CN110613703A - Application of d-borneol as adriamycin passivator - Google Patents
Application of d-borneol as adriamycin passivator Download PDFInfo
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- CN110613703A CN110613703A CN201811208165.2A CN201811208165A CN110613703A CN 110613703 A CN110613703 A CN 110613703A CN 201811208165 A CN201811208165 A CN 201811208165A CN 110613703 A CN110613703 A CN 110613703A
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- adriamycin
- borneol
- passivator
- doxorubicin
- tumor
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of d-borneol as an adriamycin passivator. The invention is based on the discovery that the dextro-borneol has the effect of inactivating the drug effect of the adriamycin when being combined with the adriamycin and applied to liver cancer cells and melanoma cells, and the invention is provided. The application of the d-borneol as the adriamycin passivator is to apply the d-borneol as the adriamycin passivator in the research of tumor mechanism; or the dextroborneol is prepared into adriamycin passivator for suspending chemotherapy and eliminating the effect of the adriamycin in the body of a tumor patient.
Description
Technical Field
The invention relates to application of d-borneol, in particular to application of d-borneol as an adriamycin passivator.
Background
Doxorubicin (Doxorubicin, DOX) belongs to the anthracycline antimetabolites and is one of the most clinically effective and widely used antineoplastic drugs. Doxorubicin can intercalate directly into the DNA molecule in an additive fashion between base pairs, causing DNA damage. The chimeric DOX can cause the synthesis of DNA and RNA to be blocked, can inhibit the activity of topoisomerase and destroy the high-level structure of DNA, and is widely used for treating breast cancer, bladder cancer, lung cancer, ovarian cancer and the like. However, doxorubicin has obvious toxic and side effects, 11% of patients have acute toxicity after treatment, and the doxorubicin belongs to one of chemotherapy drugs which are easy to cause liver damage, primary and acquired resistance of the doxorubicin also greatly influences the effect of chemotherapy, and the patients are difficult to tolerate or continue to finish treatment due to the toxic and side effects of high-dose chemotherapy drugs. Therefore, in patients who are difficult to tolerate the adverse effects of chemotherapy, it is necessary to suspend the chemotherapy and eliminate the effect of doxorubicin in the patient.
Borneol (borneel), commonly known as borneol, is a terpene and bicyclic organic compound extracted from resin and volatile oil of Dipterocarpaceae plant, and belongs to monoterpene alcohol, and is used for treating block pattern of coma, conjunctival congestion, sore throat, aphtha, sore and ulcer, unhealing after ulceration, coronary heart disease and angina pectoris. The d-borneol has low toxicity to normal cells of a human body and basically has no obvious influence. At present, the D-borneol is found to promote the medicine to pass through a blood brain barrier, and has sensitization effect on curcumin and derivatives thereof in melanoma cells, liver cancer cells and breast cancer cells. No report that D-borneol is used as an antitumor drug passivator exists, and the application of D-borneol as the passivator for weakening the drug effect of DOX and the drug resistance and toxic and side effects of chemotherapy has important research significance.
Disclosure of Invention
The invention aims to overcome the defects in the prior art and provide the application of the d-borneol as the adriamycin passivator.
The purpose of the invention is realized by the following technical scheme: the application of the d-borneol as the adriamycin passivator is based on the discovery that the d-borneol has the effect of passivating the drug effect of the adriamycin when being combined with the adriamycin to be applied to liver cancer cells and melanoma cells.
The application of the d-borneol as the adriamycin passivator is to apply the d-borneol as the adriamycin passivator in the research of tumor mechanism; or the dextroborneol is prepared into adriamycin passivator for suspending chemotherapy and eliminating the effect of the adriamycin in the body of a tumor patient.
The d-borneol is natural d-borneol.
The tumor is liver cancer or melanoma.
The adriamycin passivator comprises d-borneol and a pharmaceutically acceptable carrier.
The adriamycin passivator also comprises other components which are effective in passivating the pharmaceutical effect of the adriamycin.
When the tumor is melanoma, the dosage of the adriamycin passivator is calculated according to the ratio of 40-160 mug of dextroborneol to 0.03125-1 nmol of adriamycin; more preferably, the amount of D-borneol and adriamycin is 40-160 mug: 0.451-0.546 nmol.
When the tumor is liver cancer, the dosage of the adriamycin passivator is calculated according to the ratio of 40-80 mu g of dextroborneol to 0.561-0.662 nmol of adriamycin.
Compared with the prior art, the invention has the following advantages and effects:
the invention discovers that the effect of the adriamycin on melanoma cells and liver cancer cells can be reduced by using the dextroborneol as an adriamycin passivator, and the effect is completely different from that of the dextroborneol reported in the prior art. The d-borneol has different effects when combined with different antitumor drugs for use in different tumor cells, which opens up a way for researching different tumor mechanisms. Based on the strong side effect of the adriamycin, the d-borneol can reduce the drug effect of the adriamycin on melanoma cells and liver cancer cells, and can be used for suspending chemotherapy, eliminating the drug effect of the adriamycin in a patient body, reducing toxic and side effects and weakening chemotherapy resistance.
DETAILED DESCRIPTION OF EMBODIMENT (S) OF INVENTION
The present invention will be described in further detail with reference to specific examples, but the embodiments of the present invention are not limited thereto.
Example 1MTT method for detecting the influence of natural D-borneol and adriamycin on cell growth
Mixing hepatoma cell line HepG2 (2X 10)4One cell/mL) was seeded in a 96-well plate at 100 μ L/well, HepG2 cells were pretreated with 100 μ L of natural d-borneol (final concentrations of 40, 80 and 160 μ g/mL, i.e. concentration in cells) for 12h after the cells were attached (about 24h), and then doxorubicin was added in 6 concentration gradients (0.03125 μ M, 0.0625 μ M, 0.125 μ M, 0.25 μ M, 0.5 μ M and 1 μ M) at 3 concentrations, respectively, to HepG2 cells pretreated with 3 concentrations of natural d-borneol, and a control group was set. Adding 5mg/mL tetrazolium MTT dye solution into each well after 72h, culturing for 3h, adding DMSO for dissolution, detecting OD value with wavelength of 570nm by an enzyme-labeling instrument, calculating cell survival rate, drawing a cell growth curve, and calculating IC50The value is obtained. According to the above steps, melanoma is respectively treatedThe cell line A375, the human non-small cell lung cancer cell A549 and the breast cancer cell line MCF-7 are used as detection objects, and the detection results are shown in Table 1:
TABLE 1
The results in Table 1 show that the natural d-borneol does not all have sensitization effect on different cancer cells, and the natural d-borneol has inactivation effect on adriamycin on melanoma cells and liver cancer cells.
The above embodiments are preferred embodiments of the present invention, but the present invention is not limited to the above embodiments, and any other changes, modifications, substitutions, combinations, and simplifications which do not depart from the spirit and principle of the present invention should be construed as equivalents thereof, and all such changes, modifications, substitutions, combinations, and simplifications are intended to be included in the scope of the present invention.
Claims (9)
1. Application of d-borneol as doxorubicin deactivator is provided.
2. Use of d-borneol as a deactivant for doxorubicin according to claim 1, characterized in that: d-borneol is used as an adriamycin passivator to be applied to the research of tumor mechanism; or the dextroborneol is prepared into adriamycin passivator for suspending chemotherapy and eliminating the effect of the adriamycin in the body of a tumor patient.
3. Use of d-borneol as a doxorubicin deactivator according to claim 1 or 2, characterized in that: the d-borneol is natural d-borneol.
4. Use of d-borneol as a deactivant for doxorubicin according to claim 2, characterized in that: the tumor is liver cancer or melanoma.
5. Use of d-borneol as a deactivant for doxorubicin according to claim 2, characterized in that: the adriamycin passivator comprises d-borneol and a pharmaceutically acceptable carrier.
6. Use of d-borneol as a deactivant for doxorubicin according to claim 5, characterized in that: the adriamycin passivator also comprises other components which are effective in passivating the pharmaceutical effect of the adriamycin.
7. Use of d-borneol as a deactivant for doxorubicin according to claim 5, characterized in that: when the tumor is melanoma, the dosage of the adriamycin passivator is calculated according to the ratio of 40-160 mu g of dextroborneol to 0.03125-1 nmol of adriamycin.
8. Use of d-borneol as a deactivant for doxorubicin according to claim 7, characterized in that: the dosage of the adriamycin passivator is calculated according to the ratio of 0.451-0.546 nmol to 40-160 mug of dextroborneol and adriamycin.
9. Use of d-borneol as a deactivant for doxorubicin according to claim 5, characterized in that: when the tumor is liver cancer, the dosage of the adriamycin passivator is calculated according to the ratio of 40-80 mu g of dextroborneol to 0.561-0.662 nmol of adriamycin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811208165.2A CN110613703A (en) | 2018-10-17 | 2018-10-17 | Application of d-borneol as adriamycin passivator |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811208165.2A CN110613703A (en) | 2018-10-17 | 2018-10-17 | Application of d-borneol as adriamycin passivator |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110613703A true CN110613703A (en) | 2019-12-27 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201811208165.2A Pending CN110613703A (en) | 2018-10-17 | 2018-10-17 | Application of d-borneol as adriamycin passivator |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105147647A (en) * | 2015-08-19 | 2015-12-16 | 华南理工大学 | Application of d-borneol serving as antitumor drug sensitizer |
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2018
- 2018-10-17 CN CN201811208165.2A patent/CN110613703A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105147647A (en) * | 2015-08-19 | 2015-12-16 | 华南理工大学 | Application of d-borneol serving as antitumor drug sensitizer |
Non-Patent Citations (2)
| Title |
|---|
| 国家医师资格考试研究中心编著: "《临床执业助理医师核心考点精讲》", 30 June 2014, 世界图书出版公司北京公司 * |
| 蒋学华主编: "《药物评价方法概论》", 31 March 2005, 四川大学出版社 * |
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Application publication date: 20191227 |
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| RJ01 | Rejection of invention patent application after publication |