CN1939327A - Pharmaceutical usage of neolinarin, linarin and their composition - Google Patents
Pharmaceutical usage of neolinarin, linarin and their composition Download PDFInfo
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- CN1939327A CN1939327A CN 200510105421 CN200510105421A CN1939327A CN 1939327 A CN1939327 A CN 1939327A CN 200510105421 CN200510105421 CN 200510105421 CN 200510105421 A CN200510105421 A CN 200510105421A CN 1939327 A CN1939327 A CN 1939327A
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- linarin
- pectolinarin
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- cirsii japonici
- radix cirsii
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Abstract
An application of the pectolinarin, linarin, or their composition, and the active component of Japanese thistle containing them in preparing the medicine for treating mosebleed, spitting blood, urethremorrhage, uterine bleeding, wound haemorrhage, tuberculosis, etc is disclosed.
Description
Technical field
The present invention relates to Pectolinarin, linarin or its compositions and contain the purposes of the Radix Cirsii Japonici effective site of Pectolinarin more than 10%, linarin at preparation hemostasis and antituberculotics.Pectolinarin, linarin or its compositions and the Radix Cirsii Japonici effective site that contains these two kinds of compositions can be used for preparation treatment epistaxis, spit blood, and hematuria is had blood in stool, metrostaxis, traumatic hemorrhage, the medicine of carbuncle sore tumefacting virus and treatment or prevention tuberculosis disease.
Background technology
Radix Cirsii Japonici (Cirsium japonicum DC.) is the dried root of feverfew Radix Cirsii Japonici (Cirsium japonicumFisch.ex DC.).Have cooling blood for hemostasis, the effect of removing blood stasis to reduce swelling belongs to hemostasis class Chinese medicine.Pharmacological evaluation shows that contained Pectolinarin, linarin has hemostasis and tuberculosis effect [Pectolinarin as hemostatie[p] JP:62,240,621,1987 ,-11-12 in the extract of Radix Cirsii Japonici; Chem.Pharm.Bull.1987,35 (2): 861-864; The Chinese medicine voluminous dictionary first volume 2004,115～118].
In order to determine Radix Cirsii Japonici hemostasis and tuberculosis effective ingredient or effective site, we have adopted the targeting under the active guidance to follow the trail of separation method and have studied, and each separated part is carried out active testing.Experimental result shows that isolated Pectolinarin (Pectolinarin), linarin (Linarin) and compositions thereof all have hemostasis and antiphthisic effect with the Radix Cirsii Japonici effective site that contains these two kinds of compositions from Radix Cirsii Japonici.
Wherein the structure of Pectolinarin is:
Molecular formula: C
29H
34O
15, m/z:622.56; Colourless acicular crystal (methanol) (m.p.254～5 ℃ (decomposition).Uv λ
Max EeOHNm (log ε): 275,330; Be dissolved in diluted alkaline and pyridine, be insoluble in methanol, ethanol, acetone, ether and chloroform, water insoluble.
The structure of linarin is:
Molecular formula: C
28H
32O
14, m/z:592.55; M.p:272～274 ℃.[α]
D 9-90 ° (C=0.5, pyridine); Uv λ
Max MeOHNm (log ε): 269,325; Be dissolved in diluted alkaline and pyridine, be insoluble in methanol, ethanol, acetone, ether and chloroform, water insoluble.
Summary of the invention
The new purposes of the Radix Cirsii Japonici effective site that the object of the present invention is to provide Pectolinarin, linarin or its compositions and contain two kinds of compositions more than 10% in the preparation haemostatic medicament, wherein said haemostatic medicament can be treated epistaxis, haematemesis, hematuria, had blood in stool, metrostaxis, traumatic hemorrhage and carbuncle sore tumefacting virus disease.
The new purposes of Radix Cirsii Japonici effective site in the preparation antituberculotics that the object of the present invention is to provide Pectolinarin, linarin or its compositions and contain 10% above Pectolinarin or linarin.
Pectolinarin of the present invention, linarin and compositions thereof and to contain the preparation process of Radix Cirsii Japonici effective site of 10% above Pectolinarin or linarin as follows:
Chinese medicine Radix Cirsii Japonici fine powder, use ethanol extraction, merge extractive liquid,, reclaim ethanol to there not being the alcohol flavor, filter, filtrate adds a certain amount of distilled water, D101 type macroporous resin column on the water liquid, water, 20% ethanol, 75% ethanol and 95% ethanol elution successively, 75% ethanol elution position is through obtaining containing the Pectolinarin more than 10% or the Radix Cirsii Japonici effective site of linarin behind the concentrate drying.Further, this effective site obtains Pectolinarin or the pure product of linarin respectively after silica gel column chromatography separates.
Compositions of the present invention is made up of with 1: 9～9: 1 weight ratios Pectolinarin and linarin.Preferred Pectolinarin and linarin weight ratio are 1: 1.
1. animal acute toxicity test
(1) oral administration
Healthy male mice, body weight 18-22 gram, with Pectolinarin, linarin and contain Pectolinarin more than 10% or the Radix Cirsii Japonici effective site of linarin or compositions (Pectolinarin and linarin weight ratio are 1: 1) are made into aqueous solution and irritate stomach 5.0g/kg, in a continuous week, do not see dead mouse respectively.
(2) drug administration by injection
Healthy male mice, body weight 18-22 gram is used Pectolinarin, linarin and Radix Cirsii Japonici effective site or compositions (Pectolinarin and linarin weight ratio are 1: 1) to be made into aqueous solution respectively and is carried out lumbar injection, in a continuous week, observes the dead mouse situation.The LD of Pectolinarin
50Value is the LD of 4.83 ± 0.480g/kg, linarin
50Value is the LD of 4.51 ± 0.382g/kg, Radix Cirsii Japonici effective site
50Value is the LD of 5.80 ± 0.550g/kg, compositions
50Value is 5.10 ± 0.410g/kg.
2. to the influence of clotting time of mice
Adopt the influence of slide method, blood capillary method and docking method observation sample, the anastalsis of Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions among checking the present invention to clotting time of mice.Laboratory animal is an ICR kind mice (18.0-22.0g), and animal feeding factory provides by Green Dragon mountain.
The experimental drug thing is respectively among the present invention gained Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions (Pectolinarin and linarin weight ratio are 1: 1) among the embodiment, faces with preceding and prepares with 0.5%CMC-Na; Reference substance is etamsylate injection (state-run Wujin, a Jiangsu pharmaceutical factory lot number 001112), faces with preceding and prepares with sterile water for injection.
2.1 slide method
Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions and blank group relatively have significant difference (P＜0.01) among the present invention.The results are shown in Table 1.
Table 1 Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions are to the influence of clotting time of mice (X ± S)
| Group | Dosage (g/kg) | Number of animals (only) | Clotting time (s) |
| Blank group Pectolinarin linarin | -- 0.5 0.5 | 10 10 10 | 77.7±17.50 57.0±16.26 65.95±17.36 |
| Radix Cirsii Japonici active component composition etamsylate group | 0.5 0.5 0.2 | 10 10 10 | 52.1±13.21 49.2±19.07 51.2±16.15 |
2.2 blood capillary method
Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions and blank group relatively have significant difference (P＜0.01) among the present invention.The results are shown in Table 2.
Table 2 Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions are to the influence of clotting time of mice (X ± S)
| Group | Dosage (g/kg) | Number of animals (only) | Clotting time (s) |
| Blank group Pectolinarin linarin Radix Cirsii Japonici active component composition etamsylate group | -- 0.5 0.5 0.5 0.5 0.2 | 10 10 10 10 10 10 | 80.8±16.22 51.8±20.75 55.8±18.57 49.2±23.78 46.2±17.25 38.4±16.17 |
2.3 docking method
Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions and blank group relatively have significant difference (P＜0.05) among the present invention, the results are shown in Table 3.
Table 3 Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions are to the influence of clotting time of mice (X ± S)
| Group | Dosage (g/kg) | Number of animals (only) | Clotting time (s) |
| Blank group Pectolinarin linarin Radix Cirsii Japonici active component composition | -- 0.5 0.5 0.5 0.5 | 10 10 10 10 10 | 339.7±66.32 258.3±73.75 270.1±70.48 257.4±98.44 255.8±87.57 |
| The etamsylate group | 0.2 | 10 | 225.0±117.36 |
1. external inhibitory action to tubercule bacillus
By the bacteriostasis of in vitro tests observation sample to tubercule bacillus, the tuberculosis effect of Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions among checking the present invention.Experiment bacterial strain mycobacterium tuberculosis standard virulent strain H
37RV is available from Chinese pharmaceutical biological product institute; No. 296, clinical separation strain is through being accredited as mycobacterium tuberculosis.
The experimental drug thing is respectively among the present invention gained Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions (Pectolinarin and linarin weight ratio are 1: 1) among the embodiment, faces with preceding usefulness 0.5% CMC-Na preparation; Reference substance is streptomycin (Huabei Pharmaceutic Co., Ltd's lot number 041003), faces with preceding and prepares with sterile water for injection; The isopyknic normal saline of no medicine contrast.
2.1 it is external to tuberculosis standard bacterium H
37The inhibitory action of RV
Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions and blank group relatively have significant difference (P＜0.05) among the present invention, the results are shown in Table 4.
Table 4 Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions are to tuberculosis standard bacterium H
37The bacteriostasis of RV
| Group | Bacterium amount (ml) | Medicine and final concentration (mg/ml) | Warning natural law (d) | Judge |
| Blank group Pectolinarin linarin active component composition streptomysin | 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 | 0 2 4 2 4 2 4 2 4 1 | 1.2 3.49 5.29 3.49 5.49 12.69 ＞15 ＞15 ＞15 ＞15 | S S S S S S S S S |
Annotate: do not report to the police back two days if there is the medicine control bottle, contain medicine bottle and still do not report to the police, illustrate that medicine can suppress tubercule bacillus in this concentration, identify with " S ", otherwise with " R ".
3.2 external bacteriostasis to the strain of tuberculosis clinical isolates
Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions and blank group relatively have significant difference (P＜0.05) among the present invention, the results are shown in Table 5.
Table 5 Pectolinarin, linarin and Radix Cirsii Japonici effective site and compositions are to the bacteriostasis of tuberculosis clinical isolates strain
| Group | Bacterium amount (ml) | Nutritional solution (ml) | Medicine final concentration (mg/ml) | Warning natural law (d) | Judge |
| Blank group Pectolinarin linarin active component composition streptomysin | 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 | 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 | 0 2 4 2 4 2 4 2 4 1 | 4 8.33 13.4 7.49 11.5 8 ＞15 12.3 ＞15 ＞15 | S S S S S S S S S |
From above result of study, can draw the present invention and have following advantage:
1. the present invention has carried out new excavation to the Chinese medicine Radix Cirsii Japonici, has found Pectolinarin, linarin and compositions thereof and Radix Cirsii Japonici effective site (containing Pectolinarin and linarin more than 20%) the new purposes in pharmacy.
2. the Pectolinarin among the present invention, linarin and compositions and Radix Cirsii Japonici effective site (containing Pectolinarin and linarin more than 10%) toxicity is little, and pharmacological action is strong, has good prospect in medicine.
3. the raw material of substance Radix Cirsii Japonici resource among the present invention is extensive, inexpensive, and preparation technology is simple.
4. proved also among the present invention that the compositions of being made up of Pectolinarin and linarin also has identical medical function.
Pectolinarin among the present invention or linarin or contain the effective site or the compositions of above one or both effective ingredient can be with pharmaceutically acceptable excipient, adopt the conventional method of this area to be prepared into various dosage forms, as tablet, pill, capsule, granule, injection etc.The preferred dosage form that contains the pharmaceutical composition of Pectolinarin of the present invention and linarin is an oral formulations.Dosage be 20-500mg/ people/time, every day 1-3 time.
Various details embodiment, but content of the present invention is not limited to this fully.
The specific embodiment
Embodiment 1: Radix Cirsii Japonici fine powder 100g, and 4 times (crude drug: the weight of solvent ratio is 1: 8 with 95% ethanol extraction; 1: 6; 1: 6; 1: 6), merge extractive liquid,, reclaim ethanol to there not being the alcohol flavor, add distilled water to 500ml, last D101 type macroporous resin column, water, 20% ethanol, 75% ethanol and 95% ethanol elution successively, 75% ethanol elution position is through containing Pectolinarin or the mixed total glycosides (30g) of linarin more than 20% behind the concentrate drying.Mix total glycosides through silica gel column chromatography separate obtain Pectolinarin (95%, 7g) and linarin (95%, 6g) pure product.Through mark IR, UV, NMR and mmp and the TLC comparison of Huaihe River product respectively with Pectolinarin or linarin, determined the chemical constitution of above two pure product.
Embodiment 2: Radix Cirsii Japonici fine powder 1000g, and 3 times (crude drug: the weight of solvent ratio is 1: 8 with 70% ethanol extraction; 1: 6; 1: 6), merge extractive liquid, reclaims ethanol to there not being the alcohol flavor, add distilled water to 500ml, last D101 type macroporous resin column is used 20% ethanol, 75% ethanol and 95% ethanol elution successively, and 75% ethanol elution position is through getting Pectolinarin or the linarin (35g) more than 10% behind the concentrate drying.
Embodiment 3: will from Radix Cirsii Japonici, extract or Pectolinarin (1g) and linarin (9g) that other approach obtains fully mix with 1: 9 ratio, stir, grind the compositions (10g) of Pectolinarin and linarin.
Embodiment 4: will from Radix Cirsii Japonici, extract or Pectolinarin (5g) and linarin (5g) that other approach obtains fully mix with 1: 1 ratio, stir, grind the compositions (10g) of Pectolinarin and linarin.
Embodiment 5: will from Radix Cirsii Japonici, extract or Pectolinarin (9g) and linarin (1g) that other approach obtains fully mix with 9: 1 ratios, stir, grind the compositions (10g) of Pectolinarin and linarin.
Mix by recipe quantity with adjuvant obtaining Pectolinarin, linarin, Radix Cirsii Japonici effective site or compositions in the foregoing description, granulate, can be made into dosage forms such as tablet, capsule, be used for the treatment of the treatment epistaxis, spit blood hematuria, have blood in stool, metrostaxis, traumatic hemorrhage, diseases such as carbuncle sore tumefacting virus and treatment or prevention tuberculosis.
Claims (3)
1. Pectolinarin, linarin or its compositions and contain of the application of the Radix Cirsii Japonici effective site of Pectolinarin more than 10%, linarin at the preparation haemostatic medicament.
2. purposes according to claim 1, wherein haemostatic medicament be treatment epistaxis, haematemesis, hematuria, have blood in stool, the medicine of metrostaxis, traumatic hemorrhage and carbuncle sore tumefacting virus disease.
3. Pectolinarin, linarin or its compositions and contain the application of Radix Cirsii Japonici effective site in the medicine of preparation tuberculosis disease of Pectolinarin more than 10%, linarin.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510105421 CN1939327A (en) | 2005-09-28 | 2005-09-28 | Pharmaceutical usage of neolinarin, linarin and their composition |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510105421 CN1939327A (en) | 2005-09-28 | 2005-09-28 | Pharmaceutical usage of neolinarin, linarin and their composition |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102477055A (en) * | 2010-11-25 | 2012-05-30 | 苏州宝泽堂医药科技有限公司 | Method for extracting and purifying pectolinarin from circium japonicums |
| CN103784492A (en) * | 2014-01-12 | 2014-05-14 | 广西中医药大学附属瑞康医院 | Pratia begonafolia (Wall) Lindl. or P. nummularia (Lam.)A.Br.et Aschers extract with antitumor effect and application thereof |
| KR20210082012A (en) * | 2019-12-24 | 2021-07-02 | 경희대학교 산학협력단 | Composition comprising pectolinarin for inhibiting the formation of biofilm |
-
2005
- 2005-09-28 CN CN 200510105421 patent/CN1939327A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102477055A (en) * | 2010-11-25 | 2012-05-30 | 苏州宝泽堂医药科技有限公司 | Method for extracting and purifying pectolinarin from circium japonicums |
| CN103784492A (en) * | 2014-01-12 | 2014-05-14 | 广西中医药大学附属瑞康医院 | Pratia begonafolia (Wall) Lindl. or P. nummularia (Lam.)A.Br.et Aschers extract with antitumor effect and application thereof |
| CN103784492B (en) * | 2014-01-12 | 2018-03-23 | 广西中医药大学附属瑞康医院 | Common pratia herb extract and its application with antitumor action |
| KR20210082012A (en) * | 2019-12-24 | 2021-07-02 | 경희대학교 산학협력단 | Composition comprising pectolinarin for inhibiting the formation of biofilm |
| KR102441377B1 (en) | 2019-12-24 | 2022-09-07 | 경희대학교 산학협력단 | Composition comprising pectolinarin for inhibiting the formation of biofilm |
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