Design, Synthesis And Studies On Biological Activities Of Curcumin Cinnamic Acid Derivatives

With the development of the economy, human healthy requirements are being increasing. However, the malignant neoplasm known as cancer seriously threat to human health and now it is one of the biggest challenges people are facing now. over the years, medical researchers and scientists are committed to the anti-tumor, antioxidant and antibacterial research and development of drugs, they are trying their best to find the most effective drugs of the cancer. Studies have shown that natural compounds have a variety of biological activities and they can be modified as the guide. By modifying them, we can achieve new drugs of high efficiency, low toxicity and high bioavailability.As is known to all that curcuminod is one of the most active ingredients of turmeric, and it is divided to curcumin. demethoxy curcumin and bisdemethoxy curcumin. Numbers of studies have found that curcumin compounds have antioxidant, antibacterial, immune regulation, antitumor physiological and pharmacological effects. Besides, curcuminods which are almost non-toxic to humans and animals have broad market potential. However, they are restricted to be applied in the field of food and medicine because of their poorly water-soluble, unstable structure and low bioavailability. In order to improve the biological activities and be better used in human clinical experiments, in this study, we chose curcuumin and bisdemethoxy curcumin as precursor compounds to synthesis curcuminods derivatives. In this paper, the research work can be divided into three parts:The first part is a brief introduction of curcumin, and analyzed the research progress and the biological activity of a variety of them.The second part is the introduction of the modification of curcumin, and how to design and synthesize a series of curcuminoids in this study. Firstly, we protected the hydroxyl of cinnamic acids by acetylation method, and then combined them with curcuminoids. In this part,41 new compounds including products with acetyl are synthesized and characterized.The third part is to test the biological activities of the new compounds, we used MTT assay to study the anticancer activity of those derivatives we have obtained against 3T3, LX-2, HepG-2 and MCF-7cell lines, used drilling method to test their antibacterial activities against Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and also studies their antioxidant capacities with DPPH method. Finally, we iscussed the structure-activity relationship of those compounds.