抗脑缺血活性的红花新苷及其类似物合成和生物活性研究

Saffloneoside (XG) was a new compound of quinochalcoside and isolated from Carthamus tinctorius L. XG exhibited against cerebral ischemia injury activity in vivo. And the effect of XG was better than Butylphthalide. Furthermore, XG exhibited antiinflammatory activities by cerebral ischemia injury in vitro. And 2 patents have been authorized about the structure and pharmacological activities of XG. In addition, 3 analogues of quinochalcosides with five and six ring show protective effect against neuronal injury in vitro..The content of XG is very low in safflower, and a lot of XG were not obtained using extraction. So this topic would obtain saffloneoside by synthesis method to solve the low content and the difficult obtainment of XG. To study the structure of diversity, a series of quinochalcoside analogues with five and six ring of saffloneosides can be got by chemical synthesis method. And the synthesized compounds and saffloneoside are evaluated against cerebral ischemia injury activities, then superior precursor of drugs with new structure and high activities against cerebral ischemia injury can be got. Therefore this topic not only has great academic significance in theory, but also has the important application value.

红花新苷（XG）是从红花药材中获得的一个结构新颖的五元类醌式查尔酮碳苷类成分。体内药理实验表明其具有较强的抗脑缺血损伤作用，其作用强于丁苯酞。体外作用机制显示其对脑缺血引起的炎症具有一定的抑制作用，同时该化合物及其药理活性已获得授权专利2项。另外，通过合成得到的3个五元和六元的醌式查尔酮苷类似物的体外活性显示了它们具有神经元损伤的保护作用。.红花药材中红花新苷的含量很低，无法提取获得，所以本课题欲通过合成的方法获得红花新苷，以解决XG含量低，难以获得的问题。此外，对红花中所含有的红花新苷等五元和六元的醌式查尔酮类进行类似物的合成研究，以丰富此类成分的结构多样性，并将合成得到的化合物与XG共同进行抗脑缺血损伤体内外活性评价，进而优选出同时具有新结构和高活性的抗脑缺血药物先导物。因此该课题不仅在理论上具有显著的学术意义，而且具有重要的应用价值。

红花新苷（XG）是从红花药材中获得的一个结构新颖的五元类醌式查尔酮碳苷类成分。体内药理实验表明其具有较强的抗脑缺血损伤作用，另外，红花药材中红花新苷的含量很低，无法提取获得，所以本课题通过合成的方法获得红花新苷，解决了XG含量低，难以获得的问题。此外，对红花中所含有的红花新苷等五元和六元的醌式查尔酮类进行类似物的合成研究，共合成醌式查尔酮类似物124个，丰富此类成分的结构多样性，并将合成得到的化合物与XG共同进行抗脑缺血损伤体内外活性评价，说明红花新苷具有较好的抗脑缺血性损伤作用，与已经上市的抗脑缺血药物丁苯酞的活性相当。对合成得到的部分单体化合物进行了体外神经保护活性的筛选，一共筛选了60个化合物。12个化合物在该模型下具有较强的神经保护活性。发表SCI研究论文3篇，SCI总影响因子大于8，申请国内发明专利2项，为红花新苷及其类似物的成药性研究奠定了基础。