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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Evaluation of the antiulcerogenic activity of violacein and its modulation by the inclusion complexation with beta-cyclodextrin.
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Evaluation of the antiulcerogenic activity of violacein and its modulation by the inclusion complexation with beta-cyclodextrin.

机译：通过与β-环糊精的包合络合评估紫精的抗溃疡活性及其调节作用。

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The effects of beta-cyclodextrin (betaCD) inclusion complexation on the ability of violacein to prevent gastric ulceration in mice were studied. Violacein-betaCD inclusion complexes were prepared in 1:1 and 1:2 molar ratios and analysed by differential scanning calorimetry and powder X-ray diffractometry. Violacein previously administered orally at 10 mg/kg significantly reduced indomethacin-induced gastric lesions, as well as 100 mg/kg of cimetidine (positive control). However, betaCD complexation in both molar ratios significantly potentiated the protective action of violacein. In the HCl--ethanol-induced gastric ulcer model, violacein and the 1:2 inclusion complex (10 mg/kg, p.o.) inhibited gastric damage by almost 85%, whereas a 63% reduction was observed for the positive control, lansoprazole, at 30 mg/kg. In contrast, treatment with the 1:1 inclusion complex resulted in almost total disappearance of the antiulcer activity in this model. No significant changes in stress-induced gastric injury werefound. In addition, the 1:2 inclusion complex improved the antilipoperoxidant activity of violacein in rat liver cells exposed to t-butyl hydroperoxide, whereas the 1:1 complex was less active than violacein. In summary, the 1:2 betaCD inclusion complex has gastroprotective properties similar to or higher than that of violacein. An increase in mucosal defensive mechanisms and protection against peroxidative damage might be involved.
机译：研究了β-环糊精（βCD）包合物对紫精的预防小鼠胃溃疡的能力。以1：1和1：2的摩尔比制备紫草素-βCD包合物，并通过差示扫描量热法和粉末X射线衍射法进行分析。先前以10 mg / kg口服的紫堇青素可显着减少消炎痛诱导的胃部病变，以及100 mg / kg的西咪替丁（阳性对照）。然而，两种摩尔比的βCD络合均显着增强了紫精的保护作用。在HCl-乙醇诱导的胃溃疡模型中，紫精和1：2包合物（10 mg / kg，口服）抑制胃损伤近85％，而阳性对照兰索拉唑减少了63％， 30 mg / kg。相反，在该模型中，用1：1包合物包络的治疗导致抗溃疡活性几乎完全消失。没有发现应激引起的胃损伤有明显变化。此外，1：2包合物可以改善紫杉醇在暴露于叔丁基氢过氧化物的大鼠肝细胞中的抗脂质过氧化活性，而1：1复合物的活性却不如紫杉醇。总之，1：2 betaCD包合物具有类似于或高于紫精的胃保护特性。可能涉及粘膜防御机制的增强和对过氧化损伤的保护。

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