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通过体外形成包合物实现氯化血红素的肠道靶向消化

Intestinal-Targeted Digestion of Heme Chloride by Forming Inclusion Complexes In Vitro.

作者信息

Yu Qianfan, Huang Li, Zhang Yuemei, Teng Wendi, Wang Ying, Cao Jinxuan, Wang Jinpeng

机构信息

Key Laboratory of Geriatric Nutrition and Health, Beijing Technology and Business University, Ministry of Education, Beijing 100048, China.

School of Food and Health, Beijing Technology and Business University, Beijing 100048, China.

出版信息

Foods. 2024 Sep 27;13(19):3078. doi: 10.3390/foods13193078.

DOI:10.3390/foods13193078
PMID:39410113
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11482528/
Abstract

Hemin, a heme-like compound with significant biological activity, shows promise as an iron supplement for humans. Nonetheless, its poor solubility in water greatly impedes its absorption and utilization. To surmount this obstacle, researchers have chosen various cyclodextrins with distinct cavity sizes and derivative groups to act as hosts, forming inclusion complexes with hemin chloride. Among these, γ-cyclodextrin has been identified as the optimal carrier, based on a thorough evaluation of its encapsulation efficiency, solubility, and molecular docking. Multiple characterization techniques further confirmed the formation of these inclusion complexes. Results from IEC-6 cell experiments indicated that the cytotoxicity of the inclusion complexes was lower than that of FeSO. Static and dynamic gastrointestinal simulation digestion systems were established, and the results showed that the bioavailability of the inclusion complex was significantly higher than that of raw hemin. Additionally, only about 0.29% of hemin chloride is digested by gastric enzymes, whereas 9.52% is digested by pancreatic enzymes in the static gastrointestinal simulation digestion system, with similar outcomes observed in the dynamic system. These findings suggest that targeted digestion in the intestine significantly enhances the bioavailability of hemin chloride by forming inclusion complexes in vitro.

摘要

氯高铁血红素是一种具有显著生物活性的类血红素化合物,有望成为人类的铁补充剂。然而,其在水中的低溶解度极大地阻碍了其吸收和利用。为克服这一障碍,研究人员选择了具有不同腔径和衍生基团的各种环糊精作为主体,与氯化血红素形成包合物。其中,基于对其包封效率、溶解度和分子对接的全面评估,γ-环糊精已被确定为最佳载体。多种表征技术进一步证实了这些包合物的形成。IEC-6细胞实验结果表明,包合物的细胞毒性低于硫酸亚铁。建立了静态和动态胃肠模拟消化系统,结果表明包合物的生物利用度显著高于未加工的氯高铁血红素。此外,在静态胃肠模拟消化系统中,只有约0.29%的氯化血红素被胃酶消化,而9.52%被胰酶消化,在动态系统中也观察到类似结果。这些发现表明,通过体外形成包合物,肠道中的靶向消化显著提高了氯化血红素的生物利用度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/e9505269f263/foods-13-03078-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/db01e2e0e63f/foods-13-03078-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/38794c0dfbda/foods-13-03078-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/2699cedc56d1/foods-13-03078-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/23b653ae30aa/foods-13-03078-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/6196e97f89e6/foods-13-03078-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/5a9b32be2591/foods-13-03078-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/e9505269f263/foods-13-03078-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/db01e2e0e63f/foods-13-03078-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/38794c0dfbda/foods-13-03078-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/2699cedc56d1/foods-13-03078-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/23b653ae30aa/foods-13-03078-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/6196e97f89e6/foods-13-03078-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/5a9b32be2591/foods-13-03078-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b37e/11482528/e9505269f263/foods-13-03078-g007.jpg

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