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Chinese traditional extraction and the function containing dammarane type four-ring triterpene sapogenin

A tetracyclic triterpenoid, dammarane type technology, applied in the field of dammarane type tetracyclic triterpenoid saponin extract, can solve the problems of protein function damage, cell energy metabolism disorder, cell function damage, etc. Cardiotoxic effects

Inactive Publication Date: 2007-09-26
ZHEJIANG UNIV
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  • Claims
  • Application Information

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Problems solved by technology

However, several hypotheses have been supported by experimental evidence: 1) doxorubicin induces a large amount of oxygen free radicals, and excessive oxygen free radicals cause damage and death (or apoptosis) of cell function; 2) doxorubicin accumulates in mitochondria 3) Doxorubicin causes intracellular calcium ion overload, leading to cell apoptosis; 4) Doxorubicin causes excessive secretion of NO and superoxide anion free radicals A large amount of release, resulting in the nitro modification of the protein, leading to the destruction of protein function

Method used

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  • Chinese traditional extraction and the function containing dammarane type four-ring triterpene sapogenin
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Examples

Experimental program
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Effect test

Embodiment 1

[0016] Take 500g of Panax notoginseng medicinal material granules (3mm-8mm), dry at 50°C for 6 hours, add 10 times the amount of 70% ethanol and heat and reflux in a slightly boiling state to extract twice, each time for 2 hours, filter the extract, combine, and concentrate under reduced pressure to 0.5 g / mL (crude drug amount), above D 101 Macroporous resin. Rinse with 4 times the column volume of deionized water, discard, then rinse with 4BV of 0.05% ammonia water, discard, then rinse with deionized water until the effluent pH=7, continue to rinse with 4BV of 30% ethanol solution, discard, Finally, it was eluted with 5BV 70% ethanol solution, and the eluate was collected, concentrated under reduced pressure to no alcohol, and freeze-dried to obtain the total saponins of Panax notoginseng. Determined by HPLC external standard method, notoginseng saponin R in the refined product 1 8%, Ginsenoside Rg 1 44%, Ginsenoside Rb 1 28%, ginsenoside Rd10%, ginsenoside Re 5%, the ...

Embodiment 2

[0018] The notoginseng medicinal material is crushed to the size of soybeans to coarse powder, extracted 4 times with 40% water-containing alcohol under reflux, recovered the solvent, extracted 3 times with an equal volume of n-butanol, combined the extracts, concentrated to dryness, crushed, and washed with petroleum ether for 2 times, desolvation and drying. Adopt high performance liquid phase method (HPLC) to detect it, analysis condition is Agilent Extend-C18, mobile phase H 2 O-CH3CN, the detection wavelength is 203nm, and its content is determined by the external standard method. The contents of the five components are respectively notoginseng saponin R 1 3%, Ginsenoside Rg 1 25%, Ginsenoside Rb 1 14%, ginsenoside Rd 4%, ginsenoside Re 1.5%. The total content is 47.5%.

Embodiment 3

[0020] Cardiomyocytes from neonatal rats (Wistar rats) were isolated and seeded into 96-well plates. Cell density 5×10 5 pcs / hole. After culturing in DMEM+20% FBS medium for 48 hours, the cells adhered to the wall normally, and some cells beat regularly. Set up control group, model group (containing 0.1, 1 μ M doxorubicin hydrochloride), and different concentrations (12.5-100 μ g / ml) of notoginseng saponin group (added 1 hour before adding doxorubicin). After culturing for 24 hours, it was measured by MTT method, and the viability of cardiomyocytes was reflected by the 490nm colorimetric value. The results are shown in Figure 1 ( ** P* P<0.05).

[0021] Experiments have shown that 0.1 and 1 μM doxorubicin hydrochloride can cause significant myocardial cell damage, and the MTT value is significantly reduced; while the pre-administration of notoginseng saponin at a concentration of 12.5-100 μg / ml shows a certain protective effect. It shows that notoginseng saponins can prev...

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Abstract

The invention relates to a Chinese drug extractive which contains dammarane tetracyclic triterpene saponin. And the extractive is from notoginseng, which at least contains notoginseng saponin R1, panaxoside Rg1, Rb1, Re, and Rd at 45-95wt%. The inventive extractive on the anthracene nucleus resistant anti-cancer heart toxicity, via body test, has proved that the notoginseng saponin can significantly protect heart hurt induced by adriablastina, without reducing the anti-cancer effect of anthracene nucleus resistant anti-cancer drug. Therefore, the extractive can be used to prevent and reduce the heart toxicity of anthracene nucleus resistant anti-cancer drug, or added into other drug to form novel radiation auxiliary drug. The invention discloses the activity for resisting anthracene heart toxicity to widen the application of notoginseng.

Description

technical field [0001] The invention belongs to a traditional Chinese medicine extract, and relates to a dammarane-type tetracyclic triterpenoid saponin extract extracted from a traditional Chinese medicine Panax notoginseng. It will reduce the antitumor efficacy of the latter. technical background [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. Doxorubicin (Doxorubicin.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 and cost, and is one of the most commo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/258A61P9/00A61P35/00A61P39/02A61K31/704
Inventor 刘雳贺庆程翼宇瞿海斌师润史强霍杨窦静
Owner ZHEJIANG UNIV
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