CN103142580A - Application of barbaloin - Google Patents
Application of barbaloin Download PDFInfo
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- CN103142580A CN103142580A CN2013100621619A CN201310062161A CN103142580A CN 103142580 A CN103142580 A CN 103142580A CN 2013100621619 A CN2013100621619 A CN 2013100621619A CN 201310062161 A CN201310062161 A CN 201310062161A CN 103142580 A CN103142580 A CN 103142580A
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- barbaloin
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- propionibacterium acnes
- acne
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Abstract
The invention discloses an application of barbaloin in preparing medicines or cosmetics for preventing or treating acne caused by propionibacterium acne breeding. The invention discloses the medicines or cosmetics which contain the barbaloin which can effectively treat the acne generation caused by propionibacterium acne breeding.
Description
Technical field
The present invention relates to medical usage, specifically, relate to a kind of purposes of barbaloin.
Background technology
Barbaloin claims again aloin, is the anthraquinone analog compound of hydroxyl, is the important effective ingredient of Aloe, always as an important indicator weighing the Aloe quality.
Barbaloin is yellow or faint yellow crystallization, exist following two kinds of isomers A(left) and the B(right side), both difference is that (both glucosyl groups all replace glucosyl group in the position difference of fearing ketone group on the carbon of 10, barbaloin A molecule has transconfiguration, barbaloin B molecule has cis-structure), and the ratio that both form easily changes because of the extracting method difference of using.Isomers A has more practical value.Its chemical structural formula is as follows:
Acne also claim acne, are a kind of complexity, sebaceous gland dysfunction disease chronic and universality, mainly occur in teen-age face, shirtfront and back.Its initial performance is the tip projection that is too much caused by androgen.In recent years, have been found that a lot of pathogeny of acne, but still had some mechanism not yet clear and definite.Briefly, the genesis mechanism of acne mainly contains: the obstruction of sebaceous gland hair follicle and keratinization, the breeding of anaerobic bacteria, the generation of inflammation.
From clinical performance, acne are divided into inflammation type and the NIP type that occurs together that occurs together.The performance that the acne of NIP begin is blackhead, and it begins is sightless duskiness head, can be converted at last the acne of any type.The formation reason of duskiness head is the abnormal keratinization that the funnel-like dermal tissue of hair follicle causes.The acne of two types can be distinguished on form, and one is closed blackhead, and another is open pimple.
Generally the acne pathogeny of approval is multiplicity now, and four most important pathogeny are identified out: (1) androgen stimulates the secretion of sebaceous gland.(2) hyperkeratosis and hair follicle stop up the abnormal desquamation of the funnel-like dermal tissue that causes.(3) amount reproduction of propionibacterium acnes.(4) generation of inflammation.
An amount reproduction that key factor is antibacterial of acne morbidity is isolated the pathogenic bacterium such as propionibacterium acnes (P.acnes), propionibacterium granulosum, staphylococcus aureus, Staphylococcus intermedius and staphylococcus epidermidis from the acne pilosebaceous unit of patients with acne.Can think, in the patients with acne paathogenic factor, the antibacterial infection is one of the main reasons, and propionibacterium acnes (P.acnes) is Main Pathogenic Bacteria.
Propionibacterium acnes is a kind of antibacterial that parasitizes in the human skin pilosebaceous unit, belongs to Gram-positive without the spore anaerobe.Usually colonize on the mucosa of skin, belong to conditioned pathogen.Modern science is thought: the fat that propionibacterium acnes mainly relies in cortex is nutrition, obtains the energy of triglyceride, and triglyceride is resolved into fatty acid.Be free in fatty acid in the acne hair follicle and the quantity positive correlation of propionibacterium acnes, these free fatty acids can produce inflammatory reaction.Simultaneously, the acne hair follicle provides good anaerobic environment for the breeding of propionibacterium acnes again, and the good nutritional labeling of bacterial growth also is provided, thus the propionibacterium acnes amount reproduction.Microscopically is observed the ultrastructure of propionibacterium acnes and found: propionibacterium acnes length is 3 ~ 5um, and width is 0.4 ~ 0.7um; A large amount of ribosome is distributed in Cytoplasm; Cell wall is take Peptidoglycan as main.It is generally acknowledged, propionibacterium acnes is the main cause that many antibacterials infect, and is also main pathogenic bacterium simultaneously.Many compositions in propionibacterium acnes can stimulate keratinocyte to produce a large amount of cytokine and inflammatory factor, and these compositions comprise, the enzyme of Peptidoglycan, lipopolysaccharide, antibacterial secretion and the protein factor that some are relevant.And the keratinocyte that not infected by propionibacterium acnes produces above-mentioned cytokine hardly, these cytokines and inflammatory factor can the chemotactic inflammatory cell around acne, cause the inflammation infringement, the factor of this inflammation sample also is considered to one of pathogeny of acne.
Propionibacterium acnes also produces a large amount of exoenzymes when facilitating a large amount of cytokines, these enzymes comprise: the enzyme materials such as protease, hyaluronidase and lipase, these factors can cause the inflammatory reaction of acne.
Propionibacterium acnes can produce protease and some CFs, can cause immunoreation, induces the generation of antibody, and by the activating complement approach, causes its immune-mediated inflammatory reaction, thereby increase the weight of the generation of acne.The sebaceous gland dysfunction at the position of while acne own, the sebum metabolism disorder causes again a large amount of bacterial reproductions, these floras are accompanied by again a large amount of staphylococcuses simultaneously take propionibacterium acnes as main.Lipid component is except the nutritional labeling as propionibacterium acnes, and some participates directly in the inflammation path.
For many years, scientists is induced inflammation to produce to propionibacterium acnes and has been done a large amount of research.Think propionibacterium acnes by produce esterase, protease, hyaluronidase reduces fat becomes glycerol and fatty acid, and in this process, discharges histamine and some cell chemotaxis materials cause inflammation.But because the T lymphocytic infiltration is to find the earliest in the early stage skin lesion of acne inflammation, Recent study more is inclined to and is thought that the process that propionibacterium acnes causes inflammation to be produced is a kind of allergy.By the detection to patients serum's antibody, find that the antibody concentration for some special polysaccharide of propionibacterium acnes cell wall constituent in patient body obviously raises, and the degree of inflammation presents positive correlation with the concentration of antibody, and does not find the antigen immune reaction at other positions.The immunoglobulin that participates in serious inflammatory reaction that studies confirm that subsequently is IgG, is IgM and participate in than the main immunoglobulin in subinflammation's reaction, and the order of severity that more fully demonstrates acne is relevant with immunity.The Peptidoglycan of propionibacterium acnes cell wall may participate in immunoreation, this shorter polysaccharide fragment is easy to enter epidermis, stimulate the immunocyte of corium to generate IL-1 α, the inflammatory factors such as TNF-α, IL-8, these inflammatory factors can be regulated the expression of adhesion molecule.To sum up, propionibacterium acnes may in the acne inflammation, especially play important effect on the order of severity of acne.Certainly unique factor of neither acne producing of propionibacterium acnes, this is because all have this antibacterial in almost all people's hair follicle, and is not that each exists the hair follicle of this antibacterial can cause infection.Someone studies the density of discovery propionibacterium acnes and follows the order of severity of acne not have too large dependency, and the process of the acne inflammation formation that also has more factor participation also is described simultaneously.
Propionibacterium acnes causes that by immunization route and nonimmune approach the mechanism of local inflammation has:
(1) Peptidoglycan in the propionibacterium acnes cell wall is diffused into the hair follicle surrounding tissue, thereby the immune stimulatory cell produces tumor necrosis factor-alpha and interleukin-8, and the unconventionality expression adhesion molecule.
(2) lymphocyte chemotactic factor (LCF), neutrophilic chemotactic factor, the cytokine chemotactic lymphocyte such as TNF-α, IL-8 and neutrophilic granulocyte are in the sebaceous gland hair follicle.
(3) propionibacterium acnes and special antibodies by the complement pathway activating immune system, produce complement fragment C5a, and this fragment is the chemotactic neutrophilic granulocyte significantly.
(4) when propionibacterium acnes antibody participated in, neutrophilic granulocyte can discharge multiple hydrolytic enzyme, and these enzymes have damage corium, destroyed the effect of follicular wall.
(5) propionibacterium acnes can be secreted a large amount of esterases and protease, thereby the follicular wall structure has been caused destruction.
(6) produce granulation swelling reaction around the Peptidoglycan hair follicle stimulating in cell wall.
(7) shortage of linoleic acid material causes the generation of free radical, O
2, H
2O
2Cause the damage of surrounding tissue and the destruction of hair follicle integrity with OH.
Summary of the invention
The present invention is in order to solve above-mentioned problems of the prior art, the purposes of barbaloin as the propionibacterium acnes inhibitor is provided, further, the present invention also provides barbaloin breeding the medicine of the acne that cause or the purposes in cosmetics for the preparation of prevention or treatment by propionibacterium acnes.The present invention has disclosed barbaloin can effectively treat the acne generation that causes because of the propionibacterium acnes breeding, low to human toxicity, has good application prospect.
In the present invention, described barbaloin can obtain by extracting from the leaf skin of Aloe.The another name of described barbaloin is barbaloin or aloin, English Aloin by name or Barbaloin; No. CAS is 1415-73-2; Molecular weight is 418.39; Molecular formula is C
21H
22O
9Chemistry is by name
1,8-Dihydroxy-10-(beta-D-glucopyranosyl)-3-(hydroxymethyl)-9(10H)-anth?racenone。
In the present invention, the pharmaceutical carrier of described barbaloin can be the various carriers of this area routine, preferably comprises microsphere, liposome or microemulsion.The dosage form of described medicine can be the various exterior-applied formulations of this area routine, preferably comprises one or more in spray, ointment and emulsifiable paste etc.Wherein, the form of medication of described medicine is percutaneous drug delivery.
In the present invention, described cosmetics can be the various types of cosmetics in this area, as fancy soap, cleansing milk, cosmetic water, emulsion or cream frost etc.
In the present invention, the content of described barbaloin in described medicine or cosmetics is 0.0125-99.99wt%, is preferably 0.01%-10wt%, is more preferably 1%-3wt%.
Except barbaloin, also can comprise other active component antibiotic and/or antiinflammatory according to general knowledge in propionibacterium acnes inhibitor of the present invention, as long as this active component and barbaloin do not produce obvious antagonism.
In the medicine of the acne that prevention of the present invention or treatment are caused by propionibacterium acnes breeding or cosmetics except barbaloin, also can comprise other active component antibiotic and/or antiinflammatory according to general knowledge, as long as this active component and barbaloin do not produce obvious antagonism.
In the present invention, but above-mentioned optimum condition combination in any on the basis that meets this area general knowledge namely gets each preferred embodiment of the present invention.
Raw material of the present invention and reagent is commercially available getting all.
Positive progressive effect of the present invention is:
1, the invention provides the new purposes of barbaloin, is a kind of potential high-efficiency low-toxicity medicine, and the acne that cause for Acne treatment propionibacterium amount reproduction provide application prospect.
2, barbaloin can be made various pharmaceutical dosage forms and cosmetics form, uses easyly, is easy to use.
Description of drawings
Fig. 1 is that barbaloin is to the inhibition figure of propionibacterium acnes.
The specific embodiment
The present invention is described in further detail below in conjunction with embodiment, but the present invention includes but be not limited to this.
The inhibition experiment of embodiment 1 barbaloin to propionibacterium acnes
Experimental strain: propionibacterium acnes (ATCC6919)
Culture medium:
(1) fluid medium: tryptone 10g/L, Carnis Bovis seu Bubali cream 10g/L, glucose 5g/L, NaCl5g/L, yeast extract 3g/L, sodium acetate 3g/L, soluble starch 1g/L, cysteine hydrochloride 0.5g/L, the distilled water dissolving, regulating pH is 6.8 ± 0.2,115 ℃ of autoclaving 20min.(2) solid medium: add agar 15g/L on the basis of liquid medium within.
Experimental technique: inhibition zone is measured
Propionibacterium acnes is inoculated in solid medium, cultivates 2d in 37 ℃ of anaerobic conditions and activate, after activation directly with the bacterial plaque normal saline dilution, be prepared into bacteria suspension.After getting activation, bacteria suspension 0.5ml in fluid medium, cultivates 2d in 37 ℃ of anaerobic conditions, is the experimental bacteria suspension.Experimental technique adopts cylinder plate method, pours the 5ml solid medium in culture dish into, waits to solidify; Separately get solid culture based on dissolving in microwave oven, when temperature drops to 50 ℃ of left and right, add the experimental bacteria suspension, adjusting propionibacterium acnes concentration is 10
5CFU/ml, the solid medium that will contain propionibacterium acnes approximately 7ml is poured the solid culture epibasal tier that 5ml solidifies into, after solidifying, equidistant 2 aseptic Oxford cups [internal diameter (6.0 ± 0.1) mm of putting on culture medium, external diameter (8.0 ± 0.1) mm, high (10.0 ± 0.1) mm injects respectively 200 μ l testing samples (with the normal saline dilution that contains 40% propylene glycol) in cup, three parallel.Simultaneously with the normal saline that contains 40% propylene glycol in contrast.After 37 ℃ of anaerobism are cultivated 2d, measure the antibacterial circle diameter of barbaloin with ruler, get its meansigma methods.
Experimental result sees Table 1 and Fig. 1:
The inhibitory action of table 1 barbaloin to propionibacterium acnes
* in the test group, the concentration of barbaloin is 500 μ g/ml.
As seen from Figure 1, all produced obvious inhibition zone around the cup of specimen Oxford, the inhibition zone size sees Table 1, proves that barbaloin has obvious inhibitory action for propionibacterium acnes.
Embodiment 2 barbaloin suppress propionibacterium acnes MIC pH-value determination pH
Experimental strain: propionibacterium acnes (ATCC6919)
Culture medium: (1) fluid medium: tryptone 10g/L, Carnis Bovis seu Bubali cream 10g/L, glucose 5g/L, NaCl5g/L, yeast extract 3g/L, sodium acetate 3g/L, soluble starch 1g/L, cysteine hydrochloride 0.5g/L, the distilled water dissolving, regulating pH is 6.8 ± 0.2,115 ℃ of autoclaving 20min.(2) solid medium: add agar 15g/L on the basis of liquid medium within.
Experimental technique: the mensuration of Chinese medicine extract minimum inhibitory concentration (MIC value)
Propionibacterium acnes is inoculated in solid medium, cultivates 2d in 37 ℃ of anaerobic conditions and activate, after activation directly with the bacterial plaque normal saline dilution, be prepared into bacteria suspension, dilute bacteria suspension with fluid medium, making its final bacteria concentration is l0
5CFU/mL.
Barbaloin is become experimental concentration with the normal saline dilution that contains 40% propylene glycol: 1000,500,250,125,62.5,31.3 and 15.6 μ g/ml.Add bacteria suspension 100 μ L and medicinal liquid 100 μ L after dilution in micropore, establish simultaneously the contrast of the negative control that does not add bacterium and the normal growth that does not add medicinal liquid, every kind of drug level do 3 parallel, average.Put 37 ℃ of anaerobism and hatch, observed result after 48h adopts the direct method reading out data.The prerequisite of result judgement is that growth control is good, and the blank asepsis growth is clear, and the growth of bacterium is suppressed with the rising of drug level gradient in other hole.
Experimental result sees Table 2:
Table 2 barbaloin suppresses propionibacterium acnes MIC pH-value determination pH
"-" represents asepsis growth; "+" representative has bacteria growing
As shown in Table 2, barbaloin is 125 μ g/ml to the MIC value of propionibacterium acnes.
Application Example 1 cosmetic water preparation
Table 3 cosmetic water formula
Preparation technology:
1. with A each component Hybrid Heating to 85 ℃ mutually, fully dissolving stirs; In advance that C is mutually solvent;
2. A is cooled to mutually 45 degree, adds B, C phase;
3. the rear discharging .PH that stirs is controlled at 5.5-7.0.
Application Example 2 milky lotion preparations
Table 4 milky lotion formula
Preparation technology:
1. first card ripple 941 is dispersed in glycerol, redispersion is in water and increase the temperature to simultaneously 85 ℃, then adds B other components mutually, stirs;
With A in 85 ℃ of dissolve completes, stir;
3. A is added to the B middle homogenizing (approximately 4 minutes) that stirs mutually, froth breaking is cooled to 45 ℃;
4. add C each component mutually, discharging stirs.PH value is controlled at 5.5-7.0.
Application Example 3 cleansing milk preparations
Table 5 cleansing milk formula
Production technology:
1. with A heat phase to 80 ~ 85 ℃, stir.
2. add successively the B phase after A is uniformly dispersed mutually, is uniformly dispersed.
3.A, the B two-phase rear stopped heating that is uniformly dispersed, be cooled to 45 ℃ and add the C phase, continue to be stirred to room temperature and get final product.
Claims (10)
1. barbaloin is being bred the medicine of the acne that cause or the purposes in cosmetics for the preparation of prevention or treatment by propionibacterium acnes.
2. purposes as claimed in claim 1, it is characterized in that: described barbaloin derives from the leaf skin of liliaceous plant Aloe.
3. purposes as claimed in claim 1, it is characterized in that: the content of described barbaloin in described medicine or cosmetics is 0.01-10wt%.
4. purposes as claimed in claim 3, it is characterized in that: the content of described barbaloin in described medicine or cosmetics is 1-3wt%.
5. purposes as claimed in claim 1, it is characterized in that: the medicine of described barbaloin comprises carrier, and described carrier is microsphere, liposome or microemulsion.
6. purposes as claimed in claim 1, it is characterized in that: the dosage form of described medicine is exterior-applied formulation.
7. purposes as claimed in claim 6, it is characterized in that: described dosage form is spray, ointment or emulsifiable paste.
8. purposes as claimed in claim 7, it is characterized in that: the administering mode of described medicine is percutaneous drug delivery.
9. purposes as claimed in claim 3 is characterized in that: described cosmetics comprise fancy soap, cosmetic water, emulsion or cream frost.
10. as the described claim of claim 1-9 any one, it is characterized in that the described medicine of barbaloin or the active component that cosmetics also comprise antibiotic and/or antiinflammatory of comprising.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105625039A (en) * | 2016-02-29 | 2016-06-01 | 苏州纺友新材料有限公司 | Bacteriostatic, mouldproof and mite-driving environment-friendly textile finishing agent |
| CN106726764A (en) * | 2016-12-25 | 2017-05-31 | 江西宜信堂医疗科技有限公司 | A kind of anti-acne essence and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1723801A (en) * | 2004-07-20 | 2006-01-25 | 上海杏灵科技药业股份有限公司 | Health-care food with functions of relaxing the bowels and beautifying, and its prepn. method |
| CN101003555A (en) * | 2006-10-11 | 2007-07-25 | 上海华震科技有限公司 | Method for separating barbaloin in high purity from product of aloe |
| CN101496775A (en) * | 2009-02-26 | 2009-08-05 | 徐伟玲 | Face cosmetic |
-
2013
- 2013-02-27 CN CN2013100621619A patent/CN103142580A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1723801A (en) * | 2004-07-20 | 2006-01-25 | 上海杏灵科技药业股份有限公司 | Health-care food with functions of relaxing the bowels and beautifying, and its prepn. method |
| CN101003555A (en) * | 2006-10-11 | 2007-07-25 | 上海华震科技有限公司 | Method for separating barbaloin in high purity from product of aloe |
| CN101496775A (en) * | 2009-02-26 | 2009-08-05 | 徐伟玲 | Face cosmetic |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105625039A (en) * | 2016-02-29 | 2016-06-01 | 苏州纺友新材料有限公司 | Bacteriostatic, mouldproof and mite-driving environment-friendly textile finishing agent |
| CN106726764A (en) * | 2016-12-25 | 2017-05-31 | 江西宜信堂医疗科技有限公司 | A kind of anti-acne essence and preparation method thereof |
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Application publication date: 20130612 |