吡酮酸类抗菌药物的研究——Ⅵ.7-氯-6-氟-1-乙基-1,4-二氢-4-氧吡啶(2,3-c)并哒嗪-3-羧酸及其衍生物的合成与抗菌活性

由2,6-二氯-5-氟-3-氰基吡啶出发,经氰基水解、酰氯化、与重氮乙酸乙酯缩合、重氮基还原、环化五步反应合成了一个新的杂环体系,即取代的吡啶(2,3-c)并哒嗪Ⅵ。由Ⅵ为原料经不同途径制得21个新衍生物,其中10个游离酸进行了体外抗菌活性筛选。对金葡-15、大肠-1515、绿脓-29的MIC(μg/ml),除化合物Xa和Xb对大肠-1515为50外,其余均大于100。     

Tomato By-Products,a Source of Nutrients for the Prevention and Reduction of Malnutrition

Malnutrition is a global phenomenon that mainly affects children under five years old, the elderly and food insecure people. It can be linked to undernourishment or overnutrition. To prevent it, a healthy and balanced diet, rich in energy and micronutrients, is necessary. The objective of this study was to evaluate the nutritional composition and contribution of tomato by-products to prevent and reduce malnutrition. Thus, standard methods were used for proximate composition and bioactive compounds. Results showed that tomato by-products are rich in macronutrients and micronutrients capable of preventing undernutrition and reducing the incidence of the effects of overnutrition. The average carbohydrate, protein and lipid contents were 15.43%, 11.71% and 5.4% (DM) in peels and for seeds the contents were 58.75%, 15.4% and 22.2%, respectively. The average energy values were 280.47 kcal/100 g and 472.8 kcal/100 g DM for peels and seeds, respectively. The main minerals found were, in decreasing order, potassium, magnesium, sodium, iron and zinc. High contents of phenolic compounds, lycopene, β-carotene and vitamin C were also found in these by-products. They also presented important antioxidant activities. Due to their nutritional and bioactive compounds, tomato by-products may be included in functional food formulation programs to reduce the incidence of nutritional diseases.     

In vitro and in vivo antiplasmodial activity of 'saye', an herbal remedy used in Burkina Faso traditional medicine

'Saye', a traditional medicine used in Burkina Faso, which consists of extracts of Cochlospermum planchonii (rhizome), Cassia alata (leaf) and Phyllanthus amarus (whole plant), showed a significant effect against Plasmodium falciparum and Plasmodium berghei parasites grown in vivo (IC(50) = 80.11 +/- 3.40 microg/mL; ED(50) = 112.78 +/- 32.32 mg/kg). In vitro the activity was lower.     

64排螺旋CT动脉血管造影在头颈血管病变空间定位及测定方面的意义

目的:64排螺旋CT头颈血管造影包含信息庞大,针对几种常见头颈血管病变的临床应用体会进行初步总结,更好地发挥多排螺旋CT头颈血管造影在头颈血管病变诊断、测量和空间定位等方面的优势。方法:搜集2006-05/2007-05南方医科大学附属珠江医院行64排螺旋CT头颈动脉血管造影120例患者的影像资料。男89例,女31例,年龄19～67岁。全部患者行64排螺旋CT头颈血管造影,36例患者同时行头颈动脉数字减影检查。实验仪器:CT机采用Philips公司Brillance64排螺旋CT扫描仪,数字减影机采用siemens公司Axiom-Artis平板数字减影仪。结果:120例患者中颈内动脉和椎基底动脉狭窄病例88例,脑动脉瘤22例,脑动脉畸形10例。88例动脉狭窄病例发现中度狭窄区223处、重度狭窄区68处;291处中重度狭窄区共发现187(64%)个斑块,其中钙化斑块121个(65%),软斑块15个(8%),混合斑块51个(27%);钙化斑块CT值为324～596HU,软斑块值CT值为47～84HU;斑块表面不规则者114个(61%)。22例脑动脉瘤病例共发现29个动脉瘤,肿瘤最大直径4.5mm～2.7cm;囊状动脉瘤19例,梭形动脉瘤10例;动脉瘤起源颈内动脉10例,大脑中动脉7例,前交通动脉3例,大脑后动脉3例,起源后交通动脉、基底动脉和椎动脉各2例;2例合并部分血栓形成,3例合并出血。10例脑动脉畸形病例中8例显示有明确供血动脉,其中大脑前动脉供血为主3例、大脑中动脉供血为主2例、大脑后动脉供血为主3例;7例显示明确引流静脉,其中引流静脉主要汇入上失状窦3例,汇入横窦3例,汇入大脑深静脉2例;2例合并多发动脉瘤,2例合并出血。结论:64排螺旋CT血管造影在头颈血管病变的诊断、测量和空间定位中具有重要价值,可作为头颈血管病变首选检查方法。     

应用微型骨锚钉重建指伸肌腱止点恢复关节功能28例

目的:传统对锤状指手术治疗主要是通过抽出钢丝法重建伸指肌腱止点或关节融合等方法。观察微型骨锚钉配合中药熏洗恢复关节功能的疗效。方法:选择2006-04/2007-03广州中医药大学第一附属医院创伤骨科的28例锤状指患者,均采用微型Anchor钉重建伸肌腱止点的手术方法并配合中药祛风通络散熏洗治疗。其中男16例,女12例,年龄12～45岁。全部病例均进行临床随访,主要以电话随访和问卷填写的方式,并采用国际上评价手指活动功能常用的Dargan功能评定法评定疗效,分别从患指主动活动范围、关节稳定性及疼痛和影像学检查等评价。结果:①28例患者全部得到随访,随访时间为3～7个月,平均4个月。②本组病例伤口除1例患者切口皮肤边缘变黑外均顺利愈合,该患者2周后皮肤愈合,本组患者术后平均9 d出院。③术后按Dargan方法评定主动活动范围:优25例,良2例,可1例。④全部患者于术后6周左右复查X线片均未见骨锚松动、脱落。全部患者在术后8周远侧指间关节活动自如,均获得满意结果。结论:使用Anchor钉重建伸肌腱止点手术治疗锤状指,具有操作简便、易于掌握的优点,再加上中药熏洗促进术后功能恢复,疗效可靠。     

体外培养新生大鼠心肌细胞的形态及其增殖能力

目的:心脏组织中心肌细胞增殖分化转变发生于出生后3～4d,有细胞周期调控机制的参与。观察新生大鼠心室肌细胞培养过程中细胞形态学和细胞周期素E表达的变化规律。方法:实验于2005-01/2006-03在新乡医学院解剖学与组织胚胎学重点学科实验室完成。①实验材料:1日龄Wistar大鼠20只,体质量7～10g。②实验方法及评估:心肌细胞分离、纯化及培养后用倒置显微镜观察其形态变化,免疫细胞化学染色及图像分析方法检测培养第1～53天新生大鼠心室肌细胞周期素E的表达。结果:纳入大鼠20只,均进入结果分析。①培养心肌细胞4h后贴壁,偶见单个细胞开始自发性搏动,部分细胞为梭形;以后细胞变为双核细胞,三角形或柱形细胞。第3天细胞聚集成片并同步搏动,第10天搏动频率最快,之后搏动频率逐渐减慢。②心肌细胞周期素E位于细胞核和核周的胞浆中。培养1～3d染色较深,以后逐渐变浅。③心肌细胞核内细胞周期素E表达量逐渐下降,第2天与第1天比较,差异无显著性(P>0.05)。从第3天开始差异有显著性(P<0.05,P<0.01)。结论:新生大鼠心肌细胞出生后早期体外培养的前3天有一定增殖能力,但以后呈下降趋势。细胞周期素E表达下调与心肌细胞增殖能力降低呈正相关。     

绞股蓝酮甙A的化学结构

自葫芦科(Cucurbitaceae)植物绞股蓝(Gynostemma pentaphyum (Thunb.)Makino)中分得一新天然化合物,命名为绞股蓝酮甙A(gypentonosideA),经理化分析及光谱(IR,MS,¹H-NMR,¹³C-NMR,2D-NMR)解析,其结构式如1所示。     

Timing of oocyte activation, pronucleus formation and cleavage in humans after intracytoplasmic sperm injection (ICSI) with testicular spermatozoa and after ICSI or in-vitro fertilization on sibling oocytes with ejaculated spermatozoa

In the first study, we evaluated 101 oocytes [2, 4, 6, 8, 16, 18 and 20 h after intracytoplasmic sperm injection (ICSI)] that had been microinjected with testicular spermatozoa. Of the 70 normally fertilized oocytes (69%) 30 (43%) had two pronuclei by 6 h after ICSI. Fifty-one (73%) by 8 h, 69 (99%) by 16 h and four of them by 20 h cleaved to the 2-cell stage. In the second study, 95 cumulus-corona- oocyte complexes (CCOC) were divided into two groups. Forty-seven CCOC were inseminated by conventional in-vitro fertilization (IVF) and 40 metaphase-II oocytes by ICSI. Oocytes were evaluated at 2, 4, 6 (only after ICSI), 8, 10, 12, 18, 20, 22, 24, 26, 28 and 30 h after both ICSI and IVF. After IVF, 35 oocytes were fertilized normally (75%), four of which (11%) had two pronuclei by 8 h, 11 (31%) by 10 h, 27 (77%) by 12 h and 35 (100%) by 14 h. The first cleavages had occurred by 24 h after insemination (four oocytes, 11%). After ICSI, 34 oocytes were fertilized normally (79%), 13 of which (38%) had two pronuclei by 6 h, 27 (79%) by 8 h and 32 (94%) by 10 h. Three oocytes cleaved by 20 h after microinjection (9%) and 19 by 24 h (56%). Pronuclei developed asynchronously in six oocytes after ICSI (18%) as opposed to 16 oocytes after IVF (46%). The results of this study suggest that the timing of pronuclear formation is no different when a testicular spermatozoon is microinjected into the oocytes from when an ejaculated spermatozoon is injected. Secondly, pronuclear development and first cleavage generally take place 4 h sooner after ICSI than after IVF. On the other hand, a higher proportion of oocytes develop two pronuclei asynchronously after IVF than after ICSI.      

中药葛根及其同属植物的资源利用和评价

对我国葛属(Pueraria DC.)9种和1变种植物进行了调查研究,认为目前国内市售中药葛根的主流品种为野葛P.lobata(Wild.)Ohwi和粉葛P.thomsoni Benth.。野葛在我国大部份省区都有分布,资源最为丰富;粉葛在广西载培历史悠久;其他种主要分布在西南地区,并有少数种在当地作中药葛根用。从成分分析结果看,野葛的葛根素(puerarin)及总黄酮含量显著高于本属其它植物,粉葛次之。除野葛和粉葛外其他种均不宜作葛根药用。峨嵋葛P.omeiensis Wang et Tang是个有争议的种,我们比较了化学成分的含量,其结果与粉葛相近,而与山葛藤有所区别,有待进一步研究。     

盾叶薯蓣薯蓣皂甙元含量与气候因素的相关性研究

以简单相关、多元回归及逐步回归分析等方法研究我国湖南湖北等27个县的盾叶薯蓣皂甙元含量与七个气候生态因子的关系。结果表明:1.年降水量和年平均5 cm土温为影响盾叶薯蓣皂甙元含量的主要因素;2.盾叶薯蓣皂甙元合成与积累的最适气候生态条件为:年降水量:800～900 mm,以850 mm最佳;年平均5 cm处土温:15～17℃,以16℃最佳。