走出抗感染药不合理使用的误区

抗感染药物就是在非常低浓度下对所有的生命物质有抑制和杀灭作用的药物.目的 是把病原体杀灭,控制疾病,最终治愈疾病.但在治愈并挽救了许多患者生命的同时,也出现了由于抗感染药物的不合理应用而导致的不良后果,如不良反应的增多,细菌耐药性的增长,以及治疗的失败,给患者健康乃至生命造成重大影响.本文根据目前用药情况,就抗感染药物的临床应用问题讨论分析.     

原小檗碱类化合物的构效关系研究进展

原小檗碱类化合物是异喹啉生物碱中一个重要组成部分，具有多种药理活性。综述该类化合物的抗疟、抗菌、抗肿瘤构效关系研究进展，为以中草药作先导物进行的结构改造及新药开发，提供思路和有益信息。     

抗微生物药物的肝脏毒性

抗微生物药物的应用可引起各种各样的肝脏损害,范围从轻微、无症状的肝生化指标异常到威胁生命的暴发性肝脏衰竭,其机制不十分清楚,但反应一般是不可预测性和特异体质性的。在大多数病例中,抗微生物药物引起的肝毒性是自限性的,停药恢复。但随着慢性病毒和细菌感染的日益流行,常常需要长期的多药联合治疗,因此,早期认识和合理处理肝脏损害显得日益重要。     

鞣酸小檗碱的制备工艺改进

鞣酸小檗碱的制备工艺改进ＩＭＰＲＯＶＥＤＰＲＥＰＡＲＡＴＩＯＮＯＦＢＥＲＢＥＲＩＮＥＴＡＮＮＡＴＥ刘文江＊李凤双王卫平张晓明ａ孙菊英ａ（解放军兰州医学高等专科学校，兰州７３００２０；ａ甘肃省药品检验所，兰州７３００００）ＬＩＵＷｅｎ－Ｊｉａｎｇ＊，Ｌ...     

小檗碱的抗病原生物作用研究进展

小檗碱又名黄连素,具有非常广泛的药理活性,但其准确的作用靶点至今不清.本文主要综述其抗病毒作用、抗细菌作用、抗真菌作用及其作用的构效关系和分子机制,对揭示生命现象的本质,发现新药靶点具有重要意义,也为小檗碱的结构优化改造和应用研究提供新的线索.     

四氢小檗碱季铵化合物的合成及其抗心律失常活性

以具有心血管活性的四氢小檗碱类生物碱为先导物，结合某些钾通道阻滞剂的结构特征，设计并合成了１４个未见文献报道的四氢小檗碱季铵化合物（Ｉ１－１４），其结构均经波谱分析及元素分析得到确证，初步的药理试验表明，大多数化合物对乌头碱静脉灌注所诱发的大鼠心律失常有不同程度的保护作用，其中化合物（Ｉ６）的活性最强，保护该模型室必早搏、室性心动过速和心脏猝死的ＥＤ５０分别为２．３２ｍｇ／ｋｇ，１．９５ｍｇ＝ｋｇ     

小檗碱的药理学研究进展

目的：了解近年来国内、外关于小檗碱药理学的最新研究进展。方法：查阅美国国立生物技术信息中心（NcBI）和相关专业学术期刊全文数据库1993--2013年有关小檗碱的研究文献,对小檗碱的药理学研究进展作一整理归纳。结果与结论：小檗碱可通过抑制花生四烯酸代谢,调节葡萄糖代谢途径,降低血浆丙氨酸氨基转移酶和血浆天冬氨酸氨基转移酶,直接嵌入微生物DNA,拮抗肿瘤细胞的分化、侵袭、加速凋亡,具有对神经系统的保护等多种分子机制,进而起到抗血小板、降糖、保肝、抗茵、抗肿瘤、治疗神经系统疾病的作用,具有广阔的应用前景。     

小檗碱的研究进展

综述了小檗碱在分子生物学、药理和临床研究方面的最新进展，特别是近些年来生物化学和分子生物学的成果，对进一步认识小檗碱在体内的作用是有益的。     

Anticancer and antimicrobial activities of scorpion venoms and their peptides

Scorpion venom is a natural biological resource that contains several components, which are not only responsible for death but also have a potential therapeutic activity. Scorpion venom has been used as traditional and folk therapy in various pathophysiological conditions. Now, many scorpion venom components have been purified and identified. Based on the available structural and functional information of these components, the scientists can produce new venom-derived medications with potential therapeutic activity against many important diseases. This review focused on the importance of scorpion venoms and their peptides against cancer and microbes.     

Synthesis and Antimicrobial Activity of 5-Imidazolinone Derivatives

Several 4-arylidene-2-phenyl-1-(2,4,5-trichlorophenyl)-1H-imidazol-5(4H)-ones (4a-q), N-(4-benzylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-4-chlorobenzamides (5a-o) and N-(4-benzylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-2,4-dichlorobenzamides (6a-m) were prepared. All newly synthesized compounds have been tested for their antibacterial activity against gram (+)ve and gram (−)ve bacteria and also on different strains of fungi. Introduction of OH, OCH₃, NO₂, Cl and Br groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.     

Antimicrobial Metabolites from Three Serbian Caloplaca.

Abstract

Methanol extracts of three Caloplaca. species showed broad-spectrum antifungal and antibacterial properties against some human and plant pathogens. Fractionation with methylene chloride and isolation of pure anthraquinone derivatives substantially increased the level of antimicrobial activity. Eight anthraquinone derivatives were isolated from the three species. 1-O.-Methylparietin and 8-O.-methylparietin were isolated from lichens for the first time. Minimum inhibitory concentrations for the extracts were found to be 80–320 µg/ml for bacteria and 40–320 µg/ml for fungi, and the pure anthraquinones range from 20 to 320 µg/ml for bacteria and from 20 to 160 µg/ml for fungi.     

Antimicrobial and anti-inflammatory properties of Funtumia elastica

Context: Funtumia elastica (Preuss) Stapf. (Apocynaceae) has a long ethnopharmacological history for uses such as treatment of whooping cough, asthma, blennorhea, painful menstruation, fungal infections, and wounds.

Objective: To investigate the antimicrobial and anti-inflammatory properties of ethanol extracts from the leaves and stem bark of Funtumia elastica based on its ethnopharmacological uses and also determine the secondary metabolites present in the extracts.

Materials and methods: The antimicrobial activities of ethanol leaf and bark extracts of F. elastica were determined using the microdilution technique (MIC determination) and agar diffusion method using 10, 25, and 50?mg/mL concentrations against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, Candida albicans, Aspergillus flavus and Aspergillus niger as test organisms. Anti-inflammatory activities of the doses of extracts at 30, 100, and 300?mg/kg per body weight were determined by carrageenan-induced edema in the footpad of 7-day-old chicks and the foot volumes measured at hourly interval post-treatment for 5?h.

Results: The MIC ranges of both ethanol leaf and bark extracts against the test organisms were 125 (lowest MIC) to1550 µg/mL (highest MIC) and 125 (lowest MIC) to 1750 µg/mL (highest MIC), respectively. The ethanol leaf and bark extract of F. elastica showed significant anti-inflammatory activity (p ≤ 0.001) at 30, 100 and 300?mg/kg. Preliminary phytochemical screening revealed that F. elastica bark contains hydrolysable tannins, sapogenetic glycosides, steroids and saponins while the leaves contain hydrolysable tannins, flavonoids, starch and alkaloids. Tannin contents of the leaf and stem bark were 2.4 and 1.3% w/w (related to the dried material), respectively.

Discussion and conclusion: Both ethanol leaf and bark extracts of F. elastica showed antimicrobial and anti-inflammatory activities and these pharmacological properties may be responsible for the ethnomedicinal uses of the leaves and stem bark of the plant.     

Antimicrobial Activity of Methanol Extracts of Mosses from Serbia

Antibacterial and antifungal activity of methanol extracts of the mosses Pleurozium schreberi (Willd. Ex Brid.) Mitt. (Hylocomiaceae), Palustriella commutata (Hedw.) Ochyra (Amblystegiaceae), Homalothecium philippeanum (Spruce) Schimp. (Brachytheciaceae), Anomodon attenuatus (Hedw.) Huebener (Anomodontaceae), Rhytidium rugosum (Hedw.) Kindb. (Rhytidiaceae), Hylocomium splendens (Hedw.) Schimp. (Hylocomiaceae), Dicranum scoparium Hedw. (Dicranaceae), and Leucobryum glaucum (Hedw.) Ångstr. (Leucobryaceae), were tested against six bacterial and seven fungal species by microdilution and disc diffusion methods. The extract of A. attenuatus possessed the highest antibacterial activity (MIC of 1.25–5.0 mg/ml and MBC of 2.5–5.0 mg/ml), while L. glaucum extract showed the lowest activity (MIC of 20.0–25.0 mg/ml and MBC of 25.0 mg/ml). The best antifungal activity was obtained from P. schreberi extract (MIC of 0.5 mg/ml and MFC of 2.5–5.0 mg/ml, while the lowest antifungal potential was obtained from A. attenuatus (MIC 2.5–5 mg/ml and MFC 10 mg/ml). The extracts proved to be more active against Gram (+) bacteria than Gram (?) and showed strong antifungal activity.     

抗丙型肝炎病毒药物的研究进展

丙型肝炎（hepatitis C,HC）是一种发病率高、病死率高的传染病,全球约1.8亿人感染丙型肝炎病毒（hepatitis Cvirus,HCV）,至今无法治愈.本文概述了近几年来抗HCV药物,包括干扰素及利巴韦林、特殊靶向治疗药物和免疫调节剂等的研究进展.     

Recent advances in sialidase inhibitors

Viruses and bacteria cause diseases of vast economic importance. Sialidase inhibitors offer an opportunity to prevent or ameliorate these diseases. They have been investigated ostensibly as antiviral agents particularly against influenza viruses. The patent literature covering sialidase inhibitor compounds, their design and synthesis is reviewed from 1995 to mid-1998 with reference to the primary scientific literature. Patents are discussed by company or institution. The importance of different compound types is indicated.     

抗真菌药物作用靶位的研究进展

近年来,随着真菌感染问题的日趋严重,研究开发安全、新型和有效的抗真菌药物显得尤为重要。抗真菌药物根据其作用靶位分为抑制真菌细胞壁、细胞膜、蛋白质和核酸合成及抑制电子传递等5种类型。现从这5个方面对抗真菌药物的作用靶点研究进展作一概述。     

Antimicrobial Screening of Actinobacteria using a Modified Cross-Streak Method

Out of the 30 actinobacterial cultures screened for antimicrobial activity, 28 cultures were found to produce active products against various pathogenic microorganisms such as Gram-negative, Gram-positive bacteria and yeast, using a modified cross streak method. The modified method helped in easy quantification of results and also in ruling out probable mutual antibiosis. The actinobacterial strains that showed the ability to produce antimicrobial compounds belonged to Streptomyces (53%), Micromonospora (13%) and Actinomadura (10%) genera. Streptomyces sp. strain MMA-5 showed the highest multispecific antibiosis efficiency score value. Broad antibiotic spectrum activity was exhibited by Streptomyces sp. strain MMA-2 and Micromonospora sp. strain MMA-8. The multidrug resistant human pathogenic yeast strain Candida albicans was inhibited by 18 actinobacterial strains.     

Antimicrobial Stewardship Programs: Comparison of a Program with Infectious Diseases Pharmacist Support to a Program with a Geographic Pharmacist Staffing Model

Background:

Stewardship of antimicrobial agents is an essential function of hospital pharmacies. The ideal pharmacist staffing model for antimicrobial stewardship programs is not known.

Objective:

To inform staffing decisions for antimicrobial stewardship teams, we aimed to compare an antimicrobial stewardship program with a dedicated Infectious Diseases (ID) pharmacist (Dedicated ID Pharmacist Hospital) to a program relying on ward pharmacists for stewardship activities (Geographic Model Hospital).

Methods:

We reviewed a randomly selected sample of 290 cases of inpatient parenteral antibiotic use. The electronic medical record was reviewed for compliance with indicators of appropriate antimicrobial stewardship.

Results:

At the hospital staffed by a dedicated ID pharmacist, 96.8% of patients received initial antimicrobial therapy that adhered to local treatment guidelines compared to 87% of patients at the hospital that assigned antimicrobial stewardship duties to ward pharmacists (P < .002). Therapy was modified within 24 hours of availability of laboratory data in 86.7% of cases at the Dedicated ID Pharmacist Hospital versus 72.6% of cases at the Geographic Model Hospital (P < .03). When a patient’s illness was determined not to be caused by a bacterial infection, antibiotics were discontinued in 78.0% of cases at the Dedicated ID Pharmacist Hospital and in 33.3% of cases at the Geographic Model Hospital (P < .0002).

Conclusion:

An antimicrobial stewardship program with a dedicated ID pharmacist was associated with greater adherence to recommended antimicrobial therapy practices when compared to a stewardship program that relied on ward pharmacists.