Study on the Lipophilic Constituents for Anti-tumor Activities from the Seeds of Vitex Negundo
|School||Central South University|
|Keywords||Semen viticis negundo Chemical composition Triterpenoid Diterpene Lignans Anti-tumor effects|
The purpose of semen viticis negundo (Fructus Viticis Negundo) for the Verbenaceae (Verbenaceae) plants Huang Jing (Vitex negundo L.) dried ripe fruit, is widely distributed in the southern provinces of China. Its warm, spicy, bitter; lungs, stomach, liver, expelling wind and relieving, cough and asthma, qi digestion analgesic effect, and used for the treatment of asthma in the civil, malaria, stomach ulcers, chronic bronchitis, premenstrual syndrome and other diseases. However, semen viticis negundo chemical ingredients, pharmacological activity of basic research is seriously inadequate, leading to the active site and the active ingredient is not clear. Therefore, semen viticis negundo accurately and efficiently tracking filters in the active site and the active ingredient, and to clarify its active substance, the active substance is in-depth evaluation of its pharmacological activity on the basis of, for full use of the medicine semen viticis negundo and innovation in the development of drugs to find lead compounds laid foundation. Our group pre bioactive oriented technology, MTT assay semen viticis negundo 40% ethanol extract of seven parts of the anti-tumor activity screening, and experimental results show that the water-saturated ethyl acetate extract (Evn-50) and EDTA-2Na precipitate of parts (I) on human breast cancer (MCF-7, MDA-MB-435S, T47D), ovarian cancer (COC1), human lung carcinoma (A-549), human leukemia (HL-60), human colon ( HT-29), human hepatoma (SMMC-7721, HepG2), human cervical carcinoma (HeLa), human gastric carcinoma (SGC-7901, the MGC-803) cell lines have significant inhibitory effect, with a broad-spectrum anti-tumor activity. The systematic study of anti-tumor activity of the preliminary work has Evn-50 parts and sediment site Ⅰ (methanol dissolved part) conducted a preliminary anti-tumor activity was studied this subject continue to precipitate parts Ⅰ (two methyl chloride dissolved part) as the object of study of anti-tumor activity. Present subjects positive, RP by repeated silica gel column chromatography, recrystallization, and Sephadex LH-20 column chromatography, etc., means a combination of separation and purification methods for the precipitate portion Ⅰ (dichloromethane dissolving portion) system of the chemical composition research, and the use of the means of spectroscopy, physical and chemical properties and the reported data control and identified their structure; respectively by MTT and SRB chromogenic assay terpenes and lignans isolated compounds on cultured human chronic myelogenous The original leukemia cell line (K-562) and human lung cancer cell lines (A-549) proliferation inhibitory activity. Results from the precipitate portion Ⅰ (dichloromethane dissolving portion) separating to give 14 compounds, including 3 triterpenoid: (17RS)-17-hydroxy-3a, 1 OA-epoxy-9-EIP-Cucurbita-25-ene ( 1 2), obtusalin (8); four Diterpenoid: abietatrien-3ss-OL (3), vitexifolin C (4), Phytol (5), ()-polyalthic acid (6); 1 times semi terpene: caryophyllenol Ⅱ (7); 3 Lignans: (-)-aptosimon (9), paulownin (10), ,2-O-methyarboreol (11); three other types of components: dibutyl phthalate (12), paraben Methyl (13), β-sitosterol or alcohol (14). Which compound 12 is a new compound; compounds 7,9,10,11 for the first time isolated from Vitex, the compound 3,4,5,6 from semen viticis negundo isolated for the first time to get. Anti-tumor activity in vitro experimental results show that compound 1 2,3,4 K-562 cells with a certain inhibit proliferation of growth effect; Compound 1 2,4,6,9,10 A-549 cells has definitely inhibit the proliferation and growth role. The conclusion by the system separation semen viticis negundo lipophilic chemical ingredients from separating structural identification to get 3α, 10α-epoxy-9-eip-cucurbita type three terpene, rosin finished type two terpene, half a day to spend diterpene and double-tetrahydrofuran-type wood fat hormone , have a certain inhibition of tumor cell proliferation and growth of the role of the may semen viticis negundo anti-tumor active ingredient.