Studies On Chemical Constituents And Antitumor Activities Of The Leaves Of Rubus Chingii

Rubus chingii Hu,also known as Rubus idaeus L.,is mainly produced in Jiangxi,Zhejiang,Hubei,Hunan,etc..In the Chinese pharmacopoeia,Rubus chingii Hu is included in the fruit,but the leaves of Rubus chingii Hu are mainly used as folk recorded drugs,which have good antipyretic and detoxifying effects and are mainly used for nutrition and health care.Pharmacological studies on the leaves of Rubus chingii Hu show that it has anti-tumor,lower blood sugar and lipid,antioxidant and other effects.Based on previous studies of Rubus chingii Hu plants,our research group found that chemical components of the fruits and rhizomes of Rubus chingii Hu have significant anti-tumor effects.In order to further extract drugs with anti-tumor activities from Rubus chingii Hu,this paper continued to study chemical components of the leaves of Rubus chingii Hu and their anti-tumor activities.In this paper,40 compounds were obtained from the extract of the leaves of Rubus chingii Hu by using macroporous resin,silica gel,Sephadex LH-20,medium pressure liquid chromatography and high performance liquid chromatography,which were combined by UV,1D NMR,2D NMR,MS and other spectroscopic methods.The structures of 38 compounds were identified（See Tist 1）,including 23 diterpenoids（1-23）,7 flavonoids（24-30）,6 lignans（31-36）and 2 phenolic acids（37,38）.Eleven of them were new compounds（1*-11*）,and 23and 29-36 were isolated from raspberry for the first time.In this paper,the anti-tumor activity of the main components in the leaves of Rubus chingii Hu was screened,and five cancer cells of Bel-7402（human liver cancer cell line）,Caski（human cervical cancer cell line）,BGC-823（human gastric cancer cell line）,A2780（human ovarian cancer cell line）and HCT-116（human colon cancer cell line）were studied.Cytotoxicity activity was tested using CCK-8 assay.Compound 4showed strong cytotoxicity to Bel-7402,A2780 and HCT-116,with IC₅₀ values of10.43±0.51,and 29.03±2.94μM,respectively.Compound 8 showed moderate cytotoxic activity against Bel-7402 and HCT-116 with IC₅₀ values of 17.78±1.54 and26.23±6.14μM,respectively.The rest showed low cytotoxic activity(IC₅₀>50μM).