Application of burdock extract and composition thereof in preparation of products for preventing, delaying or improving equol deficiency related diseases or symptoms
By promoting the production of equol in the intestines through burdock extract, the problem of equol deficiency is solved, and a significant equol production effect is achieved. It is suitable for drugs and health products to prevent or improve related diseases.
Patent Information
- Application Number
- CN202511684803.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-11-17
- Publication Date
- 2026-02-17
AI Technical Summary
Some individuals are unable to produce equol in their gut, which limits the health benefits of soy isoflavones. Existing technologies have failed to effectively promote the conversion of soy isoflavones into equol by gut microbes.
Burdock extract, especially high-content burdock polysaccharide, was used in an in vitro fermentation experiment. The extract was extracted with hot water, defatted and deproteinized, and impurities were removed by dialysis. It significantly promoted the conversion of daidzein to estrol.
It significantly increases the production of equol, providing a safe and natural endogenous equol production strategy suitable for pharmaceuticals, health supplements, and functional foods, to prevent or improve equol deficiency-related diseases.
Smart Images
Figure CN121534094A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of biotechnology, and more particularly to the use of burdock extract and its compositions in the preparation of products for the prevention, delay or improvement of diseases or symptoms related to equol deficiency. Background Technology
[0002] Equol is an active substance produced from the metabolism of soy isoflavones (mainly daidzein) by specific microorganisms in the intestine. Equol exhibits strong dual regulatory effects, acting as both an estrogen-like substance and an anti-estrogen. Its binding affinity to estrogen receptors (especially ERβ) is far stronger than that of soy isoflavones, and it can efficiently target tissues such as the breast and prostate. Numerous epidemiological and intervention studies have shown that equol can effectively prevent and improve hormone-dependent cancers (such as breast and prostate cancer), alleviate menopausal syndrome, increase bone density in postmenopausal women to prevent osteoporosis, and improve lipid metabolism to combat hyperlipidemia and arteriosclerosis.
[0003] Not everyone who consumes soy can produce equol in their body. Studies show that only about 30%–60% of the Asian population and 25%–30% of the Western population have specific bacteria in their gut capable of efficiently synthesizing equol; these individuals are known as "equol producers." The vast majority of the remaining population are "non-producers." For non-producers, even consuming large amounts of soy products will not provide the numerous health benefits of equol, thus significantly limiting the potential functions of soy isoflavones. Therefore, direct equol supplementation or promoting its endogenous production through dietary means has become a research hotspot. Summary of the Invention
[0004] To address the problem of insufficient production of endogenous equol in the intestine, this invention provides the application of burdock extract and its composition in the preparation of products for preventing, delaying or improving diseases or symptoms related to equol deficiency, so as to effectively promote the production of endogenous equol in the intestine.
[0005] This invention provides the use of burdock extract in the preparation of products for the prevention, delay or improvement of diseases or conditions related to equol deficiency.
[0006] Burdock (Arctium lappa L.) is a traditional plant used for both food and medicine. Its roots are rich in various bioactive components, mainly including inulin, polyphenols, and chlorogenic acid. These components endow burdock with significant antioxidant, anti-inflammatory, and immunomodulatory functions, while effectively promoting the proliferation of beneficial bacteria in the gut and improving the intestinal environment. Although numerous studies have revealed the potential of burdock in metabolic regulation and chronic disease prevention, no existing technology has clearly reported the ability of burdock or its extracts to promote the conversion of soy isoflavones into equol by gut microbes. This novel functional application is the first disclosure of this invention.
[0007] In vitro fermentation experiments confirmed that adding the burdock extract of this invention significantly promoted the production of equol in a fermentation system containing daidzein and human gut microbiota, with a significantly higher yield compared to the positive control group containing only daidzein. This burdock extract is a safe, natural, and non-toxic raw material, providing an effective intervention strategy for promoting human gut equol production. It can be used to develop drugs, health products, or functional foods to prevent, delay, or improve diseases or conditions related to equol deficiency (such as menopausal syndrome, osteoporosis, and the risk of hormone-dependent cancers).
[0008] As a preferred use, burdock extract is used in the preparation of products for the prevention, delay or improvement of diseases or conditions associated with equadol deficiency in mammalian subjects.
[0009] Preferably, the burdock extract contains ≥90% burdock polysaccharides by mass.
[0010] This method controls the mass content of burdock polysaccharides in burdock extract to ≥90%, which can further promote the conversion of soy isoflavones into estrol by intestinal microorganisms.
[0011] Preferably, the preparation method of the burdock extract includes the following steps: burdock root is extracted by reflux extraction with hot water at a temperature of 80℃~90℃, the extract is defatted, deproteinized, precipitated with ethanol, and the precipitate is dissolved and then dialyzed to remove small molecule impurities. The dialysis membrane used for dialysis has a molecular weight cutoff of ≥3500 Da.
[0012] Preferably, the dialysis membrane used in the dialysis has a molecular weight cutoff of 3500 Da to 25000 Da.
[0013] As a preferred method, burdock root is extracted using hot water reflux at a temperature of 80℃.
[0014] Preferably, the dialysis membrane used in the dialysis has a molecular weight cutoff of 3500 Da.
[0015] Preferably, the diseases or conditions associated with equol deficiency include at least one of hormone-dependent cancer, menopausal syndrome, osteoporosis, hyperlipidemia, and arteriosclerosis.
[0016] Preferably, the hormone-dependent cancer includes at least one of breast cancer, prostate cancer, and colorectal cancer.
[0017] Preferably, the product includes at least one of pharmaceuticals, food, and health products.
[0018] The present invention provides a composition comprising burdock extract for preventing, delaying or improving diseases or conditions related to equol deficiency and pharmaceutically, food or health product acceptable excipients or carriers.
[0019] Preferably, in the composition, the burdock polysaccharide content in the burdock extract for preventing, delaying or improving diseases or symptoms related to equol deficiency is ≥90%.
[0020] Preferably, in the composition, the method for preparing the burdock extract for preventing, delaying or improving diseases or symptoms related to equol deficiency includes the following steps: extracting burdock root by reflux extraction with hot water at a temperature of 80℃~90℃, defatting and deproteinizing the extract, precipitating with ethanol, dissolving the precipitate and then dialyzing to remove small molecule impurities, wherein the dialysis membrane used for dialysis has a molecular weight cutoff of ≥3500 Da.
[0021] Preferably, the dialysis membrane used in the dialysis has a molecular weight cutoff of 3500 Da to 25000 Da.
[0022] As a preferred method, burdock root is extracted using hot water reflux at a temperature of 80℃.
[0023] Preferably, the dialysis membrane used in the dialysis has a molecular weight cutoff of 3500 Da.
[0024] Preferably, the composition further includes daidzein.
[0025] More preferably, the mass ratio of the burdock extract to the daidzein is (100~200):1, for example, it can be 100:1, 120:1, 140:1, 150:1, 170:1, 190:1, 200:1, but is not limited to the listed values. Other unlisted values within the range are also applicable.
[0026] Preferably, the dosage form of the composition includes at least one of tablets, capsules, granules, pills, powders, and oral liquids. Attached Figure Description
[0027] To more clearly illustrate the technical solutions in this invention or the prior art, the drawings used in the description of the embodiments or the prior art will be briefly introduced below. Obviously, the drawings described below are some embodiments of this invention. For those skilled in the art, other drawings can be obtained from these drawings without creative effort.
[0028] Figure 1 This is the standard curve of equadol. Detailed Implementation
[0029] To make the objectives, technical solutions, and advantages of this invention clearer, the technical solutions of this invention will be clearly and completely described below with reference to the accompanying drawings. Obviously, the described embodiments are only some, not all, of the embodiments of this invention. All other embodiments obtained by those skilled in the art based on the embodiments of this invention without creative effort are within the scope of protection of this invention.
[0030] Example 1 Extraction and purification of burdock extract Extraction of burdock root extract: The raw burdock root was pulverized and passed through a 60-mesh sieve. Water was added at a solid-liquid ratio of 1:10 (g / mL) using the hot water reflux method, and the mixture was refluxed at 80℃ for 1.5 hours. This process was repeated twice. The extracts were combined and concentrated to 1 / 3 of the original volume by rotary evaporation at 55℃ to obtain the concentrated extract.
[0031] Purification of burdock extract: First, the concentrated solution was defatted by petroleum ether extraction. Then, the Sevag method (using a mixture of chloroform and n-butanol in a 4:1 volume ratio) was employed, with repeated centrifugation to remove proteins until no white denatured protein layer was visible at the interface. The supernatant after protein removal was concentrated, and four volumes of anhydrous ethanol were added. The mixture was allowed to settle at 4°C for 12 hours. The precipitate was collected by centrifugation and dissolved in ultrapure water to form a crude extract. The crude extract was dialyzed using a dialysis bag with a molecular weight cutoff of 3500 Da to remove small molecule salts and impurities. Finally, the dialysate was freeze-dried at -18°C for 48 hours to obtain the final burdock extract (with burdock polysaccharide as the main component, containing 90% by mass).
[0032] Example 2 In vitro fermentation experiment The burdock extract obtained in Example 1 was used to observe its effect on equatorial phenol content through a simulated in vitro fermentation experiment.
[0033] Fecal sample collection and pretreatment: The collected fecal samples were diluted with phosphate-buffered saline (PBS) solution (pH 7.0, 0.2 mol / L) at a ratio of 1:10 (g / ml) by shaking to prepare a bacterial suspension.
[0034] The fermentation medium was GAM medium, which consisted of 10.0g peptone, 3.0g soybean peptone, 5.0g yeast extract, 2.2g beef extract, 13.5g digested serum powder, 1.2g beef liver extract, 3.0g glucose, 2.5g potassium dihydrogen phosphate, 3.0g sodium chloride, 5.0g soluble starch, 0.3g L-cysteine, 5.0g L-arginine, 0.3g sodium thioglycolate, 1L distilled water, and a pH of 7.0.
[0035] Experimental conditions: The following experiments were set up: (1) Blank group (30 mL of GAM medium + 15 μL of bacterial suspension) (2) Positive control group (blank group + daidzein, final concentration of daidzein 200 μM) (3) Experimental group (positive control group + burdock extract, final concentration of burdock extract 5 mg / mL or 10 mg / mL), cultured under anaerobic conditions for 48 h, and then the equadol content was determined.
[0036] Method for detecting equol content: For each sample of fermentation broth, add ethyl acetate at a volume ratio of 1:6, and repeat the extraction three times. The combined ethyl acetate was evaporated under reduced pressure until dry, then dissolved in 1 mL of methanol and analyzed by high-performance liquid chromatography (HPLC). HPLC analysis was performed using an Agilent 1220 Infinity II liquid chromatography system (Agilent Technologies), with a ZORBAX SB-C18 column (Agilent Technologies). The mobile phase ratio was acetonitrile:methanol:water = 2:3:5, the flow rate was 0.8 mL / min, the detection wavelengths were 230 nm and 260 nm, the column temperature was 28℃, and the injection volume was 20 μL.
[0037] Experimental results: as shown in Table 1 and Figure 1 As shown, compared with the positive control group (only daidzein added), the equol production in each experimental group with added burdock extract was significantly increased, and the equol production increased with increasing concentration.
[0038] Table 1
[0039] The burdock extract of this invention has a very good promoting effect on the production of equol, and this has been verified by in vitro fermentation experiments. Compared with the positive control group, the burdock extract significantly increased the equol yield. Burdock, as a traditional plant used for both food and medicine, has no known toxic side effects from its polysaccharide components. Moreover, the burdock extract of this invention is of natural origin, not synthesized, which aligns with the development trend of health products. Furthermore, it is suitable for various products such as pharmaceuticals, health foods, and ordinary foods, and its addition to food is simple due to its small dosage.
[0040] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention, and not to limit them; although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art should understand that modifications can still be made to the technical solutions described in the foregoing embodiments, or equivalent substitutions can be made to some of the technical features; and these modifications or substitutions do not cause the essence of the corresponding technical solutions to deviate from the spirit and scope of the technical solutions of the embodiments of the present invention.
Claims
1. Use of an extract of Arctium lappa in the preparation of a product for preventing, delaying or improving a disease or disorder associated with equol deficiency.
2. The use of the extract of Arctium lappa according to claim 1 in the preparation of a product for preventing, delaying or improving a disease or disorder associated with equol deficiency, characterized in that, The mass content of polysaccharides in the extract of Arctium lappa is ≥ 90%.
3. Use of the extract of Arctium lappa according to claim 1 or 2 in the preparation of a product for preventing, delaying or improving a disease or disorder associated with equol deficiency, wherein the extract of Arctium lappa is prepared by the following steps: reflux extraction of Arctium lappa roots with hot water at a temperature of 80-90°C, defatting and deproteinizing the extract, precipitating with ethanol, dissolving the precipitate, and removing small molecular impurities by dialysis after dialysis, wherein the dialysis membrane has a molecular weight cut-off of ≥ 3500 Da.
4. Use of the extract of Arctium lappa according to claim 1 or 3 in the preparation of a product for preventing, delaying or improving a disease or disorder associated with equol deficiency, wherein the disease or disorder associated with equol deficiency comprises at least one of hormone-dependent cancer, menopausal syndrome, osteoporosis, hyperlipidemia, and arteriosclerosis.
5. The use of the extract of Arctium lappa according to claim 4 in the preparation of a product for preventing, delaying or improving a disease or disorder associated with a deficiency of equol, characterized in that, The hormone-dependent cancer comprises at least one of breast cancer, prostate cancer, and colorectal cancer.
6. The use of the extract of Arctium lappa according to claim 1 or 5 in the preparation of a product for preventing, delaying or improving a disease or disorder associated with a deficiency of equol, characterized in that, The product comprises at least one of a drug, a food, and a health product.
7. A composition characterized in that, The product comprises at least one of a drug, a food, and a health product.
8. The composition of claim 7, wherein, The composition further comprises daidzein.
9. The composition of claim 8, wherein, The mass ratio of the extract of Arctium lappa to daidzein is (100-200):
1.
10. The composition according to any one of claims 7 to 9, wherein The dosage form of the composition comprises at least one of a tablet, a capsule, a granule, a pill, a powder, and an oral solution.