Synthesis and antibacterial activity studies in vitro of indirubin-3'-monoximes.

Multi-drug-resistant microbial pathogens are a serious global health problem. New compounds with antibacterial activity serve as good candidates for developing novel antibacterial drugs which is very urgent and important. In this work, based on the unique scaffold of indirubin, an active ingredient of traditional Chinese medicine formulation Danggui Luhui Wan, we synthesized 29 indirubin-3'-monoximes and preliminarily evaluated their antibacterial activities. The antibacterial activity results demonstrated that the synthesized indirubin-3'-monoximes 5a-5z and 5aa-5ad displayed good potency against S. aureus ATCC25923 (MIC = 0.4-25.6 µg mL-1). Among them, we found that the 5-F, 5-Cl and 7-CF3 substituted indirubin-3'-monoximes 5r, 5s and 5aa also showed better antibacterial efficiency for S. aureus (MICs up to 0.4 µg mL-1) than the prototype natural product indirubin (MIC = 32 µg mL-1). More importantly, indirubin-3'-monoxime 5aa has certain synergistic effect with levofloxacin against clinic multidrug-resistant S. aureus (fractional inhibitory concentration index: 0.375). In addition, relevant experiments including electron microscopy observations, PI staining and the leakage of extracellular potassium ions and nucleic acid (260 nm) have been performed after treating S. aureus with indirubin-3'-monoxime 5aa, and the results revealed that indirubin-3'-monoximes could increase the cell membrane permeability of S. aureus. Although indirubin-3'-monoxime 5aa showed some cytotoxicity toward SH-SY5Y cells relative to compounds 5r and 5s, the skin irritation test of male mice after shaving showed that compound 5aa at a concentration of 12.8 µg mL-1 had no toxicity to mouse skin, and it could be used as a leading compound for skin antibacterial drugs.

Analysis of the water-soluble polysaccharides from Camellia japonica pollen and their inhibitory effects on galectin-3 function.

Pollen has been defined as dietary supplement used to supplement the diet in many countries, but the primary structure and activity of Camellia japonica pollen polysaccharide remain unclear. In this study, the water-soluble polysaccharide extracted from Camellia japonica pollen (WCPP) was fractionated into one neutral fraction (WCPP-N) and two acidic fractions (WCPP-A1 and WCPP-A2) by DEAE-cellulose column, and WCPP-A2 was further fractionated into two homogeneous sub-fractions (WCPP-A2a and WCPP-A2b) by Sepharose CL-6B column. Monosaccharide composition results showed that WCPP-N might mainly contain starch-like glucan as well as some arabinogalactan, while WCPP-A1, WCPP-A2 and its sub-fractions might mainly composed of rhamnogalacturonan I (RG-I) pectic polysaccharide domain backbone with some different types of side chains, including arabinan, galactan, and/or arabinogalactan. The primary structure analysis of WCPP-A2a by NMR spectra analysis suggested that WCPP-A2a was an RG-I-like pectic polysaccharide, branched at the O-4 of Rha residues in the backbone, with α-(1 â†’ 3,5)-L-arabinan as well as type-II arabinogalactan side chain to which were attached. The results of galectin-3-mediated hemagglutination assay indicated that WCPP-A2a exhibited the strongest inhibitory effect on galectin-3 with MIC value around 0.27 µg/mL. These results suggested the potential use of Camellia japonica pollen polysaccharide as a galectin3 inhibitor in functional foods.

[Blood lead status and influencing factors among preschool children in urban areas of China].

OBJECTIVE: To investigate the blood lead status and influencing factors among preschool children in the sampling city. METHOD: Stratified-clustered-random sampling was used. Standardized questionnaire and peripheral blood samples were obtained from 69 968 children aged 0-6 years in fixed kindergartens and communities of Yinchuan, Xi'an, Chengdu, Wuhan, Hefei, Beijing, Harbin, Zhengzhou, Huhhot, Shijiazhuang, Haikou, Dalian, Qingdao, Guangzhou, Nanning and Changsha from 2004 to 2008, respectively. Tungsten atomic absorbtion spectrophotometry was employed to determine the blood lead level of children. RESULT: The proportion of children with blood lead level ≥ 100 µg/L was 7.57% (among which the proportion of high blood lead level, mild lead poisoning, moderate lead poisoning, severe lead poisoning were 91.0%, 2.76%, 3.32%, 2.93%, respectively) and the blood lead level was lower than those of the past studies. The proportion of high blood lead level has steadily declined from 2004 to 2008 [the proportions were 10.03%, 7.85%, 7.40%, 6.91% and 4.78%, respectively (χ(2) = 297.36, P < 0.0001)]. The proportion of children with blood lead level ≥ 100 µg/L in Haikou, Zhengzhou, Guangzhou, Shijiazhuang, Changsha, Xi'an, Wuhan, Hefei, Chengdu, Yinchuan, Harbin, Beijing, Dalian, Huhhot, Nanning and Qingdao were 12.15%, 10.49%, 10.37%, 9.69%, 9.53%, 9.46%, 9.40%, 8.50%, 7.99%, 7.98%, 7.51%, 6.10%, 3.25%, 2.89%, 2.46% and 2.39%, respectively (χ(2) = 768.21, P < 0.0001). By multiple regression method, the risk factors which influenced blood lead status of children were education status of mother, older children, behavior and dietary habit of children, boy, stay for long time in traffic busy areas, the type of housing, taking traditional Chinese and herbal medicine. The protective factors against lead poisoning in children mainly included scattered living, the nutritional status of calcium, iron, zinc, frequent intake of milk, and older mother. CONCLUSION: The blood lead level of children has decreased, but is still higher than those in developed countries. Lead exposure remains a public health issue which affects children most. The blood lead level of children is affected by multiple factors. Government and the whole society should pay attention to interrupt the lead pollutant and to promote nutritional health education. With all these efforts, it is possible to stop the progress of lead exposure and reduce its hazardous effects on the growth and development of children.

Blood lead status and influencing factors among preschool children in urban areas of China / 中华儿科杂志

<p><b>OBJECTIVE</b>To investigate the blood lead status and influencing factors among preschool children in the sampling city.</p><p><b>METHOD</b>Stratified-clustered-random sampling was used. Standardized questionnaire and peripheral blood samples were obtained from 69 968 children aged 0-6 years in fixed kindergartens and communities of Yinchuan, Xi'an, Chengdu, Wuhan, Hefei, Beijing, Harbin, Zhengzhou, Huhhot, Shijiazhuang, Haikou, Dalian, Qingdao, Guangzhou, Nanning and Changsha from 2004 to 2008, respectively. Tungsten atomic absorbtion spectrophotometry was employed to determine the blood lead level of children.</p><p><b>RESULT</b>The proportion of children with blood lead level ≥ 100 µg/L was 7.57% (among which the proportion of high blood lead level, mild lead poisoning, moderate lead poisoning, severe lead poisoning were 91.0%, 2.76%, 3.32%, 2.93%, respectively) and the blood lead level was lower than those of the past studies. The proportion of high blood lead level has steadily declined from 2004 to 2008 [the proportions were 10.03%, 7.85%, 7.40%, 6.91% and 4.78%, respectively (χ(2) = 297.36, P < 0.0001)]. The proportion of children with blood lead level ≥ 100 µg/L in Haikou, Zhengzhou, Guangzhou, Shijiazhuang, Changsha, Xi'an, Wuhan, Hefei, Chengdu, Yinchuan, Harbin, Beijing, Dalian, Huhhot, Nanning and Qingdao were 12.15%, 10.49%, 10.37%, 9.69%, 9.53%, 9.46%, 9.40%, 8.50%, 7.99%, 7.98%, 7.51%, 6.10%, 3.25%, 2.89%, 2.46% and 2.39%, respectively (χ(2) = 768.21, P < 0.0001). By multiple regression method, the risk factors which influenced blood lead status of children were education status of mother, older children, behavior and dietary habit of children, boy, stay for long time in traffic busy areas, the type of housing, taking traditional Chinese and herbal medicine. The protective factors against lead poisoning in children mainly included scattered living, the nutritional status of calcium, iron, zinc, frequent intake of milk, and older mother.</p><p><b>CONCLUSION</b>The blood lead level of children has decreased, but is still higher than those in developed countries. Lead exposure remains a public health issue which affects children most. The blood lead level of children is affected by multiple factors. Government and the whole society should pay attention to interrupt the lead pollutant and to promote nutritional health education. With all these efforts, it is possible to stop the progress of lead exposure and reduce its hazardous effects on the growth and development of children.</p>