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Liquorice extractive for decreasing medicine heart toxicity and applications thereof

A technology of licorice extract and cardiotoxicity, applied in drug combination, drug delivery, medical preparations containing active ingredients, etc., can solve the problems of large dosage and nephrotoxicity

Inactive Publication Date: 2008-07-30
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dosage of dexrazoxane is very large, usually 10 times that of doxorubicin, and it has certain nephrotoxicity
If the combination of dexrazoxane and doxorubicin is used, the economic burden of patients will be increased by 5-10 times

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] The licorice medicinal material was extracted twice with 10 times the amount of 70% ethanol, each time for 1.5 hours. After being concentrated to no alcohol, the D101 resin was separated, washed with three column volumes of water, and then washed with 70% ethanol, the effluent was collected, concentrated and dried, that is the total glycyrrhizin extract, with a yield of 10.8%. Taking liquiritin as the reference substance, the total flavonoid content of the extract was determined by UV-spectrophotometry at 25.8%. According to the provisions of "Chinese Pharmacopoeia 2005 Edition Part One", using glycyrrhizic acid as the reference substance, the content of glycyrrhizic acid was determined by HPLC method to be 15.1%.

Embodiment 2

[0014] Radix Glycyrrhiza is extracted twice with 8 times the amount of water by boiling under reflux, each time for 1.5 hours. Combined and cooled, add ethanol to 60%, ethanol precipitation overnight, centrifuge to take the supernatant, concentrate to no alcohol, separate AB-8 resin, wash with three column volumes of water and 20% ethanol in turn, and then wash with 80% ethanol Rinse, collect the effluent, concentrate and dry, that is total glycyrrhizin extract, the yield is 9.2%. Taking liquiritin as the reference substance, the total flavonoid content of the extract was determined by UV-spectrophotometry at 33.4%. According to the provisions of "Chinese Pharmacopoeia 2005 Edition Part One", using glycyrrhizic acid as a reference substance, the content of glycyrrhizic acid was determined by HPLC method to be 25.5%.

Embodiment 3

[0016] Rat cardiomyocyte cell line H 9 C 2 , seeded into a 96-well plate. The cell density is 1×105 / well. After culturing in DMEM+10% FBS medium for 24 hours, drug treatment was carried out. Set up control group, model group (containing 1 μ M doxorubicin hydrochloride), and different concentrations (0.1, 0.5, 1, 5, 10, 50, 100 μ g / ml) of licorice extract (added 30 minutes before adding doxorubicin) . After culturing for 24 hours, it was measured by MTT method, and the viability of cardiomyocytes was reflected by the 550nm colorimetric value. Experiments have shown that 1 μM doxorubicin hydrochloride can reduce the viability of cardiomyocytes by 23.4% (P<0.01), while pre-administration of licorice extract at a concentration of 1-50 μg / ml shows a certain protective effect, and the cell viability is improved compared with the model group. 11.2-14.2%, among which 10, 50 μg / ml concentration, there is a significant difference (P<0.01). It shows that the extract of total glycyr...

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Abstract

The invention provides a liquorice extract for alleviating the toxicity of heart medicines; the extract originats from legume liquorice, such as the dried roots and rhizomes of Glycyrrhiza uralensis Fisch, G. Inflata Bat, and G Glabra L. The main active components are triterpenoid saponin and materials of flavonoids glycosides; wherein, the content of triterpenoid saponin is 10 to 30 percent, and the content of flavonoids is 20 to 40 percent. The in-vivo and in-vitro experiments prove that the liquorice extract has significant protection effect for heart injury induced by adriamycin, at the same time, the liquorice extract does not lower the antitumor effect for anthracycline antitumor medicine; the extract can prevent and lighten the toxicity of anthracycline heart medicines, so the extract improves the efficacy and enlarges the clinical application range; the extract can also be applied in the preparation of anthracycline antitumor medicines for treating heart toxicity.

Description

technical field [0001] The invention belongs to a traditional Chinese medicine extract, which relates to glycosides extracted from the traditional Chinese medicine licorice, mainly including flavonoid glycosides and triterpenoid saponins. Do not weaken the antitumor effect of anthracycline antitumor drugs (such as doxorubicin). Background technique [0002] Since the first anthracycline anticancer drug, Daunorubicin, was isolated in 1957, anthracycline anticancer drugs have become a class of chemotherapy drugs widely used clinically. Doxombicin (DXR; Adriamycin, ADM) has become an anthracycline anticancer drug since it entered clinical trials in the 1970s. representative drugs. ADM is effective for a variety of tumors, including: hematological tumors, malignant lymphomas, breast cancer, bladder cancer, lung cancer, ovarian cancer, cervical cancer, testicular cancer, head and neck tumors, and bone and soft tissue tumors. ADM is low in price and relatively high in efficacy ...

Claims

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Application Information

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IPC IPC(8): A61K36/484A61K9/48A61K9/20A61K9/16A61K9/10A61K9/08A61P39/02A61K31/7048A61K31/704
Inventor 刘雳程翼宇瞿海斌张玲霍杨葛志伟水文波
Owner ZHEJIANG UNIV
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