Zhou Wenbin, Wang Man, Zhang Aiqin, Huang Danrong, Guo Hua, Shen Gangyi
Key Laboratory of Ethnomedicine (Minzu University of China), Ministry of Education, School of Pharmacy, Minzu University of China, Beijing 100081, China.
College of Life and Environmental Sciences, Minzu University of China, Beijing 100081, China.
Chin Herb Med. 2022 Nov 1;15(2):329-336. doi: 10.1016/j.chmed.2022.06.008. eCollection 2023 Apr.
To establish a method for directional screening of the cytotoxic components from the medicinal herb of by a combination of surface plasmon resonance (SPR) biosensor and chromatographic isolation technology.
Under the guidance of bioactive assessment based on binding abilities between objects and the α-Mannosidase (α-Man) target, the active components from different solvents extracts, different polar extraction parts and fractions were screened orderly and directionally using SPR. Components with a high binding ability to α-Man can be precisely oriented in a narrower fractions range and are easy to isolate. Three human cancer cells were used to evaluate the cytotoxic activity of component with the highest affinity to α-Man.
Eight compounds were isolated and identificated from for the first time. Deoxyvasicinone possessed the highest affinity to α-Man among them. Moreover, deoxyvasicinone showed good effects on inhibited proliferation of human hepatoma cells HepG2 (IC = 5.7 μmol/L), human breast cancer cells MCF7 (IC = 7.21 μmol/L) and human lung cancer cells HCC827 (IC = 0.75 μmol/L), respectively. In particular, its inhibitory effect on HCC827 was stronger than the positive drug gefitinib (IC = 1.65 μmol/L).
A comprehensive strategy of directional screening potential cytotoxic components from herb based on biomolecular interaction and chromatography was established. Deoxyvasicinone as an effective anti-cancer component was initially isolated from . It is expected that this screening strategy could provide new perspectives for rapid screening and identification of active components from natural plants with the complex matrix.
建立一种结合表面等离子体共振（SPR）生物传感器与色谱分离技术，从药用植物中定向筛选细胞毒性成分的方法。
在基于目标物与α-甘露糖苷酶（α-Man）靶点结合能力的生物活性评估指导下，利用SPR依次对不同溶剂提取物、不同极性萃取部位及馏分中的活性成分进行定向筛选。与α-Man具有高结合能力的成分能够在较窄的馏分范围内被精准定位，且易于分离。使用三种人类癌细胞评估对α-Man具有最高亲和力的成分的细胞毒性活性。
首次从该药用植物中分离鉴定出8种化合物。其中脱氧瓦西酮对α-Man具有最高亲和力。此外，脱氧瓦西酮分别对人肝癌细胞HepG2（IC = 5.7 μmol/L）、人乳腺癌细胞MCF7（IC = 7.21 μmol/L）和人肺癌细胞HCC827（IC = 0.75 μmol/L）的增殖具有良好的抑制作用。特别是，其对HCC827的抑制作用强于阳性药物吉非替尼（IC = 1.65 μmol/L）。
建立了一种基于生物分子相互作用和色谱法从草药中定向筛选潜在细胞毒性成分的综合策略。脱氧瓦西酮作为一种有效的抗癌成分首次从该药用植物中分离得到。预计该筛选策略可为从具有复杂基质的天然植物中快速筛选和鉴定活性成分提供新的视角。
