CN109481432A - A kind of application of gweicurculactone in terms of gynecological neoplasm - Google Patents

A kind of application of gweicurculactone in terms of gynecological neoplasm Download PDF

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Publication number
CN109481432A
CN109481432A CN201811304333.8A CN201811304333A CN109481432A CN 109481432 A CN109481432 A CN 109481432A CN 201811304333 A CN201811304333 A CN 201811304333A CN 109481432 A CN109481432 A CN 109481432A
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China
Prior art keywords
cell
gweicurculactone
cervical carcinoma
aromadendrene
ovarian cancer
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CN201811304333.8A
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Inventor
张长林
杨佳
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Huaian Pei Yuan Gene Technology Co Ltd
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Huaian Pei Yuan Gene Technology Co Ltd
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Priority to CN201811304333.8A priority Critical patent/CN109481432A/en
Publication of CN109481432A publication Critical patent/CN109481432A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/01Hydrocarbons
    • A61K31/015Hydrocarbons carbocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/122Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic 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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

The invention discloses a kind of application of gweicurculactone in terms of gynecological neoplasm.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

A kind of application of gweicurculactone in terms of gynecological neoplasm
Technical field
The invention belongs to field of medicaments, are related to gynaecology, and in particular to a kind of gweicurculactone is in terms of gynecological neoplasm Application.
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 gweicurculactone in terms of gynecological neoplasm.
Above-mentioned purpose of the present invention is achieved through the following technical solutions:
A kind of application of gweicurculactone in the drug of preparation treatment gynecological tumor, the gynecological tumor be oophoroma or Cervical carcinoma.
It is auxiliary to be aided with pharmaceutically acceptable using gweicurculactone as active constituent for a kind of drug for treating gynecological tumor Material, is made pharmaceutically acceptable dosage form: the gynecological tumor is oophoroma or cervical carcinoma.
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 gweicurculactone in the drug of preparation treatment gynecological tumor, it is characterised in that: the gynecological tumor For oophoroma or cervical carcinoma.
2. a kind of drug for treating gynecological tumor, it is characterised in that: using gweicurculactone as active constituent, being aided with pharmaceutically can be with Pharmaceutically acceptable dosage form is made in the auxiliary material of receiving: the gynecological tumor is oophoroma or 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.
CN201811304333.8A 2018-11-04 2018-11-04 A kind of application of gweicurculactone in terms of gynecological neoplasm Withdrawn CN109481432A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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: 20190319

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