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Use of 3β,20(s),21-trihydroxydammarane-24-ene in the preparation of tumor multidrug resistance reversal agent

A technology of trihydroxydammarane and drug resistance reversal, applied in antitumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of affecting the pharmacokinetics of anticancer drugs, not getting the expected effect, restricting the scope of application, etc. Achieve the effect of overcoming drug resistance, inhibiting proliferation, and enhancing therapeutic effects

Inactive Publication Date: 2015-10-28
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Attempts to reduce their toxicity did not have the desired effect
The second generation of sensitizers can significantly affect the pharmacokinetics of anticancer drugs, although no obvious toxicity has been found
However, most of these reversal agents have high toxicity and low activity, which seriously restrict their application [M.Susa, E.Choy, C.Yang, J.Schwab, H.Mankin, F.Hornicek and Z.Duan, J. Biomol Screen, 15287. S.S. Winter, D.M. Lovato, H.M. Khawaja, B.S. Edwards, I.D. Steele, S.M. Young, T.I. Oprea, L.A. Sklar and R.S. Larson, J Biomol Screen, 13 (2008) 185. A. Katsman, K. Umezawa and B. Bonavida, Drug Resist Update, 10 (2007) 1.]

Method used

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  • Use of 3β,20(s),21-trihydroxydammarane-24-ene in the preparation of tumor multidrug resistance reversal agent
  • Use of 3β,20(s),21-trihydroxydammarane-24-ene in the preparation of tumor multidrug resistance reversal agent
  • Use of 3β,20(s),21-trihydroxydammarane-24-ene in the preparation of tumor multidrug resistance reversal agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: CCK-8 kit detects the cytotoxicity of H6

[0037] Experimental Materials:

[0038] H6 is extracted from Gynostemma pentaphyllum, a plant of Cucurbitaceae, with a purity of not less than 95%. Human liver cancer cell line HepG2, human liver cancer cell line SMMC-7721, human liver cancer cell line Hep3B, human leukemia cell line THP-1, human leukemia cell line K562, undifferentiated human gastric cancer cell line HGC-27, human ovarian cancer cell line SKOV3, human pancreatic cancer cell line PANC-1, human colon cancer cell line SW480, human cervical cancer cell line HeLa, human lung adenocarcinoma cell line A549, and human breast cancer cell line MDA-MB-453 were purchased from Shanghai Biochemical Cell, Chinese Academy of Sciences cell bank. Human umbilical vein epithelial cells (HUVEC-2C) cell lines were purchased from Cascade Biologics Biotechnology Company.

[0039] experimental method:

[0040] Cell recovery

[0041] 1) Take out the cryotube from the li...

Embodiment 2

[0063] Example 2: CCK-8 kit detects drug-resistant cell lines' resistance to H6

[0064] Experimental Materials:

[0065] Verapamil (VPL), vincristine (VCR) and doxorubicin (ADR) were purchased from Roche Chemical Company with a purity greater than 99%. CCK-8 kit was purchased from Tongren Company.

[0066] Human oral epithelial carcinoma KB cells and their vincristine-resistant strain KB / VCR, human breast cancer MCF-7 cells and their adriamycin-resistant strain MCF-7 / ADR were prepared by Shanghai Institute of Materia Medica, Chinese Academy of Sciences.

[0067] experimental method:

[0068] The methods of cell recovery and cell cryopreservation are the same as in Example 1.

[0069] Subculture of cells: Human oral epithelial carcinoma KB cells and their vincristine-resistant strain KB / VCR were cultured in α-MEM medium containing 10% FBS, 2mM glutamine and 1mM sodium pyruvate. Adriamycin-resistant human breast cancer cell line MCF-7 / ADR was cultured in α-MEM medium contai...

Embodiment 3

[0079] Example 3: The CCK-8 method detects the reversal effect of H6 on the multidrug tolerance activity of drug-resistant cell lines

[0080] Experimental material: with embodiment 2.

[0081] experimental method:

[0082] H6 sensitization experiment: KB and KB / VCR cells were inoculated into 96-well plates at a density of 3500 / well, and after 24 hours, different concentrations of VCR, and different concentrations of VCR and H6 were mixed with α-MEM containing 10% fetal bovine serum After being prepared, it is added to each hole. After culturing for 48 hours, discard the culture medium, and use the CCK-8 kit to measure the activity of drug-resistant cell lines and their parental cells to VCR and VCR+H6 in the same manner as in Example 1, and draw a curve.

[0083] Three replicate wells were set up for each concentration, and the experiment was repeated three times.

[0084] Experimental results:

[0085] The multiplicity of drug resistance of KB / VCR cells to VCR was 81.9 t...

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Abstract

The invention belongs to the field of medicine, relates to applications of 3 beta, 20(s), 21-trihydroxydammarane-24-alkene on preparation of drugs for curing tumors, and especially relates to applications of 3 beta, 20(s), 21-trihydroxydammarane-24-alkene on preparation of tumor multi-drug resistance (MDR) reversing agents. The 3 beta, 20(s), 21-trihydroxydammarane-24-alkene is a natural product, has the function, which has been testified by tests, of reversing multi-drug resistance (MDR) of tumor cells, is capable of being used as a multi-drug resistance (MDR) reversing agent; also has the function of increasing sensitivity of multi-drug resistance (MDR) cells to anti-tumor drugs, and is capable of being used as a sensitizer. The invention also provides an anti-tumor drug, and a pharmaceutical composition, which is jointly used with 3 beta, 20(s), 21-trihydroxydammarane-24-alkene. The small molecular compound, which is used as a novel anti-tumor drug or an auxiliary component of an anti-tumor drug, has the advantages of prominent tumor inhibiting effect and environment-friendliness, and provides a novel way for curing tumors.

Description

technical field [0001] The invention belongs to the pharmaceutical field of sensitizing anti-tumor drugs and reversing multi-drug resistance of tumors, and specifically relates to the new application of gypenogenin 3β, 20(S), 21-trihydroxydammarane-24-ene, namely in the preparation of The application of tumor multidrug resistance reversal agent. Background technique [0002] Malignant tumors seriously endanger human life and health, and have become one of the main causes of disease death today. The main treatment methods for malignant tumors are surgery, radiotherapy and chemotherapy. A large number of studies have shown that malignant tumors are systemic diseases rather than local lesions. Therefore, compared with local treatment methods such as surgery and radiotherapy, tumor drug therapy, that is, chemotherapy, has become a method of treating tumors, prolonging the survival time of patients and improving the quality of life. important measure of quality of life. Accord...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61P35/00
Inventor 余龙朱恒锐刘祖龙胡立宏刘军华
Owner FUDAN UNIV
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