CN106692165A - Combined medicine for up-regulating PTEN gene expression to inhibit lung cancer cell growth - Google Patents
Combined medicine for up-regulating PTEN gene expression to inhibit lung cancer cell growth Download PDFInfo
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- CN106692165A CN106692165A CN201611266814.5A CN201611266814A CN106692165A CN 106692165 A CN106692165 A CN 106692165A CN 201611266814 A CN201611266814 A CN 201611266814A CN 106692165 A CN106692165 A CN 106692165A
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- China
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- preparation
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- lung cancer
- ergosterol
- gene expression
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
- A61K31/585—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
Abstract
The invention provides a combined medicine for up-regulating PTEN gene expression to inhibit lung cancer cell growth. The composition comprises, by weight, 20-35% of ergosterol peroxide and 65-80% of triptolide. The invention also provides a preparation adopting the combined medicine as an active component, and an application of the preparation in the preparation of lung cancer treatment medicines. The combined medicine and the preparation up-regulate the expression of a PTEN protein and PTEN mRNA, have a good tumor inhibition rate, and have good application prospect.
Description
Technical field
The invention belongs to pharmaceutical technology field, and in particular to a kind of PTEN gene expression inhibition lung cancer cell growths heightened
Composition of medicine.
Background technology
Lung cancer is one of common cancer, and current therapeutic scheme is mainly chemotherapy.But, existing available medicine is not
It is many, the predominantly common cancer therapy drug such as cis-platinum.There is researcher to attempt being treated using Chinese medicine, but the effect of gained is not very
It is good.
PTEN is first while having the tumor suppressor gene of lipid and albumen dual specificity phosphatase enzymatic activity concurrently, in 1997 from
Mankind's 10q23.3 chromosomal focis are separated and obtained, and be may participate in cell cycle regulating and are suppressed tumor cell proliferation and promotion
Apoptosis of tumor cells.When studying new cancer therapy drug, whether the expression that can heighten PTEN with it is carried out.
The content of the invention
It is an object of the invention to provide a kind of composition of medicine for heightening PTEN gene expression inhibition lung cancer cell growths, should
Composition is made up of following component by weight percentage：20-35 % ergosterol peroxides, 65-80 % triptolides.
The present invention can significantly raise the expression of PTEN.It is a discovery of the invention that when exclusive use ergosterol peroxide
Or during triptolide, influence is nearly free from the expression of PTEN.In addition, when the addition of ergosterol is very few, also not
Produce more obvious rise effect.
Preferably, the composition is made up of following component by weight percentage：25-30 % ergosterol peroxides,
70-75 % triptolides.
Used as optimal case, the composition is made up of following component by weight percentage：26 % ergosterol peroxidating
Thing, 74 % triptolides.
The present invention also aims to provide by above-mentioned composition as active component preparation, the preparation be pharmacy meaning
Acceptable any preparation in justice.
Preferably, the preparation is injection.
The preparation also includes assistant agent, and the assistant agent is acceptable any assistant agent in pharmacy meaning.
Preferably, the assistant agent is ethylene glycol.
The present invention also aims to provide the application of above-mentioned composition or preparation in terms for the treatment of lung-cancer medicament is prepared.
Beneficial effects of the present invention：
The present invention can heighten the expression of pten protein and PTEN mRNA, can produce good tumour inhibiting rate, with preferably application
Prospect.
Specific embodiment
The present invention is specifically described below by embodiment, it is necessary to it is pointed out here that be that following examples are use
It is further detailed in the present invention, it is impossible to be interpreted as limiting the scope of the invention, the field is skilled in technique
Personnel still fall within protection scope of the present invention according to some nonessential modifications and adaptations that foregoing invention content is made.
Embodiment 1
Pharmaceutical composition is prepared, by weight percentage, subordinate's component is mixed：
20-35 % ergosterol peroxides, 65-80 % triptolides.
Gained mixture is pressed 10%（W/W）Add in physiological saline, add 5%（W/W）Ethylene glycol.
Embodiment 1
Pharmaceutical composition is prepared, by weight percentage, subordinate's component is mixed：
20-35 % ergosterol peroxides, 65-80 % triptolides.
Gained mixture is pressed 10%（W/W）Add in physiological saline, add 5%（W/W）Ethylene glycol.
Embodiment 2
Pharmaceutical composition is prepared, by weight percentage, subordinate's component is mixed：
20-35 % ergosterol peroxides, 65-80 % triptolides.
Gained mixture is pressed 10%（W/W）Add in physiological saline, add 5%（W/W）Ethylene glycol.
Embodiment 3
Pharmaceutical composition is prepared, by weight percentage, subordinate's component is mixed：
20-35 % ergosterol peroxides, 65-80 % triptolides.
Gained mixture is pressed 10%（W/W）Add in physiological saline, add 5%（W/W）Ethylene glycol.
Embodiment 4
Pharmaceutical composition is prepared, by weight percentage, subordinate's component is mixed：
20-35 % ergosterol peroxides, 65-80 % triptolides.
Gained mixture is pressed 10%（W/W）Add in physiological saline, add 5%（W/W）Ethylene glycol.
Comparative example 1
Pharmaceutical composition is prepared, by weight percentage, subordinate's component is mixed：
15 % ergosterol peroxides, 85 % triptolides.
Gained mixture is pressed 10%（W/W）Add in physiological saline, add 5%（W/W）Ethylene glycol.
Comparative example 2
Triptolide is pressed 10%（W/W）Add in physiological saline, add 5%（W/W）Ethylene glycol.
Experimental example
Take the logarithm growth period Lewis lung carcinoma cell, cell is collected by centrifugation after pancreatin digestion（1 800r/min is centrifuged 5min）, with nothing
The resuspended washing of serum DMEM culture mediums simultaneously adjusts cell concentration for 1 × 107Individual/mL, cell suspension is drawn with 1mL syringes
0.2mL（Containing cell number
2×106It is individual）It is injected in C57BL/6 mouse left side armpit subcutaneous, sets up mouse subcutaneous transplanting knurl animal model.
After inoculation 10d, detection mouse is divided into experimental group and control group, respectively by satisfactory into warty condition into knurl mouse
Group is being inoculated with after 10d administration on an empty stomach from morning.1. control group：The sodium chloride solution gavage 10d of 0.2mL/10g 0.9%, and exist respectively
1st, 3,5 days sodium chloride solution 0.4mL of intraperitoneal injection 0.9%；2. experimental group（Embodiment 1-4, comparative example 1 and contrast are implemented
Example 2）：The sodium chloride solution gavage 10d of 0.2mL/10g 0.9%, and respectively in the 1st, 3,5 days intraperitoneal injection 0.4mL；Weigh knurl matter
Amount, calculates tumour inhibiting rate and the 11st day execution mouse is administered, and completely strips armpit hypodermic tumour tissue, and precision electronic balance is weighed, point
Ji Suan not each group tumour inhibiting rate, tumour inhibiting rate（%）=（The average average knurl matter of knurl quality/control group of the average knurl quality-experimental group of control group
Amount）×100%.
Western blot methods detection tumor tissues pten protein expression clip tumor tissues about 0.1g, adds RIPA thin
Cellular lysate liquid 1mL（Include 1mmol/L PMSF）Cracked, tissue total protein sample is collected by centrifugation.Through PAGE gel electricity
Swimming separates protein component, will
Albumen is needed on pvdf membrane, 5% skimmed milk power closing 2h, adds primary antibody（PTEN：500 times of dilutions）4 DEG C of overnight incubations,
Add the secondary antibody of HRP marks（1: 10 000 dilution proportion）, room temperature closing 2h, washes clean, ECL colour developing after exposure simultaneously
With Image J software analysis results.Tumor tissues 0.1g liquid nitrogen grindings are weighed, adds 1mL Trizol to extract total serum IgE.According to
RevertAidTMFirst Strand cDNA Synthesis Kit kits reverse transcriptions into cDNA, using this cDNA as fluorescence
Quantitative templates, are expanded according to specific reaction system and reaction condition, and primer sequence is the-TTT of Forward primer 5 '
- GCT TTT ACCTAG GGG GCA the AG-3 ' of GGT CAC CCTTTG AGT CC-3 ', Reverse primer 5 ', with β-
Used as internal reference, RelativeQuantification Study are analysis method to actin, and final calculating takes 2-△△Ct。
Experimental result is as shown in Table 1 and Table 2.
The tumour inhibiting rate of table 1
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Comparative example 1 | Comparative example 2 | |
| Tumour inhibiting rate（%） | 66.1 | 59.4 | 62.2 | 68.4 | 9.7 | 5.5 |
The pten protein of table 2, the expression of PTEN mRNA
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Comparative example 1 | Comparative example 2 | Control group | |
| Pten protein | 1.83 | 1.77 | 1.80 | 1.99 | 0.25 | 0.25 | 0.22 |
| PTEN mRNA | 3.44 | 3.01 | 3.39 | 3.56 | 1.13 | 1.10 | 1.06 |
Claims (8)
1. a kind of composition of medicine for heightening PTEN gene expression inhibition lung cancer cell growths, it is characterised in that the composition is pressed
Percentage by weight is made up of following component：20-35 % ergosterol peroxides, 65-80 % triptolides.
2. composition according to claim 1, it is characterised in that the composition is by weight percentage by following component group
Into：25-30 % ergosterol peroxides, 70-75 % triptolides.
3. composition according to claim 1, it is characterised in that the composition is by weight percentage by following component group
Into：26 % ergosterol peroxides, 74 % triptolides.
4. the preparation with claim 1-3 any one pharmaceutical compositions as active component, it is characterised in that the preparation is pharmacy
Acceptable any preparation in meaning.
5. preparation according to claim 4, it is characterised in that the preparation is injection.
6. the preparation according to claim 4 or 5, it is characterised in that the preparation also includes assistant agent, the assistant agent is pharmacy
Acceptable any assistant agent in meaning.
7. preparation according to claim 6, it is characterised in that the assistant agent is ethylene glycol.
8. composition described in any one of claim 1-3 or preparation described in claim any one of 4-7 are preparing treatment lung cancer side
The application of face medicine.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611266814.5A CN106692165A (en) | 2016-12-31 | 2016-12-31 | Combined medicine for up-regulating PTEN gene expression to inhibit lung cancer cell growth |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201611266814.5A CN106692165A (en) | 2016-12-31 | 2016-12-31 | Combined medicine for up-regulating PTEN gene expression to inhibit lung cancer cell growth |
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| CN201611266814.5A Pending CN106692165A (en) | 2016-12-31 | 2016-12-31 | Combined medicine for up-regulating PTEN gene expression to inhibit lung cancer cell growth |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106798913A (en) * | 2017-03-13 | 2017-06-06 | 成都育芽科技有限公司 | A kind of preparation method for heightening the polypeptide complex of PTEN gene expressions |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101708193A (en) * | 2009-01-15 | 2010-05-19 | 江西中医学院 | Pharmaceutical composition of triptolide-containing medicine and bracken and preparation and application thereof |
| CN103393598A (en) * | 2013-08-06 | 2013-11-20 | 南京中医药大学 | Triptolide liposome preparation for treatment of small cell lung cancer and preparation method thereof |
-
2016
- 2016-12-31 CN CN201611266814.5A patent/CN106692165A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101708193A (en) * | 2009-01-15 | 2010-05-19 | 江西中医学院 | Pharmaceutical composition of triptolide-containing medicine and bracken and preparation and application thereof |
| CN103393598A (en) * | 2013-08-06 | 2013-11-20 | 南京中医药大学 | Triptolide liposome preparation for treatment of small cell lung cancer and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 宋明杰 等: "椭圆嗜蓝孢孔菌中四种甾类化合物的抗肿瘤活性及构效关系分析", 《菌物学报》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106798913A (en) * | 2017-03-13 | 2017-06-06 | 成都育芽科技有限公司 | A kind of preparation method for heightening the polypeptide complex of PTEN gene expressions |
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Application publication date: 20170524 |