Camptothecin-Polysaccharide Co-assembly and Its Controlled Release.

ß-Cyclodextrin modified camptothecin (CPT-CD) was synthesized through esterification reaction and "click chemistry" to greatly improve the solubility of CPT in aqueous solution, and then, a supramolecular nanoparticle was constructed by strong noncovalent interaction between ß-cyclodextrin and adamantane and amphiphilic interaction by simply mixing CPT-CD and adamantane modified hyaluronic acid (HA-ADA) together. The obtained nanoparticle had a hydrophilic HA shell, which could target and recognize HA receptors overexpressed on the surface of cancer cells, and a hydrophobic CPT core, which could protect CPT from hydrolyzation. The results of cytotoxicity experiments showed that the nanoparticle we have designed in this work exhibited similar anticancer activities to, but with much lower side effects than, the commercial chemotherapeutic drug CPT in vitro. We believe that this work might provide a strategy for improving the treatment performance of CPT in laboratory and clinical settings.

Allyl halide induced electrochemical degradation of lignin into double-bonded phenolic monomers.

Lignin is one of the major macromolecule in nature that contains an aromatic ring structure, and also a potential source of high-value products such as biofuels and chemicals. However, Lignin is a kind of complex heterogeneous polymer which can produce many degradation products during processing or treatment. These degradation products are difficult to separate, making it challenging to use lignin directly for high-value applications. This study proposes an electrocatalytic method to degrade lignin by using allyl halides to induce double-bonded phenolic monomers, while avoiding separation. In an alkaline solution, the three basic structural units (G, S, and H) of lignin were transformed into phenolic monomers by introducing allyl halide, which could effectively expand lignin application space. This reaction was achieved using a Pb/PbO2 electrode as the anode and copper as the cathode. It was further confirmed that double-bonded phenolic monomers were obtained by degradation. 3-allylbromide has more active allyl radicals and significantly higher product yields than 3-allylchloride. The yields of 4-allyl-2-methoxyphenol, 4-allyl-2,6-dimethoxyphenol and 2-allylphenol could reach 17.21 g/kg-lignin, 7.75 g/kg-lignin, and 0.67 g/kg-lignin respectively. These mixed double-bond monomers can be used as monomer materials for in-situ polymerization without further separation, which lays the foundation for high value-added applications of lignin.

Celastrol Attenuates RANKL-Induced Osteoclastogenesis in vitro and Reduces Titanium Particle-Induced Osteolysis and Ovariectomy-Induced Bone Loss in vivo.

Excessive bone resorption by osteoclasts contributes significantly to osteoclast-related diseases such as periprosthetic osteolysis and osteoporosis. Osteolysis in a titanium particle-induced calvarial model and bone loss in an ovariectomized mice model occurred similarly to those in humans; thus, these models can be used to evaluate potential therapies for aseptic prosthetic loosening and osteoporosis. Celastrol, which is extracted from the seeds of the genus Tripterygium, has been thoroughly investigated for its anti-inflammatory and anti-cancer pharmacological effects. However, the mechanisms involving bone metabolism by which celastrol inhibits osteoclastogenesis are not yet fully understood. We demonstrated that celastrol inhibited the receptor activator of nuclear factor κB ligand-induced osteoclastogenesis and the bone resorptive function of osteoclasts in vitro by inhibiting the activation of transforming growth factor ß-activated kinase 1-mediated NF-κB and mitogen-activated protein kinase signaling pathways and downregulating osteoclastogenesis marker-related genes. Furthermore, celastrol was also shown to be beneficial in both the titanium particle-induced osteolysis calvarial and the murine ovariectomy-induced bone loss. Collectively, our results suggested that celastrol is promising for the prevention of aseptic prosthetic loosening and osteoporosis in the treatment of osteolytic diseases induced by disrupted osteoclast formation and function.

Elimination of Cr(VI) from chromium slag with poplar lignin by electrochemical treatment in sulfuric acid solution.

In this paper, we proposed a novel method to eliminate nocuous Cr(VI) from chromium slag with poplar lignin by electrochemical treatment in sulfuric acid solution. In this electrochemical process, self-made Ti/SnO2-Sb anode and graphite cathode were applied, and the oxidative degradation of lignin proceeded simultaneously with the reduction of Cr(VI) in one pot. The influences of pivotal factors on electrocatalytic redox efficiency were investigated, such as chromium slag concentration, lignin concentration, current density, sulfuric acid concentration, and reaction time. The results showed that the elimination rate of Cr(VI) in chromium slag was 97.16 ± 1.13% and the total yield of lignin degradation products reached 93.78 g/kg lignin under the optimal conditions. X-ray photoelectron spectroscopy (XPS), energy dispersive X-ray spectroscopy (EDS), and UV-visible spectrophotometer studies confirmed that most of the Cr(VI) ions were reduced to Cr(III) ions with the aid of lignin, and a small amount of Cr(VI) ions were adsorbed by lignin residue. Importantly, this method provides a typical example of "waste control by waste", which is treating waste chromium slag with waste lignin that can be an effective way to eliminate Cr(VI).

Enoxacin inhibits proliferation and invasion of human osteosarcoma cells and reduces bone tumour volume in a murine xenograft model.

Osteosarcoma is the most prevalent primary bone malignancy in children and adolescents. Neoadjuvant chemotherapy combined with surgical resection, the current standard treatment of osteosarcoma, is associated with a 5-year survival rate of only ~70%. Therefore, it is necessary to identify new, more effective treatment strategies for patients with this lethal disease. Enoxacin is a highly effective broad-spectrum fluoroquinolone antibiotic with low toxicity. The drug inhibits the growth and metastasis of numerous tumour types, but its efficacy has not been studied in osteosarcoma. This study assessed the antitumour effects of enoxacin in osteosarcoma 143B cells and in a murine tumour xenograft model. Enoxacin inhibited the proliferation, invasion and migration of 143B cells, as well as inducing their apoptosis. These effects were thought to be mediated by downregulation of Bcl-xL, Bxl-2, matrix metalloproteinase (MMP)2 and MMP9 expression. Enoxacin also significantly impaired the growth of bone tumours in nude mice without affecting their liver or kidney function, or blood cell count. Collectively, these results indicate that enoxacin is a promising new drug for osteosarcoma that warrants further evaluation in clinical studies.

Selective conversion of cotton cellulose to glucose and 5-hydroxymethyl furfural with SO4(2-)/MxOy solid superacid catalyst.

This paper presented a mild hydrothermal process for degradation of cotton cellulose with solid superacid catalyst and selective conversion of cotton cellulose to glucose and 5-hydroxymethyl furfural (HMF). Five kinds of solid superacid catalyst such as SO4(2-)/SnO2, SO4(2-)/TiO2, SO4(2-)/ZrO2, SO4(2-)/Fe2O3 and SO4(2-)/Al2O3 were prepared by impregnation method. The BET surface area of catalyst SO4(2-)/SnO2 was up to 118.8m(2)g(-1) when impregnation was performed with 1molL(-1) H2SO4 of impregnating solution at 550°C calcination temperature for 3h. It made the hydrothermal temperature of cellulose degradation decrease to 190°C successfully and suppressed the side reaction. The NH3-TPD profile of SO4(2-)/SnO2 indicated there was a wide region of stronger acid sites on the catalyst surface. The depolymerization of cotton cellulose obtained 11.0% yield and 22.0% selectivity of HMF and 26.8% yield and 53.4% selectivity of glucose, respectively. The regeneration and reuse of solid superacid catalyst were also discussed in this paper.

Direct conversion of cellulose to 1-(furan-2-yl)-2-hydroxyethanone in zinc chloride solution under microwave irradiation.

Conversion of cellulose to 1-(furan-2-yl)-2-hydroxyethanone has been demonstrated in concentrated zinc chloride solution under microwave irradiation. Compared with the conventional oil-bath heating mode, microwave irradiation significantly reduced the reaction time and increased the yield of 1-(furan-2-yl)-2-hydroxyethanone. A typical degradation reaction with cellulose produced 1-(furan-2-yl)-2-hydroxyethanone in 12.0% molar yield in ZnCl(2) solution (ZnCl(2)-H(2)O ratio=2.25:1, w/w) with microwave irradiation at 600 W for 5 minutes at 135°C.

[Expression of receptor activator of nuclear factor kappaB ligand and osteoprotegerin of mice osteoblast induced by metal ions].

OBJECTIVE: Lots of metal ions accumulation and over-expression of receptor activator of NF-kappaB ligand (RANKL) around the prosthesis could be found in revision of total hip arthroplasty. To investigate the relationship between metal ions and aseptic loosening by observing the effects of Co2+ and Cr3+ ions on the expression of RANKL and osteoprotegerin (OPG) from osteoblast. METHODS: Osteoblasts were cultured in vitro at the density of 1 x 10(5) cells/mL, and were divided into 2 groups according to different culture solutions. In control group, osteoblasts were cultured with normal medium without CoCl2 and CrCl3. In experimental group, osteoblasts were cultured with the medium including CoCl2 (10 mg/L) and CrCl3 (150 mg/L) solutions. The RT-PCR and ELISA methods were applied to detect the mRNA expression of RANKL and OPG and protein level at 24 and 48 hours after co-cultured, respectively. RESULTS: RT-PCR revealed that the mRNA expression of RANKL and OPG could be found in two groups at 24 and 48 hours after co-cultured, the expression was higher in the experimental group than in control group, especially the expression of RANKL, showing significant difference (P < 0.05). At 24 and 48 hours after co-cultured, the ratios of RANKL mRNA to OPG mRNA in the experimental group were 0.860 and 1.232, respectively, which were significantly higher than those in the control group (0.695 and 0.688, P < 0.05). ELISA revealed that the protein level of RANKL and OPG in experimental group were significantly higher than those in the control group (P < 0.05). CONCLUSION: Co2+ and Cr3+ can stimulate the mRNA expressions of RANKL, OPG and secretion of those protein from osteoblasts, especially increase of the RANKL, which promotes the formation and activation of osteoblasts and the generation of aseptic loosening.

[Inhibitory effect of curcumin on MMP-2 and MMP-9 expression induced by polyethylene wear particles and its mechanism].

OBJECTIVE: To observe the effect of different dosage of curcumin on expression of MMP-2 and MMP-9 in the tissue of cystiform in air-pouch mouse models after the injection of polyethylene wear particles, and to investigate its mechanism of intervening inflammatory response induced by wear particles. METHODS: Seventy-two kunming strain mice were used to establish air-pouch animal models by referring to the method of Yang et al. and injecting 3 mL suspension of ultra-high molecular weight polyethylene wear particles (concentration 1 x 10(8) cells/mL) into dorsal cyst cavity. Then the animals were randomized into 3 groups (n = 24 per group): group A (control group), 0.6 mL/day normal saline by gavage; group B (low-dosage experimental group), 0.6 mL/day curcumin solution at a concentration of 1.6 mg/mL by gavage; group C (high-dosage experimental group), 0.6 mL/day curcumin solution at a concentration of 3.2 mg/mL by gavage. General condition of the animals was observed after operation. The mice were killed 3, 7 and 14 days after operation (8 mice per group at a time), the tissue of cystiform was harvested to receive gross, histology and immunohistochemistry observation, as well as RT-PCR and Western blot detection. RESULTS: All mice survived till the end of experiment. White cystiform tissue was evident on the back of mice subcutaneously in each group. For diameter of the cyst cavity at each time point, group A was obviously greater than groups B and C, and group C was significantly less than group B. Microscope observation showed that inflammatory response in group A was stronger than that of groups B and C, and group C was obviously less than group B at 7 and 14 days. There was a significant difference between groups B and C and group A in terms of MMP-2 and MMP-9 expression at 7 and 14 days after curcumin delivery (P < 0.05), and no significant differences were evident at 3 days (P > 0.05). There was no significant difference between group B and group C in MMP-2 expression at 7 days after curcumin delivery (P > 0.05), and significant difference was evident at 14 days (P < 0.05). There was significant difference bewteen group B and group C in MMP-9 expression at 7 and 14 days after curcumin delivery (P < 0.05). Nuclear translocation of NF-kappaB P65 was inhibited remarkably after curcumin delivery, and there were significant differences among three groups at 7 and 14 days (P < 0.05), and no significant differences were evident at 3 days (P > 0.05). CONCLUSION: Ultra-high molecular weight polyethylene wear particles can stimulate expression of MMP-2 and MMP-9 in cystiform tissue. Curcumin can restrain expression of MMP-2 and MMP-9 in cystiform tissue of air-pouch animal models, and expression of MMP-2 and MMP-9 may be regulated by the activation of NF-kappaB.