Co-Crystals of Resveratrol and Polydatin with L-Proline: Crystal Structures, Dissolution Properties, and In Vitro Cytotoxicities
| العنوان: | Co-Crystals of Resveratrol and Polydatin with L-Proline: Crystal Structures, Dissolution Properties, and In Vitro Cytotoxicities |
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| المؤلفون: | Yusheng Cui, Guping Tang, Xiurong Hu, Yunxi Ji, Jianwei Wang, Xiajun Wu, Yijie Lou, Kaxi Yu, Hanxiao Bao, Zhaojun Wang |
| المصدر: | Molecules Volume 26 Issue 18 Molecules, Vol 26, Iss 5722, p 5722 (2021) |
| بيانات النشر: | MDPI, 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | crystal structure, Proline, Cell Survival, medicine.medical_treatment, viruses, Drug Compounding, Molecular Conformation, Pharmaceutical Science, Resveratrol, resveratrol, In Vitro Techniques, Article, Analytical Chemistry, solubility and dissolution rate, chemistry.chemical_compound, QD241-441, Pharmacokinetics, Glucosides, Bromide, Drug Discovery, Stilbenes, medicine, polydatin, Humans, Physical and Theoretical Chemistry, Solubility, Cytotoxicity, L-proline, Chemistry, Organic Chemistry, virus diseases, respiratory system, In vitro, pharmaceutical co-crystal, HEK293 Cells, Chemistry (miscellaneous), A549 Cells, Molecular Medicine, Crystallization, Adjuvant, Nuclear chemistry |
| الوصف: | Resveratrol (RSV) and polydatin (PD) have been widely used to treat several chronic diseases, such as atherosclerosis, pulmonary fibrosis, and diabetes, among several others. However, their low solubility hinders their further applications. In this work, we show that the solubility of PD can be boosted via its co-crystallization with L-proline (L-Pro). Two different phases of co-crystals, namely the RSV-L-Pro (RSV:L-Pro = 1:2) and PD-L-Pro (PD:L-Pro = 1: 3), have been prepared and characterized. As compared to the pristine RSV and PD, the solubility and dissolution rates of PD-L-Pro in water (pH 7.0) exhibited a 15.8% increase, whereas those of RSV-L-Pro exhibited a 13.8% decrease. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of pristine RSV, PD, RSV-L-Pro, and PD-L-Pro against lung cancer cell line A549 and human embryonic kidney cell line HEK-293 indicated that both compounds showed obvious cytotoxicity against A549, but significantly reduced cytotoxicity against HEK-293, with PD/PD-L-Pro further exhibiting better biological safety than that of RSV/RSV-L-Pro. This work demonstrated that the readily available and biocompatible L-Pro can be a promising adjuvant to optimize the physical and chemical properties of RSV and PD to improve their pharmacokinetics. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| تدمد: | 1420-3049 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d94a2799b6db1416399e20d5ca96df5 http://europepmc.org/articles/PMC8469398 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....1d94a2799b6db1416399e20d5ca96df5 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14203049 |
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