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一种来自汉密尔顿氏马兜铃的具有多步溃疡预防活性的新型酚结合果胶多糖。

A novel phenol-bound pectic polysaccharide from Decalepis hamiltonii with multi-step ulcer preventive activity.

作者信息

Srikanta B M, Siddaraju M N, Dharmesh S M

机构信息

Department of Biochemistry and Nutrition, CFTRI, Mysore -570020, Karnataka, India.

出版信息

World J Gastroenterol. 2007 Oct 21;13(39):5196-207. doi: 10.3748/wjg.v13.i39.5196.

Abstract

AIM

To investigate H(+), K(+)-ATPase inhibition, anti-H pylori, antioxidant, and the in vivo antiulcer potential of a pectic polysaccharide from Swallow root (Decalepis hamiltonii; SRPP).

METHODS

SRPP, with known sugar composition [rhamnose: arabinose: xylose: galactose in the ratio of 16:50:2:32 (w/w), with 141 mg/g of uronic acid] was examined for anti-ulcer potency in vivo against swim/ethanol stress-induction in animal models. Ulcer index, antioxidant/antioxidant enzymes, H(+), K(+)-ATPase and gastric mucin levels were determined to assess the anti-ulcer potency. Anti-H pylori activity was also determined by viable colony count and electron microscopic studies.

RESULTS

SRPP, containing phenolics at 0.12 g GAE/g, prevented stress-induced gastric ulcers in animal models by 80%-85%. Down regulation of gastric mucin 2-3 fold, antioxidant/antioxidant enzymes and upregulation of 3 fold of H(+), K(+)-ATPase in ulcerous animals were normalized upon treatment with SRPP. Histopathological analysis revealed protection to the disrupted gastric mucosal layer and epithelial glands. SRPP also inhibited H(+), K(+)-ATPase in vitro, at an IC(50) of 77 microg/mL as opposed to that of 19.3 microg/mL of Lansoprazole and H pylori growth at Minimum Inhibitory Concentration (MIC) of 150 microg/mL. In addition, free radical scavenging (IC(50)-40 microg/mL) and reducing power (3200 U/g) activities were also observed.

CONCLUSION

SRPP, with defined sugar composition and phenolics, exhibited multi-potent free radical scavenging, antioxidant, anti-H pylori, inhibition of H(+), K(+)-ATPase and gastric mucosal protective activities. In addition, SRPP is non-toxic as opposed to other known anti-ulcer drugs, and therefore may be employed as a potential alternative for ulcer management.

摘要

目的

研究来自燕子根(Decalepis hamiltonii;SRPP)的一种果胶多糖对H⁺,K⁺-ATP酶的抑制作用、抗幽门螺杆菌作用、抗氧化作用以及体内抗溃疡潜力。

方法

对已知糖组成[鼠李糖:阿拉伯糖:木糖:半乳糖比例为16:50:2:32(w/w),含141 mg/g糖醛酸]的SRPP进行体内抗溃疡效力研究,采用动物模型游泳/乙醇应激诱导法。测定溃疡指数、抗氧化剂/抗氧化酶、H⁺,K⁺-ATP酶和胃黏液水平以评估抗溃疡效力。还通过活菌计数和电子显微镜研究确定抗幽门螺杆菌活性。

结果

SRPP含0.12 g没食子酸当量/g酚类物质,可使动物模型中应激诱导的胃溃疡预防率达80%-85%。经SRPP治疗后,溃疡动物中胃黏液下调2-3倍、抗氧化剂/抗氧化酶以及H⁺,K⁺-ATP酶上调3倍的情况恢复正常。组织病理学分析显示对受损胃黏膜层和上皮腺体有保护作用。SRPP在体外也抑制H⁺,K⁺-ATP酶,IC₅₀为77 μg/mL,而兰索拉唑为19.3 μg/mL,SRPP对幽门螺杆菌生长的最低抑菌浓度(MIC)为150 μg/mL。此外,还观察到自由基清除(IC₅₀-40 μg/mL)和还原能力(3200 U/g)活性。

结论

具有明确糖组成和酚类物质的SRPP表现出多效性自由基清除、抗氧化、抗幽门螺杆菌、抑制H⁺,K⁺-ATP酶以及胃黏膜保护活性。此外,与其他已知抗溃疡药物不同,SRPP无毒,因此可作为溃疡治疗的潜在替代药物。

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