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Hedera helix saponin, preparation method and antineoplastic use thereof

An anti-tumor drug and saponin technology, applied in the field of natural medicine, can solve the problems of low content of active ingredients and few pharmaceutical researches on saponins, and achieve the effects of clear activity, high product yield and purity, and sufficient sources.

Active Publication Date: 2008-04-09
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are still few pharmaceutical studies on its saponin components. At present, only the isolation and identification of fulvotomentoside A (fulvotomentoside A), sapindoside B (sapindoside B) and α-hederin (α-hederin) have been reported. Three kinds of saponins, but the content of these active ingredients in plants is extremely low

Method used

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  • Hedera helix saponin, preparation method and antineoplastic use thereof
  • Hedera helix saponin, preparation method and antineoplastic use thereof
  • Hedera helix saponin, preparation method and antineoplastic use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] 5kg of Lonicera tomentosa medicinal material (dried flower buds), reflux extraction with 10 times the amount of 90%, 80% and 70% ethanol respectively, each time for 3 hours, combine the extracts three times, concentrate under reduced pressure to no alcohol; filter or high-speed centrifugation , after the macroporous resin on the filtrate or centrifugal supernatant is fully adsorbed, it is eluted with water, 30% ethanol, and 70% ethanol successively until the eluate is nearly colorless, and the 70% ethanol eluate is collected and evaporated to dryness under reduced pressure. Obtain about 1.5 kg of the total saponin parts of Lonicera tomentosa. The extract of this part was dissolved with methanol, and about 1.5kg of silica gel (200-300 mesh) was added to mix well, grinded, and subjected to silica gel column chromatography, and the chloroform-methanol system (20:1, 15:1, 10:1, 9 :2, 8:2.5, 7:3.5, 1:1), each 500ml was regarded as a fraction, and a total of 72 fractions were...

Embodiment 2

[0052] Take 2g of Lonicera saponin B, add 20mL of 5% NaOH solution, extract in a 60°C water bath under reflux for 2h, let cool, add concentrated HCL to adjust the pH value to 4-5. Add water-saturated n-butanol solution (1:1, v / v) for extraction three times, combine the n-butanol extracts, recover the solvent under reduced pressure to dryness, and obtain the n-butanol extract. The n-butanol extract was loaded on a silica gel column and eluted with ethyl acetate:methanol:water (5:1:0.1), and a total of 45 fractions were obtained, which were concentrated under reduced pressure by rotary evaporation, and 10 to 40 fractions were combined. points to obtain a white powder, which is Sapindus saponin B (1.1g).

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Abstract

The invention relates to the natural pharmaceutical field, in particular to a compound (I) which is extracted and separated from the flower buds of Lonicera fulvotomentosa of Lonicera plants, of which a frame pertains to hedera helix triterpene; the invention also relates to a preparation method of the compound and the alkaline hydrolysis product as well as the application of the new compound in the preparation of the anti-tumor drugs as the pro-drug.

Description

technical field [0001] The invention relates to the field of natural medicines, in particular to extracting and isolating a new compound from flower buds of Lonicera chrysalis, the skeleton of which belongs to ivy-type triterpene saponins; the invention also relates to a preparation method of the compound and its alkali hydrolyzate, And the application of the new compound as a prodrug in the preparation of antitumor drugs. Background technique [0002] Malignant tumor is one of the major diseases that seriously endanger human health. The prevention and treatment of tumors has become a subject of widespread attention worldwide, and the research and development of antitumor drugs is also in an extremely urgent need. Plants are a valuable source of new biologically active molecules, and finding new drugs with antitumor activity from plant sources has attracted more and more attention from medical workers. Many anticancer drugs have been isolated from plants, such as vincristi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07J17/00A61K31/704A61P35/00
Inventor 李萍陈君汤丹
Owner CHINA PHARM UNIV
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