Studies On Bioactive Constituents Of Boswellia Carterii (Frankincense)

Natural products provide drug research with new structural, curative effect as well as low toxic compounds, and have been demonstrated as the precursor and source of new drug research. In this dissertation, Boswellia carterii was chosen to have a research on its chemical constituents, purification and structure verification, as well as synthesis of boswellic acid analogues and their anti-tumor activity researches. It is divided into three parts as the following:1. The Boswellia carterii.(Frankincense) were obtained from Bozhou Guo Shao Tang Tech Co. Ltd.. Of Anhui, while it is originated from Somalia. And the frankincense were dried on the condition of light-free, powdered and extracted with99%alcohol. Extraction distribution was carried out on ethyl acetate, butanol and water, respectively. The compounds were isolated by repeated column chromatography(CC) on silica gel, RP-18, and Sephadex LH-20, as well as by preparative thin layer chromatography(PTLC), and recrystallization. The structures of these compounds were elucidated by means of spectroscopic methods including UV, EI-MS, FAB-MS,1D-NMR (’H-NMR,13C-NMR and DEPT) and2-D-NMR((1H-1H COSY, HMBC, HMQC and NOESY). From frankincense, seventeen compounds were isolated and forteen of them were structurally elucidated, and the compounds were macrocyclic deterpenoids incensole e.g., tetracyclic triterpenoids KTDA e.g., pentacyclic triterpenoids AKBA e.g.2. The Boswellia carterii contains natural anti-tumor chemical composition of3-keto-tirucall-8,24-dien-21-oic acid (KTDA) and3-acetyl-11-keto-beta-boswellic acid (AKBA). In order to improve its antitumor activity, seven derivatives were achieved through amination and esterification of KTDA on a basis of summary of previous research literatures, while three AKBA derivatives were achieved in the same way.3. In-vivo antitumor activities of New compound7that isolated from frankincense, KTDA and AKBA derivatives were evaluated by MTT assay on four tumor cells of SMMC-7721、A549、 Eca-109and KB. By a comparison of derivatives with KTDA and AKBA, we tried to figure out the structure-activity relationship of KTDA and AKBA.