Synthesis and biological activity evaluation of phthalimide-donepezil hybrids / 药学学报

A series of phthalimide-donepezil (PTA-DPZ) hybrids (5a-e, 6a-l) were designed, synthesized and evaluated as selective inhibitors of acetylcholinesterase (AChE). The results showed that some hybrids had strong AChE inhibitory activity with half maximal inhibitory concentration (IC50) at nanomolar range, which was better than the control drugs galanthamine and tacrine, and equivalent to DPZ. Compound 6k exhibited the strongest inhibition to AChE with an IC50 value of 0.13 μmol·L-1. Kinetic and molecular modeling studies showed that 6k targeted both catalytic active site and peripheral anionic site of AChE. Moreover, some compounds could inhibit AChE-induced β-amyloid (Aβ) aggregation. In addition, absorption, distribution, metabolism and excretion prediction results showed 6k conforms to the Lipinski's rule of five and had high partition coefficient P value. These compounds, especially 6k, may be considered as a dual-functional lead compound for in-depth research.

DNA methylation status of the forkhead box protein 3 gene in CD4+ T cells of patients with Henoch-Sch(o)nlein purpura and its correlation with regulatory T cells / 中华皮肤科杂志

Objective To determine the proportion of CD4+ CD25+ regulatory T (Treg) cells,mRNA expression of the forkhead box protein 3 (Foxp3) gene,and DNA methylation status of the Foxp3 promoter in peripheral CD4+ T cells from patients with Henoch-Sch(o)nlein purpura.Methods Totally,20 inpatients with Henoch-Sch(o)nlein purpura and 20 healthy controls were enrolled from Department of Dermatology,the Second Xiangya Hospital of Central South University between 2015 and 2016,and there were no significant differences in the gender and age between the two groups (both P ＞ 0.05).CD4+ T cells were isolated from the peripheral blood samples of these subjects.Real-time fluorescence-based quantitative PCR was performed to detect the mRNA expression of the Foxp3 gene,flow cytometry to determine the proportion of CD4 + CD25+ Treg cells,and sodium bisulfite sequencing PCR (BSP) to determine the DNA methylation status of the Foxp3 promoter.Statistical analysis was carried out with SPSS16.0 software by using two-sample t test for the comparison between the two groups,and linear correlation analysis for evaluating the correlations of the DNA methylation status of the Foxp3 promoter with clinical severity scores and the proportion of CD4+CD25+ Treg cells.Results Compared with the healthy control group,the Henoch-Sch(o)nlein purpura group showed significantly decreased mRNA expression of the Foxp3 gene in CD4+ T cells (0.380 ± 0.226 vs.1,t =9.503,P ＜ 0.01),proportion of CD4+CD25+ Treg cells (1.668％ ± 0.959％ vs.2.741％ ± 1.131％,t =2.552,P ＜ 0.05),but significantly increased DNA methylation status of the Foxp3 promoter (0.712 ± 0.164 vs.0.453 ± 0.147,t =3.610,P ＜ 0.01).In the Henoch-Sch(o)nlein purpura group,the DNA methylation status of the Foxp3 promoter was negatively correlated with the percentage of CD4+CD25+ Treg cells (r =-0.490,P ＜ 0.05),but positively correlated with the clinical severity scores (r =0.486,P ＜ 0.05).The DNA methylation level of the Foxp3 promoter was significantly higher in the patients with renal impairment than in those without renal impairment (P ＜0.05).Conclusion The patients with Henoch-Sch(o)nlein purpura showed increased DNA methylation status of the Foxp3 promoter in CD4+ T cells,decreased mRNA expression of the Foxp3 gene and proportion of CD4+CD25+ Treg cells,which may be related to the occurrence of Henoch-Sch(o)nlein purpura,and affect disease development and prognosis.

Kaposi varicelliform eruption with severe complications:a case report / 临床儿科杂志

Objective To investigate the clinical features and prognosis of Kaposi varicelliform eruption with severe complications. Methods The clinical data of one child with Kaposi varicelliform eruption with severe complications was retrospectively analyzed. The related literatures were reviewed. Results A 5-month-old boy presented with recurrent rash on the head and face for 3 months and aggravated for 3 days. The skin lesions showed a characteristic of typical dome-shaped blisters with hemorrhagic crusting. At admission, the boy suffered with severe hypoproteinemia, hypocalcemia, and electrolyte disorder. The hypocalcemia was aggravated gradually. On the fifth day of admission, the boy had fever, convulsions, and tachycardia. Blood culture showed methicillin-resistant Staphylococcus aureus (MASA) infection. The diagnosis of sepsis was confirmed. At that very day, the boy started to have coagulopathy, so Fusidic and Vancomycin for anti-infection, Acyclovir for antivirus, intravenous infusion immunoglobulin, albumin, cryoprecipitate, plasma and calcium gluconate were administered, supplied with albumin and blood coagulation factor. The boy's condition gradually became stable and discharged on the 19th day after admission. Conclusions When Kaposi varicelliform eruption is complicated with hypoproteinemia and hypocalcemia, the critical illness is indicated. Clinicians should be alerted to the existence of sepsis, coagulation disorders, even septic shock and disseminated intravascular coagulation.

A case of Parkes-Weber syndrome accompanied by pseudo-Kaposi's sarcoma / 中华皮肤科杂志

A girl who aged eight years and seven months presented with prunosus patches on the right buttock for 8 years,gradual unilateral enlargement of the right lower limb for more than 7 years,and multiple vegetations for 1 year.Dermatological examination showed nevus flammeus and multiple malodorous vegetations over the right lower limb with high skin temperature.The right lower limb was thicker and longer than the left lower limb.X-ray examination,magnetic resonance imaging and Doppler ultrasound examination revealed high-flow vascular malformations.Pathological examination of the vegetations showed vascular proliferation,fibroblast proliferation and erythrocyte extravasation.She was diagnosed as Parkes-Weber syndrome accompanied by pseudo-Kaposi's sarcoma.

Treatment of Kasabach-Merritt syndrome in three infants by percutaneous selective digital subtraction angiography combined with transarterial hardened embolization / 中华皮肤科杂志

Objective To develop a new treament strategy for Kasabach-Merritt syndrome.Methods Three infants who were diagnosed with Kasabach-Merritt syndrome and suffered from thrombocytopenia as well as bleeding and clotting disorders were treated with percutaneous selective digital subtraction angiography combined with transarterial hardened embolization under general anesthesia.Sclerosing agents included bleomycin A5 (4.0 mg),iodized oil (1.5 ml),dexamethasone (2.5 mg) and iopamidol (3 ml).Polyvinyl alcohol mixed with iopamidol (at a volume fraction of 0.5) served as the embolic material.Results All the three patients were successfully treated by the minimally invasive surgery.The amount of blood platelet returned to normal within 24 hours after the operation.On the fourth day,all the patients were discharged from hospital with the restoration of coagulation function.Revisits at one month and three months after the operation showed that hemangiomas markedly shrank and even subsided,and blood platelet count was maintained within normal range.Conclusions Percutaneous selective digital subtraction angiography combined with transarterial hardened embolization can result in a recovery of blood platelet count and shrinkage of hemangioma,and may serve as a minimally invasive treatment option for Kasabach-Merritt syndrome.

Langerhans cell histiocytosis: clinical analysis of 126 cases / 中华皮肤科杂志

Objective To analyze lesional and clinical characteristics of Langerhans cell histiocytosis in children.Methods A clinical retrospective study was performed on 126 patients with Langerhans cell histiocytosis collected from 2006 to 2011 at the Hunan Children's Hospital.Results Of the 126 patients,the youngest was 2months old,and the oldest was 9 years old.The ratio of male to female was 2.5 ∶ 1.Clinical manifestations included eczematid,seborrheic lesions,hemorrhagic maculopapules,yellow nodules and white macules.Of the three clinical phenotypes of Langerhans cell histiocytosis,Letter-Siwe disease was the most prevalent,and most cases of LetterSiwe disease were associated with hepatosplenomegaly,abnormal chest X-ray,impaired hematopoietic function and multifocal bone injuries.The clinical grade was mainly Ⅲ and Ⅳ in patients with Letter-Siwe disease,Ⅰ in patients with eosinophilic granuloma,and varied from Ⅰ to Ⅳ in patients with Hand-Schuller-Christian disease with Ⅱ as the most common.Of these patients,those with eosinophilic granuloma had the oldest average age with bone as the only affected organ,while those with Letter-Siwe disease had the youngest average age with the greatest number of affected organs.The treatment of Langerhans cell histiocytosis included surgical operation and combined chemotherapy.Conclusions Langerhans cell histiocytosis has characteristic skin lesions and diverse clinical manifestations.Pathology has diagnostic significance to Langerhans cell histiocytosis.Therapy strategies and curative effects are dependent on the severity of,and the organs affected by Langerhans cell histiocytosis.

Clinical observation on acupuncture for diarrhea-predominant irritable bowel syndrome patients in syndrome of liver-stagnation and spleen-deficiency and its impact on Th1/Th2 / 中国针灸

<p><b>OBJECTIVE</b>To observe clinical therapeutic effects of acupuncture for pattern of liver-stagnation and spleen-deficiency in diarrhea-predominant irritable bowel syndrome (D-IBS) and its impact on cell factors.</p><p><b>METHODS</b>Forty cases were selected and divided into an acupuncture group (21 cases) in which acupuncture was applied and a medicine group (19 cases) in which oral administration of dicetel and bifidobacterium lactobacillus triple viable capsules were applied. The symptom scores, level of Th1-type cytokine (IFN-gamma, IL-2) and Th2-type cytokine (IL-4, IL-10) and ratio of IFN-gamma to IL-4 were compared in two groups before and after treatment to analyze acupuncture effect.</p><p><b>RESULTS</b>The clinical symptoms were improved after one-week treatment in the acupuncture group (P<0.05), which had faster onset than the medicine group (P<0.05). The total effective rate was 90.48% (19/21) in the acupuncture group, which was superior to 78.95% (15/19) in the medicine group (P<0.05). Compared with medicine treatment, imbalanced condition of Th1/Th2 was turning towards the direction of Th2 after acupuncture, indicating a tendency to recover the balance.</p><p><b>CONCLUSION</b>The clinical efficacy of acupuncture for D-IBS has close relationship with effectively improving balance of Th1/Th2 in patients with liver-stagnation and spleen-deficiency.</p>

Investigation of allergens in 3,504 children with allergic diseases / 中国当代儿科杂志

<p><b>OBJECTIVE</b>To investigate the allergens of various allergic diseases in children.</p><p><b>METHODS</b>Serum levels of Fx5E, Phadiatop and specific IgE were measured by the UniCAP100 System in 3 504 children with allergic diseases.</p><p><b>RESULTS</b>The positive rate of aeroallergens was obviously higher than that of food allergens in children with allergic rhinitis, allergic conjunctivitis, asthma and papular urticaria. In contrast, the positive rate of food allergens was obviously higher than that of aeroallergens in children with Henoch-Schonlein purpura and digestive diseases. The serum specific IgE level of aeroallergens was higher than that of food allergens. The dust and mite specific IgE levels reached to grade 6, while the food allergen specific IgE levels were lower than grade 3.</p><p><b>CONCLUSIONS</b>Aaeroallergens or food allergens vary remarkably in different allergic diseases in children. The level of specific IgE of aeroallergens is higher than that of food allergens.</p>

Laparoscopic transhiatal extended gastrectomy for type II, III esophagogastric junction cancer: a preliminary report of 55 cases / 中华胃肠外科杂志

<p><b>OBJECTIVE</b>To explore the feasibility and safety of laparoscopic extended gastrectomy through the transhiatal approach in patients with esophagogastric junction cancer.</p><p><b>METHODS</b>From Feb 2008 to May 2010, 55 cases with Siewert type II or III esophagogastric junction cancer underwent laparoscopic transhiatal extended gastrectomy at the West China hospital. Clinical data were analyzed retrospectively.</p><p><b>RESULTS</b>Esophagogastric junction cancer was Siewert type II in 36 patients and Siewert type III in 19. Thirty-five cases underwent proximal gastrectomy, 20 total gastrectomy. There were 53 D2 lymph node excisions and 2 palliative resections. Fifty patients underwent laparoscopic extended gastrectomy successfully, with 5 converted to open operations. A safe anastomosis between inferior pulmonary vein and pulmonary hilum was achieved in the majority of patients. The mean operative time was(236.2±35.5) min and the mean estimated blood loss was(60.6±33.9) ml. There were no postoperative mortalities or anastomotic leakage/stenosis. No reoperations were required. Pleural laceration occurred in 11 cases during operation, of whom 10 were repaired intraoperatively and one was managed with drainage postoperatively. There were 3 patients developed pulmonary infection and one wound infection. Postoperative recovery was uneventful in other patients.</p><p><b>CONCLUSION</b>Laparoscopic transhiatal extended gastrectomy is feasible and safe for patients with esophagogastric junction cancer.</p>

Clinical analysis of 272 patients with Kawasald disease / 中华皮肤科杂志

Objective To investigate the clinical features of Kawasaki disease.Methods A retrospective analysis was performed in 272 children diagnosed as Kawasaki disease from 2002 to 2006.Clinical data,laboratory findings and auxiliary examination results were collected for these patients.Results The male-to-female ratio Was 2.58:1.Onset ages between 1 to 3 years accounted for 59.2%of patients.Of these patients,100%had a fever for more than 5 days,76.1%transient polymorphous exanthema,74.6% bilateral conjunctival hyperemia,47.8%flare and fissure on the oral lip,58.5%strawberry tongue,22.8% firm swelling of hands and feet as well as flushing of palms and soles,3 1.2%subacute desquamation at the junctional site between nail bed and skin,36%cervical lymphadenopathy.Laboratory findings showed a significant increase in the count of peripheral blood leukocytes and pefipheral blood platelets as well as erythrocyte sedimentation rate in 80.5%,87.5%and 96.2% of Patients,respectively.Additionally,81.6%of these patients were positive for C reactive protein and the frequency of coronary aaery involvement was 54.3%.All patients were treated with aspirin,and high-dose intravenous immunoglobulin was given to 258 patients.Fever relieved and the condition was controlled in all patients with an average hospitalization period of 8.9 days.Conclusions Kawasaki disease should be suspected in Patients with exanthematous lesions,fever lasting for more than 5 days and poor response to antibiotic therapy.Peripheral blood platelet count and cardiac ultrasound are of great value in the diagnosis of Kawasaki disease.Aspirin iS the first choice in treating Kawasaki disease,and adjunctive high-dose intravennous immunoglobulin treatment may facilitate the quick control offever.

Detection of serum specific IgE in 437 children with allergic disease / 中国当代儿科杂志

<p><b>OBJECTIVE</b>To investigate the distribution of allergens in children with allergic disease in Changsha.</p><p><b>METHODS</b>Total IgE and specific IgE against some allergens were examined by the AllergyScreen system in the sera of 437 children from Changsha with allergic disease.</p><p><b>RESULTS</b>The positive rates of total IgE and special IgE were 68.9% and 69.1% respectively. Dermatophagoides farina, beef, mutton, milk and fur of cats and dogs were found as common allergens. The IgE positive rate against dermatophagoides farina was the highest in children with allergic rhinitis (86.0%), followed by in those with atopic dermatitis (41.2%), eczema (27.6%) and urticaria (20.0%). Serum IgE was positive against the fur of cats and dogs in 23.5% of children with atopic dermatitis and in 18.1% of children with eczema. The IgE positive rate was lower in children with urticaria and allergic rhinitis (10.0% and 8.7% respectively). IgE positive rates against milk, beef and mutton were high in the above four allergic diseases (range: 14.0%-24.0%), but no significant differences were observed for the IgE positive rate among the four allergic diseases. The IgE positive rate to inhalant allergens in children at ages of less than 3 years was markedly higher than that in children at ages of more than 3 years (p<0.01).</p><p><b>CONCLUSIONS</b>Allergic diseases are mainly mediated by allergens. Allergens, especially dermatophagoides farina, fur of cats and dogs, beef, mutton and milk, play an important role in childhood allergic diseases in Changsha.</p>

Prognostic significance of circumferential resection margin involvement in patients of rectal cancer / 中华普通外科杂志

Objective To study the prognostic value of circumferential resection margin(CRM)status. Methods Specimens of 62 patients with rectal cancer,who underwent total mesorectal excision from December,2001 to June,2002,were examined using whole-mount sections.All patients were followed up for 4～60 months. Results Circumferential resection margin involvement(CRMI)was identified in 12 specimens.while only 4 of them were cancer positive in the resection margin.Analyzed by logistic regression test,the occurrence of CRMI was related to tumor differentiation [ P=0.015,Exp(B)=0.131]and lymph node metastases[P=0.013,Exp(B)=7.488 ],but not tumor distance to anal verge(P=0.246).The difference in local recurrence rate,overall recurrence rate,disease-free survival rate and overall survival rate between CRMI and that of CRM negative,were significant(P=0.002,0.000,0.000 and 0.003,respectively). Conclusions CRMI is an accurate prognostic factor of recurrence and postoperative survival,and its occurrence is mainly determined by biologic characteristics of the tumor.TME could decrease the incidence of CRMI.

Clinical Study of "Common Bile Duct Window" / 中国普外基础与临床杂志

0.05),but the thickness of gallbladder wall and the degree of cholecystitis affected the presence(P

Laparoscopic total mesorectal excision for low or ultralow anterior resection of rectal cancer with anal sphincter preservation / 中华外科杂志

<p><b>OBJECTIVE</b>To assess the feasibility of laparoscopic total mesorectal excision (TME) for low or ultralow anterior resection of rectal cancer.</p><p><b>METHODS</b>Excision of the mesorectum and low (ultralow) colo-anal anastomoses were performed laparoscopically in 62 patients with low rectal cancer based on the concept of TME and double stapling technique (DST).</p><p><b>RESULTS</b>Sixty-two operations with TME and DST were performed in a totally laparoscopic manner, and only one was converted to open procedures because of dysfunction of coagulation. The operative time was 125 min (110-210 min) and the operative blood loss 20 ml (5-80 ml). The time for bowel function recovery and post-operatively dietary intake was 1-2 days. Twenty-eight patients received postoperative analgesics. Average hospital stay was 8 days (5-14 days). Complications were observed in only 2 of the 62 patients, one had suffered from urinary retention and the other, anastomotic leakage.</p><p><b>CONCLUSIONS</b>Totally laparoscopic excision of the mesorectum for low or ultralow anterior resection of rectal cancer is a minimally invasive technique with sphincter preservation, less postoperative pain, and rapid recovery.</p>

The Effect of Membraniform preparation of Jie Mei Traditional Chinese Herbal Medicament for Women's Health Care on Hemorrheology in Experimental Rats / 昆明医科大学学报

It is reported in this article that the effect of Jie Mei Traditional Chinese Herbal Medica- ment for Women's Health Care on Hemorheology in experimental rats. The result suggested that the compound medicament had an evident action on antichrombosis.

Clinical study on the relation between cholesterol gallstone and insulin resistance / 中华内分泌代谢杂志

In this case-control study, the effect of insulin sensitivity on the genesis of cholesterol gallstones was not affirmed. However, raised 2h insulin level during glucose tolerance test and systolic blood pressure were risk factors in gallstone formation. Besides, less physical activity, lower serum total cholesterol and lower HDL-C concentration were found in patients with cholesterol gallstone.