重楼药材基原植物非药用部位可利用的基础研究

Paridis Rhizoma is one of the important medicinal plants in China and is the main raw material of nearly 80 Chinese patent medicines, such as ‘Yunnan Baiyao’ and ‘Gongxuening Jiaonang’. It has been mainly used as hemostatic and contractile agonist for the uterus. Chinese pharmacopoeia rules the original plant of traditional Chinese drug “Chong Lou” is the rhizome of Paris polyphylla var. yunnanensis or Paris polyphylla var. chinensis.Because of slow growth and overharvesting for many years, the wild populations of this herb have greatly declined and are in the edge of distinction.However, non-medicinal parts (leaves, stems, fibril, etc.) of this herb, which can regenerate every year, were discarded. This has resulted in enormous waste of resources. Our group found that the extract of the non-medicinal parts of P. polyphylla var. yunnanensis and P. polyphylla var. chinensis showed similar hemostatic and rat uterine contractility activities with those that the extract of rhizomes. We have obtained more than 40 steroidal glycosides from the effective parts of the stems, leaves, and fibril of P. polyphylla var.yunnanensis, including 15 new steroidal glycosides and some known steroidal saponins which had been isolated from Paridis Rhizoma. Some isolates showed significant bioactivities of platelet agonist and contractile agonist for the uterus. The project is firstly planned to illuminate their substance foundation and structure-activity relationships for platelet agonist and contractile agonist for the uterus about the non-medicinal parts of P. polyphylla var. yunnanensis and P. polyphylla var. chinensis on the basis of the quickly separation method and LC-MS deduplication technology. Secondly, we will clarify the differences of the active compounds in the rhizomes (medicinal part) and the non-medicinal parts of Paridis Rhizoma by the qualitative and quantitative analysis. According to the therapeutic material basis, we will introduce the species which non-medicinal parts may replace the rhizomes. This research can set up the therapeutic material basis to broaden and alleviate the shortage of Paridis Rhizoma resources in the following study.

重楼是重要的药用植物之一,为云南白药、宫血宁胶囊等近80种重要中成药的主要原料,主要用于止血和缩宫。《中国药典》规定重楼药材的基原为云南重楼或七叶一枝花的根茎。由于需求量大，长期靠采挖野生资源，生长周期长，生物量年积累少导致其资源濒危，但资源量更大且每年可再生的非药用部分(茎叶等)被丢弃，浪费了资源。申请人课题组前期研究发现这两种基原植物的非药用部位提取物具有类似根茎的止血和缩宫活性或更强，目前已从茎叶和须根中得到40余个化合物，包括15个结构较新颖的甾体皂苷。部分化合物显示出较好的止血和缩宫活性。本项目拟在前期研究基础上，借助已建立的甾体皂苷快速识别分离方法和LC-MS去重复技术，阐明两种基原植物的非药用部位具有止血和缩宫的物质基础和开展构效关系研究，并定性定量研究其与药用部位物质基础的差异性,从物质基础角度阐明非药用部位是否可以替代药用部位,对缓解重楼资源短缺有着极其重要的意义。

重楼是重要的药用植物之一，由于需求量大，长期靠采挖野生资源，生长周期长，生物量年积累少导致其资源濒危，但资源量更大且每年可再生的非药用部分被丢弃，浪费了资源。为了实现资源的综合利用，本项目从止血等生物活性等效性、物质基础及有效成分含量三个方面开展研究，评价非药用部位是否可以替代药用部位或开发新的用途。.本项目按照《项目任务书》执行，对重楼药材基原植物（滇重楼和七叶一枝花）的非药用部位开展了止血、抗肿瘤、抗菌等活性评价，并在此基础上对非药用部位茎叶、侧根开展了系统的化学成分研究及主要活性成分的含量分析。研究结果表明：（1）滇重楼的茎叶总皂苷诱导血小板聚集活性（止血）稍强于滇重楼根茎总皂苷，抗肿瘤活性弱于重楼根茎总皂苷；茎叶总皂苷对白色念珠菌Candida albicans (5314)和 C. albicans (Y0109) 显示出显著的抑制活性，其中对白色念珠菌C. albicans (Y0109)的抑制活性强于阳性对照药伏立康唑，并阐明了其主要的抗菌成分；（2）滇重楼和七叶一枝花的茎叶、须根及假种皮中富含甾体皂苷，从中共分离鉴定了106个化合物（主要为甾体皂苷），包括31个新的甾体皂苷，主要成分和根茎中基本一致，茎叶中含有根茎中没有的nuatigenin型甾体皂苷，侧根中主要以偏诺皂苷及其衍生物为主，并开展了止血活性的评价和构效关系研究，主要止血活性成分基本与根茎一致；（3）含量分析表明，茎叶及侧根中均含有2015版《中国药典》规定的4个皂苷，其中茎叶50%的样品符合药典规定，侧根35%的样品能达到药典要求。综上所述，重楼非药用部位在止血、抗肿瘤和抗菌方面可以替代药用部位，但其安全性和药效学仍需进行评价和深入研究。