CN106727493A - Application of the anthocyanidin in treatment anti-malarial drug is prepared - Google Patents
Application of the anthocyanidin in treatment anti-malarial drug is prepared Download PDFInfo
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- CN106727493A CN106727493A CN201611200671.8A CN201611200671A CN106727493A CN 106727493 A CN106727493 A CN 106727493A CN 201611200671 A CN201611200671 A CN 201611200671A CN 106727493 A CN106727493 A CN 106727493A
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- anthocyanidin
- medicine
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- malaria
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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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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides application of the anthocyanidin in treatment anti-malarial drug is prepared, the structural formula of anthocyanidin is as follows：And there is provided containing the described anthocyanidin and its salt compounds and pharmaceutically pharmaceutical composition of acceptable carrier composition.Weight content of the active component anthocyanidin in pharmaceutical composition is 5 95%.Determined by external antimalarial active, as a result shown, anthocyanidin and its salt compounds there are preferably external antiplasmodial activities.Therefore, can be used to prepare the medicine for the treatment of malaria, there is larger clinical value.
Description
Technical field
The present invention relates to medicine, and in particular to application of the compound anthocyanidin in treatment anti-malarial drug is prepared, especially relate to
And application of the compound anthocyanidin in the anti-malarial drug that treatment is caused by plasmodium is prepared.
Background technology
Malaria (malaria) is serious harm human body health and lives safety, influences the important of socio-economic development
Parasitic disease.Malaria is classified as the public health problem that control is needed in the whole world badly together with AIDS, tuberculosis by the World Health Organization,
It is one of 3 kinds of infectious diseases of emphasis prevention and control in the United Nations's MDGs.According to World Health Organization, only in 2015
Interior, there are 438000 malaria deaths in the whole world, and the overwhelming majority occurs less than the five years old African children on the south the Sahara.
Malaria is caused by plasmodium, and its plasmodium includes plasmodium falciparum, Plasmodium vivax, malariae and Plasmodium ovale,
Wherein with plasmodium falciparum fatal rate highest.After the female human body by mosquito bite with ripe zygoblast, plasmodium is injected into human body,
Typical malaria clinical symptoms can occur through 10~20 days, the fourth phase can be divided into：Prodromal stage, feel cold (shiver with cold) phase, hot stage, perspiration
Phase and intermittent phase.After the recurrent exerbation of malaria, patient occurs anaemia, hepatosplenomegaly, or even brain type, superelevation heat type occurs, faint
The dangerous symptom such as cold mould and gastrointestinal type, or even threat to life.With the application of chloroquine, PIPERAQUINE and qinghaosu, drawn in recent decades
The life of countless people has been rescued, but these medicines occur in that different degrees of drug resistance, and causing the incidence of disease of malaria increasingly increases,
Urgently there is the discovery of the antimalarial agent of novel therapeutic effect.
Traditional Chinese medicine with good curative effect and is improved the quality of living as malaria prevention and the important component for the treatment of
One of advantage, the important means as malaria treatment.In Chinese Famous books《Compendium of Materia Medica》With《Malaria opinion》Describe as usual
Mountain, sweet wormwood, Java brucea, tsaoko and fructus amomi etc. are in the Chinese herbal medicine for treating malaria among the people.The work found from Chinese medicine sweet wormwood
Property compound artemisinin be used to treat malaria and achieve good effect, be widely used in clinic, therefore found from Chinese medicine and have
The compound of antimalarial active is significant.The present inventor has found that the chemical composition being widely present in plant is spent by research for many years
Blue or green element (cyanidin chloride) has notable Antimalarial.
Anthocyanidin is the water-soluble flavonoids pigment during a class is widely present in plant, is present in various green plantss
In the cell liquid of the various tissues such as flower, fruit, 27 sections are distributed widely in, in 72 plants of category.So far, it is known that flower
Blue or green element can be divided into 22 major classes, and the most frequently used is following six class:Pelargonidin, cyanidin, delphinidin, Chinese herbaceous peony color
Element, morning glory pigment and malvidin.Anthocyanidin has the ability for removing very much free radical by force, and with anti-oxidant, anti-inflammatory
Effect, bacteriostasis, anti-aging, antitumaous effect and to liver, to physiologically actives such as the protective effects of cardiovascular and cerebrovascular and eyesight.
There is not yet anthocyanidin has the report of Antimalarial.
The content of the invention
The technical problems to be solved by the invention are application of the research and design anthocyanidin in treatment anti-malarial drug is prepared.
The invention provides the application of anthocyanidin and its salt compounds in treatment anti-malarial drug is prepared.
The structural formula of anthocyanidin is as follows：
External antimalarial active measurement result shows that cyanine have preferably external antiplasmodial activities.Therefore, can be used to make
The medicine of standby treatment malaria.
It is a further object of the present invention to provide with anthocyanidin and its salt form as active component, for preparing treatment malaria
Pharmaceutical composition, particularly for preparing the pharmaceutical composition of malaria that treatment is caused by plasmodium.
The anthocyanidin and its salt compounds that pharmaceutical composition of the present invention contains therapeutically effective amount are active component, with
And contain one or more pharmaceutically acceptable carrier.Wherein weight of the active component in pharmaceutical composition is 5-95%.
The pharmaceutically acceptable carrier refers to the conventional pharmaceutical carrier of pharmaceutical field, for example：Diluent, excipient are such as
Water etc.；Filler such as starch, sucrose etc.；Adhesive such as gelatin, polyvinylpyrrolidone；Wetting agent such as glycerine；Disintegrant such as carbon
Sour calcium, sodium acid carbonate；Sorbefacient such as quaternary ammonium compound；Surfactant such as hexadecanol；Absorption carrier such as kaolin and
Soap clay；Lubricant such as talcum powder, calcium stearate, polyethylene glycol etc., it can in addition contain add other assistant agents in the composition such as
Flavouring agent, sweetener etc..
The compounds of this invention can be given and rectum by oral, injection, respiratory tract, skin, schneiderian membrane in the form of compositions
Mode be applied to the patient for needing this treatment.For it is oral when, can be by its academic title conventional solid pharmaceutical preparation such as tablet, particle
Agent, capsule etc. are made liquid preparation such as water or oil-suspending agent, syrup etc.；The molten of injection can be made into during for injecting
Liquid, water or oleaginous suspension etc.；During for respiratory tract administration, spray is can be made into；During for percutaneous drug delivery, can be made into soft
Formulation of paste and percutaneous dosing etc.；During for rectally, the formulations such as suppository are can be made into.
The various formulations of pharmaceutical composition of the present invention can be prepared according to the conventional production process of pharmaceutical field.For example make work
Property composition mix with one or more carrier, be then made into required formulation.
Brief description of the drawings
Fig. 1 cyanidin chlorides and positive drug (chloroquine) are on 3D7 worms strain survival rate influence figure
In figureChloroquine group is (respectively：0th, 0.01,0.1,1 μ g/mL),Cyanidin chloride is (respectively：0、1、3、10μ
M), * P<0.05**P<0.01***P<0.001
Fig. 2 anthocyanidin and positive drug (chloroquine) are on 3D7 worms strain survival rate influence figure
In figureChloroquine group is (respectively：0th, 0.01,0.1,1 μ g/mL),Anthocyanidin is (respectively：0th, 1,3,10 μM), * P
<0.05**P<0.01***P<0.001
Specific embodiment
Embodiment：Anthocyanidin and the external antimalarial active of cyanidin chloride are determined
Cyanidin chloride and anthocyanidin (going through ancient cooking vessel from Shanghai biological).Antimalarial active can be by measuring plasmodium
DsDNA contents determine (Corey, V.C., et al., A broad analysis of resistance development
in the malaria parasite.Nat Commun,2016.7:p.11901.).Containing 20 μ L serial dilution test samples
The strain of 3D7 worms has been infected with being added in each hole of 96 orifice plates of chloroquine positive drug (being purchased from Chinese food drug assay research institute)
(100 μ L add 5g/L AlbuMAX to the red blood cell suspension of P.falciparum in the culture mediums of RPMI 1640 (Gibco)
(Gibco) and 50mg/L gentamicins (Sigma), parasitemia is made to reach 0.5%, 2%) packed cell volume reaches, then
It is placed in 37 DEG C, 5%CO2 incubators culture 48 hours.Cell lysate (Tris 2.4g/L, EDTA 1.86g/L, Saponin
0.08g/L, TritonX-100 0.8mL/L) cracked, from Sigma, dsDNA contents 10000X SYBR Green
I reagents (Invitrogen) are determined, mensuration program reference literature (Plouffe, D., et al., In silico activity
profiling reveals the mechanism of action of antimalarials discovered in a
high-throughput screen.Proc Natl Acad Sci U S A,2008.105(26):p.9059-64.).Briefly
In fact, the mixing of 100 μ L SYBR Green I reagents exactly is prepared by the mixture of 100 μ L cultivations and by document explanation, in room
The lower lucifuge of temperature cultivates 30-60 minutes and then 100 μ L are transferred in black ELISA Plate.ELISA Plate is put into EnSpire luciferase marks
In instrument (PerkinElmer), the fluorescence signal value in reading ferment target under the light absorption value of 485nm and 535nm per hole.From agent
IC is calculated in amount-effect curve50.The IC to 3D7 of anthocyanidin and cyanidin chloride50Value such as following table：
Result shows that anthocyanidin and cyanidin chloride have preferably external antiplasmodial activities.
Claims (6)
1. application of the anthocyanidin in treatment anti-malarial drug is prepared, it is characterised in that the structural formula of anthocyanidin is as follows：
2. application according to claim 1, it is characterised in that including anthocyanidin and its salt form, including chloride, amber
Amber hydrochlorate etc..
3. application according to claim 1, it is characterised in that the medicine is the medicine of the malaria that treatment is caused by plasmodium
Thing.
4. application according to claim 1, it is characterised in that the medicine is by anthocyanidin and its salt compounds conduct
Active component and the pharmaceutical composition that pharmaceutically acceptable carrier is made.
5. application according to claim 4, it is characterised in that active component anthocyanidin and its salt compounds are in medicine group
Weight content in compound is 5-95%.
6. application according to claim 4, its composition formulation can be oral administered dosage form, injecting medicine-feeding form, breathing
Canal drug administration formulation, percutaneous drug delivery formulation, nasal mucosa medicine administration formulation and forms for rectal administration.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611200671.8A CN106727493A (en) | 2016-12-22 | 2016-12-22 | Application of the anthocyanidin in treatment anti-malarial drug is prepared |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611200671.8A CN106727493A (en) | 2016-12-22 | 2016-12-22 | Application of the anthocyanidin in treatment anti-malarial drug is prepared |
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| Publication Number | Publication Date |
|---|---|
| CN106727493A true CN106727493A (en) | 2017-05-31 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201611200671.8A Pending CN106727493A (en) | 2016-12-22 | 2016-12-22 | Application of the anthocyanidin in treatment anti-malarial drug is prepared |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107837270A (en) * | 2017-09-21 | 2018-03-27 | 广东艾时代生物科技有限责任公司 | A kind of application of combination medicine in malaria is treated |
| CN107854467A (en) * | 2017-09-21 | 2018-03-30 | 广东艾时代生物科技有限责任公司 | A kind of combination medicine for treating malaria |
-
2016
- 2016-12-22 CN CN201611200671.8A patent/CN106727493A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| DAYCEM KHLIFI ET AL: "LC–MS analysis, anticancer, antioxidant and antimalarial activities of Cynodon dactylon L. extracts", 《INDUSTRIAL CROPS AND PRODUCTS》 * |
| FATIHA EL BABILI ET AL.: "Chemical study,antimalarial and antioxidant activities,and cytotoxicity to human breast cancer cells(MCF7) of Argania spinosa", 《PHYTOMEDICINE》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107837270A (en) * | 2017-09-21 | 2018-03-27 | 广东艾时代生物科技有限责任公司 | A kind of application of combination medicine in malaria is treated |
| CN107854467A (en) * | 2017-09-21 | 2018-03-30 | 广东艾时代生物科技有限责任公司 | A kind of combination medicine for treating malaria |
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Application publication date: 20170531 |