KR100752952B1 - A pharmaceutical composition containing Yacon or the extract thereof - Google Patents

Abstract

The present invention relates to a composition for treating infertility containing yacon or its extract as an active ingredient, specifically, yacon extract obtained by extracting yacon or yacon with an organic solvent increases sperm count in mammals and secretes male hormones. There is activity to promote the composition containing it can be usefully used for the prevention and treatment of infertility.

Yacon, infertility, sperm, and male hormones

Description

Pharmaceutical composition containing yacon or the extract

1 is a graph measuring the effect of yacon extract on the weight of male rats,

●: control group;

Δ: yacon 50 mg / kg administration group;

▼: yacon 100 mg / kg administration group;

◇: yacon 200mg / kg administration group

Figure 2 is a graph measuring the sperm count of the testis as a result of administering yacon 50% ethanol extract for 6 weeks in male rats,

Figure 3a is a tissue staining picture of the control group was not administered yacon extract, 3b is a tissue staining photograph of the testis of male rats after administration of 200mg / kg yacon 50% ethanol extract for 6 weeks.

The present invention relates to a composition for treating infertility containing yacon or its extract as an active ingredient.

More specifically, yacon extract obtained by extracting yacon or yacon with an organic solvent has an activity of increasing the sperm count of a mammal and promoting the secretion of male hormone, and the composition comprising the same prevents and treats infertility of a mammal. It can be usefully used.

Yacon ( Polymnia sonchifolia ) is a perennial plant belonging to the Asteraceae family and is native to Ecuador and Peru in the Andes region of South America. This plant has been used as a food for alpine Indians, and until the end of 1980, it has received little attention in the scientific community except Peru and Japan.

At present, it is known not only as a food but also as a medicinal plant in some regions, and in particular, fructooligosaccharides and phenolic compounds contained in tubers of yacon attract attention. Tubers are used as natural sweeteners and syrups, and leaves are known to have antidiabetic effects. The hypoglycemic effect of rats has been reported, but the mechanism has not been elucidated.

Recently, antifungal effects have been reported in the leaves of yacon and their physiological activity has been reported to be related to essential oils. The tubers contain fructose, glucose, saccharose and inulin type oligofructans. In addition, studies on the antioxidant effects of tubers were reported, and tryptophan and chlorogenic acid were identified as major compounds.

B. Simonovska etc. The phenolic compounds present in the ethyl acetate (ethylacetate) layer of yacon leaf and have antioxidant activity in Hepa soil site (hepatocyte) in Rats tert - butyl hydroperoxide hydroxide oxide induced by (tert -butylhydroperoxide) enemy It has been reported that there is a cytoprotective effect on oxidative damage.

The inventors of the present invention, while studying to confirm the new physiological activity of yacon, found that the administration of ethanol extract of yacon to male rats increases the sperm count and the concentration of male hormone.

It is an object of the present invention to provide a natural product which is stable in stability and can treat infertility or a decrease in reproductive function.

In order to achieve the above object, the present invention provides a pharmaceutical composition for preventing and treating infertility containing yacon or its extract.

In another aspect, the present invention provides a pharmaceutical composition for the prevention and treatment of male hormone abnormalities containing yacon or extracts thereof.

Hereinafter, the present invention will be described in detail.

The present invention provides a pharmaceutical composition containing yacon or extracts thereof.

The composition of the present invention may be contained in the form of a powder or granules by drying the yacon or in a liquid form by diluting with water. At this time, yacon is not limited to the tubers or specific parts of the leaves and stems can use all of the yacon plants, but it is preferable to use tubers.

In addition, the composition of the present invention may include a yacon extract, the extract according to the present invention may be a crude extract prepared by applying a solvent extraction method using a conventional water extract, alcohol, etc. as a solvent, and also the column chromatograph It may be a fraction extract purified using. The method for producing an extract according to the present invention can be applied to all plant extraction methods known to those of ordinary skill in the art, for example, extraction with water, alcohol or mixed solvents, extraction with a bath or room temperature, etc. Including but not limited to.

Specifically, it is preferable to contain the extract which extracted yacon with organic solvents, such as alcohol, an ether, petroleum ether, benzene, ethyl acetate, and chloroform, and it is most preferable to contain the yacon ethanol extract extracted with ethanol.

In this case, when yacon is extracted with an organic solvent, all solvents are removed by drying under reduced pressure, and then used.

Preferably the composition of the present invention is to obtain a bioactive fraction of yacon to include the purified yacon extract.

The present invention provides a pharmaceutical composition for preventing and treating infertility containing yacon or extracts thereof.

In general, male infertility may include semen or sperm abnormality, sperm movement disorder or incapacity, and due to a problem in testicular function that makes double sperm, male infertility due to disorders in sperm formation or abnormality in semen components. This accounts for more than half.

The causes of female infertility are very diverse and finding the cause is not easy. Representative examples include ovulation disorders such as difficulty passing through the fallopian tubes, amenorrhea, ovulation cycles and sporadic aovulation.

When the composition according to the present invention is administered to white rats, the number of sperm in the testicles and epididymis of the rats is significantly increased. Therefore, the composition of the present invention can be effectively used to treat or prevent male infertility due to abnormality of semen or sperm.

In addition, when the composition according to the present invention is administered to male rats for a certain period of time, the concentration of testosteron, a testosterone, is increased. Testosterone secreted by hepatocytes of male testicles plays a role in developing and maintaining male genital organs and expressing male sexual characteristics.

Therefore, the composition of the present invention can be usefully used as a composition for the prevention and treatment of male hormone abnormalities, and is effective in the treatment and prevention of infertility due to male hormone deficiency.

The composition according to the present invention may be included in an amount of 1 to 100 parts by weight based on the total weight of the final product, and may be prepared as a food or a pharmaceutical by adding one or more carriers which are food or pharmaceutically acceptable. The carrier may include, but is not limited to, saline, buffered saline, water, glycerol, ethanol, and the like, and any suitable agent known in the art may be used.

The pharmaceutical composition of the present invention prepared by the conventional method as described above can be administered orally during clinical administration and can be used in the form of general pharmaceutical preparations, and when formulated, commonly used fillers, extenders, binders, wetting agents And diluents or excipients such as disintegrants and surfactants.

The pharmaceutical composition may be applied differently depending on the age, sex, condition, absorption of the active ingredient, inactivation rate and excretion rate of the subject, and the drug used in combination, for example, 10 to 30 g per day may be orally administered. It is not limited.

Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc., and liquid preparations for oral use include suspensions, solvents, emulsions, and syrups. In addition to liquid paraffin, various excipients may be included, such as wetting agents, sweetening agents, fragrances, preservatives and the like.

Hereinafter, the present invention will be described in more detail with reference to Examples, but the scope of the present invention is not limited to these Examples, and various modifications and variations are possible within the protection scope of the present invention described in the claims. It will be apparent to those skilled in the art to which the invention pertains.

< Example  1> Preparation of Test Solution

The dried yacon root (Gyeongbuk, Bonghwa) was put into a power motor, pulverized to a suitable size, 50% ethanol was added, sonicated at 60 ° C. for 5 hours, extracted three times, and the filtrate was collected.

The filtrate was concentrated using a rotary evaporator, frozen in a -70 ° C. deep freezer, and dried using a freezing drier, to prepare an aqueous solution according to the formula shown in Table 1 below.

Prescription 1 Yacon root powder 2.5g; Purified Water 100ml Prescription 2 Yacon root powder 5.0 g; Purified Water 100ml Prescription 3 Yacon root powder 10.0 g; Purified Water 100ml

< Example  2> male rats Yacon  Administration of Extract

Six-week-old Sprague Dawley male rats (Gyeonggi-do and Samtako) were adapted to a breeding environment for one week, and then each of the control and test groups consisted of nine animals, and the solution of the prescriptions 1 to 3 was weighed 1 kg. 0 mg (control), 50 mg, 100 mg and 200 mg, respectively, were administered for 6 weeks.

< Test Example  1> Yacon  Correlation between Extract and Weight

As a result of observing the effect of yacon administration on the body weight of rats during the test period according to Example 2, no significant change was observed compared to the control group. In addition, no change in body weight was observed according to the dose of yacon extract (see FIG. 1).

< Test Example  2> Collection of testicles and epididymis

After the end of administration according to Example 2, the rats were anesthetized with ether, and then opened, and the testicles and epididymis were respectively removed and weighed.

As a result, as can be seen from Table 2, each administration group did not show a significant difference compared to the control group.

Changes in Weights of Testicles and Epididymis According to Yacon Extract Administration Weight (g) Testicle (g) Epididymis (g) Control 404.44 ± 63.86 3.200 ± 0.169 1.144 ± 0.058 Yacon 50mg / kg 415.56 ± 27.44 3.145 ± 0.252 1.111 ± 0.070 Yacon 100mg / kg 378.89 ± 31.00 3.185 ± 0.303 1.103 ± 0.119 Yacon 200mg / kg 401.25 ± 29.49 3.175 ± 0.177 1.080 ± 0.095

All test data shown in the test example of this specification is mean +/- S.D. (n = 9).

< Test Example  3> of rat Sperm count  Measure

After the end of the administration according to Example 2, the rats were anesthetized with ether, and then opened, and the testes and epididymis were respectively removed.

After peeling off the white membrane of the right testicle, 50ml of the centrifuge tube was put in 5ml distilled water and crushed twice with a homogenizer for 30 seconds, and then treated with an ultrasonic cleaner for 3 minutes. After dilution, 10 µl of the pulverized solution was taken, placed in a slide for counting blood cells, covered with a cover glass, and sperm count was measured using an optical microscope.

As a result, the number of sperm in the 200 mg / kg administration group showed a 74% increase compared to the control group (Table 3), and their increase was shown to increase in proportion to the dose (Fig. 2).

Changes in Sperm Number by Administration of Yacon Extract Control Yacon 50mg Yacon 100mg Yacon 200mg Testicle weight (g) 3.200 ± 0.169 3.145 ± 0.252 3.185 ± 0.303 3.175 ± 0.177 Total sperm count / Rat 234,154,013 ± 40,071,836 347,134,101 ± 88,948,162 375,590,640 ^* ± 57,646,572 40,9766,904 ^** ± 47,244,258 Sperm count / g ^a) 73,173,129 ± 12,522,449 110,376,503 ± 28,282,404 117,924,848 ± 18,099,395 130,033,144 ± 15,441,818 Sperm count / day ^b) 37,698,111 ± 6,667,297 59,475,012 ± 13,235,597 61,572,236 ± 9,450,258 66,700,608 ± 7,996,073

In the table, b) is a) /6.1 and 6.1 is the developmental period of the testes from stage I to IV.

* Is the significant difference from the control value (significant difference) and ANOVA test * p <0.05, ** p <0.01.

< Test Example  4> Preparation of tissue specimens

After the end of the administration according to Example 2, the rats were anesthetized with ether and then opened, and the testicles and epididymis were respectively extracted, and the left testes were soaked in Bouin's solution to make a tissue specimen.

The testicular tissue was sectioned into 1 × 1 cm size and fixed in 10% phosphate buffered neutral formalin solution. Next, after the tissue treatment process, the tissue embedding center was used to embed paraffin, and then 4 μm tissue slides were made with a rotating microtome, and stained with hematoxylin and eosin. Observed.

As a result, testicular tissues of male rats treated with Yacon 50% ethanol extract showed no pathological changes compared to the control group (see FIGS. 3A and 3B), and Leydig's and sertoli cells were also normal. On the other hand, spermatogenesis was significantly increased compared to the control group.

< Test Example  5> Measurement of Hormone Concentration

After the end of administration according to Example 2, rats were anesthetized with ether, and 5 ml of blood was collected from the abdominal aorta for centrifugation to measure hormone concentrations, and serum was separated by centrifugation at 3000 rpm for 15 minutes. Used for.

FSH, LH and Testosteron concentrations in blood were measured by RIA (Green Cross Medical Foundation, Seoul) method.

As a result, testosteron concentration of male hormone increased more than 3 times compared to control, whereas female hormone FSH decreased more than 2 times to 42% of control. On the other hand, LH was difficult to compare due to the low sensitivity and the large number of undetected individuals.

Changes in Hormone Concentrations after 6 Weeks of Yacon 200mg / kg in Male Rats FSH (mIU / ml) LH (mIU / ml) Testosteron (ng / ml) Control 1.28 ± 1.15 0.26 ± 0.68 1.66 ± 1.08 Yacon 200kg / kg 0.54 ± 0.67 0.05 ± 0.08 5.09 ± 2.53 ^*

* In the table is a significant deflection from the control value (significant defference) and the ANOVA test p <0.05.

As described above, when the yacon ethanol extract was administered to male rats, sperm count was increased in proportion to the administration concentration, and the testosterone level was significantly increased.

Therefore, yacon or its extract according to the present invention can be usefully used for the treatment and prevention of infertility due to a decrease in male sperm count and male hormone deficiency, and can be used for the prevention and treatment of male hormone abnormality.

Claims (5)

Pharmaceutical composition for the treatment and prevention of infertility containing yacon extracted with a lower alcohol having 1 to 4 carbon atoms. The pharmaceutical composition of claim 1, wherein the infertility is due to sperm abnormality or male hormone abnormality. Pharmaceutical composition for the treatment and prevention of male hormone deficiency containing an extract extracted with a lower alcohol having 1 to 4 carbon atoms. The pharmaceutical composition of claim 1 or 3, wherein the yacon extract is an ethanol extract of yacon. A food composition for enhancing reproductive function, containing an extract of yacon extracted with a lower alcohol having 1 to 4 carbon atoms.

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