Phakellia 属海绵中抗肿瘤活性环肽化合物的发现

Tumor is still a threat to human health and life. Looking for high efficiency, low toxicity anticancer drugs is one of the hot spot of marine natural products chemistry and medicinal chemistry research at present.Because of its small relative molecular mass (Mr), high activity, low toxicity, Small molecule peptide has important value in the clinical therapy of tumor.Literature shows that Phakellia genus sponge contains many cyclic peptide compounds with novel structure and significant antitumor activity .Previous studies of our research group have discovered that three species of Phakellia genus sponge contain cyclic peptide compounds and their crude extract has obvious anti-tumor activity.This project uses a bidirectional tracing combining the antitumor activity and modern spectroscopy, together with modern separation techniques and spectroscopic method, trying to separate and identify cyclic peptides with antitumor activity from the Phakellia genus sponge. The research is expected to obtain high efficiency and low toxicity antitumor active compounds or leading compounds of independent intellectual property rights and lay foundation for the development of new antitumor drugs as well as promote the development of marine natural products chemistry, medicinal chemistry and other related disciplines.

肿瘤仍是威胁人类健康和生命的巨大杀手，寻找高效、低毒的抗肿瘤药物是目前海洋天然产物化学和药物化学研究的热点之一。小分子多肽由于其具有相对分子质量(Mr) 小、活性高、毒性低的特点，在肿瘤的临床治疗上有重要的价值。文献表明Phakellia 属海绵中含有许多结构新颖，抗肿瘤活性显著的环肽类化合物。课题组前期研究发现三种Phakellia属海绵中含有环肽类化合物，且粗提物具有较强的抗肿瘤活性。本项目采用抗肿瘤活性和现代波谱学双向追踪，结合现代分离技术和光谱学方法，分离并鉴定一种Phakellia属海绵中抗肿瘤活性环肽类化合物。该研究有望直接获得具有自主知识产权的高效低毒抗肿瘤药物活性化合物或先导化合物，为研发新型抗肿瘤药物奠定基础，同时推动海洋天然产物化学、药物化学等相关学科发展。

肿瘤仍是威胁人类健康和生命的巨大杀手，寻找高效、低毒的抗肿瘤药物是目前海洋天然产物化学和药物化学研究的热点之一。本项目采用抗肿瘤活性和现代波谱学双向追踪，结合现代分离技术和光谱学方法，分离并鉴定一种Phakellia属海绵及其共生真菌中抗肿瘤活性环肽类化合物。共分离得到82个化合物，其中20个为新化合物，包括4个新的环五脂肽类化合物。并对这些化合物的生物活性进行了测试。对侧扁软柳珊瑚Subergorgia suberosa 的化学成分和活性进行研究，从柳珊瑚Subergorgia suberosa的乙醇提取液中分离得到39个化合物，其中19个为新化合物。课题组合成了9个Galaxamide 类似物，对其抗肿瘤活性进行研究。以上研究为发现海洋药用生物新资源及药物先导化合物提供了研究基础。