New ansamitocin compounds and preparation method thereof
A technology of ansomycin and compound, which is applied in the preparation of the ansomycin compound, the new ansomycin compound field, can solve the problems of cumbersome process, poor reaction specificity, complex structure, etc. Simple, low production cost effect
Inactive Publication Date: 2012-10-17
FUJIAN INST OF MICROBIOLOGY
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Problems solved by technology
Due to the low content of maytansine and its homologues in maytansine plants, massive felling of maytansine plants will cause serious damage to the ecology, and it is difficult to find raw materials from wild plants to meet the needs of industrial production; using chemical synthesis , and due to the complex structure of maytansinoid, there are disadvantages such as complicated total synthesis and semi-synthesis process, cumbersome process, low yield and poor reaction specificity.
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[0048] The separation method of Actinomyces fasciculatus bacterial strain FIM06-0063 in the present invention is as follows:
[0049] Step 100: Take the old leaves and petioles of Yunnan Meideng wood, wash them with tap water for 30 minutes, and then wash them with distilled water and place them in a sterile petri dish; After washing with water, change to 0.1% mercuric chloride (i.e. HgCl 2 ) solution for 3 minutes, then rinsed with sterile water for 5 times to remove the disinfectant; then cut the old leaves and petioles into small pieces or segments, put them into a sterile mortar and mash them into a paste;
[0050] Step 200: Dip a small amount of the paste obtained in step 100 with a sterile glass coating rod and directly spread it on the starch aspartic agar plate, and then place the plate at 28° C. for 7 to 20 days to obtain actinomycetes Single bacterial colony; in Example 1, place the plate at 28°C for 7 days; in Example 2, place the plate at 28°C for 13 days; in Exam...
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Abstract
The present invention relates to new ansamitocin compounds and a preparation method thereof. A structural formula of the new ansamitocin compound is as follow, wherein R is CH2CH3 or CH2CH(CH3)2. The preparation method for the ansamitocin compound comprises: adopting macroporous resin adsorption column chromatography, silica gel column chromatography and other methods to carry out separation and purification on fermentation products of Actinosynnema sp FIM06-0063 to obtain two new ansamitocin compounds, wherein structures of the compounds are characterized by mass spectrometry, nuclear magnetic resonance spectroscopy, ultraviolet spectrum and other technologies. The prepared ansamitocin compounds of the present invention have strong anti-tumor activities. According to the present invention, the microbial fermentation method is adopted to prepare the ansamitocin compound, such that advantages of simple process and low production cost are provided.
Description
【Technical field】 [0001] The invention relates to a compound, in particular to a novel ansamitocin compound, and also relates to a preparation method of the ansamitocin compound. 【Background technique】 [0002] In 1972, Kupchan et al. first isolated the natural anti-tumor active ingredient - the macrolide compound Maytansine - from M. serrata, which is native to tropical Africa. Maytansinoids were isolated from higher plants such as Pyramidaceae, Rhamnaceae, Euphorbiaceae and bryophytes. The most notable is the discovery of this type of compound from microorganisms. In 1977, Higashide and his colleagues screened anticancer active ingredients from Actinomycetes aurantias ( Actinosynnema pretiosum) obtained six maytansine derivatives, named ansamitocin P0, P1, P2, P3, P4, P4'. Subsequently, fifteen neoanthracins other than the above six compounds were isolated from another subspecies of A pretiosum ssp.Auranticum, whose core is a 19-C macrocyclic lactam Ring, C-3 connects c...
Claims
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IPC IPC(8): C07D498/18C12P17/18A61P35/00A61P35/02C12R1/01
Inventor 陈宏郑卫贾纬陈丽陈晓明王传喜黄维杨煌建谢颖张祝兰
Owner FUJIAN INST OF MICROBIOLOGY