治疗脑中风新天然活性成分灯盏花甙的全合成及结构优化

Erigeside I (6-O-caffeoyl-b-D-glucopyranosyl-3-O-g-pyranonoside), a new compound isolated from Erigeron breriscapus(Vant.)Hand-Mazz, has strong activity of antioxidant, scavenging oxidation free radical, and can increase the microcirculation and hemorheology, relaxing cerebral vessels and treating apoplexy of brain. In this study, the following steps have been carried out on the basis of the total synthesis of Erigeside I: 11 new compounds have been designed and synthesized; the effects of Erigeside I and its derivatives on anti-oxidation and inhibiting the apoptosis induced by hypoxia/reoxygenation have been investigated. Meanwhile, more than 30 compounds were isolated and 12 of them were the first isolated. The preliminary test show that caffeoyl conjugation compounds from Erigeron breriscapus have the activity of protecting the injury from hypoxia/reoxygenation.

从中药灯盏花中分离得到了一个新型的甙类化合物—灯盏花甙，具有很强的改善脑代谢和抗氧化活性。本研究拟对它进行全合成研究且根强其作用机制进行结构优化并合成一系列衍生物，应用改善脑代谢与抗氧化模型相结合进行活性研究，为从天然药物中开发我国自主创新的脑中风治疗药物提供科学依据和先导化合物。