Anticancer activity of bovine α‐lactalbumin treated with microbial transglutaminase

This study investigated the effects of bovine α‐lactalbumin (α‐La) treated with microbial transglutaminase on human cancer cells, cell cultures and growth rate assays. The anticancer activity for 10 mg/mL of bovine α‐lactalbumin (α‐La) was measured as ～90% in a human colorectal cancer cell line HCT 116. For the human bone cancer cell line SJSA‐1, α‐La hydrolysis resulted in higher cytotoxicity compared to untreated tumour cells. The formation of polymers of α‐La was suppressed by the addition of ethylenediaminetetraacetic acid, indicating that polymers of α‐La are promoted by metal ions such as Ca²⁺. The effect of α‐La on the morphology of SJSA‐1 cells was manifested as morphological changes compatible with apoptosis. Bovine milk α‐La with and without microbial transglutaminase is considered a valuable food ingredient and a nutraceutical for human health.     

Phenolic content, antioxidant, anti-inflammatory and anticancer activities of the edible halophyte Suaeda fruticosa Forssk

Suaeda fruticosa is an edible and medicinal halophyte known for its hypoglycaemic and hypolipidaemic activities. In this study, novel biological activities of the shoot extracts related to their phenolics were investigated. Results showed an appreciable total phenolic (31.8 mg GAE/g DW) in shoot extracts. The estimation of antioxidant capacities using oxygen radical absorbance capacity (ORAC method) and a cell based-assay (WS1) of four extracts (hexane, dichloromethane, methanol and water) showed that shoot methanol extract exhibit the highest antioxidant activities. The same extract displayed the utmost anti-inflammatory activity, inhibiting nitric oxide (NO) release, by 66.4% at 160 μg/ml in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Besides, the dichloromethane extract showed the highest anticancer activity against human lung carcinoma (A-549) and colon adenocarcinoma cell lines (DLD-1, Caco-2 and HT-29) with specificity against DLD-1 (IC₅₀ = 10 ± 1 μg/ml). These findings demonstrate the remarkable potentiality of this edible halophyte as valuable source of antioxidants which exhibit original and interesting anti-inflammatory and anticancer capacities.     

盐酸帕洛诺司琼的合成

合成新型5-HT3受体阻滞剂。以（S）-1,2,3,4-四氢-1-萘甲酸为起始原料,经酰化、缩合、还原、环合、成盐等反应合成盐酸帕洛诺司琼,总收率达36．2％。该法工艺操作简便,反应条件温和,适合工业化生产。     

The selective delivery of anticancer agents using target-sensitive liposomes

Target-sensitive (TG-S) liposomes having modified antibodies on their surface were employed to study the release of calcein and the selective delivery of the anticancer agents, doxorubicin (DOX) and methotrexate (MTX). The release of calcein from TG-S liposome occurred when the various target cells were contacted with liposomes and it was proportionally increased with the increase of antibody affinity to the target cells. Increasing the concentration of antigen molecules (major histocompatibility, MHC) on the surface of RMA-S, the release of calcein and drugs from TG-S liposomes contacting with RMA-S also rised. The destabilization of TG-S liposomes was only induced above a threshold density of surface antigen on the target cell membrane. The growth inhibition of specific target cells by the liposomal drugs was always stronger than that of the non-specific ones. For specific target cells, the IC₅₀ of liposomal DOX was about 2 times greater than that of free DOX, on the while, for non-specific target cells, more than 5 times. This indicates that the liposomal drugs were transferred preferentially to the specific target cells than the non-specific ones. Based on this phenomenon, the TG-S liposomal MTX were also applied for the selective elimination of the specific target cells in the mixed culture of specific and non-specific target cells.     

抗癌药氟他胺的合成研究

以高纯度间三氟甲基苯胺为原料，经异丁酰氯酰化，再在助剂S存在下进行硝化制得氟他胺。本法大大降低邻硝基异构体的含量，产品收率≥67.5％。     

Biological activities and health benefit effects of natural pigments derived from marine algae

The importance of marine algae as sources of functional ingredients has been well recognized due to their valuable health beneficial effects. Therefore, isolation and investigation of novel ingredients with biological activities from marine algae have attracted a great deal of attention. Among functional ingredients identified from marine algae, natural pigments (NPs) have received particular attention. These NPs exhibit various beneficial biological activities such as antioxidant, anticancer, anti-inflammatory, anti-obesity, anti-angiogenic and neuroprotective activities. This contribution focuses on biological activities of marine algae-derived NPs and emphasizing their potential applications in foods as well as pharmaceuticals areas.     

Anti‐inflammatory and anticancer activities of water‐soluble peptide extracts of buffalo and cow milk Cheddar cheeses

This article aimed to assess the anti‐inflammatory and anticancer potential of water‐soluble peptide (WSP) extracts from buffalo and cow milk Cheddar cheeses. Anti‐inflammatory activity was evaluated on the basis of nitric oxide (NO) production in lipopolysaccharide‐stimulated macrophage (RAW‐264.7) cells. A cell viability assay, cell cycle arrest and apoptosis were performed to explore anticancer activity in a colon cancer model (HT‐29). The WSP extracts of both Cheddar cheeses effectively inhibited NO production in activated macrophages. Maximum growth inhibition was observed in the HT‐29 cells at concentrations of 400 and 500 μg/mL. A significant increase in cell population at G₀/G₁ phase of the cell cycle was observed. Moreover, the WSP extracts also induced extensive apoptosis in colon cancer cells.