KR20220011254A - Composition containing sardinops extract for improving sexual function - Google Patents

Abstract

The present invention relates to a composition for improving the male sexual function comprising a Sardinops sagax extract as an active component. More specifically, the present invention relates to a composition for improving the male sexual function, which improves the male sexual function through an effect of enhancing penis erection and inhibiting prostate enlargement by including the Sardinops sagax extract as the active component. According to the composition, the composition can be taken for a long time and has no side effects, and thus can be applied as an improving agent and a therapeutic agent that can be safely used mentally and physically.

Description

Composition for improving male sexual function comprising sardine extract as an active ingredient {COMPOSITION CONTAINING SARDINOPS EXTRACT FOR IMPROVING SEXUAL FUNCTION}

The present invention relates to a composition for improving male sexual function comprising a sardine extract as an active ingredient, and more specifically, it contains a natural extract of sardine extract as an active ingredient, so that it can be taken for a long time without side effects, and it promotes erection of the penis and enlarges the prostate. It relates to a composition for improving male sexual function, comprising, as an active ingredient, a sardine extract that improves male sexual function through an inhibitory effect.

The modern living environment disrupts the circadian rhythm due to overwork, drinking, stress, environmental pollution, etc., and as the frequency of exposure to lifestyle-related diseases such as high blood pressure, diabetes, and obesity increases, energy declines from the 20s and 30s, when they should be at their peak , aging and sexual dysfunction are often present, and it is more serious in those over 40 years of age.

In particular, in a study of middle-aged men in their 40s to 70s, it was reported that more than 50% of the study subjects suffered from erectile dysfunction during sexual dysfunction. The incidence of erectile dysfunction increases rapidly after the age of 50, and it has been reported that the prevalence of erectile dysfunction in 70-year-old men is three times higher than in 40-year-old men. Erectile dysfunction not only affects men's sexual life, but also causes loss of self-confidence and depression, which adversely affects social life. Accordingly, prevention and treatment of erectile dysfunction are important for a happy life and improvement of quality of life.

Erectile dysfunction is a phenomenon in which blood does not flow normally in the corpus cavernosum tissue, and it refers to a case in which the penis is not sufficiently erected or does not persist even if it occurs more than 25% of the total sexual life. Causes are broadly classified into psychogenic and organic, and organic are classified into neurogenic, endocrine, vascular, and systemic diseases. Hormonal disturbances due to environmental influences, osteomalacia caused by heavy metal use and air pollution, renal function deterioration, nerve disorders, and testis damage are known as one of the causes of male infertility.

For the penis to have an erection, complete relaxation of the cavernous arteries and penile smooth muscle and accumulation of blood in the sinysoidal space in the cavernous body are required first. In this process, neurotransmitters and non-neurotransmitters act. In particular, nonadrenergic, noncholinergic nerve and nitric oxide (NO) release from the endothelium activates guanylate cyclase in the corpus cavernosum and increases intracellular cGMP (cyclic GMP) levels. The increase in intracellular cGMP decreases the intracellular calcium level, which induces scaphoid smooth muscle relaxation, which in turn induces penile erection through cavernous volume expansion. Since cGMP is decomposed by PDE (phosphodiesterase), its activity must be inhibited to increase the concentration of cGMP and improve erectile function.

On the other hand, when blood vessels are relaxed by inhibiting the activity of angiotensin converting enzyme (ACE), which is involved in the production of angiotensin II, a powerful vasoconstrictor in the human body, blood flow in the penis increases, which leads to penis erection. As described above, the increase in blood flow in the cavernous body of the penis occurs 5 to 6 times more actively than usual. Muscle contraction of the vulva is required.

In order to treat erectile dysfunction, a medical treatment method of applying a drug acting on the above mechanism or administration of male hormones, surgical treatment such as vascular surgery or penile prosthesis insertion, and injection of a corpus cavernosum vasodilator have been proposed. The most preferred treatment for erectile dysfunction patients is drug therapy. Adrenergic α-receptor blockers related to penile smooth muscle relaxation, cholinergic drugs, nitric oxide (NO), peptides, prostaglandins, histamine, calcium channel blockers, potassium channel openers, Non-specific vasodilators have been developed as drugs.

Men's sexual function consists of sexual desire, penis erection, ejaculation, and a sense of ecstasy, which are determined by complex physiological reactions of the nervous system, endocrine system, and vascular system, and any abnormality may cause sexual dysfunction. Although these sexual dysfunctions were mostly considered psychogenic causes 10 years ago, with the development of modern medicine, more than 50% of sexual dysfunction patients are caused by various causes such as vascular, nervous and endocrine system diseases, diabetes, high blood pressure, and drug use. it turns out to be Recently, sildenafil, a phosphodiesterase V inhibitor, has attracted a lot of attention in the treatment of sexual dysfunction. However, this treatment uses chemicals to induce temporary erection, is expensive, and increases headache and blood pressure. , heart attack and many other side effects. In particular, there are a number of cases of death due to aggravation of heart disease. Therefore, it is necessary to develop a safe and effective therapeutic agent for sexual dysfunction that enhances the human body's instinctive erectile function, and the recent trend is to increase the production of nitric oxide and cGMP, which are signal transmitters that show strong relaxation in the corpus cavernosum smooth muscle. Interest is being drawn to developing a treatment for improving sexual function that enhances the erection of the cavernous body.

In addition, existing drugs for erectile dysfunction do not improve the physical disorders related to blood circulation and endocrine function, which are the causes of erectile dysfunction, but are developed with a focus on temporary erection induction and gradually develop resistance or various side effects as they are used. may appear Accordingly, research is being actively conducted to search for an erectile dysfunction treatment without side effects from natural products and herbal medicines.

KR 10-1030608 B1

It is an object of the present invention to include a sardine extract as an active ingredient, and relates to a composition for improving male sexual function, which improves male sexual function through the effect of enhancing penis erection and inhibiting prostate enlargement.

Another object of the present invention is to provide a composition for improving male sexual function that can be taken for a long time using a natural extract and has no side effects, and can be applied as an improving agent and therapeutic agent that can be safely used mentally and physically.

In order to achieve the above object, the composition for improving male sexual function according to an embodiment of the present invention includes a sardine (Sardinops sagax) extract as an active ingredient.

The composition is to improve male sexual function through the effect of enhancing penis erection and inhibiting prostate enlargement.

The composition is to prevent male sexual diseases selected from the group consisting of erectile dysfunction, premature ejaculation, genitalia and prostatic hyperplasia.

The composition will further include a natural extract selected from the group consisting of gold (Scutellaria baicalensis) extract, thistle (Cirsium japonicum var) extract and dandelion (Taraxacum platycarpum) extract.

The natural extract may be extracted using an extraction solvent selected from the group consisting of water, C ₁ to C _{6 lower alcohols, and mixtures thereof.}

The pharmaceutical composition according to another embodiment of the present invention may include the composition for improving male sexual function.

The functional food composition according to another embodiment of the present invention may include the composition for improving male sexual function.

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

As used herein, the term 'extract' has the meaning commonly used as a crude extract in the art as described above, but in a broad sense also includes a fraction obtained by additionally fractionating the extract.

That is, the natural extract includes not only those obtained using an extraction solvent, but also those obtained by additionally applying a purification process here. For example, a fraction obtained by passing the extract through an ultrafiltration membrane having a constant molecular weight cut-off value, separation by various chromatography (prepared for separation according to size, charge, hydrophobicity or affinity), etc. The fraction obtained through the purification method is also included in the natural extract of the present invention.

The extract used in the present invention may be prepared in a powder state by an additional process such as distillation under reduced pressure and freeze-drying or spray-drying.

As used herein, the term 'active ingredient' refers to a component that can exhibit a desired activity alone or can exhibit activity together with a carrier that has no activity by itself.

As used herein, the term 'improving male sexual function' refers to induction of an erection of a male penis and/or an increase in the number of sexes. As used herein, "improving male sexual function" may be used in the meaning of "improving menopausal health" as long as it means inducing an erection of a male penis and/or inducing an increase in the number of sex.

The composition for improving male sexual function according to an embodiment of the present invention includes a sardine extract as an active ingredient.

The sardine (Sardinops sagax) is a small fish corresponding to the herring, and it is derived from the English language, which first appeared in the early 15th century, and its name is believed to have been derived from Sardinia (Sardinia), a Mediterranean region where sardines are abundant. Sardines are a representative blue-green fish, and are used for roasting or stewing, and are distributed in Korea, Japan, Taiwan, and coastal areas of China. Sardines are rich in omega 3 fatty acids, EPA and DHA, to remove saturated fatty acids. Among the blue-green fish, sardines have the highest EPA content, which not only helps platelet activity but also prevents blood clots and helps blood circulation. In addition, it is rich in calcium and vitamin D, which helps calcium absorption, has the effect of preventing osteoporosis.

The present invention contains the sardine extract to improve male sexual function, and to improve erectile dysfunction, premature ejaculation, genitalia, prostatic hypertrophy and sexual desire through the enhancement of penis erection.

The composition is to improve male sexual function through the effect of enhancing penis erection and inhibiting prostate enlargement.

In order to improve male sexual function, it is necessary to promote penile erection by making the smooth muscle of the cavernous body exhibit a strong relaxation action. Its mechanism of action is focused on increasing the production of nitric oxide (NO). In this regard, it was found in animal experiments that nitric oxide plays an important role in penile erection. Nitric oxide secreted by vascular endothelial cells is also increased in the parasympathetic periphery of the penis under sexual stimulation. Nitric oxide activates guanylate cyclase to convert guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP). The cGMP generated here provides a signal to cause the relaxation of the smooth muscle of the cavernous body and the penile artery to induce an erection of the penis. Therefore, it can be said that the production of nitric oxide is important for penile erection to last.

More specifically, the process of penile smooth muscle relaxation is mediated in part by nonadrenergic, noncholinergic (NANC) neurotransmission, and the decrease in the tension of the cavernous smooth muscle is because nitric oxide induces cavernous relaxation.

In order for the penis to be erected, complete relaxation of the cavernous arteries and penile smooth muscle and blood accumulation in the sinysoidal space in the cavernous body are required first. In this process, neurotransmitters and non-neurotransmitters act. In particular, nonadrenergic, noncholinergic nerve and nitric oxide (NO) release from the endothelium activates guanylate cyclase in the corpus cavernosum and increases intracellular cGMP (cyclic GMP) levels. The increase in intracellular cGMP decreases the intracellular calcium level, which induces scaphoid smooth muscle relaxation, which in turn induces penile erection through cavernous volume expansion. Since cGMP is decomposed by PDE (phosphodiesterase), its activity must be inhibited to increase the concentration of cGMP and improve erectile function.

Nitric oxide (NO) is biosynthesized by the biochemical action of NOS (nitric oxide synthase) in the body. And, by immunohistochemistry, NOS-containing nerves and organs in which they exist have been revealed, and their distribution has been found to be anatomically similar in rats and humans. NO, a factor that improves erectile function by promoting the relaxation of vascular smooth muscle in the cavernous body tissue, is an incomplete and unstable substance and cannot be directly quantified because its half-life is very short. By measuring, the content of NO can be estimated.

On the other hand, when blood vessels are relaxed by inhibiting the activity of angiotensin converting enzyme (ACE), which is involved in the production of angiotensin II, a powerful vasoconstrictor in the human body, blood flow in the penis increases, which leads to penis erection.

It is thought to be effective to inhibit the action of ACE, which is involved in the synthesis of angiotensin, a powerful vasoconstrictor, in order to maintain the relaxation state of the vascular muscle, which is the key to maintaining an erection, which is deeply related to the improvement and strengthening of male sexual function. In fact, so far, some ACE inhibitors have been proposed as candidates for improving and enhancing sexual function.

The angiotensin-converting enzyme (ACE; peptodyldipeptide hydrolase EC 3.4.15.1) is an enzyme that plays a very important role in regulating blood pressure, and this enzyme increases blood pressure by hydrolyzing angiotensin composed of 10 amino acids into angiotensin. Angiotensin, a potent vasoconstrictor, stimulates the secretion of aldosterone. As a result, aldosterone increases the retention of Na+ and water in the kidneys and increases arterial blood pressure.

The composition for improving male sexual function comprising the sardine extract of the present invention inhibits ACE to suppress the production of angiotensin, and can lower blood pressure, and also, when blood vessels are relaxed, blood flow in the penis increases, thereby inducing penile erection.

In addition, the size of the prostate gland in adults is ~ 20 g (± 6 g), but it can grow to 40 ~ 400 g in an abnormal condition. In the case of a normal prostate, epithelial cells and stromal cells interact closely to organically control the growth and regression of the prostate, but in the case of an enlarged prostate, apoptosis is more The smaller the volume, the larger the prostate gland.

BPH is a histologic disease in which the number of normal cells in the prostate increases and becomes enlarged.

In particular, BPH causes significant changes in stromal cells in the prostatic transition zone and the area surrounding the proximal urethra. The ratio of stromal cells to epithelial cells is 4.6:1. Growth of these stromal cells is regulated under the control of the adrenergic nerve system, and the related α1asubtype receptor is known as the adrenergic receptor most commonly found in stromal tissue inside the prostate.

In particular, there are reports that epidermal growth factor (EGF), basic fibroblast growth factor (bFGF), and transforming growth factor β (TGFβ) are involved. EGF and TGF-β are strong mitogenic factors, and prostate tissue or prostate fluid contains a large amount of EGF, so prostate enlargement caused by androgen is mediated by EGF. TGFβ is also increased in BPH, probably involved in the differentiation of matrix cells into smooth muscle cells. bFGF is a potent mitogenic factor and is also overexpressed in BPH, and bFGF is produced in both stromal cells and epithelial cells.

The composition for improving male sexual function of the present invention is to prevent male sexual diseases selected from the group consisting of erectile dysfunction, premature ejaculation, genitalia and enlarged prostate.

The erectile dysfunction (erectile dysfunction) is a phenomenon in which normal blood inflow is not achieved in the corpus cavernosum tissue, and refers to a case in which the penis is not sufficiently erected or does not persist even if it occurs more than 25% of the total sexual life.

In order to treat erectile dysfunction, a medical treatment method of applying a drug acting on the above mechanism or administration of male hormones, surgical treatment such as vascular surgery or penile prosthesis insertion, and injection of a corpus cavernosum vasodilator have been proposed. The most preferred treatment for erectile dysfunction patients is drug therapy. Adrenergic α-receptor blockers related to penile smooth muscle relaxation, cholinergic drugs, nitric oxide (NO), peptides, prostaglandins, histamine, calcium channel blockers, potassium channel openers, Non-specific vasodilators have been developed as drugs.

Premature ejaculation (premature ejaculation) is a phenomenon in which ejaculation occurs early before sexual satisfaction due to disturbance in ejaculation control, and is the most common sexual dysfunction in men. Premature ejaculation occurs when the concentration of serotonin in the central nervous system decreases, and ejaculation is affected by neurotransmitters dopamine, GABA, noradrenaline, and serotonin in the central nervous system. Among them, serotonin is the most important neurotransmitter that affects ejaculation function.

Due to the above premature ejaculation, the person may feel anxious and depressed due to severe stress and a decrease in sexual confidence, satisfaction, and self-esteem.

Yin gynecomastia is a condition caused by hyeolheo (血虛) from the continuation of emotional instability or overwork. It is a symptom in which a man's genitals do not have an erection at all or their erection is very weak.

Benign Prostatic Hyperplasia (BPH) is one of the most common diseases in men, and its incidence is rapidly increasing in recent years. BPH occurs in about 50% of people in their 60s and about 90% of people over 85 years of age, and lower urinary tract symptoms (LUTS) such as nocturia, delayed urination, frequent urination, and incontinence occur, and repeated urinary tract infections. , or urinary tract obstruction, surgery is required.

Therefore, the effect of maintaining erection of the penis and inhibiting enlargement of the prostate is an important part to improve male sexual function, and it can prevent male sexual diseases such as erectile dysfunction, premature ejaculation, genitalia and prostatic hypertrophy.

The composition will further include a natural extract selected from the group consisting of golden extract, thistle extract and dandelion extract.

Gold (Scutellaria baicalensis) is a dicotyledonous plant, a perennial herb in the family Lamiaceae, which grows in grasslands in mountainous areas. The height is 20 ~ 60cm, and several stalks come out and grow into leaves, hairy, and branched. The leaves are opposite, lanceolate, and the edges are flat. Flowers bloom in July-August, purplish and run in a raceme Žm, biased to one side. It is distributed in Siberia, Mongolia, Manchuria, and China, and in Korea, it is found in Ulleungdo, Jecheon and Cheongju in North Chungcheong Province.

Thistle (Cirsium japonicum var) is a dicotyledonous perennial plant of the order Asteraceae, which grows upright and has many white hairs like spider webs. The leaves are alternate phyllotaxis, and there are hairs on both sides in the upper right corner, and there are engraved saw teeth on the edge. There are also sharp thorns, and the lower base of the leaf gently wraps the stem. Flowers appear red or purple in June-July, and two flowers hang one at the end of branches and main stems, and they are all ornamental flowers. Before the pistil grows, the stamen grows first and releases pollen. The fruit is a skinny berry with white feathers.

Dandelion (Taraxacum platycarpum) is a dicotyledonous perennial plant in the order Asteraceae, belonging to the dicotyledonous family of the Angiosperm family, and grows in a sunny place in a field. There is no stem, and the leaves are clustered at the root and spread laterally. The leaves are in the shape of an upside-down lancet, 6-15cm long and 1.2-5cm wide, and have a pinnate shape deeply pitted, with serrated edges and some hairs. Flowers bloom in yellow from April to May, and one capillary flower hangs at the end of a flower stalk similar in length to leaves. There are white hairs on the flower stalk, but it gradually disappears, leaving only the head and hairs. The fruit is a fruit. It has a long oval shape with a length of 3 to 3.5 mm, brown, and has thorn-like projections on the upper part. The length of the root is 7~8.5mm, the tube hair is 6mm long, and it is light white. The young leaves are eaten as a vegetable in spring. The dandelion is used as a medicinal plant called pogongyeong in oriental medicine before it blooms, and is effective for heat-induced swelling, mastitis, sore throat, appendicitis, peritonitis, acute hepatitis, and jaundice. It is also used for symptoms of inability to urinate due to heat. In folklore, it is also used as a medicine to secrete milk faster.

The composition for improving male sexual function further includes a natural extract selected from the group consisting of golden extract, milk thistle extract and dandelion extract, in addition to the sardine extract, and when used as a complex extract, it is possible to better exhibit the effect of enhancing the erection of the penis have.

Preferably, the composition of the present invention may include 40 to 60 parts by weight of golden extract, 40 to 60 parts by weight of thistle extract, and 40 to 60 parts by weight of dandelion extract, based on 100 parts by weight of the sardine extract. When used as a complex extract within the above range, due to the complex action between each component, the effect of enhancing the erection of the penis is further increased compared to the case of using only the sardine extract.

More preferably, the composition for improving male sexual function comprising the extract of Jeongiri extract as an active ingredient may further include an extract of Seondeung rake (Vicia heptajuga Nakai).

The vicia heptajuga Nakai is a perennial plant that grows in mountainous areas. The leaves are alternate phyllotaxis, and the even-pinnate compound leaves are composed of 4 to 6 pairs of leaflets, with tendrils at the tip, dull at the bottom, long pointed ends, and the edges are it's bland Flowers bloom in June-July in reddish-purple, and 2~4cm inflorescences appear from the leaf axils and run in raceme inflorescences biased to one side.

When the sardine extract, golden extract, thistle extract, and dandelion extract are mixed and used, the elixir extract increases the erection enhancing effect of the penis due to the mixing action between each component, and neutralizes the fishy taste and flavor unique to the sardine extract. This makes it possible to provide a composition having excellent palatability.

Preferably, the composition of the present invention may include 40 to 60 parts by weight of golden extract, 40 to 60 parts by weight of thistle extract, 40 to 60 parts by weight of dandelion extract, and 20 to 30 parts by weight of sardine extract based on 100 parts by weight of the sardine extract. have.

When used as a complex extract within the above range, it is possible to provide a composition with excellent palatability while exhibiting an excellent effect of enhancing the erection of the penis.

The natural extract may be extracted using an extraction solvent selected from the group consisting of water, C ₁ to C _{6 lower alcohols, and mixtures thereof.}

Specifically, in order to prepare a natural extract, washing the natural product; drying after washing; pulverizing the natural product after drying; leaching the pulverized product using an organic solvent; drying the sample after leaching; leaching with water; And including the step of leaching, it is possible to obtain a natural extract.

The natural extract extracted using the organic solvent may further comprise the step of performing fractionation using an organic solvent.

The method for preparing the extract may be a conventional extraction method in the art, such as an ultrasonic extraction method, a leaching method, and a reflux extraction method. Specifically, it may be an extract obtained by extracting a natural product from which foreign substances have been removed by washing and drying with water, alcohol having 1 to 6 carbon atoms, or a mixed solvent thereof, and may be an extract extracted by sequentially applying the solvents to the sample.

The reflux extraction method is water, based on 100 mL of an alcohol having 1 to 6 carbon atoms, 10 to 30 g of a pulverized product of a natural product, a reflux time of 1 to 3 hours, and 50 to 100% alcohol or water having 1 to 6 carbon atoms. More specifically, based on 100 mL of alcohol or 100 mL of water having 1 to 6 carbon atoms, 10 to 20 g of a pulverized product of natural products, 1 to 2 hours reflux, and 70 to 90% alcohol or water having 1 to 4 carbon atoms.

The leaching method is carried out at 15 to 30° C. for 24 to 72 hours, and water or 50 to 100% alcohol having 1 to 6 carbon atoms is used as an extraction solvent. More specifically, the process is carried out at 20 to 25° C. for 30 to 54 hours, and the extraction solvent is water or 70 to 80% alcohol having 1 to 6 carbon atoms.

In the ultrasonic extraction method, the reaction is performed at 30 to 50° C. for 0.5 to 2.5 hours, and the extraction solvent is water or 50 to 100% alcohol having 1 to 6 carbon atoms. Specifically, extraction is performed at 40 to 50° C. for 1 to 2.5 hours, and the extraction solvent is water or 70 to 80% alcohol having 1 to 6 carbon atoms.

The extraction solvent may be used in an amount of 2 to 50 times, more specifically, 2 to 20 times, based on the weight of the sample. For extraction, the sample may be left for 1 to 72 hours for leaching in the extraction solvent, and more specifically, left for 24 to 48 hours.

After extraction, the extract may be fractionated by sequentially applying a fresh fractionation solvent. The fractionation solvent used for fractionation is any one or more selected from the group consisting of water, hexane, butanol, ethyl acetic acid, ethyl acetate, methylene chloride and mixtures thereof, preferably ethyl acetate or methylene chloride.

After obtaining the extract or fraction, a method such as concentration or freeze-drying may be additionally used.

Functional food according to another embodiment of the present invention may include the composition for improving male sexual function.

"Functional food" as used in the present invention is a food manufactured and processed by extracting, concentrating, refining, mixing, etc., a specific ingredient as a raw material for the purpose of health supplementation, or including health supplement food. In addition, it is a food designed and processed to sufficiently exert the biological control functions of the food ingredients, such as biological defense, regulation of biological rhythm, prevention and recovery of diseases, and functions related to disease prevention and recovery from diseases. It is assumed to include all that it has.

The pharmaceutical composition according to another embodiment of the present invention includes the composition for improving male sexual function.

The pharmaceutical composition may further include one selected from the group consisting of pharmaceutically acceptable carriers, excipients and diluents. Specifically, the pharmaceutical composition is each formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, etc., external preparations, suppositories and sterile injection solutions according to conventional methods to be used. can

In the present invention, carriers, excipients and diluents that may be included in the pharmaceutical composition include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia gum, alginate, gelatin, calcium phosphate , calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. In the case of formulation, it is prepared using commonly used diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrants, and surfactants. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc., and these solid preparations include at least one excipient in the extract and its fractions, for example, starch, calcium carbonate, It is prepared by mixing sucrose or lactose, gelatin, etc. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid preparations for oral use include various excipients, such as wetting agents, sweeteners, fragrances, and preservatives, in addition to simple diluents such as water and liquid paraffin, which are commonly used for suspensions, solutions, emulsions, and syrups. have. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Non-aqueous solvents and suspending agents include propylene glycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate. As the base of the suppository, witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin, and the like can be used.

The pharmaceutical composition of the present invention may be administered in a pharmaceutically effective amount, and the term "pharmaceutically effective amount" of the present invention means to treat or prevent a disease at a reasonable benefit/risk ratio applicable to medical treatment or prevention. It means an amount sufficient to The duration of treatment may be determined depending on factors including drugs used in combination with or concurrently with the composition of the present invention and other factors well known in the medical field. The pharmaceutical composition of the present invention may be administered alone or in combination with a known immunotherapeutic agent. Taking all of the above factors into consideration, it is important to administer an amount that can obtain the maximum effect with a minimum amount without side effects.

The composition for improving male sexual function comprising the sardine extract of the present invention as an active ingredient is a composition for improving male sexual function that improves male sexual function through the effect of enhancing penis erection and inhibiting prostate enlargement by including the sardine extract as an active ingredient, It can be taken and has no side effects, so it can be applied as an improving agent and therapeutic agent that can be safely used mentally and physically.

1 is a result of measuring the cell viability in testis cells TM3 of a composition according to an embodiment of the present invention.
2 is a result showing the ACE (Angiotensin converting enzyme) inhibitory effect of the composition according to an embodiment of the present invention.

Hereinafter, embodiments of the present invention will be described in detail so that those of ordinary skill in the art can easily carry out the present invention. However, the present invention may be embodied in several different forms and is not limited to the embodiments described herein.

[Preparation Example: Preparation of Extract]

1. Preparation of sardine extract

The sardines were thoroughly washed in running water, then dried and pulverized with a blender to prepare a powder. 50% ethanol as an extraction solvent was added to the powder sample at a ratio of 1;10 (w; v), and then completely immersed, and extracted three times for 3 hours while refluxing at 80°C. The extract is Whatman No. 2 filtered with filter paper. The filtrate was concentrated under reduced pressure at 60° C. to prepare a sardine extract (SE).

2. Preparation of golden extract

First, gold (Scutellaria baicalensis) was washed, dried, and then pulverized. The pulverized product was mixed with 60% ethanol and extracted for 2 hours, cooled and filtered with Whatman filter paper, and the filtrate was obtained to prepare a golden extract (BE).

3. Preparation of other natural extracts

Milk thistle extract (CE), dandelion extract (TE), and serrata extract (VE) were prepared by using the same method as for the preparation of the golden extract (BE).

4. Preparation of Complex Extracts

The sardine extract (SE), golden extract (BE), milk thistle extract (CE), dandelion extract (TE), and sardine rake extract (VE) were mixed as shown in Table 1 to prepare a complex extract.

SF1 SF2 SF3 SF4 SF5 SF6 SF7 SF8 SF9 SF10 SE 100 100 100 100 100 100 100 100 100 100 BE - 10 20 30 40 50 30 30 30 30 CE - 10 20 30 40 50 30 30 30 30 TE - 10 50 30 40 50 30 30 30 30 VE - - - - - - 10 20 30 40

(Unit: parts by weight)

[Experimental Example 1: Toxicity test in testicular cells TM3]

In order to test the toxicity of sardine extracts (SE, SF1) and complex extracts (SF2 to SF10), MTT analysis was used for TM3 mouse testis cells, and the presence or absence of cytotoxicity of the samples was confirmed through MTT analysis.

TM3 cells (KCLB21714) were purchased from a cell line bank in Korea. Fetal bovine serum (FBS), DMEM (Dulbecco's Modified Eagle Medium), MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide), Sigma (Sigma Chem. Co., USA) ) was purchased from As an ELISA microplate reader, VersaMax (Molecular Device, USA) was used.

First, in a 96-well plate, 180 μl (2 X 10 ⁵ cells) of TM3 cells were treated with 20 SF1 to SF10, each at a concentration of 100, 500, and 1000 ppm, and then cultured at 37 for 24 hours, followed by MTT solution (5 mg/ml) was added and incubated at 37°C for 3 hours.

After removing the supernatant, 200 μl of DMSO was added per well, reacted for 20 minutes, and then the absorbance was measured in an ELISA reader 570 nm to calculate the survival rate. The value of the normal group (the group treated with PBS instead of the sample treatment) was used as a control, and the O.D. (Optical density) value at this time was defined as 100% cell viability.

Cell viability (%) = (experimental/control) X 100

The results, as shown in Figure 1 below, were compared with the cell viability of the control group not treated with the sample as 100%, and it is usually determined that there is toxicity when the cell viability is 80% or less at a concentration of 1000 ppm. It was confirmed that there was no toxicity in SF1 to SF10.

[Experimental Example 2: Penile erection enhancement effect]

1. Determination of NO Concentration in HUVECs

HUVEC cells were used to measure the efficacy of NO production, which is involved in NOS and is closely related to erection. NO concentration was measured using a total nitric oxide assay kit. ^{HUVEC 900 (110 4} cells) per well was put in a 12-well plate and _{cultured in a 37, 5% CO 2} incubator for 24 hours, then the medium was discarded and the cultured cell surface was washed with 1X PBS. SF1 to SF10 dissolved in 1X PBS were mixed with EGM-2 to a final concentration of 500 ppm and cultured for 48 hours in _{a 37, 5% CO 2 incubator.}

NADH 25 and nitrate reductase 25 were mixed in the cultured medium, and then reacted for 30 minutes at 37°C. Then, Griess reagent 50 was added, mixed well, and allowed to stand at room temperature for 10 minutes. After the reaction was completed, the absorbance was measured to calculate the concentration of nitrate, and nitrate was measured as an indicator of NO production.

As a result, a negative control treated with a medium instead of a sample and 500 ppm of a ginseng extract as a positive control were compared to the NO production in Table 2 below.

NO concentration 0 ppm (negative control) 0.002 ± 0.092 SE, SF1 500ppm 6.038 ± 0.468 SF2 500ppm 6.838 ± 0.472 SF3 500ppm 7.438 ± 0.533 SF4 500ppm 7.508 ± 0.065 SF5 500ppm 11.704 ± 0.128 SF6 500ppm 10.210 ± 0.024 SF7 500ppm 12.508 ± 0.055 SF8 500ppm 14.323 ± 0.824 SF9 500ppm 16.369 ± 0.609 SF10 500ppm 15.648 ± 0.276 Ginseng 500ppm (positive control) 5.422 ± 0.010

(Unit: μmol/ml)

As shown in Table 2, the negative control group treated with the medium instead of the sample obtained a result of 0.002 μmol/ml, and when compared with the ginseng extract used as the positive control, SF1 to SF10 according to the present invention had a concentration of nitrate was confirmed to increase.

In particular, it was confirmed that NO production was increased in SF7 to SF10 that further contained the extract of Seondeep rake.

Therefore, it was confirmed that the present invention can improve the erectile function of the penis by increasing the production of NO, which is a vasodilator.

2. Measurement of ACE (Angiotensin converting enzyme) inhibitory effect

In order to maintain the relaxation state of the vascular muscle, which is the key to maintaining an erection, which is deeply related to the improvement and strengthening of male sexual function, the ACE inhibitory effect involved in the synthesis of angiotensin, a vasoconstrictor, was measured.

NHippuryl-His-Leu was used instead of Angiotensin, a substrate of ACE, and ACE was extracted from rabbit lung tissue powder and used as an enzyme solution.

For ACE inhibitory activity, 50 μl of ACE coenzyme solution was added to SF1 to SF10, followed by pre-reaction at 37° C. for 5 minutes, followed by addition of a substrate solution, followed by reaction at 37° C. for 30 minutes. 150 μl of 0.1 M HCl was added to stop the reaction, and 750 μl of ethyl acetate was added thereto, followed by stirring for 15 seconds. After centrifugation at 3000 rpm for 5 minutes, the supernatant was completely dried, dissolved in 3 ml of distilled water, and absorbance was measured at 228 nm.

As a negative control, distilled water was used instead of the crude enzyme solution, and as a positive control, Enalapril maleate salt was used, and the ACE inhibition rate was calculated using the following formula.

ACE inhibition rate (%) = [1-(ACE test/ACE control)] X 100

For the inhibition rate, 5 mg/ml HHL (hippuryl-histidyl-leucine) was used as a substrate, and absorbance was measured at 228 nm by reacting 0.1 g/ml ACE coenzyme solution at 37° C. for 30 minutes.

The results are shown in FIG. 2 below, and when the inhibition rates for each SF1 to SF10 sample were compared, it was confirmed that the ACE inhibition rate was superior to that of the positive control when the Seondeep rake extract was further included.

Therefore, the present invention can maintain an erection by indirectly increasing the blood flow of the penis through the relaxation of blood vessels.

[Experimental Example 3: Inhibitory effect of prostate enlargement]

1. Prostatic Hyperplasia Mice Animal Experiments

For male Sprague Dawley rats, each group was divided as follows. Experimental group was divided into vehicle control group (VCTL), testosterone-only group (TP-CTL), testosterone-administered finasteride as a positive control group (TP + FS), and group administered with SF1 to SF10 of the present invention. was performed, n = 4 for each group, and testosterone was injected subcutaneously for 2 weeks to induce an enlarged prostate. While maintaining the situation, it was confirmed whether the progression of prostate enlargement was inhibited by oral administration of SF1 to SF10 of the present invention every day.

The day after the last administration was finished, the body weight was measured, and blood was collected and the prostate was removed by sacrificing. The extracted prostate was weighed after removing surrounding fat and foreign substances, and the weight ratio of the prostate per body weight was calculated using the following formula.

Prostate weight (g) /body weight (g) x 100

The results are shown in Table 3 below.

prostate weight prostate/weight V-CTL Ratio TP-CTL Ratio V-CTL 0.55 ±0.04 0.12 ±0.008 100.0 ± 6.2 - TP-CTL 1.22 ±0.12 0.30 ±0.019 249.9 ±19.4 100.0 ±7.8 TP+ FS (2 mg/kg) 0.95 ±0.12 0.22 ±0.018 185.7 ±15.1 74.3 ±3.2 TP + SF1 (2 mg/kg) 1.14 ±0.06 0.27 ±0.021 226.6 ±17.6 90.7 ±7.0 TP + SF2 (2 mg/kg) 1.10 ±0.04 0.27 ±0.019 223.9 ±15.9 88.4 ±7.3 TP + SF3 (2 mg/kg) 1.08 ±0.18 0.24 ±0.005 219.4 ±11.2 87.2 ±3.3 TP + SF4 (2 mg/kg) 1.06 ±0.87 0.22 ±0.025 213.8 ±16.3 85.7 ±3.5 TP + SF5 (2 mg/kg) 1.05 ±0.28 0.22 ±0.002 210.2 ±11.1 84.4 ±9.2 TP + SF6 (2 mg/kg) 1.05 ±0.02 0.23 ±0.025 211.1 ±12.5 85.6 ±10.7 TP + SF7 (2 mg/kg) 1.03 ±0.07 0.21 ±0.045 203.4 ±12.7 81.6 ±6.3 TP + SF8 (2 mg/kg) 1.03 ±0.11 0.20 ±0.078 202.1 ±20.3 81.3 ±4.9 TP + SF9 (2 mg/kg) 1.02 ±0.16 0.20 ±0.002 199.7 ±28.4 80.6 ±6.7 TP + SF10 (2 mg/kg) 1.03 ±0.54 0.21 ±0.007 202.0 ±24.8 81.6 ±5.4

(unit: %)

As shown in Table 3, in the case of TP-CTL compared to V-CTL, the size of the prostate increased to 249% by administration of TP for 5 weeks, which is the point at which the experiment was finished. The drug-induced weight reduction of the enlarged prostate showed a statistically significant difference compared to TP-CTL in the FS treatment group (3 mg/kg/day) and SF1 to SF10 treatment group (2 mg/kg). (P < 0.05).

In the case of weight ratio considering the body weight, compared to TP-CTL, the FS group showed an effect of reducing the size by 74.3%, and it was significantly smaller in the group administered with 2 mg/Kg of SF7 to SF10 containing the extract of serratus rake. appeared to be losing.

[Experimental Example 4: Taste Test]

1. Sensory evaluation test

A tea beverage was prepared by diluting the complex extracts SF1 to SF10. The tea drinks were tasted by 10 tasters, and the taste and aroma were expressed as an index of 1 to 10, and the average value (0.5 rounding applied) is shown in Table 4 below. In the following index, the higher the number, the higher the degree of preference.

SF1 SF2 SF3 SF4 SF5 SF6 SF7 SF8 SF9 SF10 taste 6.0 6.0 6.5 7.0 7.5 6.0 8.0 8.5 9.0 8.5 incense 6.0 6.5 6.5 7.0 7.5 7.0 7.5 8.5 9.0 7.5 Overall preference (average) 6.0 6.0 7.0 7.0 7.5 6.5 8.0 8.5 9.0 8.5

(Unit: Index)

Referring to Table 4 above, in the case of SF1, sardine extract (SE) was used alone to lower the taste and flavor preference, and in the case of mixing SF2 to SF10, natural extracts with different taste and flavor of hemp extract It can be seen that the preference increases as it is neutralized by

In particular, it was confirmed that, in the case of SF7 to SF10, which further contains the extract of Seondeung rake, the taste and flavor were highly evaluated, and the preference was greatly increased.

Therefore, in the case of the complex extracts SF7 to SF10 of the present invention, it is possible to provide a functional food having an excellent effect on the erection of the penis with a higher preference for flavor and taste.

Although preferred embodiments of the present invention have been described in detail above, the scope of the present invention is not limited thereto, and various modifications and improvements by those skilled in the art using the basic concept of the present invention as defined in the following claims are also provided. is within the scope of the

Claims (7)

Contains Sardinops sagax extract as an active ingredient.
A composition for improving male sexual function. According to claim 1,
The composition improves male sexual function through the effect of enhancing penis erection and inhibiting prostate enlargement
A composition for improving male sexual function. According to claim 1,
The composition is for preventing male sexual diseases selected from the group consisting of erectile dysfunction, premature ejaculation, genitalia and benign prostatic hyperplasia
A composition for improving male sexual function. According to claim 1,
The composition further comprises a natural extract selected from the group consisting of gold (Scutellaria baicalensis) extract, thistle (Cirsium japonicum var) extract and dandelion (Taraxacum platycarpum) extract
A composition for improving male sexual function. According to claim 1,
The extract is extracted using an extraction solvent selected from the group consisting of water, C ₁ to C _{6 lower alcohols and mixtures thereof.}
A composition for improving male sexual function. A composition for improving male sexual function according to any one of claims 1 to 5
pharmaceutical composition. A composition for improving male sexual function according to any one of claims 1 to 5
Functional food composition.

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