Bioassay-guided isolation of novel and selective urease inhibitors from Diospyros lotus / 中国天然药物

Two new dimeric naphthoquinones, 5',8'-dihydroxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (1; Di-naphthodiospyrol D) and 5',8'-dihydroxy-5,8-dimethoxy-6,6'-dimethyl-7,3'-binaphthyl-1,4,1',4'-tetraone (2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin (3) and 8-hydroxy diospyrin (4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments. The fractions and compounds 1-4 were evaluated for urease activity and phosphodiesterase-I, carbonic anhydrase-II and α-chymotrypsin enzyme inhibitory activities. Compounds 1 and 2 and their corresponding fractions showed significant and selective inhibitory effects on urease activities. The IC values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 µmol·L, respectively, using thiourea (IC = 21 ± 0.11 µmol·L) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.

systematic review and meta-analysis comparing intravitreal ranibizumab with bevacizumab for the treatment of myopic choroidal neovascularisation

Intravitreal injections of ranibizumab [IVR] and bevacizumab [IVB] have both been used as treatments for myopic choroidal neovascularisation. We aimed to produce a meta-analysis of published literature comparing IVR with IVB for the treatment of myopic choroidal neovascularisation, by searching electronic databases from January 1950 to March 2013. Our search produced three suitable studies that reported on 117 patients in total. The results of the meta-analysis demonstrated that the mean number of lines improvement after IVR appeared better compared with IVB [fixed effects model: SMD = 0.46, 95% CI [0.09, 0.83], z = 2.44, p = 0.01]. The number of patients who had a greater than 3 line improvement was similar between groups [fixed effects model: RR = 0.95, 95% CI [0.67, 1.32], z = 0.33, p = 0.74]. At follow up there was no difference in number of those who had an absence of leakage [fixed effects model: RR = 1.04, 95% CI [0.93, 1.16], z = 0.64, p = 0.52]. There was no statistical significance between the two groups in relation to the number of injections [random effects model: SMD = -0.25, 95% CI [-1.12, 0.61], z = 0.57, p = 0.57]. Early evidence therefore suggests that intravitreal injections of ranibizumab are comparable to intravitreal injections of bevacizumab in the treatment of myopic choroidal neovascularisation. Both treatments result in a statistically significant increase in visual acuity with high numbers of patients maintaining stable vision. Further studies are still needed to strengthen results

Antipyretic and antinociceptive activity of Diospyros lotus L. in animals

<p><b>OBJECTIVE</b>To evaluate pharmacologically the traditional use of Diospyros lotus as antipyretic and antinociceptive in various animal models.</p><p><b>METHODS</b>In vivo experimental models were used in this study. Antipyretic activity of extract/fractions was evaluated in brewer's yeast induced hyperthermic mice while antinociceptive activity was studied in acetic acid induced writhing test at 50 and 100 mg/kg i.p.</p><p><b>RESULTS</b>The crude extract strongly ameliorated the induced pyrexia during various assessment times. Upon fractionation, the antipyretic effects were strongly augmented by the chloroform and ethyl acetate fractions of the plant. However, hexane and butanol fractions were insignificant in their effect as antipyretic. The extract showed marked inhibition on the noxious simulation induced by post acetic acid injection. The effect was strongly supported by other fraction expect hexane.</p><p><b>CONCLUSIONS</b>In short, our study scientifically validated the traditional use of the plant as antipyretic.</p>

Experiences of stigma among hepatitis B and C patients in Rawalpindi and Islamabad, Pakistan

Hepatitis B and C are chronic diseases with mental and social impacts which can result in poor quality of life. The aim of this study was to determine the experiences of stigma in a sample of hepatitis B- and C-positive patients in Pakistan. In a cross-sectional study, 140 inpatients and outpatients from 3 tertiary-care hospitals in Islamabad and Rawalpindi answered a semi-structured questionnaire about stigma experienced from relatives, friends, spouse and health-care providers, and about work/financial problems. The majority of patients [75%] said they had had to change their lifestyle, and significantly more were males than females. Stigma was marked in terms of disease transmission, with 66% of patients fearing that they could transmit the infection to others; 19% said that family members avoided sharing towels, soap and eating and drinking utensils. Marital relationships were affected for 51% of married patients who had told their spouse. Patients' comments showed a sense of family and societal discrimination resulting in feelings of disappointment and isolation

Developing learning outcomes and integrated curricula across a health sciences faculty

Every student should have a clear understanding of what is expected of them during their course of study and at the time of graduation. Improving the clarity for both students and teachers of the intended learning outcomes using outcomebased- education [OBE] will increase the relevance of learning opportunities and additionally provide a framework to help unify a curriculum. This paper describes how the Faculty of Medicine, Dentistry and Health Sciences at the University of Western Australia approached the specification and documentation of learning outcomes for its undergraduate courses, using examples from the Medicine course. It discusses how the Faculty began the journey of shifting the culture of the learning environment towards one focused on learner outcomes. The challenges faced and successes experienced offer insights into the adoption of OBE for others

Is intravenous paracetamol a useful adjunct for intraoperative pain?

Paracetamol is a safe and cost effective intravenous [IV] analgesic. This survey was conducted to assess the satisfaction of anesthetics with the intra-operative use of IV paracetamol as an adjunt for intra-operative pain relief. This cross-sectional survey was conducted for 3 months in a tertiary care university hospital in Karachi, Pakistan. All patients admitted for surgery and received IV paracetamol were enrolled. Data was collected by administering a pre-coded questionnaire to anesthetists about the patient and response to the IV paracetamol. In total 270 patients were enrolled. Of all, most were young males [59%] with American Society of Anaesthesiology [ASA] II status. In addition to paracetamol, pethidine was most often used. There was a 94% satisfaction rate and most anesthetics felt that the cost was justified. Heart rate was the variable most affected [60%]. Most anesthetists were satisfied with the use of IV paracetamol as an adjunct to intra-operative analgesia

Analytical approaches to paclitaxel, an anti cancer domain

Cancer is the uncontrolled growth of abnormal cells in the body. Symptoms of cancer depend on the type and location of the cancer. Paclitaxel obtained from Taxus brevifolia is an effective natural drug used in cancer treatment, so there arises a need of its estimation in biological fluids for the pharmacokinetic studies in clinical trials and in various pharmaceutical dosage forms including nanoparticles, cremophore based formulations and paclitaxel releasing stents. Literature survey reveals many chromatographic methods for estimation of paclitaxel by HPLC, LC-MS-MS and UPLC to get very accurate, precise and robust method with lower run time and higher recovery. An important step in the development of liposome-based formulations is estimation of the free drug concentration in the aqueous solution surrounding liposomes

Sonographic fetal biometry charts for a Pakistani cohort

This study aimed to develop growth centiles at different gestational weeks for fetal biparietal diameter, abdominal circumference, femur length and head circumference in a Pakistani cohort. Data were collected at a tertiary referral hospital from pregnant women at gestational ages 13-40 weeks referred for obstetric ultrasound as a part of routine antenatal care. A total of 1599 fetal sonographic biometric measurements were collected after screening for the inclusion criteria. For each measurement, separate regression models were derived to estimate the mean, standard deviation and reference percentiles at each week of gestational age for this cohort. The best fitting model for each variable was selected. These charts will help radiologists and clinicians in predicting dates of delivery, assessing fetal growth and identifying intrauterine fetal insufficiency in the Pakistani population

Young adult and giant cervical exostosis

Degenerative changes in the spine can result in the formation of osteophytes on the anterior surface of the cervical spine. Depending on their site, osteophytes can bring on clinical manifestations such as dysphagia, hoarseness, and stridor. We discuss an interesting case of a young adult patient who presented with dysphagia along with neck discomfort, and on investigation was found to be suffering from diffuse idiopathic skeletal hyperostosis. Here, we briefly portray the presenting features, radiographic findings, and management options

Aneurysmal bone cyst of pubis a rare presentation

Aneurysmal bone cyst is a benign usually expansile, solitary lytic lesion of bone; with blood filled cystic cavities, which tend to grow eccentrically. Such eccentric growth may, on occasion, attain considerable size before it is clinically recognized, particularly if the tumor arises in a deeply situated bone. Aneurysmal bone cyst of pubis is a rare entity. In the following case report, an aneurysmal bone cyst, originating from the superior pubic ramus, expanded into the groin and first manifested itself as a gradually increasing fullness in groin and pain especially with weight bearing. The size and location of this vascular tumor posed difficulties in treatment. It was managed by curettage with high speed burr and reconstruction of the defect with an iliac crest cancellous bone graft

Clinical characteristics and outcome of pediatric patients with stage IV Hodgkin lymphoma

While treatment outcomes for patients with Hodgkin lymphoma [HL] have improved remarkably, patients with disseminated disease still have a poorer outcome. Stage IV HL is often repported with other "advanced stage" categories, confusing the specific contribution of disease dissemination to the outcome. This single-institution report looks at characteristics and outcomes of this specific category. The medical records of pediatric HL patients [<14 years] from 1975 through 2003 were retrospectively reviewed and the data analyzed. Stage IV patients [n=67] had more poor -risk characteristics than patients in stages I-III [n=300] [B symptoms 86.6% vs. 19.3%, bulky disease 57.6% vs. 45.5% and mediastinal mass 77.6% vs. 29.7%; P < .001 for all characteristics]. The liver was the most common extralymphatic site [in 51.5% of patients with stage IV diseease. Stage IV patients received chemotherapy [CT] alone [n=55] or combined modality therapy [CMT] [n=12]. Fifty-four patients [80.6%] achieved complete remission, 2 [3%] partial remission, 10 [14.9%] had progressive disease and 1 was lost to follow up. Overall survival was 79.4% and event-free survival [EFS] was 63.9% at 5 years. There was a non-significant benefit for CMT [OS=91.7% v. 77.1%, P=.3; EFS=70.7% v. 62.7%, P=.3]. Ten of 12 relapsed and only 1 of 10 progressive disease patients were salvaged. On multivariate analysis, failure to achieve complete remission with CT was associated with a poorer outcome. Stage IV disease is associated with poor risk features and confers a worse outcome than stage I-III disease. Achievement of complete remission with CT is an important prognostic feature. Slow responders may require novel and/or aggressive therapy to achieve complete remission