AU2021104170A4

AU2021104170A4 - Composition for improving male function and use thereof

Info

Publication number: AU2021104170A4
Application number: AU2021104170A
Authority: AU
Inventors: Jiansheng Chen; Zhigang DUAN; Yaying Hou; Tong Zhang
Original assignee: Hoboomlife Bio Technology Shenzhen Co Ltd
Current assignee: Hoboomlife Bio Technology Shenzhen Co Ltd
Priority date: 2021-07-15
Filing date: 2021-07-15
Publication date: 2021-09-09
Anticipated expiration: 2029-07-15

Abstract

The present application belongs to field of nutritional supplement research and development, and particularly relates to a composition for improving male function and use thereof. The composition for improving male function contains NR derivative and L-arginine: when NR derivative is NMN, the composition also contains oyster peptide; when NR derivative is NADH, the composition also contains epimedium extract. Exogenous supplementation of NMN and/or NADH as well as L-arginine can increase the synthesis amount of NO; oyster peptide can promote the production of testosterone and improve body fatigue; epimedium extract can increase the eNOS content in the corpus cavernosum. The composition according to the present application is reasonable in terms of its formula and has proper compatibility, and it has a significant effect on improving male function.

Description

COMPOSITION FOR IMPROVING MALE FUNCTION AND USE THEREOF

Field of the Application

The present application belongs to field of nutritional supplement research and

development, and particularly relates to a composition for improving male function

and use thereof.

Background of the Application

Male erectile dysfunction refers to an ability of the normally anatomized penis which

cannot be erected or the erection hardness and time are not enough to complete

normal sexual intercourse in an appropriate environment and place with a sufficient

sexual stimulation. The causes of erectile dysfunction include psychological factors,

endocrine disorders, neurovascular diseases and etc. Most of the erectile dysfunctions

are caused by endocrine dysfunction. Endocrine disorders can be caused by

abnormalities in any link of the hypothalamic-pituitary-gonadal axis, which can lead

to decreased testosterone levels or low sexual function, thereby causing erectile

dysfunction. Male erectile dysfunction seriously affects the life of couples, easily

causes male mental inferiority, and causes family disharmony. There is no research

report on the use of NR derivatives for male function.

Summary of the Application

To this end, the present application provides a safe, non-toxic and side-effect

composition for improving male function and use thereof. The technical solutions of

the present application are as follows:

A composition for improving male function, comprising NR derivative and

L-arginine.

Further, the NR derivative is NMN or NADH.

Further, when the NR derivative is NMN, the composition further comprises oyster

peptide; when the NR derivative is NADH, the composition further comprises

epimedium extract.

Further, in parts by weight, comprising 150 to 220 parts of NMN, 100 to 150 parts of

L-arginine and 30 to 80 parts of oyster peptide; preferably, comprising 160 to 200

parts of NMN, 110 to 130 parts of L-arginine and 40 to 55 parts of oyster peptide.

Further, in parts by weight, comprising 10 to 30 parts of NADH, 40 to 80 parts of

L-arginine and 80 to 120 parts of epimedium extract; preferably, comprising 25 to 30

parts of NADH, 50 to 70 parts of L-arginine and 90 to 110 parts of epimedium extract.

Further, the composition further comprises excipient(s), the excipient is any one or

more selected from the group consisting of mannitol, erythritol, microcrystalline

cellulose, magnesium stearate, silicon dioxide, guarana extract, D-ribose, glutamine,

zinc citrate, magnesium oxide, betaine, creatine, taurine, black ginger extract, tongkat

ali extract, maca extract, octacosanol, sodium bicarbonate, sodium vitamin C, gastric

coating agent, and enteric coating agent.

Use of any one of the above-mentioned composition in improving male function.

Compared with the prior art, the beneficial effects of the present application are as

follows:

(1) In the corpus cavernosum, NO is a main neurotransmitter that mediates the

relaxation function of the corpus cavemosum smooth muscle, and is a key

neurotransmitter for penile erection. Nitric oxide synthase (NOS) plays a key role in mediating the relaxation of penile artery smooth muscle and cavernous sinus smooth muscle, and its decreased activity is considered to be the main pathological mechanism of erectile dysfunction. Therefore, reactivating NOS can increase the release of NO and induce a rapid relaxation response of the human corpus cavernosum smooth muscle, causing dilation of corpus cavemosum sinus and enlargement of the penis. The coenzyme of NOS is NMN and/or NADH. Exogenous supplementation of NMN and/or NADH can stimulate the synthesis of NO and increase the synthesis amount by up to 10 times;

(2) L-arginine is a substrate for the endogenous synthesis of NO, which produces NO

under the catalysis of NOS and exerts physiological effects. NO is a key

neurotransmitter for penile erection. Exogenous supplementation of L-arginine can

increase the amount of synthesized NO, thereby improving male function;

(3) Oyster peptide can increase the levels of hemoglobin and blood testosterone,

promote the inhibition of StAR mRNA expression, thereby promoting the production

of testosterone; in addition, oyster peptide has a certain antioxidant effect, which has

obvious scavenging effects on these three free radicals, i.e.

1,1-diphenyl-2-trinitrophenylhydrazine (DPPH•), hydroxyl radical (•OH) and

superoxide anion (02-), and can improve body fatigue;

(4) Epimedium extract is rich in icariin, volatile oil, wax alcohol, phytosterol, tannin,

vitamin E and other ingredients, which can increase the body's androgen levels,

increase the contents of hypothalamic monoamine neurotransmitter DA and 5-HT,

improve the structure of penile erectile tissue, increase the content of eNOS in corpus

cavernosum, and reduce the content of ET-1.

The composition for improving male function provided by the present application is

reasonable in terms of its formula, has proper compatibility, is convenient to use,

has good absorption effect, but has no adverse effects or toxic side effects, and it has a significant effect on improving male functions.

Detailed Description of the Application

The technical solutions of the present application will be clearly and completely

described below in conjunction with specific embodiments. Obviously, the described

embodiments are only a part of the embodiments of the present application, rather

than all the embodiments. Based on the embodiments of the present application, all

other embodiments obtained by those skilled in the art without creative work should

fall within the protection scope of the present application

Example

20 parts of NADH, 100 parts of epimedium extract, and 80 parts of L-arginine were

respectively passed through a 60-80 mesh sieve, and then mixed in a mixer at 20r/min

for 20 minutes to obtain a first component; excipients glutamine, black ginger extract,

mannitol, microcrystalline cellulose, sodium bicarbonate, sodium vitamin C, and

magnesium stearate were respectively passed through a 60-80 mesh sieve, and then

put into the mixer containing the first component and mixed at 20r/min for 40 minutes,

and then discharged and tableted to obtain Composition 1.

180 parts of NMN, 50 parts of oyster peptide, and 120 parts of L-arginine were

for 20 minutes to obtain a first component; excipients taurine, zinc citrate, magnesium

oxide, erythritol, and silicon dioxide were respectively passed through a 60-80 mesh

sieve, and then put into the mixer containing the first component and mixed at

20r/min for 40 minutes, and then discharged and tableted to obtain Composition 2.

Experimental Example

36-38g Kunming mice from Shanghai Experimental Animal Center, with 40 females

and 20 males, were purchased. Viagra (sildenafil citrate), produced by Pfizer

Pharmaceuticals. Estradiol valerate, produced by DELPHARM Lille S.A.S., France,

and subpackaged by Bayer Healthcare Co., Ltd. Guangzhou Branch. Progesterone

injection, produced by Zhejiang Xianju Pharmaceutical Co., Ltd. Sodium

nitroprusside (sodium nitrosoferricyanide, SNP) was purchased from Sigma. cGMP

determination kit was purchased from Abcam, and NO determination kit was provided

by Nanjing Jiancheng Institute of Bioengineering.

Male mice were randomly divided into 4 groups according to body weight: blank

control group, positive drug control group, Composition 1 group and Composition 2

group, with 5 in each group. The blank control group was given distilled water 2mg/d

(given general diet); the positive drug control group was given Viagra 5mg/kg/d; the

Composition 1 and 2 groups were given the Composition 1~2 10mg/kg/d, respectively.

The mice in the above groups were given intragastric administration for 7 days

continuously, and 0.5h after the last administration, the sexual behavior was observed.

Before performing the sexual behavior observation experiment, the female mice were

placed in the male mice mating box to adapt to the environment every day, and trained

for 10-15 minutes until the male mice have a stable mating response. 48h before the

formal experiment, female mice were given estradiol valerate 0.03mg/mouse, and

then 4h before the formal experiment injected with progesterone injection

50ug/mouse.

1. Observation of sexual behavior

The observation time of the experiment was from 19:00 to 24:00 at night. The room

was kept quiet and the experiment was carried out under red dim light. The female

mice in estrus were placed in the male mice mating box, and the number of female

mice was twice the number of male mice. The sexual behavior of male mice was

observed, namely the straddling number and straddling time. The results are shown in

Table 1. Compared with the blank control group, both the Compositions 1 and 2

groups can effectively increase the straddling numbers and straddling time of the

mice.

Table 1 Comparison of sexual behavior of mice ( x SEM, n=5)

Groups N Straddling number Straddling time (s)

(times)

Blank control group 5 2.12±0.89 222.09± 8.45

Positive drug control 5 5.98 ± 1.22 476.83 ± 10.57

group

Composition 1 group 5 4.25 ±0.76 397.09 7.51

Composition 2 group 5 3.67 ±0.45 356.84 9.02

*P<0.05

2. Effect on relaxation of corpus cavernosum

It has been confirmed that there are three mechanisms involved in the regulation of

the spiral artery tension in the posterior corpus cavernosum, namely, adrenergic,

cholinergic and non-adrenergic, non-cholinergic (NANC). The latter is considered to

be the main mechanism of relaxation of corpus cavernosum vascular smooth muscle.

NO is a neural mediator of NANC. NO acts on guanosine cyclase (GC) to form a

NO-GC complex, and binds to the porphyrin site of the enzyme, resulting in

configuration change and activation of GC, thereby causing the massive formation of

cGMP in cells, which is the NO-cGMP pathway closely related to genital erectile

function.

10 umol/L SNP (sodium nitroprusside) and isolated corpus cavernosum with

destroyed endothelium were incubated at 37°C for 1 hour to stimulate the corpus

cavernosum to produce cGMP. The results are shown in Table 2. Compared with the

blank control group, the cGMP in the Compositions 1 and 2 groups was significantly increased, which proved that the composition of the present application has an activating effect on nitric oxide synthase.

Table 2 Effects of NADH and/or NMN on NO release and cGMP accumulation in

mouse corpus cavernosum tissue

Groups NO (umol/g protain) cGMP (umol/g) n

Blank control group 18.43 ±4.78 63.25 ± 11.34 5

Positive drug control 66.76 ±7.56 525.25 ±29.01 5

group

Composition 1 group 36.86 ±4.03 134.87 ±21.66 5

Composition 2 group 28.47 ± 3.02 101.43 ± 18.78 5

Means, *P<0.05

The above are only preferred embodiments of the present application. It should be

pointed out that for those skilled in the art, several improvements and modifications

can be made without departing from the principle of the present application, these

improvements and modifications should also be regarded as the protection scope of

the present application.

Claims

1. A composition for improving male function, wherein the composition comprises

NR derivative and L-arginine.

2. The composition according to claim 1, wherein the NR derivative is NMN or

NADH.

3. The composition according to claim 2, wherein when the NR derivative is NMN,

the composition further comprises oyster peptide.

4. The composition according to claim 2, wherein when the NR derivative is NADH,

the composition further comprises epimedium extract.

5. The composition according to claim 3, comprising 150 to 220 parts by weight of

NMN, 100 to 150 parts by weight of L-arginine and 30 to 80 parts by weight of oyster

peptide.

6. The composition according to claim 5, comprising 160 to 200 parts by weight of

NMN, 110 to 130 parts by weight of L-arginine and 40 to 55 parts by weight of oyster

peptide.

7. The composition according to claim 4, comprising 10 to 30 parts by weight of

NADH, 40 to 80 parts by weight of L-arginine and 80 to 120 parts by weight of

epimedium extract.

8. The composition according to claim 7, comprising 25 to 30 parts by weight of

NADH, 50 to 70 parts by weight of L-arginine and 90 to 110 parts by weight of

epimedium extract.

9. Use of the composition according to any one of claims 1-8 in improving male

function.