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壳聚糖包封染料木黄酮的合成与表征:其抗增殖和抗血管生成活性。

Synthesis and characterisation of chitosan-encapsulated genistein: its anti-proliferative and anti-angiogenic activities.

机构信息

Department of Biology, Mashhad Branch, Islamic Azad University, Mashhad, Iran.

Mashhad Branch, Agricultural Biotechnology Research Institute of Iran (ABRII), Agricultural Research, Education, and Extension Organization (AREEO), Mashhad, Iran.

出版信息

J Microencapsul. 2020 Jun;37(4):305-313. doi: 10.1080/02652048.2020.1740804. Epub 2020 Mar 20.

DOI:10.1080/02652048.2020.1740804
PMID:32148140
Abstract

The study was carried out to synthesise and characterise the chitosan-encapsulated genistein (CHI-En/Gen) and determine its anti-cancer and anti-angiogenic properties. The cytotoxic and anti-angiogenic activity of CHI-En/Gen was performed using MTT and chorioallantoic membrane assay. The molecular action was determined using flow cytometry and gene expression. The synthesised CHI-En/Gen was in submicron size, spherical in shape and with entrapment efficiency and loading efficiency of 76.8% (w/w) and 32.6% (w/w), respectively. The CHI-En/Gen notably inhibited the growth and proliferation of human colorectal cancer cells (HT-29) while did not affect the viability of human dermal fibroblast as normal cell. The flow cytometry and the caspase-3 gene expression analyses revealed the apoptotic cells death in the HT-29 cells. Moreover, the encapsulated genistein showed anti-angiogenic activity. The CHI-En/Gen appeared as a promising carrier for the colon delivery of genistein to be used in complementary health approaches for the cancer prevention.

摘要

本研究旨在合成并表征壳聚糖包裹染料木黄酮(CHI-En/Gen),并确定其抗癌和抗血管生成特性。采用 MTT 和鸡胚尿囊膜试验测定 CHI-En/Gen 的细胞毒性和抗血管生成活性。采用流式细胞术和基因表达测定法确定分子作用。合成的 CHI-En/Gen 呈亚微米级大小,呈球形,包封效率和载药量分别为 76.8%(w/w)和 32.6%(w/w)。CHI-En/Gen 显著抑制人结直肠癌细胞(HT-29)的生长和增殖,而对正常细胞人真皮成纤维细胞的活力没有影响。流式细胞术和 caspase-3 基因表达分析显示 HT-29 细胞发生凋亡性细胞死亡。此外,包裹的染料木黄酮表现出抗血管生成活性。CHI-En/Gen 似乎是一种很有前途的载体,可将染料木黄酮递送至结肠,用于癌症预防的补充健康方法。

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