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Claims for Patent: 6,432,452

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Claims for Patent: 6,432,452

Title: Anti-cancer compounds
Abstract:This invention relates to a compound or group of compounds present in an active principle derived from plants of the species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.
Inventor(s): Aylward; James Harrison (St. Lucia, AU)
Assignee: Peplin Biotech Pty. Ltd. (Fortitude Valley, AU)
Application Number:09/486,199
Patent Claims: 1. A method of treating a subject with skin cancer, the method comprising topically administering to the subject in need thereof a therapeutically effective amount of at least one compound selected from the group consisting of an angeloyl-substituted ingenane obtained from the sap of Euphorbia peplus and an active derivative of an angeloyl-substituted ingenane obtained from the sap of Euphorbia peplus, wherein said active derivative exhibits the same activity as said angeloyl-substituted ingenane.

2. The method of claim 1, wherein the derivative of an angeloyl-substituted ingenane obtained from the sap of Euphorbia peplus is an acetylated derivative.

3. The method of claim 1, wherein the at least one compound is selected from the group consisting of a 20-O-acetyl-ingenol-3-angelate and an ester derivative of a 20-O-acetyl-ingenol-3-angelate.

4. The method of claim 3, wherein compound comprises a pharmaceutically acceptable salt of the 20-O-acetyl-ingenol-3-angelate or the 20-O-acetyl-ingenol-3-angelate ester derivative.

5. The method of claim 1, wherein at least one compound is obtained from the sap of Euphorbia peplus by subjecting the sap to aqueous extraction and collecting the aqueous fraction.

6. The method of claim 1, wherein the compound is obtained from the sap of Euphorbia peplus by the process of extracting said sap with 95% v/v ethanol, discarding a soluble fraction and retaining a solid fraction.

7. The method of claim 1, wherein the skin cancer is a malignant melanoma.

8. The method of claim 1, wherein the skin cancer is a Merkel cell carcinoma.

9. The method of claim 1, wherein the skin cancer is a squamous cell carcinoma.

10. The method of claim 1, wherein the skin cancer is a basal cell carcinoma.

11. The method of claim 1, wherein the skin cancer is a solar keratosis.

12. The method according to claim 1 wherein the subject is human.
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