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Medical use of a pair of ginseng saponin aglycones and their mixture

A mixture and drug technology, applied in the field of medicine, can solve the problems of poor effect, many toxic and side reactions, and complicated process.

Inactive Publication Date: 2012-11-07
CHIA TAI TIANQING PHARMA GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tumor chemotherapy basically focuses on directly killing tumor cells. This treatment mode often has the following problems: it has poor or almost no effect on slow-growing solid tumors; the drug has little selectivity and has many and severe side effects, including bone marrow suppression. is the most important dose limiting factor
Although there are not too many toxic and side effects, due to strict technical requirements and complicated processes, the price is high, which is unbearable for many cancer patients and their families, which affects its popularization in the field of cancer treatment

Method used

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  • Medical use of a pair of ginseng saponin aglycones and their mixture

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: sodium hydroxide hydrolysis method prepares 25Rmdt and 25Smdt and their mixture (racemate)

[0030] Take by weighing 10 g of total saponins of ginseng fruit, dissolve in 1000 ml of sodium hydroxide with a concentration of 2.5 mol / L, and a concentration of 80% in methanol aqueous solution for 24 h, and then use 2.5 mol / L hydrochloric acid to neutralize the reaction solution, recover methanol under reduced pressure, and use The reaction solution was extracted with chloroform, and the chloroform phase was washed with water, dried over anhydrous sodium sulfate, and evaporated to dryness to collect the residue, separated by silica gel column chromatography, and gradient eluted with petroleum ether: ethyl acetate (10:1-1:1) to obtain 86 Fractions, fractions 52-55 were recrystallized from ethyl acetate to obtain 25Rmdt; fractions 56-58 were combined after TLC inspection, and after removing the solvent, ethyl acetate recrystallized to obtain a mixture of 25Rmdt and...

Embodiment 2

[0031] Embodiment 2: hydrochloric acid hydrolysis method prepares 25Rmdt and 25Smdt and their mixture (racemate)

[0032] Weigh 10 g of total saponins from American ginseng leaves, dissolve in 1000 ml of 80% methanol aqueous solution with hydrochloric acid concentration of 2.5 mol / L and sonicate. Ultrasonic conditions: frequency: 50kHz; power: 3KW; time: 30 minutes; hydrolyze at 40°C for 12 hours, neutralize the reaction solution with 2.5mol / L sodium hydroxide, recover methanol under reduced pressure, extract the reaction solution with chloroform, and chloroform phase Washed with water, dried over anhydrous sodium sulfate, evaporated to dryness to collect the residue, separated by silica gel column chromatography, chloroform: ethyl acetate (15:1-1:1) gradient elution to obtain 58 fractions, fractions 30-35 were 25Rmdt was obtained after ethyl acetate recrystallization; Fractions 36-38 were combined after TLC inspection, and after removing the solvent, ethyl acetate was recryst...

Embodiment 3

[0033] Example 3: 25Rmdt and 25Smdt and their mixtures inhibit the growth of human cancer cells in vitro

[0034] Using 6 kinds of human malignant tumor (human leukemia cell HL-60, human prostate cancer cell Du145, human breast cancer cell MCF-7, human colon cancer cell Colon205, human lung cancer cell A549 and human liver cancer cell Hep3B / HepG2) cell lines, adopt The in vitro anticancer activity of 25Rmdt and 25Smdt and their mixture was measured by MTT method, the concentration of which was measured was 0-500 μM, and the treatment time was 72 hours. Significant differences in sensitivity to these compounds were observed between different cell lines. For 25Rmdt and 25Smdt and their mixtures, the IC50 values ​​of most cell lines were in the lower μM level. (Preferably provide test data)

[0035] Table 1 IC50 of 25Rmdt and 25Smdt and their mixtures against 6 kinds of human tumor cells (μmol / L) (%) (M±SE)

[0036] MCF-7 HepG2 A549 Du145 Colon205 HL-60 ...

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Abstract

The invention belongs to a filed of medicine technology, which relates to a novel pair of panaxsapogenol and a medical application of a mixture thereof. The pair of compounds are 20(R)-25-methoxyl-dammarane-3beta, 12beta, 20-triol(25Rmdt for short) and 20(S)-25-me-thoxyl-dammarane-3beta, 12beta, 20-triol(25Smdt for short). The 25Rmdt and 25Smdt and the mixture thereof have the antitumor activities of inhibiting the growth and multiplication of a plurality of tumor cells, inducing the differentiation and withering of tumor cells, inhibiting the generation of tumor angiogenic blood vessels, inhibiting the invasion and transfer of tumors, enhancing the body immunity and reducing the toxic and side effects of chemotherapeutic drugs, which is substantially used for treating malignant tumors, with a total effective dosage of 1-100mg / kg / d.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a pair of new ginsenogenins and the medical application of their mixture. Specifically related to compounds 20(R)-25-methoxy-dammarane-3β,12β,20-triol and 20(S)-25-methoxy-dammarane-3β,12β,20-triol[ Namely 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol (25Rmdt for short) and 20(S)-25-me-thoxyl-dammarane-3β, 12β, 20-triol (25Smdt for short)] [0002] and their mixtures in inhibiting human tumor cells (human breast cancer, human small cell lung cancer, human gastric cancer, human colon cancer, human glial carcinoma, human melanoma, human cervical cancer, human liver cancer, promyelocytic leukemia, sarcoma S-180, liver cancer ascites type, mouse cervical cancer-14 and Ehrlich ascites carcinoma, etc.) growth and proliferation, induce tumor cell differentiation and apoptosis, inhibit tumor angiogenesis, inhibit tumor invasion and metastasis, and enhance the body's immunity application ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61P35/00
Inventor 赵余庆吴春福李巍杨静玉曹家庆张弘孙宝山
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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