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根皮素与异烟肼的共晶：制备、表征及评价

Cocrystal of phloretin with isoniazid: preparation, characterization, and evaluation.

作者信息

Lu Zhongyu, Chen Hankun, Mo Jiaxin, Yuan Xiaohong, Wang Dawei, Zheng Xianhui, Zhu Wei

机构信息

The Second Clinical College of Guangzhou University of Chinese Medicine, Guangzhou University of Chinese Medicine Guangzhou China

Research and Development Department, Guangzhou Qinglan Biotechnology Company Limited Guangzhou China.

出版信息

RSC Adv. 2023 Apr 6;13(16):10914-10922. doi: 10.1039/d3ra00750b. eCollection 2023 Apr 3.

DOI:10.1039/d3ra00750b
PMID:37033443
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10077513/
Abstract

Phloretin (Phl) is a natural flavonoid compound with wide range of biological activities but demonstrates poor water solubility and limited pharmacological effects. In this study, one cocrystal of phloretin-isoniazid (Phl-Inz) was prepared successfully using the solvent evaporation method. The physical properties of cocrystal were characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TG), powder X-ray diffraction (PXRD), Fourier-transform infrared (FT-IR) and single crystal X-ray diffraction (SCXRD). The Hirshfeld surface analysis explained further interactions in the cocrystal. The solubility test showed that the solubility of the cocrystal was increased at pH 1.2 and pH 6.8 compared to that of the pure drug. The test simulated gastrointestinal digestion showed that the release of phloretin in the cocrystal was better than that in the pure phloretin. The results of the DPPH and ABTS scavenging activity showed that the antioxidant activity of the cocrystal was improved. The anticancer assay exhibited improved cytotoxicity in the Phl-Inz cocrystal as compared with the pure Phl.

摘要

根皮素（Phl）是一种具有广泛生物活性的天然黄酮类化合物，但水溶性差，药理作用有限。本研究采用溶剂蒸发法成功制备了根皮素-异烟肼共晶体（Phl-Inz）。通过差示扫描量热法（DSC）、热重分析（TG）、粉末X射线衍射（PXRD）、傅里叶变换红外光谱（FT-IR）和单晶X射线衍射（SCXRD）对共晶体的物理性质进行了表征。Hirshfeld表面分析进一步解释了共晶体中的相互作用。溶解度测试表明，与纯药物相比，共晶体在pH 1.2和pH 6.8时的溶解度增加。模拟胃肠道消化试验表明，共晶体中根皮素的释放优于纯根皮素。DPPH和ABTS清除活性结果表明，共晶体的抗氧化活性有所提高。抗癌试验表明，与纯Phl相比，Phl-Inz共晶体的细胞毒性有所改善。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/c05f1d353f28/d3ra00750b-f12.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/c05f1d353f28/d3ra00750b-f12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/d286e116d149/d3ra00750b-f1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/d20fbcadead7/d3ra00750b-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/9511b5d77372/d3ra00750b-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/af07ce933919/d3ra00750b-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/7d9f72339b16/d3ra00750b-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/6893255377cd/d3ra00750b-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/78234fb78749/d3ra00750b-f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/a19dd71d736f/d3ra00750b-f10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/4e1909621ecc/d3ra00750b-f11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0da6/10077513/c05f1d353f28/d3ra00750b-f12.jpg

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