Key Laboratory of Modern Preparation of Traditional Chinese Medicine under Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, P. R. China.
College of Chemistry and Chemical Engineering, Central South University, Changsha, P. R. China.
J Sep Sci. 2022 Feb;45(4):938-944. doi: 10.1002/jssc.202100775. Epub 2021 Dec 28.
Traditional bioassay-guided investigation of bioactive compounds from natural products comprises critical steps, such as extraction, repeated column separation, and activity assay. Thus, the development of facile, rapid, and efficient technology is critically important. Here, a HepG2 cell-based extraction method was first developed to rapidly screen potential antitumor compounds from the seeds ofCassia obtusifolia. Then, an online extraction and enrichment-high-speed counter-current chromatography (HSCCC) strategy was fabricated to facilely and efficiently isolate target antitumor compounds, which included direct extraction from solid C. obtusifolia, removal of polar interferences, enrichment of target compounds, and preparative isolation by HSCCC using flow rate stepwise increasing mode. After further purification by Sephadex LH-20 column, five antitumor anthraquinones, aurantio-obtusin, 1-desmethylaurantio-obtusin, chryso-obtusin, obtusin, and questin, were obtained for structural characterization and bioassay verification. The results may not only provide new perspectives for facile and rapid investigation of bioactive compounds from complex natural products, but also offer a scientific basis for the potential applications of C. obtusifolia.
传统的生物活性化合物的导向生物测定方法包括从天然产物中提取、重复柱分离和活性测定等关键步骤。因此，开发简便、快速和高效的技术至关重要。在这里，首次开发了一种基于 HepG2 细胞的提取方法，用于快速筛选决明子种子中的潜在抗肿瘤化合物。然后，构建了一种在线提取和富集-高速逆流色谱（HSCCC）策略，以简便高效地分离目标抗肿瘤化合物，包括从固体决明子中直接提取、去除极性干扰、富集目标化合物以及采用流速逐步增加模式的 HSCCC 制备分离。进一步通过 Sephadex LH-20 柱纯化后，获得了 5 种抗肿瘤蒽醌类化合物，包括橙黄决明素、1-去甲基橙黄决明素、金雀异黄素、决明素和大黄素，用于结构表征和生物测定验证。这些结果不仅为从复杂天然产物中简便快速地研究生物活性化合物提供了新的视角，也为决明子的潜在应用提供了科学依据。
