CN105919988A - Preparation and application thereof - Google Patents

Preparation and application thereof Download PDF

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Publication number
CN105919988A
CN105919988A CN201610314186.7A CN201610314186A CN105919988A CN 105919988 A CN105919988 A CN 105919988A CN 201610314186 A CN201610314186 A CN 201610314186A CN 105919988 A CN105919988 A CN 105919988A
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CN
China
Prior art keywords
preparation
gallic acid
present
cell
oral
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201610314186.7A
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Chinese (zh)
Inventor
黄林芳
杨贤英
连增林
汤晓飞
陈士林
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Institute of Medicinal Plant Development of CAMS and PUMC
Original Assignee
Institute of Medicinal Plant Development of CAMS and PUMC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Institute of Medicinal Plant Development of CAMS and PUMC filed Critical Institute of Medicinal Plant Development of CAMS and PUMC
Priority to CN201610314186.7A priority Critical patent/CN105919988A/en
Publication of CN105919988A publication Critical patent/CN105919988A/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 

Abstract

The invention relates to a preparation and an application thereof. The preparation is gallic acid or a mixture containing the gallic acid or a compound having a gallic acid activity, and the molecular formula of the preparation is shown as (OH)3C6H2COOH.H2O. The preparation disclosed by the invention is suitable for inhibiting the growth of oral carcinoma cells, so that the preparation can be further used for treating oral carcinoma and improving an effect on treating the v. the preparation disclosed by the invention provides experimental data to the research and development of new drugs for treating the oral carcinoma in the clinical field; and the preparation is applicable to the inhabitation of the growth of the oral carcinoma cells.

Description

A kind of preparation and application thereof
Technical field
The present invention relates to antitumor research and development field, particularly relate to a kind of preparation and application thereof.
Background technology
Oral cancer is to occur at the general name of the malignant tumor in oral cavity, and major part belongs to squamous cell cancer, so-called glutinous Film morphs.Oral cancer is one of incidence malignant tumor more typically.Oral cancer is common with male.In oral cancer case, Most common with tongue movable part cancer, it is secondly carcinoma of buccal mucosa.Generally pathological changes further away from lip near oropharynx or center line, Tumor Differentiation journey Spending the lowest, rate of lymph-node metastasis is the highest.The mucosa differential diagnosis of diseases of getting up early is only the shallow tuberosity of table or shallow ulcer, can be with slightly Pain.Advanced lesions generally invade to lower section muscle or bone causes organ to fix and language, dysphagia.Lymph node Transfer mostly is under the jaw of homonymy, the upper and lower neck of digastric or middle lymphonodi cervicales.Exceed the pathological changes meeting of center line at the bottom of oral cavity, the tip of the tongue or mouth Occur that contralateral lymph is carried down shifting.Varying in size of tumor, its rate of transform is the most different.Getting up early pathological changes (T1) is 10-20%, and mid-term is sick Becoming (T2) is 25-30%, and advanced lesions (T3, T4) is 50-70%.Metastasis below cervical region seldom occurs.
At present, the therapeutic modality of oral cancer is divided into: excision, radiation cure, chemotherapy.Oral cancer in early days is such as Have no that cervical lymph shifts, be then used alone operation or radiotherapy all has good treatment effect.The oral cancer of middle and advanced stage, relatively It is suitable for making surgically to merge postoperative and radiation cure.But excision, radiation cure, chemotherapy are the most each deposited In different side reactions.
Summary of the invention
In view of current technology above shortcomings, the present invention provides a kind of preparation and application thereof, the preparation of the present invention, answers For suppressing oral cancer growth of tumour cell, further apply treatment oral cancer, improve the therapeutic effect of oral cancer, the present invention Research and development for clinical treatment oral cancer new drug provide experimental basis, can be applicable to suppress in the suppression that cancer cell of oral cavity grows.
The present invention adopts the following technical scheme that
A kind of preparation, described preparation is gallic acid or the mixture containing gallic acid or contains the chemical combination that gallic acid is active Thing.
As the preferred technical solution of the present invention, described preparation is gallic acid, and structural formula is: , molecular formula is: (OH)3C6H2COOH.H2O。
As the preferred technical solution of the present invention, described preparation is carrier pharmaceutically or diluent.
As the preferred technical solution of the present invention, described preparation be tablet, coated tablet, capsule, injection, solution, emulsion, Ointment, emulsifiable paste, inhalant, aerosol or suppository.
The other one side of the present invention, the purposes of a kind of preparation, described preparation is gallic acid or mixing containing gallic acid Compound or the compound containing gallic acid activity.
As the preferred technical solution of the present invention, apply in tumour medicine.
As the preferred technical solution of the present invention, it is applied to suppress oral cancer growth of tumour cell.
As the preferred technical solution of the present invention, it is applied to treat oral cancer.
A kind of preparation of the present invention and application thereof, wherein, described preparation is gallic acid or the mixing containing gallic acid Thing or the compound containing gallic acid activity, molecular formula is: (OH)3C6H2COOH.H2O, the preparation of the present invention, it is applied to press down Donsole chamber cancerous protuberance tumor cell growth, further applies treatment oral cancer, improves the therapeutic effect of oral cancer, and the present invention is clinical The research and development for the treatment of oral cancer new drug provide experimental basis, can be applicable to suppress in the suppression that cancer cell of oral cavity grows.
Accompanying drawing explanation
For the technical scheme being illustrated more clearly that in the embodiment of the present invention, below by use required in embodiment Accompanying drawing is briefly described, it should be apparent that, the accompanying drawing in describing below is only some embodiments of the present invention, for ability From the point of view of the those of ordinary skill of territory, on the premise of not paying creative work, it is also possible to obtain the attached of other according to these accompanying drawings Figure.
Fig. 1 is the preparation of the present invention inhibitory action schematic diagram to oral cavity intraepithelial neoplasia cells DOK.
Fig. 2 is the inhibitory action schematic diagram of the preparation oral cavity squamous cell carcinoma cell CAL-27 of the present invention.
Fig. 3 is the inhibitory action schematic diagram of the preparation oral cavity squamous cell carcinoma cell SCC-15 of the present invention.
Detailed description of the invention
Below in conjunction with the accompanying drawing in the embodiment of the present invention, the technical scheme in the embodiment of the present invention is carried out clear, complete Describe, it is clear that described embodiment is only a part of embodiment of the present invention rather than whole embodiments wholely.Based on Embodiment in the present invention, it is every other that those of ordinary skill in the art are obtained under not making creative work premise Embodiment, broadly falls into the scope of protection of the invention.
The present invention provides a kind of preparation, and preparation is gallic acid or the mixture containing gallic acid or contains gallic acid The compound of activity, say, that said preparation can be single material, it is also possible to for the mixture containing gallic acid, and Can also is that the compound containing gallic acid activity, wherein the concrete molecular formula of gallic acid is: (OH)3C6H2COOH.H2O, The entitled Gallic Acid of chemistry, the numbered 5995-86-8 of CAS;Outward appearance is white powder, molecular weight 188.13, knot Structure formula is:.Wherein configuration and the storage method of gallic acid solution is: by former for gallic acid medicine It is dissolved in DMSO, is made into 40mg/ml and stores liquid, be stored in-20 DEG C of refrigerators.
In the present invention, said preparation can be tablet, coated tablet, capsule, injection, solution, emulsion, ointment, emulsifiable paste, suction Enter agent, aerosol or suppository.
The another side of the present invention, the purposes of a kind of preparation, the preparation during wherein said preparation is the present invention, namely Galla Chinensis Acid or containing gallic acid activity mixture or containing gallic acid activity compound.
In the present invention, said preparation can be applied in tumour medicine, and is applied to suppress oral cancer tumor cell raw Long, can apply to further treat oral cancer, specifically by the shadow of mtt assay detection gallic acid oral cancer cell propagation Ringing, Cleaning Principle is that the succinate dehydrogenase in living cells mitochondrion can make exogenous MTT be reduced to water-insoluble bluish violet Crystallization first a ceremonial jade-ladle, used in libation is also deposited in cell, and dead cell is without this function.Dimethyl sulfoxide (DMSO) can dissolve the first a ceremonial jade-ladle, used in libation in cell, uses Microplate reader measures its absorbance value at 490nm wavelength, in the range of certain cell number, and the amount of MTT crystallization formation and cell number It is directly proportional.Absorbance (OD value) according to recording seeks calculation suppression ratio, judges living cells quantity.
Further, with complete culture solution by storage liquid be diluted to concentration be 25 μ g/ml, 50 μ g/ml, five times of 100 μ g/ml Sub-acid is respectively acting on oral precancerous lesion cell DOK, cancer cell of oral cavity SCC-15, cancer cell of oral cavity CAL-27.Detect respectively The above-mentioned three strain cell of gallic acid effect 24 hours, 48 hours, the effect of cell proliferation after 72 hours, result display Galla Chinensis Acid is respectively provided with certain inhibitory action to the propagation of above-mentioned three strain cells.
In the present invention, the present invention has expanded gallic application approach, for being applied to gallic acid suppress oral cancer Growth of tumour cell so that it is can further apply treatment oral cancer, improves the therapeutic effect of oral cancer.The present invention is to this chemical combination The scope of the application of thing includes the growth inhibited for cancer cell of oral cavity, and then the propagation of suppression tumor, thus delays tumor Deteriorate.Meanwhile, in the medical constituent being also used for Galla Chinensis in the present invention suppressing cancer cell of oral cavity to grow, it is also possible to include The carrier of pharmaceutical acceptable.Carrier can be excipient, filler, binding agent, diluent, disintegrating agent, absorption enhancer or sweet Taste agent, but and for being only limitted to this.Pharmaceutical preparation of the present invention can be manufactured according to the preparation method of general medicine, by gallic acid Combining with more than one carrier, this dosage form can include lozenge, powder, granule, capsule or other preparations, but not as Limit.
In the present invention, to be illustrated, the preparation sole active agent of the present invention is gallic acid, in other words The present invention uses single material to reach to suppress oral cancer growth of tumour cell, treats oral cancer further, improves oral cancer Therapeutic effect, research and development that the present invention is clinical treatment oral cancer new drug provide experimental basis, can be applicable to suppress oral cancer thin In the suppression of intracellular growth.
A specific embodiment presented below is expanded on further the present invention.
Embodiment 1
As shown in Figure 1-Figure 3, the preparation of the present invention is used to be respectively acting on oral precancerous lesion cell DOK, cancer cell of oral cavity SCC-15, the situation of cancer cell of oral cavity CAL-27, specific as follows:
Experiment material: oral precancerous lesion cell DOK, oral squamous cell carcinoma SCC-15 and cancer cell of oral cavity CAL-27 tri-strain, Gallic acid storing solution, MTT, hyclone, DMEM, DMEM-F12, trypsin, DMSO, 96 orifice plates, integrated enzyme reaction labelling Instrument, micropore concussion instrument, inverted microscope.
Dental clinic SCC-15 is incubated at DMEM-F12: hyclone: the dual anti-culture medium for 89:10:1, is placed in 5%CO2, the saturated humidity incubator of 37 DEG C is cultivated.Cell ferrum wall grows, and within 2-3 days, passes on.Oral precancerous lesion cell DOK, mouth Chamber squamous cell carcinoma CAL-27 is incubated at DMEM: hyclone: the dual anti-culture medium for 89:10:1, is placed in 5%CO2, 37 DEG C Saturated humidity incubator is cultivated.Cell ferrum wall grows, and within 2-3 days, passes on.
Concretely comprise the following steps: the trophophase Dental clinic SCC-15 that takes the logarithm, oral precancerous lesion cell DOK and people's tongue squama Shape cell CAL-27 tri-strain, after trypsinization, receives suspension, centrifugal (1100r, 4min), abandons supernatant, add culture medium cell After counting, being diluted to concentration is 5 × 104Individual/ml, adds 96 orifice plates, every hole 100ul.After cultivation overnight, remove original fluid, real Test group add Chinese medicine extract final concentration of 100ug/ml, 50ug/ml, 25ug/ml culture fluid, matched group add containing with experiment Organize same amount of solvent (DMSO).Remove original fluid after acting on 24h, 48h, 72h respectively, add 10ul MTT reagent, 37 degree of incubators Take out after 4h and remove supernatant, add 100ul DMSO and after concussion 15nim, exist with integrated enzyme reaction marking appliance on micropore concussion instrument Wavelength is that 490nm surveys absorbance (OD value), and record result obtains proliferation inhibition rate, as Figure 1-3.
From Fig. 1-Fig. 3, it can be seen that gallic acid is respectively provided with certain suppression and makees the propagation of above-mentioned three strain cells With.
The above, the only detailed description of the invention of the present invention, but protection scope of the present invention is not limited thereto, and any Those skilled in the art in technical scope disclosed by the invention, the change that can readily occur in or replacement, all answer Contain within protection scope of the present invention.Therefore, protection scope of the present invention should be with described scope of the claims Accurate.

Claims (8)

1. a preparation, it is characterised in that described preparation is gallic acid or the mixture containing gallic acid or contains five times The compound of sub-acid activity.
A kind of preparation the most according to claim 1, it is characterised in that described preparation is gallic acid, and structural formula is:, molecular formula is: (OH)3C6H2COOH.H2O。
A kind of preparation the most according to claim 1, it is characterised in that described preparation is carrier pharmaceutically or diluent.
4. according to the arbitrary described a kind of preparation of claim 1-3, it is characterised in that described preparation is tablet, coated tablet, glue Capsule, injection, solution, emulsion, ointment, emulsifiable paste, inhalant, aerosol or suppository.
5. the purposes of a preparation, it is characterised in that described preparation is gallic acid or the mixture containing gallic acid or contains There is the compound of gallic acid activity.
The purposes of a kind of preparation the most according to claim 5, it is characterised in that apply in tumour medicine.
The purposes of a kind of preparation the most according to claim 5, it is characterised in that be applied to suppress oral cancer tumor cell raw Long.
The purposes of a kind of preparation the most according to claim 5, it is characterised in that be applied to treat oral cancer.
CN201610314186.7A 2016-05-13 2016-05-13 Preparation and application thereof Pending CN105919988A (en)

Priority Applications (1)

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CN201610314186.7A CN105919988A (en) 2016-05-13 2016-05-13 Preparation and application thereof

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Application Number Priority Date Filing Date Title
CN201610314186.7A CN105919988A (en) 2016-05-13 2016-05-13 Preparation and application thereof

Publications (1)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1559392A (en) * 2004-03-10 2005-01-05 牛凤兰 Applicaton of gallic acid in prepn. of medicine for antitumor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1559392A (en) * 2004-03-10 2005-01-05 牛凤兰 Applicaton of gallic acid in prepn. of medicine for antitumor

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
CHAO-LIN KUO ET AL.: "Gallic acid inhibits migration and invasion of SCC-4 human oral cancer through actions of NF-κB, Ras and matrix metalloproteinase-2 and -9", 《ONCOLOGY REPORTS》 *
HIDEYUKI ITO ET AL.: "Polyphenols from Eriobotrya japonica and Their Cytotoxicity against Human Oral Tumor Cell Lines", 《 CHEM. PHARM. BULL.》 *
汤晓飞等: "Nrf2和NF-κB在口腔癌和癌前病变细胞中的表达及意义", 《北京口腔医学》 *

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Application publication date: 20160907

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