甲硝唑与替硝唑体外抗阴道毛滴虫效果的实验研究

目的 比较甲硝唑与替硝唑体外抗四川省南充地区阴道毛滴虫虫株的效果.方法 采用肝浸液培养法获取并纯化10株阴道毛滴虫临床株.针对每一虫株,在培养基中加入不同质量浓度甲硝唑与替硝唑,37℃培养24 h,计算虫株死亡率,分析和比较两种药物的最低杀灭质量浓度.结果 甲硝唑与替硝唑平均最低杀灭质量浓度分别为84.4、17.2 μg/mL,替硝唑最低杀灭质量浓度低于甲硝唑,10株临床虫株中对甲硝唑敏感性下降2株,其中1株对替硝唑敏感性也有所下降.结论 甲硝唑和替硝唑对于杀灭四川省南充地区阴道毛滴虫临床虫株非常有效.在达到相同杀灭效果时,替硝唑用药量少于甲硝唑,而在用药量相同时,替硝唑效果优于甲硝唑.阴道毛滴虫对两种药物敏感度有关联性,替硝唑可能并不是理想的替代甲硝唑的药物.     

天然产物斑蝥素对阴道毛滴虫作用的研究

目的体外观察斑蝥素对8株抗甲硝唑阴道毛滴虫的杀灭效果及安全性。方法以斑蝥素终质量浓度为15.313~490.000μg/mL作用于体外培养的阴道毛滴虫。结果 30.625μg/mL为斑蝥素体外杀灭阴道毛滴虫的最低有效质量浓度。结论斑蝥素对体外阴道毛滴虫有杀灭效果。     

替硝唑泡腾片抗家兔阴道毛滴虫感染效果

应用家兔阴道毛滴虫感染模型，对替硝唑、甲硝唑泡腾片抗阴道毛滴虫感染的作用进行观察。结果表明，阴道毛滴虫半数抑虫率用药剂量，替硝唑为5．34mg／kg，甲硝唑为8．50mg／kg，两者有显著性差异。     

沙棘体外抗阴道毛滴虫作用研究

目的探讨沙棘果粉体外抗阴道毛滴虫的效果。方法将不同浓度的沙棘果粉作用于体外培养的阴道毛滴虫,在光镜下观察药物作用前后阴道毛滴虫的形态变化,并记录药物作用后不同时间阴道毛滴虫死亡率。结果沙棘果粉作用后,在高倍显微镜下观察到的阴道毛滴虫体内充满大量颗粒和空泡,部分虫体裂解、内容物外溢。随着药物作用时间的延长和药物浓度的增加,阴道毛滴虫死亡率增高。沙棘果粉杀灭阴道毛滴虫的最低有效浓度为50mg/ml。结论沙棘果粉具有抗阴道毛滴虫作用。     

替硝唑栓体内外抗阴道毛滴虫作用

目的 :观察替硝唑栓体内外抗阴道毛滴虫作用。方法 :经临床分离阴道毛滴虫 3 5株 ,观察替硝唑栓体外抗阴道毛滴虫作用 ;临床阴道滴虫病病人 75例用替硝唑栓 ( 0 .1g/粒 )治疗 ,隔日晚上睡时放入阴道 1粒 ,疗程 3d ,观察替硝唑栓体内抗阴道毛滴虫作用。选用甲硝唑栓作对照。结果 :替硝唑栓体外对阴道毛滴虫最小致死浓度为3 .72± 1 .2 4 μg/ml;替硝唑栓对临床阴道滴虫病治疗有效率 89% ,滴虫转阴率 99% ,与甲硝唑栓作用相似。 结论 :替硝唑栓体内外抗阴道滴虫作用与甲硝栓相似 ,但体内治疗替硝唑栓疗程比甲硝唑栓缩短。     

替硝唑洗液的抗厌氧菌活性及对人阴道滴虫的杀灭作用

目的 :观察替硝唑洗液的抗厌氧菌活性及对人阴道滴虫的杀灭作用。方法 :采用肉汤试管稀释法测定抗厌氧菌的MIC及MBC ;采用家兔阴道感染人阴道滴虫的模型 ,观察其抗阴道毛滴虫的作用。结果 :替硝唑洗液对 2 0 0株厌氧菌 (除乳杆菌、直杆菌外 )均有较好的抗菌活性 ,其MIC50 均在 2mg/L以下 ,MIC90 略高 ( 1 6mg/L) ,MBC约为MIC的 4～ 1 6倍。替硝唑洗液阴道内直接给药和阴道内冲洗 ,5mg/kg以上对阴道毛滴虫具有明显的杀灭作用 ,2 0mg/kg达痊愈。结论 :替硝唑洗液具有明显的抗厌氧菌活性 ,且对人阴道毛滴虫具有很好的杀灭作用 ,其杀灭滴虫的作用强度优于碧洁洗液     

复方替硝唑栓剂体内外抗阴道毛滴虫研究

目的观察复方替硝唑栓剂的体内外抗阴道毛滴虫作用。方法将临床确诊的滴虫性阴道炎患者100例随机分为两纽，试验纽用复方替硝唑栓治疗，对照组用双唑泰栓治疗，每晚睡前放入阴道1粒。6d为1个疗程，共治疗2个疗程；选用临床分离的阴道毛滴虫9株。观察复方替硝唑栓的体外抗阴道毛滴虫作用。结果临床治愈率复方替硝唑栓为100％，双唑泰栓为78．7％，两者有显著性差异（P〈0．05）；复方替硝唑栓体外抗阴道毛滴虫的抑虫50％浓度（MIC50）、抑虫90％浓度（MIC50）厦最低杀虫浓度（MBC）范围均低于双唑泰栓。结论复方替硝唑检体内外抗阴道毛滴虫作用显著．比双唑泰栓疗效更佳。     

替硝唑洗液的抗厌氧菌活性及对人阴道滴虫的杀灭作用

目的:观察替硝唑洗液的抗厌氧菌活性及对人阴道滴虫的杀灭作用。方法:采用肉汤试管稀释法测定抗厌氧菌的MIC及MBC ;采用家兔阴道感染人阴道滴虫的模型,观察其抗阴道毛滴虫的作用。结果:替硝唑洗液对200株厌氧菌(除乳杆菌、直杆菌外)均有较好的抗菌活性,其MIC₅₀均在2mg/L以下,MIC₉₀ 略高(16mg/L) ,MBC约为MIC的4～16倍。替硝唑洗液阴道内直接给药和阴道内冲洗,5mg/kg以上对阴道毛滴虫具有明显的杀灭作用,20mg/kg达痊愈。结论:替硝唑洗液具有明显的抗厌氧菌活性,且对人阴道毛滴虫具有很好的杀灭作用,其杀灭滴虫的作用强度优于碧洁洗液     

香薷HPLC指纹图谱及多指标成分定量分析

目的:建立香薷的HPLC指纹图谱及其咖啡酸、迷迭香酸、木犀草素、芹菜素、黄芩素-7-甲醚、香荆芥酚、麝香草酚7个成分的HPLC含量测定方法。方法:采用Eclipse XDB-C₁₈色谱柱(250 mm×4.6 mm, 5μm),流动相为0.1%甲酸水溶液(A)-乙腈(B),梯度洗脱(0～17 min, 12%B→20%B;17～30 min, 20%B→30%B;30～40 min, 30%B→45%B;40～55 min, 45%B→54%B),流速为1.0 mL·min^-1,检测波长为280、330 nm,柱温为30℃,进样量为5μL。结果:建立了香薷HPLC指纹图谱，共确定了14个共有峰，并指认其中5个共有峰，分别为咖啡酸(5号峰)、迷迭香酸(10号峰)、黄芩素-7-甲醚(12号峰)、香荆芥酚(13号峰)、麝香草酚(14号峰),17批香薷样品的相似度均>0.910;对17批药材中指认的7个成分进行含量测定，其质量浓度分别在1.04～52.0μg·mL^-1(r=0.999 3,n=5)、6.0～300.0μg·...     

替硝唑注射液与其他注射剂配伍后稳定性研究进展

替硝唑(Tinidazole)系硝基咪唑类抗厌氧菌及抗原虫药，为甲硝唑同系物，其抗厌氧菌活性是甲硝唑的2-4倍，对90％厌氧菌的最低抑菌浓度(MIC)为2ug／ml，维持体内有效血药浓度时间也比甲硝唑长约6倍，而消化道不良反应等毒副作用比甲硝唑轻微，病人耐受性好，是甲硝唑的理想换代产品。本品在口腔科，妇产科.     

麝柳洗剂治疗96例瘙痒性皮肤病疗效观察

目的观察麝柳洗剂治疗瘙痒性皮肤病的临床疗效。方法随机抽取本中心皮肤病门诊96例瘙痒性皮肤病患者,使用麝柳洗剂治疗,每日2～3次外用,2周为1个疗程。治疗结束后观察疗效。结果麝柳洗剂对丘疹性荨麻疹疗效最好,对单纯性瘙痒、湿疹、神经性皮炎这些慢性病治愈率稍差,但有效率均较高。结论麝柳洗剂治疗瘙痒性皮肤病疗效显著,安全方便。     

金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸的肠吸收研究

目的 考察金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸的肠吸收特性,确定金莲花汤中活性成分。方法 采用HPLC法测定肠吸收样品中咖啡酸、葛根素、牡荆素、迷迭香酸,以大鼠肠外翻吸收实验和Caco-2细胞模型转运实验计算各成分的累积吸收量、吸收速率常数和表观渗透系数。结果 随着金莲花汤的质量浓度增加,咖啡酸、葛根素、牡荆素、迷迭香酸的吸收速率常数呈线性关系增加,符合零级吸收速率,且吸收率均小于1.4%,在肠道中吸收效果普遍较差,其中咖啡酸的吸收较为明显。各成分的表观渗透系数值大小为迷迭香酸>咖啡酸>葛根素>牡荆素。结论 金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸均可在肠道中被吸收,吸收方式为被动扩散,咖啡酸和迷迭香酸可能是金莲花汤中发挥药效的活性物质,葛根素和牡荆素可能是前药。     

Characterization of anticonvulsant and antiepileptogenic potential of thymol in various experimental models

The present study was to investigate the anticonvulsant and antiepileptogenic potential of thymol. Anticonvulsant activity of thymol (5–100 mg/kg i.p.) was studied using maximal electroshock, pentylenetetrazole (PTZ), strychnine and 4-aminopyridine (4-AP) models. Thymol at the selected dose was also studied for its effect on locomotion. Antiepileptogenic property of thymol (5–25 mg/kg) was evaluated using PTZ-induced kindling model along with its effect on malondialdehyde and glutathione levels. Thymol (50 and 100 mg/kg, i.p.) showed anticonvulsant activity against maximal electroshock and pentylenetetrazole (66.66 and 83.33 % protection at 50 and 100 mg/kg, respectively) model but not against strychnine and 4-aminopyridine models. Thymol exhibited decreased locomotor activity in dose-dependent manner at the same dose range. Thymol at the dose of (25 mg/kg, i.p.) significantly decreased the seizure score, increased glutathione levels and decreased malondialdehyde levels in pentylenetetrazole-induced kindling model. Thymol exhibited significant anticonvulsant and antiepileptogenic property.     

Rosmarinic acid and caffeic acid reduce the defensive freezing behavior of mice exposed to conditioned fear stress

Abstract Rationale. We previously showed that rosmarinic acid from the leaves of Perilla frutescens Britton var. acuta Kudo (Perillae Herba) and its major metabolite caffeic acid have antidepressive-like activity in the forced swimming test. Objective. The present study was designed to examine whether rosmarinic acid and caffeic acid might also be effective in other types of stress model. Methods: The conditioned fear stress paradigm was used as a stress model for assessing the effects of rosmarinic acid and caffeic acid. Results. Rosmarinic acid (0.25–4 mg/kg, IP) induced a dose-dependent, U-shaped reduction in the duration of the defensive freezing behavior of mice exposed to conditioned fear stress. Caffeic acid (1–8 mg/kg, IP) also dose-dependently reduced this freezing behavior. However, neither substance, at doses that produced a significant reduction in the freezing behavior, affected spontaneous motor activity. Conclusions. These results confirm that rosmarinic acid and caffeic acid may inhibit the emotional abnormality produced by stress. Electronic Publication     

Synthesis, and antiprotozoal and antibacterial activities of S-substituted 4,6-dibromo- and 4,6-dichloro-2-mercaptobenzimidazoles.

The synthesis and some germicidal activities in vitro of two congener series of S-substituted 4,6-dihalogeno-2-mercapto-1H-benzimidazoles are reported. There was no substantial difference between antibacterial activities of corresponding 4,6-dichloro- and 4,6-dibromo-derivatives. The present results confirm lower susceptibility to substituted benzimidazoles of Gram-negative compared to Gram-positive bacteria. Minimum inhibitory concentrations (MICs) of a majority of the novel derivatives ranged between 25 and 100microg/ml for Gram-positive bacteria. The most active compounds (MICs for Gram-positive bacteria: 0.78-50microg/ml) were 4,6-dichloro-2-(4-nitrobenzylthio)-1H-benzimidazole and 4,6-dibromo-2-(4-nitrobenzylthio)-1H-benzimidazole that were 4-32 times more potent than nitrofurantoin against all Gram-positive bacteria utilized but Escherichia faecalis, against which they were, respectively, 2 and 4 times less potent than nitrofurantoin. Among Gram-negative bacteria used, Stenotrophomonas maltophilia and Bordetella bronchiseptica were most sensitive (as evidenced by a number of MICs 400microg/ml). All the new compounds were at least several times more active against Giardia intestinalis (IC(50): 0.006-0.053microg/ml), and a half of them were at least several times more active against Trichomonas vaginalis (IC(50): 0.0015-0.182microg/ml) than metronidazole (IC(50): 0.210 and 0.037microg/ml, respectively), the drug of choice in the treatment of G. intestinalis and T. vaginalis infections.     

1,4-Bis-[1-methyl-5-nitroimidazolyl-(2-methyleneimino)]-piperazine, a new drug with marked activity against Entamoeba histolytica. Short communication.

1,4-Bis-[1-methyl-5-nitroimidazolyl-(2-methyleneimino)]-piperazine (HOE 316) administered orally produces an effect which is clearly superior to that of metronidazole against Entamoeba histolytica in the golden hamster and slightly inferior against Trichomonas fetus and T. vaginalis in the mouse. The acute tolerance of the compound is very good (LD 50% greater than 10 g/kg body weight). It is assumed that the possible main metabolite of HOE 316 is a monohydrazone: 1-methyl-2-(4-amino-piperazino-1-imino-methyl)-5-nitroimidazole.     

Thymol nanospheres as an effective anti-bacterial agent

Among thymol, carvacrol, citronellal, eugenol and terpinen-4-ol, thymol showed the highest antibacterial activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Thymol was then encapsulated into water dispersible submicron sized ethylcellulose/methylcellulose spheres, attaining the relatively high thymol loading level of 43.53% (weight of encapsulated thymol to weight of the thymol-loaded spheres). When tested against the same three bacterial strains, the encapsulated thymol gave comparable minimal inhibition concentration (MIC) and minimal bactericidal concentration (MBC) values to the unencapsulated compound while mostly showing lower MIC and MBC values than the conventionally used preservative, methyl-p-hydroxybenzoate (methylparaben). The use of encapsulated thymol at 0.078, 0.156 and 0.625 mg ml(-1) (0.52, 1.04 and 4.16 mmol(-1), respectively) in cosmetic lotion formulations provided total suppression of viable E. coli, S. aureus and P. aeruginosa growth (all initially seeded at 10(5) cfu ml(-1)), respectively, over the three month test period, whereas unencapsulated thymol showed effective suppression for only 2-4 weeks. Effective bacterial suppression by encapsulated thymol was also observed when used in cream and aqueous gel cosmetic formulations.     

Rosmarinic acid and caffeic acid produce antidepressive-like effect in the forced swimming test in mice

We previously showed that rosmarinic acid from the leaves of Perilla frutescens Britton var. acuta Kudo (Perillae Herba) has antidepressive-like activity. The aim of the present study was to examine (i) whether caffeic acid, a major metabolite of rosmarinic acid, also has antidepressive-like activity, and (ii) whether these substances inhibit either the uptake of monoamines to synaptosomes or mitochondrial monoamine oxidase activity. Rosmarinic acid (2 mg/kg, i.p.) and caffeic acid (4 mg/kg, i.p.) each significantly reduced the duration of immobility in the forced swimming test in mice. In contrast, neither substance, at doses that produced a significant reduction in the immobile response in the forced swimming test, affected spontaneous motor activity. These results indicate that, like rosmarinic acid, caffeic acid also possesses antidepressive-like activity. In neuropharmacological studies, neither rosmarinic acid (10 x (-9)-10 x (-3) M) nor caffeic acid (10 x (-9)-10 x (-3) M) affected either the uptake of monoamines to synaptosomes or mitochondrial monoamine oxidase activity in the mouse brain. These results suggest that both caffeic acid and rosmarinic acid may produce antidepressive-like activity via some mechanism(s) other than the inhibition of monoamine transporters and monoamine oxidase.     

Clinical effects of nifuratel in vulvovaginal infections. A meta-analysis of metronidazole-controlled trials

Nifuratel (CAS 4936-47-4) displays a strong antiprotozoarian and antibacterial activity and is provided with certain fungicidal effect, but it is not active against the physiologic flora. Its therapeutic effectiveness has been evaluated in more than 12,000 patients. The wide clinical experience with nifuratel confirms that the drug is safe and effective for the treatment of trichomoniasis, bacterial vaginosis, candidosis, and, particularly, in patients suffering from mixed vaginal infection. A meta-analysis of clinical trials comparing nifuratel and metronidazole (CAS 443-48-1) in vulvovaginal infections was performed. All parallel-group metronidazole-controlled trials carried out in patients with vulvovaginal infections have been included, complying with the following criteria: 1) cure assessed both as disappearance of symptoms and signs, and negative microbiological findings; 2) microbiological tests performed with valid methods still used in current practice. Seven clinical trials have been selected, including overall 1767 patients, 832 out of whom were treated with nifuratel and 935 with metronidazole. The results of the meta-analysis confirmed the equivalence between nifuratel and metronidazole: overall proportion of cured patients in the two groups were 88.5% and 90.0%, respectively, in the presence of homogeneity among studies (p = 0.342). In the fixed and random effect analyses, the confidence interval of Odds ratio included 1 and the p values for testing the hypothesis of no difference between treatments were 0.656-1.266, p = 0.582 (fixed effects) and 0.643-1.290, p = 0.599 (random effects), respectively, indicating equivalence. Furthermore, some controlled studies and the wide clinical experience showed that the cure rate of nifuratel in patients with mixed infections due to Trichomonas vaginalis + Candida or Trichomonas vaginalis + bacteria or with bacterial vaginosis and mixed bacterial flora is higher than that of metronidazole, due to the wide spectrum of action of nifuratel.     

Prooxidant action of rosmarinic acid: transition metal-dependent generation of reactive oxygen species.

Rosmarinic acid and its constituent caffeic acid produced reactive oxygen species in the presence of transition metals. Complex of rosmarinic acid or caffeic acid with iron inactivated aconitase the most sensitive enzyme to oxidative stress. The inactivation of aconitase was iron-dependent, and prevented by TEMPOL, a scavenger of reactive oxygen species, suggesting that the rosmarinic acid/iron-mediated generation of superoxide anion is responsible for the inactivation of aconitase. Direct spectrophotometric determination of hydrogen peroxide and superoxide anion confirmed the rosmarinic acid/iron-dependent production of reactive oxygen species. Treatment of DNA from plasmid pBR322 and calf thymus with rosmarinic acid plus copper caused strand scission and formed 8-hydroxy-2'-deoxyguanosine in DNA. Rosmarinic acid and caffeic acid showed a potent activity that reduces transition metals. These results suggest that transition metals reduced by rosmarinic acid can form superoxide radical by one electron reduction of oxygen molecule: superoxide radical in turn converts to hydrogen peroxide and hydroxyl radical causing the formation of DNA base adduct. Cytotoxicity of rosmarinic acid may be related to the prooxidant action resulting from metal-reducing activity.