# US 2010/0168451 A1 · Preparative method of dihydrocucurbitacin f-25-o-acetate and the use thereof in the manufacture of medicaments for treating cancers

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- Number: US 2010/0168451 A1
- Document ID: US20100168451A1
- Status: Published application
- Kind: A1
- Application number: 12/601,303
- Filed: 2007-10-19
- Published: 2010-07-01
- Earliest claimed: 2007-10-19
- Inventors: Xiane Fan; Renwei Zhang; Huijia Cheng
- Web page: https://patentgrep.com/patent/US20100168451A1

## CPC

- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61P 35/02: specific for leukemia
- A61P 35/04: specific for metastasis
- C07J 9/00: Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07J: STEROIDS (seco-steroids C07C)

## Abstract

A method for producing dihydrocucurbitacin F-25-0-acetate consisting of the steps as followed: percolating radix hemsleyae using acetone as solvents to obtain extract; eluting the extract in silica gel column using chloroform: methanol as eluting agent (gradient) to obtain the crude; recrystallizating the crude using methanol or ethanol to obtain di-hydrocucurbitacin F-25-O-acetate (purity:>98%). And the use of dihydrocucurbitacin F-25-O-acetate in the manufacture of medicaments for treating cancers of liver, lung, stomach, larynx, prostate and leukemia.

## Claims

### Claim 1

A preparation method of curcurbitacin IIa, comprising the following steps:
a, the tuber of Hemsleya amalils Diels plant is obtained and comminuted, then extracted by a percolation method, using acetone of 18-26 weight times as solvent, then the extractant is recycled in water bathe of 60-70° C. for extract paste;
b. the obtained extract paste is mixed with silica gel of 1-2 weight times, then dried and subjected to the silica gel column, then gradient eluted by a mixed solvent comprising chloroform and methanol, wherein a volume concentration of the methanol is 2-10%, then the eluent is recycled and crude product is obtained;
c. the crude product is heated and dissolved in a water bath using methanol or ethanol, then the obtained solution is filtered and placed in a room temperature for recrystallization, then the obtained prismy crystals is the curcurbitacin IIa of 98% purity.

### Claim 2 (depends on 1)

The preparation method of curcurbitacin IIa according to claim 1, wherein the Hemsleya amalils Diels plant is Hemsleya maerosperma, Hemsleya dolichocarpa W. J. Chang, and Hemsleya emeiensis L. T. Shen.

### Claim 3 (depends on 1)

The preparation method of curcurbitacin IIa according to claim 1, wherein in the step b, at first pure chloroform is used to elute impurity, and then a mixed solvent comprising chloroform and methanol is used for gradient eluting.

### Claim 4 (depends on 1)

Use of curcurbitacin IIa according to claim 1 in preparing medicament for treat hepatic cancer.

### Claim 5 (depends on 1)

Use of curcurbitacin IIa according to claim 1 in preparing medicament for treat lung cancer.

### Claim 6 (depends on 1)

Use of curcurbitacin IIa according to claim 1 in preparing medicament for treat gastric cancer.

### Claim 7 (depends on 1)

Use of curcurbitacin IIa according to claim 1 in preparing medicament for treat laryngeal cancer.

### Claim 8 (depends on 1)

Use of curcurbitacin IIa according to claim 1 in preparing medicament for treat leukemia.

### Claim 9 (depends on 1)

Use of curcurbitacin IIa according to claim 1 in preparing medicament for treat prostate cancer.