CN101708202B - Medicament for inhibiting asodilatatioin - Google Patents
Medicament for inhibiting asodilatatioin Download PDFInfo
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- CN101708202B CN101708202B CN2009102420374A CN200910242037A CN101708202B CN 101708202 B CN101708202 B CN 101708202B CN 2009102420374 A CN2009102420374 A CN 2009102420374A CN 200910242037 A CN200910242037 A CN 200910242037A CN 101708202 B CN101708202 B CN 101708202B
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- loropetalum
- chinens
- extract
- crude extract
- oliv
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Abstract
The invention relates to a medicament for inhibiting asodilatatioin. A main active component of the medicament is prepared from Loropetalum chinense. Through animal experiments and in vitro experiments on crude extract of the Loropetalum chinense, the crude extract of the Loropetalum chinense is verified to have obvious effect of inhibiting the asodilatatioin, have good safety, and not to influence platelet aggregation of animals or blood coagulation.
Description
Technical field:
The present invention relates to the vasodilative medicine of a kind of inhibition, particularly relate to a kind of medicine with its main effective ingredient of Loropetalum chinens preparation.
Background technology:
Loropetalum chinense (R. Br.) Oliv. has indomitable vitality, extremely strong regeneration, adhesive power naturally, and the phenomenon of mystery is a fusion growth mutually between Loropetalum chinense (R. Br.) Oliv. and the Loropetalum chinense (R. Br.) Oliv. the most.Loropetalum chinens claims to spend in vain Loropetalum chinense (R. Br.) Oliv. again, is a kind of of Loropetalum chinense (R. Br.) Oliv..
Chinese medical theory thinks that Loropetalum chinens has anastaltic effect, the inside and outside wound that can be used for healing, and as convergence or hemorrhage class medicine, clinical traumatic hemorrhage and the hemorrhage and burn due to hot liquid or fire of internal organs of the body official of being used for.
But not seeing has human Loropetalum chinens or its extract to be used to suppress vasodilation or promotes vasoconstrictive purpose.
Summary of the invention:
The objective of the invention is to develop a kind of medicine that uses Loropetalum chinens as feedstock production.
The present invention has found that the extract of Loropetalum chinens or Loropetalum chinens has the vasodilative effect of inhibition, can be used for preparation and suppresses vasodilative medicine.
Said Loropetalum chinens comprises flower, stem, leaf, the branch of Loropetalum chinens plant.
The extract of said Loropetalum chinens is the medicament acceptable solvent is carried out the lixiviate gained to Loropetalum chinens a crude extract.
Said medicine acceptable solvent is selected from the mixture of water, organic solvent or water and organic solvent, and said organic solvent is selected from alcohol, ether or ester.
Extract the used leach extraction method of Loropetalum chinens; Can adopt this area leach extraction method commonly used; Like percolation, steam distillation, circumfluence method, infusion process, supercritical extraction method, ultrasonic extraction, also can adopt the isolating conventional methods of effective ingredients in plant such as post separation, ion exchange.Do not destroy under the prerequisite of active substance composition guaranteeing, make every effort to adopt the process for cleanly preparing of energy-saving and emission-reduction, ecological, environmental protective formula.
The Loropetalum chinense (R. Br.) Oliv. extract is spent in biologic enzymolysis method extractive technique preparation in vain, is to spend the preferred method for distilling of Loropetalum chinense (R. Br.) Oliv. in vain like the method for Chinese patent 200710149826.4.
The idiographic flow that the Loropetalum chinense (R. Br.) Oliv. extract is spent in biologic enzymolysis method extractive technique preparation in vain is: and the raw material sampling analysis detections → raw material examination → degree of depth cleaning → combination bacterium enzymolysis → deactivation before the production line → dynamic warm macerating extraction → cryoconcentration → flash freezing → high speed centrifugation is settlement separate → and spray drying → packing detects → spends in vain the Loropetalum chinense (R. Br.) Oliv. crude extract.
Spend Loropetalum chinense (R. Br.) Oliv. biological wall breaking product in vain with what above-mentioned biological wall breaking method obtained; Adopt dynamic warm macerating method to extract; Extract extractum and remove oil-soluble impuritieses such as chlorophyll earlier with ethanol extract from water precipitation; The reuse decoction and alcohol sedimentation technique is removed water-solubility impurities such as saccharide, and to spending the crude extract initial gross separation purification of Loropetalum chinense (R. Br.) Oliv. in vain, what obtain matters of containing biological activities spends Loropetalum chinense (R. Br.) Oliv. chemistry position in vain.
Carry out the biologic enzymolysis method extractive technique and prepared the comparative observation that the Loropetalum chinense (R. Br.) Oliv. extract is spent in the water extraction preparation of spending Loropetalum chinense (R. Br.) Oliv. extract and routine in vain in vain; The result shows that the effective shell-broken effect of biologic enzymolysis method makes and spends in the Loropetalum chinense (R. Br.) Oliv. extract content of effective in vain and improve that its biochemical action is stronger.
The present invention has carried out following zoopery and experiment in vitro with the Loropetalum chinens crude extract, confirms:
(1) the Loropetalum chinens crude extract to Kallidin I 1,10, under the 100 μ g/mL concentration due to vasodilation all have remarkable vasoconstrictive effect, prove that it has tangible vasodilation inhibitory action.
(2) Loropetalum chinens crude extract single mouse stomach dosage 10g/kg does not see the overt toxicity reaction, belongs to the avirulence material.
(3) the experiment in vitro result shows, the Loropetalum chinens crude extract is not seen under 500 μ g/mL concentration has the effect that promotes platelet aggregation.
(4) the Loropetalum chinens crude extract is not seen obvious influence with continuous 7 days gastric infusions of 200mg/kg to normal clotting time of mice.
Experimental result shows that the Loropetalum chinens extract not only has the vasodilative effect of inhibition, and safety is good.And the anastaltic effect of Loropetalum chinens through promoting that platelet aggregation plays a role, does not therefore influence the animal platelet aggregation, does not influence coagulation function yet.
Loropetalum chinens extract and the acceptable any carrier of medicine, excipient, the adjuvant of above-mentioned treatment effective dose are combined, can be made into and suppress vasodilation or promote vasoconstrictive medicine.
Also can Loropetalum chinens extract and other medicines active component be processed compound medicine according to different situations.
In order to guarantee medicine better therapeutic and more excellent physicochemical character; Also can in medicine, add preparation adjuvant commonly used; Regulate material like antiseptic, permeation-promoter, solubilizing agent, surfactant, PH, those skilled in the art can add according to the needs of different dosage form and use.
Description of drawings:
Fig. 1 spends Loropetalum chinense (R. Br.) Oliv. extract ultraviolet detection chromatogram in vain;
Fig. 2 spends Loropetalum chinense (R. Br.) Oliv. in vain to extract chromatography of ions figure thing;
Fig. 3, Fig. 4, Fig. 5 be respectively the Loropetalum chinens final concentration when being 1 μ g/ml, 10 μ g/ml, 100 μ g/ml to the vasodilatory inhibitory action of Kallidin I.
The left side is a tunnel name among the figure, and the right scale is a tension force numerical value, after the curve representative adds the Loropetalum chinens crude extract among the figure, to vasodilatory contraction behind the preparatory adding Kallidin I.
The specific embodiment
Through embodiment further detailed description is done in experiments such as the leaching process of Loropetalum chinens extract, drug effect, safety below.But the present invention is not limited to the crude extract that this thick kind method is obtained.In fact, Loropetalum chinens suppresses vasorelaxation action with the extract of additive method gained, also within the scope of the invention.
The extraction of embodiment 1 Loropetalum chinens crude extract
Spend the thick thing of Loropetalum chinense (R. Br.) Oliv. in vain with the biologic enzymolysis method extraction.Idiographic flow is: and the raw material sampling analysis detections → raw material examination → degree of depth cleaning → combination bacterium enzymolysis → deactivation before the production line → dynamic warm macerating extraction → cryoconcentration → flash freezing → high speed centrifugation is settlement separate → and spray drying → packing detects → spends in vain the Loropetalum chinense (R. Br.) Oliv. crude extract.
Concrete method for distilling is that it is broken to spend Loropetalum chinense (R. Br.) Oliv. green wood material in vain.Adopt combination bacterium enzyme solution to obtain to spend Loropetalum chinense (R. Br.) Oliv. biological wall breaking product in vain, adopt dynamic warm macerating method to extract (85 ℃ of temperature, time 120m, pH value 6.5 ± 0.2), warm macerating extraction time is 16 hours, obtains extracting extractum.Remove oil-soluble impuritieses such as chlorophyll earlier with ethanol extract from water precipitation, the reuse decoction and alcohol sedimentation technique is removed water-solubility impurities such as saccharide, to spending the crude extract initial gross separation purification of Loropetalum chinense (R. Br.) Oliv. in vain, obtains crude extract, and weight is the 5.5-6% of raw material weight.
The used strain of said combination bacterium enzymolysis is Dutch strain spore, derives from Jingde plate chicken yeast powder, is produced by Jingde, Jiangxi plate chicken industrial corporation.
The Dutch strain spore of former strain is unique strain that does not produce enterotoxin, through cultivating, in the secondary metabolism, isolates D429, and process is the meat soup slant culture.Paraffin wax is sealed after 2 months separating thallus once more up for safekeeping, and the group amplification culture, and then separates, and after expand the crowd, extracts its of algae floating life, is lyophilized into active thalline powder.(bacterium culture medium is a bouillon agar etc.).
The present invention has carried out the biologic enzymolysis method extractive technique and has prepared the comparative observation that the Loropetalum chinense (R. Br.) Oliv. extract is spent in the water extraction preparation of spending Loropetalum chinense (R. Br.) Oliv. extract and routine in vain in vain; The result shows that the effective shell-broken effect of biologic enzymolysis method improves the content of spending above-mentioned three constituents in the Loropetalum chinense (R. Br.) Oliv. extract in vain, and its biochemical action is stronger.
Embodiment 2 spends Loropetalum chinense (R. Br.) Oliv. chemical constituent initial analysis report in vain
One, sample preparation
The smart title, slightly carried powder 1.06mg, and the 1mL50% dissolve with methanol is crossed 0.45 μ m microporous filter membrane, promptly gets.
Two, chromatographic condition
High performance liquid chromatograph: Agilent 1200 series of high efficiency chromatograph of liquid (U.S. Agilent Technologies company) comprise PDAD, quaternary gradient pump, online degasser, automatic sampler.
Chromatographic column: YMC-Pack Pro C
18(150mm * 3.0mm ID, 5 μ m);
Mobile phase: A (methanol), B (0.1% formic acid H
2O)
Gradient elution (0 → 35min, A:10% → 98%; 35min-40min, A:98% → 98%; );
Flow velocity 0.3mL/min;
UV scanning scope: 200-400nm;
Detect wavelength: 200-400nm; Column temperature: 40 ℃.
Three, mass spectrum condition
1, mass spectrograph: QTRAP
TMType quadrupole rod-linear ion hydrazine tandem mass spectrometer (Applied Biosystems/MDSSCIEX, USA), ion source: the ESI source of adopting the anion detecting pattern.
2, LC-MS condition determination:
Scan?Type Enhanced?MS(EMS)
Polarity Negative
Scan?Mode Profile
Ion?Source Turbo?spray
Scan?Rate： 4000Da/s
LIT?fill?time 80.00msec
Q3?Entry?Barrier 8.00V
Curtain?Gas(CUR) 25.00
CAD High
lonspray?Voltage(IS) -4.5kV
TEM 350.00
Nebulizer?Gas(GS1) 70
Source?Gas?2(GS2) 60
ihe： ON
Declustering?Potential(DP) -80V
Entrance?Potential(EP) -10V
Collision?Energy(Experiment?1)?-10V
Collision?Energy(Experiment?2)?-40eV
Table 1 is spent the Loropetalum chinense (R. Br.) Oliv. main chemical compositions in vain
| t R(min) | [M-H] - (m/z) | Production | Molecular formula | The chemical compound title |
| 13.97 | 353.2 | 191.0，179.0， 173.0 | C 16H 18O 9 | Chlorogenic acid |
| 16.44 | 337.2 | 191.2 | C 13H 22O 10 | Quinic acid+rhamnose |
| 17.42 | 415.2 | - | C 21H 20O 9 | Apigenin-O-glucoside |
| 18.49 | 477.1 | 313.2 | C 22H 22O 12 | Isorhamnetin-3-O-glucoside |
| 19.50 | 479.3 | 316.0 | C 21H 20O 13 | Ampelopsin-3-O-glucoside |
| 20.69 | 463.2 | 316.1 | C 21H 20O 12 | Ampelopsin-3-O-rhamnoside |
| 21.36 | 463.2 | 301.0 | C 21H 20O 12 | Quercetin-7 (3)-O-glucoside |
| 22.12 | 599.2 | 447.1，313.2 | C 28H 24O 15 | Astragaloside-2 (6)-O-epicatechol gallate |
| 22.83 | 447.2 | 285.1 | C 21H 20O 11 | Kaempferol (luteolin)-3 (7)-O-glucoside |
| 23.14 | 447.2 | 301.1 | C 21H 20O 11 | Quercetin-O-rhamnoside |
| 25.07 | 431.2 | 285.1 | C 27H 30O 15 | Kaempferol (luteolin)-O-rhamnoside |
| 25.95 | 301.2 | - | C 15H 10O 7 | Quercetin |
| 26.38 | 593.0 | 285.1 | C 27H 30O 15 C 30H 26O 13 | Luteolin (kaempferol)-7-O-rutinoside kaempferol-3-(6 "-to the hydroxyl cinnamyl)-glucoside |
| 28.42 | 285.1 | - | C 15H 10O 6 | Kaempferol (luteolin) |
Embodiment 3 Loropetalum chinens crude extracts are to the influence of vasorelaxation action due to the rat BK
One, material
Animal: the Wistar rat, male, body weight 250g, Institute of Experimental Animals, Chinese Academy of Medical Sciences provides, the quality certification number, SCXK (capital) 2008-0004.
Receive test product: the Loropetalum chinens crude extract, brown powder shape solid is provided by Deyu Group Corp. Jiangxi Prov..Face with preceding and be configured to desired concn with normal saline.
Liquid is used in experiment:
1) KH liquid (adds NaCl:13.7918g successively in the 2000ml distilled water; KCl:0.7008g; CaCl2:0.56605g; Anhydrous MgSO4:0.2841g; KH2PO4:0.3212g; NaHCO3:4.1803g; Glucose:4.3994g.Application of sample is magnetic agitation simultaneously, and is subsequent use)
2) final concentration is the Kallidin I of 3 μ mol/L, with the normal saline preparation, is stored in-20 ℃;
3) final concentration is the Klorvess Liquid of 60mmol/L.
Two, method
1) uses the pentobarbital sodium anesthetized rat; Take out the thoracic aorta section rapidly, be fixed in the cake wax that contains pre-cooling KH liquid, remove blood vessel connective tissue and fat on every side; Be cut into the long vascular strip of about 3-4mm; Overlap respectively on two triangular wire hooks, one of them is fixed in the bottom of bath, and another connects tension transducer.
2) regulate the load that tension transducer gives vascular strip 0.5g, stablize the load that gives 1g after 15 minutes again, stablize the load that gives 1.5g after 15 minutes again, stablize the load that gives 2g after 15 minutes again, begin test after steadily.Changed one time KH liquid in per during this time 10 minutes.
3) the stable back adding of vascular strip 200ulKCl solution makes vasoconstriction; When reaching the balance backlash, contraction cleans KCl; Again adjustment of tonicity is 2 grams, and steadily back adding 30ul final concentration is 3 μ mol/L Kallidin I solution once more, when diastole reaches maximum; Adding receives test product after steadily about half an hour, detects the easypro situation that contracts of blood vessel after about 30 minutes.Calculate the vasoconstriction suppression ratio of medicine.Each concentration receives test product must detect the suppression ratio of 3 groups (vascular strips of different rat same positions), averages.Computing formula is:
Three, result
Table 2 Loropetalum chinens crude extract is to vasoconstrictive influence (n=3) due to the Kallidin I
| Loropetalum chinens crude extract concentration (μ g/ml) | Suppression ratio (%) |
| 100 | 90.67±1.63 |
| 10 | 38.08±4.74 |
| 1 | 38.12±11.7 |
Fig. 3, Fig. 4, Fig. 5 be the Loropetalum chinens crude extract when final concentration is respectively 1 μ g/ml, 10 μ g/ml and 100 μ g/ml to the vasodilatory inhibitory action of Kallidin I.Measure Acq373 software analysis, record gained image with the BioPac polygraph.The left side is a tunnel name among the figure, and the right scale is a tension force numerical value, after the curve representative adds the Loropetalum chinens crude extract among the figure, to vasodilatory contraction behind the preparatory adding Kallidin I.
Four, conclusion
Given the test agent Loropetalum chinens crude extract has the obvious suppression effect, suppression ratio 90.67 ± 1.63% to vasodilation due to the Kallidin I under 100 μ g/ml concentration; It is also inhibited under 10 μ g/ml and 1 μ g/ml concentration, and suppression ratio is about 38%, but this inhibitory action is not seen concentration dependent.
Embodiment 4 Loropetalum chinens crude extracts are to the influence (experiment in slide method-body) of clotting time of mice
One, material
Receive test product: the Loropetalum chinens crude extract, brown powder shape solid is provided by Deyu Group Corp. Jiangxi Prov..Face the solution for standby that is mixed with desired concn with distilled water with preceding.
Animal: Kunming mouse, body weight 18 20g, male, available from Institute of Experimental Animals, Chinese Academy of Medical Sciences, credit number: SCXK (capital)-2007-0001.
Two, method
Animal is divided into 2 groups at random, 10 every group, is respectively normal control group, Loropetalum chinens crude extract 200mg/kg group.Administration group every morning gastric infusion once, the administration volume is 0.1ml/10g, successive administration 7 days, the normal control group gives the equal-volume distilled water.Half an hour after administration in the 7th day, get blood by mice right eye venous plexus.Each one is bled in the microscope slide two ends, and the about 5mm of drop of blood diameter uses manual time-keeping immediately.Whenever provoked once gently inwards from the drop of blood edge with the cleaning pin at a distance from 30 seconds, and observation has or not the blood streak to provoke.Begin to end from blood sampling, be clotting time between institute lasts to provoking the blood streak.Another is bled and supplies last the reinspection.The record clotting time is done the mean test of significance.
Data analysis: data represent that with mean+SD data analysis is taked t check between group.
Three, result
Compare Loropetalum chinens crude extract (117.3 ± 28.3 seconds) group unknown significance difference (P＞0.05) (seeing table 3) with normal control group clotting time of mice (153.6 ± 83.1 seconds).
Table 3 Loropetalum chinens crude extract is to the influence of clotting time of mice (mean ± SD)
| Group | Sample number | Dosage (mg/kg) | PCT (S) |
| The |
10 | —— | 153.6±83.1 |
| The Loropetalum chinens |
10 | 200 | 117.3±28.3 |
*P＜0.01 is compared with model control group;
Four, conclusion
The Loropetalum chinens crude extract is not seen obvious influence with continuous 7 days gastric infusions of 200mg/kg to normal clotting time of mice.
Embodiment 5 Loropetalum chinens crude extracts are to the in vitro study that influences of rat platelet aggregation function
One, material
1, receive test product: the Loropetalum chinens crude extract, brown powder shape solid is provided by Deyu Group Corp. Jiangxi Prov..
2, reagent: pentobarbital sodium, available from ancient cooking vessel state Bioisystech Co., Ltd, specification: 25g, lot number: 76I10203; Sodium citrate, Beijing Chemical Plant's product, lot number: 20000809, distilled water is mixed with 3.8% solution; Thrombin of beef, specification: 1000U, Sigma Company products import packing product, solid powdery is prepared 100U/ml with normal saline ,-20 ℃ of preservations after the packing; Medical saline, available from Shijiazhuang Siyao Co., Ltd's product, lot number: 080904110.
3, instrument: the desk-top high capacity centrifuge of flying pigeon board TDL-40B type low speed, Beijing science equipment company limited is produced; LBY-NJ4 type platelet aggregation instrument, Li Pusheng company in Beijing produces; Stopwatch etc.
Two, method
1, anesthesia: get male SD rat, 280-300g, 1.5% pentobarbital sodium anesthesia (dosage is 0.4ml/100g).2, get blood: abdominal aortic blood, the anticoagulant in 9: 1 by volume of 3.8% sodium citrate.
2, hematoblastic preparation: get upper strata ecru suspension behind the centrifugal 10min of whole blood 1200r/min, be platelet rich plasma (PRP), get the upper strata stillness of night behind the centrifugal 10min of residue blood plasma 3000r/min, be platelet poor plasma (PPP).With PPP platelet counts among the PRP being adjusted to instrument shows between the absorbance 300-400.
3, the mensuration of platelet maximum agglutination rate:
(1) the Loropetalum chinens crude extract gathers effect to hematoblastic directly urging: in cuvette, add 300 μ l PPP adjustment instrument zero; Other gets cuvette and adds stirrer and 300 μ l PRP successively; Preparatory temperature 5min; After adding receives test product (the system final concentration is 500 μ g/mL), thrombin (the system final concentration is 6.4U/mL) or normal saline 20 μ l respectively, platelet maximum agglutination rate in the immediate record 5min.
(2) Loropetalum chinens crude extract and thrombin Combined application are gathered effect to platelet is short: in cuvette, add 300 μ l PPP adjustment instrument zero; Other gets cuvette and adds stirrer, 300 μ l PRP and normal saline successively or receive test product 15 μ l (the system final concentration is 500 μ g/mL); Add 10 μ l thrombins (the system final concentration is 3.2U/ml) behind the incubation 5min, platelet maximum agglutination rate in the record 5min.
4, data analysis
Data represent that with mean+SD data analysis is taked t check between group.
Three, result
1, receive test product to the hematoblastic directly short effect research that gathers
Compare with the normal saline group, Loropetalum chinens crude extract group is to platelet maximum agglutination rate no difference of science of statistics.In addition, the platelet maximum agglutination rate of Loropetalum chinens and normal saline group all significantly is lower than the thrombin group.Explain that 500 μ g/mL Loropetalum chinens and normal saline all can not directly cause significant platelet aggregation, do not have the effect of short platelet aggregation.
See table 4.
Table 4 Loropetalum chinens crude extract list is used the influence to the rats in vitro platelet aggregation
| Group | n | Concentration | Maximum agglutination rate (%) |
| Normal saline | 3 | —— | 25.45±8.43 * |
| The Loropetalum chinens crude extract | 3 | 500μg/mL | 8.23±9.71 * |
| Thrombin | 3 | 6.4U/mL | 86.93±12.64 |
*Compare P＜0.001 with the thrombin group.
2, receive test product and thrombin that platelet is united the short effect research that gathers
Table 5 Loropetalum chinens crude extract and thrombin Combined application are to the influence of rats in vitro platelet aggregation
| Group | n | Concentration (μ g/mL) | Maximum agglutination rate (%) |
| Normal saline+thrombin | 3 | —— | 65.94±6.6 |
| Loropetalum chinens crude extract+thrombin | 3 | 500 | 66.26±4.4 |
Compare with the normal saline group, Loropetalum chinens crude extract group and thrombin Combined application are used hematoblastic maximum agglutination rate no difference of science of statistics.Explain that 500 μ g/mL Loropetalum chinens crude extracts and thrombin synergy can not significantly promote platelet aggregation.
Four, conclusion
This experiment proof Loropetalum chinens crude extract all has remarkable vasoconstrictive effect 1,10 under the 100 μ g/mL concentration.This experimentation the influence of Loropetalum chinens crude extract to platelet aggregation, experimental result shows, the Loropetalum chinens crude extract is not seen under 500 μ g/mL concentration has the effect that promotes platelet aggregation.Infer that in view of the above the anastaltic effect of Loropetalum chinens maybe be through not promoting that platelet aggregation plays a role.
Embodiment 6 Loropetalum chinens crude extract mice single-dose acute toxicity preliminary tests
One, purpose
Adopt maximum dosage method, irritate the stomach Loropetalum chinens, observe poisoning symptom, degree of intoxication, character, recovery situation and death etc. that mice occurs through the mice single.
Two, material
Receive test product: the Loropetalum chinens crude extract, brown ceramic powder, soluble in water; Provide by Deyu Group Corp. Jiangxi Prov..Face the solution for standby that is mixed with desired concn with distilled water with preceding.
Animal: Kunming mouse, body weight 18 20g, male and female half and half, available from Institute of Experimental Animals, Chinese Academy of Medical Sciences, credit number: SCXK (capital)-2007-0001.
Two, method
According to the maximum dosage-feeding method, use 40 mices, male and female half and half, each 20 of blank group and administration groups.The administration group gives suitable administration concentration (concentration is 0.25g/ml) with maximum administration volume (0.4ml/10g body weight), and dosage is 10g/kg, and matched group gives the distilled water with volume.Itemized record administration animal on same day performance is cutd open inspection to dead animal, observes 14 days behind the survival medicine, cuts open inspection on the 15th day.
Four, result
There is not dead mouse after the Loropetalum chinens administration; Do not see after the administration that mice has unusual performance, mice all movable normal, hair color is smooth, food ration is normal, feces is normal, weight increase, gross necropsy no abnormality seen (seeing Fig. 2-5).Write down the mice body weight every day after the administration, and the result sees table 5.
Table 5 Loropetalum chinens single-dose toxicity test the weight of animals record (g) (n=10)
Five, conclusion
Under this experimental condition, the LD50 of single gastric infusion Loropetalum chinens does not see death and ANOMALOUS VARIATIONS greater than 10g/kg, receives test product Loropetalum chinens extract to belong to the avirulence material.
Claims (4)
1. one kind is suppressed vasodilative medicine, and its active component is the Loropetalum chinens extract; Said Loropetalum chinens extract is that Loropetalum chinens green wood material is broken, adopts combination bacterium enzyme solution to obtain Loropetalum chinens biological wall breaking product, adopts dynamic warm macerating method to extract 16 hours, obtains extracting extractum; Remove oil-soluble impuritieses such as chlorophyll earlier with ethanol extract from water precipitation, the reuse decoction and alcohol sedimentation technique is removed water-solubility impurities such as saccharide, to the crude extract initial gross separation purification of Loropetalum chinens, obtains crude extract, and weight is the 5.5-6% of raw material weight.
2. the Loropetalum chinens extract suppresses vasodilation or promotes the purposes in the vasoconstriction medicine in preparation; Said Loropetalum chinens extract is that Loropetalum chinens green wood material is broken, adopts combination bacterium enzyme solution to obtain Loropetalum chinens biological wall breaking product; Adopt dynamic warm macerating method to extract 16 hours, obtain extracting extractum; Remove oil-soluble impuritieses such as chlorophyll earlier with ethanol extract from water precipitation, the reuse decoction and alcohol sedimentation technique is removed water-solubility impurities such as saccharide, to the crude extract initial gross separation purification of Loropetalum chinens, obtains crude extract, and weight is the 5.5-6% of raw material weight.
3. the described purposes of claim 2, said Loropetalum chinens is selected from flower, stem, leaf, the branch of Loropetalum chinens.
4. the described purposes of claim 2, the used strain of said combination bacterium enzymolysis is Dutch strain spore.
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