Composition for preventing or alleviating benign prostatic hyperplasia, comprising lycopus lucidus extract

Abstract

The present invention relates to a composition for preventing or alleviating benign prostatic hyperplasia, the composition comprising a Lycopus lucidus extract. The Lycopus lucidus extract was found to have the effect of significantly reducing an increase in prostate weight and prostate index in a benign prostatic hyperplasia animal model, and is thus provided as a composition for preventing, alleviating or treating benign prostatic hyperplasia.

Description

Composition for preventing or improving benign prostatic hyperplasia containing extract of Takran

[0001] The present invention relates to a composition for preventing or improving benign prostatic hyperplasia containing an extract of Lycopus lucidus.

[0002] Benign prostatic hyperplasia (BPH) is a condition in which the prostate gland enlarges and puts pressure on the urethra, causing urinary problems such as difficulty urinating, frequent urination, nocturia, and urgency. The prostate is a male reproductive organ located just below the bladder, surrounding the urethra and producing some of the semen. The prostate begins to gradually enlarge after puberty, and BPH usually begins to appear in men in their 40s, affecting 60-70% of men in their 60s, and almost all men in their 70s. The cause of BPH is not yet clearly known, but it is known to be closely related to aging and the male hormone testosterone, and genetic factors, obesity, smoking, and drinking are also known to have an effect.

[0003] The main symptoms of BPH include frequent urination (the need to urinate frequently); a feeling of residual urine (a feeling of residual urine remaining in the bladder after urinating); a weak and thin urine stream (urinary incontinence); interrupted urine flow (urinary retention), prolonged urination (neglecting to urinate); and nocturia (waking up at night to urinate). Diagnosis of BPH is primarily based on a medical history, physical examination, urine tests, blood tests, prostate-specific antigen (PSA) testing, and prostate ultrasound.

[0004] Treatment for BPH includes wait-and-see, medication, minimally invasive treatment, and surgery. For mild symptoms, wait-and-see or medication are recommended. For severe symptoms or complications, surgery may be considered. For prevention, regular exercise, adequate sleep, and a balanced diet are important, as is avoiding smoking and drinking. Current medications for BPH include alpha-blockers and 5-alpha-reductase inhibitors. However, these medications often have sexual side effects. Therefore, there is a pressing need to develop new medications derived from natural sources with fewer side effects to treat BPH.

[0005] [Prior Art Literature]

[0006] [Patent Document]

[0007] Korean Patent Publication No. 10-1706857 (Published on February 16, 2017)

[0008] The purpose of the present invention is to provide a pharmaceutical composition for preventing or treating benign prostatic hyperplasia, which contains an extract of Lycopus lucidus as an active ingredient.

[0009] The present invention provides a pharmaceutical composition for preventing or treating benign prostatic hyperplasia, comprising an extract of Lycopus lucidus as an active ingredient.

[0010] In addition, the present invention provides a health functional food composition for preventing or improving benign prostatic hyperplasia, which contains an extract of Lycopus lucidus as an active ingredient.

[0011] According to the present invention, since it has been confirmed that the extract of Lycopus lucidus has the effect of significantly reducing the increase in prostate weight and prostate index in an animal model of benign prostatic hyperplasia, it can be provided as a composition for preventing, improving or treating benign prostatic hyperplasia.

[0012] Figure 1 shows the results of analyzing the effect of the extract of Takran on changes in prostate weight in a benign prostatic hyperplasia model.

[0013] Figure 2 shows the results of analyzing the effect of the extract of Taeran on changes in prostate index in a model of benign prostatic hyperplasia.

[0014] The terms used in this specification have been selected from widely used, current terms, taking into account the functions of the present invention. However, these terms may vary depending on the intentions of those skilled in the art, precedents, the emergence of new technologies, etc. Furthermore, in certain cases, terms may be arbitrarily selected by the applicant, and in such cases, their meanings will be described in detail in the relevant description of the invention. Therefore, the terms used in this invention should not be defined simply as names, but rather based on their inherent meanings and the overall content of the present invention.

[0015] Unless otherwise defined, all terms used herein, including technical or scientific terms, have the same meaning as commonly understood by one of ordinary skill in the art to which this invention pertains. Terms defined in commonly used dictionaries should be interpreted as having a meaning consistent with their meaning in the context of the relevant technology, and shall not be interpreted in an idealized or overly formal sense unless explicitly defined herein.

[0016] Hereinafter, the present invention will be described in more detail.

[0017] The present invention provides a pharmaceutical composition for preventing or treating benign prostatic hyperplasia, comprising an extract of Lycopus lucidus as an active ingredient.

[0018] In the present invention, the extract includes all extracts prepared from part or all of a plant using conventional plant extraction methods known in the art. Preferably, the extract is a crude extract, a polar solvent-soluble extract, or a non-polar solvent-soluble extract.

[0019] In the present invention, the extract can be prepared by an extraction method such as hot water extraction, cold immersion extraction, reflux cooling extraction or ultrasonic extraction at 50°C to 100°C for 1 to 6 hours with a polar solvent selected from water, ethanol, lower alcohols having 1 to 4 carbon atoms or a mixed solvent thereof, preferably a mixed solvent of water or ethanol, more preferably 50% (v / v) to 90% (v / v) ethanol, in a volume of about 1 to 100 times, preferably about 2 to 20 times, the weight of the sample after grinding the material, and more preferably reflux cooling extraction at 80°C for 3 hours with 70% (v / v) ethanol.

[0020] The Lycopus lucidus extract of the present invention exhibits a weight reduction effect on the prostate in a benign prostatic hyperplasia model.

[0021] The pharmaceutical composition of the present invention can be manufactured in a unit dose form or can be manufactured by placing it in a multi-dose container by formulating it using a pharmaceutically acceptable carrier according to a method that can be easily performed by a person having ordinary skill in the art to which the present invention pertains.

[0022] The pharmaceutically acceptable carriers mentioned above are those commonly used in formulations, and include, but are not limited to, lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia gum, calcium phosphate, alginate, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methyl cellulose, methyl hydroxybenzoate, propyl hydroxybenzoate, talc, magnesium stearate, and mineral oil. In addition to the above components, the pharmaceutical composition of the present invention may further include a lubricant, a wetting agent, a sweetening agent, a flavoring agent, an emulsifier, a suspending agent, a preservative, and the like.

[0023] In the present invention, the content of the additive included in the pharmaceutical composition is not particularly limited and can be appropriately adjusted within the content range used in conventional formulations.

[0024] The above pharmaceutical composition may be formulated in the form of one or more external preparations selected from the group consisting of injectable formulations such as aqueous solutions, suspensions, emulsions, pills, capsules, granules, tablets, creams, gels, patches, sprays, ointments, ointments, lotions, liniments, pastes, and cataplasmas.

[0025] The pharmaceutical composition of the present invention may further comprise pharmaceutically acceptable carriers and diluents for formulation. The pharmaceutically acceptable carriers and diluents include, but are not limited to, excipients such as starches, sugars, and mannitol; fillers and extenders such as calcium phosphate; cellulose derivatives such as carboxymethylcellulose and hydroxypropylcellulose; binders such as gelatin, alginates, and polyvinyl pyrrolidone; lubricants such as talc, calcium stearate, hydrogenated castor oil, and polyethylene glycol; disintegrants such as povidone and crospovidone; and surfactants such as polysorbates, cetyl alcohol, and glycerol. The pharmaceutically acceptable carriers and diluents may be biologically and physiologically compatible with the subject. Examples of diluents include, but are not limited to, saline, aqueous buffers, solvents, and / or dispersion media.

[0026] The pharmaceutical composition of the present invention may be administered orally or parenterally (e.g., intravenously, subcutaneously, intraperitoneally, or topically) depending on the intended method. In the case of oral administration, it may be formulated as tablets, troches, lozenges, aqueous suspensions, oily suspensions, prepared powders, granules, emulsions, hard capsules, soft capsules, syrups, or elixirs. In the case of parenteral administration, it may be formulated as injections, suppositories, powders for respiratory inhalation, aerosols for sprays, ointments, powders for application, oils, creams, etc.

[0027] The dosage of the pharmaceutical composition of the present invention may vary depending on the patient's condition and weight, age, sex, health status, dietary constitution, nature of the formulation, severity of the disease, administration time of the composition, administration method, administration period or interval, excretion rate, and drug form, and may be appropriately selected by a person skilled in the art. For example, the dosage may range from about 0.1 to 10,000 mg / kg, but is not limited thereto, and may be administered once or several times a day in divided doses.

[0028] The pharmaceutical composition may be administered orally or parenterally (e.g., intravenously, subcutaneously, intraperitoneally, or topically) depending on the intended method. The pharmaceutically effective amount and effective dosage of the pharmaceutical composition of the present invention may vary depending on the formulation method, administration method, administration time, and / or administration route of the pharmaceutical composition, and a person skilled in the art can easily determine and prescribe an effective dosage for the intended treatment. The pharmaceutical composition of the present invention may be administered once a day or divided into several doses.

[0029] In addition, the present invention provides a health functional food composition for preventing or improving benign prostatic hyperplasia, which contains an extract of Lycopus lucidus as an active ingredient.

[0030] The present invention can be generally used as a commonly used food.

[0031] The food composition of the present invention can be used as a health functional food. The term "health functional food" refers to a food manufactured and processed using raw materials or ingredients with functional properties beneficial to the human body, as defined by the Health Functional Food Act. "Functionality" refers to ingestion for the purpose of obtaining beneficial effects for health purposes, such as regulating nutrients for the structure and functions of the human body or physiological effects.

[0032] The food composition of the present invention may include conventional food additives, and its suitability as the "food additive" is determined by the specifications and standards for the relevant item in accordance with the general provisions and general test methods of the Food Additive Code approved by the Ministry of Food and Drug Safety, unless otherwise specified.

[0033] Items listed in the above "Food Additives Code" include, for example, chemical compounds such as ketones, glycine, potassium citrate, nicotinic acid, and cinnamic acid; natural additives such as persimmon pigment, licorice extract, crystalline cellulose, high-molecular-weight pigment, and guar gum; and mixed preparations such as sodium L-glutamate preparations, alkaline agents for noodles, preservative preparations, and tar color preparations.

[0034] The food composition of the present invention can be manufactured and processed in the form of tablets, capsules, powders, granules, liquids, pills, etc.

[0035] For example, among health functional foods in capsule form, hard capsules can be manufactured by mixing and filling a composition according to the present invention with additives such as excipients into a conventional hard capsule, and soft capsules can be manufactured by mixing the composition according to the present invention with additives such as excipients and filling it into a capsule base such as gelatin. The soft capsules may contain a plasticizer such as glycerin or sorbitol, a coloring agent, a preservative, etc., as needed.

[0036] The definitions of terms for the above excipients, binders, disintegrants, lubricants, flavoring agents, etc. are described in literature known in the art and include those with identical or similar functions. There are no specific restrictions on the type of food, and all health functional foods in the conventional sense are included.

[0037] As used herein, the term "prevention" refers to any action that suppresses or delays the onset of a disease by administering a composition according to the present invention. The term "treatment" refers to any action that improves or beneficially alters the symptoms of a disease by administering a composition according to the present invention. As used herein, "improvement" refers to any action that improves the worsening condition of a disease by administering or ingesting a composition according to the present invention to a subject.

[0038] Hereinafter, to aid understanding of the present invention, experimental examples and examples will be described in detail. However, the following experimental examples and examples are merely illustrative of the present invention and are not intended to limit the scope of the present invention. The experimental examples and examples of the present invention are provided to more fully explain the present invention to those of average skill in the art.

[0039] [Experimental Example] Experimental Materials and Methods

[0040] The following experimental examples are intended to provide experimental examples commonly applied to each embodiment according to the present invention.

[0041] 1. Preparation of Lycopus lucidus extract

[0042] Dried Lycopus lucidus was purchased from Dongwoo Dang Pharmaceutical (Gyeongbuk, Korea). Using a heating mantle (MS-DM606, Misung Scientific Equipment Co., Ltd., Gyeonggi-do, Korea), Lycopus lucidus was extracted with 10-fold dilution of 70% ethanol at 80°C for 3 h under reflux cooling. The Lycopus lucidus extract was filtered through filter paper (Whatman™, Cytiva, USA), and the filtrate was concentrated in a rotary evaporator (N-1200A, EYELA, Tokyo, Japan) at 45°C. The concentrated Lycopus lucidus extract was freeze-dried (FDU-1200, EYELA, Tokyo, Japan).

[0043] 2. Laboratory animals

[0044] Ten-week-old male Sprague-Dawley rats were supplied by Coretech Co., Ltd. (Gyeonggi-do, Korea). The rats were acclimated to the experimental environment for one week. During the rearing period, the breeding space was maintained at a temperature of 23±1°C, a humidity of 40%–60%, and a 12-h light / dark cycle. Food and water were available ad libitum.

[0045] 3. Induction of benign prostatic hyperplasia and administration of extracts

[0046] Rats acclimated to the breeding space were randomly assigned to five groups: Sham group, control group, positive control group (finasteride administration group, 1 mg / kg / day), low-dose group (100 mg / kg / day) of taekran extract, and high-dose group (200 mg / kg / day) of taekran extract. Castration was performed under isoflurane inhalation anesthesia. After an incision was made in the midline of the abdomen, the testes, epididymis, and epididymal fat on both sides were resected. After resection, the abdominal skin was sutured and the rats were allowed to recover for 1 week. In the Sham group, the abdominal skin was incised and then sutured without any tissue resection. Prostatic hypertrophy (BPH) was induced in rats by subcutaneous injection of testosterone propionate (TCI, Tokyo, Japan) dissolved in olive oil at a concentration of 3 mg / kg once daily for 28 days. The sham group received subcutaneous injections of olive oil once daily for 28 days. Along with the induction of BPH, the rats were administered orally once daily for 28 days with T. melanogaster extract and finasteride (Organon, New Jersey, USA) dissolved in purified water. The sham and control groups received orally purified water once daily for 28 days. The dose was 1 mg / kg subcutaneously and 10 mL / kg orally.

[0047] 4. Prostatectomy

[0048] Rats were fasted overnight before sacrifice, and fasting body weights were measured on the day of sacrifice. The prostates were removed under isoflurane inhalation anesthesia, and their weights (mg) were measured. The prostate index was calculated as the prostate weight (mg) per 100 g of fasting body weight. The inhibition rate (%) of prostate weight and prostate index was calculated as (control value - treatment value) / (control value - sham value) χ 100.

[0049] [Example] Effect of Takran extract on prostate weight and prostate index

[0050] To evaluate the preventive, ameliorating, and therapeutic effects of the extract of Taxus lanceolata, a model of benign prostatic hyperplasia was created in rats, and the extract was administered for 28 days, after which the weight and prostate index of the prostate were analyzed. As shown in Figure 1, the control group (Con) with induced prostatic hyperplasia showed an increase in prostate weight compared to the sham group. The positive control group (Fina), which received finasteride, a drug for treating benign prostatic hyperplasia, showed a decrease in prostate weight compared to the control group (Con). In addition, the high-dose group (200 mg / kg / day) of Taxus lanceolata extract also showed a decrease in prostate weight, similar to the positive control group. In addition, as shown in Figure 2, the prostate index of the control group (Con) with induced prostatic hyperplasia increased compared to the sham group. The positive control group (Fina), which received finasteride, a drug for treating benign prostatic hyperplasia, showed a decrease in prostate index compared to the control group (Con). Additionally, the high-dose Lycopus lucidus extract group (200 mg / kg / day) also showed a decrease in prostate index, similar to the positive control group. These results demonstrate that Lycopus lucidus extract has a preventive, ameliorating, or therapeutic effect on benign prostatic hyperplasia.

[0051] While specific aspects of the present invention have been described in detail above, it should be apparent to those skilled in the art that these specific descriptions merely represent preferred embodiments and are not intended to limit the scope of the present invention. In other words, the substantial scope of the present invention is defined by the appended claims and their equivalents.

[0052] Numerical ranges are inclusive of the values ​​defined in the ranges above. Any maximum numerical limitation given throughout this specification includes any lower numerical limitation, as if that lower numerical limitation were explicitly stated. Any minimum numerical limitation given throughout this specification includes any higher numerical limitation, as if that higher numerical limitation were explicitly stated. Any numerical limitation given throughout this specification will include any better numerical range within the broader numerical range, as if that narrower numerical limitation were explicitly stated.

Claims

1. A pharmaceutical composition for preventing or treating benign prostatic hyperplasia containing Lycopus lucidus extract as an active ingredient.

2. A pharmaceutical composition according to claim 1, characterized in that the extract is a water or ethanol extract.

3. A pharmaceutical composition according to claim 1, characterized in that the extract of the ginseng has a weight-reducing effect on the prostate.

4. A health functional food composition for preventing or improving benign prostatic hyperplasia, containing Lycopus lucidus extract as an active ingredient.

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