Insights of synthetic analogues of anti-leprosy agents

Today, the emergence of the phenomenon of drug or multidrug-resistance for community-associated diseases represents a major concern in the world. In these contexts, the chronic infectious disease, leprosy, grounded by a slow-growing bacterium called Mycobacterium leprae or Mycobacterium lepromatosis is a leading cause of severe disfiguring skin sores and nerve damage in the arms, legs, and skin areas around the body. Even, over 200,000 new leprosy cases are being accounted every year along with the relapsed leprosy cases. Nonetheless, this has been considered a curable disease with a higher dose of multidrug therapy (MDT) for a long period of time. The prolonged action of a high dose of combination drugs administration may cause an adverse reaction that can significantly affect patient compliance, particularly the outbreak of multidrug-resistance in the infected person. To overcome these shortfalls or prevent the resistance-associated problems, researchers are diligently involved in the structural modifications of the clinically used anti-leprosy drugs or the allied compounds for the structure-antimycobacterial activity relationship study. This review article described the detailed synthesis and biological assays of different anti-leprosy compounds reported by several research groups.     

湿热地区简单式屋顶绿化的截流雨水效应

城市内涝是困扰各大城市的环境问题,其主观原因是来自迅速增加的城市不透水面.国外运用屋顶绿化作为截留雨水的措施得到广泛实践,而屋顶绿化滞留雨水能力随气候条件的变化而变化.湿热气候区具有气温高、湿度高、雨量大的气候特点,在此气候条件下探讨屋顶绿化截留雨水的效能具有重要意义.本研究以在夏季雨热同期的广州市为例,搭建3个简单式屋顶绿化测试平台,通过13个月试验期的气象观测和数据测定推算其截留雨水的效能.结果表明: 基质厚度30、50和70 mm简单式屋顶绿化的降雨滞留率分别为27.2%、30.9%和32.1%,平均峰值减少量为18.9%、26.2%和27.7%.广州市建成区面积1035.01 km²,屋顶面积约占37.3%,假设在此区域推行30 mm厚度基质的屋顶绿化,小、中、大雨的总迟滞比率分别为72.8%、22.6%和17.4%,以此推算得出可滞留雨水体积达14317×10⁴ m³,说明简单式屋顶绿化的截留雨水效应具有巨大潜力.本研究结果可为湿热气候区城市缓解城市内涝、建设海绵城市的构想提供参考.     

Polymorphisms and phenotypic analysis of cytochrome P450 2D6 in the Tibetan population

The cytochrome P450 2D6 enzyme (CYP2D6) metabolizes about 25% of prescribed drugs in the endoplasmic reticulum, and genetic polymorphisms in CYP2D6 can greatly affect its activity and lead to differences among individuals in drug efficacy and adverse drug reactions. To investigate genetic polymorphisms in CYP2D6 among Tibetan Chinese, we directly sequenced the whole gene in 96 unrelated, healthy Tibetans from The Tibet Autonomous Region of China and screened for genetic variants in the promoter, exons, introns, and 3′UTR. We detected fifty-one genetic polymorphisms in CYP2D6, and 16 of them are novel. The allele frequencies of CYP2D6*1, *2, *5, *10, *41, and *49 were 0.25, 0.43, 0.02, 0.29, 0.02, and 0.01, respectively. The frequency of CYP2D6*10, a putative poor-metabolizer allele, was lower in our sample population compared with that in the Han Chinese population (p < 0.001). In addition, haplotype analysis allowed 15 CYP2D6 haplotypes to be classified into three groups. In conclusion, our results provide basic information about CPY2D6 alleles in Tibetans and suggest that the enzymatic activities of CYP2D6 may differ among the diverse ethnic populations of China. Our results provide a basis for safer drug administration and better therapeutic treatment among Tibetans.     

Small ruminant production in smallholder and pastoral/extensive farming systems in Kenya

A survey was conducted by way of personal interviews with 562 respondents comprising 459 farmers and 103 butchers/traders in selected districts in the central and western parts of Kenya, consisting of three predominantly smallholder and four predominantly pastoral/extensive districts. The study aimed to provide a better understanding of smallholder and pastoral/extensive sheep and goat farming systems in the tropics, by taking Kenya as an example. The results showed that 58% of the pastoral/extensive farmers and 46% of the smallholders indicated livestock as their main activity. Small ruminants ranked closely behind cattle in their importance. Thirty-four percent of the households kept only sheep, 18% only goats and 48% both species. The survey demonstrated the relative importance to the farmers of tangible benefits of farming sheep and goats (e.g., regular cash income, meat, manure and, in the case of goats, milk) versus intangible benefits (e.g., the role of small ruminants as an insurance against emergencies). Regular cash income and an insurance against emergencies were the highest priorities. Seventy-eight percent of the farmers reported animal sales over the previous 12 months of the survey date. Of these sales, the income was spent on school fees (32%), purchase of food (22%), farm investment (18%), medical expenses (10%), off-farm investment (9%), social activities (5%) and re-stocking (4%). Indigenous genotypes were predominant among the pastoralists and mixed crosses predominant among the smallholders. A range of traits: growth rate, body size, body shape, drought tolerance, meat quality, fertility, disease and heat tolerance, prolificacy and temperament were all considered important for both sheep and goats in both farming systems and across the different genotypes. Compared with other pure breeds, the Red Maasai sheep and the Small East African goats were rated poorly in terms of body size, body shape, growth and fertility, but highly in terms of drought and (for the Red Maasai) heat tolerance by both smallholder and pastoralist farmers. In general, crosses were perceived less favourably than indigenous pure breeds. Body size and performance ranked as the most important traits in the choice of breeding males. Approximately half the farmers inherited their males, reared them on the farm and kept them for an average of 2–3 years. Uncontrolled mating within the household's flock was predominant in both farming systems. Over 98% of the farmers reported incidence of disease, especially pneumonia (in pastoral/extensive areas), helminthosis, tick-borne diseases, diarrhoea and foot-rot. Over 95% of the farmers fed supplements in both dry and wet seasons. Pure exotic and indigenous × exotic genotypes fetched higher prices than indigenous genotypes due to their heavier body weight. In conclusion, the foregoing issues need attention in genetic improvement programmes, with more emphasis on the conservation and utilisation of indigenous small ruminant genotypes.     

毛竹种植对土壤细菌和真菌群落结构及多样性的影响

为揭示天然林改为毛竹林过程中土壤微生物变化规律,在浙江省湖州市安吉县和长兴县两地选择不同种植历史的粗放经营毛竹林,分层采集0～20和20～40 cm的混合土壤样品,应用PCR-DGGE技术分析土壤细菌和真菌群落结构及多样性变化.结果表明: 在马尾松林改种毛竹林或毛竹林入侵杂灌阔叶林形成毛竹纯林过程中,土壤细菌和真菌的群落结构均发生明显变化,且细菌结构对毛竹种植的响应更敏感;随着毛竹生长时间的延长,表层土壤细菌群落表现出抵抗干扰、最后向改种毛竹之前状态恢复的趋势.毛竹种植时间、样地和土层均对土壤细菌和真菌多样性产生显著影响,其中样地和土层的影响明显大于种植时间.土壤性质和细菌、真菌结构的冗余分析结果表明,不同地点、不同土层驱动土壤微生物结构随时间变化的主要因子没有一致规律,且第1、2轴对样地变化的解释率大多低于65.0%,说明除本研究分析的5个土壤化学指标外,可能还有其他土壤理化性质共同驱动微生物结构的变化.     

Measurement of conformational constraints in an elastin-mimetic protein by residue-pair selected solid-state NMR

We introduce a solid-state NMR technique for selective detection of a residue pair in multiply labeled proteins to obtain site-specific structural constraints. The method exploits the frequency-offset dependence of cross polarization to achieve ¹³CO_i ¹⁵N_i ¹³C_i transfer between two residues. A ¹³C, ¹⁵N-labeled elastin mimetic protein (VPGVG)_n is used to demonstrate the method. The technique selected the Gly3 C signal while suppressing the Gly5 C signal, and allowed the measurement of the Gly3 C chemical shift anisotropy to derive information on the protein conformation. This residue-pair selection technique should simplify the study of protein structure at specific residues.     

A thermodynamic view of networks

Networks can be described by the frequency distribution of the number of links associated with each node (the degree of the node). Of particular interest are the power law distributions, which give rise to the so-called scale-free networks, and the distributions of the form of the simplified canonical law (SCL) introduced by Mandelbrot, which give what we shall call the Mandelbrot networks. Many dynamical methods have been obtained for the construction of scale-free networks, but no dynamical construction of Mandelbrot networks has been demonstrated. Here we develop a systematic technique to obtain networks with any given distribution of the degrees of the nodes. This is done using a thermodynamic approach in which we maximise the entropy associated with degree distribution of the nodes of the network subject to certain constraints. These constraints can be chosen systematically to produce the desired network architecture. For large networks we therefore replace a dynamical approach to the stationary state by a thermodynamical viewpoint. We use the method to generate scale-free and Mandelbrot networks with arbitrarily chosen parameters. We emphasise that this approach opens the possibility of insights into a thermodynamics of networks by suggesting thermodynamic relations between macroscopic variables for networks.     

Does the liposuction method influence the phenotypic characteristic of human adipose-derived stem cells?

Adipose-derived stem cells (ASCs) possess a high differentiation and proliferation potential. However, the phenotypic characterization of ASCs is still difficult. Until now, there is no extensive analysis of ASCs markers depending on different liposuction methods. Therefore, the aim of the present study was to analyse 242 surface markers and determine the differences in the phenotypic pattern between ASCs obtained during mechanical and ultrasound-assisted liposuction. ASCs were isolated from healthy donors, due to mechanical and ultrasound-assisted liposuction and cultured in standard medium to the second passage. Differentiation potential and markers expression was evaluated to confirm the mesenchymal nature of cells. Then, the BD LyoplateTM Human Cell Surface Marker Screening Panel was used. Results shown that both population of ASCs are characterized by high expression of markers specific for ASCs: cluster of differentiation (CD)9, CD10, CD34, CD44, CD49d, CD54, CD55, CD59, CD71 and low expression of CD11a, CD11c and CD144. Moreover, we have noticed significant differences in antigen expression in 58 markers from the 242 studied. Presented study shows for the first time that different liposuction methods are not a significant factor which can influence the expression of human ASCs surface markers.