福建省中部地区抗寒速生尾巨桉优株筛选

本文通过自然选择与优势木选择方法,选择了适生性状良好的尾巨桉品种的多个优良单株。根据不同选择标准,筛选出抗寒适生优良单株21株,抗寒速生优势木单株13株;对所选单株采用无性系繁殖方法,利用1000mg/L ABT生根粉处理所选择优良单株的穗条,用营养袋扦插培育无性系种苗,并建立无性系采穗圃和优良单株基因库。     

桡骨远端不稳定骨折的治疗策略

目的：探讨桡骨远端不稳定骨折的最佳治疗方案,以便能够获取更好的功能康复。方法：2007年1月-2011年12月共收治桡骨远端不稳定骨折51例,其中采用外支架撑开复位外固定5例,后路复位钢板内固定治疗23例,前路钢板固定17例,前后路联合固定6例,术后均早期进行关节功能锻炼。结果：51例均获得随访,X片提示均已骨性愈合。采用Gartland和Werley评分系统评估腕关节功能,其中外支架固定,优1例,良1例,中2例,差1例,优良率40％;后路固定,优12例,良6例,中3例,差2例,优良率78-3％;前路固定,优9例,良6例,中1例,差1例,优良率88．2％;前后路联合,优2例,良1例,中2例。差1例,优良率50％。结论：桡骨远端不稳定骨折正确的手术策略能够获得更好的功能恢复,其中前路手术固定效果优于后路固定。     

重组合异种骨治疗股骨非感染性骨不连的长期疗效观察

目的:探讨重组合异种骨治疗股骨非感染性骨不连的长期临床疗效。方法:对2000年1月至2006年9月间我院应用重组合异种骨(RBX)治疗的37例股骨非感染性骨不连患者进行回顾性分析,其中男26例,女11例;年龄4～70岁,平均31.6岁。骨折部位:股骨近端4例,中段30例,远端3例。骨不连类型:肥大型9例,营养不良型6例,萎缩型22例。固定方式:加压钢板24例,髓内钉11例,外固定架2例。结果:37例患者获得51-131个月的随访,平均90.2个月,骨不连一次手术愈合率:94.6%,4例股骨近端骨不连患者采用Harris评分系统评定疗效,优3例,良1例,差0例,优良率100%。3例股骨远端骨不连患者采用美国膝关节协会评分系统(KSS)评定疗效,优1例,例良1例,差1例,优良率66.7%。30例股骨干骨不连患者采用Harris评分系统和KSS评定疗效,优21例,良8例,差1例,优良率96.7。总优良率94.6%。长期观察均无免疫排斥反应表现。结论:RBX用于治疗股骨非感染性骨不连具有材料充足、骨折愈合率高、组织兼容性好长期应用无免疫排斥反应等优点,是一种良好的自体骨替代材料。     

Glycosyl trichloroacetylcarbamate: a new glycosyl donor for O-glycosylation

Glycosyl trichloroacetylcarbamates, readily obtained by reacting 1-hydroxy sugars with trichloroacetylisocyanate, have been found as excellent glycosyl donors, and the corresponding O-glycosides are formed in good to excellent yields with a fairly good degree of selectivity.     

贵州茯苓优良菌株的筛选

以l6个不同来源的茯苓菌株为试验材料,分别进行了菌丝生长初筛、复筛、高产性能筛选、遗传稳定性分析等一系列优良菌株筛选试验,获得4个长势强、产量高、商品性好、遗传稳定、适合贵州人工栽培的优良菌株;并在此基础上初步建立优良茯苓菌株筛选模型。     

《动物病理学》精品课程建设的探索与实践

为加深精品课程内涵的深刻认识,加强对精品课程的指导与建设,有效促进课程体系及教学内容、教学方法和教学手段的改革,以安徽农业大学《动物病理学》国家精品课程的建设为例,从提高教学团队素质、提升教学资源建设、推进课程教学改革等方面总结该门精品课程的建设经验和心得体会。     

Fixation techniques for fine needle aspiration biopsy smears prepared off site

OBJECTIVE: To identify a simple, cost-effective, reliable fixation method for fine needle aspiration biopsy (FNAB) yielding a specimen suitable for mail transport. STUDY DESIGN: Smears prepared from 59 FNABs of surgical specimens were fixed by continuous fixation in 95% ethanol, spray fixation, air drying, ethanol fixation for either 5 minutes or 4 hours followed by spray fixation, or fixation in 95% ethanol for either 30 minutes or 4 hours followed by air drying. Fixation was graded as unsatisfactory, suboptimal, average, good or excellent. RESULTS: Of smears continuously fixed in ethanol, 96.6% were graded as excellent. Of smears fixed in ethanol followed by spray fixation, 93.2% were excellent irrespective of fixation time; 64.4% of spray-fixed smears were excellent and 27.1% good. Of air dried smears, 93.2% were unsatisfactory or suboptimal; 83.0% of smears fixed in ethanol for 30 minutes and 74.6% of smears fixed for 4 hours prior to air drying were unsatisfactory or suboptimal. CONCLUSION: Fixation of smears in 95% ethanol followed by spray fixation produces excellent results, comparable to those with continuous fixation in ethanol. Spray fixation is generally good but not consistently excellent. Air drying or fixation in ethanol followed by air drying yields unsatisfactory or suboptimal results in most cases.     

Discovery and SAR of spirochromane Akt inhibitors

A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided compounds with excellent Akt enzyme and cell activities but greatly diminished selectivity over PKA.     

Cryothalamectomy for Parkinson's Disease

In a review of 61 patients with Parkinson''s disease who were treated by cryothalamectomy, the technique of freezing a surgical target as compared with destroying it by alcohol or thermal heat was found effective and to a degree safer than other techniques. One patient died of unexpected cerebral hemorrhage. Of patients considered excellent candidates for the operation, 80 per cent had excellent and good results, while those considered good candidates showed 85 per cent excellent and good results. The results are more dependent on the selection of the patient as a candidate and the diffuseness of the pathophysiological circuits involved than on the technical factors of the cryogenic procedure.     

Long-term therapy of essential tremor with propranolol.

In a double-blind crossover study 12 patients with essential tremor were treated with propranolol and a placebo; 8 improved with propranolol and 3 with the placebo; the degree of improvement with propranolol was greater. In a similar study with diazepam 5 of 12 improved with diazepam and 4 of 12 with the placebo; the degree of improvement was less than that achieved with propranolol. Response in 21 patients to treatment with propranolol for 2 to 4 years was excellent in 4, good in 4 and fair in 10; the condition of 1 was unchanged and that of 2, worse. Excellent response was maintained for as long as 4 years, but response tended to deteriorate with time if initially it was less than excellent. Response decreased with increasing age. No patient 60 years of age or older had an excellent response, and the four with an excellent response were under age 55, three being under age 35; all four had had their tremor less than 12 years. Patients with essential tremor should be given a 3-month trial of propranolol at 120 mg/d; if no significant response is seen the dose should be decreased, then the drug discontinued.     

Talent in autism: hyper-systemizing,hyper-attention to detail and sensory hypersensitivity

We argue that hyper-systemizing predisposes individuals to show talent, and review evidence that hyper-systemizing is part of the cognitive style of people with autism spectrum conditions (ASC). We then clarify the hyper-systemizing theory, contrasting it to the weak central coherence (WCC) and executive dysfunction (ED) theories. The ED theory has difficulty explaining the existence of talent in ASC. While both hyper-systemizing and WCC theories postulate excellent attention to detail, by itself excellent attention to detail will not produce talent. By contrast, the hyper-systemizing theory argues that the excellent attention to detail is directed towards detecting ‘if p, then q’ rules (or [input–operation–output] reasoning). Such law-based pattern recognition systems can produce talent in systemizable domains. Finally, we argue that the excellent attention to detail in ASC is itself a consequence of sensory hypersensitivity. We review an experiment from our laboratory demonstrating sensory hypersensitivity detection thresholds in vision. We conclude that the origins of the association between autism and talent begin at the sensory level, include excellent attention to detail and end with hyper-systemizing.     

The Management of Patients with Malignant Lymphoma

The prognosis of patients with malignant lymphoma discovered in the localized state and adequately treated is excellent. The prognosis for patients with malignant lymphoma, in general, is much more favorable than is generally recognized.Radiation therapy is the treatment of choice for localized malignant lymphoma. Radiation therapy and chemotherapy can produce excellent palliation in patients with advanced disease and long-term survival in many of them.     

Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors

A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated potent (～ 0.100 μM IC(50)) growth inhibition in a PTEN deficient cancer cell line.     

The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus

A novel and potent small molecule glucagon receptor antagonist for the treatment of diabetes mellitus is reported. This candidate, (S)-3-[4-(1-{3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy}butyl)benzamido]propanoic acid, has lower molecular weight and lipophilicity than historical glucagon receptor antagonists, resulting in excellent selectivity in broad-panel screening, lower cytotoxicity, and excellent overall in vivo safety in early pre-clinical testing. Additionally, it displays low in vivo clearance and excellent oral bioavailability in both rats and dogs. In a rat glucagon challenge model, it was shown to reduce the glucagon-elicited glucose excursion in a dose-dependent manner and at a concentration consistent with its rat in vitro potency. Its properties make it an excellent candidate for further investigation.     

杂草稻种质资源的综合评价

从韩国引入34份杂草稻种质资源,在云南生态条件下进行田间农艺性状、抗病性及品质的综合鉴定,从中筛选出6份综合性状优良或具有某种优异性状的种质,可供育种利用。     

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

Herein we describe the discovery and development of a novel class of M(4) positive allosteric modulators, culminating in the discovery of ML293. ML293 exhibited modest potency at the human M4 receptor (EC(50)=1.3 μM) and excellent efficacy as noted by the 14.6-fold leftward shift of the agonist concentration-response curve. ML293 was also selective versus the other muscarinic subtypes and displayed excellent in vivo PK properties in rat with low IV clearance (11.6 mL/min/kg) and excellent brain exposure (PO PBL, 10 mg/kg at 1h, [Brain]=10.3 μM, B:P=0.85).     

后侧手术入路、锁定钢板固定治疗胫骨平台后髁骨折的临床疗效

目的：探讨采用膝关节后内和后外侧切口、锁定钢板固定治疗胫骨平台后髁骨折的临床疗效。方法：选取2009年1月～2011年12月来我院治疗的13例胫骨平台后髁骨折患者作为研究对象,所有患者采用后内和后外侧切口、锁定钢板固定治疗,观察术后骨折愈合情况,采用Rasmussen放射学评分评定骨折复位情况,采用HSS评分系统评定膝关节功能疗效。结果：术后随访6～24个月,平均13．6个月,所有患者骨折均于16周内愈合。Rasmussen放射学评分15～18分,平均17．4分,其中优8例,良3例,可2例,优良率为84．7％。末次随访时膝关节功能HSS评分73~97分,平均91．4分,其中获优7例,良5例,可1例,优良率为92．3％。结论：采用膝关节后内和（或）后外侧切口、锁定钢板固定治疗胫骨平台后髁骨折具有操作简单、显露清晰、直视下复位骨折及关节面、固定牢靠、利于早期功能锻炼、临床疗效确切、并发症少等优点。     

2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors

Screening of the Amgen compound library led to the identification of 2-phenylamino-6-cyano-1H-benzimidazole 1a as a potent CK1 gamma inhibitor with excellent kinase selectivity and unprecedented CK1 isoform selectivity. Further structure-based optimization of this series resulted in the discovery of 1h which possessed good enzymatic and cellular potency, excellent CK1 isoform and kinase selectivity, and acceptable pharmacokinetic properties.     

Pyrazolopyrimidinone Based Selective Inhibitors of PDE5 for the Treatment of Erectile Dysfunction

Continuing research with our earlier finding of sildenafil based analogs in the search of new inhibitors of PDE5 for erectile dysfunction suggested that there is a scope of modifications at N-methylpiperazine ring with hydrophobic region followed by hydrogen bond donor or acceptor region. However, the leads identified earlier had some limitations like poor pharmacokinetic (PK) profile, low aqueous solubility and poor bioavailability. In this direction, a new series of sildenafil based analogs were designed, synthesized and screened for their PDE5 inhibitory activity. In this series compound 18 was found to have excellent in vitro activity with selectivity towards PDE5 isozyme, also the in vivo activity and pharmacokinetic profile was excellent. The cyp inhibition and CaCO₂ permeability was also excellent for compound 18 .     

The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase

Herein we describe the discovery of a novel series of ATP competitive B-Raf inhibitors via structure based drug design (SBDD). These pyridopyrimidin-7-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimization led to the identification of compound 17, a potent, selective and orally available agent with excellent pharmacokinetic properties and robust tumor growth inhibition in xenograft studies.