CN109432069A - A kind of application of loudspeaker tea alkene in terms for the treatment of of human cervical cancer - Google Patents
A kind of application of loudspeaker tea alkene in terms for the treatment of of human cervical cancer Download PDFInfo
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- 241001122767 Theaceae Species 0.000 title claims abstract description 19
- 150000001336 alkenes Chemical class 0.000 title claims abstract description 19
- 238000011282 treatment Methods 0.000 title claims abstract description 19
- 206010008342 Cervix carcinoma Diseases 0.000 title abstract description 6
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 title abstract description 6
- 201000010881 cervical cancer Diseases 0.000 title abstract description 6
- 208000019065 cervical carcinoma Diseases 0.000 claims abstract description 22
- 208000009849 Female Genital Neoplasms Diseases 0.000 claims abstract description 11
- 239000003814 drug Substances 0.000 claims description 12
- 229940079593 drug Drugs 0.000 claims description 7
- 239000000463 material Substances 0.000 claims description 5
- 239000002552 dosage form Substances 0.000 claims description 4
- 239000002775 capsule Substances 0.000 claims description 2
- 239000000470 constituent Substances 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 239000011344 liquid material Substances 0.000 claims description 2
- 208000026037 malignant tumor of neck Diseases 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 abstract description 18
- 206010033128 Ovarian cancer Diseases 0.000 abstract description 17
- UIDUJXXQMGYOIN-UHFFFAOYSA-N aromadendrin Natural products CC1(C)C2C1CCC(C)C1C2C(C)CC1 UIDUJXXQMGYOIN-UHFFFAOYSA-N 0.000 abstract description 14
- 230000035755 proliferation Effects 0.000 abstract description 11
- AYXPYQRXGNDJFU-AOWZIMASSA-N Ledol Chemical compound [C@@H]1([C@](CC[C@@H]2[C@H]3C2(C)C)(C)O)[C@H]3[C@H](C)CC1 AYXPYQRXGNDJFU-AOWZIMASSA-N 0.000 abstract description 10
- CKZXONNJVHXSQM-UHFFFAOYSA-N Ledol Natural products CC(C)C1CCC(C)(O)C2C3CC(C)CC123 CKZXONNJVHXSQM-UHFFFAOYSA-N 0.000 abstract description 10
- 230000002401 inhibitory effect Effects 0.000 abstract description 8
- OGJFTQVVQQMGJG-MRVPVSSYSA-N (8r)-1,5,8-trimethyl-7,8-dihydro-6h-azuleno[6,5-b]furan-2-one Chemical compound C=1C2=C(C)C(=O)OC2=CC(C)=C2CC[C@@H](C)C2=1 OGJFTQVVQQMGJG-MRVPVSSYSA-N 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 7
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- BRMFFEZRHCLFKV-UHFFFAOYSA-N Isorupestonic acid Natural products CC1CCC(C(=C)C(O)=O)CC2=CC(=O)CCC12 BRMFFEZRHCLFKV-UHFFFAOYSA-N 0.000 abstract description 4
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- 206010028980 Neoplasm Diseases 0.000 description 5
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- 238000002512 chemotherapy Methods 0.000 description 5
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- 229930014626 natural product Natural products 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 108091003079 Bovine Serum Albumin Proteins 0.000 description 3
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- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- 229930182555 Penicillin Natural products 0.000 description 2
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- 239000008103 glucose Substances 0.000 description 2
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- 150000002576 ketones Chemical class 0.000 description 2
- 229940049954 penicillin Drugs 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- GJHJZCGMDGIUKC-BQELKBSMSA-N (2s)-2-[(5r)-5-ethenyl-5-methyloxolan-2-yl]-4,4-dimethylhex-5-en-3-one Chemical compound C=CC(C)(C)C(=O)[C@@H](C)C1CC[C@](C)(C=C)O1 GJHJZCGMDGIUKC-BQELKBSMSA-N 0.000 description 1
- 208000005641 Adenomyosis Diseases 0.000 description 1
- GJHJZCGMDGIUKC-UHFFFAOYSA-N Artemone Natural products C=CC(C)(C)C(=O)C(C)C1CCC(C)(C=C)O1 GJHJZCGMDGIUKC-UHFFFAOYSA-N 0.000 description 1
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 description 1
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- 208000029082 Pelvic Inflammatory Disease Diseases 0.000 description 1
- 241000863480 Vinca Species 0.000 description 1
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- 150000001298 alcohols Chemical class 0.000 description 1
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- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 description 1
- 229940127093 camptothecin Drugs 0.000 description 1
- 239000012930 cell culture fluid Substances 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
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- 230000009429 distress Effects 0.000 description 1
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 description 1
- 238000007876 drug discovery Methods 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 201000009274 endometriosis of uterus Diseases 0.000 description 1
- 229930013356 epothilone Natural products 0.000 description 1
- HESCAJZNRMSMJG-KKQRBIROSA-N epothilone A Chemical class C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 HESCAJZNRMSMJG-KKQRBIROSA-N 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000035558 fertility Effects 0.000 description 1
- 238000011337 individualized treatment Methods 0.000 description 1
- 238000011221 initial treatment Methods 0.000 description 1
- 201000010260 leiomyoma Diseases 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 230000031700 light absorption Effects 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 230000010355 oscillation Effects 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 201000008016 ovarian benign neoplasm Diseases 0.000 description 1
- 208000025661 ovarian cyst Diseases 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 210000004999 sex organ Anatomy 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 210000004291 uterus Anatomy 0.000 description 1
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Classifications
-
- 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
- A61K31/01—Hydrocarbons
- A61K31/015—Hydrocarbons carbocyclic
-
- 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
-
- 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
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
-
- 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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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of application of loudspeaker tea alkene in terms for the treatment of of human cervical cancer.It is a discovery of the invention that gweicurculactone, isorupestonic acid, 7- aromadendrene -6- ketone and 4- aromadendrene have excellent inhibited proliferation to human ovarian cancer SKOV3 cell and human cervical carcinoma Hela cell;Although loudspeaker tea alkene is chemically the dehydration product of ledol in structure, chemical structure is more similar, but to the proliferation inhibition activity of human ovarian cancer SKOV3 cell, human cervical carcinoma Hela cell, but difference is larger, wherein: loudspeaker tea alkene is obvious to human cervical carcinoma Hela cell's inhibited proliferation, human ovarian cancer SKOV3 cell inhibitory effect is acted on unobvious, and ledol acts on obviously human ovarian cancer SKOV3 cell inhibitory effect, it is unobvious to human cervical carcinoma Hela cell's inhibited proliferation.Loudspeaker tea alkene, ledol, gweicurculactone, isorupestonic acid, 7- aromadendrene -6- ketone and 4- aromadendrene may be incorporated for treatment gynecological tumor.
Description
Technical field
The invention belongs to field of medicaments, are related to gynaecology, and in particular to a kind of loudspeaker tea alkene answering in terms for the treatment of of human cervical cancer
With.
Background technique
Gynecological tumor is a kind of common disease for seriously threatening body of women health, frequently-occurring disease, is divided into benign and malignant.Often
The gynaecology's benign tumour seen includes benign tumor of ovary, ovary tumor-like lesion (pure ovarian cyst and chocolate cyst of ovary
Deng), pelvic inflammation mass, uterus adenomyosis, fibroid etc., treatment requires according to the age of patient, fertility, symptom it is tight
Principal characteristic, extent of disease, the past treatment history and the wish of patient and take individualized treatment measure, specific method include operation, medicine
Object, intervention etc., wherein operation is main therapeutic modality, but its damage to ovarian function is gradually paid attention in recent years.In
Medical treatment gynaecology benign tumour can control and reduce tumor size for being not up to the patient of surgical indication, it is allowed to avoid
Operation wound;For the patient of peri-operation period, preoperative Chinese medicine treatment can improve general status, improve tolerance, facilitate
Operation carries out, and healthy tendency can be improved in postoperative Chinese medicine treatment, prevents from recurring.Common gynecologic malignant tumor has cervical carcinoma, endometrium
Cancer and oophoroma, treatment is with auxiliary surgical based on radiotherapy, chemotherapy.No matter perform the operation or radiotherapy, chemotherapy, easily damage human body is being just
Gas leads to insufficiency of vital energy and blood, imbalance of yin and yang, and a series of toxicity or complication occurs.
Oophoroma is one of big malignant tumour of female sex organs 3, however case fatality rate but occupies the first place of gynecologic malignant tumor.Closely
The disease incidence of Nian Lai, oophoroma increase year by year.The concealment of oophoroma early symptom often has already appeared abdominal cavity before symptom appearance and turns
It moves, when 60%~70% patient assessment has been in advanced stage.Oophoroma initial treatment is based on performing the operation, supplemented by chemotherapy, Combined with Radiotherapy
Treatment, biologic treatment etc..Although can reach complete incidence graph by initial surgery and chemotherapy, most patients with terminal still can be 2~3
Year recurrence, and finally development is dead for chemotherapy resistance.
Cervical carcinoma is common one of gynecologic malignant tumor, and in women worldwide malignant tumour, disease incidence occupies
3, in developing country women, the disease incidence of the disease and its caused mortality are above developed country.With other cancers
Disease is compared, and cervical carcinoma frequently-occurring disease is in middle-aged women, and this age bracket women is in cause and looks after the important period of family.Palace
The generation of neck cancer brings considerable distress and threat to patient and its family.
Natural products is the important sources of existing drug, also have in anti-tumor drug discovery procedure important role and
Meaning.According to statistics, 50% directly or indirectly derives from natural products in the new drug listed between 1981 to 2006.Individually
For antineoplastic, there are about 2/3 medicament sources in natural products.Some anti-tumor drugs from natural products are such as purple
China fir alcohols, camptothecin, vinca, podophillotoxines, epothilones etc. have played important function in treatment tumour.
Summary of the invention
The purpose of the present invention is to provide a kind of application of loudspeaker tea alkene in terms for the treatment of of human cervical cancer.
Above-mentioned purpose of the present invention is achieved through the following technical solutions:
A kind of application of loudspeaker tea alkene in the drug of preparation treatment gynecological tumor, the gynecological tumor are cervical carcinoma.
A kind of drug for treating gynecological tumor is aided with pharmaceutically acceptable auxiliary material using loudspeaker tea alkene as active constituent,
Pharmaceutically acceptable dosage form is made.
Further, the auxiliary material is solid or Auxiliary Liquid Material.
Further, the dosage form is tablet, capsule or injection.
The utility model has the advantages that
It is a discovery of the invention that gweicurculactone, isorupestonic acid, 7- aromadendrene -6- ketone and 4- aromadendrene are to human ovarian cancer
SKOV3 cell and human cervical carcinoma Hela cell have excellent inhibited proliferation;Although loudspeaker tea alkene is chemically in structure
The dehydration product of ledol, chemical structure is more similar, but to human ovarian cancer SKOV3 cell, human cervical carcinoma Hela cell
Proliferation inhibition activity but difference is larger, in which: loudspeaker tea alkene is obvious to human cervical carcinoma Hela cell's inhibited proliferation, to people
The effect of oophoroma SKOV3 cell inhibitory effect is unobvious, and ledol is bright to the effect of human ovarian cancer SKOV3 cell inhibitory effect
It is aobvious, it is unobvious to human cervical carcinoma Hela cell's inhibited proliferation.Loudspeaker tea alkene, ledol, gweicurculactone, different alpine yallow herb
Ketone acid, 7- aromadendrene -6- ketone and 4- aromadendrene may be incorporated for treatment gynecological tumor.
Detailed description of the invention
Fig. 1 is the chemical structural formula for the compound that the present invention tests.
Specific embodiment
Essentiality content of the present invention is specifically introduced below with reference to embodiment, but does not limit protection model of the invention with this
It encloses.
One, experimental material
The structural formula of compound is tested as shown in Figure 1, including loudspeaker tea alkene, ledol, gweicurculactone, different alpine yallow herb
Ketone acid, 7- aromadendrene -6- ketone and 4- aromadendrene, standard items purchase or self-control, purity >=98%.
Human ovarian cancer SKOV3 cell, human cervical carcinoma Hela cell are purchased from Chinese Academy of Sciences Shanghai cell bank.
DMEM/F12 culture medium, DMEM in high glucose culture medium, fetal calf serum are purchased from GIBCO company.
Methyl thiazoly tetrazolium assay (MTT), DMSO are purchased from SIGMA company.
Dual anti-solution, trypsase are purchased from U.S. Hyclone company.
Two, experimental method
1, cell culture
Human ovarian cancer SKOV3 cell culture (contains 10% fetal calf serum, 100U/ml penicillin, 100U/ml in DMEM/F12
Streptomysin) culture solution, in 37 DEG C, 5%CO2, adherent growth under conditions of saturated humidity, every 3~4 days with 0.25% trypsase
Had digestive transfer culture, logarithmic growth phase cell is for testing.
Human cervical carcinoma Hela cell is incubated at DMEM in high glucose (containing 10% fetal calf serum, 100U/ml penicillin, 100U/ml chain
Mycin) culture solution, in 37 DEG C, 5%CO2, adherent growth under conditions of saturated humidity, disappeared with 0.25% trypsase within every 3~4 days
Change passage, logarithmic growth phase cell is for testing.
2, mtt assay measures each compounds on ovarian cancer, the inhibiting effect of cervical cancer cell
(1) human ovarian cancer SKOV3 cell, the human cervical carcinoma Hela cell of logarithmic growth phase are collected, adjustment cell suspension is dense
It spends to 5 × 104100 μ L cell suspensions, bed board is added in a/mL, every hole.
(2) 96 orifice plates are placed in 37 DEG C, 5%CO2Incubator is incubated for for 24 hours.
(3) each compound is dissolved separately in DMSO, 7 concentration gradients, 5 repeating holes of each concentration is set.
(4) 96 orifice plates are placed in 37 DEG C, 5%CO2Incubator after being incubated for 48h, abandons culture solution, it is fresh that 100 μ L are added in every hole
Cell culture fluid;10 μ LMTT solution (5mg/mL) are added in every hole, continue to cultivate 4h.
(5) 150 μ L dimethyl sulfoxides are once added in each hole, low-speed oscillation 5min, abundant to purple crystal thing
Dissolution.Light absorption value of each hole at OD490nm is read under enzyme-linked immunosorbent assay instrument.
(6) inhibiting rate of each compound on tumor cell is calculated according to the following formula, according to inhibition rate of tumor cell, uses SPSS
17.0 statistics softwares calculate IC50 (half-inhibitory concentration) value.
Inhibition rate of tumor cell=(1- experimental group OD/ control group OD) × 100%.
Three, experimental result
Each compound is as shown in table 1 to the IC50 value of human ovarian cancer SKOV3 cell, human cervical carcinoma Hela cell.
Table 1 tests compound to the IC50 value of human ovarian cancer SKOV3 cell, human cervical carcinoma Hela cell
The above results show gweicurculactone, isorupestonic acid, 7- aromadendrene -6- ketone and 4- aromadendrene to people's ovary
Cancer SKOV3 cell and human cervical carcinoma Hela cell have excellent inhibited proliferation;Although loudspeaker tea alkene is chemically in structure
For the dehydration product of ledol, chemical structure is more similar, but thin to human ovarian cancer SKOV3 cell, human cervical carcinoma Hela
But difference is larger for the proliferation inhibition activity of born of the same parents, in which: loudspeaker tea alkene is obvious to human cervical carcinoma Hela cell's inhibited proliferation, right
The effect of human ovarian cancer SKOV3 cell inhibitory effect is unobvious, and ledol acts on human ovarian cancer SKOV3 cell inhibitory effect
Obviously, unobvious to human cervical carcinoma Hela cell's inhibited proliferation.It is loudspeaker tea alkene, ledol, gweicurculactone, one different
Artemone acid, 7- aromadendrene -6- ketone and 4- aromadendrene may be incorporated for treatment gynecological tumor.
The effect of above-described embodiment is specifically to introduce essentiality content of the invention, but those skilled in the art should know
Protection scope of the present invention should not be confined to the specific embodiment by road.
Claims (4)
1. a kind of application of loudspeaker tea alkene in the drug of preparation treatment gynecological tumor, it is characterised in that: gynecological tumor is uterine neck
Cancer.
2. a kind of drug for treating gynecological tumor, it is characterised in that: using loudspeaker tea alkene as active constituent, being aided with can pharmaceutically be connect
Pharmaceutically acceptable dosage form is made in the auxiliary material received;The gynecological tumor is cervical carcinoma.
3. drug according to claim 2, it is characterised in that: the auxiliary material is solid or Auxiliary Liquid Material.
4. drug according to claim 2, it is characterised in that: the dosage form is tablet, capsule or injection.
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN110613685A (en) * | 2019-10-23 | 2019-12-27 | 李金鹏 | Injection for treating gynecological tumor |
CN116768826A (en) * | 2023-04-25 | 2023-09-19 | 中国科学院新疆理化技术研究所 | Rupestonic acid amide derivative containing nitrogen heterocycle, and preparation method and application thereof |
CN117159552A (en) * | 2023-09-06 | 2023-12-05 | 南京诺源医疗器械有限公司 | Application of petaganine green in preparation of ovarian cancer and/or cervical cancer subcutaneous transplantation tumor inhibitor |
-
2018
- 2018-11-04 CN CN201811304331.9A patent/CN109432069A/en not_active Withdrawn
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN110613685A (en) * | 2019-10-23 | 2019-12-27 | 李金鹏 | Injection for treating gynecological tumor |
CN110613685B (en) * | 2019-10-23 | 2021-03-19 | 成植温 | Injection for treating gynecological tumor |
CN116768826A (en) * | 2023-04-25 | 2023-09-19 | 中国科学院新疆理化技术研究所 | Rupestonic acid amide derivative containing nitrogen heterocycle, and preparation method and application thereof |
CN117159552A (en) * | 2023-09-06 | 2023-12-05 | 南京诺源医疗器械有限公司 | Application of petaganine green in preparation of ovarian cancer and/or cervical cancer subcutaneous transplantation tumor inhibitor |
CN117159552B (en) * | 2023-09-06 | 2024-02-13 | 南京诺源医疗器械有限公司 | Application of petaganine green in preparation of ovarian cancer and/or cervical cancer subcutaneous transplantation tumor inhibitor |
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Application publication date: 20190308 |