CN101632655A - Resveratrol and bioflavonoid nutritional composition for delaying senility - Google Patents
Resveratrol and bioflavonoid nutritional composition for delaying senility Download PDFInfo
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Abstract
The invention relates to a resveratrol and bioflavonoid nutritional composition for delaying senility or used for treating and preventing diseases relevant to aging. The invention adopts the combination of resveratrol and bioflavonoid and prepares oral liquid, capsules, tablets, granules and powder. The invention overcomes the defect that the absorptivity of antitype resveratrol in the prior art is very high, but the bioavailability is very low; A composition of the resveratrol and quercetin can prolong the detention time of the resveratrol in blood and enhance the acting time of the resveratrol, but only part of the resveratrol is not metabolized and acts together with the quercetin to enhance the function of delaying senility; and the rest part of the resveratrol after being converted into the sulfate or glucuronic acid salt of the resveratrol by metabolism does not generate a synergistic action with the quercetin again, and the effect of the resveratrol for delaying senility is lowered. The invention greatly prolongs the detention time of the resveratrol in a human body, exerts the function of the resveratrol for resisting senility, solves the problem that the resveratrol is metabolized, and is innoxious.
Description
Technical field
The present invention relates to a kind of nutraceutical composition, particularly a kind of slow down aging or be used for the treatment of and the resveratrol of prevention and aging diseases associated and the alimentation composition of bioflavonoids.
Background technology
In the fifties, few people can live unnecessary 100 years old or even 90 years old, yet after half a century, the meals of flourishing medical skill and health and the variation of life style have improved the health status and the quality of the life of old and feeble colony significantly, the people at 85 years old and above age is more and more, but when people live more for a long time, also have more disease and other diseases in old and feeble colony, delaying senility course and the nutraceutical composition that reduces the age-related disease sickness rate become pressing for of people.
Trans-resveratrol is a kind of non-flavonoid polyphenolic substance of finding in some plants, and these plants much are the parts of human diet, as Fructus Mori, Semen arachidis hypogaeae, Fructus Vitis viniferae and red wine.Particularly in the past 10 years, trans-resveratrol becomes the focus of many researchs, and these researchs are devoted to explore its health-benefiting.A lot of evidences show that trans-resveratrol is a kind of free radical scavenger and a kind of potent antioxidant, promote NO production, increase high density lipoprotein (HDL) cholesterol, suppress the oxidation of platelet aggregation and low density lipoprotein, LDL.Verified, 3 Main Stage that trans-resveratrol takes place cancer (start, promote and progress) all have positive resistant function.The neuroprotective properties of trans-resveratrol has also obtained proof, some Notes of Key Datas, and trans-resveratrol is brought into play regulating action in the number of mechanisms that Alzheimer disease pathologic is learned, diabetic neuropathy is had potential health-benefiting.
Before this method invention, cholesterol levels, anti-platelet aggregation, the Oxidation of anti-human low density lipoprotein, the research of antitumaous effect aspect that resveratrol is regulated in the blood mainly as antioxidant are more, also apply in medicine and the nourishing healthy product simultaneously to sell on market.
Studies show that of recent years, trans-resveratrol can prolong the life-span of many species, prove that it has very big potential as the defying age factor, antidotal resveratrol product has also just appearred on the market much being known as, but these products are because not enough to the antidotal metabolic mechanism of resveratrol understanding, its as the defying age thing without any actual effect.With regard to its mechanism, the absorbance of oral single trans-resveratrol is very high, but bioavailability is very low.This is because about oral single resveratrol half-life 4h, just loses efficacy behind oral about 2h, in blood, just detect fully less than.After trans-resveratrol absorbs, the resveratrol of part in first pass metabolism (First Pass Metabolism) process by biotransformation rapidly and widely, after phenolic group in its structure (phenol group) combines by metabolic pathway and the sulfate (sulphate) identified and glucuronic acid (glucuronic acid), the time that stops in blood is very short, excrete by liver and kidney rapidly, have little time to act on relevant antidotal biorgan, also just do not have any anti-aging effects.
The research of up-to-date slow down aging is the compositions that resveratrol adds quercetin, show by adding the variation that quercetin (Quercetin) can suppress its resveratrol activity conformation, thereby the holdup time of significant prolongation resveratrol in blood, extend to 4～7 times of former time, can improve the action time of resveratrol, significantly strengthen the function of resveratrol slow down aging.But nearest studies show that, because after resveratrol enters blood, have only the part resveratrol to strengthen function in delaying senility with the quercetin combined effect not by metabolism, and after the resveratrol of remainder is transformed into the sulfate or glucuronate salt of resveratrol by metabolism, no longer with quercetin generation synergism, part has reduced the effect of resveratrol slow down aging.
Summary of the invention
Purpose of the present invention just is to overcome above-mentioned defective, by the combination of resveratrol and bioflavonoids, develops a kind of antidotal alimentation composition or health medicine.
Technical scheme of the present invention is:
The resveratrol of slow down aging and bioflavonoid nutritional composition, its major technique is characterised in that by resveratrol, bioflavonoids to be formed, bioflavonoids is that one or more the material in quercetin, Semen Vitis viniferae extract, blue berry extract, green tea extract, the curcumin is formed, and described unit dose scope is resveratrol 10～350mg, quercetin 8～500mg, Semen Vitis viniferae extract 20～500mg, blue berry extract 10～500mg, green tea extract 10～500mg, curcumin 10～500mg.
The further technical scheme of the present invention is, compositions can be used as the additive of some food or medicine or supplementary and joins in the product (especially for prevention and old and feeble diseases associated), bread and cheeses such as cookies, confection, beverage for example, health food, food of special nutrients, nutrient prime replenisher, medicine etc.
Though advantage of the present invention and effect are that resveratrol time of staying in human body is short, equally have the time that behind the bioflavonoids (as Semen Vitis viniferae extract, blue berry extract and green tea extract) of the variation that can suppress its effective active conformation resveratrol is stopped with quercetin in human body and prolong greatly but add, thereby give full play to its antidotal effect and effect; And the bioflavonoids from plant extract that adds; have a kind of " stealth technology "; utilize resveratrol and them to contain identical benzene ring structure and polyhydric phenols hydroxyl structure exactly; can the out-trick identification of body metabolism system of common structure; can be after making resveratrol enter blood flow by metabolism; thereby the protection resveratrol is not subjected to make the influence of the factor that its recurring structure changes; solved simultaneously resveratrol by metabolic defect problem and in blood too short problem of the time of staying; therefore have fabulous bioavailability, given full play to the function of resveratrol slow down aging.Semen Vitis viniferae extract, blue berry extract, green tea extract and curcumin itself also have antidotal function and cooperate with resveratrol, jointly aging are had inhibitory action, give full play to synergism; And the Semen Vitis viniferae extract of increase, blue berry extract, green tea extract and curcumin can't bring toxic and side effects all from natural, and be promptly nontoxic.
Description of drawings
Fig. 1-------trans-resveratrol mean plasma concentration time plot.
The specific embodiment
Embodiment 1:
Get resveratrol 60mg, quercetin (Quercetin) 50mg, Semen Vitis viniferae extract 100mg, blue berry (Yue Fructus Citri tangerinae) extract 50mg, green tea extract 100mg, curcumin 100mg, mix homogeneously; The adjuvant that adding dosage form and mouthfeel needs can be made into oral liquid, capsule, tablet, granule, powder.
Embodiment 2:
Get resveratrol 150mg, Semen Vitis viniferae extract 300mg, blue berry extract 150mg, green tea extract 250mg, curcumin 250mg, mix homogeneously; The adjuvant that adding dosage form and mouthfeel needs can be made into oral liquid, capsule, tablet, granule, powder.
Embodiment 3:
Get resveratrol 45mg, quercetin 20mg, Semen Vitis viniferae extract 40mg, blue berry extract 10mg, mix homogeneously; The adjuvant that adding dosage form and mouthfeel needs can be made into oral liquid, capsule, tablet, granule, powder.
Embodiment 4:
Get resveratrol 45mg, Semen Vitis viniferae extract 40mg, blue berry extract 50mg, mix homogeneously; The adjuvant that adding dosage form and mouthfeel needs can be made into oral liquid, capsule, tablet, granule, powder.
Embodiment 5:
Get resveratrol 10mg, green tea extract 220mg, curcumin 165mg, mix homogeneously; The adjuvant that adding dosage form and mouthfeel needs can be made into oral liquid, capsule, tablet, granule, powder
Embodiment 6:
Get resveratrol 250mg, Semen Vitis viniferae extract 400mg, green tea extract 350mg, mix homogeneously; The adjuvant that adding dosage form and mouthfeel needs can be made into oral liquid, capsule, tablet, granule, powder
Embodiment 7:
Get resveratrol 45mg, Semen Vitis viniferae extract 300mg, mix homogeneously; The adjuvant that adding dosage form and mouthfeel needs can be made into oral liquid, capsule, tablet, granule, powder
The lipid peroxidation that free radical and metabolite thereof cause that studies show that in recent years can cause aging and Senile disease, SOD is a key enzyme of removing free radical in the body, detect the active height of SOD, can reflect body removing free radical ability indirectly, MDA is the catabolite of free radical challenge organism, the degree of injury that how much can reflect tissue indirectly that MDA generates.The compositions that shows resveratrol and bioflavonoids by experiment can improve mouse aging SOD in serum content, reduce the MDA level, therefore can accelerate the removing of free radical, has stronger oxidation resistance, the compositions of resveratrol and bioflavonoids can also be resisted aging that the lipid peroxidation that caused by free radical and metabolite thereof causes, can slow down the body atrophy of thymus gland, thereby make cell quantity increase increased functionality, the human body immunity improving function, can also delay body, tissue injury's process is so have function in delaying senility.
Particularly:
1. the compositions that studies show that resveratrol and bioflavonoids can be by prolonging the life-span of fruit bat and mice to the regulation and control of insulin approach.By a large amount of experimentatioies and document verification, surpass old man at the age of one hundred years old and have insulin replies efficiently usually, therefore can prove by adjusting it is to postpone relevant disease of age to the insulin signaling transduction pathway, reach the purpose of slow down aging.
2. behind the flavonoid such as oral resveratrol and Semen Vitis viniferae extract, blue berry extract and green tea extract, experimental results show that and to stop resveratrol by the variation of metabolism and conformation, prolong the life-span of resveratrol active structure, in blood, can keep high valid density, thereby make resveratrol that be arranged sufficiently long action time, reach the function of slow down aging.
3. the active component of above compositions has different mechanism of action, compare with the single composition of resveratrol, have synergism, can more effectively act on the different key signal transduction pathway that relates to aging, thus delay senility and aging diseases related.Compositions of the present invention can partly delay cell or biological aging course by acting on nutrient sensation and insulin signaling transduction pathway (it was associated with old and feeble and life-span).Specifically, compositions of the present invention also can start ancient existence reflex mechanism in the organism, quickens living cells and makes the aging resistance ferment, activates Sirtuins defying age enzyme, and stabilized DNA prolongs cell survival.
4. laboratory and zooscopy result show that clearly " resveratrol " and its derivant are all quite active; Yet as if we notice that resveratrol is very fast at the metabolic rate of human body, and this will have influence on the absorbance problem of resveratrol.The method of improving the resveratrol absorbance is thought in research, is the bioflavonoids that adds from plant extract, as Semen Vitis viniferae extract, blue berry extract and green tea extract, can slow down the metabolic rate of resveratrol,, improve its bioavailability to increase its absorbance.
5. after the present invention carries out such combination; it or not simple stack;, the DNA in the coordinating protection cell mitochondrial (DNA (deoxyribonucleic acid)) prolongs the life-span of cell but exempting from chemical damage; through relevant experimental study; the present invention can bring into play tangible function in delaying senility, and safe without toxic side effect.
Experimental results show that:
Resveratrol (resveratrol; Res), quercetin, Semen Vitis viniferae extract, blue berry extract, green tea extract, curcumin all have stronger antioxidation, the effect of free radical resisting, the main life-span that prolongs cell by the activity that activates histon deacetylase (HDAC).Res is a kind of Polyphenols chemical substance that produces naturally, extensively is present in some plants, and as Fructus Vitis viniferae, berry and Semen arachidis hypogaeae, it is a kind of non-flavone polyphenol compound that contains the stilbene class formation, has important biological action.Resveratrol can play the highest activation activity to Sir2 by the Km value that reduces the acetylation substrate, makes its life-span prolong 70%.Utilize resveratrol Come to increase the life-span of fat mouse, find that he has reversed some and diabetes are arranged in all gene expressions of high caloric diet mouse, heart disease and other and all fat relevant diseases, and find that first this micromolecular compound resveratrol is to mammiferous benefit, successively have some studies show that in recent years, resveratrol helps to prolong the life-span of yeast, nematicide etc.
Resveratrol has the form of two kinds of existence: cis and trans.Naturally occurring resveratrol is generally trans, after trans-resveratrol is absorbed and enters blood of human body, when not having the common existence of bioflavonoids, in blood, change cis-resveratrol. rapidly into, excrete with urine, and add bioflavonoids common absorb enter blood after, they will suppress trans-resveratrol and change cis-resveratrol. into, and prolong its time of staying in vivo, give full play to its effect.And resveratrol is when existing jointly with bioflavonoids, and resveratrol will change when combining with the SIRT1 gene, regulates the phase legumin gene of p53-AMC, thereby increases the survival of cell, prolongs the life-span of cell greatly.
Resveratrol and bioflavonoids are collaborative, can start ancient existence reflex mechanism in the organism, quicken living cells and make the aging resistance ferment, activate Sirtuins defying age enzyme, and stabilized DNA prolongs cell survival.Resveratrol and bioflavonoids are collaborative to improve the yeast life-span, and its while also can prolong the life-span of fruit bat, allows general originally about one month fruit bat that only lives live last ten days more.When using when giving yeast, time just in the dust yeast can many again divisions 15 times to divide 25 originally.
To a kind of useful nutrition Said usually, it must be by biological utilisation, and this just means that it must easily be absorbed by digestive tract and enter blood flow, and can keep the sufficiently long time in blood flow, makes it can arrive required cell.Laboratory and zooscopy result show that clearly " resveratrol " and its derivant are all quite active; Oral resveratrol can be absorbed (at least 70%) well by digestive tract, but its bioavailability is almost 0.This obvious " contradiction " owing to resveratrol can by fast widely metabolism be Two kind chemical derivative: sulfate Class and glucuronide.Mostly the Number resveratrol can be converted into these metabolites in metabolism, and these products more easily absorb and enter blood flow.This process is approximately finished in half an hour by liver.As a result, in fact not not metabolic resveratrol can retain down Come and enter blood flow and act on corresponding system and organ.
We adopt a kind of " stealth technology "; it is the bioflavonoids that adds from plant extract; as Semen Vitis viniferae extract, blue berry (Yue Fructus Citri tangerinae) extract and green tea extract; utilize resveratrol and them to contain identical benzene ring structure and polyhydric phenols hydroxyl structure; can the out-trick identification of body metabolism system of common structure; make resveratrol more easily enter blood flow, and can protect it not to be subjected to make the influence of the factor that it changes, therefore have fabulous bioavailability.Because this technology can guarantee efficiently to be transported to free resveratrol in the blood, thereby make that the resveratrol level is higher in the blood, and owing to have common structure, resveratrol can all not discharged or be released into the same area immediately, therefore can in blood, be maintained at higher level, so resveratrol can there be more time Come to bring into play its benefit.In a research, behind the oral resveratrol, detect point free resveratrol in blood any time.Find that behind the oral single resveratrol, still having at first can detected level, but descends fast subsequently, has approximately just disappeared after half an hour.Yet, simultaneously behind oral resveratrol and Semen Vitis viniferae extract, blue berry extract and the green tea extract, can prolong the life-span of the resveratrol of load, after 12 hours, just can not detect, prove that resveratrol can keep the sufficiently long time in blood flow.So we think the method for improving the resveratrol bioavailability, add bioflavonoids exactly from plant extract, as Semen Vitis viniferae extract, blue berry extract, green tea extract and curcumin, can slow down the metabolic rate of resveratrol, to increase its absorbance, improve its bioavailability.
Prescription with embodiment 3 carries out the first research of trans-resveratrol at healthy volunteer's drug disposition dynamic metabolism as the product of testing, object of study has 4 groups, every group of 10 healthy adult experimenters (5 male, 5 women), for 4 groups of experimenters, select wherein 1 group to give placebo (SD group) at random, the 2nd group gives single trans-resveratrol (R group), the 3rd group gives trans-resveratrol and quercetin (RQ group), and the 4th group gives resveratrol and quercetin, Semen Vitis viniferae extract and blue berry extract (RQP group).In preceding 4 hours after taking medicine, per hour measure the concentration of 1 interior trans-resveratrol of blood plasma, after this measured 1 time every 2 hours.Make the change curve of mean plasma concentration value and time.We can see from curve, and after single dose was taken, the half-life of trans-resveratrol was 2 hours, take 4 hours after, in the blood plasma just after testing less than.And take resveratrol and quercetin, the concentration of trans-resveratrol maintains about 4ng/mL substantially in the blood plasma, takes resveratrol and quercetin, Semen Vitis viniferae extract and blue berry extract concentrations and maintains about 7ng/mL substantially.Can learn thus, resveratrol adds quercetin, Semen Vitis viniferae extract and blue berry extract) after can prolong its concentration in blood, thereby can continuous action, increase its bioavailability, reach the physiological function of resveratrol slow down aging, and do not find in the laboratory detection index clinical relevant abnormalities is arranged, aspect vital sign, neurologic check and electrocardiographic recorder, all there is not the significantly clinical announcement that appears in the newspapers unusually.
In the research to mouse, will test mouse and be divided into four groups: first group gives general diet (being called for short the SD group); Second group of diet that gives high heat, wherein percent 60 of total amount of heat from fat (being called for short the HC group); The 3rd group give with second group of identical food, and add to edible resveratrol and quercetin (being called for short HCR organizes); The 4th group give with second group of identical food, and add to edible resveratrol and quercetin, Semen Vitis viniferae extract and blue berry extract (being called for short HCRP organizes).All mouse all are that about 52 weeks are big when beginning to do experiment, are equivalent to the mankind in middle age.
In 60 weeks when big, HC group, HCR group and HCRP group mouse survival rate begin difference and keep 3 to 6 months difference.In 114 weeks when big, the HC group has percent 58 death, and HCR group and SD group have only percent 42 death, and HCRP organizes and has only percent 30 death.Find that resveratrol can make the mortality rate of HC group reduce by percent 31, reduce near percent 50 and add the mortality rate of finding the HCRP group behind Semen Vitis viniferae extract and the blue berry extract, do not have significantly increase even compare mortality rate yet, lower mortality rate is arranged on the contrary with the SD group.In 130 whens week, HC organizes percent 100 death, and SD organizes percent 80 death, and HCR organizes percent 70 death, and the HCRP group has only percent 50 death.In 150 whens week, SD organizes percent 100 death, and HCR organizes percent 90 death, and the HCRP group has only percent 80 death.170 when week HCR organize percent 100 death; 180 when week HCRP organize percent 100 death; We can see thus, because the life-span of this mouse is two-and-a-half years (131 weeks), the life-span of the life-span of resveratrol and quercetin (being called for short the HCR group) than normal group (SD) prolongs 13.3%; HCRP group (Semen Vitis viniferae extract and blue berry extract group) prolongs 20% than the life-span of normal group (SD), than the life-span of HCR group to prolong 7% more.Undoubtedly, we have seen that mouse can increase the life-span, and it is about percent 15 that the middle life-span increases, and the terminal life increase is about percent 20.
Research finds that also HCR group and HCRP group have extraordinary body constitution, the mouse that surpasses the HC group far away in physical stamina test.The mouse of feeding resveratrol and compositions is just long-lived, and their vigor is better, can test result prove aging improving.
Studies show that each polyphenoils all has unique effect to human body, cooperate each other to produce " synergism ", go deep into each cell of human body and tissue, really reach free radical resisting, antioxidative optimum efficiency.The collaborative conformation that promptly can suppress resveratrol of resveratrol and quercetin changes and prolongs its time of staying in blood; and flavonoid such as Semen Vitis viniferae extract, blue berry extract and green tea extract can effectively improve the bioavailability of resveratrol, and their common characteristic is exactly that DNA (DNA (deoxyribonucleic acid)) in the coordinating protection cell mitochondrial exempts from chemical damage and brings into play function of delaying senility.
The present invention is raw materials used can both to buy from the market, used resveratrol raw material is a trans-resveratrol, be that from plant such as Fructus Vitis viniferae, Rhizoma Polygoni Cuspidati etc., extract or synthetic by chemical method, the effective ingredient of Semen Vitis viniferae extract is procyanidin (〉=80%), the effective ingredient of blue berry (Yue Fructus Citri tangerinae) extract is anthocyanidin (〉=20%), the effective ingredient of quercetin is Quercetin (〉=80%), the effective ingredient of green tea extract is catechin ((〉=40%), the effective ingredient of curcumin 〉=60%.
The claimed scope of the present invention is not limited only to the description of the foregoing description.
Claims (8)
1. the resveratrol of slow down aging and bioflavonoid nutritional composition, it is characterized in that forming by resveratrol, bioflavonoids, bioflavonoids is that one or more the material in quercetin, Semen Vitis viniferae extract, blue berry extract, green tea extract, the curcumin is formed, and described unit dose scope is resveratrol 10～350mg, quercetin 8～500mg, Semen Vitis viniferae extract 20～500mg, blue berry extract 10～500mg, green tea extract 10～500mg, curcumin 10～500mg.
2. the resveratrol of slow down aging according to claim 1 and bioflavonoid nutritional composition is characterized in that unit dose contains resveratrol 60mg, quercetin 50mg, Semen Vitis viniferae extract 100mg, blue berry extract 50mg, green tea extract 100mg, curcumin 100mg.
3. the resveratrol of slow down aging according to claim 1 and flavonoid alimentation composition is characterized in that unit dose contains resveratrol 150mg, Semen Vitis viniferae extract 300mg, blue berry extract 150mg, green tea extract 250mg, curcumin 250mg.
4. the resveratrol of slow down aging according to claim 1 and bioflavonoid nutritional composition is characterized in that unit dose contains resveratrol 45mg, quercetin 20mg, Semen Vitis viniferae extract 40mg, blue berry extract 10mg.
5. the resveratrol of slow down aging according to claim 1 and bioflavonoid nutritional composition is characterized in that unit dose contains resveratrol 45mg, Semen Vitis viniferae extract 40mg, blue berry extract 50mg.
6. the resveratrol of slow down aging according to claim 1 and bioflavonoid nutritional composition is characterized in that unit dose contains resveratrol 10mg, green tea extract 220mg, curcumin 165mg
7. the resveratrol of slow down aging according to claim 1 and bioflavonoid nutritional composition is characterized in that unit dose contains resveratrol 250mg, Semen Vitis viniferae extract 400mg, green tea extract 350mg
8. the resveratrol of slow down aging according to claim 1 and bioflavonoid nutritional composition is characterized in that unit dose contains resveratrol 45mg, Semen Vitis viniferae extract 300mg.
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