CN105267267A - Applications of L-cysteine composition in prevention, removal (or elimination) of carcinogenic factor acetaldehyde generated during smoking and drinking - Google Patents

Applications of L-cysteine composition in prevention, removal (or elimination) of carcinogenic factor acetaldehyde generated during smoking and drinking Download PDF

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Publication number
CN105267267A
CN105267267A CN201410244419.1A CN201410244419A CN105267267A CN 105267267 A CN105267267 A CN 105267267A CN 201410244419 A CN201410244419 A CN 201410244419A CN 105267267 A CN105267267 A CN 105267267A
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pharmaceutical composition
acetaldehyde
cys
cell
drinking
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和光学
许绍衡
柴琳
和萧远
李静宜
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Abstract

The present invention relates to applications of L-cysteine and a composition thereof in prevention, removal (or elimination) of a carcinogenic factor acetaldehyde generated during smoking and drinking, and particular relates to a carcinogenic substance acetaldehyde entering human body through digestive tract and respiratory tract, and applications in prevention of occurrence of upper respiratory tract and upper digestive tract cancers of people with smoking, drinking and unhealthy food habits, and in drugs and medical devices, wherein L-cysteine is respectively subjected to compatibility with a ginkgo leaf extract, ginseng, procyanidin, trace elements and the like, and the obtained material and a pharmaceutically acceptable excipient are combined into the pharmaceutical preparation and the medical device thereof.

Description

Cys compositions preventing, the application of carcinogenic factor acetaldehyde of removing (or eliminate) smoking, producing when drinking
Technical field:
The present invention relates to Cys pharmaceutical composition smoking, drink time produce upper respiratory tract, upper digestive tract acetaldehyde carcinogenic in application, belong to the technical field of medicine.
Background technology:
Cancer is the formidable enemy threatening human health longevity, will seize the life of tens of millions of people every year, now prove, the cancer that upper respiratory tract, upper digestive tract occur becomes positive correlation addicted to cigarette, long-time excessive consumption of alcohol repeatedly with Bad Eating Habit with the mankind's.In October, 2009, international cancer research institution announces: acetaldehyde is a class carcinogen, is present in a large number in Nicotiana tabacum L., pick-me-up.According to estimates, all caused by smoking and drinking up to the oral cavity of 80%, pharynx and the esophageal carcinoma in developed country.The research worker of Finland is pointed out, this kind of Lesions in Upper Gastrointestinal Tract popular in drink and smoking causes upper digestive tract to touch acetaldehyde, and at this moment carcinogenic factor is just seized the opportunity simultaneously and enters, and brings out the generation of cancer.
Cys is a kind of common aminoacid in organism, Chinese is referred to as again half aminoacid, is mainly used in the middle of cosmetic field and food industries at present, and main purpose uses as additive or modifying agent, and use in field of medicaments at present and limit to very much especially, be mainly used in eliminating the phlegm; Especially for treatment bronchitis and the effect of reducing phlegm.Data show; contact with acetaldehyde and the cancer of bringing out occupy 40% ratio; the medicine that a kind of novel, effective elimination of R and D is carcinogenic is for this reason current problem demanding prompt solution; to a large amount of smoking, drink and the upper respiratory tract of crowd of bad habit, upper gastrointestinal cancer bring Gospel; while removal carcinogen acetaldehyde; also can receive protection liver, kidney; reduce blood fat; the release of blood circulation promoting and NO (nitric oxide), plays a significant role in immunoprotection.Reduce simultaneously and reduce the infringement of cancer to the mankind, save a large amount of resource medicine, protection human health.
Summary of the invention:
The object of the invention is to be used by drug regimen, solve the class carcinogen acetaldehyde removed and entered human body by digestive tract, respiratory tract.Prevention and smoking, drink and the upper respiratory tract of crowd of Bad Eating Habit, the generation of upper gastrointestinal cancer.
In order to solve the above problems, the present invention adopts following technical scheme:
The present invention relates to a kind of Cys pharmaceutical composition to be combined by one or more in active component Cys and Folium Ginkgo extract, Radix Ginseng, procyanidin Lac regis apis, trace element and make;
Above-mentioned Cys pharmaceutical composition, its active component optical isomer, pharmaceutical salts and hydrate;
Above-mentioned Cys pharmaceutical composition, its active component is according to parts by weight: other active component containing the Cys of 5 ~ 100 parts and 10 ~ 200 parts; One or more preferably in 10 parts of Cys and 30 parts of Folium Ginkgo extract, Radix Ginseng, procyanidin Lac regis apis, trace element of its active component combine and form.
Above-mentioned Cys pharmaceutical composition, pharmaceutical composition can make medically pharmaceutical preparation and medical apparatus and instruments thereof.
Above-mentioned Cys pharmaceutical composition, this pharmaceutical composition is used in preventing, remove smoking, the application of the aspect that upper respiratory tract, upper digestive tract acetaldehyde are carcinogenic when drinking.
One or more combinations that the applicant has carried out in Cys and Folium Ginkgo extract, L-arginine, Radix Ginseng, procyanidin, trace element have carried out pharmacodynamic experiment research, respectively to set forth the beneficial effect of pharmaceutical composition provided by the invention further.
One pharmaceutical composition proportioning screening experiment
Inventor has carried out compatibility by the Cys pharmaceutical composition of different prescription, following experimental program has been formulated by orthogonal experiment: and by pharmaceutical composition to the eliminating effect of acetaldehyde and to A549 intracellular environment antioxidative influence research, again demonstrate following drug regimen and there is good curative effect.
1.1 concrete drug component proportioning compositions A 1~ G 1
Table 1 drug component proportioning compositions A 1~ G 1group
More than select proportioning, "+" represents proportioning, and "-" represents not proportioning, and proved by " pharmaceutical composition is to the research of acetaldehyde eliminating effect " pharmacological evaluation, said medicine compatible composition has significant protective effect to the A549 cell injury that acetaldehyde is induced.
1.2 concrete pharmaceutical units proportioning compositions A 2~ G 2medicine
Table 2 pharmaceutical units proportioning compositions A 2~ G 2medicine
More than select proportioning, proved by " compositions is to the research of acetaldehyde eliminating effect " pharmacological evaluation, above-mentioned active ingredient unit proportioning compositions has significant protective effect to the A549 cell injury that acetaldehyde is induced.Wherein pharmacological research shows, wherein proportioning adopts active component I10 part and active component II30 part successful, and wherein active component II compatibility selects B 2effect is better.
Two pharmaceutical compositions are to the research of acetaldehyde eliminating effect
1.1 materials, reagent and instrument
Non-small Cell Lung Cancer A 549 is provided by Lung Cancer in Tianjin institute.Acetaldehyde (content 40%), pharmaceutical composition (A 2~ G 2), RPMI-1640 culture medium, hyclone, mycillin mixed liquor (100 ×), trypsin, tetrazolium bromide (MTT), dimethyl sulfoxide (DMSO), PBS buffer, determination of lactate dehydrogenase test kit, determination of nitric oxide test kit, BCA method measure ultramicron protein content test kit, superoxide dismutase measures test kit Nanjing and builds up Bioengineering Research Institute.Heraeus Inc. of HERAcell150 CO2 gas incubator Germany; BDS200-PH inverted biological microscope Chongqing Ao Te optical instrument company; The MultiskanSpectrum all-wave long microplate reader Shanghai vigorous biological company limited of thunder.
1.2 cell culture
By A549 cell culture in 1640 culture medium containing 10% hyclone, mycillin mixed liquor (1 ×), in 37 DEG C, saturated humidity, to cultivate under 5%CO2 condition, change liquid 1 time according to cell growth state every 2 ~ 3d.After cell covers with 80%, cell is digested for Secondary Culture or for experiment.
1.3MTT method detects cells growth activity
With 1640 culture medium diluting cells to the 6 × 104/mL containing 10% hyclone, and be seeded to 96 well culture plates, every hole adds 100L cell suspension, and (blank well does not add cell, only add culture medium) cultivate 24h, treat that cell covers with about 80%, change serum-free medium into continue to cultivate 24h, make cell synchronization; Then pharmaceutical composition (A is added respectively 2~ G 2), the process such as acetaldehyde factor, each dosage repeats 6 holes, puts in incubator after hatching 24h and detects.Supernatant 20L is abandoned in suction, it is 5mg/mLMTT (whole mass concentration is 0.5mg/mL) that every hole adds 20L mass concentration, culture medium is abandoned after continuing to hatch 4h, every hole adds 150LDMSO cessation reaction, lucifuge low speed jolting 10min makes darkviolet resolution of precipitate, OD value is measured, experiment repetition 3 times in microplate reader wavelength 570nm place.
1.4 cell conditioned medium liquid LDH activity measure
With 1640 culture medium diluting cells to the 6 × 104/mL of 10% hyclone, cell is seeded in 24 orifice plates, every hole adds cell suspension 1mL, put 5%CO2 incubator, cultivate 24h for 37 DEG C, cover with after culture plate until cell attachment, the culture fluid cultivation 24h used instead containing serum-free makes cell synchronization.Add different disposal factor subsequently to continue to cultivate 24h, often organize cultivation 3 porocyte.Cultivate after stopping, the centrifugal 3min of 3000r/min, careful Aspirate supernatant, measure LDH vigor by test kit description, experiment repetition 3 times.
NO determination of activity in 1.5 cell conditioned medium liquid
Cell is made the cell suspension that density is 6 × 104/mL, be seeded in 24 well culture plates and cultivate, when cell covers with 80%, press packet transaction above, often group establishes 3 multiple holes.Supernatant 100L is got in every hole, builds up Bioengineering Research Institute's test kit requirement measure NO content according to Nanjing, experiment repetition 3 times.
SOD vitality test in 1.6 cells
Cell is made the cell suspension that density is 6 × 104/mL, be seeded in 24 well culture plates and cultivate, when cell covers with 80%, press packet transaction above, often group establishes 3 multiple holes.After stopping cultivation, add cell pyrolysis liquid, the centrifugal 15min of 4 DEG C of cracking 30min, 12000r/min, get supernatant BCA method and measure protein concentration, build up Bioengineering Research Institute's test kit requirement according to Nanjing simultaneously and measure SOD vigor.Experiment repetition 3 times.
1.7 statistical analysis
The data of this experiment represent with x ± s, adopt t inspection to carry out statistical analysis to each group of variability.Statistical significance is indicated with P < 0.05.
2 results and analysis
2.1 acetaldehyde and pharmaceutical composition (A 2~ G 2) the influence research result of A549 cells growth activity is shown, along with acetaldehyde concentration increases, the growth activity of A549 cell obviously declines, wherein 200,300, the acetaldehyde group of 900mol/L compares with blank group, its difference has statistical significance (P < 0.05).Pharmaceutical composition (A 2~ G 2) in scope, its concentration and A549 cells growth activity are proportionate, and show pharmaceutical composition (A in this concentration range 2~ G 2) protective effect of concentration to impaired A549 cell is concentration dependent, and B 2compare with blank group, its difference has statistical significance (P < 0.05); But as pharmaceutical composition (A 2~ G 2) be greater than A 2~ G 2time, cell viability declines to some extent, shows too high pharmaceutical composition (A 2~ G 2) be unfavorable for its protective effect to A549 cell.
2.2 acetaldehyde are to A549 cell and pharmaceutical composition (A 2~ G 2) the influence research result of LDH activity in acetaldehyde damage A549 cell conditioned medium liquid is shown, along with acetaldehyde concentration increases, in A549 cell conditioned medium liquid, LDH vigor strengthens, wherein 200,300, the acetaldehyde group of 900mol/L compares with blank group, its difference has statistical significance (P < 0.05).Pharmaceutical composition A 2~ G 2in scope, along with pharmaceutical composition (A 2~ G 2) consumption increase, in the A549 cell conditioned medium liquid after the effect of variable concentrations acetaldehyde, LDH vigor obviously declines, and as pharmaceutical composition B 2time, in the A549 cell conditioned medium liquid after the effect of variable concentrations acetaldehyde, LDH vigor compares with blank group, and its difference has statistical significance (P < 0.05).
2.3 acetaldehyde are to A549 cell and pharmaceutical composition (A 2~ G 2) the influence research result of N0 content in acetaldehyde damage A549 cell conditioned medium liquid is shown, along with acetaldehyde concentration increases, the NO content of A549 cell release is in rising trend, wherein 200,300, the acetaldehyde group of 900mol/L compares with blank group, its difference has statistical significance (P < 0.05).In pharmaceutical composition A 2~ G 2in scope, along with pharmaceutical composition A 2~ G 2concentration increases, and the NO content of the A549 cell release after the effect of variable concentrations acetaldehyde is on a declining curve, and as pharmaceutical composition B 2time, the NO content of the A549 cell release after the effect of variable concentrations acetaldehyde compares with blank group, and its difference has statistical significance (P < 0.05).
2.4 acetaldehyde are to A549 cell and pharmaceutical composition (A 2~ G 2) the influence research result of SOD activity in acetaldehyde damage A549 cell is shown, along with acetaldehyde concentration increases, SOD vigor is on a declining curve, wherein 200, the acetaldehyde group of 300mol/L and 900mol/L compares with blank group, and difference has statistical significance (P < 0.05).In pharmaceutical composition A 2~ G 2in scope, along with pharmaceutical composition (A 2~ G 2) proportioning increase, the A549 cell SOD vigor after the effect of variable concentrations acetaldehyde rises gradually, and as pharmaceutical composition B 2time, the A549 cell SOD vigor after the effect of variable concentrations acetaldehyde compares with blank group, and difference has statistical significance (P < 0.05).
3 discuss
Test by acetaldehyde cell growth active, acetaldehyde is inquired into the oxidative damage effect of A549 cell and pharmaceutical composition (A to the detection of LDH leakage, NO burst size and SOD vigor 2~ G 2) protective effect to it.Result of study shows, acetaldehyde has obvious damaging action to A549 cell, and presents concentration dependent; Increase with acetaldehyde concentration, LDH leakage and NO burst size increase gradually, reason may be acetaldehyde damaging cells film, LDH omission amount and induction NO burst size is caused to increase, increase with acetaldehyde concentration, total SOD vigor is on a declining curve, illustrates that higher concentration acetaldehyde can suppress the SOD of A549 cell active.Concomitant drugs compositions (A 2~ G 2) consumption increase, the A549 cell LDH leakage after variable concentrations acetaldehyde acts on simultaneously and NO burst size obviously decline, and SOD vigor rises gradually, and pharmaceutical composition (A is described 2~ G 2) to the A549 cell injury of acetaldehyde induction, there is significant protective effect, and at A 2~ G 2in scope, its protective effect is dose-effect relationship.What is more important B 2pharmaceutical composition all shows as the best protection concentration to A549 cell in all tests.
Three detailed description of the invention
The preparation of embodiment 1 sublingual lozenge
1, prescription:
2, get vinpocetine, L-arginine, Folium Ginkgo extract, hydroxypropyl emthylcellulose (E-50), hydroxypropyl emthylcellulose (E-4M), hydroxypropyl cellulose, micropowder silica gel, magnesium stearate to progressively increase method mix homogeneously with equivalent, be directly compressed into sublingual lozenge, obtain final product.
The preparation of embodiment 2 capsule
1, prescription:
2, prepare:
Get Radix Ginseng powder and be broken into fine powder, cross 80 orders, for subsequent use; By Radix Ginseng fine powder, Cys, L-arginine, mix homogeneously, adds procyanidin Lac regis apis granule, dry, then after adding magnesium stearate mix homogeneously, incapsulates, and to obtain final product.
The preparation of embodiment 3 medicine chewing gum
1, prescription:
2, prepare:
Raw material is eaten gum base and be heated to 80 ~ 120 DEG C, fully stir, then add edible plasticizer and wetting agent in a heated condition, mix homogeneously, adds the sweeting agent of sweeting agent total amount 60 ~ 70%, then add, filler, above material stirs, and stops heating; (2) after temperature is down to 60 DEG C, add Cys, L-arginine, olive oil residue sweeting agent stir; Gained express material, tabletting, cutting, molding and get final product.
The preparation of embodiment 4 cigarette holder
Gets Cys, L-arginine adds in the middle of 30ml microemulsion and adsorb, then get four micropore filter discs respectively and adhere to, compacting, then the micropore filter disc this being loaded with medicine is used in the middle of the cigarette holder of production of cigarettes.

Claims (6)

1. a Cys pharmaceutical composition, is characterized in that described pharmaceutical composition is formed by following two kinds of active component and pharmaceutically acceptable excipient:
Composition 1:L-cysteine;
Composition II: one or more in Folium Ginkgo extract, Radix Ginseng, procyanidin Lac regis apis, trace element.
2. Cys pharmaceutical composition according to claim 1, is characterized in that active component comprises optical isomer, pharmaceutical salts and hydrate.
3. Cys pharmaceutical composition according to claim 1, is characterized in that active component is according to parts by weight: containing the composition 1 of 5 ~ 100 parts and the composition II of 10 ~ 200 parts.
4. Cys pharmaceutical composition according to claim 3, is characterized in that preferably 10 parts of compositions 1 and 30 parts of composition II form described active component.
5. Cys pharmaceutical composition according to claim 1, is characterized in that this pharmaceutical composition can make medically pharmaceutical preparation and medical apparatus and instruments thereof.
6. the Cys pharmaceutical composition according to right 1 or 5, is characterized in that the application of this pharmaceutical composition aspect that upper respiratory tract, upper digestive tract acetaldehyde are carcinogenic for preventing, remove smoking, when drinking.
CN201410244419.1A 2014-06-05 2014-06-05 Applications of L-cysteine composition in prevention, removal (or elimination) of carcinogenic factor acetaldehyde generated during smoking and drinking Pending CN105267267A (en)

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Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1430983A (en) * 2003-01-31 2003-07-23 厦门蓬岛医药服务有限公司 Liquid preparation of gingko leaves and its preparing method
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CN101926503A (en) * 2009-06-16 2010-12-29 成进学 Anti-cancer macrobiotic cigarette rich in trace elements selenium and germanium and having function of powerfully eliminating toxicity of tar smoke
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Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1430983A (en) * 2003-01-31 2003-07-23 厦门蓬岛医药服务有限公司 Liquid preparation of gingko leaves and its preparing method
CN101668522A (en) * 2006-05-22 2010-03-10 拜奥希特公司 Composition and method for binding acetaldehyde in stomach
CN101306074A (en) * 2008-04-01 2008-11-19 中国人民解放军空军航空医学研究所 Anti-alcohol and liver- protection medicine composition
CN101926503A (en) * 2009-06-16 2010-12-29 成进学 Anti-cancer macrobiotic cigarette rich in trace elements selenium and germanium and having function of powerfully eliminating toxicity of tar smoke
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Title
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Application publication date: 20160127