This study evaluated the anti-inflammatory potential of a grasshopper ketone (GK) isolated from the brown alga Sargassum fulvellum on lipopolysaccharide (LPS)-induced RAW 264.7 murine macrophage cell line. GK was isolated and purified from the n-hexane fraction and its structure was verified on the basis of NMR spectroscopic data. GK up to 100 μg/ml is not cytotoxic to RAW 264.7, and is an effective inhibitor of LPS-induced NO production in RAW 264.7 cells. The production of pro-inflammatory cytokines, including IL-6, IL-1β, and TNF-α was found significantly reduced in 0.1-100 μg/ml dose ranges of GK treatment (p < 0.05). We confirmed the dose-dependent and significant inhibition of iNOS and COX-2 proteins expression. In addition, it has been shown that GK induces anti-inflammatory effects by inhibiting MAPKs (ERK, JNK, and p38) and NF-κB p65 phosphorylation. Our results show that the anti-inflammatory properties of GK may be due to the inhibition of the NF-κB and MAPKs pathways, which are associated with the attenuation of cytokine secretion.
Temozolomide (TMZ) is an alkylating chemotherapy agent used in the clinical treatment of glioblastoma multiforme (GBM) patients. Piperine (PIP) is a naturally occurring pungent nitrogenous substance present in the fruits of peppers. We investigated the anti-cancer efficacies of PIP alone and in combination with TMZ in GBM cellsusingparameters such as cell proliferation, cellular apoptosis, caspase-8/-9/-3 activities, cell cycle kinetics, wound-healing ability, and loss of mitochondrial membrane potential (MMP). Treatment with PIP and alow concentration of PIP-TMZ, inhibited cell growth, similar to TMZ.PIP-TMZ promoted apoptosis by activation of caspase-8/-9/-3, MMP loss, and inhibition of in vitro wound-healing motility. Reverse transcription polymerase chain reaction analysis showed significant inhibition of Cyclin-dependent kinases (CDK)4/6−cyclin D and CDK2−cyclin-E expression upon treatment with a low concentration PIP-TMZ, suggesting an S to G1 arrest. Our findings provide insight into the apoptotic potential of the combination of a low concentration of PIP-TMZ, though further in vivo study will be needed for its validation.
Well-defined amphiphilic gradient copolymers of poly(ethylene glycol) methyl ether methacrylate (PEGMA) and styrene were successfully synthesized using atom transfer radical polymerization. The relative reactivity ratio of PEGMA to styrene was determined using the Jaacks method. The initial feed ratio of the two monomers had a significant effect on the copolymer's gradient composition. The resultant copolymers were characterized by nuclear magnetic resonance and Fourier transform-infrared spectroscopy to confirm their structures and monomer compositions. The lower critical solution temperature behavior of the copolymers was investigated using ultraviolet-visual spectroscopy. The micellization behavior of the PEGMA and styrene copolymers in aqueous solution was observed by transmission electron microscopy and dynamic laser scattering.
This study investigated the characterization and functionality of Undaria pinnatifida root (UPT) extracts, degraded using a crude enzyme from Shewanella oneidensis PKA1008. To obtain the optimum degrading conditions, the UPT was mixed with alginate degrading enzymes from S. oneidensis PKA 1008 and was incubated at 30°C for 0, 3, 6, 12, 24, and 48 h. The alginate degrading ability of these enzymes was then evaluated by measuring the reducing sugar, viscosity, pH and chromaticity. Enzymatic extract at 24 h revealed the highest alginate degrading ability and the lowest pH value. As the incubation time increased, the lightness (L *) also decreased and was measured at its lowest value, 39.84, at 12 hours. The redness and yellowness increased gradually to 10.27 at 6 h and to 63.95 at 3 h, respectively. Moreover, the alginate oligosaccharides exhibited significant anti-inflammatory activity. These results indicate that a crude enzyme from S. oneidensis PKA 1008 can be used to enhance the polysaccharide degradation of UPT and the alginate oligosaccharides may also enhance the anti-inflammatory effect.
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