CN102000098B - The purposes of ginsenoside Rg1 - Google Patents

The purposes of ginsenoside Rg1 Download PDF

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Publication number
CN102000098B
CN102000098B CN201010543658.9A CN201010543658A CN102000098B CN 102000098 B CN102000098 B CN 102000098B CN 201010543658 A CN201010543658 A CN 201010543658A CN 102000098 B CN102000098 B CN 102000098B
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ginsenoside
purposes
cgmp
mice
spongy body
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CN102000098A (en
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张均田
王晓英
郝顺祖
黄诒森
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Institute of Materia Medica of CAMS
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Abstract

The present invention relates to the novelty teabag of ginsenoside Rg1, especially prevention or treatment male sexual disorder as erection disturbance in purposes.

Description

The purposes of ginsenoside Rg1
Invention field
The present invention relates to the novelty teabag of ginsenoside Rg1, especially prevention or treatment male sexual disorder as erection disturbance in purposes.
Background technology
Ginsenoside Rg1 is a kind ofly present in many plants as the known chemical monomer in Radix Ginseng.Its structure and be biological activities associatedly reported in relevant textbooks or delivered in document.But the purposes that ginsenoside Rg1 is preventing and/or treating male's sexual direction is not reported so far.
Summary of the invention
The present inventor now finds that ginsenoside Rg1 is by suppressing di-phosphate ester ester V (PDE after deliberation v) and improve CGMP concentration, thus promote spongy body erection function.
Therefore, first aspect present invention relates to ginsenoside Rg1 purposes in for the preparation of the product preventing and/or treating sexual dysfunction.
Further aspect of the present invention relates to the product for preventing and/or treating sexual dysfunction, and it comprises panaxoside monomer and excipient or carrier.
According to the present invention, term " sexual dysfunction " citing is said and be can be erection disturbance.
In the present invention, product list says functional food or medicine.
According to the present invention, ginsenoside Rg1 prepares by commercially available or known method.Product of the present invention is by being mixed with ginsenoside Rg1 and excipient or carrier.
Accompanying drawing explanation
Fig. 1 a straddles result for giving ginsenoside Rg1 mice.
Fig. 1 b is for giving ginsenoside Rg1 mice number of copulations.
Detailed description of the invention
The following examples are used for further illustrating the present invention, but it does not mean that any limitation of the invention.
Materials and methods
Animal
Kunming mice, 36-38g, female, hero provides by Chinese Academy of Medical Sciences's Experimental Animal Center.New zealand white rabbit, 2.5-3kg, male, provided by PLA General Hospital Experimental Animal Center.Room temperature 18-22 DEG C, illumination 12hr: 12hr (light: dark), uses prospective adaptation environment 3 days.
Reagent and preparation
Methacholine chloride (MCH), sodium nitroprusside (sodium nitroprusside, SNP) purchased from Sigma, phenylephrine hydrochloride inj (PE), Shanghai City Tian Feng pharmaceutical factory produces, DMEM is purchased from Gibco BRL company, cGMP measures test kit purchased from Chinese Atomic Energy Research Institute, panaxoside monomer Rg1, Rb1 (content > 98%), thered is provided by Norman Bethune Medical University's Organic Chemistry Laboratory, NO mensuration test kit builds up Bioengineering Research Institute by Nanjing to be provided, testosterone measures test kit purchased from Shanghai Biological Products Inst., Ministry of Public Health.All the other reagent are domestic analytical pure.Nutritional solution forms: sodium chloride 118.2, potassium chloride 2, potassium dihydrogen phosphate 0.5, calcium chloride 0.7, sodium bicarbonate 25, glucose 11.1m molL -1, compound method: CaCl 2after being baked to constant weight, be first made into the mother solution that concentration is application liquid 100 times; NaCHO 3, glucose takes before use, adds nutritional solution; The mother solution that concentration is application liquid 20 times is made into after the mixing of other compositions.Mother solution dilutes before use, adjusts PH to 7.4, passes to 95%O 2, 5%CO 2the presaturation of mixing oxygen stand-by.
Instrument and equipment
Thermostatic water-circulator bath HSZ-H, Harbin Dong Lian electronic technology development corporation, Ltd. product, tonotransducer LW-10 is purchased from Shanghai red flag instrucment and meter plant, monitor TYPE-3066 is Japanese Shimadzu Corporation product, β liquid scintillation counter LS9800 is Beckman Products, and homogenizer is purchased from LITTAU-LUZERN factory of Sweden, and refrigerated centrifuge is Japanese Shimadzu Corporation product, the visible grating spectrophotometer of 752Z, purchased from Shanghai the 3rd analytical tool factory.Tonotransducer LW-10 is purchased from Shanghai red flag instrucment and meter plant, and monitor TYPE-3066 is Japanese Shimadzu Corporation product.
Laboratory animal preparation and screening
By female KM mice with etherization, be fixed on operation plate, with 75% alcohol disinfecting, thorough excision bilateral ovaries, ligation is sewed up, after making it recover 1 week, subcutaneous injection estrogen and progestogen are promoted the sexual maturity, after it is emotionally stable, female mice is placed in male Mus covering box in 2: 1 ratios, and every day trains 10-15 minute, after treating that male Mus mating reaction is comparatively stable, according to the mating behavior number of times of continuous 5 days, male mice is divided into groups, make often to organize mice and straddle with number of copulations as far as possible close, react more weak and discard with nonresponder.
Embodiment 1 Rg1 is on the impact of mice sexual behaviour
Before experiment, mice trained, select, divide into groups, make often to organize mice sexual behaviour experience and copulation background is substantially identical, in every morning lumbar injection Rg1,10,5,25mg/kg once, female Mus is placed in male mouse cage by night, observes its sexual behaviour and namely straddles (mounting) and copulation (mating) number of times, and result proves Rg1 administration about 2 weeks, mice sexual behaviour significantly improves, and the results are shown in Figure 1a and 1b.
Embodiment 2 is on the impact of spongy body diastole effect
Confirm that three kinds of mechanism participate in the adjustment of spongy body rear screw angiosthenia, i.e. adrenergic, cholinergic and non-epinephrine, non-cholinergic (NANC), the latter is considered to the main frame mechanism of spongy body relaxing the VSM, and NO is the neurotransmitter of NANC, NO acts on bird adenosine cyclase (GC) and forms NO-GC complex, and combine with the porphyrin position of this enzyme, configuration is caused to change and activate GC, thus cGMP in cell is formed in a large number, this is the NO-cGMP path that one 5 genitals erection functions have close association, for this reason, we observe Rg1, on the impact of cGMP accumulation and NO release in spongy body diastole and spongy body.
The instrument medicine that we adopt MeCh (MCH) to discharge for endogenous NO observes Rg1 to the impact of the spongy body diastole effect that MCH mediate, and the diastole effect of result proof Rg1 to the spongy body that MCH mediates has obvious booster action, the results are shown in Table 1.
Table 1. ginsenoside Rg1 causes the impact of isolated rabbit spongy body diastole effect to MCH
Mean±s
10 μm of dSNP (sodium nitroprusside) and the in vitro spongy body that oneself smashes up endothelium are incubated 1 hour in 37 DEG C of temperature, cGMP is produced to stimulate spongy body, found that the cGMP of Rg1 group is significantly higher than matched group (table 2), prompting Rg1 has inhibitory action to phosphodiesterase (PDE).
Table 2. ginsenoside Rg1 is on the impact that mice cavernosal tissue NO discharges and IGMP gathers
Mean±s, *P<0.05, **P<0.01 vs Control
Embodiment 3
PDB5 (5 type PDE) in cyclic nucleotide phosphodiesterase (PDE) extended familys and reproductive system close relation, in the cavernosal tissue that it is mainly distributed in animal and platelet, take cGMP as specific substrate, GTP forms cGMP under GC effect, cGMP is hydrolyzed to 5 ' GMP through PDEs effect and lost efficacy, therefore suppress PDEs can make cGMP accumulation in spongy body, and then cause spongy body vasodilation, erection.
The ginsenoside that institute of materia medica of China provides, code name is: sldenafil: by DaLian, China, pfizer inc produces, lot number 25883002; 125i radioimmunity cGMp testing cassete is Amersham Products, lot number 60440504; PDE is Mark company gene recombinaton engineering product; Lot number: CA92039-2087; Produce in dimethyl sulfoxide (dimethylsmlphoxide, DMSO) Hong Sheng chemical plant; Lot number 950726.Instrument is GC-911 γ radiation immunity arithmometer (single probe, full-automatic) version number V2.1A, and Zhong Jia branch company of Creation Stock Co., Ltd of Chinese University of Science and Technology manufactures on April 16th, 2002.MTM Magnetic Isolation system system Amersham Products.
Method: according to Amersham company " ' I put exempt from testing cassete description operation.
Result
CPM Panaquilon's concentration (nmol/L) CGMP concentration (fmol/L)
4369 0 363.1 (PDE5 without inhibitors)
3711 2.5 562.2
4151 5.0 419.5
3998 10.0 464.3
3854 20.0 510.9
4158 40.0 417.5
CPM Sldenafil concentration (nmol/L) CGMP concentration (fmol/L)
3854 0 510.9 (adding degeneration PDE5)
3983 2.5 468.9
4282 5.0 384.7
4059 10.0 446.9
3931 20.0 485.3
3849 40.0 512.5
IC is calculated by logfit method 50for 7.24nmol/L, matched group sldenafil IC 50for 3.42nmol/L.
Design a pipe in experiment and add PDB5 without inhibitor, result C*MP concentration is 363.lfmol/L, another design one pipe adds degeneration PDES without inhibitor, and result cGMP concentration is 510.9fmol/L, suffices to show that rising to caused by panaquilon and sldenafil inhibitory action of cGMP concentration in experiment.Can show that panaquilon has thus suppress PDE5 effect and improve cGMP concentration, spongy body erection function be had to the facilitation of affirmative.

Claims (4)

1. ginsenoside Rg1 is for the preparation of the purposes prevented and/or treated in the product of male sexual disorder.
2. the purposes of claim 1, wherein said sexual dysfunction is erection disturbance.
3. pharmaceutical composition is for the preparation of the purposes prevented and/or treated in the product of male sexual disorder, and wherein said pharmaceutical composition comprises ginsenoside Rg1 monomer and excipient or carrier.
4. the purposes of claim 3, wherein said sexual dysfunction is erection disturbance.
CN201010543658.9A 2004-08-11 2004-08-11 The purposes of ginsenoside Rg1 Expired - Lifetime CN102000098B (en)

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CN101264096B (en) * 2007-03-12 2011-11-09 中国医学科学院药物研究所 Use of ginsenoside Rg1 in preparing spermatogenic product
US9314493B2 (en) 2007-05-28 2016-04-19 Amorepacific Corporation Method for treating vascular inflammation, improving skin beauty and improving male sexual function using ginseng berry
KR20080104600A (en) * 2007-05-28 2008-12-03 (주)아모레퍼시픽 Composition for treatment of ischemic heart disease, facilitation of blood circulation and angiogenesis

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Publication number Priority date Publication date Assignee Title
CN1353991A (en) * 2000-11-18 2002-06-19 唐修文 Ginsenoside enteric-coated tablet

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Publication number Priority date Publication date Assignee Title
CN1353991A (en) * 2000-11-18 2002-06-19 唐修文 Ginsenoside enteric-coated tablet

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
郝顺祖等.人参皂甙Rg1 对体外磷酸二酯酶5 活性的影响.《江苏大学学报(医学版)》.2004,第14卷(第1期),11-12. *

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