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β-环糊精-姜黄素自组装增强姜黄素在前列腺癌细胞中的递送。

beta-Cyclodextrin-curcumin self-assembly enhances curcumin delivery in prostate cancer cells.

机构信息

Cancer Biology Research Center, Sanford Research/USD, Sioux Falls, SD 57105, USA.

出版信息

Colloids Surf B Biointerfaces. 2010 Aug 1;79(1):113-25. doi: 10.1016/j.colsurfb.2010.03.039. Epub 2010 Apr 3.

Abstract

Curcumin, a hydrophobic polyphenolic compound derived from the rhizome of the herb Curcuma longa, possesses a wide range of biological applications including cancer therapy. However, its prominent application in cancer treatment is limited due to sub-optimal pharmacokinetics and poor bioavailability at the tumor site. In order to improve its hydrophilic and drug delivery characteristics, we have developed a beta-cyclodextrin (CD) mediated curcumin drug delivery system via encapsulation technique. Curcumin encapsulation into the CD cavity was achieved by inclusion complex mechanism. Curcumin encapsulation efficiency was improved by increasing the ratio of curcumin to CD. The formations of CD-curcumin complexes were characterized by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), thermo-gravimetric analysis (TGA), scanning electron microscope (SEM), and transmission electron microscope (TEM) analyses. An optimized CD-curcumin complex (CD30) was evaluated for intracellular uptake and anti-cancer activity. Cell proliferation and clonogenic assays demonstrated that beta-cyclodextrin-curcumin self-assembly enhanced curcumin delivery and improved its therapeutic efficacy in prostate cancer cells compared to free curcumin.

摘要

姜黄素是一种源自姜黄根茎的疏水性多酚化合物,具有广泛的生物应用,包括癌症治疗。然而,由于其在肿瘤部位的药代动力学不佳和生物利用度差,其在癌症治疗中的突出应用受到限制。为了提高其亲水性和药物传递特性,我们通过包封技术开发了一种β-环糊精(CD)介导的姜黄素药物传递系统。通过包合机制将姜黄素包封到 CD 腔中。通过增加姜黄素与 CD 的比例来提高姜黄素的包封效率。通过傅里叶变换红外(FTIR)、差示扫描量热法(DSC)、热重分析(TGA)、扫描电子显微镜(SEM)和透射电子显微镜(TEM)分析来表征 CD-姜黄素复合物的形成。优化后的 CD-姜黄素复合物(CD30)用于细胞内摄取和抗癌活性评估。细胞增殖和集落形成实验表明,与游离姜黄素相比,β-环糊精-姜黄素自组装增强了姜黄素的递送,并提高了其在前列腺癌细胞中的治疗效果。

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