HIV-1 fusion inhibitors are a new class of anti-HIV compounds, which block the entry of HIV into target cells through preventing the fusion between viral and cell plasma membrane and thus interrupt the initial steps of viral replication. T-20 (enfuvirtide), which has been clinically approved as the first fusion inhibitor of HIV-1 by U.S. FDA in 2003, can suppress replication of HIV variants with multi-drug resistance to reverse transcriptase and protease inhibitors. Peptides and small molecules display potent anti-HIV fusion activities by targeting gp41 thus inhibit its fusogenic function. In recent years, with the development of studies on the molecular mechanism of HIV membrane fusion process and the function of gp41, many new fusion inhibitors are found and some have been in advanced clinical trials. This review discusses recent progress in the development of HIV-1 fusion inhibitors targeting the gp41.

Objective To investigate the relationship between the TRAb-producing cell precursors and different clinical stages of Graves' disease.Methods Peripheral lymphocytes were infected with Epstein-Barr virus,a kind of lymphocyte precursor stimulator,and were stimulated to produce TRAb.Results Of the total wells containing Ig-producing B cell precursors,there were 34.6% and 29.1% from 2 untreated patients,30% from 1 relapsing patient and only 1.3% and 3.8% from 2 healthy controls that secreted TRAb,respectively.As for the wells containing B cell precursors from 2 remission patients with undetectable TRAb in circulation,the percentage (10.7%) of TRAb-containing wells from one was higher than that from the other (5.3%).And the latter had similar percentage of TRAb-positive wells with the controls.The isotype of TRAb in supernatants of our EBV-transformed B lymphocytes was predominantly IgM.Conclusion The frequencies of TRAb-specific precursors were different at three distinct clinical stages of the disease.

Objective To investigate the heritability of Graves′ disease (GD) and to discuss its clinical significance. Methods The heritability of GD was calculated using Falconer′s formula and by investigating the GD numbers of 1968 first relatives of 526 established GD patients. Results The heritability of GD was 45%, appearantlymuchlowerthanthoseofprevious reports in China. Conclusion The onset of GD is affected by both inheritant and environmental factors, the latter seems to be predominant over the former.

Objective To observe the clinical therapeutic effect of Capsule Long-Bi-Xiao(LBX) in treating benign prostatic hyperplasia(BPH).Methods 64 patients of deficiency of Qi and blood stasis type suffered with BPH were randomly divided into two groups.30 patients in the control group were treated with Capsule Long-Bi-Shu,while other 34 patients in the treated group were treated with LBX.Each group was observed for there months respectively.Results LBX decreased the international index of prostatic symptom(I-Pss) and the bother score(BS),improved the prostatic symptoms,raised the peak flow rate(Qmax) and the average flow rate(Qave),shrinked a portion of patients′ volume of prostate gland,reduced the volume of residual urine.After treatment,in the treated group,I-PSS and BS were reduced distinctly,and Qmax and Qave were heightened obviously,which was more effective than those in the control group.Conclusion LBX can achieve good action in the therapy of BPH by improving clinical symptoms,diminishing the volume of prostate and ameliorating the difficulty of urination.

Aim To study the analgesic effect of geraniol on neuropathic pain and to explore the possible mechanism.Method A neuropathic pain rat model of Spared Nerve Injury(SNI) was established to measure changes in the threshold of paw withdrawal before and after i.p.administration of geraniol.Patch clamp whole-cell recording was performed to measure activity of sodium channels using ipsilateral L3/L4/L5 dorsal root ganglion(DRG) cells isolated from the SNI rats.In addition, HEK 293 cells expressing hNav1.7 and hTRPA1 channels were used for measuring the changes in channel activities with or without geraniol by whole-cell patch clamp.Results Geraniol had a fast analgesic effect on hypersensitivity of mechanical pain in the SNI model.It significantly inhibited sodium channels on DRGs isolated from SNI rats and hNav1.7 but not hTRPA1 channels expressed by HEK293 cells.However, high concentrations of geraniol facilitated the activation of HTRPA1 channel stimulated by AITC.Conclusion Geraniol may abirritate hypersensitivity of mechanical pain in the SNI model by specifically inhibiting Nav1.7 channel activity on the DRG cells.

Objective To investigate the anti-tumor effects of a combination of Kanglaite injection (KI) and photodynamic therapy (PDT) on human pancreatic cancer SW1990 xenograft in nude mice.Methods The animal model of human pancreatic cancer was developed by suturing small pieces of SW1990 tumors into the dorsum of nude mice.60 rats were randomly divided into six groups:group A ( control group without treatment),group B ( receiving 1.25g/kg KI via the tail vein prior to PDT and continuously for 10 days),group C (receiving 2.5g/kg KI via the tail vein continuously for 10 days),group D (PDT group,2 mg/kg Photosan 48h prior to laser irradiation),group E ( group B + group D),group F ( group C + group D)with 10 rats in each group.The tumor sizes were measured twice per week.The mice were sacrificed on the 14th day of PDT treatment.The tumor was took out and weighted and the tumor inhibitory rate was analyzed.Results The tumor volumes of group A to F were 9550.08±52.46)mm3,(519.71±46.44)mm3,(405.29±38.67 ) mm3,( 199.27±37.37) mm3,( 107.47±14.13 ) mm3 and (75.58±12.53 )mm3,the weight of group A to F were (0.82±0.08)g,(0.77±0.06)g,(0.61±0.06)g,(0.41±0.05)g,(0.28±0.04)gand (0.16±0.04)g,respectively.The tumor volumes and tumor weights of the two combined groups were significandy smaller than those in the other groups (P＜0.05).The combination group of 1.25 g/kg KI increased the tumor inhibitory rate from 50% in PDT group to 65.9%.The combination group of 2.5 g,/kg KI increased the tumor inhibitory rate to 80.5%.Conclusions KI had attenuated effect on PDT therapy,and the combination of KI and PDT could significantly inhibit the tumor growth.

Objective Using Sevoflurane in general anesthesia in cesarean operation , to evaluate change of stress response by monitoring maternal plasma concentrations of HSP70 and the expression of HSP70 in the placenta tissue and provide an ideal and basis of safty and effectiveness in obstetric general anesthesia. Methods Sixty caesarean operation puerperas undergoing general anesthesia in women and children′s hospital of Guangdong province were selected and randomly divided into the sevoflurane group (S group) and the propofol group (P group) through random number table, each group had 30 cases. We tested materal blood concentration and expression of HSP70 in placenta tissue. Results HSP70 concentration (when) in the P group was significantly higher than that before surgery (P < 0.05); Comparing with the group S at the same time point, the difference was statistically significant (P < 0.05); In expression of HSP70 in placental tissue, P group was obviously higher than the S group (P < 0.05), Conclusion Sevoflurane used in general anesthesia for cesarean operation is safe and effective , which can reduce the concentration of HSP70 in maternal blood and expression of HSP70 in placental tissue.

Objective To evaluate clinical outcomes of treating displaced intra-articular calcaneal fractures with Orthofix external fixation (EF) in comparison with open reduction and internal fixation (ORIF).Methods Between February 2013 and December 2014,39 patients with 41 calcaneal fractures were treated operatively and fully followed up at our department.They were 27 men and 12 women,aged from 27 to 56 years(average,42.5 years).The left foot was affected in 15 cases and the right in 26.By the Sanders classification,there were 11 cases of type Ⅱ,22 ones of type Ⅲ and 8 ones of type Ⅳ.The 5 open fractures were Gustilo type Ⅰ (2 cases) and Gustilo type Ⅱ (3 cases).Of the 11 fractures complicated with soft tissue injury,4 were Tscherne-Oestern type Ⅰ and 7 Tscherne-Oestern type Ⅱ.The patients were divided into group EF (25 cases) and group ORIF (16 cases) according to the operation they had received.The 2 groups were compared in intraoperative indexes and follow-up radiological data.The American Orthopaedic Foot and Ankle Society (AOFAS) scores for ankle and hindfoot were recorded at the final follow-up for every patient.Results The mean duration of surgery,intraoperative bleeding,time for hospitalization and bone healing in group EF were significantly less than in group ORIF (P ＜ 0.05).There were no significant differences between the 2 groups in follow-up duration,AOFAS score,Bthler angle,Gissane angle,calcaneal axis,calcaneal horizontal length,tuberosity height,hillock calcaneal height,calcaneal width,or talar inclination angle (P ＞ 0.05).According to the AOFAS scores at the final follow-ups,15 cases were rated as excellent,8 as good and 2 as fair in group EF while 10 were rated as excellent,5 as good and one as fair in group ORIF.Conclusions All types of calcaneal fracture can be treated using Orthofix external fixation which may lead to advantages of earlier surgery regardless of soft tissue condition,minimal invasiveness with less devascularization to the calcaneus and decreased risk of complications,and good clinical outcomes.

[Summary] Sixty-one patients suffering from pituitary apoplexy( PA) were mainly diagnosed according to pathologic findings, and were collected from case record, pathology, and MRI databases. They were classified into 4 types according to the clinical condition: the insidious type was characterized with only positive pathological findings;the asymptomatic type had both positive pathologic and MRI findings; the subacute type had PA associated symptoms longer than 2 weeks; and the acute type had PA associated symptoms for 2 weeks or less. The latter 2 types had positive pathological and MRI findings additionally. The basic lesions, acute or chronic symptoms, endocrinopathies and MRI findings were compared among 4 types. Results showed as followed. In all patients, there were headache(60. 7% ), blurred vision(55. 7% ), vomiting(21. 3% ), and dizziness(14. 8% ). Apoplexy associated symptoms comprised severe headache (24. 6% ), rapid vision loss (29. 5% ), and blepharopotosis or diplopia (9. 83% ). Insidious, asymptomatic, subacute, and acute types were composed of 15 (24. 6% ), 9 (14. 8% ), 19 (31. 1% ), and 18 (29. 5% ) cases, respectively. Aging and intracranial space-occupying symptoms as first complaint showed increasing trend from mild to severe types(both P<0. 05), while in chronic course it showed decreasing trend(P<0. 05). Acute massive symptoms(P<0. 01), and non-functional tumor(P<0. 01) in the 2 clinical types were much more frequent than in the two mild types. Half or more pituitary-target glands showed impaired functions in each type, and the impairment showed increasing trend through mild to severe types(P<0. 01). The present study provided a brief typing system in order to expand PA concept to a wider span covering various conditions. Some differences in tumor composition and endocrinopathies existed among the four types.

Objective To observe the occurrence and risk factors of arrhythmia in chronic kidney disease (CKD) patients in different stages of renal function. Methods A total of 405 CKD patients were enrolled in this study and none of them received renal replacement therapy.The 24 h dynamic electrocardiogram (DCG) was performed,and baseline characteristics were compared.Multivariable Logistic regression analysis was used to examine the relationship between the severe arrhythmia and the potential risk factors,such as age,gender,CKD stage,diabetes,hypertension,hyperpotassaemia,left ventricular hypertrophy (LVH),etc. Results There were 69 patients (17.04％),79 patients (19.51％),82 patients (20.25％),88 patients (21.73 ％) and 87 patients (21.48％) in CKD stage 1,2,3,4 and 5,respectively.As high as 45.68％ of all the patients had severe arrhythmia,represented by 27.54％,29.11％,42.68％,57.95％ and 65.52％ in CKD stages 1-5 respectively.The occurrence of severe arrhythmia increased as the eGFR decreased in CKD stages 2,3,4 (p＜0.05).On multivariable Logistic regression analysis,the occurrence of severe arrhythmia was related to LVH,CKD stage,diaberes hyertension and hyperpotassaemia are signidicantly assoxiated with severe arrhythmia.