CN108042527A - Purposes of the Praeruptorin B in drug induced hepatic injury protection drug is prepared - Google Patents
Purposes of the Praeruptorin B in drug induced hepatic injury protection drug is prepared Download PDFInfo
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- CN108042527A CN108042527A CN201711269421.4A CN201711269421A CN108042527A CN 108042527 A CN108042527 A CN 108042527A CN 201711269421 A CN201711269421 A CN 201711269421A CN 108042527 A CN108042527 A CN 108042527A
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- praeruptorin
- liver
- hepatic injury
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- 239000002547 new drug Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- MBRLOUHOWLUMFF-UHFFFAOYSA-N osthole Chemical compound C1=CC(=O)OC2=C(CC=C(C)C)C(OC)=CC=C21 MBRLOUHOWLUMFF-UHFFFAOYSA-N 0.000 description 1
- 230000001151 other effect Effects 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
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- 231100000572 poisoning Toxicity 0.000 description 1
- 230000000607 poisoning effect Effects 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000004321 preservation Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- ZCCUUQDIBDJBTK-UHFFFAOYSA-N psoralen Chemical class C1=C2OC(=O)C=CC2=CC2=C1OC=C2 ZCCUUQDIBDJBTK-UHFFFAOYSA-N 0.000 description 1
- UFUVJROSOIXJGR-UHFFFAOYSA-N qianhucoumarin H Natural products C1=CC(=O)OC2=C1C=CC1=C2C(OC(=O)CC(C)C)C(OC(=O)C(C)=CC)C(C)(C)O1 UFUVJROSOIXJGR-UHFFFAOYSA-N 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- PYWVYCXTNDRMGF-UHFFFAOYSA-N rhodamine B Chemical compound [Cl-].C=12C=CC(=[N+](CC)CC)C=C2OC2=CC(N(CC)CC)=CC=C2C=1C1=CC=CC=C1C(O)=O PYWVYCXTNDRMGF-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
- A61K31/37—Coumarins, e.g. psoralen
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
Abstract
The present invention relates to a kind of Coumarins ingredient Praeruptorin B for separating, preparing from the root of purple-flowered peucedanum and its applications in drug induced hepatic injury protection drug and health products are prepared.By inside and outside experimental study, find that Praeruptorin B monomeric compound has antiradiation drug hepatic injury pharmacological activity for the first time.Chemical composition of the present invention has good antiradiation drug hepatic injury effect, is conducive to carry out the research and development of novel medicine physical property liver injury protection drug and health products.
Description
Technical field
The present invention relates to drug fields, and in particular to a kind of effective monomer compound is preparing Drug liver in the Chinese medicine root of purple-flowered peucedanum
Application in injury protection drug.
Background technology
Liver is maximum glandula digestive in human body, dominates human metabolism, is " chemical plant " huge in human body.Hepatic injury
It is a kind of pathological state that a variety of liver diseases share, is mainly shown as necrosis of liver cells or apoptosis, degeneration of liver cells, liver cell
Steatosis, silt courage damage and inflammatory reaction etc..Long-term hepatic injury is that liver fibrosis or even hepatic sclerosis, liver cancer is caused to occur
Important make reason plain.
In investigated population of China, hepatic injury number is up to 1.3 hundred million people, since hepatic injury illness causes death toll near
500000 people.In recent years increase sharply with clinical application species and patient's voluntarily take medicine or arbitrarily increase probability of drug dose increase,
Drug induced hepatic injury incidence also accordingly increases, and has 900 kinds or more drugs (such as carbon tetrachloride, bromobenzene, fluothane, resistive connections according to statistics
Core medicine, antibiotic, non-steroidal anti-inflammatory drugs etc.) it can clearly cause drug induced hepatic injury.Therefore, drug induced hepatic injury serious threat
Human health and life are arrived, protection liver health has been a very urgent task of the pendulum in face of us.
Modern medicine has no the specific drug of medicine physical property hepatic injury, mostly using rest, adjusts diet, supplement dimension life
Element and symptomatic treatment (selection antiviral drugs, immunoregulation medicament, protecting liver, lowering enzymes drug), severe patient need to be forced to terminate medication,
In order to avoid aggravate hepatic injury.Current application Chinese herbal medicine and its preparation for treating liver diseases are fairly common in China, and modern pharmacology is ground
Study carefully and show that many Chinese medicines can be treated effectively (including compound, single medicinal material and monomer component) or improve drug induced hepatic injury disease
Disease, and Chinese medicine, then because liver protection curative effect affirms that toxic side effect is smaller, multicomponent, Mutiple Targets work and increasingly receive favor.
The root of purple-flowered peucedanum is the dry root of samphire RADIX PEUCEDANI Peucedanum praeruptorum Dunn, has sending down abnormally ascending
Resolving sputum, relieve heat heat-clearing and other effects.Available for treating, yellow thick glutinous, the chest diaphragm of strongly fragrant lung heat phlegm, affection of exogenous wind-heat, cough and phlegm, phlegm is completely bored etc.；
Its main pharmacological resists myocardial ischemia, is anti-oxidant, is antitumor, antibacterial, anti-inflammatory, blood pressure lowering, kobadrin etc..
Root of purple-flowered peucedanum chemical composition is mainly coumarin kind compound, using angle-style dihydropyran Coumarins ingredient as main medicine
Active ingredient is imitated, such as praeruptorin A, Praeruptorin B, Praeruptorin C, Praeruptorin D, RADIX PEUCEDANI E elements
Deng.Research in recent years proves that peucedanocoumarin constituents main pharmacological includes antibacterial, anti-oxidant, anti-inflammatory, antitumor, myocardium guarantor
(Inner Mongol medicine, 2017,2 (3) such as shield, eliminating the phlegm, antibechic：142-143；Asia-Pacific traditional medicine, 2016,12 (18)：75-76；Food
Product and drug, 2010,12 (11)：442-445).Moreover, it has been found that Praeruptorin B has anti-hyperlipidemia, hyperglycaemia, non-
Pharmacological activity (the application for a patent for invention number such as alcoholic fatty liver and diabetes B：201710046028.2).
In addition, coumarin kind compound is also widely present in other Chinese medicines (such as Rhizoma Et Radix Notopterygii, the root of Dahurain angelica, frutus cnidii, psoralea corylifolia),
Research shows that coumarin kind compound has many-sided biological activity, such as AntiHIV1 RT activity, anticancer, decompression, anti-arrhythmia, anti-bone
(CHINA JOURNAL OF CHINESE MATERIA MEDICA, 2005,30 (6) such as matter is loose, antibacterial：410-414；Chinese Journal of New Drugs, 2013,22 (20)：2392-
2404).Separately there are some researches prove some coumarin kind compounds also have liver-protecting activity, and including Osthole, (herbal pharmacology is with facing
Bed, 2006,22 (2)：21-22), phellopterin (Arch Pharm Res, 1993,16 (1)：13-17), 8- methoxyl groups psoralea corylifolia
Plain (Chinese Journal of Modern Applied Pharmacy, 2012,29 (8)：682-686)；It has also been found that 5 kinds of furocoumarin class chemical combination in Radix changii root skin
Object, which has, inhibits hepatoma cell proliferation active (Chinese experimental pharmacology of traditional Chinese medical formulae magazine, 2012,18 (6)：203-205) and Imperatoria ostruthium
Element and Isomperatorin have cytochromes P450 enzymatic activity inhibitory activity (CHINA JOURNAL OF CHINESE MATERIA MEDICA, 2013,38 (8)：
1237-1241)。
However, so far, the pharmacological action of Praeruptorin B confrontation drug induced hepatic injury has not yet to see report.
The content of the invention
The object of the present invention is to provide application of the root of purple-flowered peucedanum active ingredient in drug induced hepatic injury protection drug is prepared.
The compound that the present invention is studied is related in the Chinese medicine root of purple-flowered peucedanum a kind of dihydropyran Coumarins for separating, being prepared
Ingredient, chemical constitution is as follows, can separate and be prepared from natural drug, can be also prepared by chemical synthesis.
Praeruptorin B chemical constitution
The present invention is by investigating compound to carbon tetrachloride (CCl4) damage suckling mouse primary hepatocyte survival rate, alanine
Aminopherase (ALT), aspartate aminotransferase (AST), the shadow of malonaldehyde (MDA) and superoxide dismutase (SOD)
It rings, finds that Praeruptorin B has antiradiation drug hepatic injury effect for the first time.
The present invention is by investigating compound to CCl4ALT, AST content, liver morphology, liver in the mice serum of damage
Middle liver index, the influence of MDA, SOD and glutathione (GSH) and to MDA in liver cell mitochondria, atpase activity and film electricity
The influence of position finds that Praeruptorin B has antiradiation drug hepatic injury effect for the first time.
The present invention has found the antiradiation drug hepatic injury pharmacological activity of a kind of monomer component in the root of purple-flowered peucedanum by pharmacological evaluation, can use
In preparing drug and functional food with respective action, be conducive to carry out novel medicine physical property liver injury protection drug and health care
The research and development of product.
The drug of the present invention can be any pharmaceutically useful dosage form, including tablet, capsule, oral liquid, syrup, particle
Agent, pill, powder, paste, sublimed preparation, injection, suppository, creme, spray, pill, patch, sustained release preparation and controlled release preparation
Deng.
The form of oral liquid can be aqueous or oily solution, suspension, emulsion, syrup or elixir, can
Containing conventional additive, including solvent such as water, ethyl alcohol, suspending agents for example sorbierite, syrup, methylcellulose, gelatin,
Hydroxyethyl cellulose etc., emulsifier is such as lecithin, anhydro sorbitol monooleate, Arabic gum, and preservative is for example to hydroxyl
Base benzene methyl, propylparaben, sorbic acid etc..
Oral solid formulation can contain common excipient, such as adhesive, filler, diluent, lubricant, disintegration
Agent, colorant, flavoring agent and wetting agent, can be coated applicable filler to tablet if necessary includes cellulose, mannose
Alcohol, lactose and other similar fillers.Suitable disintegrant includes starch, polyvinylpyrrolidone and starch derivatives, example
Such as sodium starch glycollate.Suitable lubricant includes magnesium stearate.Suitable wetting agent includes lauryl sodium sulfate.
Description of the drawings
The tested monomeric compounds of Fig. 1 are to CCl4Damage the influence of murine liver tissue pathological change
Normal group (A), model group (B), legalon group (C), Praeruptorin B 8mg/kg groups (D), RADIX PEUCEDANI second
Plain 16mg/kg groups (E), the mouse liver pathological change (× 200) of Praeruptorin B 32mg/kg groups (F)
Normal group hepatic tissue is clear in structure as it can be seen that liver cell aligned orderly, in the same size, and hepatic cell cords is in apparent radiation
Shape, portal area is without lesions such as denaturation, necrosis and inflammatory cell infiltrations；The apparent oedema of model group mouse liver cell, balloon sample become, liver
Rope is disorganized, and liver cell spotty necrosis, liver parenchyma has more cell infiltration；Legalon group hepatic tissue visible inflammatory cell soaks
Profit is substantially reduced compared with model group, and liver cell is without significant change；Each dosage group of Praeruptorin B has different degrees of inflammatory cell
Infiltration, but it is substantially reduced compared with model group.
Specific embodiment
It can be used for the substantive content for preparing drug induced hepatic injury protection drug and health products in order to preferably explain the present invention,
It is further illustrated below by way of specific experiment embodiment.Following embodiment is illustrative, the present invention is not done
Any restriction.
Embodiment 1：Influence of the tested monomeric compound to the suckling mouse primary hepatocyte of carbon tetrachloride-injured
1 material, reagent and instrument
1.1 main materials and reagent
Test compound controls product (Praeruptorin B, legalon) are purchased from the limited public affairs of Chengdu Puffy moral biotechnology
Department；L-02 cells (Shaanxi Mai Yuan bio tech ltd)；DMEM/F12 culture mediums (Gibco companies of the U.S.)；Hyclone
(Gibco companies of the U.S.)；CCK-8 cell proliferation detecting kits (Suo Laibao bio tech ltd)；Carbon tetrachloride
(CCl4)(Sigma)；Mycillin is dual anti-(Gibco companies of the U.S.)；PBS (Suo Laibao bio tech ltd)；96 holes are thin
Born of the same parents' culture plate (Thermo companies)；0.22um filter membranes (Corning)；Blood counting chamber (Zhengjiang City Dantu Kodak medical supplies
Factory)；ALT, AST, SOD, MDA detection kit (Bioengineering Research Institute is built up in Nanjing).
1.2 key instrument
5%CO2Incubator (Thermo companies)；Desk centrifuge (Changsha Xiang Yi centrifuges Instrument Ltd.)；Biology
Safety cabinet (Purifying Equipment Co., Ltd., Suzhou)；Microplate reader (TECAN)；- 80 DEG C of refrigerators (Thermo companies).
2 methods
2.1 given the test agent solution are prepared
Each Test compound controls product is taken to be dissolved in DMSO in right amount, the given the test agent that DMSO dissolves is taken to be arrived with normal saline dilution
Required concentration.
2.2 modelings and administration
Plating cells：Cell, which is resuspended, makes its concentration be 1 × 105A/mL spreads 10000 cells (100 μ L), cell per hole
Put 3 repetitions, 37 DEG C of 5%CO2After cultivating 12h, each experimental drug processing is for 24 hours.Final concentration of 10mmol/L is then added in per hole
CCl4, put 37 DEG C of 5%CO2Cultivate 6h.
Experiment packet includes：Blank group (containing only culture medium)；Normal group；Solvent control group (1 ‰ DMSO)；Solvent control group
+CCl4(model group)；Legalon group (60 μm of ol/mL of concentration)+CCl4(positive controls)；Praeruptorin B (80 μ of concentration
mol/mL、160μmol/mL、320μmol/mL)+CCl4。
2.3 cell survival rates measure (CCK-8 methods)
100 μ L/ holes serum free mediums are replaced, add 10 μ L/ holes CCK-8 stostes, 5%CO22h is incubated in incubator altogether,
Absorbance is measured at 450nm.
2.4ALT, AST, MDA, SOD assay
It is measured by the specific steps of kit specification.
2.5 calculate and count
Cell survival rate (living cells relative populations %)=A (dosing)-A (blank)/A (0 dosing)-A (blank) × 100；
SPSS17.0 softwares are calculated and counted, ANOVA one-way analysis of variance significant differences (P<0.05).
3 experimental results
Compound is to CCl4Cause the influence of suckling mouse the primary hepatocyte survival rate, ALT, AST, MDA, SOD of damage
Legalon (positive control) can play hepatocytoprotection, the study find that it is remarkably improved CCl4Damage
Hepatocyte viability, while significantly reduce ALT, AST, MDA content, and dramatically increase SOD contents, illustrate cell pathology model
Reliably.The same with legalon, each dosage group of Praeruptorin B can improve CCl to a certain extent4The liver cell of damage
Survival rate, wherein 160 μ g/mL, 320 μ g/mL groups and model group have significant difference；And each dosage group of Praeruptorin B is equal
ALT, AST, MDA content can be significantly reduced, and dramatically increases SOD contents, shows that the compound has antiradiation drug hepatic injury activity
(table 1).
1 test-compound of table is to CCl4Cause suckling mouse primary hepatocyte survival rate, the shadow of ALT, AST, MDA, SOD of damage
Ring (n=3,)
Compared with model group,#P<0.05,##P<0.01,###P<0.001。
Embodiment 2：Influence of the tested monomeric compound to carbon tetrachloride-injured mouse liver and serum indices
1 material, reagent and instrument
1.1 animal
5~6 week old male cleaning grade Kunming mouses, 18~22g of weight, purchased from the limited public affairs of the long-living biotechnology in Liaoning
Department, the certification of fitness number：SCXK (the Liao Dynasty) 2015-0001.Before experiment, the equal adaptability of animal used is raised 3 days.It is raised in adaptability
Period, the free feeding of animal, free water.It keeps quite in receptacle, indoor temperature maintains 23-25 DEG C, humidity 55%~
75%, fluorescent lamp lighting, middle holding 12h illuminations 12h is dark for 24 hours daily.
1.2 main materials and reagent
Test compound controls product (Praeruptorin B, legalon) are purchased from the limited public affairs of Chengdu Puffy moral biotechnology
Department；ALT、AST、MDA、SOD、GSH、Na+-K+- ATP enzyme, Ca2+-Mg2+- atpase assay kit is purchased from Nanjing and builds up biology
Graduate School of Engineering；BCA determination of protein concentration kit is purchased from green skies biotechnology research institute；CCl4It analyzes pure.
1.3 key instrument
MILLI-Q ultrapure water systems (Millipore companies of the U.S.)；Electronic analytical balance, PB-10pH meters (Germany
Sartorius)；Glass homogenizer (NingBo XinZhi Biology Science Co., Ltd)；UV-1800PC types UV, visible light is divided light
Degree meter (Shanghai Ao Yi Instrument Ltd.)；(eastern KingMax neoformation science and technology is limited for Infinite M200Pro multi-function microplate readers
Company)；Plus384 light absorptions microplate reader (Molecular Devices companies of the U.S.)；HR/16M is freezed at a high speed
Centrifuge (Hunan He Xi instrument and equipment Co., Ltd).
2 experimental methods
Male Kunming strain mice is randomly divided into 6 groups, every group 10, i.e. normal group (physiological saline), model group (0.1%
CCl4Peanut oil), the low middle high dose group of legalon (positive controls, 16mg/kg), Praeruptorin B (8mg/kg,
16mg/kg、32mg/kg)；Each group mouse is with the dosage gastric infusion of 10mL/kg, continuous 7d, 1 time a day, in last dose
Start modeling after 1h.By CCl4It is dissolved in peanut oil, is made into 0.1% CCl4Peanut oil solution is carried out by the dosage of 10mL/kg
Intraperitoneal injection, establishes acute liver model.Normal group intraperitoneal injection equivalent peanut oil.
It is deprived of food but not water after poisoning, eyeball is plucked after 16h, blood, whole blood room temperature is taken to separate serum after putting 2h, -80 DEG C of preservations are standby
With；It takes after blood that cervical dislocation puts to death mouse immediately, takes liver rapidly, eliminating surface with the physiological saline rinsing of 4 DEG C of precoolings floats blood,
Filter paper wipe it is dry after weigh, calculate liver index.3 mouse are chosen from every group and take same area liver, cutting tissue block is placed in 10%
It is fixed in formalin for 24 hours, for check pathological section；Remaining liver is placed in -80 DEG C of refrigerators and preserves, and is taken out when to be detected, claims
Its 0.2g is taken to be put in glass homogenizer to shred, adds the physiological saline of 2mL precoolings that 10% tissue homogenate is made in ice-water bath,
3000rpm centrifuges 10min, and supernatant is put 4 DEG C and saved backup.
3 Indexs measures
3.1 liver index
Liver is taken respectively, is weighed, and liver index is calculated by liver index=[liver weight g/ weight g] × 100%.
3.2 Biochemical Indices In Serums measure
Serum alt, the measure of AST are measured using improvement reitman-frankel method by the specific steps of kit specification.
3.3 hepatic tissue Biochemical Indexes
100 μ L of liver tissue homogenate's liquid are taken, are operated according to kit specification, MDA, SOD and the GSH measured in hepatic tissue contains
Amount.
3.4 pathological study
Hepatic tissue is fixed in 10% formalin fixer to be rinsed with water rear graded ethanol elution for 24 hours, and dimethylbenzene is transparent,
The thin slice of 4 μ m-thicks, HE dyeing observations are cut into after progress paraffin embedding processing.
3.5 liver cell mitochondria indexs of correlation
3.5.1 liver cell mitochondria separates
The mouse liver for being stored in -80 DEG C of refrigerators is taken out, clip each group liver organization, is filled with the physiological saline of precooling respectively
Divide and clean residual blood, prune away connective tissue, with filter paper suck dry moisture, weigh (about 0.1g)；Hepatic tissue is transferred to the glass of precooling
Glass homogenizer nozzle is shredded hepatic tissue to without apparent tissue block, the mitochondria separating liquid of addition 1mL precoolings with the scissors of precooling
(0.21M mannitol, 0.07M sucrose, 10mM Tris base, 1mM EDTA, 0.5mM EGTA, pH to 7.4), in ice-water bath
Homogenate 10 times；Tissue homogenate is transferred to respectively in 1.5mL centrifuge tubes, in 4 DEG C, 1000 × g centrifugation 10min discard precipitation,
Supernatant is transferred in another centrifuge tube, 4 DEG C, and 10000 × g centrifugation 10min, gained precipitation is liver cell mitochondria.
3.5.2 liver cell mitochondria film potential measures
Extract liver cell mitochondria, ledger line mitochondrial membrane potential measure medium (0.25M sucrose, 5mM MgCl2,10mM KCl,
5mM KH2P04,10mM Hepes, 10mM succinates, pH 7.4) suspension is mixed into, with BCA determination of protein concentration reagents
Box measures mitochondrial protein concentration；100 μ L mitochondrial suspensions are taken, 2.9mL is added in and measures medium, add 5 μ L Rhodamine 123s
After 37 DEG C keep the temperature 30min, fluorescence intensity is surveyed under excitation wavelength 484nm, launch wavelength 534nm for mixing.
3.5.3 liver cell mitochondria MDA contents, atpase activity measure
Liver cell mitochondria is extracted, physiological saline is added to be mixed into suspension, with BCA determination of protein concentration kit measurement lines
Mitochondrial protein concentration；100 μ L mitochondrial suspensions are taken respectively, are operated according to kit specification, are measured in liver cell mitochondria
MDA, Na+-K+- ATP enzyme and Ca2+-Mg2+The activity of-ATP enzyme.
4. statistical procedures each group of data uses mean ± standard deviationIt represents, using 11.0 statistical softwares of SPSS
Analyzing and processing data carries out comparison among groups, P using one-way analysis of variance<0.05 thinks there is significant difference.
5 experimental results
5.1 tested monomeric compounds are to CCl4Damage the influence of mouse liver index
Compared with normal group, the liver weight and liver index of model group mouse significantly raise, and prompt liver damage；With model group phase
Than the liver weight and liver index of legalon group (positive control) mouse significantly reduce, and illustrate that legalon can effectively be alleviated
CCl4Caused hepatic injury；The same with legalon, the liver index of each dosage group of Praeruptorin B is significantly reduced (with model
Group is compared), show that Praeruptorin B has antiradiation drug hepatic injury activity (table 1).
1 tested monomeric compound of table is to CCl4Damage mouse liver index influence (N=10)
Compared with model group,#P<0.05,##P<0.01,###P<0.001。
5.2 tested monomeric compounds are to CCl4Damage the influence of mice serum ALT, AST
Compared with normal group, ALT, AST in model group mice serum are significantly raised, modeling success；Compared with model group,
ALT, AST in legalon group mice serum are significantly reduced, and show that legalon can effectively alleviate CCl4Caused hepatic injury；With
Model group is compared, and ALT, AST content reduce to a certain extent in each dosage group mice serum of Praeruptorin B, wherein
16mg/kg dosage groups and model group difference have conspicuousness, show that Praeruptorin B has the active (table of antiradiation drug hepatic injury
2)。
2 tested monomeric compound of table is to CCl4Damage mice serum ALT, AST influence (N=10)
Compared with model group,#P<0.05。
5.3 tested monomeric compounds are to CCl4Damage the influence of mouse liver MDA, SOD and GSH
Compared with normal group, the MDA contents in model group mouse liver significantly raise, and the content of SOD and GSH significantly drop
It is low, modeling success；Compared with model group, the MDA contents in legalon group mouse liver significantly reduce, the content of SOD and GSH
Significantly rise, shows that legalon can effectively alleviate CCl4Caused hepatic injury；Compared with model group, each dosage of Praeruptorin B
Group can reduce MDA contents, wherein increased SOD, the content of GSH, 8mg/kg dosage groups and model group difference to a certain extent
With conspicuousness, illustrate that Praeruptorin B has antiradiation drug hepatic injury activity (table 3).
3 tested monomeric compound of table is to CCl4Damage mouse liver MDA, SOD and GSH content influence (N=10)
Compared with model group,#P<0.05,##P<0.01。
5.4 tested monomeric compounds are to CCl4Damage the influence of mouse liver mitochondria MDA, ATP enzyme and film potential
Compared with normal group, the MDA contents in model group mouse liver mitochondria significantly raise, Na+-K+- ATP enzyme and Ca2 +-Mg2+The activity of-ATP enzyme significantly reduces, and liver cell mitochondria fluorescence intensity significantly increases, and mitochondrial membrane potential is caused to collapse,
Show modeling success；Compared with model group, the MDA contents in legalon group mouse liver significantly reduce, Na+-K+- ATP enzyme and
Ca2+-Mg2+The activity of-ATP enzyme significantly rise, mitochondria fluorescence intensity are remarkably decreased, so as to alleviate the degree of film potential collapse,
Show that legalon can effectively alleviate CCl4Caused hepatic injury.Compared with model group, Praeruptorin B 8mg/kg dosage group energy
MDA contents are significantly reduced, raise Na+-K+- ATP enzyme and Ca2+-Mg2+The activity of-ATP enzyme；And its 16mg/kg dosage group can be significantly
Mitochondria fluorescent value is reduced, alleviates the collapse degree of film potential, the results showed that Praeruptorin B can be by adjusting mitochondria work(
Can and resist Drug hepar damnification (table 4)
4 tested monomeric compound of table is to CCl4Damage mouse hepatic mitochondria MDA, ATP enzyme and film potential influence (n
=10)
Compared with model group,#P<0.05,##P<0.01。
Claims (5)
1. application of the Praeruptorin B in drug induced hepatic injury protection drug and health products are prepared, structural formula are as follows：
2. a kind of drug of drug induced hepatic injury protection, it is characterised in that：Including Praeruptorin B.
3. a kind of drug of drug induced hepatic injury protection, it is characterised in that：Including Praeruptorin B and other with Drug
The drug of liver injury protection effect.
4. drug as claimed in claim 2 or claim 3, dosage form is oral formulations.
5. drug as claimed in claim 4, which is characterized in that its dosage form is tablet, granule, capsule, oral liquid, suspension
Deng.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110731960A (en) * | 2018-07-19 | 2020-01-31 | 国家海洋局第三海洋研究所 | Application of peucedanum praeruptorum and its analogue in preparing medicine for resisting inflammatory disease |
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| CN101904839A (en) * | 2010-08-06 | 2010-12-08 | 中国人民解放军第二军医大学 | Application of imperatorin in preparing medicament for preventing and treating hepatitis or liver injury |
| KR101265872B1 (en) * | 2012-11-30 | 2013-05-22 | 순천대학교 산학협력단 | Pharmaceutical composition for preventing or treating osteoporosis, comprising praeruptorin a or pharmaceutical salt thereof as an active ingredient |
| KR20150087145A (en) * | 2014-01-21 | 2015-07-29 | 주식회사 엘지생활건강 | Composition for improving skin |
| CN106727507A (en) * | 2017-01-22 | 2017-05-31 | 中国药科大学 | The medical usage of Praeruptorin B |
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| CN101904839A (en) * | 2010-08-06 | 2010-12-08 | 中国人民解放军第二军医大学 | Application of imperatorin in preparing medicament for preventing and treating hepatitis or liver injury |
| KR101265872B1 (en) * | 2012-11-30 | 2013-05-22 | 순천대학교 산학협력단 | Pharmaceutical composition for preventing or treating osteoporosis, comprising praeruptorin a or pharmaceutical salt thereof as an active ingredient |
| KR20150087145A (en) * | 2014-01-21 | 2015-07-29 | 주식회사 엘지생활건강 | Composition for improving skin |
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| CN110731960A (en) * | 2018-07-19 | 2020-01-31 | 国家海洋局第三海洋研究所 | Application of peucedanum praeruptorum and its analogue in preparing medicine for resisting inflammatory disease |
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