CN106420875A - Application of gymnema sylvestre schult fruits in anti-inflammatory drug and composition of application of gymnema sylvestre schult fruits - Google Patents
Application of gymnema sylvestre schult fruits in anti-inflammatory drug and composition of application of gymnema sylvestre schult fruits Download PDFInfo
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Abstract
The invention discloses application of gymnema sylvestre schult fruits in an anti-inflammatory drug and a composition of the application of the gymnema sylvestre schult fruits in the anti-inflammatory drug. The composition of the application of the gymnema sylvestre schult fruits in the anti-inflammatory drug is characterized in that the composition contains the gymnema sylvestre schult fruits having an anti-inflammatory effect, and the gymnema sylvestre schult fruits exist in a form of gymnema sylvestre schult fruit water extract or gymnema sylvestre schult fruits and 70-percent alcohol total extract. The anti-inflammatory action of the gymnema sylvestre schult fruit water extract and the gymnema sylvestre schult fruits and 70-percent alcohol total extract is researched by using xylene, a glacial acetic acid and carrageenan as pro-inflammatory cytokines, a result shows that mouse auricle swelling reaction caused by the xylene can be inhibited by the gymnema sylvestre schult fruit water extract and the gymnema sylvestre schult fruits and 70-percent alcohol total extract, increment of mouse peritoneal vascular permeability induced by the glacial acetic acid can be reduced, mouse toe swelling caused by the carrageenan can be inhibited, an anti-inflammatory effect is obtained, fewer adverse effects exist after taking the composition, and the safety is better; an extracting method and an extracting preparation method in the invention are simple in operation and easy to understand.
Description
Technical field
The invention belongs to technical field of traditional Chinese medicines is and in particular to a kind of application in anti-inflammatory drug for gymnema sylvestre fruit and its application
Composition.
Background technology
Gymnema sylvestre is trailing plants section Gymnema plant, also known as australian cowplant root or leaf, goat's horn, Smilax china L, is distributed widely in India, print
Buddhist nun, Africa, Vietnam and China Guangdong, Guangxi, Fujian, Taiwan and Yunnan Province, it is mild-natured, bitter, and complete stool is used as medicine, and has heat-clearing solution
The effects such as poison, muscle-growing and detumescence, wind-expelling pain-stopping.Modern pharmacological research shows, gymnema sylvestre has hypoglycemic, reducing blood lipid, anti-caries tooth, suppression
Sweet taste reaction processed, antiviral, antiallergy etc. act on.It has been developed into antidiabetic medicine such as gymnema sylvestre compound granules, hypoglycemic soup
Deng.Research both domestic and external is limited only to the research to Gymnema latifolium Wall. ex Wight at present, also few to the research report of its stem, but is at present
Only, also not having about there is the relevant report that antiinflammatory action is studied to its fruit and gymnema sylvestre fruit, especially changing in its fruit
The research studying point still belongs to blank, therefore in order to make full use of gymnema sylvestre each position resource, necessary in prior art
Technically, develop the pharmaceutical usage of gymnema sylvestre fruit.
Content of the invention
The present invention is directed to problem above, it is an object of the present invention to provide a kind of gymnema sylvestre fruit is applied in anti-inflammatory drug and its should
Composition, can make full use of gymnema sylvestre each position resource, the pharmaceutical usage of exploitation gymnema sylvestre fruit, and the effect developed
Good, bad reaction is low.
In order to achieve the above object, the present invention is realized in：
A kind of application in anti-inflammatory drug for gymnema sylvestre fruit.
The composition of application in anti-inflammatory drug for a kind of gymnema sylvestre fruit as mentioned above, anti-containing having in described composition
The gymnema sylvestre fruit of scorching effect.
Further, described gymnema sylvestre fruit is gymnema sylvestre fruit Aqueous extracts or the gymnema sylvestre fruit total medicinal extract of 70% ethanol,
Further, the main matter that described gymnema sylvestre fruit has antiinflammatory action is amyrin cinnamic acid ester and lupin
Alcohol cinnamic acid ester.
Further, the preparation method of described gymnema sylvestre fruit Aqueous extracts is：Will be broken for gymnema sylvestre fruit, leaching is then repeated
Bubble, boils at least 3 times, cold filtration, carries out being concentrated into dilute cream shape, obtain final product gymnema sylvestre fruit Aqueous extracts after taking filtrate.
Further, described immersion is the water at the total amount top adding and there just be not gymnema sylvestre fruit；Described broken granularity
For≤1cm.
Further, the preparation method of the described gymnema sylvestre fruit total medicinal extract of 70% ethanol is：Gymnema sylvestre fruit is successively shone
Dry, pulverize after add volumetric concentration to be to carry out refluxing extraction after 70% ethanol soaks, repeatedly extract at least 20 times and collect afterwards and extract
Liquid, the extract obtaining successively is obtained medicinal extract, the total medicinal extract of as 70% ethanol again after decompression recycling ethanol, concentration, drying.
Further, the described amount adding volumetric concentration to be 70% ethanol is just there be not the total amount top of gymnema sylvestre fruit；Institute
State moisture content≤5% drying；The granularity of described pulverizing is≤1cm.
The formulation that a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit is made as mentioned above, composition is added
Country and professional standard and regulation allow the auxiliary material adding, and can be made into tablet, capsule, pill, granule, paste, injection
And spray.
The medicine being related in the present invention all can purchased on the market.
Compared with prior art, beneficial effects of the present invention are：
1. the present invention passes through paraxylene, glacial acetic acid and carrageenan as pro-inflammatory cytokine research gymnema sylvestre fruit Aqueous extracts and
The antiinflammatory action of the total medicinal extract of 70% ethanol, result shows that gymnema sylvestre fruit Aqueous extracts and the total medicinal extract of 70% ethanol all can suppress caused by dimethylbenzene xylene
The auricle edema reaction of mouse, reduces increasing of the mouse peritoneal vasopermeability that glacial acetic acid induces, and suppression carrageenan causes little
The toes swelling of mouse, has preferable antiinflammatory action, and takes that bad reaction is lower, and security is more preferable；And experimental result table
Bright, gymnema sylvestre fruit Aqueous extracts and the total medicinal extract of 70% ethanol all can reduce the inflammatory exudate PGE2 that carrageenan causes mouse swelling foot,
Recover the SOD vigor of inflammation mouse, reduce MDA content, the antiinflammatory action of prompting gymnema sylvestre fruit Aqueous extracts and 70% ethanol extract can
Can be by suppressing COX approach, blocking synthesis and the release of inflammatory mediator PGs, and be attacked by free radical by reducing body cell
The degree hit, reducing the snperoxiaized degree of body inner lipid and cellular damage, thus reducing inflammatory reaction, reaching the effect of anti-inflammatory
Really.SOD plays vital effect to the oxidative and anti-oxidative balance of body, and this enzyme can remove ultra-oxygen anion free radical
（O2-）, protect cells from damaging, the height indirect reaction of SOD vigor body removes the ability of free radical；The amount of MDA is usually
The snperoxiaized degree of body inner lipid can be reflected, indirectly reflect that body cell is attacked, by free radical, the order of severity damaged.
This measuring carrageenan causes mouse swelling foot PGE2, MDA content and SOD activity, and the present invention passes through gymnema sylvestre fruit anti-inflammatory
The evaluation experimental of activity, test result indicate that：Gymnema sylvestre fruit Aqueous extracts and the total medicinal extract of 70% ethanol all can reduce carrageenan cause little
The inflammatory exudate PGE2 of mouse swelling foot, recovers the SOD vigor of inflammation mouse, reduces MDA content, points out gymnema sylvestre fruit Aqueous extracts
May be by suppressing COX approach with the antiinflammatory action of 70% ethanol extract, block synthesis and the release of inflammatory mediator PGs, and lead to
Crossing and reduce the degree that body cell is attacked by free radical, reducing the snperoxiaized degree of body inner lipid and cellular damage, thus dropping
Low inflammatory reaction, reaches the effect of anti-inflammatory.
2. in the present invention, extracting method and medicinal extract preparation method are simple to operate, understandable, and used molten in preparing medicinal extract
The ethanol of 70% concentration has only been used in agent, and solvent is prepared simply, and the application adopts direct refluxing extraction simultaneously, is not required to ooze for a long time
Filter and dip operation, the time is short, efficiency high.
Brief description
Fig. 1 is amyrin cinnamic acid ester infrared spectrogram of the present invention；
Fig. 2 is amyrin cinnamic acid ester EI-MS collection of illustrative plates of the present invention；
Fig. 3 is amyrin cinnamic acid ester of the present invention13C-NMR and DEPT composes；
Fig. 4 is amyrin cinnamic acid ester of the present invention1H-NMR composes；
Fig. 5 is lupeol cinnamic acid ester infrared spectrogram of the present invention；
Fig. 6 is lupeol cinnamic acid ester EI-MS collection of illustrative plates of the present invention；
Fig. 7 is lupeol cinnamic acid ester of the present invention13C-NMR and DEPT composes；
Fig. 8 is lupeol cinnamic acid ester of the present invention1H-NMR composes.
Specific embodiment
The present invention will be further described with specific embodiment below in conjunction with the accompanying drawings, but protection scope of the present invention is not limited to
Embodiment.
Embodiment 1：
Gymnema sylvestre fruit is cleaned and smashs into sposh shape to pieces, that is, obtain gymnema sylvestre fruit active compound.Directly smeared using the active compound obtaining
To inflamed wound, often 3 medicines in the sky, were obviously improved after one week.
Embodiment 2：
（1）Gymnema sylvestre fruit particle size after cracking is 1cm, the water being subsequently adding the total amount top just not having gymnema sylvestre fruit soaks
60min, boil 20min, the water being subsequently adding the total amount top just not having gymnema sylvestre fruit soaks 10min, boils 40min, then
The water adding the total amount top just not having gymnema sylvestre fruit soaks 5min, boils 20min, and cold filtration carries out dense after taking filtrate
It is reduced to dilute cream shape, obtain final product gymnema sylvestre fruit Aqueous extracts.
（2）Gymnema sylvestre fruit is successively dried and was not just had gymnema sylvestre to moisture content 5%, grinding particle size for adding after 8mm
The total amount top of fruit, volumetric concentration are that 70% ethanol soaks 10h and then carries out refluxing extraction, and extraction repeatedly is collected afterwards for 3 times and extracted
Liquid, the extract obtaining successively is obtained medicinal extract, the total medicinal extract of as 70% ethanol again after decompression recycling ethanol, concentration, drying.
By gymnema sylvestre fruit Aqueous extracts obtained above, country and professional standard and regulation can be added to allow the auxiliary material of addition,
Can be made into injection or spray.
By total for 70% ethanol obtained above medicinal extract, country and professional standard and regulation can be added to allow the auxiliary material of addition, can
Make tablet, capsule, pill, granule or paste.
Embodiment 3：The evaluation of gymnema sylvestre fruit anti-inflammatory activity
1. experimental technique
1.1 animal used as test
Kun Ming mice, 22～24g, male, regular grade（CV）, carried by Guangxi University of Chinese Medicine's Experimental Animal Center
For.
Animal feeding condition：Room temperature：25±1℃（Air-conditioning）；Relative humidity：70%, freely ingest and drink water, each group feed
Identical with drinking water.
1.1.1 mouse caused by dimethylbenzene xylene ear swelling test
1.1.2 packet and administration
Take male mice, be randomly divided into 8 groups, every group 8, i.e. blank control group；Dexamethasone group；Aqueous extracts are high, medium and low
Dosage group（It is followed successively by：12g crude drug/kg, 6g crude drug/kg, 3g crude drug/kg）, the high, medium and low dosage group of the total medicinal extract of 70% ethanol（According to
Secondary it is：24g crude drug/kg, 12g crude drug/kg, 6g crude drug/kg）, gastric infusion, Dexamethasone group gavage dexamethasone 6mg/kg,
Blank control group gives isopyknic distilled water, successive administration 10d；After last dose 45min, uniform in mouse right ear positive and negative
Only smear dimethylbenzene 20 μ L/, left ear compares, after 15min, de- cervical vertebra puts to death mouse, with 8mm card punch in left and right ear identical
Ear disk is laid at position, is precisely weighed.
1.1.3 Data Processing in Experiment and calculating
Swelling (mg)=auris dextra auricle weight (mg)-left ear auricle weight (mg),
Inhibiting rate (%)=(the average swelling of the average swelling-administration group of blank control group) average swelling of/blank control group
Degree × 100%.
1.2 mouse peritoneal capillary permeability experiments
1.2.1 packet and administration
Take male mice, be randomly divided into 8 groups, every group 8, i.e. blank control group；Dexamethasone group；Aqueous extracts are high, medium and low
Dosage group（It is followed successively by：12g crude drug/kg, 6 crude drugs/kg, 3g crude drug/kg）, the high, medium and low dosage group of the total medicinal extract of 70% ethanol（Successively
For：24g crude drug/kg, 12g crude drug/kg, 6g crude drug/kg）, gastric infusion, Dexamethasone group gavage dexamethasone 6mg/kg, empty
White control group gives isopyknic distilled water, successive administration 10d.After last dose 45min, tail vein injection 0.5% Evans blue
Solution 0.1ml/10g, only, after 15min, de- cervical vertebra puts to death mouse, abdominal cut skin to lumbar injection 0.6% glacial acetic acid 0.2ml/ immediately
Skin, rinses abdominal cavity, collection peritoneal fluid, plus physiological saline to 10ml with 6ml physiological saline lumbar injection, and 3000 revs/min of centrifugations take
Supernatant, with spectrophotometer under wavelength 590nm mensuration absorbance（OD）Value.
1.3 carrageenans cause mouse toes swelling experiment
1.3.1 animal packet and medication
Male mice, is randomly divided into 8 groups, every group 8, i.e. blank control group；Dexamethasone group；High, medium and low dose of Aqueous extracts
Amount group（It is followed successively by：12g crude drug/kg, 6g crude drug/kg, 3g crude drug/kg）, the high, medium and low dosage group of the total medicinal extract of 70% ethanol（Successively
For：24g crude drug/kg, 12g crude drug/kg, 6g crude drug/kg）, gastric infusion, Dexamethasone group gavage dexamethasone 6mg/kg, empty
White control group gives isopyknic distilled water, is administered once daily, continuous 7d.After last dose 1h, every right side of mice toes skin
Lower injection 1% carrageenan 0.05mL, and 60min, 120min, 180min after injection, with the measurement of toes capacity measurer
The toes volume of mouse；Cut normal foot along ankle-joint after 4h and cause scorching foot, weigh, calculate swelling and inhibiting rate.
1.3.2 Carrageenan causes mouse swelling foot PGE2, MDA content and the impact of SOD activity
Take mouse to cause scorching foot and the right foot of Normal group mouse, weigh, shred, be dipped in physiological saline by 10% concentration, leaching
After bubble 2h, centrifugation, take supernatant.Take supernatant 200 μ L, plus 0.5mol/l potassium hydroxide-methanol solution 2mL, in 50 DEG C of water-baths
After isomerization 20min, with methanol dilution to 4mL, measure its absorbance at wavelength 278nm in ultraviolet-visible spectrophotometer
(OD value), represents the growing amount of PGE2；Separately take supernatant, respectively according to superoxide dismutase（SOD）And MDA（MDA）Examination
Detection method in agent box measures SOD activity and MDA content.
2. experimental result
All data add and subtract standard deviation with meanRepresent, between each group, mean difference carries out t with SPSS statistical software
Inspection, the results are shown in Table 1～table 2.
2.1 gymnema sylvestre fruit Aqueous extracts and the gymnema sylvestre fruit total medicinal extract of 70% ethanol（The total medicinal extract of hereinafter referred to as 70% ethanol）To diformazan
Benzene causes the impact of mice auricle swelling
Table 1 gymnema sylvestre fruit Aqueous extracts paraxylene causes the impact of mice auricle swelling
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Table 2 gymnema sylvestre fruit 70% ethanol total medicinal extract paraxylene causes the impact of mice auricle swelling
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Be can be seen that by table 1～table 2：It is little that the gymnema sylvestre fruit total medicinal extract of 70% ethanol of high dose can substantially mitigate caused by dimethylbenzene xylene
Mouse auricle edema reacts, and compared with blank control group, has significant difference（P ＜ 0.05）, in terms of inhibiting rate, each administration group is one
Determine in degree, mice caused by dimethylbenzene xylene auricle edema all can be suppressed to react.
Result shows：Gymnema sylvestre fruit Aqueous extracts and the gymnema sylvestre fruit total medicinal extract of 70% ethanol all can suppress mice caused by dimethylbenzene xylene ear
Wide swelling reaction, wherein gymnema sylvestre fruit 70% ethanol total medicinal extract rejection ability are the strongest；Aqueous extracts and gymnema sylvestre fruit 70% ethanol always soak
The inhibiting rate of cream paraxylene cause mice auricle swelling reaction may be relevant with dosage, reduces with dosage, inhibiting rate reduces.
The impact to mouse peritoneal vasopermeability of 2.2 gymnema sylvestre fruit Aqueous extracts and the total medicinal extract of 70% ethanol
The impact to mouse peritoneal vasopermeability for the table 3 gymnema sylvestre fruit Aqueous extracts
| Group | Number of animals（n） | Dosage（g/kg） | OD value | Inhibiting rate（%） |
| Blank control group | 8 | — | 0.8813±0.2750 | |
| Dexamethasone control group | 8 | 0.006 | 0.5554 ± 0.1698** | 36.97 |
| High dose group | 8 | 13.33 | 0.6060 ± 0.0871* | 31.23 |
| Middle dose group | 8 | 6.65 | 0.7479±0.0751 | 15.13 |
| Low dose group | 8 | 3.33 | 0.7662±0.1580 | 13.06 |
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
The fruit impact to mouse peritoneal vasopermeability for the total medicinal extract of 70% ethanol of table 4 gymnema sylvestre
| Group | Number of animals（n） | Dosage（g/kg） | OD value | Inhibiting rate（%） |
| Blank control group | 8 | — | 0.8813±0.6342 | |
| Dexamethasone control group | 8 | 0.006 | 0.5554 ± 0.1698** | 36.97 |
| High dose group | 8 | 24 | 0.5727 ± 0.1560* | 35.01 |
| Middle dose group | 8 | 12 | 0.8725±0.0964 | 1 |
| Low dose group | 8 | 6 | 0.8802±0.2046 | 0.12 |
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Be can be seen that by table 3～table 4：Dexamethasone group can significantly inhibit acetic acid induction mouse peritoneal vasopermeability in pole
Increase, after giving gymnema sylvestre fruit Aqueous extracts and 70% ethanol extract, abdominal cavity vasopermeability has also obtained to a certain degree mouse
Suppression, the particularly high dose group of Aqueous extracts and 70% ethanol extract, compared with blank control group, have significant difference（P ＜
0.05）.Test result indicate that：Gymnema sylvestre fruit Aqueous extracts and 70% ethanol extract can suppress acetic acid induction mouse peritoneal vascular permeability
Property increase, its inhibiting rate may be relevant with dosage, with dosage reduce, inhibiting rate reduce.
2.3 gymnema sylvestre fruit Aqueous extracts and the impact of 70% ethanol total medicinal extract Carrageenan cause mouse toes swelling
The impact to mouse swelling whole toe volume for the table 5 gymnema sylvestre fruit Aqueous extracts
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
The fruit impact to mouse swelling whole toe volume for the total medicinal extract of 70% ethanol of table 6 gymnema sylvestre
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Table 7 gymnema sylvestre fruit Aqueous extracts Carrageenan causes the impact of mouse toes swelling
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Table 8 gymnema sylvestre fruit 70% ethanol total medicinal extract Carrageenan causes the impact of mouse toes swelling
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Be can be seen that by table 5～table 8：Dexamethasone group can significantly inhibit carrageenan cause mouse toes swelling, with sky in pole
White control group is compared, and has pole conspicuousness difference justice（P ＜ 0.01）；The high dose group of gymnema sylvestre fruit Aqueous extracts and low dose group can be extremely aobvious
Write the growth that suppression carrageenan causes mouse toes swelling volume（P ＜ 0.01）, Aqueous extracts middle dosage and the total medicinal extract of 70% ethanol equal
The growth that carrageenan causes mouse toes swelling volume can be significantly inhibited（P ＜ 0.05）；Gymnema sylvestre fruit Aqueous extracts and the leaching of 70% ethanol
Cream all can significantly inhibit the growth that carrageenan causes mouse swelling lumping weight amount（P ＜ 0.05）.
Test result indicate that：Gymnema sylvestre fruit Aqueous extracts and 70% ethanol extract all can suppress carrageenan to cause mouse toes to swell
Swollen.
2.4 Carrageenan cause mouse swelling foot PGE2, MDA content and the impact of SOD activity
Table 9 Aqueous extracts Carrageenan causes the impact of mouse swelling foot PGE2, SOD activity and MDA content
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Table 10 70% ethanol extract Carrageenan causes the impact of mouse swelling foot PGE2, SOD activity and MDA content
Note：1 is compared with blank control group：* P ＜ 0.05, * * P ＜ 0.01
Be can be seen that by table 9～table 10：Gymnema sylvestre fruit Aqueous extracts and 70% ethanol extract all can reduce carrageenan cause little
The inflammatory exudate PGE2 of mouse swelling foot, compared with Normal group, has pole significant difference（P ＜ 0.01）, can recover simultaneously
Its SOD vigor, reduces MDA content, compared with Normal group, has significant difference（P ＜ 0.05）.
Embodiment 3：
Further, the gymnema sylvestre fruit total medicinal extract of 70% ethanol that Example 1 obtains, after silica gel mixed sample, adopts stone successively
Oily ether, ethyl acetate, n-butanol, 95% alcohol reflux extract, and recycling design concentrates, obtains petroleum ether part medicinal extract, ethyl acetate
Position medicinal extract, n-butanol portion medicinal extract, 95% ethanol position medicinal extract.
Take petroleum ether part medicinal extract, separated with silica gel column chromatography, with petroleum ether-ethyl acetate as eluant, eluent, gradient elution,
40：1 elution fraction, obtains the grease of yellow, and solution first washes away the grease of yellow with petroleum ether, then with acetone repeatedly
It is recrystallized to give white pinniform crystallization, be compound amyrin cinnamic acid ester（β-Amyrin cinnamate）；
Take ethyl acetate extract, separated with silica gel column chromatography, chloroform-methanol gradient elution, with iodine vapor, phosphomolybdic acid ethanol
Solution, vanillic aldehyde-concentrated sulfuric acid solution colour developing inspection is known.100:1 elution fraction, obtains white powder material, cut from cut
Dissolved with ethyl acetate afterwards, silica gel is mixed thoroughly, upper silica gel chromatographic column uses petroleum ether-ethyl acetate gradient elution, 80:1 wash-out portion
Point, obtain a white powder, obtain compound lupeol cinnamic acid ester（lupeol cinnamate）.
To the amyrin cinnamic acid ester in above-described embodiment 3（β-Amyrin cinnamate）With lupeol cinnamic acid
Ester（lupeol cinnamate）The identification carrying out：
1. amyrin cinnamic acid ester（β-Amyrin cinnamate）Identification：
1.1 physical property：White pinniform crystallization, 229～230 DEG C of mp, it is dissolved in petroleum ether, acetone；Water insoluble.
1.2IR (KBr compressing tablet)：1767cm-1Absworption peak shows carbonyl to be existed.
1.3EI-MS（m/z）：556, determine that molecular formula is C in conjunction with its nuclear magnetic data39H56O2.1H-NMR(500MHz,
CDCl3) spectrum, 7.68（1H, d, J=16.0）With 6.44（1H, d, J=16.0）For trans alkene hydrogen, 7.52（2H, m）With 7.38（3H,
m）For 5 fragrant hydrogen, illustrate monosubstituted for a phenyl ring.13C-NMR(500MHz,CDCl3) give a cinnamoyl letter in spectrum
Number：δC166.8th, 119.0,144.2,134.7,128.0,128.8,130.1, therefore infer there is a cinnamoyl structure fragment.Carbon
Remaining in spectrum also have 30 carbon signals, in conjunction with DEPT spectrogram it is known that containing 8 methyl, 10 methylene, 5 first in structure
Base and 6 quaternary carbons are thus it is speculated that be triterpenoid structure.δC145.2 and δC121.7 is the feature ethylene linkage carbon signal of oleanane, is judged as
The triterpene of oleanane type.It can be seen that the structure of this compound is cinnamoyl structure and oleanane structure connects together.Nuclear-magnetism number
According to document report[57]Amyrin cinnamic acid ester（β-Amyrin cinnamate）Data is basically identical, infers this chemical combination
Thing is amyrin cinnamic acid ester（β-Amyrin cinnamate）, structural formula is：
Its nuclear magnetic data ownership is shown in Table 1.1, and explanation is shown in by related collection of illustrative plates
Book accompanying drawing Fig. 1 Fig. 4.
Carbon modal data (500MHz, the CDCl of table 1.1 amyrin cinnamic acid ester3)
2. lupeol cinnamic acid ester（lupeol cinnamate）Identification：
2.1 white powder, are dissolved in petroleum ether and ethyl acetate, insoluble in methyl alcohol, second alcohol and water.
2.2IR (KBr compressing tablet)：1710.39cm-1Absworption peak shows-C=O to be existed, 1639.25cm-1、1495.78cm-1、
1450.39cm-1Absworption peak shows phenyl ring to be existed.
2.3EI-MS（m/z）:556, determine that molecular formula is C in conjunction with its nuclear magnetic data39H56O2.1H-NMR(500MHz,
CDCl3, δ ppm) and spectrum, 7.66（1H, d, J=16.0）With 6.44（1H, d, J=16.0）For trans alkene hydrogen, 7.52（2H, m）With 7.38
（3H, m）For 5 fragrant hydrogen, illustrate monosubstituted for a phenyl ring,13C-NMR(500MHz,CDCl3, δ ppm) spectrum in give one
Cinnamoyl signal：δC166.8th, 119.0,144.2,134.7,128.0,128.8,130.1, therefore infer there is a cinnamoyl structure
Fragment.Remaining in carbon spectrum also have 30 carbon signals, in conjunction with DEPT spectrogram it is known that also containing 7 methyl, 12 methylenes in structure
Base, 6 methines and 5 quaternary carbons, δC151.0 and δC109.4 is the feature branch terminals ethylene linkage carbon signal of lupinane, judges
This compound is the triterpene compound of lupin type.δC28.1st, 16.7,16.2,16.0,14.6,18.0,19.3 is 7 first
The carbon signal of base.Nuclear magnetic data and document report[59]Lupeol cinnamic acid ester data basically identical, infer that this compound is
Lupeol cinnamic acid ester, structural formula is such asIts nuclear magnetic data ownership is shown in
Table 2.1, Figure of description 5～8 is shown in by related collection of illustrative plates.
Carbon modal data (500MHz, the CDCl of table 2.1 lupeol cinnamic acid ester3)
Embodiment of above only technology design to illustrate the invention and feature, its object is to allow and is familiar with technique
People understands present invention and is carried out, and can not be limited the scope of the invention with this, all real according to present invention spirit
Equivalence changes or the change modifying the such as preparation temperature of gymnema sylvestre fruit Aqueous extracts, pressure size, boiling time etc. that matter is made,
All should cover within the scope of the present invention.
Claims (9)
1. application in anti-inflammatory drug for a kind of gymnema sylvestre fruit.
2. a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit according to claim 1 is it is characterised in that combine
The gymnema sylvestre fruit with antiinflammatory action is contained in thing.
3. a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit according to claim 1 is it is characterised in that described
Gymnema sylvestre fruit is gymnema sylvestre fruit Aqueous extracts or the gymnema sylvestre fruit total medicinal extract of 70% ethanol.
4. a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit according to claim 1 is it is characterised in that described
The main matter that gymnema sylvestre fruit has antiinflammatory action is amyrin cinnamic acid ester and lupeol cinnamic acid ester.
5. a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit according to claim 3 is it is characterised in that described
The preparation method of gymnema sylvestre fruit Aqueous extracts is：Will be broken for gymnema sylvestre fruit, immersion is then repeated, boils at least 3 times, cooled
Filter, carries out after taking filtrate being concentrated into dilute cream shape, obtains final product gymnema sylvestre fruit Aqueous extracts.
6. a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit according to claim 5 is it is characterised in that described
Immersion is the water at the total amount top adding and there just be not gymnema sylvestre fruit；Described broken granularity is≤1cm.
7. a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit according to claim 3 is it is characterised in that described
Gymnema sylvestre fruit the total medicinal extract of 70% ethanol preparation method be：Volumetric concentration is added after gymnema sylvestre fruit is successively carried out drying, pulverizes
Carry out refluxing extraction after soaking for 70% ethanol, repeatedly extract at least 20 times and collect extract afterwards, by the extract obtaining again first
Obtain medicinal extract, the total medicinal extract of as 70% ethanol after decompression recycling ethanol, concentration, drying afterwards.
8. a kind of composition of application in anti-inflammatory drug for gymnema sylvestre fruit according to claim 7 is it is characterised in that described
The amount adding volumetric concentration to be 70% ethanol is just there be not the total amount top of gymnema sylvestre fruit；Described moisture content≤5% drying；
The granularity of described pulverizing is≤1cm.
9. the composition of application in anti-inflammatory drug for a kind of gymnema sylvestre fruit as described in any one in claim 2-8 is made
Formulation it is characterised in that：Composition is added country and professional standard and regulation allows the auxiliary material that adds, be used for making tablet,
Capsule, pill, granule, paste, injection and spray.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201610932019.9A CN106420875A (en) | 2016-10-25 | 2016-10-25 | Application of gymnema sylvestre schult fruits in anti-inflammatory drug and composition of application of gymnema sylvestre schult fruits |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110184115A (en) * | 2019-07-04 | 2019-08-30 | 李洪 | Environmentally friendly coolant liquid and preparation method thereof |
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2016
- 2016-10-25 CN CN201610932019.9A patent/CN106420875A/en active Pending
Non-Patent Citations (3)
| Title |
|---|
| JENG-SHIOW LAI等: "Studies on the Constituents of the Fruits of Gymnema alternifolium (Lour.) Merr.", 《PROC. NATL. SCI. COUNC. ROC（A）》 * |
| TOSHIHIRO AKIHISA等: "Anti-Inflammatory and Chemopreventive Effects of Triterpene Cinnamates and Acetates from Shea Fat", 《JOURNAL OF OLEO SCIENCE》 * |
| 甄汉深等: "匙羹藤茎化学成分研究", 《中药材》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110184115A (en) * | 2019-07-04 | 2019-08-30 | 李洪 | Environmentally friendly coolant liquid and preparation method thereof |
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