](ClO(4))(2) (0.091 and 0.13 microM, respectively) and [Pt(R,R-dach)(phen)](ClO(4))(2) (0.54 and 1.50 microM, respectively) were more cytotoxic than cisplatin (0.31 and 0.50 microM, respectively) and considerably more cytotoxic than their methylated counterparts, [Pt(Me(2)-R,R-dach)(phen)](ClO(4))(2) and [Pt(Me(2)-S,S-dach)(phen)](ClO(4))(2) (both>23 microM). Chiral discrimination for [Pt(S,S-dach)(phen)](ClO(4))(2) over its R,R-enantiomer was observed in all 13 cancer cell lines investigated. Moreover, [Pt(S,S-dach)(phen)](ClO(4))(2) was more active than cisplatin in all cell lines tested and shows only partial cross-resistance to cisplatin in two cisplatin resistant cell lines.     

Bio-screening of a few green seaweeds from India for their cytotoxic and antioxidant potential

BACKGROUND: It has been evidenced in several epidemiological studies that seaweeds when consumed as diet protect against several chronic oxidative stress‐related diseases. Seaweeds, raw, cooked, or dried, are used as food in many cultures, although not very popularly in India. Globally, several studies have indicated that seaweeds are a rich source of phenolic compounds and have antioxidant properties. In the present study, we screened methanolic extracts (MEs) of five species of green seaweeds commonly found in India for their cytotoxic activity by brine shrimp lethality assay and antioxidant properties using various in vitro assays, including 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) radical scavenging, reducing power and metal ion chelating assays. RESULTS: A markedly variable, dose‐dependent activity was observed in all the seaweed extracts relative to their total phenolic content. Statistical analysis indicated a significantly strong correlation between the DPPH radical scavenging activity and total phenolic content (R² = 0.88, P < 0.05) as well as reducing power and total phenolic content (R² = 0.99, P < 0.01) of the dry MEs. Also, a very poor correlation between total phenolic content and metal chelating activity (R² = 0.13, P > 0.05) was noted. None of the seaweed extracts were potently cytotoxic. CONCLUSION: The underlying results endorse seaweeds as a rich, novel source of antioxidant compounds needing systemic exploration. Copyright © 2011 Society of Chemical Industry     

Enhanced antibody-dependent cellular phagocytosis by chimeric monoclonal antibodies with tandemly repeated Fc domains

We previously reported that chimeric monoclonal antibodies (mAbs) with tandemly repeated Fc domains, which were developed by introducing tandem repeats of Fc domains downstream of 2 Fab domains, augmented binding avidities for all Fcγ receptors, resulting in enhanced antibody (Ab)-dependent cellular cytotoxicity. Here we investigated regarding Ab-dependent cellular phagocytosis (ADCP) mediated by these chimeric mAbs, which is considered one of the most important mechanisms that kills tumor cells, using two-color flow cytometric methods. ADCP mediated by T3-Ab, a chimeric mAb with 3 tandemly repeated Fc domains, was 5 times more potent than that by native anti-CD20 M-Ab (M-Ab hereafter). Furthermore, T3-Ab-mediated ADCP was resistant to competitive inhibition by intravenous Ig (IVIG), although M-Ab-mediated ADCP decreased in the presence of IVIG. An Fcγ receptor-blocking study demonstrated that T3-Ab mediated ADCP via both FcγRIA and FcγRIIA, whereas M-Ab mediated ADCP exclusively via FcγRIA. These results suggest that chimeric mAbs with tandemly repeated Fc domains enhance ADCP as well as ADCC, and that Fc multimerization may significantly enhance the efficacy of therapeutic Abs.     

Interaction of spherical silica nanoparticles with neuronal cells: size-dependent toxicity and perturbation of calcium homeostasis

The effects of St?ber silica nanoparticles on neuronal survival, proliferation, and on the underlying perturbations in calcium homeostasis are investigated on the well-differentiated neuronal cell line GT1-7. The responses to nanoparticles 50 and 200 nm in diameter are compared. The 50-nm silica affects neuronal survival/proliferation in a dose-dependent way, by stimulating apoptotic processes. In contrast, the 200-nm silica does not show any toxic effect even at relatively high concentrations (292 μg mL?1). To identify the mechanisms underlying these effects, the changes in intracellular calcium concentration elicited by acute and chronic administration of the two silica nanoparticles are analyzed. The 50-nm silica at toxic concentrations generates huge and long-lasting increases in intracellular calcium, whereas the 200-nm silica only induces transient signals of much lower amplitude. These findings provide the first evidence that silica nanoparticles can induce toxic effects on neuronal cells in a size-dependent way, and that these effects are related to the degree of perturbation of calcium homeostasis.     

A novel oleanolic acid-loaded PLGA-TPGS nanoparticle for liver cancer treatment

Objectives: Hepatocellular carcinoma is the third most common cause of cancer death. Oleanolic acid (OA) is a natural triterpenoid, has many important biological actions, including antitumor effect, but its poor solubility often leads to poor pharmacodynamics. The aim of our work is to make OA-loaded poly (lactide-co-glycolide)-d-α-tocopheryl polyethylene glycol 1000 succinate (PLGA-TPGS) nanoparticles (OPTN) to improve its efficacy to liver cancer and characterize it.

Methods: OPTN were prepared by ultrasonic emulsification-solvent evaporation technique using PLGA with or without the addition of TPGS (OPN). The coumarin-6-loaded nanoparticles were used as a fluorescence marker. The nanoparticles were characterized for surface morphology, surface charge, particle size, drug loading, encapsulation efficiency, in vitro drug-release, cellular uptake, cytotoxicity by human liver cancer cell line HepG2 cells, and therapeutic effect in vivo.

Key findings: The prepared nanoparticles were found to be spherical in shape. The in vitro drug-release profile of both nanoparticle formulations showed a biphasic release pattern. There was an increased level of uptake and cytotoxicity of OPTN in the HepG2 cells compared with that of OPN. The treatment of OPTN group was better than OPN and FS groups in vivo.

Conclusion: The results showed advantages of OPTN in terms of sustainable release and efficacy in liver cancer chemotherapy compared with OPN. OPTN could be acted as a novel and new dosage form to be used in cancer treatment study.     

PEGylated nanostructured lipid carriers (PEG–NLC) as a novel drug delivery system for biochanin A

With the aim to develop a lipid nanoparticle for biochanin A (BCA) by emulsion-evaporation and low temperature-solidification technique. The results revealed that BCA–PEG–NLC not only have small mean particle (148.5?±?2.88?nm) with narrow polydispersity index (PI) (0.153?±?0.01), encapsulation capacity (99.62?±?0.06%), payload (9.06?±?0.01%), zeta potential (?19.83?±?1.19?mV), but also slower release rate compared with BCA suspension over 48?h by the dialysis method (n=3). The crystallinity of lipid matrix within BCA–PEG–NLC was evaluated by differential scanning calorimetry (DSC) which verified the BCA successfully into the nanoparticles. Particularly, in pharmacokinetic, the BCA–PEG–NLC of C_max values and AUC (area under curve) was higher than BCA suspension (approximately 15.8 and 2.9 times, respectively), meanwhile, the mean residence time (MRT) was significantly longer. Furthermore, in vitro cytotoxicity BCA–PEG–NLC showed higher cytotoxicity against MCF-7 cell line compared with BCA suspension. This study suggested that PEG–NLC is a novel anti-cancer nanoparticle, which could provide attractive treatment for a wide variety of tumors and improved the oral bioavailability of poorly water-soluble drug.