喹诺酮类药物及莫西沙星的药理作用特点

喹诺酮类抗菌药物(QNs)是由萘啶酸发展起来的合成抗菌药物,都具有吡啶酮酸的共同结构,通过抑制DNA促旋酶,阻断DNA的复制而产生抗菌作用.新一阶段QNs代表药莫西沙星(拜复乐),既保持了早期QNs对G-菌良好的抗菌活性,又增强了对G+菌、"非典型"病原体和厌氧菌的抗菌活性;口服吸收快速完全,现就其特点综述如下.     

氨噻肟唑头孢菌素(SCE-1365)的抗菌活性

氨噻肟唑头孢菌素(Cefmenoxime,SCE-1365,A-50912)是一种有治疗价值的、新型的半合成头孢菌素。本文以琼脂稀释法或肉汤稀释法比较SCE-1365与唑啉头孢菌素、噻吩甲氧头孢菌素和羟苄四唑头孢菌素对486株细菌的抗菌活性,同时比较SCE-E65与氨噻肟头孢菌素(HR756)对114株细菌的抗菌活性。实验结果表明,SCE-1365和HR756的抗菌谱极广,抗菌活性几乎相同,除金葡菌外,两者对所有的需氧菌和兼性需氧菌的活     

头孢噻肟国产品与联邦德国产品对常见病原菌的体外抗菌活性比较

头孢噻肟(Cefotaxime,HR-756,CTX)是一种广谱、高效、低毒的第三代头孢菌素,对β-内酰胺酶很稳定。其抗菌谱广,对肠杆菌科菌有强大的抗菌活性,对金色葡萄球菌仍有抗菌活性,对绿脓杆菌也有一定作用。 四川抗菌素工业研究所新近合成了国产的头孢噻肟钠。本文报告头孢噻肟国产品(效     

稠环磺酰胺衍生物的合成与抗菌活性研究

为了寻找抗菌候选化合物,在前期研究基础上,18个稠环磺酰胺衍生物被设计合成,经1H NMR、13C NMR和MS确认结构.采用两倍稀释法对目标物进行体外抗菌活性测试,结果表明:该类衍生物对所测细菌有不同程度的抑制活性,尤以化合物Ⅱi、Ⅱr的抗菌活性最为突出,其中前者对金葡菌(S.aureus)、大肠埃希菌(E.coli...     

查耳酮的合成及体外抗真菌活性

目的合成查耳酮类化合物并测定其抗真菌活性. 方法利用Claisen-Schmidt反应合成查耳酮,并针对四种真菌(白色念珠菌、新生隐球菌、烟曲霉菌、红色毛癣菌)做了体外抗真菌活性筛选. 结果显示所合成化合物大多具有体外抗真菌活性,尤其化合物8, 其针对浅表菌的抗真菌活性与氟康唑相当.本文还对部分查耳酮的合成做了一些探索.结论所合成的查耳酮均有不同程度的抗真菌活性,其化学结构差异与抗菌活性相关.     

环丙沙星与头孢甲肟不宜配伍

环丙沙星具广谱抗菌作用,尤其对需氧革兰阴性杆菌抗菌活性高,对多重耐药菌也具有抗菌活性,对青霉素耐药的淋病奈瑟菌、产酶流感菌和莫拉菌属均具有高度抗菌活性;头孢甲肟为半合成的第3代头孢霉素,抗菌谱与头孢噻肟相近,这两种药在临床广泛应用。我们在护理工作中发现,上述两种     

环丙沙星与头孢甲肟不宜配伍

环丙沙星具广谱抗菌作用,尤其对需氧革兰阴性杆菌抗菌活性高,对多重耐药菌也具有抗菌活性,对青霉素耐药的淋病奈瑟菌、产酶流感菌和莫拉菌属均具有高度抗菌活性;头孢甲肟为半合成的第3代头孢霉素,抗菌谱与头孢噻肟相近,这两种药在临床广泛应用。我们在护理工作中发现,上述两种     

一种新型广谱多肽类抗生素——Gratisin的类似物

Tamaki等设计并合成了多肽类抗生素gratisin(GR)的类似物——环(-Val-Orn-Leu-D-Phe-Pro-D-Lys-)2,这种类似物对所有革兰阳性和革兰阴性受试菌都有强大的抗菌活性,并且对铜绿假单孢菌IFO 3080的活性是短杆菌肽S(gramicidin S,GS)的2倍。     

氟喹诺酮类抗菌药prulifloxacin

日本Ｓｈｉｎｙａｋｕ公司的科学家合成了一系列(1,3)硫氮杂环(3,2ａ)喹诺酮3羧酸及其酯类化合物,并评价它们的抗菌活性。发现化合物ｐｒｕｌｉｆｌｏｘａｃｉｎ(ＮＭ441)具有令人满意的药动学性质,动物实验的口服活性优于环丙沙星。抗菌活性　ｐｒｕｌｉｆｌｏｘａｃｉｎ是氟喹诺酮类抗菌前药,其活性代谢物是ＮＭ394。体内外实验表明,ＮＭ394具有很强的广谱抗菌活性,它对Ｇ+菌的抗菌活性与氧氟沙星和环丙沙星类似,对Ｇ-菌的活性与环丙沙星相同。对肠杆菌和绿脓杆菌,ＮＭ394则有更强的活性。ＮＭ394和环丙沙星一样可抑制大多数厌氧菌,但是对…     

硫酸头孢匹罗类似物的合成及其抗菌活性研究

目的 研究硫酸头孢匹罗类似物的合成及其抗菌活性.方法 以7-氨基头孢烷酸(7-ACA)为原料,在三乙胺催化下与苯并噻唑硫醇活性酯(MAEM)缩合得头孢噻肟酸,然后在KI作用下与取代吡啶进行3-位取代反应,最后硫酸成盐得目标化合物,并通过平皿二倍稀释法对它们的体外抗菌活性进行评价.结果 合成的12个目标化合物均未见文献报道,其结构经MS,IR和~1H-NMR确证.结论 初步体外抗菌活性实验结果表明,化合物1a对革兰阴性菌的活性总体上与硫酸头孢匹罗相当,特别是对大肠埃希菌和铜绿假单胞菌的活性优于硫酸头孢匹罗.     

Antibacterial Activity of Some Medicinal Plants of Papua New Guinea

Crude drug samples were prepared from stem bark of 16 medicinal plants belonging to 9 different families, and screened for antibacterial activities against Gram positive (Bacillus subtilis and Staphylococcus aureus) and Gram negative (Pseudomonas aeruginosa and Escherichia coli) bacteria. Most of them showed good antibacterial activity against Gram positive bacteria, and some of them exhibited antibacterial activity against Gram positive as well as Gram negative bacteria.     

浙江沿海海洋细菌抗菌活性及代谢产物的初步研究

目的 对浙江沿海海洋细菌进行抗菌活性筛选,并初步研究活性菌株代谢产物的结构.方法 用琼脂块法进行抗菌活性筛选,利用高效液相等手段对其代谢产物进行分离纯化,利用核磁共振和质谱等手段对活性化合物进行结构鉴定.结果 与结论共发现31株活性菌株,选择其中6株活性菌株进行研究,对其中活性较强的5个化合物进行结构鉴定,初步确定其化...     

石榴皮鞣质的抗菌活性及其对金黄色葡萄球菌的抗菌机制

目的:研究石榴皮鞣质(tannins from Pericarpium Granati,TPG)的抗菌活性及对金黄色葡萄球菌(Staphylococcus aureus,SA)的抗菌机制。方法:实验采用牛津杯法和试管二倍稀释法研究了石榴皮鞣质对5种不同细菌的抗菌活性,并以药物敏感性最强的金黄色葡萄球菌为供试菌,通过测定菌体胞外碱性磷酸酶(AKP)含量、胞外钾离子(K⁺)浓度、大分子核酸的吸光度值、胞内和胞外总三磷酸腺苷酶(T-ATPase)、聚丙烯酰胺凝胶电泳(SDS-PAGE)和透射电镜(TEM)观察,研究了石榴皮鞣质对金黄色葡萄球菌的抗菌机制。结果:石榴皮鞣质对革兰阳性菌具有较强的抗菌活性,而对革兰阴性菌抗菌活性较弱,经药物作用后金黄色葡萄球菌菌体胞外AKP、K⁺和核酸含量与对照组相比均升高,胞内ATP酶浓度显著降低。SDS-PAGE分析表明石榴皮鞣质能够抑制菌体蛋白质合成,尤其是大相对分子质量蛋白。透射电镜表明菌体细胞膜结构和完整性被破坏。结论:石榴皮鞣质对革兰阳性菌具有较强的抗菌活性,能够显著影响金黄色葡萄球菌的细胞壁和细胞膜结构,且对菌体内蛋白合成具有一定的抑制作用。     

Screening of Ethanol, Petroleum Ether and Chloroform Extracts of Medicinal Plants, Lawsonia inermis L. and Mimosa pudica L. for Antibacterial Activity

Organic extracts (ethanol, petroleum ether and chloroform) of two medicinal plants Lawsonia inermis L. and Mimosa pudica L. were proven for antibacterial properties against 15 Gram-positive and Gram-negative human pathogenic bacteria. Among the three types of extracts tested, ethanol extract was found to possess maximum antibacterial activity. The diameter of the zone of inhibition of bacterial growth showed that Gram-negative bacteria are more sensitive than Gram-positive bacteria to plant extracts. Between the two plants species studied, Lawsonia inermis extract showed more antibacterial activity compared to Mimosa pudica extract.     

岗梅感冒灵颗粒体外抗菌作用

目的探讨岗梅感冒灵颗粒的体外抗菌作用。方法以临床分离细菌为受试菌,采用琼脂稀释法,观察岗梅感冒灵颗粒的最低抑菌浓度。结果岗梅感冒灵颗粒对所有受试菌基本有不同程度的抑菌作用。结论岗梅感冒灵颗粒对上呼吸道感染常见致病菌有较好的抑菌作用。     

Antibacterial spectrum of plant polyphenols and extracts depending upon hydroxyphenyl structure

The relationship between the structure and antibacterial activity of 22 polyphenols was analyzed by using minimum inhibitory concentration (MIC) as a criterion against 26 species of bacteria which can grow in Mueller-Hinton medium. There was no clear correlation between Gram-staining and bacterial susceptibility to polyphenols, and the extent of the susceptibility was approximately dependent on the species of bacteria. In the same Gram-negative bacteria, the antibacterial activity of the polyphenols against Aeromonas hydrophila, Vibrio parahaemolyticus and Vibrio vulnificus was comparatively strong. On the other hand, the activity against 11 species of the Enterobacteriaceae was comparatively weak, and the activity against six species of aerobic bacteria causing plant disease was moderate. Polyphenols having pyrogallol groups showed strong antibacterial activity, and those with catechol and resorcinol rings showed lower activity. The structure-activity relationship was extended to 26 polyphenol-rich plant extracts which could have potent antibacterial activity suitable for commercial use.     

Antibacterial effect of parabens against planktonic and biofilm Streptococcus sobrinus.

Tooth decay is an infectious disease caused by bacteria immobilized on the tooth surfaces. Eradication of these bacteria, for example Streptococcus sobrinus (S. sobrinus), from the oral cavity is essential in the prevention and treatment of tooth decay. We have tested the antimicrobial effect of several paraben derivatives such as methyl (MP), ethyl (EP), propyl (PP) and butyl (BP) against immobilized and planktonic S. sobrinus. The antibacterial effect was as follows: MP>EP>PP=BP on immobilized bacteria and MP>EP=PP>BP on planktonic bacteria. An antibacterial synergistic effect was found between several combinations of parabens on immobilized and planktonic S. sobrinus. Our results indicate that parabens are potential antibacterial agents against immobilized or planktonic bacteria found in the oral cavity.     

Mechanism of decreased susceptibility for Gram-negative bacteria and synergistic effect with ampicillin of indole-3-carbinol

Indole-3-carbinol (I3C) is a natural compound found in a wide variety of plant food substances including members of the family Cruciferae with antioxidant and potential chemopreventive properties. In a previous study, I3C exhibited broad spectrum antibacterial activities. Particularly, it showed a more potent antibacterial activity against Gram-positive bacteria than Gram-negative bacteria. To elucidate this disparity of antibacterial activity between Gram-positive and Gram-negative bacteria, we investigated the actions of the efflux pumps and the lipopolysaccharide (LPS) barrier of the outer membrane of Gram-negative bacteria. The results showed that the antibacterial activity of I3C was affected by the barrier action of LPS in the outer membrane rather than by the efflux pumps. To assess its potential for combination therapy in treating bacterial infections, we investigated its synergy effects in combination with conventional antibiotics. The results demonstrated that I3C showed considerable synergistic activity in combination with ampicillin against drug-resistant isolates.     

Synthesis of novel porphyrin-based lipids and their antibacterial activity

The purpose of this study was to investigate the antibacterial activity of newly developed cationic amphiphilic lipids having porphyrin as head group against two types of gram-positive bacteria and three types of gram-negative bacteria. The antibacterial activity of quantitatively prepared porphyrin-based amphiphilic lipids is evaluated by the disc-diffusion method against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae and Proteus vulgaris. These results are compared with the standard antibacterial activity of chloramphenicol. Both lipids showed antibacterial behaviour against gram-positive and gram-negative bacteria.     

Comparison of antibacterial activity of cefmenoxime with other cephalosporins against clinically isolated bacteria (author's transl)

We examined the antibacterial activity of MX in comparison with those of other CEPs, using aerobic Gram-positive cocci, aerobic Gram-negative bacilli and anaerobic bacteria, 870 strains in total, all isolated from clinical specimens, in 1979 and 1980. Against Streptococcus, CMX showed superior antibacterial activity than those of CFX, CMZ, CXM and CTM. Against H. influenzae, CMX also showed superior antibacterial activity than those of CFX, CMX, CXM, CTM and CEZ. ABPC-and PIPC-resistant strains were sensitive to CMX. CTX, CPZ and CZX also showed antibacterial activities equivalent to that of CMX. Against enteric bacteria, E. coli, Klebsiella, E. cloacae, Serratia, C. freundii and Proteus, CMX showed superior antibacterial activity than those of CFX, CMZ, CXM, CTM and CEZ. Especially, against E. coli, Klebsiella, P. mirabilis, P. rettgeri and P. inconstans, CMX showed strong antibacterial activity. As to non-fermentation bacteria, CMX's antibacterial activity was relatively weak except P. putrefaciens, Alcaligenes and Comamonas. However, it was superior than that of CEZ. In comparison with other CEPs, the strength of CMX varied according to the kinds of bacteria. As to anaerobic bacteria, CMX showed strong antibacterial activity against Peptococcus, Peptostreptococcus, Lactobacillus, Propionibacterium, C. perfringens, Veillonella and Fusobacterium. However, its antibacterial activity against Bacteroides was similar to those of other CEPs.