CN109331008A - Application of the rcumenol in the drug of preparation prevention and treatment psoriasis - Google Patents
Application of the rcumenol in the drug of preparation prevention and treatment psoriasis Download PDFInfo
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- CN109331008A CN109331008A CN201811509907.5A CN201811509907A CN109331008A CN 109331008 A CN109331008 A CN 109331008A CN 201811509907 A CN201811509907 A CN 201811509907A CN 109331008 A CN109331008 A CN 109331008A
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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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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Abstract
The present invention relates to application of the rcumenol in the drug of preparation prevention and treatment psoriasis.Drug described in the application is made of rcumenol and medically acceptable auxiliary material, and it is 0.1%~50% that wherein rcumenol, which is used in the mass percentage in drug,.Drug of the present invention has antipsoriatic effect, can be used for preventing and treating psoriasis.
Description
Technical field
The present invention relates to the pharmaceutical products containing organic effective component, and in particular to the drug containing sesquiterpenoids.
Background technique
Psoriasis is a kind of common autoimmune skin disease, is easy recurrence, the state of an illness period is long, and can cause
Complication, such as psoriatic arthritis, inflammatory bowel disease, tumour, Metabolic Syndrome etc..Currently, by the people of this sickness influence
Mouth about 15,000,000, accounts for total world population 2%-3%, and show an increasing trend year by year.According to the coincident with severity degree of condition of patient
It is selected, mainly includes local treatment, systematic treating and phototherapy.Western medicine is in the preferable work for the treatment of psoriasis middle or short term display
With long-time service also produces some side effects.Though the fiest-tire medication vitamin D derivative as local treatment has definite treatment
Effect, but be used for a long time easily cause metabolism it is not normal, glucocorticoid treatment psoriasis in be widely used, but be discontinued after often
It will appear " knock-on " phenomenon of Repigmentation or exacerbation.Acitretin, methotrexate (MTX) and cyclosporine are conventionally used for psoriasis system
The drug treated is ruled, some adverse reactions also occurs, taking Acitretin for a long time will lead to the dry damage of skin and mucosa, first ammonia butterfly
The most common side effect of purine is hepatotoxicity wind agitation, and cyclosporine can then cause the side effects such as lesions of liver and kidney, gastrointestinal reaction.Find effectively,
The curing psoriasis drug of safety seems particularly significant.
Existing literature (prevent and treat in psoriasis and its Study on mechanism [J] by Li Fuchang, Li Jin surprise curcuma zedoary alcohol extract emulsifiable paste
Medicine pharmacology and clinical, 2016,32 (03): 95-98.) and the Publication No. CN 105079720A patent applications report first of curcuma zedoary
Alcohol extracting thing has the function of preventing and treating psoriasis.It is well known that alcohol extracting thing is dissolved in the chemical component of alcohol (methanol or ethyl alcohol),
Wherein certainly containing the effective component of a large amount of non-treatment psoriasis.Therefore, it is selected from numerous chemical components of curcuma zedoary alcohol extract
It is used as medicine with compound and treats psoriasis, it is clear that pays creative labor.
Rcumenol (Curcumol), alias curcumol, cowherb flavol, Curcumol etc. are a kind of sesquiterpenoids,
It is present in yak Er Miao section, Ericaceae and zingiberaceous plant (such as curcuma zedoary), molecular formula C more15H24O2, molecular weight 236 is
Colourless acicular crystal, fusing point are 141~142 DEG C.Rcumenol is soluble in chloroform, ether, can be dissolved in the organic solvents such as ethyl alcohol, slightly soluble
In petroleum ether, it is practically insoluble in water.Rcumenol has extensive pharmacological activity, has good antitumor action, to gastric cancer, white
Blood disease, gynecological tumor, liver cancer, lung cancer etc. have good result, and mechanism of action may be by inhibiting nucleic acid metabolism, inducing cell
Apoptosis has relationship；In addition, rcumenol also has antibacterial, antiviral and antithrombotic isoreactivity.But at present still without out in document
Existing rcumenol is used to treat the report of psoriasis.
Summary of the invention
The technical problem to be solved in the present invention is to provide the new applications of rcumenol, i.e., the new opplication in pharmacy.
The above-mentioned new opplication in pharmacy is application of the rcumenol in the drug of preparation prevention and treatment psoriasis；Wherein, described
Drug be not curcuma zedoary alcohol extracting thing, shown in the chemical structure of the rcumenol such as following formula (I):
In above-mentioned application, the rcumenol can use conventional method can also as extracted in curcuma zedoary from natural plants
By synthesizing or other methods are made.
In above-mentioned application, the drug is made of rcumenol and medically acceptable auxiliary material, wherein rcumenol is in medicine
Mass percentage in object is 0.1%~50%.
In above-mentioned application, the drug can be clinically acceptable gelling agent, ointment, capsule or tablet.
The present invention is studied using effect of the imiquimod induction psoriasis mouse model to rcumenol prevention and treatment psoriasis
It was found that rcumenol can protect imiquimod to induce psoriasis mouse model, mitigate the skin being grievously injured degree, improves tissue morphology.
It is described that specific experimental method is as follows.
Detailed description of the invention
Fig. 1 is blank control group, model control group, rcumenol low dose group and rcumenol high dose group back of mice skin lesion
Situation photo.
Fig. 2 is blank control group, model control group, rcumenol low dose group and rcumenol high dose group mouse the skin being grievously injured
Extent index PASI score curve figure.
Fig. 3 is that blank control group, model control group, rcumenol low dose group and rcumenol high dose group HE stained slice are aobvious
Micro- photo.
Specific embodiment
One, effect experimental examples
1 drug and reagent
Given the test agent: rcumenol is purchased from Shanghai Aladdin biochemical technology limited liability company (lot number: C1617191), adds
Enter carbomer and triethanolamine, is made into the gelling agent containing rcumenol 0.01% and 0.1% two concentration.Imiquimod ointment,
It is purchased from Sichuan Mingxin Drug Industry Co., Ltd.；
Experimental animal: BalB/C mouse 24, male, weight 18-22g is purchased from Guangdong Province medical animal experiment center；
2 experimental methods
2.1 experimental groups and administration
BalB/C mouse 24 are taken, male, weight 18-22g is randomly divided into 4 groups, every group 6, i.e. blank control group, mould
Type control group, rcumenol high dose group and rcumenol low dose group.In addition to blank control group, other group every mornings are smeared
5% imiquimod ointment；Wherein model control group applies Blank gel matrix every afternoon outside, and the high low dosage of rcumenol applies cowherb respectively
The gel of the concentration of art alcohol 0.1% and 0.01%, it is each every time to smear 0.1g.
2.2 imiquimods cause mouse psoriasis model:
Using imiquimod inducing mouse psoriasis model, experiment the previous day shaves back of mice hair, formed 2cm ×
3cm area is uniformly applied to back of mice skin using 5% imiquimod ointment (62.5mg), once a day, continuous to apply
It smears 6 days, makes psoriasis mouse model.Stopping modeling in 7th day, cervical dislocation put to death mouse after, take back skin lesion 0.5cm ×
0.5cm area, 4% paraformaldehyde are fixed, and paraffin embedding is spare.
2.3 mouse Pigs with Psoriasis areas and disease severity scoring:
Observation back of mice skin lesion daily, and according to psoriatic lesion severity index (Psoriasis Area
And Severity Index, PASI) standards of grading, give erythema at mouse skin lesion, the scales of skin that peel off and the product for infiltrating thickened degree 0-4
Point, three is integrated into addition and obtains total mark.PASI standards of grading are as follows: 0: nothing；1: slight；2: moderate；3: severe；4: extremely heavy
Degree.
2.4 mouse skin lesion histopathology histological observations:
HE dyeing be the different material in slice is dyed into different colours under the action of different dye liquors and is shown, then
The various structures in tissue are observed by optical microscopy, it is dyeing the most conventional, can contribute to do skin lesion degree
It diagnoses out.
Histopathology operation is fixed including materials, is dehydrated transparent, waxdip embedding, slice and patch, is de- in skin lesion tissue
Batik color, is dehydrated the several steps of transparent and sealing at HE dyeing.
2.5 statistical methods:
As a result it is indicated with mean ± standard error (Mean ± S.E.M.), and is analyzed using 17.0 statistical software of SPSS,
Not comparison in difference one-way analysis of variance (One-way ANOVA) (not assuming that homogeneity of variance Dunnett's T3) between each group.P<
0.05 indicates that difference has statistical significance.
3 results:
Influence of 3.1 rcumenols to imiquimod inducing mouse psoriasis model skin lesion situation
After the last administration, back of mice skin lesion situation is as shown in Figure 1, PASI appraisal result is as shown in Figure 2.Wherein blank group
Back of mice is smooth, and no erythema shows no scales of skin that peel off, and without thickening phenomenon；Compared to the blank group, the skin lesion of model group back of mice increases
More, skin infiltration thickens, and cerise is presented to aubergine in skin lesion color, and skin lesion shows there is scales of skin that peel off covering, and the scales of skin that peel off is thick, stratification, and
There is a small amount of obscission, PASI scoring is far longer than blank group；Compared with model group, administration group PASI scoring decline, mouse skin
Damage still has the scales of skin that peel off, but the scales of skin that peel off is reduced trend compared with model, and skin lesion thickens situation and also makes moderate progress, and illustrates rcumenol to miaow quinoline
Mo Te induction psoriasis mice all has protective effect.
Influence of 3.2 rcumenols to imiquimod inducing mouse skin lesion tectology
HE dyeing display structure is as shown in Figure 3.Compared with blank group, model group parakeratosis, epidermis prickle cell's quantity increases
Add, stratum spinosum epidermidis thickens, and similar psoriasiform pathological change illustrates this model modeling success；After rcumenol treatment, epidermis cortex
More smooth, parakeratotic cell significantly reduces, and thickens situation lower than model group, illustrates that rcumenol can improve imiquimod and lure
The mouse psoriasiform effect led.
4 conclusions
The results show that rcumenol has good preventive and therapeutic effect to psoriasis.
Two, medicine preparation example
Example 1:(gelling agent)
Rcumenol 1000mg is taken, soya-bean oil 10mL dissolution is increased, is added to and is mixed with the carbomer 10g that 500mL water impregnates, added
Distilled water is added triethanolamine and adjusts pH value to 10 or so to get 0.1% rcumenol gelling agent to 1000g after being sufficiently stirred.
Example 2:(ointment)
Cichoric acid 1000mg is taken, citric acid 1000mg, sodium citrate 500mg are added, sodium chloride 1800mg adds the note of 1000ml
It penetrates and uses water, be stirred to dissolve, the note of every 2mg/2ml is made through 100 DEG C of 15 minutes flowing steam sterilizations in degerming filtration, encapsulating
Liquid is penetrated to use for injection.
Rcumenol 1000mg is taken, stearic acid 120g, glycerin monostearate 35g, liquid paraffin 60g, vaseline is added
10g, lanolin 50g are placed in container, and water-bath is sufficiently stirred evenly to 75 DEG C；Distilled water is added to 725g, water-bath is to 75 DEG C, sufficiently
It stirs evenly, is poured slowly into the oily phase such as stearic acid, is stirred well to emulsification completely, lets cool to get 0.1% rcumenol ointment.
Example 3:(capsule)
Take rcumenol 500mg and 4000mg microcrystalline cellulose, 500mg sodium carboxymethyl starch, 400mg lauryl sodium sulfate
Equal auxiliary materials are sufficiently mixed, and are carried out dry granulation using roll-in method, then mix with appropriate magnesium stearate, are packed into 3# Capsules,
The capsule that specification is 10mg/ is made to supply to be administered orally.
Example 4:(tablet)
It takes rcumenol 500mg to be uniformly mixed with 4000mg starch, 200mg cross-linked pvp, 300mg sodium carboxymethyl starch, uses
75% ethanol solution of 5%PVP is pelletized as adhesive, softwood processed with 18 meshes, 1h after 60 DEG C of dryings, is added after 20 mesh whole grains
Enter appropriate talcum powder, mix, tabletting, the tablet that specification is 10mg/ piece is made and supplies to be administered orally.
Claims (3)
1. application of the rcumenol in the drug of preparation prevention and treatment psoriasis；Wherein, the drug is not the alcohol extracting thing of curcuma zedoary,
Shown in the chemical structure of the rcumenol such as following formula (I):
2. application according to claim 1, which is characterized in that the drug is by rcumenol and medically acceptable auxiliary
Material composition, it is 0.1%~50% that wherein rcumenol, which is used in the mass percentage in drug,.
3. according to application described in right 2, which is characterized in that the drug is gelling agent, ointment, capsule or tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811509907.5A CN109331008A (en) | 2018-12-11 | 2018-12-11 | Application of the rcumenol in the drug of preparation prevention and treatment psoriasis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811509907.5A CN109331008A (en) | 2018-12-11 | 2018-12-11 | Application of the rcumenol in the drug of preparation prevention and treatment psoriasis |
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| Publication Number | Publication Date |
|---|---|
| CN109331008A true CN109331008A (en) | 2019-02-15 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811509907.5A Pending CN109331008A (en) | 2018-12-11 | 2018-12-11 | Application of the rcumenol in the drug of preparation prevention and treatment psoriasis |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523675A (en) * | 2015-01-23 | 2015-04-22 | 广东省中医院 | Application of curcuma zedoary epoxy ketone in preparation of medicine or food for preventing and treating psoriasis |
| CN105079720A (en) * | 2015-09-22 | 2015-11-25 | 四川省人民医院 | Curcumenol extract emulsifiable paste and application of curcumenol extract emulsifiable paste in medicine for treating psoriasis |
| CN106632383A (en) * | 2016-11-21 | 2017-05-10 | 辽宁大学 | Curcumenol derivative as well as preparation method and application thereof in antitumor drugs |
| CN108939047A (en) * | 2018-07-20 | 2018-12-07 | 暨南大学 | Rcumenol and TRAIL are preparing the application in antineoplastic combination medication |
-
2018
- 2018-12-11 CN CN201811509907.5A patent/CN109331008A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104523675A (en) * | 2015-01-23 | 2015-04-22 | 广东省中医院 | Application of curcuma zedoary epoxy ketone in preparation of medicine or food for preventing and treating psoriasis |
| CN105079720A (en) * | 2015-09-22 | 2015-11-25 | 四川省人民医院 | Curcumenol extract emulsifiable paste and application of curcumenol extract emulsifiable paste in medicine for treating psoriasis |
| CN106632383A (en) * | 2016-11-21 | 2017-05-10 | 辽宁大学 | Curcumenol derivative as well as preparation method and application thereof in antitumor drugs |
| CN108939047A (en) * | 2018-07-20 | 2018-12-07 | 暨南大学 | Rcumenol and TRAIL are preparing the application in antineoplastic combination medication |
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Application publication date: 20190215 |