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Rat tissue concentrations of chlorimipramine, chlorpromazine and their N-demethylated metabolites after a single oral dose of the parent compounds. 单次口服母体化合物后氯丙咪嗪、氯丙嗪及其n -去甲基化代谢物的大鼠组织浓度。
Pub Date : 1900-01-01 DOI: 10.1016/1043-6618(95)86446-6
G. Sgaragli, M. Valoti, M. Palmi, M. Frosini, M. Giovannini, L. Bianchi, L. Della Corte
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引用次数: 8
In-situ absorption, protein binding and pharmacokinetic studies of S002-853, a novel antidiabetic and antidyslipidaemic flavone derivative in rats. 新型降糖降血脂黄酮衍生物S002-853在大鼠体内的原位吸收、蛋白结合及药代动力学研究。
Pub Date : 1900-01-01 DOI: 10.1211/jpp/62.05.0007
N. Gautam, H. Kushwaha, R. Pratap, Shio Kumar Singh
OBJECTIVESThe aim of the study was to investigate the in-situ absorption kinetics, plasma protein binding and pharmacokinetic characteristics of a novel synthetic flavone derivative, S002-853, which shows pronounced antidiabetic and antidyslipidaemic activity.METHODSQuantification of S002-853 in plasma was performed by the LC-MS/MS method and in-situ sample analysis was carried out by the HPLC-UV method.KEY FINDINGSThe absorption rate constant was 0.274/h in a mild alkaline environment, which S002-853 experiences in the intestine following oral dose administration. Plasma protein binding was found to be 26.37 +/- 2.58% at a concentration of 1 microg/ml. The pharmacokinetic parameters were determined in male rats after administration of a single 40 mg/kg oral dose and 10 mg/kg intravenous dose. The peak plasma concentration (C(max)) was found to be 60.93 ng/ml at 8 h after oral administration. Irregular concentration-time profiles with secondary peaks were observed after oral dose administration. The elimination half-life of the compound was 19.56 h and 16.30 h after oral and intravenous doses, respectively. Comparison of the AUC after oral and intravenous dosing of S002-853 indicates that only about 29.48% (bioavailability) of the oral dose reaches the systemic circulation.CONCLUSIONSIn-situ study of S002-853 shows slow absorption from the gastrointestinal tract. S002-853 also shows low plasma protein binding. The pharmacokinetic parameters after oral and intravenous dose reveal low oral bioavailability and high mean residence time.
目的研究一种新型合成黄酮类化合物S002-853的原位吸收动力学、血浆蛋白结合及药动学特性。方法采用LC-MS/MS法定量血浆中S002-853的含量,采用HPLC-UV法进行原位样品分析。S002-853口服给药后,在温和碱性环境下的吸收速率常数为0.274/h。在浓度为1微克/毫升时,血浆蛋白结合率为26.37 +/- 2.58%。测定雄性大鼠单次口服剂量40 mg/kg和静脉注射剂量10 mg/kg后的药代动力学参数。口服后8 h血药浓度(C(max))为60.93 ng/ml。在口服给药后,观察到不规则的浓度-时间分布和二次峰。口服和静脉给药后,化合物的消除半衰期分别为19.56 h和16.30 h。S002-853口服和静脉给药后的AUC比较表明,口服剂量到达体循环的生物利用度仅为29.48%左右。结论原位研究表明S002-853在胃肠道吸收缓慢。S002-853也显示低血浆蛋白结合。口服和静脉给药后的药动学参数显示口服生物利用度低,平均停留时间长。
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引用次数: 1
Acute withdrawal induced by adenosine A-receptor activation in isolated guinea-pig ileum: role of opioid receptors and effect of cholecystokinin. 腺苷a受体激活诱导离体豚鼠回肠急性戒断:阿片受体的作用和胆囊收缩素的作用。
Pub Date : 1900-01-01 DOI: 10.1211/jpp/62.05.0010
P. Marini, L. Romanelli, D. Valeri, P. Tucci, P. Valeri, M. Palmery
OBJECTIVESIn isolated guinea-pig ileum, the mu-opioid acute withdrawal response is under control of several neuronal systems, including the kappa-opioid and the A(1)-adenosine systems, which are involved in the mu-withdrawal response inhibitory control. After mu-opioid system stimulation, indirect activation of both kappa-opioid and A(1)-adenosine systems is prevented by the peptide cholecystokinin-8 (CCk-8). Guinea-pig ileum exposed to A(1)-adenosine agonist (CPA), shows a withdrawal contracture precipitated by the A(1)-adenosine antagonist (CPT). We investigated this response.METHODSWe investigated the involvement of the opioid system in the A(1)-adenosine acute withdrawal response in guinea-pig ileum, the potential induced cross-dependence between the A(1) and the opioid system and also the interaction between the CCk-8 and A(1) systems.KEY FINDINGSWe found that in the guinea-pig ileum preparation exposed to CPA, mu- and kappa-opioid antagonists increased the withdrawal response to CPT. Tissues exposed to CPA showed a contractile response to the opioid receptor antagonist naloxone only after complete removal of the A(1)-agonist. In the presence of CPA, the response to CCk-8 was inhibited while a significant increase in CPT response intensity was observed.CONCLUSIONSIn guinea-pig ileum, stimulation of the A(1) system indirectly activates both mu- and kappa-opioid systems; this indirect activation is significantly, albeit not completely, antagonised by CCk-8. Cross dependence between A(1) and opioid systems was also observed.
目的:在离体豚鼠回肠中,阿片类药物急性戒断反应受多个神经元系统的控制,包括kapa -阿片类和A(1)-腺苷系统,它们参与了阿片类药物戒断反应的抑制控制。在mu-阿片系统刺激后,kapa -阿片和A(1)-腺苷系统的间接激活被缩胆素-8 (CCk-8)肽阻止。豚鼠回肠暴露于A(1)-腺苷激动剂(CPA)后,表现出由A(1)-腺苷拮抗剂(CPT)引起的退缩性挛缩。我们调查了这种反应。方法研究阿片系统在豚鼠回肠A(1)-腺苷急性戒断反应中的作用、A(1)与阿片系统的交叉依赖性以及CCk-8与A(1)系统的相互作用。我们发现,在暴露于CPA的豚鼠回肠制剂中,mu-和kappa-阿片类拮抗剂增加了对CPT的戒断反应。暴露于CPA的组织仅在完全去除a(1)-激动剂后才对阿片受体拮抗剂纳洛酮表现出收缩反应。在CPA存在的情况下,CCk-8的应答被抑制,而CPT应答强度显著增加。结论在豚鼠回肠中,A(1)系统的刺激可间接激活mu-和kappa-阿片系统;这种间接激活被CCk-8显著地(尽管不是完全地)拮抗。A(1)和阿片系统之间的交叉依赖也被观察到。
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引用次数: 3
Potable water. 饮用水。
Pub Date : 1900-01-01 DOI: 10.4135/9781446247501.n3081
N. Burman, E. Taylor
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引用次数: 7
Acoustic emission during the deformation of alpha-lactose monohydrate and anhydrous alpha-lactose monocrystals. α -乳糖单水和无水α -乳糖单晶变形过程中的声发射。
Pub Date : 1900-01-01 DOI: 10.3109/03639048809152005
D. Wong, M. Waring, P. Wright, M. Aulton
During the deformation of single crystals of alpha-lactose monohydrate and anhydrous alpha-lactose in a crushing strength rig, their acoustic activity was monitored using a portable activity meter. The acoustic parameters measured were the average signal level (ASL), count rates and total acoustic counts. Both types of lactose, even though deformed by fragmentation, differed fundamentally in the degree and nature of this fragmentation. Close correlation was observed between the ASL, count rate profiles and the force-displacement profiles. The monohydrate form is acoustically more active than the anhydrous form during deformation. Small internal fractures which were neither visually observed nor detected in the force-displacement profiles (in particular the anhydrous alpha-lactose) were detected by monitoring the acoustic signals during the deformation of these crystals. This work illustrates the potential of using the acoustic emission technique as an aid in the assessment of the deformation characteristics of pharmaceutical materials during single crystal compression studies.
在抗压强度试验装置中,对一水α -乳糖单晶和无水α -乳糖单晶进行变形过程中,采用便携式活性仪监测其声活性。测量的声学参数包括平均信号电平(ASL)、计数率和总声计数。这两种类型的乳糖,尽管由于破碎而变形,但在这种破碎的程度和性质上有根本的不同。ASL、计数率曲线与力-位移曲线密切相关。在变形过程中,一水形式比无水形式在声学上更活跃。通过监测这些晶体变形过程中的声学信号,可以检测到既没有目测到也没有在力-位移剖面中检测到的小的内部裂缝(特别是无水α -乳糖)。这项工作说明了在单晶压缩研究中使用声发射技术作为药物材料变形特性评估的辅助手段的潜力。
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引用次数: 22
Effect of acute hepatic failure on the hepatic first-pass effect of 5-fluorouracil in rats. 急性肝功能衰竭对5-氟尿嘧啶肝首过效应的影响。
Pub Date : 1900-01-01 DOI: 10.1211/jpp/62.05.0006
M. Nagata, Y. Hidaka, M. Hidaka, Y. Kawano, T. Iwakiri, M. Okumura, K. Arimori
OBJECTIVESIn cancer chemotherapy for hepatocellular carcinoma, 5-fluorouracil is widely used and has typically been given by intrahepatic arterial (i.a.) infusion to increase treatment efficacy and reduce systemic toxicity. 5-Fluorouracil is eliminated primarily by the liver and so the hepatic first-pass effect after intrahepatic arterial administration of 5-fluorouracil may be lower in patients with hepatic failure, and systemic toxicity may not be reduced. In this study, we have investigated the effect of acute hepatic failure on the first-pass effect of 5-fluorouracil in rats.METHODSExperimental acute hepatic failure was induced by treatment with carbon tetrachloride (CCl4). 5-Fluorouracil was infused for 15 min into the hepatic artery or the saphenous vein of rats at a dose of 1.25 mg/kg.KEY FINDINGSHepatic availability in 50% CCl4-treated (severe hepatic failure) rats was higher than in controls.CONCLUSIONSThe hepatic first-pass effect after intrahepatic arterial administration of 5-fluorouracil was lower in severe hepatic failure. Therefore, the reducing effect of the systemic toxicity after intrahepatic arterial administration may be lower in severe hepatic failure.
目的:在肝癌化疗中,5-氟尿嘧啶被广泛使用,通常通过肝动脉输注来提高治疗效果,降低全身毒性。5-氟尿嘧啶主要由肝脏排出,因此肝功能衰竭患者肝动脉内给药5-氟尿嘧啶后的肝脏首过效应可能较低,全身毒性可能不会降低。在本研究中,我们研究了急性肝功能衰竭对大鼠5-氟尿嘧啶首过效应的影响。方法采用四氯化碳(CCl4)诱导实验性急性肝衰竭。5-氟尿嘧啶以1.25 mg/kg的剂量注入大鼠肝动脉或大鼠隐静脉15 min。50%的ccl4治疗(严重肝功能衰竭)大鼠的肝脏可用性高于对照组。结论重型肝功能衰竭患者肝动脉灌注5-氟尿嘧啶后肝脏首过效应较低。因此,严重肝功能衰竭时,肝动脉内给药对全身毒性的降低作用可能较低。
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引用次数: 5
Pectin-based microspheres for colon-specific delivery of vancomycin. 以果胶为基础的万古霉素结肠特异性递送微球。
Pub Date : 1900-01-01 DOI: 10.1211/jpp/61.01.0006
F. Bigucci, B. Luppi, L. Monaco, T. Cerchiara, V. Zecchi
OBJECTIVESThe aim of this study was to describe a colon-specific delivery system based on pectin hydrogels formed by complexation with chitosan.METHODSHydrogels were prepared at different weight ratios (4:1, 7:1, 10:1; pectin/chitosan), loaded with vancomycin hydrochloride (2:1, 4:1; polymer/drug weight ratio) and collected by spray-drying. The microspheres obtained were characterized in terms of morphology, swelling behaviour, mucoadhesive properties and drug loading efficiency. The influence of different pectin/chitosan hydrogels on the release behaviour of microspheres at pH 2.0, 5.5 and 7.4 were evaluated in vitro with and without pectinolytic enzyme.KEY FINDINGSThe results showed that water uptake was increased by raising the environmental pH (from 2.0 to 7.4) and the pectin/chitosan weight ratio, while drug availability was increased by raising the environmental pH (from 2.0 to 7.4) and decreased by raising the pectin/chitosan weight ratio. In the presence of pectinase, the glycoside bonds of pectin were degraded and a considerable amount of drug was released in a short time.CONCLUSIONSThis study suggested that pectin/chitosan microspheres were able to limit the release of vancomycin under acidic conditions and release it under simulated colonic conditions, confirming their potential for a colon-specific drug delivery system.
目的研究以壳聚糖与果胶水凝胶络合形成的结肠特异性给药体系。方法制备不同质量比的水凝胶(4:1、7:1、10:1;果胶/壳聚糖),负载盐酸万古霉素(2:1,4:1;聚合物/药物重量比),喷雾干燥收集。对制备的微球进行了形貌、溶胀性能、黏附性能和载药效率等方面的表征。考察了不同果胶/壳聚糖水凝胶在pH 2.0、5.5和7.4条件下对微球体外释放行为的影响。结果表明:提高环境pH值(2.0 ~ 7.4)和果胶/壳聚糖质量比可提高植物的吸水率;提高环境pH值(2.0 ~ 7.4)可提高植物的药物利用度,提高果胶/壳聚糖质量比可降低植物的药物利用度。在果胶酶的作用下,果胶的糖苷键被降解,并在短时间内大量释放药物。结论果胶/壳聚糖微球能够在酸性条件下限制万古霉素的释放,并在模拟结肠条件下释放万古霉素,证实了其作为结肠特异性给药系统的潜力。
{"title":"Pectin-based microspheres for colon-specific delivery of vancomycin.","authors":"F. Bigucci, B. Luppi, L. Monaco, T. Cerchiara, V. Zecchi","doi":"10.1211/jpp/61.01.0006","DOIUrl":"https://doi.org/10.1211/jpp/61.01.0006","url":null,"abstract":"OBJECTIVES\u0000The aim of this study was to describe a colon-specific delivery system based on pectin hydrogels formed by complexation with chitosan.\u0000\u0000\u0000METHODS\u0000Hydrogels were prepared at different weight ratios (4:1, 7:1, 10:1; pectin/chitosan), loaded with vancomycin hydrochloride (2:1, 4:1; polymer/drug weight ratio) and collected by spray-drying. The microspheres obtained were characterized in terms of morphology, swelling behaviour, mucoadhesive properties and drug loading efficiency. The influence of different pectin/chitosan hydrogels on the release behaviour of microspheres at pH 2.0, 5.5 and 7.4 were evaluated in vitro with and without pectinolytic enzyme.\u0000\u0000\u0000KEY FINDINGS\u0000The results showed that water uptake was increased by raising the environmental pH (from 2.0 to 7.4) and the pectin/chitosan weight ratio, while drug availability was increased by raising the environmental pH (from 2.0 to 7.4) and decreased by raising the pectin/chitosan weight ratio. In the presence of pectinase, the glycoside bonds of pectin were degraded and a considerable amount of drug was released in a short time.\u0000\u0000\u0000CONCLUSIONS\u0000This study suggested that pectin/chitosan microspheres were able to limit the release of vancomycin under acidic conditions and release it under simulated colonic conditions, confirming their potential for a colon-specific drug delivery system.","PeriodicalId":366080,"journal":{"name":"The Journal of pharmacy and pharmacology","volume":"35 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121080794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 42
Change in tolbutamide permeability in rat jejunum and Caco-2 cells by Sho-saiko-to (Xiao Chai Hu Tang), a Chinese traditional medicine. 中药消柴胡汤对大鼠空肠和Caco-2细胞甲磺丁胺通透性的影响
Pub Date : 1900-01-01 DOI: 10.1211/jpp/62.05.0014
N. Nishimura, Tomichika Uemura, K. Iwamoto, K. Naora
OBJECTIVESThis study was designed to investigate the effects of Sho-saiko-to (Xiao Chai Hu Tang), a Chinese traditional medicine, on the membrane permeability of tolbutamide in the intestinal tract. We carried out an in-situ loop study with rat jejunum and a transport study with Caco-2 cell monolayers.METHODSIn the in-situ loop study, absorption clearance of tolbutamide was estimated from the drug concentrations in the loop and plasma. The apical-to-basolateral and basolateral-to-apical transport of tolbutamide and d-mannitol, a paracellular transport marker, was assessed using Caco-2 cell monolayers cultured on a polycarbonate membrane.KEY FINDINGSThe absorption clearance of tolbutamide was enhanced by a concomitant dose of Sho-saiko-to over 10 min in the rat in-situ loop. Sho-saiko-to increased the apical-to-basolateral transport of tolbutamide, whereas the basolateral-to-apical transport of this drug was reduced by Sho-saiko-to. On the other hand, in both directions the P(app) of d-mannitol was reduced by the presence of Sho-saiko-to. Furthermore, the apical-to-basolateral transport of tolbutamide in ATP-depleted Caco-2 cells was diminished by Sho-saiko-to. These findings suggest that Sho-saiko-to can facilitate the epithelial membrane permeability of tolbutamide across the rat jejunum in-situ and Caco-2 cell monolayers. Since Sho-saiko-to suppressed the passive transport of tolbutamide from the apical-to-basolateral side, enhanced permeability may be related to effects of Sho-saiko-to on the energy-dependent transport of tolbutamide in the intestine.CONCLUSIONSOur findings suggest that Sho-saiko-to might facilitate the energy-dependent transport of tolbutamide across the rat jejunum in-situ and Caco-2 cell monolayers.
目的观察中药消柴胡汤对大鼠肠道内甲磺丁胺膜通透性的影响。我们对大鼠空肠进行了原位环研究,并对Caco-2细胞单层进行了转运研究。方法原位环法研究中,通过环内药物浓度和血浆中药物浓度估算对甲苯丁胺的吸收清除率。利用聚碳酸酯膜上培养的Caco-2细胞单层,评估了甲磺丁酰胺和d-甘露醇(一种细胞旁转运标志物)的根尖到基底外侧和基底外侧到根尖的转运。主要发现:在大鼠原位环中,同时给药10 min以上的shoo -saiko-to可增强甲苯丁酰胺的吸收清除率。shoo -saiko-to增加了甲磺丁胺从基底外侧到基底外侧的转运,而shoo -saiko-to则减少了甲磺丁胺从基底外侧到基底外侧的转运。另一方面,在两个方向上,d-甘露醇的P(app)都因shoo -saiko-to的存在而降低。此外,在atp耗尽的Caco-2细胞中,shoo -saiko-to减少了甲磺丁酰胺的尖向基底侧转运。这些结果表明,shoo -saiko-to可以促进甲苯丁胺在大鼠空肠原位和Caco-2细胞单层上的上皮膜通透性。由于shoo -saiko-to抑制了tolbutamide从根尖到基底外侧的被动运输,因此增强的通透性可能与shoo -saiko-to对肠道中tolbutamide的能量依赖性运输的影响有关。结论shoo -saiko-to可能促进了甲苯丁胺在大鼠空肠原位和Caco-2细胞单层上的能量依赖性运输。
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引用次数: 1
Molecularly imprinted polymers as drug delivery systems for the sustained release of glycyrrhizic acid. 分子印迹聚合物作为甘草酸缓释的药物传递系统。
Pub Date : 1900-01-01 DOI: 10.1211/jpp/62.05.0003
G. Cirillo, O. I. Parisi, M. Curcio, F. Puoci, F. Iemma, U. G. Spizzirri, N. Picci
OBJECTIVESThe aim was to synthesize molecularly imprinted polymers (MIPs) with high recognition properties towards glycyrrhizic acid and to evaluate the performance of these materials to act as base excipients in glycyrrhizic acid sustained release in gastrointestinal simulating fluids.METHODSMIPs were synthesized using methacrylic acid (MAA) as acidic, 2-(dimethylamino)ethyl methacrylate (DMAEMA) as basic, and 2-hydroxyethylmethacrylate (HEMA) as neutral functional monomers, while ethylene glycol dimethacrylate (EGDMA) was chosen as a crosslinking agent. The imprinting effect was evaluated by binding experiments using glycyrrhizic acid and glycyrrhetic acid (analogue molecule) solutions and in-vitro release studies were performed in gastrointestinal simulating fluids.KEY FINDINGSGood recognition and selectivity properties were found in all the synthesized materials in both ethanol and ethanol-water mixture. The release from non-imprinted polymers was indeed higher at acidic pH, while a slower release was observed in MIPs' case, because of the presence of imprinted cavities in the polymeric structure. The stronger capacity of MAA to interact by hydrogen bonds with the template makes MAA-containing MIPs the most effective materials in both rebinding and release experiments.CONCLUSIONSThe release tests confirm the applicability of imprinted polymer for glycyrrhizic acid sustained release in gastrointestinal simulating fluids.
目的合成对甘草酸具有高识别性能的分子印迹聚合物(MIPs),并评价其在甘草酸胃肠模拟液中作为基础赋形剂的性能。方法以甲基丙烯酸(MAA)为酸性,2-(二甲氨基)甲基丙烯酸乙酯(DMAEMA)为碱性,2-甲基丙烯酸羟乙酯(HEMA)为中性功能单体,乙二醇二甲基丙烯酸酯(EGDMA)为交联剂合成smip。通过甘草酸和甘草酸(类似分子)溶液的结合实验来评估印迹效果,并在胃肠道模拟液体中进行体外释放研究。主要发现所有合成材料在乙醇和乙醇-水混合物中均具有良好的识别和选择性。在酸性pH下,非印迹聚合物的释放确实更高,而在MIPs的情况下,由于聚合物结构中存在印迹腔,释放速度较慢。MAA通过氢键与模板相互作用的能力更强,使得含MAA的MIPs在重结合和释放实验中都是最有效的材料。结论印迹聚合物对甘草酸在胃肠道模拟液体中的缓释具有一定的适用性。
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引用次数: 18
Large molecules as anti-adhesive compounds against pathogens. 大分子作为抗粘附化合物对抗病原体。
Pub Date : 1900-01-01 DOI: 10.1055/S-2007-986869
N. Wittschier, C. Lengsfeld, S. Vorthems, U. Stratmann, J. Ernst, E. Verspohl, A. Hensel
Anti-adhesive compounds are potential prophylactic tools in alternative treatment regimes against bacterial infection, as bacterial adhesion is commonly mediated by carbohydrate-protein interactions between surface adhesions of microorganisms and the host cell. The use of exogenous polyvalent, high-molecular carbohydrates and tannin-like plant-derived compounds should antagonize the adhesive interaction. A range of carbohydrates and carbohydrate- and proanthocyanidin-enriched plant extracts were screened for potential anti-adhesive effects against Helicobacter pylori, Campylobacter jejuni, Porphyromonas gingivalis and Candida albicans in different in-situ assays on primary tissue. The adhesion of H. pylori on human stomach tissue was effectively blocked by glucuronic acid-enriched polysaccharides from immature okra fruits (Abelmoschus esculentus). These compounds also had strong in-vitro effects against C. jejuni (inhibition up to 80%), but were ineffective in an in-vivo study in infected chicken broilers due to metabolism in the gastrointestinal system. Polysaccharides from Glycyrrhizia glabra, also enriched with glucuronic acid, showed strong anti-adhesive properties against H. pylori and P. gingivalis (inhibition 60-70%). Pelargonium sidoides extract, containing mainly polymeric proanthocyanidins, was effective against H. pylori in a dose-dependent manner. Due to the multifunctional adhesive strategy of C. albicans, no effective compounds were detected against this yeast. Structure-activity relationships are presented and the potential in-vivo use of carbohydrate-based anti-adhesives is discussed.
抗黏附化合物是针对细菌感染的替代治疗方案中潜在的预防性工具,因为细菌黏附通常是由微生物与宿主细胞表面黏附之间的碳水化合物-蛋白质相互作用介导的。使用外源的多价高分子碳水化合物和单宁类植物源化合物可以拮抗粘附相互作用。通过不同的原位测定,筛选了一系列碳水化合物和富含碳水化合物和原花青素的植物提取物对幽门螺杆菌、空肠弯曲杆菌、牙龈卟啉单胞菌和白色念珠菌的潜在抗粘附作用。从秋葵果实中提取的富含葡萄糖醛酸的多糖可有效阻断幽门螺杆菌对人胃组织的粘附。这些化合物在体外对空肠梭菌也有很强的抑制作用(抑制率高达80%),但在受感染的肉鸡体内研究中,由于胃肠道系统的代谢,这些化合物无效。甘草多糖也富含葡萄糖醛酸,对幽门螺杆菌和牙龈卟啉卟啉具有较强的抗粘附作用(抑制率为60-70%)。天竺葵提取物对幽门螺杆菌具有一定的抗幽门螺杆菌作用,其主要成分为高分子原花青素。由于白色念珠菌的多功能粘附策略,没有检测到有效的化合物。提出了结构-活性关系,并讨论了碳水化合物基抗粘连剂在体内的潜在应用。
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引用次数: 46
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The Journal of pharmacy and pharmacology
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