CN1857237B - New use of falcarindiol - Google Patents
New use of falcarindiol Download PDFInfo
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- CN1857237B CN1857237B CN2006100274219A CN200610027421A CN1857237B CN 1857237 B CN1857237 B CN 1857237B CN 2006100274219 A CN2006100274219 A CN 2006100274219A CN 200610027421 A CN200610027421 A CN 200610027421A CN 1857237 B CN1857237 B CN 1857237B
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Abstract
The present invention discloses the application of falcarindiol in preparing antiphlogistic and analgetic medicine.
Description
Technical field
The present invention relates to medical technical field, specifically is a kind of new purposes of monomeric compound.
Background technology
The molecular structural formula of falcarindiol (falcarindiol) is as follows:
Falcarindiol once was found in Radix Angelicae Sinensis.The root of Radix Angelicae Sinensis contains volatile oil about 0.3%, the main n-butene husband lactone (n-butylidenephthalide) that contains the tool special aroma contains the positive pentanone of adjacent carboxyl benzene (n-vakerophenone-o-carboxylicacid), △ 2 in addition in the oil, 4-dihydro phthalic anhydride (△ 2,4-dihydrophthalic anhydride) and several sesquiterpene compounds.There is report Radix Angelicae Sinensis volatile oil master to contain ligustilide (ligustilide), accounts for 45%, secondly n-butene husband lactone.In addition, root still contains vitamin B12, sucrose, cupreol, fatty acid, folinic acid (folinic acid) or citrovorum factor (citrovorumfactor), Yan acid and biotin similar substances such as (biotin).According to another report, the water-soluble portion of root contains ferulic acid (ferulic acid), succinic acid (succinic acid), Yan acid (nicotinic acid), uracil (uracil), adenine (adenine), scopoletin (scopoletin), umbelliferone (umbelliferone), vanillic acid (vanillic acid) and choline (choline), and the ether dissolubility partly contains sickleleaf celery alcohol (falcarinol), sickleleaf celery ketone (falcarinolone), falcarindiol (falcarindiol).Chemical identification to Radix Angelicae Sinensis is a reference substance with butylene husband lactone.As seen the content of falcarindiol in Radix Angelicae Sinensis is very little.Because of falcarindiol can't be separated from Radix Angelicae Sinensis in a large number, therefore, the Drug therapy effect of falcarindiol still imperfectly understands.
The inventor is through years of researches, and separation and purification has gone out falcarindiol from other plant, therefore just the purposes of its medical aspect has been carried out comparatively deep exploration.
Summary of the invention
The present invention seeks to study the new purposes of falcarindiol anti-inflammatory and antalgic.
The present invention realizes by following experimental example:
Experiment grouping and every group of used medicine: be divided into 5 groups, promptly the blank group gives normal saline 10ml/kg; The indometacin matched group gives indometacin 1.25mg/kg; The basic, normal, high dosage group of falcarindiol is equivalent to the falcarindiol of 5 times of amounts of clinical human, 10 times of amounts, 20 times of amounts respectively, and high dose group is 4.75mg/ml, in, low dose group does the equivalent dilution of medicine respectively.
Experimental example one, falcarindiol xylol cause the effect of mice ear
Get 50 of male KM mices,, be divided into 5 groups at random by above-mentioned group technology.Successive administration 4 days, every mice left side of 30min ear is coated with dimethylbenzene 50ul after the last administration, and auris dextra is made blank, after causing scorching 15min mice is taken off cervical vertebra execution, cut two ears, (diameter 7mm) lays auricle at the same position of two ears respectively with card punch, weigh, calculate swelling degree and inhibitory rate of intumesce.
Formula: swelling degree=left auricle weight-auris dextra sheet weight
The result: the result shows, blank group mice left side ear redness, the ear swelling degree is up to 0.0148 ± 0.0016g, and the ear swelling degree of falcarindiol high, medium and low dosage group mice and indometacin matched group is all less than the blank group, and high, medium and low dosage group of falcarindiol and blank group relatively have significant difference (P＜0.01), with indometacin matched group zero difference (P〉0.05) relatively.The results are shown in Table 1.
Table 1 falcarindiol xylol causes the influence of mice ear
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01
Experimental example two, falcarindiol Dichlorodiphenyl Acetate cause the analgesic activity of mouse writhing
Get 50 of body weight 18-22g mices, by above-mentioned group technology, divide 5 groups at random, gastric infusion 40min pneumoretroperitoneum is injected 0.6% acetic acid 0.1ml/10g, observes mouse writhing number of times in the 15min immediately.
The result: the result shows, with the blank group relatively, basic, normal, high dosage group of falcarindiol and indometacin matched group all have significant difference (P＜O.01).See Table 2.
Table 2 falcarindiol Dichlorodiphenyl Acetate causes the influence (x ± S) of mouse writhing reaction
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.0l
Experimental example three, falcarindiol cause the analgesic activity of pain mice to hot plate method
Get female mice, under 20 ℃ of environment of room temperature, adjusting water bath with thermostatic control temperature to 554 ± 0.5 ℃, the bottom contact water surface of metal dish.Then female mice is placed on the hot plate, drop into hot plate with stopwatch record mice and the pain threshold of the response time (incubation period) of metapedes occur licking to 60s as this mice, lick the metapedes person screens 50 so that 5s-30s is internal energy before the medicine, divide 5 groups at random, the pain reaction incubation period of 15min, 30min, 60min, 120min behind the 10ml/kg gastric infusion.
Formula:
The result: the result shows, compare with the blank group, falcarindiol administration animal pain threshold behind administration 15min in the dosage group significant difference (P＜O.05) is arranged, high dose group has utmost point significant difference (P＜O.01), behind the 30min during to off-test each administration group utmost point significant difference (P＜O.01) is all arranged, compare zero difference with the indometacin group.The results are shown in Table 3,4.
Table 3 falcarindiol is to the influence of hot plate mice pain threshold (x ± S)
Annotate: with comparison before the administration
*P＜0.05,
*P＜0.01
Table 4 falcarindiol is to the influence of hot plate mice threshold of pain raising rate (x ± S)
Experimental example four, falcarindiol cause the influence that the mouse peritoneal capillary permeability increases to the lumbar injection azovan blue
Get 50 of body weight 18-22g mices (male and female half and half), divide 5 groups at random, 1h tail vein injection 0.5% azovan blue normal saline solution 0.1ml/10g body weight behind the animals administer, lumbar injection 0.6%HAc0.20ml/ only immediately, take off cervical vertebra behind the 20min and put to death, cut off skin of abdomen muscle, divide the washing abdominal cavity 3 times with the 6ml normal saline, suction pipe sucking-off cleaning mixture, merging back add normal saline to 10ml, the centrifugal 15min of 3000rpm; Get supernatant and 590nm colorimetric determination, record OD value is carried out statistical analysis.
The result: the result shows, compare with the blank group, low, the middle dosage group of falcarindiol has significant difference (P＜0.05), and the high dose group there was no significant difference (P〉0.05), indometacin matched group and blank group relatively have utmost point significant difference (P＜0.01).The results are shown in Table 5.
Table 5 falcarindiol causes the influence that the mouse peritoneal capillary permeability increases (x ± S) to lumbar injection HAc
Annotate: compare with the blank group,
*P＜0.05,
*P＜0.01
By above experimental example as seen, falcarindiol has antiinflammatory, analgesic effect, and its curative effect is suitable with the Western medicine indometacin.The inflammatory factor that falcarindiol can cause multiple reason discharges and the pain that causes plays therapeutical effect preferably, just can be used in the medicine of preparation treatment inflammatory painful diseases.In addition, falcarindiol can react the analgesic activity of Ligusticum delavayi Franch., is the pharmaceutically active monomer in the Ligusticum delavayi Franch., therefore, and can be as the detection index of Ligusticum delavayi Franch..
Advantage of the present invention: falcarindiol is the monomer extract of Chinese medicine, finds no any toxic and side effects, uses safer and more effective; Can be used as the Ligusticum delavayi Franch. plant or contain the index that the Chinese patent medicine of Ligusticum delavayi Franch. plant detects, promote understanding Chinese medicine.
The specific embodiment
Embodiment 1
Take by weighing falcarindiol 100g, cross 100 mesh sieves, 90-95% alcohol granulation behind starch 300g, the lactose 600g mixing.Be loaded in the capsule shells behind the granulate.Be used for the treatment of headache, migraine.
Embodiment 2
Take by weighing falcarindiol 50g, cross 100 mesh sieves, the alcohol granulation of 90-95%, dried granule and 30g magnesium stearate mixing tabletting behind starch 320g, the lactose 600g mixing.
Embodiment 3(being used for evaluation) to Chinese crude drug or Chinese patent medicine
Getting falcarindiol, accurate claim surely, with the acetonitrile dissolving and be made into the solution of 2.0mg/ml, draw 30 μ l, put on silica gel g thin-layer plate, be developing solvent with petroleum ether (60-90 ℃)-ethyl acetate (3: 1), launch, and exhibition distance: 8cm, taking-up is dried; Spray is dried with 5% ethanol solution of sulfuric acid, and 105 ℃ of bakings 5 minutes, speckle showed black, and Rf value is 0.38; Not having other speckle on the used lamellae shows.
Embodiment 4(being used for evaluation) to Chinese crude drug or Chinese patent medicine
Getting falcarindiol, accurate claim surely, with the acetonitrile dissolving and be made into the solution of 2.0mg/ml, draw 30 μ l, put on silica gel thin-layer plate, be developing solvent with petroleum ether (60-90 ℃)-acetone (3: 1), launch, and exhibition distance: 8cm, taking-up is dried; Spray is with 5% ethanol solution of sulfuric acid, and after drying, 105 ℃ of bakings 5 minutes, speckle showed black, R
fValue is 0.40; Not having other speckle on the used lamellae shows.
Embodiment 5(being used for evaluation) to Chinese crude drug or Chinese patent medicine
Getting falcarindiol, accurate claim surely, with the acetonitrile dissolving and be made into the solution of 2.0mg/ml, draw 30 μ l, put on silica gel thin-layer plate, be developing solvent with petroleum ether (60-90 ℃)-acetone (4: 1), launch, and exhibition distance: 8cm, taking-up is dried; Spray is with 5% ethanol solution of sulfuric acid, and after drying, 105 ℃ of bakings 5 minutes, speckle showed black, R
fValue is 0.40; Not having other speckle on the used lamellae shows.
Claims (2)
1. the application of falcarindiol in preparation treatment inflammatory painful diseases medicine, described inflammatory painful diseases is headache.
2. application as claimed in claim 1, described headache is a migraine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2006100274219A CN1857237B (en) | 2006-06-08 | 2006-06-08 | New use of falcarindiol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2006100274219A CN1857237B (en) | 2006-06-08 | 2006-06-08 | New use of falcarindiol |
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| CN1857237A CN1857237A (en) | 2006-11-08 |
| CN1857237B true CN1857237B (en) | 2010-12-01 |
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| CN2006100274219A Expired - Fee Related CN1857237B (en) | 2006-06-08 | 2006-06-08 | New use of falcarindiol |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN113812400A (en) * | 2021-11-06 | 2021-12-21 | 刘春玲 | Cryopreservation protection solution for constructing umbilical cord mesenchymal stem cell bank and construction method of cell bank |
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Non-Patent Citations (2)
| Title |
|---|
| 杜艳芬等.偏头痛患者血浆一氧化氮和镁含量测定及发病机制探讨.天津药学30 11.2002,30(11),650-652. |
| 杜艳芬等.偏头痛患者血浆一氧化氮和镁含量测定及发病机制探讨.天津药学30 11.2002,30(11),650-652. * |
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