Inhibition of herpes simplex virus type 1 and adenovirus type 5 by heterocyclic Schiff bases of aminohydroxyguanidine tosylate

Eleven heterocyclic Schiff bases of aminohydroxyguanidine tosylate (SB-AHGs), compounds I-XI, were tested for antiviral activity against herpes simplex virus type 1 (HSV-1) and adenovirus type 5 (Ad 5) via plaque reduction and virus yield reduction assays. This work was undertaken to test the hypothesis that low molecular weight SB-AHGs (MW < 235 for the free SB) make better antiviral agents than high MW SB-AHGs (MW > 300). The plaque reduction assay method demonstrated that three compounds, I, VII and IX, had moderate activity against HSV-1, with 50% inhibitory concentration (IC50) values of 38.0, 23.5 and 52.1 microM, respectively. Against Ad 5, compounds I, VIII and XI exhibited moderate activity, with IC50 values of 52.7, 19.3 and 5.1 microM, respectively. Among the compounds screened, compound I (1-[(3'-hydroxy-6'-methyl-2'-pyridyl)methylene]amino-3-hydroxyguanidi ne tosylate) was the most promising antiviral candidate, with selectivity indices (SI) of 10.2 (HSV-1) and 7.6 (Ad 5), respectively. Virus yield reduction assays indicated that compound I had less antiviral potency against HSV-1 than against Ad 5. The antiviral effects of compound I at a high input virus multiplicity of infection (MOI > 5) indicated that compound I had effective anti-adenoviral activity at 24 h post infection. This work demonstrated that some of SB-AHGs only have moderate antiviral activities against Ad 5 and HSV-1 viruses. In general, low MW SB-AHGs have low cytotoxicities to the host cells.     

pD2-, pA2- and pD2'-values of a series of compounds in a histaminic and a cholinergic system.

(1) Affinity and intrinsic activity values of 75 compounds for a histaminergic and a cholinergic system are presented. The quantitative correlations between the affinity values of 35 compounds and some physicochemical constants (Van der Waals volume, lipophilicity, number of hydrogen atoms on the protonated amine) are discussed. (2) Absence of systematic differences between pD2 and pA2 of partial agonists supports the assumption that these values are equivalent expressions of the same affinity. (3) The "mimetic moiety" in a number of the antihistaminic test compounds hardly contributes to their affinity. The affinity mainly depends on an interaction tendency with additional receptor areas. (4) The correlation between pA2 and pD2' of the whole series of compounds in the histaminergic system is artificial. The method only allows determination of both values if their ratio lies between certain limits. (5) The correlation between pA2 and pD2' for 16 closely related compounds in the guinea pig ileum and for nearly all compounds in the rat intestine has to be explained by an influence of the structural differences on drug transference and/or the less specific binding forces. (6) The metactoid receptors in the two systems are different structures. (7) Possible molecular modifications to maximize the separation of antihistaminic form cholinergic affinity are suggested.     

益母草的化学、药理和临床研究进展

查阅近20年有关文献，对益母草的化学成分、药理作用、临床应用研究进展进行综述。益母草主要含有生物碱类、黄酮类、二萜类、脂肪酸类、挥发油类等化合物；药理作用研究证明其具有调经止血、保护心肌缺血再灌注损伤、抗血小板聚集、降低血液黏度等作用；在临床上常用来治疗流产后出血、冠心病、心肌缺血、高黏血症、痛经等疾病。益母草具有广泛的药理活性，对其药效学物质基础进行深入研究和开发，将具有重要意义。     

Development of multifocal duodenal erosions after anti-Helicobacter pylori triple therapy.

BACKGROUND AND PURPOSE: Anti-Helicobacter pylori triple therapy is effective for healing duodenal ulcer (DU) diseases and reducing disease recurrence. However, multifocal duodenal erosions or shallow ulcers may develop after triple therapy. The purpose of this study was to investigate the incidence and outcome of duodenal erosions that developed after triple therapy. METHODS: A total of 106 Taiwanese with active DU and with H. pylori infection were enrolled in this study. All patients received anti-H. pylori triple therapy (i.e., 2 weeks of antimicrobial agents combined with treatment for 4 to 6 weeks with acid suppression agents). Follow-up endoscopy was performed immediately after stopping treatment. The incidence of multifocal erosions or shallow ulcers over the bulb and/or second portion of the duodenum was studied. Additional acid suppression agent was given for 4 weeks whenever duodenal erosions or shallow ulcers were found. RESULTS: Out of 106 patients, 11 (10.4%) were found to have multifocal duodenal erosions and/or shallow ulcers on the duodenal bulb and/or second portion of the duodenum at the end of treatment. Ten of the 11 patients with newly developed erosions had healed DU in the S1 or S2 stage, and all 11 had successful H. pylori eradication. The duodenal erosions and/or shallow ulcers of these 11 patients were healed after an additional 4 weeks of histamine-2-receptor antagonist therapy. CONCLUSIONS: Multifocal duodenal erosions and/or shallow ulcers were noted in around 10% of Taiwanese DU patients who received anti-H. pylori triple therapy. An additional 4 weeks therapy with acid suppression agents healed these lesions.     

Interventions to enhance the Quality of Life of older people in residential long-term care: A systematic review

PurposeIn residential long-term care (LTC), a growing interest exists in the older residents’ Quality of Life (QoL). The Active Ageing-concept (AA) extended this focus, since AA has the aim to enhance QoL by optimising the opportunities for health, participation and security. In LTCs, AA can be outlined by 9 determinants. This systematic review aimed at identifying interventions to improve the QoL of LTC-residents. These interventions were organised according to the AA-determinants.MethodsPubMed, Web of Science, Psychinfo and Sociological Abstracts were screened systematically. Articles were excluded when they only concerned a specific group of LTC-residents.ResultsThirty five relevant articles, encompassing 3910 subjects were found. These concerned interventions concentrating on one or more of the 9 AA-determinants. The largest proportion of interventions regarded the physical activity level or the psychological factors of the residents. Overall, no systematic effects on QoL could be found and a low methodological quality was generally present.ConclusionCurrently, studies aimed at enhancing the QoL of older LTC-resident are limited and often directed to physical and psychological interventions. The lack of a systematic effect on QoL is possibly related to the fact that these interventions were often not multidimensional, whereas QoL is a multidimensional concept.     

Palpebral emphysema following a dental procedure

Palpebral emphysema is a rare occurrence after a dental procedure. However, it can be associated with severe complications, such as soft tissue infection, pneumomediastinum, pneumothorax, optic nerve ischemia or even blindness. Early diagnosis and prompt management are mandatory for emergency physicians.