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首页> 外文期刊>Drug delivery. >Potent in vivo anticancer activity and stability of liposomes encapsulated with semi-purified Job's tear (Coix lacryma-jobi Linn.) extracts on human colon adenocarcinoma (HT-29) xenografted mice
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Potent in vivo anticancer activity and stability of liposomes encapsulated with semi-purified Job's tear (Coix lacryma-jobi Linn.) extracts on human colon adenocarcinoma (HT-29) xenografted mice

机译:半纯化乔布斯眼泪(Coix lacryma-jobi Linn。)提取物包裹的脂质体对人结肠腺癌(HT-29)异种移植小鼠的体内抗癌活性和稳定性

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摘要

The in vivo anticancer activity and stability of liposomes encapsulated with semi-purified Job's tear (Coix lacryma-jobi Linn.) extracts (S5L), prepared by supercritical carbon dioxide fluid technique, on human colon adenocarcinoma (HT29) xenografted mice were investigated. For the stability and the physicochemical characteristics, S5L showed a high stability of pH, good dispersibility, small particle size and stable zeta potential. Liposomes can protect linoleic acid in the extract comparing with the free S5. S5L kept at 4 degrees C for 3 months showed the highest linoleic acid content of 63.50%, whereas at 45 degrees C, the lowest linoleic acid content of 42.66% was observed. The anticancer activity and toxicity on xenografted mice were observed for 14 days. At the end of the experiment, the relative tumor volume (RTV) in the S5L-treated xenografted mice showed a significant RTV reduction. The high dose of S5 and S5L were potent with the highest inhibition of tumor growth of 48.67 and 54.75%, which was 86.94% and 97.81% of 5-fluorouracil, respectively. The apoptotic activity was shown in xenografted mice treated with S5 at medium and high dose, S5L, 5-fluorouracil and commercial product. All treated xenografted mice showed no toxic signs and symptoms, abnormality of internal organs histopathology and blood chemistry. This study has demonstrated the high physicochemical stability of liposomes encapsulated with semi-purified Job's tear extract and their potent anticancer activity on human colon adenocarcinoma xenografted model with the potential for further development to anticolon cancer drug.
机译:研究了用超临界二氧化碳流体技术制备的半纯化约伯眼泪(Coix lacryma-jobi Linn。)提取物(S5L)包裹的脂质体对人结肠腺癌(HT29)异种移植小鼠的体内抗癌活性和稳定性。就稳定性和理化特性而言,S5L具有较高的pH稳定性,良好的分散性,较小的粒径和稳定的Zeta电位。与游离S5相比,脂质体可以保护提取物中的亚油酸。 S5L在4摄氏度下放置3个月显示出最高的亚油酸含量为63.50%,而在45摄氏度下,观察到的最低亚油酸含量为42.66%。在异种移植小鼠中观察了14天的抗癌活性和毒性。在实验结束时,经S5L处理的异种移植小鼠的相对肿瘤体积(RTV)显示出显着的RTV降低。高剂量的S5和S5L对肿瘤生长的抑制作用最高,分别为48.67和54.75%,分别为5-氟尿嘧啶的86.94%和97.81%。在用中和高剂量的S5,S5L,5-氟尿嘧啶和市售产品处理的异种移植小鼠中显示出凋亡活性。所有处理过的异种移植小鼠均未显示中毒症状和体征,内部器官组织病理学和血液化学异常。这项研究表明,半纯化的乔布斯眼泪提取物封装的脂质体具有很高的理化稳定性,并且对人结肠腺癌异种移植模型具有强大的抗癌活性,并有可能进一步发展为抗结肠癌药物。

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