CN102440984A - Application of dried orange peel polymethoxylated flavonoids in preparation of gastrointestinal power promoting medicines - Google Patents
Application of dried orange peel polymethoxylated flavonoids in preparation of gastrointestinal power promoting medicines Download PDFInfo
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- CN102440984A CN102440984A CN2011101560312A CN201110156031A CN102440984A CN 102440984 A CN102440984 A CN 102440984A CN 2011101560312 A CN2011101560312 A CN 2011101560312A CN 201110156031 A CN201110156031 A CN 201110156031A CN 102440984 A CN102440984 A CN 102440984A
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- pericarpium citri
- polymethoxyflavone
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Abstract
The invention discloses application of dried orange peel polymethoxylated flavonoids in preparation of gastrointestinal power promoting medicines, and relates to the technical field of traditional Chinese medicine active site separation and application. The dried orange peel is an important medicine for regulating the flow of qi and strengthening the spleen, and can be used as both a medicine and a food. The animal experiment indicates that the dried orange peel polymethoxylated flavonoids have stronger actions on promoting gastrointestinal power than domperidone, and have smaller dosage. The dried orange peel polymethoxylated flavonoids have wide application prospects when being used as a novel gastrointestinal power promoting traditional Chinese medicine for treating gastrointestinal power disorder.
Description
Technical field
The present invention relates to the Chinese medicine active site and separate and the purposes technical field, more specifically, relate to the application of Pericarpium Citri Reticulatae polymethoxyflavone compounds in the preparation digestive tract power reinforcing medicine.
Background technology
Gastroenteropathy is one type of commonly encountered diseases and frequently-occurring disease, and its sickness rate is about 60%.Gastrointestinal motility disorder is an aspect of gastrointestinal disease, and gastritis, peptic ulcer and abdominal postoperative often suppress with the gastrointestinal motility function.Some functional gastrointestinal diseases such as anti-fluidity esophageal disease, functional dyspepsia (FD) then are to be main pathological manifestations with gastrointestinal motility disorder.The prevalence of FD accounts for about 50% of Gastroenterology Clinic up to 20 ~ 30% in recent years.
Western medical treatment gastrointestinal motility disorder property disease is to be the short digestive tract power reinforcing medicine of representative with motilium (domperidone), mosapride at present.Cisapride is as the complete once fashionable whole world of digestive tract power reinforcing medicine; But along with its extensive use, finding has serious heart toxic and side effects, and many patients use and occur the Q-T interval behind the cisapride and prolong and arrhythmia; Particularly serious torsades de pointes property ventricular tachycardia; Even cause death, so calendar year 2001 cisapride quit listing because of the serious cardiovascular incident whole world, China has also stopped the sale of this medicine at present.Though the motilium safety is higher, when life-time service, its side effect also is tangible; Like convulsions, muscle spasm, sialorrhea, dysequilibrium, The extrapyramidal symptoms (child Geng Yi generation) such as dizzy; Abdominal cramps, women's lactogenic and gynaecomastia, menoxenia etc.
The Chinese traditional treatment dyspepsia is often used regulating qi-flowing for strengthening spleen class Chinese medicine, and Pericarpium Citri Reticulatae is one of representative drugs of regulating qi-flowing for strengthening spleen, and Pericarpium Citri Reticulatae also is the integration of edible and medicinal herbs kind, has good safety, and this Drug therapy to functional disease is even more important.Pericarpium Citri Reticulatae (
Pericarpium Citri Reticultae) be rutaceae orange (
Citrus reticulataBlanco) and the dry mature skin of variety.Application at China's Pericarpium Citri Reticulatae has long history, and work the beginning is stated from Shennong's Herbal and classifies as top gradely, thinks its " the main heat of crust in the heart, contrary gas, diuretic paddy, the clothes therapeutic method to keep the adverse QI flowing downwards of deodorizing for a long time." record of Li Shizhen (1518-1593 A.D.) Compendium of Material Medica: " the great meaning of the physician Tao Jing of the Southern Song Dynasty ' Pericarpium Citri Reticulatae is treated gas and won completely, and old person of a specified duration is good for palpus ' ", visible regulating the flow of vital energy is the main effect of Pericarpium Citri Reticulatae.Southern china Pericarpium Citri tangerinae aboundresources, but waste is serious, only part is used for clinical prescription and Chinese patent medicine, and its medical value does not fully excavate and exploitation.
Summary of the invention
The object of the present invention is to provide the new application of Pericarpium Citri Reticulatae polymethoxyflavone compounds.
The objective of the invention is to realize like this: the application of Pericarpium Citri Reticulatae polymethoxyflavone compounds in the preparation digestive tract power reinforcing medicine.
Pericarpium Citri Reticulatae polymethoxyflavone compounds according to the invention is one or more mixing of Pericarpium Citri tangerinae element, Nobiletin and Heptamethoxyflavone.
The preparation of Pericarpium Citri Reticulatae polymethoxyflavone chemical compound according to the invention is the plant separation means that adopts active guiding.
The detection of Pericarpium Citri Reticulatae polymethoxyflavone chemical compound according to the invention comprises chemical analysis and bioassay.
The present invention learns that through experiment Pericarpium Citri Reticulatae polymethoxyflavone compounds has good short digestive tract power effect really.Prepared medicine can through promote gastric emptying with intestinal transmission quicken the digestion of food, thereby treatment gastrointestinal motility disorder property disease, like reflux esophagitis, functional dyspepsia, and diseases such as abdominal distention, belch, nauseating, vomiting and abdominal part distending pains.
Specific embodiments
Understand technology contents of the present invention in order more to know, the special following examples of lifting specify.
Embodiment 1.
Ji'an, Jiangxi product citrus reticulata (
C.reticulateCv. Unshiu) peel 500g puts Steam by water bath 0.5h in the aluminum pot, takes out shredding, adds 12 times of water; Decoct 1h, totally 2 times, filter merging filtrate; And be concentrated into 500mL, and add 0.5% dilute hydrochloric acid, transferring PH is 2 ~ 3, with petroleum ether extraction 3 times; Get the about 25g of petroleum ether extract behind the reclaim under reduced pressure petroleum ether, carry out the branch quantitative analysis with ultraviolet spectrophotometry, the polymethoxyflavone kind compound content of sample is 32.7%.Sample detects through ultraviolet spectrophotometry should not contain Neosynephrine; Sample carries out bioassay after with 0.5% tween 80 hydrotropy, and it does not produce obvious inhibitory action to spontaneous contraction of the gastrointestinal smooth muscle that exsomatizes.
Embodiment 2.
The Jiangxi Lignum cinnamomi camphorae produces Pericarpium Citri Reticulatae (deriving from red Fructus Citri tangerinae) 600g, adds 12 times of water, soaks 30min, decocts 1h, and totally 2 times, filter, merging filtrate, and to be concentrated into 500mL be Pericarpium Citri Reticulatae water extract.The water extract adds 0.5% dilute hydrochloric acid, and transferring PH is 2 ~ 3,, with ethyl acetate extraction 3 times, decompression and solvent recovery gets ethyl acetate extract and water-soluble portion.Ethyl acetate extract is used an amount of petroleum ether dissolution, adds equivalent silica gel, mixes thoroughly, the dry method upper prop; Use petroleum ether: ethyl acetate is carried out gradient elution; Eluent reclaims solvent, obtains 2 column chromatography separation components behind the drying under reduced pressure, and wherein component 1, component 2 quality are respectively 1.305g, 1.086g.Carry out the branch quantitative analysis with ultraviolet spectrophotometry, the polymethoxyflavone kind compound content of two samples is for being respectively 58.4%, 55.40%.Sample detects through ultraviolet spectrophotometry should not contain Neosynephrine; Sample carries out bioassay after with 0.5% tween 80 hydrotropy, and it does not produce obvious inhibitory action to spontaneous contraction of the gastrointestinal smooth muscle that exsomatizes.
Below through zoopery the new purposes of Pericarpium Citri Reticulatae polymethoxyflavone compounds of the present invention is described.All data are used
± S representes that statistical comparisons adopts one factor analysis of variance and uses
tCheck is compared between organizing.
The experiment medicine: the Pericarpium Citri tangerinae petroleum ether extract, Pericarpium Citri Reticulatae chromatographic isolation component 1,2 is all used 0.5% tween 80 hydrotropy, faces the time spent and joins at present.
Positive control medicine: motilium, Xian-Janssen Pharmaceutical Ltd., batch number: 10030197; The JUYUANSUNMOSHABILI capsule, friendship Pharmaceutical limited company of last Hisense produces, batch number: 090702.
Laboratory animal: cleaning level Male Kunming strain mice, body weight (20 ± 2) g, the Jiangxi College of Traditional Chinese Medicine Experimental Animal Center provides.
The 1st experiment divided into groups: animal is divided into 5 groups at random, 12 every group, is respectively distilled water matched group, Pericarpium Citri Reticulatae petroleum ether extract group (5g, 2.5gkg
-1), Pericarpium Citri Reticulatae water soluble part group (10gkg
-1), mosapride group (3mgkg
-1).
The 2nd experiment divided into groups: mice is divided into 6 groups at random, 12 every group, is respectively 0.5% tween 80 matched group, Pericarpium Citri Reticulatae chromatographic isolation component group (15mgkg
-1, 5mgkg
-1), motilium group (6mgkg
-1).
Experimental technique: gastric infusion, volume are 0.4mL/10g, 1 time/d, and successive administration 5d; 4d begins fasting and can't help water 24h, and after 5d prohibited water 2h, (carboxymethyl cellulose 2.5g added 60mL water to irritate the semi-solid paste of clothes nutrition; Fully stir dissolving, add milk powder 4g then, sugared 2g, starch 2g; The 1mL burnt black ink is made into the pastel of 75mL) 0.5mL/ only, all behind 15min, take off neck and put to death, cut the abdominal cavity open; Ligation stomach cardia and pylorus are got stomach, wipe away with filter paper and do back title stomach total quality, cut off body of stomach along greater gastric curvature then; Wiping away driedly behind the flush away gastric content, claim stomach clean quality, is stomach residue quality with the difference of the clean quality of stomach total quality stomach function regulating, and it is the gastric residual rate that the latter gives the percentage ratio of paste quality with institute.To the propulsive influence of mouse small intestine; Take out whole gastrointestinal on laboratory table after cutting the abdominal cavity open; Peel off gently; The shop is straight, measures the extremely semi-solid distance of sticking with paste the forward position of pylorus to caecum portion total length and pylorus, and the percentage rate that accounts for pylorus to ileocecus total length to semi-solid paste Front distance with pylorus serves as that semi-solid the paste advances percentage rate.
The 1st experimental result: compare low dose group (2.5gkg with the distilled water matched group
-1) the gastric residual rate significantly reduces that statistical significance is arranged (
p＜0.05), mosapride group, petroleum ether extract high dose group (5gkg
-1Though) have and reduce but do not reach statistical remarkable meaning, Pericarpium Citri Reticulatae water solublity group (10gkg
-1) the gastric residual rate raises than matched group on the contrary to some extent; Mosapride group intestinal propulsion rate and matched group relatively have highly significant rising (
p＜0.01) (table 1).
2 extractions of table 1 Pericarpium Citri Reticulatae position is to the influence of mice gastric emptying and intestinal propulsion
Compare a with matched group:
p＜0.05; Petroleum ether extract and water soluble part be b relatively:
p＜0.05.
The 2nd experimental result: compare component 3 low dose group (5mgkg with the tween 80 matched group
-1) and motilium group gastric residual rate significantly reduce statistical significance arranged (
p＜0.05); Component 2 high and low dose group intestinal propulsion rates all with matched group relatively have significant rising (
p＜0.05), and component 3 high and low dose group intestinal propulsion rates a little less than matched group (
p＞0.05) (table 2).
Table 2 Pericarpium Citri Reticulatae extract is to the influence of mice gastric emptying and intestinal propulsion
Annotate: compare a with matched group:
p＜0.05.
Conclusion: Pericarpium Citri Reticulatae polymethoxyflavone compounds shows good short digestive tract power effect; Particularly aspect short gastric emptying; The gastric residual rate of twice result of experiment demonstration Pericarpium Citri Reticulatae polymethoxyflavone active site is all less than motilium or mosapride; Explain that the polymethoxyflavone compounds in the Pericarpium Citri Reticulatae truly has the good effect that is good for the stomach, and confirmed the tcm clinical practice practice of Pericarpium Citri Reticulatae over the past thousands of years; And dose is littler than motilium.Therefore can be used as novel short digestive tract power Chinese medicine, be used to prepare the medicine of treating gastrointestinal motility disorder, have broad application prospects.
Claims (8)
1. the application of Pericarpium Citri Reticulatae polymethoxyflavone compounds in the preparation digestive tract power reinforcing medicine.
2. according to the application of the said Pericarpium Citri Reticulatae polymethoxyflavone of claim 1 compounds, it is characterized in that: said polymethoxyflavone compounds is Pericarpium Citri tangerinae element, Nobiletin, Heptamethoxyflavone (3', 4'; 3,5,6; The mixing of one or more 7,8-Heptamethoxyflavone).
3. according to the application of the said Pericarpium Citri Reticulatae polymethoxyflavone of claim 1 compounds, it is characterized in that: said polymethoxyflavone compounds can extract preparation from Citrus chachiensis Hort., Fructus Citri tangerinae, Fructus Citri junoris skin or fruit.
4. according to the application of the said Pericarpium Citri Reticulatae polymethoxyflavone of claim 3 compounds, it is characterized in that: the total content scope of polymethoxyflavone compounds is 50% ~ 90% in the short digestive tract power effective site of Pericarpium Citri Reticulatae.
5. according to the application of the said Pericarpium Citri Reticulatae polymethoxyflavone of claim 3 compounds, it is characterized in that: contain one or more the mixing of tangeritin, Nobiletin, Heptamethoxyflavone of effective dose in the short digestive tract power active site of Pericarpium Citri Reticulatae.
6. according to the application of claim 4 or 5 said Pericarpium Citri Reticulatae polymethoxyflavone compounds, it is characterized in that: the Neosynephrine and the volatile oil component that do not contain obvious inhibition gastrointestinal motility in the said Pericarpium Citri Reticulatae polymethoxyflavone compounds active site.
7. according to the application of the said Pericarpium Citri Reticulatae polymethoxyflavone of claim 4 ~ 6 compounds, it is characterized in that: any dosage form of the pharmaceutical dosage form that said polymethoxyflavone compounds is processed for medically approving.
8. according to the application of the said Pericarpium Citri Reticulatae polymethoxyflavone of claim 7 compounds in the medicine of preparation treatment gastrointestinal motility disorder.
Priority Applications (1)
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|---|---|---|---|
| CN2011101560312A CN102440984A (en) | 2011-06-12 | 2011-06-12 | Application of dried orange peel polymethoxylated flavonoids in preparation of gastrointestinal power promoting medicines |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108619130A (en) * | 2017-03-22 | 2018-10-09 | 深圳市青杉医药科技有限公司 | Nobiletin is preparing the application in treating Gastric accommodation disorder remedies |
| CN113577131A (en) * | 2021-06-29 | 2021-11-02 | 内蒙古民族大学 | Application of Mongolian medicine extract of lomatogonium carinthiacum |
-
2011
- 2011-06-12 CN CN2011101560312A patent/CN102440984A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108619130A (en) * | 2017-03-22 | 2018-10-09 | 深圳市青杉医药科技有限公司 | Nobiletin is preparing the application in treating Gastric accommodation disorder remedies |
| CN108619130B (en) * | 2017-03-22 | 2019-07-30 | 深圳市青杉医药科技有限公司 | Application of the Nobiletin in preparation treatment Gastric accommodation disorder remedies |
| CN113577131A (en) * | 2021-06-29 | 2021-11-02 | 内蒙古民族大学 | Application of Mongolian medicine extract of lomatogonium carinthiacum |
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Application publication date: 20120509 |