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A new concise and facile method was explored to synthesize a collection of new 3-arylidene azetidin-2-ones, which could be regarded as the derivatives of the hybrid scaffold of bioactive natural cinnamamide and heterocycle azetidi-2-one. The structures of the synthesized compounds were characterized by 1H, 13C NMR, and MS; and their antifungal activity were evaluated against Alternaria solani Sorauer. These antifungal data were subjected to a quantitative structure-activity relationship (QSAR) analysis using Codessa software on the basis of the results from B3LYP/6-31G(d,p) quantum calculations. The best regressive model revealed that potentially more active compounds should have low dipole moments and QC-min (minimal net atomic charge for a C atom), and high QO-max (maximal net atomic charge for an O atom) and QN-min (minimal net atomic charge for an N atom). The most potent compound 7k could lead to intracellular accumulation of reactive oxygen species, dissipation of mitochondrial transmembrane potential, and an autophagy-like cell death process in A. solani Sorauer. Taken together, these results laid the foundation for further design of improved crop-protection agents based on this hybrid scaffold.

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Alternaria/efectos de los fármacos , Antifúngicos/farmacología , Azetidinas/farmacología , Diseño de Fármacos , Antifúngicos/síntesis química , Antifúngicos/química , Azetidinas/síntesis química , Azetidinas/química , Relación Dosis-Respuesta a Droga , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad

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In our continued efforts to improve the potential utility of the α-methylene-γ-lactone scaffold, 62 new and 59 known natural α-methylenelactam analogues including α-methylene-γ-lactams, α-arylidene-γ and δ-lactams, and 3-arylideneindolin-2-ones were synthesized as the bioisosteric analogues of the α-methylenelactone scaffold. The results of antifungal and cytotoxic activity indicated that among these derivatives compound (E)-1-(2, 6-dichlorobenzyl)-3-(2-fluorobenzylidene) pyrrolidin-2-one (Py51) possessed good selectivity with the highest antifungal activity against Colletotrichum orbiculare with IC50 = 10.4 µM but less cytotoxic activity with IC50 = 141.2 µM (against HepG2 cell line) and 161.2 µM (against human hepatic L02 cell line). Ultrastructural change studies performed by transmission electron microscope showed that Py51 could cause important cell morphological changes in C. orbiculare, such as plasma membrane detached from cell wall, cell wall thickening, mitochondria disruption, a dramatic increase in vacuolation, and eventually a complete loss in the integrity of organelles. Significantly, mitochondria appeared one of the primary targets, as confirmed by their remarkably aberrant morphological changes. Analysis of structure-activity relationships revealed that incorporation of the aryl group into the α-exo-methylene and the N-benzyl substitution increased the activity. Meanwhile, the α-arylidene-γ-lactams have superiority in selectivity over the 3-arylideneindolin-2-ones. Based on the results, the N-benzyl substituted α-(2-fluorophenyl)-γ-lactam was identified as the most promising natural-based scaffold for further discovering and developing improved crop-protection agents.

Asunto(s)

Antifúngicos/síntesis química , Colletotrichum/efectos de los fármacos , Lactamas/farmacología , Antifúngicos/farmacología , Línea Celular Tumoral , Forma de la Célula/efectos de los fármacos , Diseño de Fármacos , Hongos/efectos de los fármacos , Hongos/ultraestructura , Células Hep G2 , Humanos , Concentración 50 Inhibidora , Lactamas/síntesis química , Especificidad de la Especie , Relación Estructura-Actividad

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Through exploring the cause of medical students' professional identity status and further analyzing the present misunderstanding that exists in medical students' humanistic education,this paper thoroughly discussed the dialectical relationship between medical humanities education and medical students' professional identity.It analyzed the effects of medical humanistic education on medical students' professional values,professional expectations,professional sense of belonging and how medical humanistic education plays a role in them.

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Up to 80% of type 1 diabetes melitus children present with diabetic ketoacidosis (DKA). Stroke in children with DKA children is uncommon but life-threatening. Various types of stroke, such as ischemic, cerebral venous thrombosis, and hemorrhagic stroke were observed in children with DKA. In this article, we review the literatures regarding stroke in children with DKA.

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BACKGROUND:The functions of homo heterogeneous ribonucleoprotein E1 are very wide. It can participate in the expression of skeleton proteins in the nervous system. OBJECTIVE:To construct the recombinant plasmid of homo heterogeneous ribonucleoprotein E1 and observe its expression in nerve cells for further studying the functions of it in neurocytes. METHODS:Using pcDNATM4/His C, the homo heterogeneous ribonucleoprotein E1 was subcloned into recombinant plasmid E1-pcDNATM 4/His C, fol owed by enzyming and sequencing. After SH-SY5Y cells were transfected with the recombinant plasmid, western blot analysis and real time RT-PCR were used to detect the expression of homo heterogeneous ribonucleoprotein E1 in SH-SY5Y cells. And the growth of SH-SY5Y cells was observed. RESULTS AND CONCLUSION:We successful y constructed the eukaryotic expressed vector of homo heterogeneous ribonucleoprotein E1. The recombinant plasmids were verified to express in SH-SY5Y cells correctly at mRNA and protein levels. And SH-SY5Y cells generated quickly after homo heterogeneous ribonucleoprotein E1 was over-expressed. The homo heterogeneous ribonucleoprotein E1 is an important protein in neural development. And this vector offers the premise for further studying its function in nervous system.

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Objective To investigate the clinical features and treatment of mycoplasma pneumoniae infection complicated with allergic purpura.Methods 40 children with mycoplasma pneumoniae infection complicated with allergic purpura were selected.Clinical symptoms,disease treatment and outcome were analyzed retrospectively.Results 25 cases were abdominal type allergic purpura,9 cases were articulated joints allergic purpura,6 cases were kidney patients with allergic purpura.In addition,some patients showed upper or lower respiratory tract infections.All the patients received blood circulation improvement,anti-allergy and other conventional treatment,and on the basis of this,azithromycin,low-dose dexamethasone or gamma globulin was given.All 40 patients were cured,the average length of hospital stay was (18.6 ± 3.1) d.Conclusion Mycoplasma pneumoniae infection may trigger allergic purpura purpura-like rash,the clinical symptoms,some accompanied by lower respiratory infections,should give the conventional anti-mycoplasma pneumoniae infection treatment,and the treatment time should be sufficient to cure allergic purpura,shortening hospitalization time,has an important role in the prevention of recurrent disease.

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This research adopts both quantitative and qualitative analytical methods to analyze high-frequency medical words, morphemes and clusters, with the aid of corpora and statistical measures. The result of this research can help teachers arrange their teaching according to the difficulty and frequency of the words, morphemes and clusters.For students, they can put more time and effort on these frequently used words, morphemes and clusters, and thus improve learning efficiency.

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@#ObjectiveTo study the treatment and nursing care for intracranial aneurysm in elderly patients. Methods67 patients aged over 60 with intracranial aneurysm were reviewed. ResultsThe outcome was well (Glasgow Outcome Scale scores, 4～5) in 50 cases, and poor in 17 cases(Glasgow Outcome Scale scores, 1～3)．The median of time staying in hospital was 19 d in patients accepted surgery, and 11 d in the patients accepted intervention (P<0.05)． The preoperative Hunt-Hess grade was related with the outcome (P<0.05). ConclusionThe Hunt-Hess grades and the location of aneurysms are related with the outcome, but the treatment of surgery or intervention is not.

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Objective To discuss the effect and influence of nursing intervention on patients with cervical myelopathy treated by anterior cervical locking plate fixation. Methods Outpatient doctors and nurses screened out patients with cervical myelopathy, giving them propagands and education, instructing them to accept selective surgery. 42 hospitalized patients who obeyed medical orders were given preoperative and postoperative nursing intervention and rehabilitative instruction. The functional recovery of patients were evaluated by follow-up after discharge. Results The function restoration ratio reached 68.8% after 6-month-follow-up. Conclusions Appropriate and timely nursing intervention may promote function restoration of patients with cervical myelopathy.

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@#Objective To observe the effect of improved body turning approach on wound healing after operation of congenital craniovertebral junction abnormity.Methods 82 patients with congenital craniovertebral junction abnormity were performed occipital-cervical bony grafting posteriorly and they were cared with improved or routine body turning approach.Results The incidence of wound healing was 95.1% in routine group and was 100% in improved group.Conclusion The improved body turning approach could improve the wound healing after operation of congenital craniovertebral junction abnormity.

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Objective To investigate the relation of morbidity law of upper gastronintestinal hemo rrhage and cycle of Heavenly Stems and Earthly Branches in Gansu province. Methods Investigative statistical forms were set up and analyzed by computer about twelve years in-patient of upper gastronintestinal hemorrhage in TCM hospital of these district. Results High morbidity corresponded with theory of YUNQI, in 1988 (year of the fifth of ten Hevenly Stems and the fifth of the twelve Earthly Branches, HUOYUN is high sufficient), 1995 (year of the second of ten Hevenly Stems and the last of the twelve Earthly Branches, JINYUN is insufficient), and Baiyin district in 1994 (year of the first of ten Hevenly Stems and the eleventh of the twelve Earthly Branches TUYUN is high sufficient), Cheng district in 1996 (year of the third of ten Hevenly Stems and the first of the twelve Earthly Branches, SHUIYUN is high sufficient), YUNQI was high sufficient or insufficient, which causing diseases conform to five internal organs and geographical position. Conclusion Morbidity law of upper gastronintestinal hemorrhage corresponds with cycle of Heavenly Stems and Earthly Branches.

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Objective To investigate the relation between TCM syndromes of upper gastrointestinal hemorrhage and solar terms change in different years. Methods Data of upper gastrointestinal hemorrhage in-patients in seven districts of TCM hospital of Gansu province in twelve years were filled in investigative statistical forms and analyzed by computer. Results There was obvious difference in TCM syndromes among different solar terms and different years. Conclusion Atmospheric pressure, atmospheric temperature, air humidity, diurnal temperature range of solar terms change in different years directly effect TCM syndromes of upper gastrointestinal hemorrhage.

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OBJECTIVE To apply the clinical pathway in hospital infection control in order to cut down the development of hospital infection.METHODS To take clinical pathway combined with clinic,to establish scientific,effective and standard measures to reduce hospital infection.RESULTS To practice clinical pathway could raise medical quality,rationally utilize the health resources,decrease economy burden of the patient and control hospital infection.CONCLUSIONS It′s of practical importance to promote the hospital infection management through clinical pathway.

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OBJECTIVE To understand the infection of Acinetobacter baumannii(ABA) in children and make analysis for its resistance to 15 antibiotics.METHODS The collection of clinical strains of ABA isolated from the hospital.the pathogens were identified by MicroScan WalkAway-40 system.RESULTS Eighty-one(95%) ABA among 85 isolates were from respiratory tract.The result of drug susceptibility showed that ABA was highly sensitive to the 15 antibiotics.Multi-resistant ABA bacteria accounted for 8.2%(7/85).CONCLUSIONS ABA strains isolated from children patients show the trend of multi-drug resistance.we should pay more attention to monitor the susceptibility to antibiotics.

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The article gives a brief analysis of student characteristics of medical independent college and the aim and purpose of medical education to propose the corresponding measures to improve the students work of independent college.

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The thesis,from the aspect of professional guidance of education,focuses on the outstanding problems that exist in the work of professional guidance,analyzes the main reasons that caused those outstanding problems,and gives the feasible suggestions to professional guidance in current university education.