CN1399957A - Application of shikonin and its derivative in pharmaceutical industry - Google Patents

Application of shikonin and its derivative in pharmaceutical industry Download PDF

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Publication number
CN1399957A
CN1399957A CN 01123916 CN01123916A CN1399957A CN 1399957 A CN1399957 A CN 1399957A CN 01123916 CN01123916 CN 01123916 CN 01123916 A CN01123916 A CN 01123916A CN 1399957 A CN1399957 A CN 1399957A
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CN
China
Prior art keywords
shikonin
acetylshikonin
derivant
medicine
acetyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN 01123916
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Chinese (zh)
Inventor
王飞欣
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BEIJING JINBENCAO CHINESE HERBAL MEDICINE TECHNOLOGY DEVELOPMENT Co Ltd
Original Assignee
BEIJING JINBENCAO CHINESE HERBAL MEDICINE TECHNOLOGY DEVELOPMENT Co Ltd
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Application filed by BEIJING JINBENCAO CHINESE HERBAL MEDICINE TECHNOLOGY DEVELOPMENT Co Ltd filed Critical BEIJING JINBENCAO CHINESE HERBAL MEDICINE TECHNOLOGY DEVELOPMENT Co Ltd
Priority to CN 01123916 priority Critical patent/CN1399957A/en
Publication of CN1399957A publication Critical patent/CN1399957A/en
Pending legal-status Critical Current

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Abstract

The present invention is aimed at providing shikonin and new application of its all derivatives. Said invention includes the following contents: purity of shikonin, effective portion of its all derivatives and monomer when they are used for preparing medicine; medicine preparation by using shikonin and two kinds or more than two kinds of its all derivatives; compound patent medicine made up by using shikonin, its all derivatives and other medicine according to different mixing ratio; daily dosage of every monomer or several monomers mixture; and application in preparation of medicine for curing and preventing microbial infection diseases, inflammation diseases, malignant tumor, hemorrhage and hemopathy and immunoregulatory diseases and its administration mode.

Description

Shikonin (Shikonin) and the application of derivant in pharmacy thereof
(1) technical field
The present invention relates to the purposes of shikonin (Shikonin) and whole derivants thereof, relate in particular to the purposes in pharmaceutical field.Particularly shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikon) thereof, β, beta-dimethyl-acryloyl shikonin (β, the purposes of β-Dimethylacrylshikonin),
(2) background technology
Shikonin (Shikonin) and all derivant be the chemical compound that discloses, wherein shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, the molecular formula and the molecular structure of beta-dimethyl-acryloyl shikonin (β, β-Dimethylacryl shikonin) are:
Figure A0112391600041
Shikonin (Shikonin) R=-H wherein, molecular formula: C 16H 16O 5, be the crystallization of brown micropin shape, divide
The son amount is 288; Acetyl-shikonin Acetylshikonin (Acetylshikonin) Molecular formula: C 18H 18O 6, be reddish brown
Toner powder, molecular weight are 330; β, beta-dimethyl-acryloyl shikonin, (β, β-Dimethylacryl shikonin)
Figure A0112391600043
Molecular formula: C 21H 22O 6, be kermesinus
Crystalline particulate, molecular weight are 370;
Shikonin (Shikonin) and derivant thereof are all water insoluble, are soluble in oil, alcohol, ethers.
Shikonin (Shikonin) and all derivant can by comfrey Radix Arnebiae (Radix Lithospermi) (Lithospernnunerythrorhizor.Sieb.et.Zucc), lithospermum euchromum Royle (Arnebia euchroma, pahnst.), extract in the arnebia guttata Bunge (Arnebia gutlata Bunge) and make.
(3) summary of the invention
The object of the present invention is to provide the new purposes of shikonin (Shikonin) and whole derivants thereof, i.e. new application in pharmacy.Particularly shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetyl-shikon) thereof, β, beta-dimethyl-acryloyl shikonin (β, the new purposes in pharmacy of β-Dimethylacrylshikonin).
In fact, the present invention relates to use shikonin (Shikonin) and the purity when all the effective site of derivants and monomer are done medicine thereof.
The present invention relates to use shikonin (Shikonin) and all in the derivant two or more various combination do medicine; Relate to and use shikonin (Shikonin) and whole derivant thereof to press different proportioning compound recipe patent medicine with other medicines.
The present invention relates to shikonin (Shikonin) and day use amount that all each monomer of derivant is used as medicine and effective site is used as medicine thereof.
The invention still further relates to shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, and beta-dimethyl-acryloyl shikonin (β, β-Dimethylacrylshikonin) as preparing the function attending scope for the treatment of or preventing the new drug of human body diseases.
Simultaneously, the invention still further relates to shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) β thereof, beta-dimethyl-acryloyl shikonin (β, the administering mode of finished drug product in the human body therapy process of β-Dimethylacrylshikonin).
The invention still further relates to shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) β thereof, (β, the finished drug product of β-Dimethylacrylshikonin) is for the therapeutic domain of human organ for beta-dimethyl-acryloyl shikonin.
(4) specific embodiment
Purpose of the invention process is to provide the new purposes of shikonin (Shikonin) and whole derivants thereof, i.e. new application in pharmacy.Particularly shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikon) thereof, β, beta-dimethyl-acryloyl shikonin (β, the new purposes in pharmacy of β-Dimethylacrylshikonin).
The present invention relates to use shikonin (Shikonin) and whole derivant thereof in implementation process, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, beta-dimethyl-acryloyl shikonin (β, during purity when the effective site of β-Dimethylacrylshikonin) and monomer are done medicine, emphasize particularly to use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof with shikonin (Shikonin) and whole derivant thereof; β, and beta-dimethyl-acryloyl shikonin (β, purity was more than 70% (containing 70%) when the effective site of β-Dimethylacrylshikonin) was done medicine, and purity is more than 80% (containing 80%) when doing medicine with monomer.
The present invention relates in implementation process can use shikonin (Shikonin) and whole two or more compound mixtures arbitrarily in the derivant thereof, takes different compound modes to do medicine according to actual needs; Also relate to can use shikonin (Shikonin) and all in the derivant any one chemical compound or more than one multiple chemical compound combination press different proportioning compound recipe patent medicine with other medicines.
The present invention in implementation process, relate to shikonin (Shikonin) and all in the derivant any one monomer be used as medicine or day use amount scope of some monomer mixtures when being used as medicine, in shikonin (Shikonin) and the whole derivant thereof any one monomer be used as medicine or some monomer mixtures when being used as medicine day use amount between 10 μ g-20g.
The present invention also relates to shikonin (Shikonin) and whole derivant thereof in implementation process, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, (the application in the medicine that β, β-Dimethylacrylshikonin) catch as preparation treatment or prevention human microorganism of beta-dimethyl-acryloyl shikonin.
Relate to shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, and beta-dimethyl-acryloyl shikonin (β, β-Dimethylacrylshikonin) as the application in the medicine of preparation treatment or the various inflammation diseases of prevention human body.
Also relate to shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, and beta-dimethyl-acryloyl shikonin (β, β-Dimethylacrylshikonin) as the application in the medicine of preparation treatment or prevention human malignant tumor disease.
Also relate to shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, beta-dimethyl-acryloyl shikonin (β, β-Dimethylacrylshikonin) as the preparation treatment or the prevention human body is hemorrhage and the medicine of blood disease in application.
Also relate to shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, and beta-dimethyl-acryloyl shikonin (β, β-Dimethylacrylshikonin) as the application in the medicine of preparation treatment or prevention human immunity modulability disease.
Simultaneously, the present invention also relates to shikonin (Shikonin) and whole derivant thereof in implementation process, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, beta-dimethyl-acryloyl shikonin (β, the administering mode of finished drug product in the human body therapy process of β-Dimethylacrylshikonin), that finished drug product of the present invention can use when acting on the human body therapy process is for oral administration, the administering mode of external, injection, suction, being that finished drug product of the present invention can be oral medicine, also can be medicine for external use, injecting drug use, inhaled medication.
The present invention also relates to shikonin (Shikonin) and whole derivant thereof in implementation process, particularly use shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) β thereof, beta-dimethyl-acryloyl shikonin (β, the finished drug product of β-Dimethylacrylshikonin) is for the therapeutic domain of human organ, shikonin (Shikonin) and whole derivant thereof, particularly use shikonin (Shi-konin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) β thereof, beta-dimethyl-acryloyl shikonin (β, the finished drug product of β-Dimethylacrylshikonin) for the therapeutic domain of human organ is: the respiratory system of human body, digestive system, urinary system, reproductive system, blood system, blood circulation and skin, mucosal sites.

Claims (9)

1, shikonin (Shikonin) and all derivant, particularly shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, (β, β-Dimethylacrylshikonin) is the application in the medicine aspect treatment human microorganism infection, inflammation, tumor, hemorrhage, hematopathy, immunomodulating for beta-dimethyl-acryloyl shikonin.
2, shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, beta-dimethyl-acryloyl shikonin (β, molecular formula and the molecular structure of β-Dimethylacrylshikonin) are: Shikonin (Shikonin) R=-H molecular formula: C 16H 16O 5Acetyl-shikonin Acetylshikonin (Acetylshikonin) Molecular formula: C 18H 18O 6β, beta-dimethyl-acryloyl shikonin
Figure A0112391600023
Molecular formula: C 21H 22O 6(β, β-Dimethylacrylshikonin)
3, use shikonin (Shikonin) and whole derivant, particularly shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, and beta-dimethyl-acryloyl shikonin (β, purity was more than 70% (containing 70%) when the effective site of β-Dimethylacrylshikonin) was done medicine; Purity is more than 80% (containing 80%) when using monomer whose to do medicine.
4, use two or more various combination of shikonin (Shikonin) and whole derivants thereof to do medicine.
5, use shikonin (Shikonin) and whole derivant thereof and other medicines to press different proportion compound recipe patent medicine.
6, shikonin (Shikonin) and all any monomer in the derivant be used as medicine or some monomer mixtures when being used as medicine, each monomer or some monomer mixtures are used as medicine day, use amount was between 10 μ g-20g.
7, shikonin (Shikonin) and all derivant, particularly shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, (that β, the finished drug product of β-Dimethylacrylshikonin) can use in the human body therapy process beta-dimethyl-acryloyl shikonin is for oral administration, the administering mode of external, injection, suction.
8, shikonin (Shikonin) and all derivant, particularly shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, and beta-dimethyl-acryloyl shikonin (β, β-Dimethylacrylshikonin) therapeutic domain to human microorganism's infection and inflammation is: respiratory system; Digestive system; Urinary system; Reproductive system; Blood system; Blood circulation and skin, mucosa position.
9, shikonin (Shikonin) and derivant Acetyl-shikonin Acetylshikonin (Acetylshikonin) thereof; β, (β, β-Dimethylacrylshikonin) therapeutic domain to human tumor is to dislike the part tumor to beta-dimethyl-acryloyl shikonin.
CN 01123916 2001-08-03 2001-08-03 Application of shikonin and its derivative in pharmaceutical industry Pending CN1399957A (en)

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102198130A (en) * 2011-03-30 2011-09-28 中国人民解放军第二军医大学 Use of shikonin as antifungal medicine synergist
CN103113335A (en) * 2011-11-17 2013-05-22 复旦大学 Benzoquinone compound and use thereof for preparing anti-tumour drug
KR101828563B1 (en) 2017-01-10 2018-02-13 경희대학교 산학협력단 A composition for prevention and treatment of foulbrood

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102198130A (en) * 2011-03-30 2011-09-28 中国人民解放军第二军医大学 Use of shikonin as antifungal medicine synergist
CN102198130B (en) * 2011-03-30 2012-08-29 中国人民解放军第二军医大学 Use of shikonin as antifungal medicine synergist
CN103113335A (en) * 2011-11-17 2013-05-22 复旦大学 Benzoquinone compound and use thereof for preparing anti-tumour drug
CN103113335B (en) * 2011-11-17 2015-06-17 复旦大学 Benzoquinone compound and use thereof for preparing anti-tumour drug
KR101828563B1 (en) 2017-01-10 2018-02-13 경희대학교 산학협력단 A composition for prevention and treatment of foulbrood

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