Studies On The Chemical Constituents Of Isodon. Excia (Maxin.) Hara

Isodon. excia ( Maxin.) Hara, of the Labiatae,mainly founded in Jilin, Liaoning, Yunnan province in our country and far east region in Japan, Korea etc . In the past few years, along with the researchers all over the world taking more attention to the compounds of ent-kaurane ,the chemical composition in the Iso. excia and relevant pharmacodynamical action was subjected to be concerned . Our job was mainly to obtain the diterpenoids from the herbs ,combing with the natural organic compounds of collection, separation, purification and identification , mixing with contemporary precisely analyzing apparatus and installation and got two purified compounds , whose name were kamebanin and kamebakaurin. The same time , we used the GC-MS to analyze the volatile oil that get from the Iso. excia. We scaned the spectra data base and got 78 peaks,34 of which were identified. It was the first time in the country to research this item in this kind plant . Besides, we measured the content of flavonoids in the stems and leaves of Iso. excia and the results was 0.1402%, which may supply the reference data for the future researching works.There were so many record about the Isodon liverworts in ? Herbs for saving? as early as Ming Dynasty. At that time, people had been acquired the medical uses of this kind plant and had used them as folk medicine all around. For example, it carried 24 kinds of plants in the ? Outline For Chinese Herbs? , wrote by WuZhengYi. But at that time , its accurate effect was not to be definite. Along with the development of the modern science ,the people s ability to analyze the structure of the natural products had been more accurate than ever. More people paid much attention to the relationship between the effect and the structure of the compounds. It had been confirmed that the diterpenoids from the genus Isodon which had the structure of ent-kaurane showed better activities such as anti-bacterial and resisted-tumor. The kaur-16-ent-15-one was the main center part for this effec. This gave large support for the chemistry researches. Now, the two diterpenoids structure we isolated from the Isodon. excia (Maxin.) Hara had been confirmed by IR, UV and NMR etc. So we made a conclusion that the Isodon. excia ( Maxin.) Hara had the same effect to the tumor. This plant had the large space for being researched and it was necessary to do lots works on it to extend its value in medical uses, at the same time ,enriched the plant resources of our country.In the past few years, being aimed at the pharmacodynamics of the Isodon. excia (Maxin.) Hara, researchers had carried a lot of works which related to the whole body system almost .Except for the traditional being used for treating injuries from the snakes and worm , lots of the researches discovered that the Isodon. excia ( Maxin.) Hara . still had the effect of anti-bacteria, eliminate inflammation, resisted tumor improve myocardium blood rate of flow etc. It also had the good effect for the cells infected with the HSV-1 in brain. So we did lots of works to find what the relationship between the structure of compounds with the pharmacology and got the good result.The scientific reports published in the lasted decade reported that because there were so many categories in the Isodon livesoures, 90 kinds in our country and spreading in almost all provinces, it was confused to judge whose the kind belonged to. The same time, it had no systematic method to isolate the constituents from them . Combining the equipment at hand ,we groped for a set path for isolation and purification. The operation was convenient. In our research work we avoided the traditional method to heat the materials .using the supersonic way to extract the resources. It was not only avoid the structure changes caused by the high temperature , but also reduced to extract more chlorophyll and big molecular in the solvent part. My work used the ADS-7 the first time to departed the whole extraction, which made the path more easily and saved lots of time and manpower. At the same time we used the way to fill the column in silica power but separate in a wet way . This method used few solvent and the results was satisfied.The dryed stems and leaves of Isodon. excia ( Maxin.) Hara we used in this work were collected at LinJiang city of JiLin province in early August 2003, identified by Dr. HuQuanDe. After smashed , the whole material were extracted with 70% EtOH in supersonic at 50°C ,100MHZ,3 times together. The combined extracts were concentrated in vacuo and got the residue. Then we pull two times water into it and used the active C power to delete chlorophyll. Filtered , then put the liquid into the refrigerator for one week. Take out the liquid then make the filtering go through the ADS-7 and use 40% , 70%, 90%EtOH to smash the column separately, one by one collected. The three parts of the fluid were concentrated and evaporated in vacuo to give a residue parts and numbered them A,B,C,D,E,F. By chemical reaction, we discovered that there are flavonoids in the part F. D was yellow powerand was subjected to CC on silica gel eluted with CHC13: Me2CO (2:1) as eluent, the same fractions combined and the residue was separated on a silica gel column with CHCI3: Me2CO: MeOH, (8:2:1) as eluent . Followed by prep. TLC. Fr. Nos. 8-9 as combined and recrystallized from MeOH gave the colorless needles, kamebanin ,and Fr. Nos. 12-15 was combined and recrystallized from the MeOH gave the white compounds kamebakaurin. The two compounds were purified by recrystallize .Two compounds isolated in the experiments identified by chemical reaction , phytochemical properties and spectral analysis (IR, UV,MS and NMR), structures of them was elucidated as diterpenoids. They are kamebanin and kamebakaurin, which structure belongs to the ent-kaurane, might had the action of anti-tumor etc.The material we used for volatile oil analysis were picked back at the LinJiang city of JiLin province. The volatile was extracted in the way of vapouring with water liquid for 4 hours then filtered with Me20. After drying with Na2SO4) the yellow oil was analyzed by GC-MS . There are much fat chain hydrocarbon compound and little unrighted fat acid.