Rubiaceae type cyclopeptide used as tumor metastasis inhibitor as well as preparation method and application thereof

Abstract

The invention provides a rubiaceae type cyclopeptide compound RA-V (1) and a glycoside RA-XII (2) thereof as a tumor metastasis inhibitor, a drug composition with the rubiaceae type cyclopeptide compound and the glycoside as active ingredients, a preparation method of the compound and an application of the compound to preparation of anti-tumor metastasis drugs. The method can be used for obtaining cyclopeptide through rapid separation, is less in sample loss, relatively low in cost and convenient to operate, has good controllability and repeatability, ensures that solvents can be recycled, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular, relates to a kind of Rubiaceae type cyclic peptides used as tumor metastasis inhibitors, a pharmaceutical composition using it as an active ingredient, its preparation method and its application in the preparation of anti-tumor metastasis drugs. Background technique [0002] Tumor is a new organism formed by the body's abnormal growth due to the loss of normal regulation of its growth at the gene level by the cells of local tissues under various tumorigenic factors. Tumors are generally divided into benign and malignant. Malignant tumors, including carcinoma and sarcoma, are one of the major diseases that seriously threaten human life and health. According to statistics released by the World Health Organization, the incidence of malignant tumors in my country is 299.12 / 100,000, which is higher in cities than in rural areas; the death rate is 184.67 / 100,000, which is higher i...

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Problems solved by technology

[0005] The separation and purification of Rubiaceae-type cyclic peptides is difficult and has certain characteristics, mainly because Rubia plants are rich in anthraquinone pigments and have a wide range of polarity distribution, so it is difficult to obtain high-purity cyclic peptides

In the prior art, several methods have been published for isolating cyclic peptide components from Rubia plants. These methods generally have the disadvantages of large sample loss, high solvent cost, poor controllability and repeatability, such as Lee, J.E., etc. It was reported that after extracting the roots of Rubiaceae Rubiaceae with methanol, the methanol extract was obtained, suspended in water and extracted with chloroform, and the chloroform part was sequentially chromatographed on silica gel, alumina, aminopropyl bond and silica gel column to obtain the cyclic peptide enriched fraction , enrich the cyclic peptides by recrystallization, and then combine various means to separate and purify the crystallization or mother liquor, and obtain a series of cyclic peptides, including large and small amounts of cyclic peptides [Lee, J.E. et al. Structures of cytotoxic bicyclic hexapeptides, RA‐XIX, ‐XX,‐XXI,and–XXII,from Rubia cordifolia L.Tetrahedron.,2008,64,4117‐4125], its disadvantages are the large amount of sample loss, the process is too complicated, the separation cost is high and the recrystallization technology is controllable and poor reproducibility

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