Method for extracting homoharringtonine

Abstract

The invention discloses a method for extracting homoharringtonine. The method includes the steps that a dried and pulverized cephalotaxus sinensis raw material is extracted with methanol-chloroform mixed liquor, filtration is performed, filter liquor is concentrated to obtain extract, chloroform precipitation is performed, filtration is performed, filter liquor is concentrated at 65-70 DEG C to obtain crude homoharringtonine, and the crude homoharringtonine is subjected to reversed-phase column chromatography, concentration, extraction, recrystallization, separation and purification to obtainfinished homoharringtonine, wherein the homoharringtonine content is larger than 98%. The method is simple and easy to operate, short in production cycle, low in cost, high in yield, and suitable forindustrial application and market promotion.

Description

technical field [0001] The invention relates to an industrialized production method for extracting homoharringtonine from dried rough bark of Torreya bark. Background technique [0002] Homoharringtonine (Homoharringtonine) is an alkaloid obtained from the three-pointed plant Three-pointed Sequoia or its genus; it has inhibitory effect on the incorporation of 3H-labeled asparagine into proteins, and it has an inhibitory effect on the incorporation of 3H-labeled thymidine into Incorporation of DNA also affects; homoharringtonine can also induce cell differentiation, increase the content of cAMP, and inhibit glycoprotein synthesis; under the electron microscope, it can be seen that chromatin concentrates and condenses toward the edge of the nucleus, forming chromosome clumps that bulge outward , develop into "litter bodies" with nuclear separation, and finally nuclear fragmentation. [0003] Homoharringtonine has inhibitory effect on animal metastatic leukemia P-388 and L-121...

AI Technical Summary

Problems solved by technology

[0004] There are 9 species of plants in the genus Haerringtonaceae, 8 of which are produced in my country; this genus contains a variety of alkaloids, namely harringtonine, homoharringtonine, isoharringtonine and Deoxyharringtonine; harringtonine has a significant anticancer effect, because of its use value and economic value, in recent years, a series of researches have been carried out on the chemical, pharmacological and clinical aspects of this genus of plants at home and abroad. Research work, vying for development, has extracted and isolated harringtonine and homoharringtonine from the cloverleaf plant for clinical application; but due to the limited resources of cloverleaf plants, the esters with anticancer activity The content of alkaloids is extremely low, so it is far from meeting the clinical needs; at present, my country mainly uses these trees as raw materials, and extracts active ingredients from them for clinical use; A large number of felling, resulting in several endangered species, and seriously disrupted the ecological balance

[0006] (1) Homoharringtonine exists in a very low amount in nature, and contains a lot of impurities, making it difficult to extract;

[0007] (2) At present, there are many extraction methods for homoharringtonine. Although some methods extract high purity products, the yield is very low and the production volume is small, so it cannot be popularized for industrial production; that is, some extraction methods can increase the yield, but It is also not conducive to scale-up and industrial production because of high operating requirements, complicated control, and immature technology;

[0008] (3) Due to the long production cycle and low extraction efficiency of homoharringtonine, it is difficult to promote application and large-scale production, and it is difficult to obtain ideal curative effect for synthetic products;

[0009] (4) Due to the use of different fillers, problems such as low yield, poor impurity removal effect, and product degradation during column chromatography cannot be well applied to large-scale production