Preparation method for two novel compounds with antitumor activity extracted from isodon excisoides and application of two novel compounds

Abstract

The invention relates to a preparation method for two novel compounds with antitumor activity extracted from isodon excisoides and an application of the two novel compounds. The novel compounds are extracted from the isodon excisoides and are applied to the preparation of antitumor drugs. The method comprises the steps: adding water into the isodon excisoides, carrying out boiling extraction, introducing an extract sample to a macroporous adsorption resin column, and carrying out gradient elution by using water and ethanol, so as to obtain Fr. A, Fr. B, Fr. C and Fr. D; subjecting part of Fr. C to gel column chromatography and methanol-water gradient elution, so as to obtain Fr. C1, Fr. C2, Fr. C3 and Fr. C4; and subjecting part of Fr. C2 to silica-gel column chromatography and petroleum ether-acetone and methanol gradient elution, so as to obtain Fr. B1-1, Fr. B1-2, Fr. C2a, Fr. C2b, Fr. C2c and Fr. C2d, subjecting Fr. C2c to methanol recrystallization so as to obtain an acetonitrile-water for white powder as eluate, carrying out semipreparative HPLC purification, collecting chromatographic peaks at 56.4min and 61.2min, separately placing products in a solvent, and carrying out anhydrous sodium sulfate dehydrating and nitrogen gas drying-up, thereby obtaining a compound 1 and a compound 2. The preparation method provided by the invention is easy in operation, high in orienting property, high in separating rate, high in efficiency and high in product purity and can be effectively used for preparing the antitumor drugs.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method and application of a new compound with anti-tumor activity extracted from pseudo-fragrance-deficient tea vegetables. Background technique [0002] The Camellia genus is considered to be the most promising medicinal plant for obtaining anti-tumor lead compounds. In recent years, a large number of new cytotoxic diterpenoids of Camellia have been discovered, and a number of compounds have entered research and development as anti-tumor candidate compounds stage, such as Rubescensin A, Eucalyptin A, Dayexiangchagenin, etc., the sales of related traditional Chinese medicine products are also increasing year by year, such as Three Sisters Tablets (Xiyexiangchacai), Winter Lingcao syrup, tablets (Donglingcao), anti-inflammatory and gallbladder tablets (containing Xihuangcao), etc. Isodon excisoides (Y.Z.Sun ex C.H.Hu) Hara, also known as wild perilla, was first recorded in "...

AI Technical Summary

Problems solved by technology

However, only more than 20 diterpenoids have been reported from this plant for many years. Preliminary studies have shown that more new compounds with novel structures and significant anti-tumor activities can be obtained from Quasi-Chrysanthemum. A new lead compound with poor stability in protic solvents but significant anti-tumor effect obtained from tea leaves lacking in fragrance, and used for the preparation of anti-tumor drugs has not been publicly reported so far

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