新型黄连素肉桂酸类衍生物的设计与合成

The Design and Synthesis of Novel Cinnamic Berberine Derivatives

黄连素是从中草药黄连等植物中提取分离得到的一类异喹啉类生物碱,具有抗菌、抗肿瘤、抗氧化、降糖、降血脂、治疗心血管疾病等多种生物活性,在药物开发领域具有重要价值,因此其衍生物的设计与合成受到广泛关注。本文在前期构效关系研究的基础上,在9号位设计并引入一系列肉桂酸基团,合成出十种新型黄连素肉桂酸类衍生物,其分子结构已经过1HNMR和ESI-MS鉴定,为后续生物活性研究提供经验基础。

Berberine,an isoquinoline alkaloid extracted from Chinese herbs such as rhizome coptidis,was involved with a variety of biological activities,known as antibacterial,antineoplastic,antioxidative,anti-inflammatory,antidiabetic,antihyperlipidemic and curing angiocardiopathy effect,which could be of much value in the field of drug development. As a result,the design and synthesis of derivatives of berberine have aroused a great deal of concern in medicinal chemistry. In this paper,ten novel cinnamic berberine derivatives were designed and synthesized based on the structure-activity relationships early. Their structures were fully characterized by 1 H-NMR and ESI-MS spectroscopies which provide empirical basis for the study of biological activities.