CN101926852B - Application of roots and leaves of common fig in preparing auxiliary therapy medicine and health food for hepatitis - Google Patents
Application of roots and leaves of common fig in preparing auxiliary therapy medicine and health food for hepatitis Download PDFInfo
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- CN101926852B CN101926852B CN2010102455501A CN201010245550A CN101926852B CN 101926852 B CN101926852 B CN 101926852B CN 2010102455501 A CN2010102455501 A CN 2010102455501A CN 201010245550 A CN201010245550 A CN 201010245550A CN 101926852 B CN101926852 B CN 101926852B
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Abstract
The invention discloses an application of roots and leaves of common fig in preparing an auxiliary therapy medicine and health foods for hepatitis, wherein Bergapten is one of active constituents of the roots and leaves of the common fig of the preparation. The medicine and the health food taking the roots and leaves of the common fig and Bergapten as the active constituents can effectively cure and prevent cocaine toxic hepatitis, carbon tetrachloride toxic hepatitis, acetaminophen toxic hepatitis, thioacetamide toxic hepatitis and dimethylformamide toxic hepatitis.
Description
Technical field
The present invention relates to extraction and the purposes in medicine, health food of a kind of plant Fructus Fici medical material (root and leaf), specifically, be Radix Fici and leaf extract, method for preparing extractive and wherein as the bergapton of one of effective ingredient in the adjuvant therapy medicaments of preparation hepatitis or the purposes in health food.
Background technology
Liver as most important detoxifcation organ, is the important target spot of many medicines, xenobiotics.Hepatic injury is generation, the development of multiple serious hepatic disease and initiating link and the common pathway that finally moves towards liver failure.The pathogenesis of hepatic injury is very complicated, is coefficient result on multifactor, stage construction, many target spots.Hepatic injury due to various harmful factors can show as hepatic necrosis, fatty liver, cholestasis, hepatic fibrosis, liver cirrhosis and hepatocarcinoma etc.China is the popular more serious country of hepatopathy, and the whole world has more than 100 ten thousand patients to die from hepatopathy every year, and wherein 1/3 in China.Along with the continuous increase of medicament categories, the incidence rate of medicamentous liver lesion is corresponding rising also.Medicamentous liver lesion accounts for 10%～15% of whole adverse effect, and China's drug induced hepatitis accounts for 10% of acute hepatitis inpatient.The report of domestic relevant dimethylformamide poisoning is also of common occurrence, and between statistics nineteen ninety to 2007 year, total poisoning report is 54, and Poisoning Number reaches 933 people.National occupational health standard GBZ85 regulation in 2002: the poisoning special efficacy antidote that there is no of DMF, the Therapeutic Principle protects the liver, suits the medicine to the illness and Supporting Therapy.In addition, the sickness rate of viral hepatitis and alcoholic liver and fatty liver all presents obvious ascendant trend.Control to hepatic injury is still a global severe problem at present.By setting up the Experimental Hepatic Damage animal model, the mechanism of research hepatopathy is screened hepatic, explores the hepatoprotective effect principle, is of great practical significance.
According to introductions such as " Chinese Plants will ", Fructus Fici (Ficus caricaLinn) is machaka or dungarunga, up to 3～10m.Herb tool milk; Multi-branched, sprig is sturdy, and surperficial brown is by rare undercoat.The leaf alternate; Long 2～the 5cm of petiole is sturdy; Holder leaf egg shape lanceolar is about 1cm, redness; Blade thick film matter, width egg shape or oval, long 10～24cm, wide 8～22cm, 3～5 split, sliver is avette, and there is irregular cognate at the edge, above bottle green, coarse, below the tiny cystolith of close life and yellowish-brown pubescence, the shallow heart of base portion, base is given birth to 3～5, arteries and veins, 5～7 pairs of lateral veins.Dioecism, hypanthodium, the receptacle of inflorescence list is born in axil; Male flower and gall flower are born in same receptacle of inflorescence; Male flower is born in the inwall oral area, stamen 2, tapel 3～4; Gall flower style adnation, short; Female Semen arachidis hypogaeae in another receptacle of inflorescence, tapel 3～4, the style adnation, stigma 2 splits.Banyan fruit (receptacle of inflorescence) pyriform, ripe duration 3～5cm is aubergine or yellow green, meat, sink in the top, and base portion has 3 bracts.The flower, the fruit 8～November of phase.All there is cultivation China various places.
Fructus Fici cures mainly laryngopharynx swelling and pain; The cough caused by dryness hoarseness; Milk is rare; The hot constipation of intestinal; Inappetence; Dyspepsia, dysentery; Carbuncle; The tinea disease.The present invention has found Radix Fici and the new purposes of leaf treatment hepatitis and the effective ingredient bergapton of liver-protecting activity thereof.Toxicological experiment shows bergapton rat oral LD
50Greater than 30,000mg/kg, its mouse oral LD
50Be 8100mg/kg, safety is higher.Bergapton is as the medicinal ingredient for the treatment of vitiligo and Corii Bovis seu Bubali moss.Radix Fici and Ye Zhongjun contain bergapton, and in leaf, the content of bergapton is 0.39%.The research of bergapton focused mostly at its phototoxicity and antitumaous effect in the past.Studies show that bergapton can suppress liver microsomes P450 system, experiment in vitro shows that bergapton can suppress the growth and breeding of liver neoplasm cell line.But do not have at present the research report for bergapton antagonism chemical liver injury aspect.
The english name of bergapton is: 5-Methoxypsoralen
Other titles: 5-MOP, bergapten.
Molecular formula: C
12H
8O
4
Molecular weight: 216.19
CAS registration number: 484-20-8
Chemical structural formula:
Summary of the invention
The new purposes that the purpose of this invention is to provide Radix Fici and leaf and bergapton, i.e. new application in preparation hepatitis adjuvant therapy medicaments and health food.
Another object of the present invention is to provide a kind of medicine of hepatitis auxiliary treatment.
A further object of the present invention is to provide a kind of health food of hepatitis auxiliary treatment.
Purpose of the present invention also comprises provides easy to prepare, health care and the good Radix Fici of therapeutic effect and leaf extract and preparation method thereof.
The inventor is according to " 2003 annual drug research technological guidance principle---Chinese medicine, natural goods fascicle " (State Food and Drug Administration, 2003), " new drug preclinical study guideline " (1993, Bureau of Drugs Supervision of country) and " function of health food assessment process " (Ministry of Public Health, 2003) etc. medicine and the health food method of hepatitis auxiliary treatment, Fructus Fici has been carried out extract preparation, pharmaceutical dosage form preparation, animal pharmacology and pathological study.
The preparation method of Radix Fici or leaf extract is: get the decoction pieces 1000g that makes after Radix Fici or leaf drying, pulverize, wash 3～4 times, decoct with water three times, each 15 minutes, collecting decoction, filter, it is 1.12～1.25 thick paste that filtrate is condensed into relative density, after continuing drying, fine powder processed, and get final product.This product is brown granule; Special fragrance, lightly seasoned sweet is arranged.
The inventor finds, with the extract oral administration of Radix Fici or leaf, obvious effect arranged, and serum liver biochemical function index and pathological index all improve significantly.
When treating with Radix Fici and leaf extract, it can be with form oral administrations such as powder, granule, tablet, capsule, pill and liquid preparations; Also can be non-through enteral administration with forms such as injection, suppository, percutaneous preparation, sprays.The effective agent of Radix Fici and leaf extract, be by with suitable medicinal blend, as mixing such as excipient, binding agent, penetrating agent, lubricants and be mixed with.
Radix Fici and leaf extract dosage change with patient's the state of an illness, route of administration, patient's age and body weight.In the oral administration situation, dosage is generally adult 1000～3000mg/ days, is preferably 500～1000mg/ days.Also same principle in the health food application facet.
Advantage of the present invention is: Radix Fici and leaf can be used as the compound of cocaine poisoning hepatitis auxiliary treatment.Cocaine is popular analeptic drugs in a kind of world wide.2002 the end of the year China major drug-related cases of 100 kilograms of cocaine smugglings have just occured.Hepatitis is a lethal major reason of cocaine poisoning.Also do not treat in the world at present the generally acknowledged medicine of cocaine poisoning hepatitis.Acting on internal and international of the antitoxin product cocaine of Fructus Fici is all to find first.Except the hepar damnification of anti-cocaine, we also observe Fructus Fici simultaneously has certain inhibitory action to the mice exaltation effect that cocaine brings out.In addition, we find that also bergapton is that Fructus Fici protects the liver one of main active of drug effect.Bergapton (80mg/kg) under very low dose namely has the effect of obvious antagonism carbon tetrachloride hepatic injury.
The Fructus Fici preparation method is fairly simple, and plant growing the characteristic study also more thorough had the planting base of certain scale, so the source of medical material and economy are all secure.The market recognition of medicine-food two-purpose plant is higher, and the acceptance in market is high, good market prospects.
The specific embodiment
The embodiment that the below provides is used for further illustrating the present invention, and does not consist of limitation of the scope of the invention.
1. material
Embodiment Radix Fici used and leaf pick up from the Beijing area in autumn and spring.Radix Fici and leaf are dried respectively, be cut into decoction pieces, respectively kept dry.
Embodiment bergapton used is extracted from Chinese medicine by this laboratory, through mass spectrum and nmr analysis, is accredited as bergapton.
Other medicine, reagent and laboratory animal can be commercial easily.
2. preparation method is routine
Get Radix Fici decoction pieces or leaf 1000g, pulverize, wash 3 times, add water 2500ml and decoct, totally three times, each 15 minutes, collecting decoction, filtration, it is 1.28 thick paste that filtrate is condensed into relative density, continues to be evaporated to dried, gets brown ceramic powder 47g, and get final product.
Take a certain amount of bergapton, the tween 80 with 1% is prepared into suspension, mixing before administration.
Application example is enumerated,
(1) get 1kg Radix Fici or leaf extract and pulverize and cross 100 mesh sieves, enter the appropriate amount of starch mixing, the preparation granule carries out packing, every bag of 2g after granulate.
(2) get the extract 1000g of Radix Fici or leaf, hydroxyethyl-cellulose 10g, tabletting is made tablet, is placed in normal temperature dryer standby.
(3) Radix Fici and leaf extract are water-soluble, can directly use on demand normal saline preparation injection.
(4) Radix Fici and leaf extract are water-soluble, can directly be mixed with oral liquid.
(5) Radix Fici and leaf extract can coordinate with the medicine such as Radix Glycyrrhizae extract and make compound mixture and be used for the treatment of hepatitis.
3. test method
The auxiliary treatment drug effect study portion of the anti-various drug intoxication hepatitis of the extract of Radix Fici or leaf and main component bergapton.
Laboratory animal is male ICR mouse or MT (/-) mice, and body weight is 22～26g.Duration of test provides tap water and the normal diet of capacity, and animal housing keeps 22 ℃, automatic ventilation.The grouping of animal is pressed the body weight random packet with processing with mice.Toxic hepatitis modeling group did not give any processing in front 3 days, the 4th day subcutaneous injection modeling compound.Fructus Fici extract or bergapton+modeling compound component is with various dose gavage 4 days, every day 1 time.After the 4th day gastric infusion 30 minutes, subcutaneous or lumbar injection modeling compound solution.The contamination of modeling compound is after 24 hours, and all animal endocanthions are got blood, and disconnected marrow is put to death; leave and take at once liver, weigh, maximum leaf is dipped in 10% formalin fixing; carry out the observation of liver cardinal principle and leave and take liver specimens, the hepatic pathology intensity of variation is observed in HE dyeing.Utilize the 7170A automatic analyzer, adopt enzyme connection-ultraviolet continuous detecting method, measure alanine transaminase (ALT) and aspartate transaminase (AST) and lactic acid dehydrogenase (LDH) activity in serum.The statistical analysis technique experimental data represents with mean ± standard deviation.Application EXCEL statistical software adopts the methods analysts such as variance analysis, t check to process to experimental result, p＜0.05 thinks that group difference has significance.
4. experimental result
(1) effect of Radix Fici extract anti-cocaine mice toxic hepatitis can be referring to table 1.
The effect (Biochemical Indices In Serum) of table 1 Radix Fici extract anti-cocaine toxic hepatitis
Compare * p＜0.05, * * p＜0.01 with the cocaine model group
(2) effect of the anti-carbon tetrachloride mice of Radix Fici extract toxic hepatitis can be referring to table 2.
The effect (Biochemical Indices In Serum) of the anti-carbon tetrachloride poisoning hepatitis of table 2 Radix Fici extract
Compare * p＜0.05, * * p＜0.01 with the carbon tetrachloride model group
(3) effect of the anti-acetaminophen mice of Radix Fici extract toxic hepatitis can be referring to table 3.
The effect (Biochemical Indices In Serum) of the anti-acetaminophen toxic hepatitis of table 3 Radix Fici extract
Compare * p＜0.05, * * p＜0.01 with the acetaminophen model group
(4) effect of the anti-thioacetamide mice of Radix Fici extract toxic hepatitis can be referring to table 4.
The effect (Biochemical Indices In Serum) of the anti-thioacetamide toxic hepatitis of table 4 Radix Fici extract
Compare * p＜0.05, * * p＜0.01 with the thioacetamide model group
(5) effect of the anti-dimethyl formamide mice of Radix Fici extract toxic hepatitis can be referring to table 5.
The effect (Biochemical Indices In Serum) of the anti-dimethylformamide poisoning hepatitis of table 5 Radix Fici extract
Compare * p＜0.05, * * p＜0.01 with the dimethyl formamide model group
(6) effect of fig leaf extract anti-cocaine mice toxic hepatitis can be referring to table 6.
The effect (Biochemical Indices In Serum) of table 6 fig leaf extract anti-cocaine toxic hepatitis
Compare * p＜0.05, * * p＜0.01 with the cocaine model group
(7) effect of the anti-acetaminophen mice of fig leaf extract toxic hepatitis can be referring to table 7.
The effect (Biochemical Indices In Serum) of the anti-acetaminophen toxic hepatitis of table 7 fig leaf extract
Compare * p＜0.05, * * p＜0.01 with the acetaminophen model group
(8) effect of the anti-carbon tetrachloride mice of bergapton toxic hepatitis can be referring to table 8.
The effect (Biochemical Indices In Serum) of the anti-carbon tetrachloride poisoning hepatitis of table 8 bergapton
Compare * p＜0.05, * * p＜0.01 with the carbon tetrachloride model group
Claims (1)
1. Radix Fici extract or fig leaf extract are in the medicine of preparation treatment hepatitis and the application in health food, wherein Radix Fici extract or fig leaf extract prepare by the following method: get the decoction pieces of making after Radix Fici or leaf drying, pulverize, wash 3～4 times, decoct with water three times, each 15 minutes, collecting decoction filters, and it is 1.12～1.25 thick paste that filtrate is condensed into relative density, after continuing drying, fine powder processed; Described hepatitis is selected from cocaine poisoning hepatitis, acetaminophen toxic hepatitis.
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| CN102550755B (en) * | 2011-12-29 | 2014-01-15 | 威海新异生物科技有限公司 | Fig tea bag |
| CN103191105B (en) * | 2013-03-18 | 2015-08-19 | 中山大学 | One class furocoumarin compound is preparing the application in anti-hepatitis B virus (HBV) medicine |
| CN105029347A (en) * | 2015-07-30 | 2015-11-11 | 潍坊友容实业有限公司 | High-nutrient plant salt with various flavoring functions and preparation method thereof |
| CN108185422A (en) * | 2018-02-07 | 2018-06-22 | 浙江省农业科学院 | A kind of relieving alcoholism and protecting liver type fig ferment and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660354A (en) * | 2005-01-14 | 2005-08-31 | 北京大学 | Application of five-finger fig in preparing adjuvant for treating hepatitis and health foods |
| KR20100018993A (en) * | 2008-08-08 | 2010-02-18 | 김범식 | Manufacturing method for a fig and a fig beverage |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1660354A (en) * | 2005-01-14 | 2005-08-31 | 北京大学 | Application of five-finger fig in preparing adjuvant for treating hepatitis and health foods |
| KR20100018993A (en) * | 2008-08-08 | 2010-02-18 | 김범식 | Manufacturing method for a fig and a fig beverage |
Non-Patent Citations (2)
| Title |
|---|
| HPLC法测定五指毛桃药材中补骨脂素和佛手柑内酯的含量;钟镜金等;《中药新药与临床药理》;20070331;第18卷(第2期);全文 * |
| 钟镜金等.HPLC法测定五指毛桃药材中补骨脂素和佛手柑内酯的含量.《中药新药与临床药理》.2007,第18卷(第2期),全文. |
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