Study On The Active Constituents Of Fructus Forsythiae And Coleus Forskohlii (Wild.) Briq. As Well As The Quality Analysis Of The Latter

Forsythia suspensa (Thunb.) Vahl. is a widely-used Traditional Chinese Medicine. Modern pharmacological studies have shown that Forsythia Fruit has many biological functions and is very active in clinical usages for anti-inflammatory, antiviviral,detoxifing,liver-defence,subduing swelling,dissolving lumps ,drainage and antidotal purposes.Researcher Xin Chin from NIH observed that Forsythia suspensa (Thunb.) Vahl. could selectively block SDF-1α/CXCR₄,but knew nothing about the material base. Increasing evidences have shown that chemoattractant CXCL₁₂/SDF-1α and its receptor CXCR₄ play a vital role in many diseases such as various tumors ,HIV infection and inflammation and so on. So an antagonist of SDF-1α/CXCR₄ may be a key treatment for such diseases, which is the very goal and point of our project. In order to assistant him to search for the active compounds, systematic studies on the chemical constituents were carried out.In this dissertation, the chemical constituents study was carried out, adopting phytochemistry isolation with molecular biology screening, in order to search for the bioactive compounds. Dry fruits of Forsythia suspensa (Thunb.) Vahl. were refluxed three times with hot 75% alcohol .The alcohol solution was concentrated to a small volume under vacuum, diluted with water, fully stirred, then removed the last trances of alcohol and filtered through gauze to get two parts: solution and residue. The residue was taken up with tripolite, dried thoroughly and then put in a Soxhlet extractor, extracted successively with PE, EtoAc and EtOH to get 3 fractions. These 3 fractions were tested for bioactivity by SDF-1α/CXCR₄ screening. It was shown that the EtoAc fraction was the bioactive fraction, with significant difference to the other 2. The EtoAc active fraction was then subjected to repeated column chromatography on silica gel, Toyopearl HW-40F, Sephadex LH-20 etcetra, eluted with appropriate solvent system by gradually increasing the ratio, according to respective cases. As a result, 16 compound were obtained, which were elucidated and identified based on comparison with authentic samples and by spectral methods as phillygenin (â… ), epipinoresinol (â…¡), phillyrin (â…¢), (-)isolarlciresinol (â…£), Betulic acid (â…¤), 2a-hydroxy betulinic acid (â…¥), Oleanolic acid (â…¦), ursolic acid (â…§),2,23-OH ursolic acid (â…¨), β-Amyrine acetate (â…©), iso-Baurenyl acetate (â…ª),...