人参二醇与人参三醇衍生物的氧化及细胞毒活性
The Oxidation and Cytotoxic Activity Screening of Panaxadiol and Panaxatriol Derivatives
-
摘要: 目的 以人参二醇和人参三醇为起始原料制备达玛烷型三萜衍生物, 并进行体外细胞毒活性筛选.方法 以人参二醇和人参三醇经PCC (氯铬酸吡啶盐) 氧化、DDQ (二氯二氰基苯醌) 氧化后的产物为原料, 进一步与间氯过氧苯甲酸 (m-CPBA) 进行氧化反应, 得到的开环产物采用MTT法进行体外细胞毒活性筛选.结果共制备了4个开环产物 (化合物2、4、6、8) .结论 这4个开环产物均为新化合物, 化合物2和4对几种肿瘤细胞株具有显著的细胞毒活性.Abstract: Objective To study the synthesis of dammarane-type triterpene derivatives by using Panaxadiol and Panaxatriol as starting materials and screen their cytotoxic activity in vitro. Methods The products derived from PCC oxidation and DDQ oxidation of panaxadiol and panaxatriol, were further oxidized with m-chloroperoxybenzoic acid (m-CPBA) , as a result, four ring opening products were obtained, which were subjected to in vitro cytotoxic activity screening with MTT method. Results Four ring-opening derivatives were prepared (Compound2, 4, 6, 8) . Conclusion The four ring-opening derivatives are new compounds, and compound 2 and 4 show significant cytotoxicity against several cancer cell lines.
-
Key words:
- Panax notoginseng /
- Panaxadiol /
- Panaxatriol
-
[1]云南省药物研究所·云南重要天然药物[M].昆明:云南科技出版社, 2006:9. [2] [2]POPOVICH D, KITTS D.Structure-function relationship exists for ginsenosides in reducing cell proliferation and inducing apoptosis in the human leukemia (THP-1) cell line[J].Arch Biochem Biophys, 2002, 406 (1) :1-8. [3]张春红, 李向高, 张连学, 等.人参二醇衍生物抗肿瘤活性比较的初步结果[J].中国天然药物, 2004, 2 (6) :369-371. [4]邹澄, 赵庆, 郝小江, 等.丰产易得天然产物结构改造值得重视[J].中国民族民间医药杂志, 2004, 68 (8) :135-137. [5]张莲卿, 段文越, 邹澄, 等, 人参三醇酸酐酯化衍生物的制备[J].云南中医学院学报, 2015, 38 (1) :4-6. [6]蒲洪, 董成梅, 邹澄, 等, 三七二醇型皂苷氧化降解产物衍生物的合成及其抗肿瘤活性研究[J].天然产物研究与开发, 2016, 28 (2) :749-753. [7]蒲洪, 董成梅, 邹澄, 等, 三七二醇型皂苷元磺酰胺类衍生物的合成及抗肿瘤活性研究[J].天然产物研究与开发, 2014, 26 (6) :1739-1744. [8]董成梅, 蒲洪, 邹澄, 等, 酸酐酯化法制备人参二醇衍生物[J].昆明医科大学学报, 2014, 35 (6) :4-8. [9] 魏均娴, 陈业高, 张红彬, 等, 达玛烷型皂苷人参低元醇衍生物及制备方法[P].中国专利:ZL93.1.08189.0, 199501 11. [10]曹青青, 邹澄, 胡建林, 等.人参二醇和人参三醇氧化反应的研究[J].云南中医学院学报, 2013, 36 (6) :4-6. [11] [11]MOSMANN T.Rapid colorimetric assay for cellular growth and survival:application to proliferation and cytotoxicity assays[J].J Immunol Methods, 1983, 65 (5) :55-63.
点击查看大图
计量
- 文章访问数: 1674
- HTML全文浏览量: 624
- PDF下载量: 121
- 被引次数: 0