GABAB 受体变构剂药学研究进展

Y-氨基丁酸B受体(GABAB receptor,GABABR)是最具有药理学意义的药物靶点之一,具有复杂而精细的激活机制.传统的GABABR靶点药物开发集中于激动剂和拮抗剂,这类药物受到多种因素的制约,包括较强的副作用、药物代谢困难、机体耐药性明显等.变构剂结合于正构位点之外,能够调节GABABR异源二聚体亚基或结构域间的相互作用.正向变构剂(positive allosteric modulators,PAMs)和负向变构剂(negative allosteric modulators,NAMs)分别可以提高或降低GABABR的活性,并具有较高的特异性和药物安全性,同时还能够保持GABABR信号在时间和空间上的可控性.变构剂为GABABR靶点药物开发提供了新思路.     

GABAB受体变构剂药学研究进展

Y-氨基丁酸B受体(GABAB receptor,GABABR)是最具有药理学意义的药物靶点之一,具有复杂而精细的激活机制.传统的GABABR靶点药物开发集中于激动剂和拮抗剂,这类药物受到多种因素的制约,包括较强的副作用、药物代谢困难、机体耐药性明显等.变构剂结合于正构位点之外,能够调节GABABR异源二聚体亚基或结构域间的相互作用.正向变构剂(positive allosteric modulators,PAMs)和负向变构剂(negative allosteric modulators,NAMs)分别可以提高或降低GABABR的活性,并具有较高的特异性和药物安全性,同时还能够保持GABABR信号在时间和空间上的可控性.变构剂为GABABR靶点药物开发提供了新思路.     

Pupal colour dimorphism in a desert swallowtail (Lepidoptera: Papilionidae) is driven by changes in food availability,not photoperiod

1. The swallowtail butterfly Battus polydamas archidamas Boisduval, 1936, exhibits polyphenism for pupal coloration (green and brown). It is distributed across arid regions with winter rains and is monophagous on Aristolochia plants, which emerge after the winter rains and dry out the during summer. Thus, day length does not covary positively with host plant productivity. It was hypothesised that pupal colour was driven by food availability, not photoperiod. The benefits of pupal coloration matching the colour of pupation sites in terms of field survival were also investigated to evaluate the adaptive value of pupa colour. 2. Larvae were reared under a factorial array of two photoperiods (LD 10:14 h and LD 14:10 h) and two food availability regimes (leaves ad libitum and available every other day) to assess the frequency of green and brown pupae. Field survival of green and brown pupae was quantified in three commonly used habitats that differ in background coloration (cacti, rocks and shrubs). 3. Food availability determined pupal colour. Larvae in the ad libitum regime resulted mostly in green pupae, while those with restricted food were mostly brown. In contrast, photoperiod did not influence pupal colour. Survival probability of pupae placed on cacti was higher than those placed on rocks and shrubs, and the lowest predation risk across habitats was for green pupae on cacti. 4. Food availability plays a major role in the seasonal polyphenism for pupal colour of specialist butterflies inhabiting arid environments with winter rains.     

湖南瓦乡人体质特征研究

本文对308例(男156例,女152例)世居在湖南省沅陵县的瓦乡人进行了70项体质人类学指标(观察项目25项,测量项目45项)的调查, 并计算了21项体质指数, 对部分指数进行了分型统计。结果表明: 湖南瓦乡人毛发浓密, 黑而平直; 上睑皱褶出现率较高, 眼裂开度中等, 上斜型眼裂; 少蒙古褶; 鼻根较高, 鼻梁男多直形、女多凹形, 鼻基上翘, 鼻翼高度中等; 口裂宽度中度, 上唇皮肤部多正唇, 红唇较厚; 耳壳多椭圆或卵圆形, 耳垂形状多圆形。体质特征表现为身材矮短, 体型中间型; 窄肩型; 中腿型; 超狭面型; 圆头型、高头型、中头型; 中鼻型。与我国南方其他27个少数民族群体的头面部及身高10项测量值进行聚类分析, 结果显示湖南瓦乡人体质特征与云南独龙族及拉祜族最接近, 与广西傈僳族、广西侗族及湘西土家族次之。湖南瓦乡人属于蒙古人种的南亚类型, 具有现代黄种人的容貌特征。     

湖南侗族的手纹研究

报道了湖南通道侗族337例正常人的指纹型、总指纹嵴数（TFRC）、a-b纹嵴线（a-bRC)、atd角、轴三角百分距（tPD)、大鱼际纹、小鱼际纹、指间区纹、掌褶纹、掌纹主线横向指数（MLIT）等手纹参数正常值,并与侗族不同人群和湖南周边不同民族进行了比较,发现湖南侗族手掌真实花纹和掌褶纹分布频率与湖南周边其他已研究过的民族和侗族群体存在明显差异。     

青稞麸皮油脂肪酸成分分析及其对高血脂症大鼠脂质代谢的影响

为了开发利用资源丰富的青稞麸皮,分析了青稞麸皮油的脂肪酸组成并研究了其对高血脂症大鼠的降血脂作用.通过GC-MS分析,从青稞麸皮油中检测到了10种脂肪酸,并发现其亚油酸含量为75.08%.在青稞麸皮油降血脂实验中,选用24只雄性SD大鼠随机分为空白对照组、高脂模型组和青稞麸皮油组,除空白对照组饲喂普通饲料外,其余各组饲喂高脂饲料并进行干预实验比较.3周后,高脂模型组血清TC、TG、LDL-C和AI 4项指标均显著高于空白对照组(P＜0.05或P＜0.01),而HDL-C/TC显著降低(P＜0.05);青稞麸皮油组的血清TC、TG、LDL-C和AI 4项指标均显著低于高脂模型组(P＜0.05或P＜0.01),而HDL-C/TC显著升高(P＜0.05).结果表明青稞麸皮油对大鼠的高血脂症和动脉硬化的形成有明显的抑制作用,而造成这一结果的原因可能是青稞麸皮油中的高亚油酸含量.     

西藏芫根提取物对小鼠抗缺氧作用的初步研究

实验研究西藏芫根提取物的抗缺氧活性.通过建立小鼠常压缺氧模型、急性脑缺血性缺氧模型以及亚硝酸钠中毒模型,以蒸馏水作为空白对照,盐酸普萘洛尔作为阳性对照,观察芫根水、65%乙醇及95%乙醇提取物的10 g/kg、15 g/kg和20 g/kg剂量组对小鼠缺氧的保护作用,同时观察各提取物10 g/kg剂量组对红细胞数量和血红蛋白含量的影响.结果表明,芫根水提取物、65%乙醇提取物及95%乙醇提取物均能明显延长模型小鼠在常压缺氧、急性脑缺血性缺氧及亚硝酸钠中毒时的存活时间,并可增加外周血象中红细胞数与血红蛋白含量,显示芫根提取物具有抗缺氧活性.     

Statistical optimization of a culture medium for biomass and poly(3-hydroxybutyrate) production by a recombinant Escherichia coli strain using agroindustrial byproducts.

A statistically based Plackett-Burman screening design identified milk whey and corn steep liquor concentrations as well as ionic strength (based on phosphate buffer concentration) as the three main independent components of the culture medium that significantly (p < 0.05) influenced biomass and poly(3-hydroxybutyrate) (PHB) production in recombinant cells of Escherichia coli. This strain carries a plasmid encoding phb genes from a natural isolate of Azotobacter sp. Response surface methodology, using a central composite rotatable design, demonstrated that the optimal concentrations of the three components, defined as those yielding maximal biomass and PHB production in shaken flasks, were 37.96 g deproteinated milk whey powder/l, 29.39 g corn steep liquor/l, and 23.76 g phosphates/l (r2 = 0.957). The model was validated by culturing the recombinant cells in medium containing these optimal concentrations, which yielded 9.41 g biomass/l and 6.12 g PHB/l in the culture broth. Similar amounts of PHB were obtained following batch fermentations in a bioreactor. These results show that PHB can be produced efficiently by culturing the recombinant strain in medium containing cheap carbon and nitrogen sources.     

湖北侗族的体质人类学

对448例(男232例,女216例)湖北侗族进行了90项体质人类学特征的调查(观察项目32项,测量项目58项),计算出40项体质指数,对身高和10项指数进行了分型统计。结果表明,1)湖北侗族上睑皱褶出现率88.11%,蒙古褶出现率47.13%,达尔文结节出现率82.14%;多数人前额发际为三角形;颧部与颏部突出不甚明显;头发浓密,黑而平直;眼裂上斜型,高度中等;鼻根及鼻翼高度中等,鼻梁男多直形、女多凹形,鼻基与鼻尖上翘型居多;口裂男性较宽,女性中等;上唇皮肤部多正唇且红唇较厚;耳壳多椭圆或卵圆形,耳垂以圆形为主。2)体质特征表现为身材矮短;瘦长体型;中躯干型;窄肩型;中腿型;宽手型;圆头型、高头型、中头型;阔鼻型;阔面型。3)与我国南方其他36个少数民族群体进行聚类分析,结果显示湖北侗族体质特征与湖南侗族和贵州布依族最接近。湖北侗族具有典型的蒙古人种的南亚类型体质特征。