Chemical Constituents Of Triterpenoids From The Roots Of Actinidia Cylindrica Var. Reticulata And Their Antitumor Bioactivity

Actinidia cylindrica var.reticulata is a plant of the genus Actinidia.The monomer compounds from the roots of the genus Actinidia have good biological activities.The literature showed that the triterpenes from roots of Actinidia had good anti-tumor,antiviral,and other activities.To better develop and utilize the resources of Actinidia plants,the chemical constituents were studied on the roots of Actinidia reticulata.1.The research progress of chemical constituents and biological activities of the triterpenoids from the roots of Actinidia was reviewed.2.A total of 11 pure compounds were isolated from the n-butanol extracts of roots of Actinidia Reticulata by the traditional column chromatography and high-performance liquid chromatography（HPLC）.The structures of compounds（1-8）were identified by NMR,IR,MS and other modern spectroscopic techniques and compared with literature data.Eight triterpenoids were identified as 2α,3α,24-trihydroxyolean-12-en-28-oic acid（1）,2α,3β,24-trihydroxyolean-12-en-28-oic acid（2）,2α,3α,24-trihydroxyurs-12-en-28-oic acid（3）,2α,3β,23-trihydroxyurs-12-en-28-oic acid（4）,2α,3β,24-trihydroxyurs-12-en-28-oic acid（5）,2α,3α-dihydroxy-12-en-28-oic acid（6）,2α,3α,23-trihydroxyurs-12-en-28-oic acid（7）,and 2α,3α,24-trihydroxyurs-12,20（30）-dien-28-oic acid（8）.Compounds（9-11）were characterized by hydrogen and carbon spectra,respectively.NMR signals suggested that it had the framework of 12-ene-28-oleanolic acid,but the exact structure could not be determined..Compounds 1-8 were isolated from the roots of Actinidia chinensis for the first time.3.Chemical constituents were analyzed by HPLC method and the results provided guidance for the separation work.Ursolic acid was selected as the main index component,the content determination method was studied,the quantitative method of chemical composition was established,and the technical indexes for quality evaluation were put forward.The purpose of this study was to establish the fingerprint of radix actinidia chinensis and establish the HPLC method for the determination of the active components in radix actinidia chinensis.The results provided a basis for the quantitative study of the root of Actinidia reticulata,and were beneficial to the establishment of its quality control standard.4.Compounds（1～8）were tested against human colon cancer cell SW480,human colon cancer cell Lo Vo,human liver cancer cell HUH7,human malignant melanoma cell A375,and human non-small cell lung cancer cell NCI-H1993 by CCK8 method.The results showed that compounds 1 and 8 inhibit A375 cells,and compounds 1,3and 4 inhibit SW480 cells and their values of IC₅₀are close to the positive control.Compounds 1～5,7 and 8 showed cytotoxic activity against human malignant melanoma cell line A375 with IC₅₀values ranging from 30.1μM to 61.2μM.Partial Some compounds showed weak cytotoxic activity against the other human cancer cell lines.