Pharmaceutical Informatics Institute, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
SZYY Group Pharmaceutical Limited, Taizhou 225500, China.
Molecules. 2018 Oct 16;23(10):2649. doi: 10.3390/molecules23102649.
Flower of (FAM) is clinically effective to treat chronic kidney disease (CKD) with a relatively high dosage. To improve the efficacy and the compliance of patients, macroporous resins were adopted to enrich and purify flavonoids from FAM, which are thought to be the major renal protective constituents in FAM. After screening six different kinds of macroporous resins, HPD-100 was selected for its great adsorption and desorption capacity. Then, orthogonal design tests were used to optimize parameters in the processes of impurity removal and flavonoids of FAM desorption on column chromatogram. Moreover, process scale-up was performed, and purification effects maintained after amplification. After purification, the content of seven main flavonoids in the product increased from 8.29% to 51.43%. Protective and anti-inflammatory effects of crude extract and the flavonoid component of FAM after purification were investigated on the adriamycin-damaged HK-2 cells and lipopolysaccharide-stimulated Raw 264.7 cells models. Both bioactivities were improved greatly after purification for these two cell models. Therefore, the purification process had enriched the main bioactive constituents with potential alleviating kidney injury activities. The flavonoid component of FAM is worthy of being developed as an improved remedy for CKD with better patients' compliance.
（FAM）花在高剂量下对治疗慢性肾病（CKD）具有临床疗效。为提高疗效和患者的顺应性，采用大孔树脂从 FAM 中富集和纯化黄酮类化合物，这些化合物被认为是 FAM 中主要的肾保护成分。经过筛选六种不同的大孔树脂，HPD-100 因其高吸附和解吸能力而被选中。然后，采用正交设计试验对柱色谱上杂质去除和 FAM 中黄酮类化合物解吸过程的参数进行了优化。此外，还进行了工艺放大，放大后仍保持了纯化效果。经纯化后，产品中七种主要黄酮类化合物的含量从 8.29%增加到 51.43%。对阿霉素损伤的 HK-2 细胞和脂多糖刺激的 Raw 264.7 细胞模型研究了粗提取物和 FAM 黄酮成分的保护和抗炎作用。这两种细胞模型的生物活性在经过纯化后都得到了显著提高。因此，该纯化工艺富集了具有潜在缓解肾损伤活性的主要生物活性成分。FAM 的黄酮成分值得开发为一种改善 CKD 患者顺应性的改良药物。
