Application of 23-hydroxylbetulinic acid in preparing medicine for treating and preventing AIDS

Abstract

The invention discloses a novel purpose of 23-hydroxylbetulinic acid, namely, an application of 23-hydroxylbetulinic acid in preparation of drug for treating or preventing AIDS. The drug for treating or preventing lever cancer is a drug compound with 23-hydroxylbetulinic acid as the active ingredient. 23-hydroxylbetulinic acid is safe, nontoxic, strong in pharmacological action and promising with a good prospect in pharmacy; pasqueflower, the Chinese traditional medicine, in the raw material, is rich in resource, low in cost and simple in preparation process.

Description

[0001] This application is a divisional application. The application number of the original application is 03152904.6, the filing date is September 02, 2003, and the title of the invention is: Application of 23-hydroxybetulinic acid in the preparation of drugs for the treatment or prevention of tumors and AIDS. Technical field

[0002] The invention relates to the use of 23-hydroxybetulinic acid in the preparation of medicines for treating or preventing AIDS. Background technique

[0003] It has been reported in the literature that betulinic acid can selectively kill human melanoma cells [NatureMedicine, 1995; 1(10):1645-1651]; the anti-cancer activity of betulinic acid and some derivatives has been subcutaneously implanted in mice Nude mice with sarcoma 180 cells (JP 87,301,580), which inhibit the growth of P338 lymphocytic leukemia cells in vitro [Planta Medica, 1988; 511-513], especially by inhibiting ornithine decarboxylase (WO 95 / 04526), ​​etc. Be proven. The Chinese patent (...

Examples

Embodiment 1

[0025] Example 1: Weigh 1.0 kg of dry coarse powder of Pulsatilla root, percolate with 3000ml of 15% ethanol, combine the ethanol percolate, recover under reduced pressure to be alcohol-free, filter, and adjust the filtrate to pH 2 with hydrochloric acid and heat for 30 minutes. Obtain the precipitate, let it cool, filter, wash with water, and dry to obtain the crude product. The crude product was refluxed with ethyl acetate Soxhlet, the reflux solution was concentrated to an appropriate amount, placed, and filtered with suction to obtain 38.2 g of 23-hydroxybetulinic acid.

Embodiment 2

[0026] Example 2: Weigh 1.0 kg of dry coarse powder of Pulsatilla root, percolate it with 3000ml of 60% ethanol, combine the ethanol percolate, recover under reduced pressure until it has no alcohol smell, filter, and adjust the filtrate to pH 2 with hydrochloric acid and heat for 30 minutes. Obtain the precipitate, let it cool, filter, wash with water, and dry to obtain the crude product. The crude product was refluxed with ethyl acetate Soxhlet, the reflux solution was concentrated to an appropriate amount, placed, and filtered with suction to obtain 51.0 g of 23-hydroxybetulinic acid.

Embodiment 3

[0027] Example 3: Weigh 1.0 kg of dry coarse powder of Pulsatilla root, percolate it with 3000ml of 95% ethanol, combine the extracts, recover under reduced pressure until there is no alcohol smell, filter, adjust the filtrate to pH 2 with hydrochloric acid, and heat for 30 minutes to obtain a precipitate Let it cool, filter, wash, and dry to get a crude product. The crude product was refluxed with ethyl acetate Soxhlet, the reflux solution was concentrated to an appropriate amount, placed, and filtered with suction to obtain 45.6 g of 23-hydroxybetulinic acid.

[0001] This application is a divisional application. The application number of the original application is 03152904.6, the filing date is September 02, 2003, and the title of the invention is: Application of 23-hydroxybetulinic acid in the preparation of drugs for the treatment or prevention of tumors and AIDS. Technical field

[0002] The invention relates to the use of 23-hydroxybetulinic acid in the preparation of medicines for treating or preventing AIDS. Background technique

[0003] It has been reported in the literature that betulinic acid can selectively kill human melanoma cells [NatureMedicine, 1995; 1(10):1645-1651]; the anti-cancer activity of betulinic acid and some derivatives has been subcutaneously implanted in mice Nude mice with sarcoma 180 cells (JP 87,301,580), which inhibit the growth of P338 lymphocytic leukemia cells in vitro [Planta Medica, 1988; 511-513], especially by inhibiting ornithine decarboxylase (WO 95 / 04526), ​​etc. Be proven. The Chinese patent (...

Examples

Embodiment 1

[0025] Example 1: Weigh 1.0 kg of dry coarse powder of Pulsatilla root, percolate with 3000ml of 15% ethanol, combine the ethanol percolate, recover under reduced pressure to be alcohol-free, filter, and adjust the filtrate to pH 2 with hydrochloric acid and heat for 30 minutes. Obtain the precipitate, let it cool, filter, wash with water, and dry to obtain the crude product. The crude product was refluxed with ethyl acetate Soxhlet, the reflux solution was concentrated to an appropriate amount, placed, and filtered with suction to obtain 38.2 g of 23-hydroxybetulinic acid.

Embodiment 2

[0026] Example 2: Weigh 1.0 kg of dry coarse powder of Pulsatilla root, percolate it with 3000ml of 60% ethanol, combine the ethanol percolate, recover under reduced pressure until it has no alcohol smell, filter, and adjust the filtrate to pH 2 with hydrochloric acid and heat for 30 minutes. Obtain the precipitate, let it cool, filter, wash with water, and dry to obtain the crude product. The crude product was refluxed with ethyl acetate Soxhlet, the reflux solution was concentrated to an appropriate amount, placed, and filtered with suction to obtain 51.0 g of 23-hydroxybetulinic acid.

Embodiment 3

[0027] Example 3: Weigh 1.0 kg of dry coarse powder of Pulsatilla root, percolate it with 3000ml of 95% ethanol, combine the extracts, recover under reduced pressure until there is no alcohol smell, filter, adjust the filtrate to pH 2 with hydrochloric acid, and heat for 30 minutes to obtain a precipitate Let it cool, filter, wash, and dry to get a crude product. The crude product was refluxed with ethyl acetate Soxhlet, the reflux solution was concentrated to an appropriate amount, placed, and filtered with suction to obtain 45.6 g of 23-hydroxybetulinic acid.

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