CN102048993A - Application of galangal extract in preparation of medicine for inhibiting calcium channel - Google Patents
Application of galangal extract in preparation of medicine for inhibiting calcium channel Download PDFInfo
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- CN102048993A CN102048993A CN2009102364779A CN200910236477A CN102048993A CN 102048993 A CN102048993 A CN 102048993A CN 2009102364779 A CN2009102364779 A CN 2009102364779A CN 200910236477 A CN200910236477 A CN 200910236477A CN 102048993 A CN102048993 A CN 102048993A
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Abstract
The invention aims to extend application of a galangal extract which contains galangin and is used to inhibit the calcium channel, in particular TRP (Transient ReceptorPotential) channel, so as to prevent and treat heart cerebrovascular diseases such as atherosclerosis and the like. The TRP channel is a non-selective cation channel and has a close relation with heart cerebrovascular diseases such as atherosclerosis and the like. By inhibiting the activity of TRPC channel of vascular endothelial cells, the vascular function can be improved obviously and the vascular pathological changes of atherosclerosis can be improved obviously too. Chemical protection, antioxidation, antiviral and antibacterial action, anti-cancer effect of galangin are further explored previously and the invention extends the use of the galangal extract to prepare medicine for preventing and treating heart cerebrovascular diseases.
Description
Technical field
The present invention relates to a kind of Rhizoma Alpiniae Officinarum extract that contains galangin and prevent and treat application in the cardiovascular and cerebrovascular diseases medicaments such as hypertension, atherosclerosis in preparation, relate in particular to galangin and pass through to suppress instantaneous sensor cationic channel (transient receptor potential in preparation, and then suppress the application of flow of calcium ions TRP).
Background technology
Instantaneous sensor cationic channel (TRP passage) is a kind of transmembrane protein, and the cation that allows when being activated to comprise calcium ion is striden the film transportation.Different with other calcium channel such as voltage-gated channel and the ligand gated channel cell function that participates in relative specialization, the fascinating part of TRP family is the universality and the multiformity of its potential cell function.The TRP gene is quite conservative in stammbaum, is present in from microorganism to high vertebrates.Its tissue distribution is also very extensive, except the central nervous system, also is distributed in sensory organ and cardiovascular, gastrointestinal tract, breathing, urogenital, hemopoietic, the immune system.In 28 kinds of certified mammal TRP passage hypotypes, have at least 19 kinds to express at vascular endothelial cell.These passages have been participated in multiple vascular function, comprise regulating antiotasis, vascular permeability, participate in the mechanical signal conduction, blood vessel secretory function, angiogenesis, endotheli ocytosis, endothelial cell apoptosis and death or the like.The TRP channel function may cause the unusual of human cardiovascular system unusually.
Discussed the treatment that the TRPC passage is used for cardiovascular and cerebrovascular disease in the WO2006/074802A1 application for patent.It studies show that and utilize gene technology, at the atherosis model of rabbit arterial, and by suppressing vascular endothelial cell TRPC3, TRPC6 and TRPC7 activity, vascular function can obviously improve, and obviously improves atherosclerotic vascular pathological and change.TRPC passage and cardiovascular and cerebrovascular disease such as atherosclerotic the contact have been set up in this research.
Studies have shown that in Atherosclerosis Model, TRPC1 albumen is high expressed in vascular smooth muscle that is damaged and new intima, D.J.Beech etc. utilize the blocking antibody (T1E3) of TRPC1 significantly to reduce the formation of people's saphena new intima of In vitro culture, and endothelial function is not had the obvious suppression effect; Its result of study prompting TRPC1 blocker can suppress vascular smooth muscle cell curing and inner membrance new life, thereby proved the effect of TRPC1 antagonist in treatment blood vessel injury disease, therefore be that target treatment obstructive angiopathy has good prospect [document Biochim Biophys Acta.2007,1772 (8): 907-14.] with TRPC1.The migration, the propagation that studies have shown that TRPC5 and TRPM3 passage and vascular smooth muscle cell are closely related.Smooth muscle cell migration is the important pathological process of diseases such as atherosclerosis, myocardial hypertrophy with propagation.
Rhizoma Alpiniae Officinarum is zingiberaceous plant Rhizoma Alpiniae Officinarum (Alpinia officinarum Hance.) dry rhizome.Be conventional Chinese medicine, have the merit of warming stomach for dispelling cold, pain relieving spasmolytic.Galangin (galangin, 3,5,7 one trihydroxyflavones) is a kind of natural flavonols chemical compound, is one of main effective ingredient of Chinese medicine Rhizoma Alpiniae Officinarum.The pharmacological effect activity of this composition has been carried out big quantity research abroad in recent years, comparatively deep to its exploration of chemical protection effect, antioxidation, antiviral, antibacterial action, antitumor action.Galangin can suppress the contraction of caffeine and the inductive isolated pig smooth muscle of bladder of carbachol, and (document Planta Medica 2005,71 (10): 962-964), its mechanism of action is relevant with the calcium mobilization of smooth muscle.Other there are some researches show that galangin can suppress stupid epinephrine or the inductive isolated rat thoracic aorta of KCL vessel segment are shunk, and galangin may play a role by influencing vascular endothelial function and suppressing flow of calcium ions.
But still not studies show that the inhibitory action of Rhizoma Alpiniae Officinarum, and the purposes of galangin in cardiovascular disease prevention to the TRPC passage.
Summary of the invention
The invention provides the new purposes of Rhizoma Alpiniae Officinarum extract in cardiovascular disease prevention that contains galangin.
Rhizoma Alpiniae Officinarum extract is to the diastole effect of rat chest aorta:
Get SD rat chest aorta myocardium vessel ring, utilize potassium chloride (final concentration 45mmol/L) to stimulate blood vessel to cause the vasoconstriction model, in order to estimate the diastole effect of medicine blood vessel.
Adopt ALC-M in vitro tissue organ experimental system, add KH liquid in the bath as isobaric isosmotic solution.Precision takes by weighing the 2.43mg galangin, adds the dimethyl sulfoxide (DMSO) of 100ul and the KH liquid of 900ul.Be made into the galangin mother solution.The galangin mother solution is become gradient solution by 3 times of gradient dilutions, swash blood vessel in advance with KCL and make its contraction, after stablizing to antiotasis, the administration of accumulative total concentration, per twice administration time be 10min at interval.Final Concentraton gradient is: 3 * 10
-7Mol/l, 1 * 10
-6Mol/l, 3 * 10
-6Mol/l, 1 * 10
-5Mol/l, 3 * 10
-5Mol/l, 9 * 10
-5Mol/l, 2.7 * 10
-4Mol/l, result show that galangin has good vasorelaxation action, and median effective dose is 1.17mmol/L.
Galangin is to the inhibitory action of TRP passage:
Galangin can suppress flow of calcium ions by suppressing TRP albumen.
The activity analysis of TRPC passage may further comprise the steps among the present invention:
(1) cell and the fluorescent dye of expression TRPC passage are hatched jointly
(2) utilize the ion channel activator to stimulate flow of calcium ions, add testing compound then.
Detect change in fluorescence
(3) detect change in fluorescence.
The activity analysis of TRP passage also comprises and utilizes patch clamp technique, the inside and outside ion of full cell currents technology for detection cell to change.
The cell of expression TRPC passage of the present invention comprises HEK293, SMC, Chinese hamster ovary celI etc.Fluorescent dye of the present invention comprises Furo2, Fluo4, Di-4-ANEPPS etc.The ion channel activator comprises gadolinium, pregnenolone, OAG etc.
HEK293 cell transfecting TRPC5cDNA, after the tetracycline screening, cell membrane stability is expressed TRPC5 albumen.Fluorescent dye Fura2 incubated cell is after 1 hour, and galangin alcoholic solution 10 μ M incubated cells 15 minutes add gadolinium 50 μ M as agonist.Carrying out fluorescence concentration at calcium channel high throughput fluorescence analyser Flexstation II384 reads.Accompanying drawing 1 is the inhibitory action figures (Gadolinium 50 μ Ms as agonist) of 10 μ M galangin to the TRPC5 passage.Galangin is 0.2uM to the half-inhibition concentration of TRPC5.
With pregnenolone sulphate 1 μ M is agonist, and galangin 1 μ M solution has the obvious suppression effect to the TRPM3 passage.
The present invention has following advantage: galangin suppresses flow of calcium ions by suppressing the TRPC passage, and then influences the migration and the hypertrophy of endothelial function and smooth muscle cell.Galangin is used for cardiovascular and cerebrovascular disease particularly myocardial ischemia, atherosclerotic control by suppressing the TRPC passage, has brand-new mechanism of action, has a good application prospect.
The specific embodiment
Below in conjunction with specific embodiment the present invention is done further explaination, but do not limit the present invention
The preparation 1 of embodiment 1 Rhizoma Alpiniae Officinarum total flavones
Rhizoma Alpiniae Officinarum 10kg, 10 times of 95% alcohol reflux 2 hours, 8 times of 95% alcohol reflux 1 hour, merge extractive liquid,, reclaim under reduced pressure is to there not being the alcohol flavor.
Equal-volume ethyl acetate extraction 3-4 time (is indication with galangin or flavone color reaction), the combined ethyl acetate extract.Reclaim ethyl acetate, regenerant disperses with 20% ethanol, macroporous resin on the back, and behind 2 column volumes of 30% ethanol elution, 5 column volumes of reuse 70% ethanol elution get the Rhizoma Alpiniae Officinarum total flavones.Extract route and see accompanying drawing 2
The preparation 2 of embodiment 2 Rhizoma Alpiniae Officinarum total flavones
Rhizoma Alpiniae Officinarum 10kg, 10 times of 95% alcohol reflux 2 hours, 8 times of 95% alcohol reflux 1 hour, merge extractive liquid,, reclaim under reduced pressure is to there not being the alcohol flavor.
Last macroporous resin, 5 column volumes of first water eluting, reuse 30% ethanol elution is indication with the flavone color reaction, 5 column volumes of eluting; 5 column volumes of reuse 70% ethanol elution get the Rhizoma Alpiniae Officinarum total flavones.Extract route and see accompanying drawing 3
The preparation of embodiment 3 Rhizoma Alpiniae Officinarum total flavones tablets
Prepare the Rhizoma Alpiniae Officinarum extractive of general flavone according to embodiment 1 described method, the 60-80 mesh sieve is crossed in extract dry back below 80 ℃, gets Rhizoma Alpiniae Officinarum total flavone valid target 200 grams, adds an amount of microcrystalline Cellulose and magnesium stearate, mixing, and dry-pressing becomes 1000.
The preparation of embodiment 4 Rhizoma Alpiniae Officinarum total flavones granules
Prepare the Rhizoma Alpiniae Officinarum extractive of general flavone according to embodiment 1 described method, extract is below 80 ℃ after the drying, get Rhizoma Alpiniae Officinarum total flavone valid target 200 grams, add sucrose 100g, hyprolose 100g, micropowder silica gel 20g, make wetting agent with an amount of 70% ethanol, wet granulation, oven dry, 100 bags of granules are made in packing.
The preparation of embodiment 5 Rhizoma Alpiniae Officinarum total flavones oral liquids
It is an amount of to get distilled water, add Tween-80 and make solution, add Rhizoma Alpiniae Officinarum extractive of general flavone 200g again, heating while stirring makes it dissolving, in addition sucrose 30g, antiseptic are dissolved in distilled water in right amount, under agitation slowly add in the above-mentioned solution, adding distil water is to 1000ML, mixing, filter, be distributed into 200, sterilization gets oral liquid.
Claims (10)
1. a medicine for the treatment of cardiovascular and cerebrovascular disease is characterized in that, it is a kind of Rhizoma Alpiniae Officinarum extract, and wherein the Rhizoma Alpiniae Officinarum total flavones is 50-85%, and galangin content is 5-10%.
2. preparation method for the treatment of cardiovascular and cerebrovascular diseases medicament is characterized in that:
(1) the Rhizoma Alpiniae Officinarum rhizome cleans up, oven dry.
(2) alcohols reflux, extract,, merge extractive liquid,, reclaim under reduced pressure gets extract.After extract adds aqueous dispersion, last macroporous resin, with the ethanol elution remove impurity of 10-30% concentration, reuse 60-80% concentration ethanol eluting gets the Rhizoma Alpiniae Officinarum extractive of general flavone earlier.Reach more than 50% with general flavone content in the ultraviolet method mensuration extract, the content that adopts the HPLC method to measure galangin in the extract reaches more than 5%.
3. preparation method as claimed in claim 2 is characterized in that, the used alcohols of reflux, extract, is ethanol, methanol, ethyl acetate, preferred alcohol.
4. the purposes in the Rhizoma Alpiniae Officinarum extract preparation control cardiovascular and cerebrovascular diseases medicament as claimed in claim 1 is characterized in that the application of Rhizoma Alpiniae Officinarum extract in suppressing the calcium channel medicine.
5. the application of Rhizoma Alpiniae Officinarum extract as claimed in claim 4 is characterized in that: the application of galangin in preparation inhibition calcium channel medicine.
6. the application of galangin as claimed in claim 5 is characterized in that: the application of galangin in preparation inhibition TRP passage medicine.
7. the application of galangin as claimed in claim 6 is characterized in that: the application of galangin in preparation inhibition TRPC passage medicine.
8. the application of galangin as claimed in claim 6 is characterized in that: the application of galangin in preparation inhibition TRPM passage medicine.
9. treatment cardiovascular and cerebrovascular diseases medicament according to claim 1 is characterized in that, described medicine is to have the Rhizoma Alpiniae Officinarum total flavones to add injection or oral agents that pharmaceutic adjuvant is made.
10. the medicine of treatment cardiovascular and cerebrovascular disease according to claim 9 is characterized in that, described oral agents is tablet, capsule, drop pill.
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| CN 200910236477 CN102048993B (en) | 2009-10-29 | 2009-10-29 | Application of galangal extract in preparation of medicine for inhibiting calcium channel |
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| CN 200910236477 CN102048993B (en) | 2009-10-29 | 2009-10-29 | Application of galangal extract in preparation of medicine for inhibiting calcium channel |
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| CN102048993B CN102048993B (en) | 2012-05-30 |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106421589A (en) * | 2016-11-17 | 2017-02-22 | 武汉药谷科技开发有限公司 | Traditional Chinese medicinal effective part for decreasing uric acid as well as preparation method and application thereof |
| WO2021208985A1 (en) * | 2020-04-16 | 2021-10-21 | 江苏苏中药业集团股份有限公司 | USE OF QUERCETIN-3'-O-β-D-GLUCOSIDE AS CALCIUM CHANNEL INHIBITOR |
| CN113651789A (en) * | 2021-08-31 | 2021-11-16 | 广东轻工职业技术学院 | Method for separating galangin from galangal flavone by high performance liquid chromatography |
| CN117180262A (en) * | 2023-11-02 | 2023-12-08 | 西北农林科技大学深圳研究院 | Application of galangin in preparation of shrimp white spot syndrome treatment drug |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101002762A (en) * | 2006-12-26 | 2007-07-25 | 广东药学院 | Application of galangin for treating irritable bowel syndrome, and its extraction method |
-
2009
- 2009-10-29 CN CN 200910236477 patent/CN102048993B/en not_active Expired - Fee Related
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106421589A (en) * | 2016-11-17 | 2017-02-22 | 武汉药谷科技开发有限公司 | Traditional Chinese medicinal effective part for decreasing uric acid as well as preparation method and application thereof |
| WO2021208985A1 (en) * | 2020-04-16 | 2021-10-21 | 江苏苏中药业集团股份有限公司 | USE OF QUERCETIN-3'-O-β-D-GLUCOSIDE AS CALCIUM CHANNEL INHIBITOR |
| CN113651789A (en) * | 2021-08-31 | 2021-11-16 | 广东轻工职业技术学院 | Method for separating galangin from galangal flavone by high performance liquid chromatography |
| CN117180262A (en) * | 2023-11-02 | 2023-12-08 | 西北农林科技大学深圳研究院 | Application of galangin in preparation of shrimp white spot syndrome treatment drug |
| CN117180262B (en) * | 2023-11-02 | 2024-01-26 | 西北农林科技大学深圳研究院 | Application of galangin in preparation of shrimp white spot syndrome treatment drug |
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| CN102048993B (en) | 2012-05-30 |
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