Agent for liver function improvement and / or cholesterol reduction

A cynaropicrin-containing material addresses the lack of research on its effects by providing a liver function-improving and cholesterol-lowering agent, demonstrating significant reductions in liver enzymes and cholesterol levels through appropriate daily intake.

JP2025056524APending Publication Date: 2025-04-08ICHIMARU PHARCOS CO LTD
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Patent Information

Application Number
JP2023166052
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2023-09-27
Publication Date
2025-04-08

AI Technical Summary

Technical Problem

The effects of cynaropicrin on improving liver function and lowering cholesterol in humans have not been fully studied.

Method used

A material containing cynaropicrin is developed as an agent for improving liver function and/or lowering cholesterol, with daily intake recommendations ranging from 0.00010 mg/kg/day to 50 mg/kg/day, and can be formulated into various oral compositions such as foods, drinks, and pharmaceutical products.

Benefits of technology

The cynaropicrin agent effectively improves liver function and lowers cholesterol levels by reducing AST, ALT, LDL, and T-cho levels in human subjects.

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Abstract

To provide a material (agent) and so on for liver function improvement and / or cholesterol reduction for use in human beings, etc.SOLUTION: There are provided: (1) an agent for liver function improvement containing cynaropicrin; (2) an agent for cholesterol reduction containing cynaropicrin; (3) an oral composition containing the agent according to (1) or (2); and so on.SELECTED DRAWING: None
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Description

[Technical field]

[0001] The present invention relates to a material containing cynaropicrin for improving liver function and / or lowering cholesterol. [Background technology]

[0002] Various effects of cyanaropicrin have been discovered (Patent Document 1). However, the effects of cyanaropicrin have not yet been fully studied. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] International Publication No. WO2021246200 Summary of the Invention [Problem to be solved by the invention]

[0004] The present invention provides a material (agent) for improving liver function and / or lowering cholesterol, for use in humans, etc. [Means for solving the problem]

[0005] The present invention has been made to solve the above problems, and was invented after discovering a new effect of cynaropicrin.

[0006] The present invention includes the following embodiments. (1) An agent for improving liver function that contains cynaropicrin. (2) A cholesterol-lowering agent containing cynaropicrin. (3) An oral composition comprising the agent according to (1) or (2). Effect of the Invention

[0007] The agent of the present invention etc. can be used to improve liver function and / or lower cholesterol in humans etc. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0008] (Cynaropicrin) Cynaropicrin (PubChem CID: 119093) is a type of sesquiterpene and has the following molecular formula: 19 H 22 He is O6.

[0009] [ka]

[0010] The daily intake of cynaropicrin used in the present invention (when taken in an oral composition) can be adjusted as appropriate depending on the intake form, purpose of use, age, body weight, etc., but in order to achieve the desired effects (improvement of liver function, lowering of blood cholesterol, etc.), the daily intake of cynaropicrin for an adult human is preferably 0.00010 mg / kg / day or more, more preferably 0.0010 mg / kg / day or more, and even more preferably 0.010 mg / kg / day or more, and from the viewpoint of safety in humans when taking the intake, it is preferably 1000 mg / kg / day or less, more preferably 100 mg / kg / day or less, and even more preferably 50 mg / kg / day or less.

[0011] (Improved liver function) The improvement of liver function refers to the improvement of the circulatory function, excretory function, metabolic function, protective and detoxifying function, or hematological function of the liver. Moreover, the decline in liver function refers to the decline in the circulatory function, excretory function, metabolic function, protective and detoxifying function, or hematological function of the liver. Although not limited thereto, liver function can be measured by enzymes such as AST (GOT, glutamic oxaloacetic transaminase) level, ALT (GPT, glutamic pyruvic transaminase) level, and γ-GTP (γ-glutamyl transpeptidase) in blood, or by microscopic observation of liver cell slices (paragraph 0049 of JP 2018-070570 A). In the test described in the following examples, the presence or absence of an effect of improving liver function was confirmed by measuring the GOT and GPT levels in blood and confirming the presence or absence of a decline in the GOT and GPT levels.

[0012] (Cholesterol reduction) Cholesterol is essential for maintaining the morphology and function of cells as a component of biological cell membranes. Cholesterol is also an important component as a precursor of steroid hormones and bile acids. Measuring the total cholesterol level in blood can suggest diseases that cause lipid metabolism disorders. Cholesterol is bound to lipoproteins and solubilized in the blood, and is divided into good cholesterol (HDL) and bad cholesterol (LDL, VLDL) depending on the type of lipoprotein to which it is bound. HDL has the function of removing excess cholesterol attached to the blood vessel walls and transporting it to the liver for catabolism. Cholesterol cannot be broken down in peripheral tissues. HDL is known to be a risk prevention factor for arteriosclerosis. Therefore, HDL is also called good cholesterol. On the other hand, LDL and VLDL are responsible for transporting cholesterol from the liver to peripheral tissues. However, if LDL or VLDL is denatured for some reason, it deposits cholesterol in the blood vessel walls and destroys tissues. Therefore, it is also called bad cholesterol. The ratio of HDL, LDL, and VLDL to total cholesterol (T-cho) is used to diagnose lipid metabolism disorders and estimate the severity of the disease (Patent Publication No. 2005087247, paragraph 0031). In the tests described in the following examples, the LDL and T-cho levels in blood were measured to confirm whether or not the LDL and T-cho levels had decreased, thereby confirming whether or not the cholesterol-lowering effect had been achieved.

[0013] (Oral Composition) The oral composition according to the present invention is, for example, a food or drink (including functional foods, foods for specified health uses, supplements, etc.), a pharmaceutical product, and the like.

[0014] For example, when the oral composition is a food or drink, the form of the food or drink may be various foods and drinks such as breads, cakes, noodles, confectioneries, jellies, frozen foods, ice creams, dairy products, beverages, etc., as well as forms similar to those of the oral administration preparations described above (tablets, capsules, syrups, etc.) Foods in various forms can be prepared by using the active ingredient of the present invention alone or in appropriate combination with other food materials, solvents, softeners, oils, emulsifiers, preservatives, flavorings, stabilizers, colorants, antioxidants, moisturizers, thickeners, etc.

[0015] For example, when the oral composition is a pharmaceutical product, the pharmaceutical product may be in the form of, for example, solid or liquid, although the pharmaceutical product is generally easy to be assembled into a convenient daily dosage regimen that can be adjusted according to the degree of pain. The solid form may include, for example, powder, tablet, pill, capsule, cachet, lozenge, suppository and dispersible granule. For example, in powder, the carrier is generally a finely divided solid that is mixed with the finely divided active ingredient. For example, in tablet, the active ingredient is generally mixed with the carrier having the necessary binding capacity in an appropriate ratio and molded into the desired shape and size. Suitable carriers may include, but are not limited to, for example, magnesium carbonate, magnesium stearate, talc, sugar, lactose, pectin, dextrin, starch, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose, low melting wax, cocoa butter and the like. The pharmaceutical may also contain ingredients such as excipients, stabilizers, preservatives, binders, disintegrants, hydrocarbons, fatty acids, alcohols, esters, pH adjusters, and preservatives as necessary, within the range that does not impair the desired effects.

[0016] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples. In the following examples, the unit % of the numerical value showing the content of the components contained in the agent of the present invention means % by mass. EXAMPLES

[0017] Examples of the present invention will be described below.

[0018] [Experiment 1: Human monitor test] A human monitor test was conducted on 21 healthy men and women (1 man and 20 women, a total of 21 people). The 21 people were divided into two groups: a placebo intake group (11 women, average age 45.7 years) and a cynaropicrin intake group (1 man and 9 women, average age 43.6 years).

[0019] (How to take) It was taken as follows: Placebo group: Participants took one capsule (containing 260 mg of dextrin) once a day between breakfast and lunch for 12 weeks. Cynaropicrin intake group: Participants orally took one capsule (containing 150 mg of Cynaropicrin F (manufactured by Ichimaru Pharcos Co., Ltd.) and 110 mg of dextrin, packed into a No. 2 capsule, once a day between breakfast and lunch, for 12 weeks.

[0020] The No. 2 capsule used was a gelatin capsule for food (e.g., manufactured by Qualicaps Co., Ltd.) The dextrin used was maltodextrin (Pinedex #1, Matsutani Chemical Industry Co., Ltd.).

[0021] The cynaropicrin F was prepared by adding water to the leaves of Cynara scolymus L. (Compositae) to produce an extract, adding an excipient to the extract, and drying the extract to produce a powder. The powder (the cynaropicrin F) contained 1.1% by mass of the above-mentioned cynaropicrin.

[0022] During the intake period (12 weeks), both the cynaropicrin intake group and the placebo intake group performed exercise once a day, burning 60 kcal, using a stepper exercise machine (Health Stepper Nice Day, Shop Japan).

[0023] During the intake period (12 weeks), subjects were asked to try to continue their lifestyle in the same way as before the start of the study, except for taking the capsules orally and exercising using a stepper exercise machine.

[0024] (Blood sampling and blood tests) Blood samples were taken at a designated medical institution before the start of intake (day 0) and after intake (12 weeks later). The AST (GOT), ALT (GPT), LDL and T-cho values ​​in the blood obtained from the blood samples were measured. The results of the measurements are described below. All results below are presented as the average values ​​for each group. The results of the Student's t-test are also described.

[0025] (AST (GOT) measurement results) In the placebo group, the score was 17.91 before ingestion and 17.45 after ingestion, whereas in the cynaropicrin group, the score was 16.90 before ingestion and 14.90 after ingestion (significantly decreased from the 16.90, p<0.05).

[0026] (ALT (GPT) level measurement results) In the placebo group, the mean score was 15.18 before ingestion and 13.91 after ingestion. On the other hand, in the cynaropicrin group, the mean score was 13.50 before ingestion and 10.90 after ingestion (a significant decrease from the mean score of 13.50, p<0.05).

[0027] (LDL level measurement results) In the placebo group, the mean score was 212.45 before ingestion and 204.91 after ingestion, whereas in the cynaropicrin group, the mean score was 223.40 before ingestion and 204.00 after ingestion (a significant decrease from the mean score of 223.40, p<0.01).

[0028] (T-cho value measurement results) In the placebo group, the mean score was 115.27 before ingestion and 115.55 after ingestion. On the other hand, in the cynaropicrin group, the mean score was 139.90 before ingestion and 126.90 after ingestion (a significant decrease from the mean score of 139.90, p<0.05).

[0029] At least in the cynaropicrin intake group, a significant effect of intake (reduction in AST (GOT) values, ALT (GPT) values, LDL values, and T-cho values) was confirmed.

[0030] The above describes the embodiment of the present invention (including examples) with reference to the drawings. However, the specific configuration of the present invention is not limited to this, and even if there are design changes, etc., within the scope that does not deviate from the gist of the present invention, they are included in the present invention. [Industrial Applicability]

[0031] INDUSTRIAL APPLICABILITY The present invention can provide a material (agent) for use in humans etc., for improving liver function and / or lowering cholesterol.

Claims

1. An agent for improving liver function that contains cynaropicrin.

2. An agent for lowering cholesterol, containing cynaropicrin.

3. An oral composition comprising the agent according to claim 1 or 2.

Citation Information

Patent Citations

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    WO2021246200A1