62 results about "Bufalin" patented technology

The invention discloses a bufalin glycosylation derivative and a preparation method and application thereof in preparation of anti-tumour medicaments. The structure of the bufalin glycosylation derivative is shown in a formula I or formula II. The synthesis method of the bufalin glycosylation derivative comprises the following steps of: oxidizing bufalin into a ketone-form derivative by pyridinium chloropyridine hydrochloride; then performing a nucleophilic addition reaction with methoxyamine hydrochloride; removing monomolecular water to generate an oxime-form intermediate; enabling the oxime-form intermediate to react with a tert-butylamine borane hydrochloride compound to generate alpha-configuration aglycone and beta-configuration aglycone; and finally enabling the aglycones of two configurations to react with reducing sugar respectively to generate the bufalin glycosylation derivative. According to the method disclosed by the invention, bufalin is modified to be the glycosylation derivative thereof, and the water solubility can be improved while the anti-tumour activity is kept and enhanced; and moreover, in-vivo experiments prove that the toxic and side effects of the bufalin glycosylation derivative disclosed by the invention on normal cells are reduced compared with those of a parent compound of bufalin.

The present invention relates to methods of treating cancer comprising administering a bufalin derivative compound of Formula I, wherein the compound is administered at least once a week for at leasttwo weeks.

The invention relates to a traditional Chinese medicine venenum bufonis extract. A method for extracting the extract includes steps of extracting traditional Chinese venenum bufonis medical materials at the temperature ranging from 60 DEG C to 90 DEG C by ethanol water with volume percent of 60-95% in a backflow manner, separating extract liquid via silicagel columns after the extract liquid is concentrated, adopting petroleum ether and acetone with volume ratio of 1-8:1 as eluant to realize gradient elution, collecting parts of eluent, and filtering, concentrating and drying the eluent in a pressure reduction manner to obtain the traditional Chinese medicine vanenum bufonis extract containing mixture of three types of bufotalin including resibufogenin, cinobufagin and bufalin, wherein the sum of the weight percentages (calculated when three types of the bufotalin are dried) of the three types of the bufotalin is higher than or equal to 95%. The invention further provides the preparation method for the traditional Chinese medicine venenum bufonis extract. The sum of the weight percentages of the three types of the bufotalin in the traditional Chinese medicine venenum bufonis extract is higher than 95%, extraction transfer rate is high, the quantity of used solvent is lower, residual solvent is little, pollution degree is lower, operation is simple and convenient, and industrial production is realized easily.