异落新妇甙的结构研究

从百合科菝葵属植物土茯苓(Smilaxg labra Roxb.)根茎的乙醇提取物中分得一个新的天然化合物(I),命名为异落新妇甙(isoastilbin)。根据元素分析,UV,IR,¹H-NMR,¹³C-NMR,2DNMR及FAB-MS,确定化合物I的结构为5,7,3',5'-四羟基二氢黄酮醇-3-O-α-L-鼠李糖甙。     

吡酮酸类抗菌药物的研究Ⅷ.1-对氟苯基-6-氟-1,4-二氢-4-氧-7-(1-哌嗪)噌啉-3-羧酸及其类似物的合成和构效关系

为探讨构效关系,合成了1-对氟苯基-6-氟-1,4-二氢-4-氧-7-(1-哌嗪)噌啉-3-羧酸及其喹啉、萘啶、吡啶[2,3-C]哒嗪环系类似物16个。测定了对大肠杆菌的MIC。用Hückel分子轨道理论(HMO)方法计算了四个母体环上电子密度。结果表明:环中氮的位置对药效团——3位羧基和4位羰基氧原子上电子密度的影响较大而影响其抗菌活性。喹啉、萘啶两环系的3位羧基和4位羰基氧原子上的电子密度较高,其体外抗菌活性较高;而噌啉及吡啶[2,3-C]哒嗪两环系的电子密度较低,其体外抗菌活性较低甚至消失。     

Ameloblastoma: analysis of 207 cases in a Nigerian teaching hospital.

OBJECTIVE: The aim of the study was to review all the cases of ameloblastoma seen at the Oral and Maxillofacial Surgery Clinic of the Lagos University Teaching Hospital, Nigeria, between 1980 and 2003. METHODS AND MATERIALS: In this retrospective study, case files and biopsy reports of new cases of ameloblastoma covering a 24-year period were retrieved and analyzed for sex, age on presentation, histologic type, and site distribution. RESULTS: A total of 207 cases of ameloblastoma were seen in the given period. One hundred and ninety-eight (95.7%) were benign, and 9 (4.3%) were malignant. A male-to-female ratio of 1.1:1 was found. The average ages on presentation for ameloblastoma and ameloblastic carcinoma were 31.67 and 46.44 years, respectively. The lesion was found to be more common in the premolar-molar region of the mandible. The most common histologic type was follicular ameloblastoma (25.1%). Nine (4.3%) cases of ameloblastic carcinoma were also reported. CONCLUSIONS: Ameloblastoma with a predilection for the posterior mandibular region is relatively common in our environment. Sex and site distributions are similar to previous reports in the literature.     

FDA evaluations using in vitro metabolism to predict and interpret in vivo metabolic drug-drug interactions: impact on labeling.

Recent advances in in vitro metabolism methods have led to an improved ability to predict clinically relevant metabolic drug-drug interactions. To address the relationships of in vitro metabolism data and in vivo metabolism outcomes, the Office of Clinical Pharmacology and Biopharmaceutics in the Center for Drug Evaluation and Research, Food and Drug Administration, evaluated a number of recently approved new drug applications. The goal of these evaluations was to determine the contribution of in vitro metabolism data in (1) predicting in vivo drug-drug interactions, (2) determining the need to conduct an in vivo drug-drug interaction study, and (3) incorporating findings into drug product labeling. Ten cases are presented in this article. They fall into two major groups: (1) in vitro data were predictive of in vivo results, and (2) in vitro data were not predictive of in vivo results. Discussion of these cases highlights factors limiting predictability of in vivo metabolic interactions from in vitro metabolism data. The integration of these findings into drug product labeling is also discussed.     

Prevalence of hepatitis B surface antigen among patients suspected of liver diseases in a Nigerian hospital

Hepatitis B virus (HBV) infection has been reported to be the aetiological factor for hepatocellular carcinoma (HCC), hepatitis and liver cirrhosis. This study was therefore carried out to determine the seroprevalence of hepatitis B surface antigen (HBsAg), a specific marker of HBV infection in patients with suspected liver diseases. The investigation was carried out among patients attending the University of Maiduguri Teaching Hospital (UMTH), Nigeria with clinical symptoms suggestive of liver diseases and others with non-specific clinical features during the period from 1990-1995. A total of 197 (38%) of 517 patients tested positive for HBsAg, 81 (49%) out of 144 with symptoms suggestive of hepatitis, 75 (50%) of 149 HCC and 10 (56%) of 18 liver cirrhosis were HBsAg positive. Comparison of the yearly total prevalence values of HBsAg for the six years under study showed no significant difference. Similarly, yearly prevalence values amongst patients with suspected liver diseases showed no significant differences. Nevertheless, significant difference, (P < 0.05) between the prevalence of HBsAg among suspected cases of liver diseases and others with non-specific signs and symptoms was observed. Similarly, HBsAg was statistically significantly higher among males than females. The high prevalence rate of HBsAg in our environment may be associated with the suspected cases of liver diseases, which are equally prevalent in our locality. Health education to prohibit traditional practices that could predispose individuals to HBV infections is emphasised. The incorporation of HBV vaccination in the national programme on immunization currently in use in Nigeria is highly recommended. This would be an effective method of preventing HBV infection from childhood.     

The antioxidant and neuroprotective effects of the Psychotria camptopus Verd. Hook. (Rubiaceae) stem bark methanol extract contributes to its antiepileptogenic activity against pentylenetetrazol kindling in male Wistar rats

A substantial number of epileptic patients are resistant to the current medication thus necessitating the search for alternative therapies for intractable forms of the disease. Previous studies demonstrated the acute anticonvulsant properties of the methanol extract of the stem bark of Psychotria camptopus (MEPC) in rats. This study investigated the effects of MEPC on pentylenetetrazole-kindled Wistar rats. Kindling was induced by intraperitoneal injection of pentylenetetrazole (37.5 mg/kg) on every alternate day, 1 h after each daily oral pretreatment of rats (8?≤?n?≤?10) with MEPC (40, 80 and 120 mg/kg), vehicle or diazepam (3 mg/kg) for 43 days. The kindling development was monitored based on seizure episodes and severity. Rats’ brains were collected on day 43 for the determination of oxidative stress parameters. The histomorphological features and neuronal cell viability of the prefrontal cortex (PFC) and hippocampus were also assessed using H&E and Cresyl violet stains. Chronic administration of pentylenetetrazole time-dependently decreased the latency to myoclonic and generalized seizures, and increased seizure scores and the number of kindled rats. MEPC and diazepam significantly increased the latencies to myoclonic jerks and generalized tonic-clonic seizures. These substances also reduced seizure score and the number of rats with PTZ-kindling. MEPC improved glutathione status and decreased lipid peroxidation in the brains of kindled rats. MEPC also exhibited neuroprotection against pentylenetetrazole-induced hippocampal and PFC neuronal damages. These results suggest that P. camptopus has antiepileptogenic activity, which might be related to the augmentation of antioxidant and neuroprotective defense mechanisms, and further confirm its usefulness in the management of epilepsy.

     

Suicide in Nigeria: observations from the content analysis of newspapers

BackgroundSuicide is a global public health problem and Nigeria is one of the epicentres of suicide in the world. However, there is a dearth of research exploring the epidemiological aspects of suicide in Nigeria.AimTo examine the demographic information and precipitating events for suicides in Nigeria by analysing the contents of newspaper reports of suicide.MethodsWe searched, collected, and analysed published news reports about suicide from 10 English newspapers in Nigeria. A total of 350 suicide reports were assessed between January 2010 and December 2019 after screening and sorting.ResultsThe mean (SD) age of the reported cases was 36.33 (15.48) years. Majority of the reported cases were male (80.6%), married (51.8%), students (33.6%), living in a semi-urban area (40.3%) and among the age group of 25–34 (25.3%). Hanging (48.6%) and poisoning (32.2%) were the most commonly reported methods of suicide. Financial constraints and marital conflicts were most commonly assumed precipitating factors.ConclusionThis study suggests that being male, married, or living in semi-urban areas are associated with suicide in Nigeria. Further community-based studies are warranted to generalise the findings and adopt appropriate preventive strategies.