CN106380459A - Lipid-lowering flavonoid - Google Patents

Lipid-lowering flavonoid Download PDF

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Publication number
CN106380459A
CN106380459A CN201610744109.5A CN201610744109A CN106380459A CN 106380459 A CN106380459 A CN 106380459A CN 201610744109 A CN201610744109 A CN 201610744109A CN 106380459 A CN106380459 A CN 106380459A
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China
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cooh
composition
anhydroicartin
flavone compound
lipid
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李会军
徐晓军
郑祖国
张鑫
周亚萍
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China Pharmaceutical University
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China Pharmaceutical University
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/74Benzo[b]pyrans, hydrogenated in the carbocyclic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention discloses a lipid-lowering flavonoid. The flavonoid is commercially available, or is a monomer or a pharmaceutical salt thereof prepared according to an existing method. The pharmaceutical salt comprises a basic salt, such as sodium salt, potassium salt and calcium salt. The lipid-lowering flavonoid can be used for preparing drugs, health-care products, or functional food.

Description

A kind of flavone compound of lipid-loweringing
Technical field
The invention belongs to natural medicine field, disclose a kind of compound of lipid-loweringing, specifically disclose a kind of Huang of lipid-loweringing Ketone compounds.
Background technology
Barrenwort (Epimedium brevicornum Maxim) is jamaicin section plant barrenwort, Epimedium sagittatum, soft Hair barrenwort or the dried leaf of korean epimedium herb.Barrenwort is just loaded in《Sheng Nong's herbal classic》, " the main impotence of barrenwort described in book Hinder absolutely, pains in the penis, diuresis, beneficial gas power, strong will ".Barrenwort is traditional help class Chinese medicine, quilt《Chinese Pharmacopoeia》Recorded, Main product, in Shaanxi, Liaoning, Shandong, Sichuan and other places, has the effects such as kidney-replenishing, strengthening the bones and muscles, wines used as antirheumatic, to impotence, seminal emission, muscles and bones Aching and limp, numb in every limb contraction, climacteric hypertension, cardiovascular and cerebrovascular disease and improve immunity of organisms, the aspect such as antitumor has Significant curative effect.Epimedium active constituent and its extract have extensive physiologically active, and its research range is concentrated mainly on To the aspect such as osseous system, immunological regulation and anti-aging, reproductive system, cardiovascular system.
The flavone compounds such as anhydroicartin (Anhydroicaritin) are the main of traditional traditional tonic medicine barrenwort One of active monomer component.Recent study finds anhydroicartin to nervous system, internal system, cardiovascular system System, immune system all show performance pharmacological action to various diseases.So far there are no relevant anhydroicartin and its derivative fall The report of fat.
Content of the invention
The invention discloses a kind of flavone compound of lipid-loweringing, structural formula is as follows:
The invention discloses a kind of flavone compound of lipid-loweringing, in Formula one
R1=H ,-CH2CH3、CH3、rha、rha-glc、rha-xyl、rha-rha、
-CH2CH2CH=CH2、-CH2CH2OCH3、-CH2CH2Br、
-CH2CH=C (CH3)、-H2PO4、-HSO4
-CH2CH2OH、-CH2CH=CH2、-CH2COOH、-COO、
-COCH3、-CH(COOH)CH3、-CH2OCH3
-CH2CH2CH2OH、-CH2CH2NH2
-CH2CH=C (CH3)2、-CH2CH2CH2COOH、
-CH2COOCH2CH3、-(CH2)2O(CH2)2O(CH2)2OH、
-CH2CH=CHCOOH ,-(CH2)2COCH2
-CH(COOH)2、-COOC(CH)3,-COCH=C (CH3)2
-CH(CH3)COOCH2CH3、-CH(COOH)2
-(CH2)3COOCH2CH3、-CH2CHN(CH3)CH3
-CH2COOH、-(CH2)2OCH3、-(CH2)2OCH3、-SO2CH3
-CH2CH=CHCOOCH2CH3、-CO(CH2)2COOH
-CH2H2PO3、CH(COOH)CH3、-(CH2)2COOH
-CH2OCH3、-(CH2)2N(CH3)2、-CH2CH=CHCOOH
-COCH2CH2CH3
R2=H, glc, CH3、-CH2CH3、-CH2CH2OH、
-CH2CH=CH2、-CH2Ph、
-COCH3、-COOH、-CH(COOH)CH3、-CH2OCH3
-CH2CH2CH2OH、-CH2CH2NH2
-CH2CH=C (CH3)2、-(CH2)3COOH、
-CH2COOCH2CH3、-CH2CH=CHCOOH,
-CH(CH3)COOCH2CH3、-(CH2)2COOCH2CH3
-CH2COOH、-(CH2)2Ph、-SO3CH3
-CH2CH=CHCOOCH2CH3、-CH(COOH)CH3
-(CH2)2COOH、-CH2Ph、-(CH2)3COOH
-CH2CH=CHCOOH ,-COCH2CH2CH3
-CH(COOCH2CH3)
R3=H ,-CH3、-COCH3、-CH2CH3、-CH2Ph
The invention discloses a kind of flavone compound of formula one is used for preparing the composition of lipid-loweringing;
The invention discloses a kind of flavone compound of formula one is used for the composition that preparation reduces triglycerides;
The invention discloses a kind of flavone compound of formula one is used for the composition that preparation reduces T-CHOL;
The invention discloses a kind of flavone compound of formula one is used for the composition that preparation reduces intracellular triglyceride;
The invention discloses a kind of flavone compound of formula one is used for the composition that preparation reduces intracellular T-CHOL;
The invention discloses a kind of flavone compound of formula one is used for the composition that preparation reduces triglycerides in blood plasma;
The invention discloses a kind of flavone compound of formula one is used for the composition that preparation reduces T-CHOL in blood plasma;
The invention discloses a kind of pharmaceutical salts of the flavone compound of formula one include basic salt such as sodium salt, sylvite and calcium Salt;
The invention discloses a kind of flavone compound of formula one is made:Medicine, health products or functional food, figuration Agent or carrier are conventional excipient in pharmacy or field of food or carrier, such as diluent, disintegrant, lubricant etc..
The invention discloses anhydroicartin is used for preparing the composition of lipid-loweringing;
The invention discloses anhydroicartin is used for the composition that preparation reduces triglycerides;
The invention discloses anhydroicartin is used for the composition that preparation reduces T-CHOL;
The invention discloses anhydroicartin is used for the composition that preparation reduces intracellular triglyceride;
The invention discloses anhydroicartin is used for the composition that preparation reduces intracellular T-CHOL;
The invention discloses anhydroicartin is used for the composition that preparation reduces triglycerides in blood plasma;
The invention discloses anhydroicartin is used for the composition that preparation reduces T-CHOL in blood plasma;
The invention discloses anhydroicartin be:Anhydroicartin that is commercially available or pressing known method preparation or its medicine Use salt;
Wherein anhydroicartin pharmaceutical salts include basic salt such as sodium salt, sylvite and calcium salt;
Composition is made:Medicine, health products or functional food, excipient or carrier are normal in pharmacy or field of food Excipient or carrier, such as diluent, disintegrant, lubricant etc..
The invention discloses anhydroicartin is used for preparing the composition of lipid-loweringing.
The invention discloses anhydroicartin is used for preparing the composition of lipid-loweringing, the consumption of anhydroicartin is 30- 60mg/kg.
The invention discloses anhydroicartin be used for preparing lipid-loweringing composition, the consumption of anhydroicartin is 30mg/kg.
The invention discloses anhydroicartin be used for preparing lipid-loweringing composition, the consumption of anhydroicartin is 60mg/kg.
The invention discloses anhydroicartin is used for preparing the composition of lipid-loweringing, composition is made:Medicine, health products, Or functional food, excipient or carrier are conventional excipient in pharmacy or field of food or carrier, such as diluent, disintegration Agent, lubricant etc..
The invention discloses anhydroicartin is used for preparation treatment or the composition of prevention NASH;
The invention discloses anhydroicartin:For anhydroicartin that is commercially available or pressing known method preparation or its medicine Use salt;
Wherein anhydroicartin pharmaceutical salts include basic salt such as sodium salt, sylvite and calcium salt;
Composition is made:Medicine, health products or functional food, excipient or carrier are normal in pharmacy or field of food Excipient or carrier, such as diluent, disintegrant, lubricant etc..
The invention discloses anhydroicartin is used for preparation treatment or the composition of prevention NASH.
The invention discloses anhydroicartin is used for preparation treatment or the composition of prevention NASH, dehydration The consumption of icariine is 30-60mg/kg.
The invention discloses anhydroicartin is used for preparation treatment or the composition of prevention NASH, dehydration The consumption of icariine is 30mg/kg.
The invention discloses anhydroicartin is used for treating or prevent the composition of NASH, it is dehydrated excessive sheep The consumption of leaves of pulse plants element is 60mg/kg.
The invention discloses anhydroicartin is used for preparation treatment or the composition of prevention NASH, system Become:Medicine, health products or functional food, excipient or carrier are conventional excipient in pharmacy or field of food or carrier, As diluent, disintegrant, lubricant etc..
The invention discloses icariine is used for preparing the composition of lipid-loweringing;
The invention discloses icariine is used for the composition that preparation reduces triglycerides;
The invention discloses icariine is used for the composition that preparation reduces T-CHOL;
The invention discloses icariine is used for the composition that preparation reduces intracellular triglyceride;
The invention discloses icariine is used for the composition that preparation reduces intracellular T-CHOL;
The invention discloses icariine is used for the composition that preparation reduces triglycerides in blood plasma;
The invention discloses icariine is used for the composition that preparation reduces T-CHOL in blood plasma;
The invention discloses icariine be commercially available or by known method preparation icariine or its pharmaceutical salts;
Wherein icariine pharmaceutical salts include basic salt such as sodium salt, sylvite and calcium salt;
Composition is made:Medicine, health products or functional food, excipient or carrier are normal in pharmacy or field of food Excipient or carrier, such as diluent, disintegrant, lubricant etc..
The invention discloses icariine is used for preparing the composition of lipid-loweringing.
The invention discloses icariine is used for preparing the composition of lipid-loweringing, composition is made:Medicine, health products or work( Energy property food, excipient or carrier are conventional excipient in pharmacy or field of food or carrier, such as diluent, disintegrant, profit Lubrication prescription etc..
The invention discloses different anhydroicartin is used for preparing the composition of lipid-loweringing;
The invention discloses different anhydroicartin is used for the composition that preparation reduces triglycerides;
The invention discloses different anhydroicartin is used for the composition that preparation reduces T-CHOL;
The invention discloses different anhydroicartin is used for the composition that preparation reduces intracellular triglyceride;
The invention discloses different anhydroicartin is used for the composition that preparation reduces intracellular T-CHOL;
The invention discloses different anhydroicartin is used for the composition that preparation reduces triglycerides in blood plasma;
The invention discloses different anhydroicartin is used for the composition that preparation reduces T-CHOL in blood plasma;
The invention discloses different anhydroicartin be commercially available or by known method preparation different anhydroicartin or Its pharmaceutical salts;
Wherein different anhydroicartin pharmaceutical salts include basic salt such as sodium salt, sylvite and calcium salt;
Composition is made:Medicine, health products or functional food, excipient or carrier are normal in pharmacy or field of food Excipient or carrier, such as diluent, disintegrant, lubricant etc..
The invention discloses different anhydroicartin is used for preparing the composition of lipid-loweringing.
The invention discloses different anhydroicartin is used for preparing the composition of lipid-loweringing, composition is made:Medicine, health care Product or functional food, excipient or carrier are conventional excipient in pharmacy or field of food or carrier, and such as diluent collapses Solution agent, lubricant etc..
The invention discloses icariin is used for the composition that preparation reduces intracellular triglyceride;
The invention discloses icariin is used for the composition that preparation reduces intracellular triglyceride;Composition is made:Medicine Thing, health products or functional food, excipient or carrier are conventional excipient in pharmacy or field of food or carrier, such as dilute Release agent, disintegrant, lubricant etc..
The invention discloses icariin II is used for the composition that preparation reduces intracellular triglyceride;
The invention discloses icariin II is used for the composition that preparation reduces intracellular triglyceride;Composition is made: Medicine, health products or functional food, excipient or carrier are conventional excipient in pharmacy or field of food or carrier, such as Diluent, disintegrant, lubricant etc..
In order to make it easy to understand, being described in detail to the purposes of the present invention below by the drawings and specific embodiments.Need Will be it is emphasized that specific embodiments and the drawings be merely to explanation is it is clear that those skilled in the art can be according to herein Illustrate, the present invention being carried out with various corrections or changing, these are revised and change and also will include within the scope of the invention.
Brief description
Fig. 1. the mouse model changes of weight curve that anhydroicartin induces to high fat
Fig. 2. the mouse model food-intake change curve that anhydroicartin induces to high fat
Fig. 3. the mouse model hepatic pathology section oil red dyeing that anhydroicartin induces to high fat
Fig. 4. the mouse model hepatic pathology section HE dyeing that anhydroicartin induces to high fat
Fig. 5. the mouse model white adipose section HE dyeing that anhydroicartin induces to high fat
Fig. 6. the mouse model brown fat section HE dyeing that anhydroicartin induces to high fat
Become, with AHI structure similar monomer, the aglycon dividing in Fig. 7 barrenwort
Become, with AHI structure similar monomer, the glycosides dividing in Fig. 8 barrenwort
Fig. 9 reduces the activity of cell TC
Figure 10 reduces the activity of cell TG
The data recordation of the present invention is in following form:
The impact of the mouse model food-intake that table 1. anhydroicartin induces to high fat
Content of triglyceride in table 2. excrement
Total cholesterol level in table 3. excrement
Content of triglyceride in table 4. blood plasma
Total cholesterol level in table 5. blood plasma
Table 6. blood plasma middle-high density lipoprotein content
Low-density lipoprotein content in table 7. blood plasma
Table 8. liver weight
Total cholesterol level in table 9. liver
Content of triglyceride in table 10. liver
Specific embodiment
Embodiment 1
In order to study the impact to the mouse model that high fat induces for the anhydroicartin, using C57BL mouse, SPF level, hero Property, body weight (20 ± 2) g, it is randomly divided into two groups, first group 12, be normal group, give chow diet, remaining mouse (40) It is divided into 4 groups, give high lipid food (basal feed adds 20% lard, 1.25% cholesterol, 0.5% sodium taurocholate) and freely take the photograph Food, drinking-water.Give matrix, Lovastatin group (30mg/kg), anhydroicartin low concentration medicine (30mg/kg), dehydration respectively Icariine high concentration group (60mg/kg).Continuous nursing 6 weeks.
The collocation method of anhydroicartin:With 0.5% CMC-Na solution dissolving.
Observation index:
The ordinary circumstance of a animal
Animal used as test, illumination 12h night 12h, free diet drinking-water, during experiment, animal state is normal.
B observes weekly food-intake, body weight
C excrement triglycerides and total cholesterol level measure
The mouse model food-intake initial data of table 1. high fat induction
As Fig. 1. shown model group is compared normal group body weight and is significantly raised, and prompting modeling is very successful, and anhydroicartin is controlled After treating 6 weeks, body weight significantly reduces.As Fig. 2. and model group fasting amount shown in table 1. is higher, same prompting modeling success, dehydration is excessive Sheep leaves of pulse plants extract for treating after 6 weeks food-intake decrease.
Content of triglyceride in table 2. excrement, unit:mM
Compare with high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
Total cholesterol level in table 3. excrement, unit:mM
Compare with high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
In the excrement of mouse after modeling, T-CHOL (TC), triglycerides (TG) all significantly raise, and have significant system Difference learned by meter, shows modeling success, is administered TC, TG, the reduction of equal conspicuousness concentration dependent, has significant statistics poor Different, illustrate that therapeutic effect is notable.
Embodiment 2
The effect to the mouse model that high fat induces for the anhydroicartin
1st, animal used as test and method:
C57BL mouse, SPF level, male, body weight (20 ± 2) g, it is randomly divided into two groups, first group 12, be normal group, give With chow diet, remaining mouse (40) is divided into four groups of groups, give high lipid food (basal feed adds 20% lard, 1.25% Cholesterol, 0.5% sodium taurocholate) freely ingest, drink water.Give matrix, Lovastatin group (30mg/kg) respectively, be dehydrated excessive sheep Leaves of pulse plants element low concentration medicine (30mg/kg), anhydroicartin high concentration group (60mg/kg).After continuous nursing 6 weeks, blood sampling, place Extremely, take liver organization.
2nd, observation index:
The ordinary circumstance of a animal
Animal used as test is raised in SPF Animal House, illumination 12h night 12h, free diet drinking-water, animal-shaped during experiment State is normal.
B blood lipids:TC、TG、HDL、LDL
3rd, experimental result:
Result shows:Anhydroicartin can obviously reduce T-CHOL (TC) and triglycerides (TG) in blood plasma, rises High HDL (HDL-C), reduces after low-density lipoprotein (LDL-C) administration terminates and measures mouse, blood lipid level.Use T inspection carries out statistical analysis.Result shows, anhydroicartin has improvement result to high fat, has notable significant difference.
Content of triglyceride in table 4. blood plasma, unit:mM
Compare with high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
Total cholesterol level in table 5. blood plasma, unit:mM
* P < 0.05, * * P < 0.01, * * * P < 0.001
Table 6. blood plasma middle-high density lipoprotein content, unit:mM
Compare with high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
Low-density lipoprotein content in table 7. blood plasma, unit:mM
Compare with high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
T-CHOL (TC), triglycerides (TG) in the blood of mouse after modeling, HDL (HDL-C), low close Degree lipoprotein (LDL-C) all significantly raises, and has significant significant difference, shows modeling success, is administered TC, TG, LDL-C The reduction of equal conspicuousness concentration dependent, has significant significant difference, illustrates that therapeutic effect is notable.
HDL-C primarily serves the purpose of cholesterol metabolism from blood transportation to liver, is therefore referred to as " good " cholesterol, resists Atherosclerotic cholesterol, rising modeling group HDL-C due to TC significantly raises, and Lovastatin group and administration group all can show The content of the rising this " good cholesterol " of work property, illustrates that therapeutic effect is notable.Anhydroicartin can be effectively improved in a word Hyperlipidemia, reduces TG, TC, LDL-C, raises the content of " good cholesterol " HDL-C.
Embodiment 3
The therapeutic action to NASH for the anhydroicartin
Animal used as test and method:
C57BL mouse, SPF level, male, body weight (20 ± 2) g, it is randomly divided into two groups, first group 12, be normal group, give With chow diet, remaining mouse (40) gives to give high lipid food respectively, and (basal feed adds 20% lard, and 1.25% courage is solid Alcohol, 0.5% sodium taurocholate) freely ingest, drink water.It is divided into high fat group, high fat+Lovastatin group (30mg/kg), high fat+dehydration Icariine low concentration group (30mg/kg), high fat+anhydroicartin high concentration group (60mg/kg).Administration 6 weeks
Observation index:
The ordinary circumstance of a animal
Animal used as test, illumination 12h night 12h, free diet drinking-water, during experiment, animal state is normal.
B blood lipids:TC、TG、HDL、LDL
C pathological examination:HE dyes
D Liver lipids accumulate index of correlation:TC in TG in liver weight, liver, liver
Administration measures mouse, blood lipid level after terminating.Carry out statistical analysis using t inspection.
2. interpretation of result
TC in the blood of mouse after modeling, TG, HDL-C, LDL-C all significantly raise, and have significant significant difference, Show modeling success, be administered TC, the reduction of TG, LDL-C equal conspicuousness concentration dependent, there is significant significant difference, say Mingzhi's therapeutic effect is notable.
HDL-C primarily serves the purpose of cholesterol metabolism from blood transportation to liver, is therefore referred to as " good " cholesterol, resists Atherosclerotic cholesterol, rising modeling group HDL-C due to TC significantly raises, and Lovastatin group and administration group all can show The content of the rising this " good cholesterol " of work property, illustrates that therapeutic effect is notable.
In data display liver, the result of triglycerides and cholesterol level shows, triglycerides liter in liver after modeling Height, cholesterol about raises, and illustrates that in liver, triglycerides Cholesterol Accumulation is notable, gives Lovastatin and anhydroicartin Return to normal.In sum, the modeling of data display NASH is set up, and after administration, therapeutic effect is notable, has Significant difference.
Table 8. liver weight, unit:g
With high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
Total cholesterol level in table 9. liver, unit:Mg cholesterol/g fresh liver tissue
With high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
Content of triglyceride in table 10. liver, unit:Mg cholesterol/g fresh liver tissue
With high fat group, * P < 0.05, * * P < 0.01, * * * P < 0.001
The preparation of embodiment 4 anhydroicartin
Anhydroicartin tablet
Anhydroicartin 10mg, starch 88g, magnesium stearate 3g
Preparation technology:Take anhydroicartin to cross 100 mesh sieves, plus starch, magnesium stearate mix, and make particle, do Dry, compressing tablet, obtain final product.
Anhydroicartin capsule
Anhydroicartin 10mg, starch 88g, magnesium stearate 3g
Preparation technology:Take anhydroicartin to cross 100 mesh sieves, plus starch, magnesium stearate mix, and make particle, do Dry, encapsulated, obtain final product.
Anhydroicartin parenteral solution
Anhydroicartin 47mg, sodium chloride for injection 7mg
Preparation technology:Anhydroicartin is taken to cross 100 mesh sieves, plus the dissolving of 1.9mL water for injection, add sodium chloride for injection To isotonic, adjust pH value to 7~7.1, filter, refrigerate 24 hours, inject water to ormal weight, filtration, embedding, sterilizing, that is, ?.
Embodiment 6
Cell culture condition:Take the logarithm the HepG2 cell in growth period, planted in 6 orifice plates with 2.5 × 105 density. training After supporting 24, go to the medium culture 18h. cellular cholesterol containing medicine or DMSO, triglyceride determination kit carries out courage Sterol and triglyceride determination.
Tested by external Lipid-lowering activities, investigate the external fall with AHI structure similar monomer composition (Fig. 7,8) in barrenwort Fat activity,
These monomeric compounds are respectively anhydroicartin (AHI), ring anhydroicartin (AICT), the excessive sheep of different dehydration Leaves of pulse plants element (IAHI), icariine (ICT) and icariin (ICA), icariin I (ICAI), icariin II (ICA II), court The leaves of pulse plants determines A (EPM A), Epimedin B (EPM B), epimedin C (EPM C).The triglyceride (TG) intracellular to HepG2 and courage are solid The impact of alcohol (TC) content.Administration concentration:20μM.
Result such as Fig. 9, shown in Figure 10, AHI, ICT, IAHI are respectively provided with significant reduction cell TC, the activity of TG.And AICT Lipid-lowering activities not notable.
Meanwhile, in glycosides compound, ICA I and ICA II can significantly reduce intracellular TG content, but the impact to TC Not notable.And other glycosides compounds all do not significantly reduce cell TG, the activity of TC content.Therefore, external Lipid-lowering activities Experiment shows, in addition to anhydroicartin (AHI), different anhydroicartin (AICT), icariine (IAHI) and its part Glycosides compound also has Lipid-lowering activities.

Claims (10)

1. a kind of flavone compound of lipid-loweringing, structural formula is as follows:
R1=H ,-CH2CH3、CH3、rha、rha-glc、rha-xyl、rha-rha、
-CH2CH2CH=CH2、-CH2CH2OCH3、-CH2CH2Br、
-CH2CH=C (CH3)、-H2PO4、-HSO4
-CH2CH2OH、-CH2CH=CH2、-CH2COOH、-COO、
-COCH3、-CH(COOH)CH3、-CH2OCH3
-CH2CH2CH2OH、-CH2CH2NH2
-CH2CH=C (CH3)2、-CH2CH2CH2COOH、
-CH2COOCH2CH3、-(CH2)2O(CH2)2O(CH2)2OH、
-CH2CH=CHCOOH ,-(CH2)2COCH2
-CH(COOH)2、-COOC(CH)3,-COCH=C (CH3)2
-CH(CH3)COOCH2CH3、-CH(COOH)2
-(CH2)3COOCH2CH3、-CH2CHN(CH3)CH3
-CH2COOH、-(CH2)2OCH3、-(CH2)2OCH3、-SO2CH3
-CH2CH=CHCOOCH2CH3、-CO(CH2)2COOH
-CH2H2PO3、CH(COOH)CH3、-(CH2)2COOH
-CH2OCH3、-(CH2)2N(CH3)2、-CH2CH=CHCOOH
-COCH2CH2CH3
R2=H, glc, CH3、-CH2CH3、-CH2CH2OH、
-CH2CH=CH2、-CH2Ph、
-COCH3、-COOH、-CH(COOH)CH3、-CH2OCH3
-CH2CH2CH2OH、-CH2CH2NH2
-CH2CH=C (CH3)2、-(CH2)3COOH、
-CH2COOCH2CH3、-CH2CH=CHCOOH,
-CH(CH3)COOCH2CH3、-(CH2)2COOCH2CH3
-CH2COOH、-(CH2)2Ph、-SO3CH3
-CH2CH=CHCOOCH2CH3、-CH(COOH)CH3
-(CH2)2COOH、-CH2Ph、-(CH2)3COOH
-CH2CH=CHCOOH ,-COCH2CH2CH3
-CH(COOCH2CH3)
R3=H ,-CH3、-COCH3、-CH2CH3、-CH2Ph.
2. a kind of flavone compound according to claim 1 the purposes preparing lipid-lowering composition it is characterised in that:For making Make preparation for dropping low triglyceride or and, reduce T-CHOL composition.
3. a kind of flavone compound according to claim 1 the purposes preparing lipid-lowering composition it is characterised in that:Dehydration is excessive Sheep leaves of pulse plants element.
4. a kind of flavone compound according to claim 2 the purposes preparing lipid-lowering composition it is characterised in that:Dehydration is excessive Sheep leaves of pulse plants element.
5. a kind of flavone compound according to claim 1 or 2 the purposes preparing lipid-lowering composition it is characterised in that:De- The consumption of water icariine is 30-60mg/kg.
6. a kind of flavone compound according to claim 1 the purposes preparing lipid-lowering composition it is characterised in that:Dehydration is excessive Sheep leaves of pulse plants element is for the composition of preparation treatment or prevention NASH.
7. according to claim 1 or, a kind of purposes preparing lipid-lowering composition of 2 flavone compound it is characterised in that: Icariine or, different anhydroicartin.
8. a kind of flavone compound according to claim 1 the purposes preparing lipid-lowering composition it is characterised in that:Barrenwort Glycosides or, icariin II.
9. a kind of flavone compound according to claim 1 the purposes preparing lipid-lowering composition it is characterised in that:Barrenwort Glycosides or, icariin II be used for preparation reduce triglycerides composition.
10. a kind of flavone compound according to claim 1 the purposes preparing lipid-lowering composition it is characterised in that:
Flavone compound pharmaceutical salts include basic salt such as sodium salt, sylvite and calcium salt;
Composition is made:Medicine, health products or functional food;
Excipient or carrier are conventional excipient in pharmacy or field of food or carrier.
CN201610744109.5A 2016-08-25 2016-08-25 Lipid-lowering flavonoid Pending CN106380459A (en)

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