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CN1795868A - Medication possessing activity of fighting against senium - Google Patents

Medication possessing activity of fighting against senium Download PDF

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Publication number
CN1795868A
CN1795868A CNA2004101004542A CN200410100454A CN1795868A CN 1795868 A CN1795868 A CN 1795868A CN A2004101004542 A CNA2004101004542 A CN A2004101004542A CN 200410100454 A CN200410100454 A CN 200410100454A CN 1795868 A CN1795868 A CN 1795868A
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ginsenosides
polarity
low
aging
ginsenoside
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杨凌
刘勇
何克江
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Dalian Institute of Chemical Physics of CAS
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Dalian Institute of Chemical Physics of CAS
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Abstract

本发明涉及具有抗衰老活性的药物，为一种或多种在20位碳上无糖基的低极性人参皂苷，具有拮抗性激素降解、提高性激素血浆水平的活性，从而发挥抗衰老的功效。该类低极性人参皂苷可以是天然或化学合成的前体化合物或衍生物经过口服后的胃酸或/和肠道菌等转化后产生的。本发明为男性PADAM和女性更年期早期提供了一种更为安全有效治疗方法。可单独使用，发挥其抗衰老的疗效，也可与目前市场上用于抗衰老的激素类和抑制前列腺增生的药物制成复方制剂，可在保持疗效的同时，减少激素类药物的用量，降低了性激素替代疗法的副作用。本发明既可应用于药物，也可开发成保健品，有广阔的应用前景。The invention relates to a drug with anti-aging activity, which is one or more low-polarity ginsenosides without sugar groups on the 20th carbon, which has the activity of antagonizing the degradation of sex hormones and increasing the plasma level of sex hormones, thereby exerting anti-aging effects. Such low-polarity ginsenosides can be produced by transformation of natural or chemically synthesized precursor compounds or derivatives by gastric acid or/and intestinal bacteria after oral administration. The invention provides a safer and more effective treatment method for male PADAM and early female menopause. It can be used alone to exert its anti-aging effect, and it can also be made into a compound preparation with anti-aging hormones and drugs for inhibiting benign prostatic hyperplasia on the market, which can reduce the dosage of hormone drugs while maintaining the curative effect. Side effects of sex hormone replacement therapy. The invention can be applied to medicines and can also be developed into health care products, and has broad application prospects.

Description

Medicine with activity of fighting against senium
Technical field:
The present invention relates to have the medicine of activity of fighting against senium, particularly relate to the listed low polarity ginsenoside of table 1.Described low polarity ginsenoside structurally all belongs to the ginsenoside of sugar based on 20 carbon, has the degraded of antagonism gonadal hormone, improves the activity of gonadal hormone blood plasma level, thereby bring into play antidotal effect.
Background technology:
Radix Ginseng is medicinal in the history in existing thousands of years of China, it has multiple physiology and pharmacological action, as antitumor, enhance immunity, microcirculation improvement, steadily blood pressure, blood sugar regulation, blood fat reducing, calm the nerves, defying age, antitonic, adjusting digestive function, prevention of digestive tract ulcers, raising quality of life, hypermnesis and learning capacity etc.But for many years, it is not clear that the multiple pharmacologically active of Radix Ginseng faces effective ingredient always, the query that mechanism is unclear.
Generally acknowledge that at present the ginsenoside is the effective ingredient of Radix Ginseng, still, the natural ginseng saponin is water soluble compound, by the ability extreme difference of intestinal absorption, is difficult to into blood performance drug action.The medicinal forms of Radix Ginseng has bright ginseng, Radix Ginseng and Radix Ginseng Rubra, and three's relation is that bright ginseng obtains Radix Ginseng through the room temperature drying, and is Radix Ginseng Rubra through steaming after drying.Use experience and study of pharmacy show that the drug effect of Radix Ginseng Rubra is higher than Radix Ginseng and bright ginseng.Unique drug effect of modern study proof Radix Ginseng Rubra has benefited from wherein containing distinctive Rg 2, Rg 3, Rh class, Rk class and natural trace such as polyacetylene compound such as Panaxynol or rare composition.In addition, foreign study finds that natural ginseng saponin intestinal metabolite is the real pharmacological component of Radix Ginseng.
In mid-aged population, with advancing age, in various degree unusual all easily takes place in all links of human hypothalamic-hypophysis-gonad axis, and man's testosterone takes place and partly lacks (partical androgendeficiency in aging male, PADAM in the male.Sometimes also claim the male menopause, andropause or malemenopause) syndrome, women's generation climacteric syndrome.Male PADAM and Women all are because of due to free serum gonadal hormone (testosterone or estrogen) level descends significantly.Old people's free serum gonadal hormone (testosterone or estrogen) level drops to due to the three big reasons significantly: the secretion of (1) gonadal hormone after 50 years old obviously descends, and especially reaches floor level in 70 years old later on; (2) serum sex hormone binding protein (SHBG) level progressively increased with the age, Zong cause the fall of the fall of free gonadal hormone greater than testosterone; (3) old people's liver CYP450 enzyme is significantly higher than young and middle-aged people, causes gonadal hormone catabolism to be strengthened, and has strengthened the fall of free gonadal hormone.
At present, male PADAM and Women mainly adopt the gonadal hormone alternative medicine.The gonadal hormone alternative medicine has the defective of itself: treatment may cause erythrocytosis and sleep apnea syndrome as testosterone, and this old man to the heart reservation function reduction can cause damage.Report is arranged, and testosterone increases benign prostatic hyperplasia (benign prostatic hyperplasia) and risk of prostate cancer; Estrin treatment significantly increases the sickness rate of women's heart disease, apoplexy, blood clot and breast carcinoma.Even more serious is to adopt the gonadal hormone alternative medicine in early days at male PADAM and Women, will speed up the dysregulation of hypothalamic pituitary gonadal axis, causes vicious cycle.
The technology contents of invention:
The present invention aims to provide the medicine with activity of fighting against senium, for male PADAM and Women provide a kind of safer effective Therapeutic Method in early days.Such has the low polarity ginsenoside of the medicine of activity of fighting against senium for one or more sugar based on 20 carbon, activity with the degraded of antagonism gonadal hormone, raising gonadal hormone blood plasma level, the hormone that is promoted is brought into play direct anti-aging effects on the one hand, form the vicious cycle of negative feedback blocking-up hypothalamic pituitary gonadal axis dysregulation on the one hand, thereby bring into play antidotal effect.
Described low polarity ginsenoside comprises one or more of the low polarity ginsenoside that lists in the table 1:
Table 1 has the low polarity ginsenoside of activity of fighting against senium
Grouping Low polarity ginsenoside
The triol group I PPT II PT，Δ 20(21)-PPT，Δ 20(22)-PPT III 20-(R)-Rg 2，20-(S)-Rg 2，20-(R)-Rh 1，20-(S)-Rh 1 IV Rg 6、Rk 3、Rs 7，F 4、Rh 4、Rs 6
The glycol group I PPD II PD，Δ 20(21)-PPD，Δ 20(22)-PPD III 20-(R)-Rg 3、20-(S)-Rg 3、20-(R)-Rh 2And 20-(S)-Rh 2 IV Rk 1，Rk 2，Rs 5，Rg 5，Rh 3，Rs 4
Its chemical structural formula is:
Ginsenoside R R’ R”
Diol type Triol type (20S)Rb 1 (20S)Rb 2 (20S)Rb 3 (20S)Rc (20S)Rd (20S，R)Rg 3 (20S，R)Rh 2 (20S，R)Rs 3 C-K C-Y Mx Mc PPD (20S)Re (20S)Rg 1 (20S，R)Rg 2 (20S)Rf (20S，R)Rh 1 PPT O-Glc 2- 1Glc O-Glc 2- 1Glc O-Glc 2- 1Glc O-Glc 2- 1Glc O-Glc 2- 1Glc O-Glc 2- 1Glc O-Glc O-Glc 2- 1Glc-Ac OH OH OH OH OH OH OH OH OH OH OH H H H H H H H H H H H H H O-Glc 2- 1Rha O-Glc O-Glc 2- 1Rha O-Glc 2- 1Glc O-Glc OH O-Glc 6- 1Glc O-Glc 6- 1Arap O-Glc 6- 1Xyl O-Glc 6- 1Araf O-Glc OH OH OH O-Glc O-Glc 6- 1Arap O-Glc 6- 1Xyl O-Glc 6- 1Araf OH O-Glc O-Glc OH O-Glc OH OH
Glc：β-D-glucopyranosyl；Arap：α-L-arabinopyranosyl；
Xyl：β-D-xylopyranosyl；Araf：α-D-arabinofuranosyl；
Rha：-L-rhamnopyranosyl；Ac：6’-O-Acetyl.
Ginsenoside R R’ Ginsenoside R R’
Diol Type Triol Type Rg 5 Rh 3 Rs 4 Δ 20(22)-PPD F 4 Rh 4 Rs 6 Δ 20(22)-PPT O-Glc 2- 1Glc O-Glc O-Glc 2- 1Glc-Ac OH OH OH H H H O-Glc 2- 1Rha O-Glc O-Glc-Ac Rk 1 Rk 2 Rs 5 Δ 20(21)-PPD Rg 6 Rk 3 Rs 7 Δ 20(21)-PPT O-Glc 2- 1Glc O-Glc O-Glc 2- 1Glc-Ac OH OH OH H H H O-Glc 2- 1Rha O-Glc O-Glc-Ac
The present invention has in the medicine of activity of fighting against senium, and the gastric acid after precursor compound that described low polarity ginsenoside can be natural or chemosynthesis or derivant process are oral is or/and intestinal etc. transform the back generation.
The present invention has in the medicine of activity of fighting against senium, and anti-aging effects can realize that dosage is counted 1-50mg/Kg/ days with total low polarity ginsenoside by using one or more low polarity ginsenosides.
The present invention has in the medicine of activity of fighting against senium, and low polarity ginsenoside can make the preparation of various pharmaceutical dosage forms with any officinal with compounding ingredient and excipient.
The present invention has in the medicine of activity of fighting against senium, low polarity ginsenoside can use separately, also can make compound preparation with the medicine (as testosterone 5 alpha reductase inhibitors) that is used for antidotal hormones (as testosterone or estrogen) and inhibition prostatic hyperplasia in the market.
The present invention has in the medicine of activity of fighting against senium, and described dosage form is any of oral, injection or local application's dosage form.
The present invention has in the medicine of activity of fighting against senium, and peroral dosage form can be tablet, powder, suspension, emulsion, capsule, granule, coated tablet, pill, liquid, spirit, syrup or limonada etc.
The present invention has in the medicine of activity of fighting against senium, and injection type can be water preparation, suspension or liposome solutions etc.
The present invention has in the medicine of activity of fighting against senium, and local application's dosage form can be ointment, solid, suspension, water preparation, spirit, powder, paste, suppository, aerosol, paste, liniment, lotion, enema or Emulsion etc.
The present invention has in the medicine of activity of fighting against senium, excipient can be one or more in following: (a) the powdery excipient of peroral dosage form such as lactose, crystalline cellulose, starch, dextrin, calcium phosphate, calcium carbonate, synthetic or natural aluminium dioxide, exsiccant aluminium hydroxide, magnesium stearate, sodium bicarbonate and surfactant such as phospholipid, cholic acid, Cremorphor, polysorbate (Tween) 80, Pluronic L64 and poloxamor etc.; (b) the powdery excipient of local application's dosage form such as zinc oxide, Talcum, starch, high potter's clay, borate powder, zinc stearate, magnesium stearate, magnesium carbonate, winnofil, bismuth subgallate, aluminum potassium sulfate powder and surfactant such as phospholipid, cholic acid, Cremorphor, polysorbate (Tween) 80, PluronicL64 and poloxamor or the like; (c) liquid usefulness excipient such as water, glycerol, propylene glycol, sweet taste syrup, ethanol, fatty oil, Ethylene Glycol, Polyethylene Glycol, sorbitol; The ointment excipient, as mixing-in fat, fatty oil, lanoline, vaseline, glycerol, wax, Japan wax, paraffin, sulphuric acid paraffin, resin, higher alcohol, plastics, ethylene glycol, water or surfactant (comprise liposoluble base, water-soluble base and the base that suspends, as with surfactant such as phospholipid, cholic acid, Cremorphor, polysorbate (Tween) 80, Pluronic L64 and poloxamor) etc.
Low polarity ginsenoside provided by the present invention, its CYP 450 enzymatic activitys suppress to be characterised in that:
(1) only has that the low polarity Radix Ginseng soap barrack furniture of sugar based has inhibitory action on 20 carbon;
(2) inhibition strength and glycosyl quantity are inversely proportional to;
(3) triol type ginsenoside's inhibitory action is greater than the diol type ginsenoside.
The antidotal effective ingredient and the defying age mechanism thereof of Radix Ginseng that the present invention is clear and definite provides the low polarity ginsenoside with activity of fighting against senium, for male PADAM and Women provide a kind of safer effective Therapeutic Method in early days.Such low polarity ginsenoside has the degraded of antagonism gonadal hormone, improves the activity of gonadal hormone blood plasma level, thereby brings into play antidotal effect.
The specific embodiment:
Embodiment 1 Protopanaxatriol is to serum androgen level affects
A), method: with the male mice is laboratory animal, the animal model of stress method making the low-level testosterone of blood plasma with suspention, vein gives various dose PPT, and testosterone concentration is to investigate the influence of chemical compound to androgen level in the serum in the radioimmunoassay detection serum.
B), experimental result: as shown in table 2:
Table 2.PPT is to the influence of level of serum testosterone
Group n Testosterone concentration in the serum (pmol/L)
The low-level testosterone group of normal control group PPT 5mg/kg PPT 10mg/kg PPT 20mg/kg 12 10 12 11 12 3341.1±1182.2 ** 1130.2±414.8 ## 1457.2±662.6 ## 2349.1±975.3 #，* 3058.2±987.6 **
#: with matched group ratio, P＜0.05; ##: with matched group ratio, P＜0.01
*: with low-level testosterone group ratio, P＜0.05; *: with low-level testosterone group ratio, P＜0.01
The result shows that PPT can significantly improve testosterone levels in the blood, and improves the standard and be directly proportional with dosage.
Embodiment 2 each prescription are to the serum androgen level affects
A), method: with the male mice is laboratory animal, the animal model of stress method making the low-level testosterone of blood plasma with suspention, give the different prescriptions of ginsenoside and testosterone, testosterone concentration is to investigate the influence of chemical compound to sex hormone level in the serum in the radioimmunoassay detection serum.
B), experimental result: as shown in table 3:
Each prescription of table 3. is to the influence of level of serum testosterone
Group n Testosterone concentration in the serum (pmol/L)
The low-level testosterone group of normal control group PPT 20mg/kg testosterone 5mg/kg 12 10 12 12 3341.1±1182.2 ** 1130.2±414.8 ## 3058.2±987.6 ** 2131.4±848.6 ##，**
PPT 10mg/kg+ testosterone 5mg/kg PT 20mg/kg Rh 1 20mg/kg Rh 2 20mg/kg Rg 2 20mg/kg PD 20mg/kg PPD 20mg/kg F 4 20mg/kg RK 1 20mg/kg Rb 1，Rb 2, the prescription of Rc (2: 2: 1) 20mg/kg 11 12 12 11 12 12 12 11 12 11 2844.3±1025.1 ** 2451.6±978.2 #，** 2113.5±691.1 ##，* 2071.2±775.2 ##，* 1964.8±579.4 ##，* 2295.1±814.4 ##，** 2746.2±1010.3 ** 1691.7±439.7 ##，* 1624.4±516.3 ##，* 1304.5±496.8 ##
#: with matched group ratio, P＜0.05; ##: with matched group ratio, P＜0.01
*: with low-level testosterone group ratio, P＜0.05; *: with low-level testosterone group ratio, P＜0.01
The result shows, the multiple rudimentary property ginsenoside of intravenously administrable can the antagonism male hormone metabolism, improve the androgen blood plasma level, and its effect is PPT＞PPD＞PT＞PD＞Rh in proper order 1＞Rh 2＞Rg 2＞F 4＞RK 1And natural ginseng saponin Rb 1, Rb 2, Rc is that main prescription does not have this activity.
Embodiment 3 Protopanaxatriols influence the serum estrogen level
A), method: with the female mice is laboratory animal, make the low-level estrogenic animal model of blood plasma with the removal ovary method, vein gives various dose PPT, and estradiol and progesterone concentration are to investigate the influence of chemical compound to estrogen level in the serum in the radioimmunoassay detection serum.
B), experimental result: as shown in table 4:
Table 4.PPT is to the influence of serum estrogen level
Group n Estradiol concentration in the serum (pg/ml) Progesterone concentration (ng/ml) in the serum
Normal control group castration group PPT 5mg/kg PPT 10mg/kg PPT 20mg/kg 12 12 12 11 12 44.9±3.2 ** ＜20 ## ＜20 ## 24.3±1.9 ##，* 39.7±2.4 ** 5.9±1.2 ** 1.5±0.2 ## 1.9±0.6 ## 3.8±1.0 #，* 5.5±3.2 **
#: with matched group ratio, P＜0.05; ##: with matched group ratio, P＜0.01
*: with castration group ratio, P＜0.05; *: with castration group ratio, P＜0.01
The result shows that PPT can significantly improve estradiol and progesterone level in the blood, and improves the standard and be directly proportional with dosage.
Embodiment 4 each prescription influence the serum estrogen level
A), method: with the female mice is laboratory animal, make the low-level estrogenic animal model of blood plasma with the removal ovary method, give the different prescriptions of ginsenoside and estradiol, estradiol and progesterone concentration are to investigate the influence of chemical compound to estrogen level in the serum in the radioimmunoassay detection serum.
B), experimental result: as shown in table 5:
Each prescription of table 5. is to the influence of serum estrogen level
Group n Estradiol concentration in the serum (pg/ml) Progesterone concentration (ng/ml) in the serum
Normal control group castration group PPT 20mg/kg estradiol 0.5mg/kg PPT 10mg/kg+ estradiol 0.5mg/kg PT 20mg/kg Rh1 20mg/kg Rh 2 20mg/kg Rg 2 20mg/kg PD 20mg/kg PPD 20mg/kg F 4 20mg/kg RK 1 20mg/kg Rb 1，Rb 2, the prescription of Rc (2: 2: 1) 20mg/kg 12 12 12 12 12 12 11 12 12 12 12 11 12 12 44.9±3.2 ** ＜20 ## 39.7±2.4 ** 28.6±1.8 ##，* 37.4±3.6 #，** 29.9±2.5 ##，* 25.4±2.1 ##，* 26.8±2.1 ##，* 22.1±1.7 ##，* 30.4±2.5 ##，* 37.5±3.1 ** ＜20 ## ＜20 ## ＜20 ## 5.9±1.2 ** 1.5±0.2 ## 5.5±3.2 ** 3.8±1.4 #，* 5.2±2.7 ** 4.2±1.5 #，* 2.3±0.8 ## 2.6±1.0 ## 1.9±0.2 ## 4.4±1.9 #，* 5.3±2.8 ** 1.9±0.4 ## 1.7±0.2 ## 1.7±0.3 ##
#: with matched group ratio, P＜0.05; ##: with matched group ratio, P＜0.01
*: with castration group ratio, P＜0.05; *: with castration group ratio, P＜0.01
The result shows, the multiple rudimentary property ginsenoside of intravenously administrable can the antagonism estrogen metabolism, improve the estrogen blood plasma level, and its effect is PPT＞PPD＞PD＞PT＞Rh in proper order 2＞Rh 1＞Rg 2＞F 4＞RK 1And natural ginseng saponin Rb 1, Rb 2, Rc is that main prescription does not have this activity.
It is active that embodiment 5CYP450 suppresses
A), method: be experimental system with rat liver microsomes, people's hepatomicrosome and recombined human CYP3A4 respectively, the activity of indicating CYP3A with testosterone 6 beta-hydroxy reactions, (S-Rg3 is 1 μ M to add 100 μ M ginsenosides, PT and PPT are 20 μ M) detect it to the active inhibition of CYP3A, the special inhibitor ketoconazole (KTZ) of CYP3A is as positive control, 37 ℃ were reacted 10 minutes, and HPLC detects.
B), experimental result: as shown in table 6.
Table 6. ginsenoside is to the inhibitory action of CYP3A
CYP3A activity (%)
Rat liver microsomes People's hepatomicrosome Recombined human CYP3A4
Control group Rb1 Rb2 Rc Rd R-Rg3 S-Rg3 Rh2 C-K PPD Re Rg1 Rg2 Rh1 PT PPT 100.0±1.7 104.9±1.0 89.0±1.8 93.7±1.3 86.3±3.0 102.9±1.2 8.6±1.1 * 53.5±1.4 * 107.0±2.8 31.6±2.0 * 95.9±1.5 96.4±5.0 70.6±7.2 * 62.0±2.3 * 14.2±1.0 * 19.4±3.1 * 100.0±2.5 106.0±2.9 90.6±2.6 92.9±4.1 41.2±1.6 * 104.1±2.1 10.1±3.4 * 42.8±4.5 * 105.0±4.4 13.8±1.8 * 105.0±1.1 99.7±1.3 75.5±5.3 * 37.2±4.3 * 31.2±1.5 * 9.0±1.7 * 100.0±3.6 117.9±2.0 * 101.7±7.2 107.5±2.5 24.4±1.0 * 101.2±1.6 17.7±2.9 * 22.5±1.0 * 98.1±4.1 36.5±1.0 * 110.6±5.6 111.1±4.0 9.9±1.9 * 38.4±1.6 * 7.8±1.8 * 20.1±1.4 *
F 4 RK 1 KTZ 87.1±2.9 91.2±3.2 39.9±0.8 * 80.2±1.6 * 82.1±2.3 * 5.3±1.1 * 72.4±2.0 * 85.5±2.1 * 9.5±1.6 *
*: with matched group ratio, P＜0.01
The result shows, ginsenoside Rd, S-Rg 3, Rh 2, PPD, Rg 2, Rh 1, PT, PPT, F 4, RK 1CYP3A there is inhibitory action.

Claims (10)

1、一种具有抗衰老活性的药物，其特征在于：所述药物为一种或多种在20位碳上无糖基的低极性人参皂苷，具有拮抗性激素降解、提高性激素血浆水平的活性。1. A drug with anti-aging activity, characterized in that: the drug is one or more low-polarity ginsenosides without sugar groups on the 20th carbon, which has the activity of antagonizing the degradation of sex hormones and increasing the plasma level of sex hormones . 2、按照权利要求1所述具有抗衰老活性的药物，其特征在于：所述的低极性人参皂苷包括以下低极性人参皂苷的一种或多种：2. The medicine with anti-aging activity according to claim 1, characterized in that: said low-polarity ginsenosides include one or more of the following low-polarity ginsenosides: (1)三醇型人参皂苷苷元(1) Triol type ginsenoside aglycone 原人参三醇(protopanaxatriol，PPT)；Protopanaxatriol (PPT); (2)三醇型人参皂苷苷元衍生物(2) Triol type ginsenoside aglycon derivatives 人参三醇(panaxatriol，PT)；Panaxatriol (PT); 3β，6α，12β-三羟-20(21)，24(25)-二烯-达玛烷[dammar-3β，6α，12β-trihydroxyl-20(21)，24(25)-diene，简称Δ20(21)-PPT]；3β, 6α, 12β-trihydroxyl-20(21), 24(25)-diene-dammarane [dammar-3β, 6α, 12β-trihydroxyl-20(21), 24(25)-diene, referred to as Δ 20(21) -PPT]; 3β，6α，12β-三羟-20(22)，24(25)-二烯-达玛烷[dammar-3β，6α，12β-trihydroxyl-20(22)，24(25)-diene，简称Δ20(22)-PPT]；3β, 6α, 12β-trihydroxyl-20(22), 24(25)-diene-dammarane [dammar-3β, 6α, 12β-trihydroxyl-20(22), 24(25)-diene, referred to as Δ 20(22) -PPT]; (3)20位羟基游离的三醇型人参皂苷(3) Triol-type ginsenoside with free hydroxyl group at the 20th position 20-(R)-Rg2、20-(S)-Rg2、20-(R)-Rh1和20-(S)-Rh1；20-(R)-Rg 2 , 20-(S)-Rg 2 , 20-(R)-Rh 1 and 20-(S)-Rh 1 ; (4)20位烯键的三醇型人参皂苷(4) Triol-type ginsenosides with 20-position ethylenic bond Δ20(21)-三醇型人参皂苷：Rg6、Rk3、Rs7；Δ 20(21) -triol type ginsenosides: Rg 6 , Rk 3 , Rs 7 ; Δ20(22)-三醇型人参皂苷：F4、Rh4、Rs6；Δ 20(22) -triol type ginsenosides: F 4 , Rh 4 , Rs 6 ; (5)二醇型人参皂苷苷元(5) Diol type ginsenoside aglycone 原人参二醇(protopanaxadiol，PPD)；Protopanaxadiol (PPD); (6)二醇型人参皂苷苷元衍生物(6) Diol type ginsenoside aglycon derivatives 人参二醇(panaxadiol，PD)；Panaxadiol (PD); 3β，12β-二羟-20(21)，24(25)-二烯-达玛烷[dammar-3β，12β-dihydroxyl-20(21)，24(25)-diene，简称Δ20(21)-PPD]；3β, 12β-dihydroxyl-20(21), 24(25)-diene-dammarane [dammar-3β, 12β-dihydroxyl-20(21), 24(25)-diene, referred to as Δ 20(21) -PPD]; 3β，12β-二羟-20(22)，24(25)-二烯-达玛烷[dammar-3β，12β-dihydroxyl-20(22)，24(25)-diene，简称Δ20(22)-PPD]；3β, 12β-dihydroxyl-20(22), 24(25)-diene-dammarane [dammar-3β, 12β-dihydroxyl-20(22), 24(25)-diene, referred to as Δ 20(22) -PPD]; (7)20位羟基游离的二醇型人参皂苷(7) Diol-type ginsenoside with free hydroxyl group at the 20th position 人参皂苷20-(R)-Rg3、20-(S)-Rg3、20-(R)-Rh2和20-(S)-Rh2；Ginsenosides 20-(R)-Rg 3 , 20-(S)-Rg 3 , 20-(R)-Rh 2 and 20-(S)-Rh 2 ; (8)20位烯键的二醇型人参皂苷(8) Diol type ginsenosides with 20 ethylenic bonds Δ20(21)-二醇型人参皂苷：Rk1、Rk2、Rs5；Δ 20(21) -diol type ginsenosides: Rk 1 , Rk 2 , Rs 5 ; Δ20(22)-二醇型人参皂苷：Rg5、Rh3、Rs4。Δ 20(22) -diol type ginsenosides: Rg 5 , Rh 3 , Rs 4 . 3、按照权利要求1和2所述具有抗衰老活性的药物，其特征在于：所述低极性人参皂苷是天然或化学合成的前体化合物或衍生物经过口服后在胃酸或/和肠道菌作用下转化产生的。3. The drug with anti-aging activity according to claims 1 and 2, characterized in that: said low-polarity ginsenosides are natural or chemically synthesized precursor compounds or derivatives that are released in gastric acid or/and intestinal tract after oral administration. Transformed by bacteria. 4、按照权利要求1和2所述具有抗衰老活性的药物，其特征在于：所述的低极性人参皂苷，剂量以总低极性人参皂苷计为1-50mg/Kg/天。4. The drug with anti-aging activity according to claims 1 and 2, characterized in that the dosage of said low-polarity ginsenosides is 1-50 mg/Kg/day based on total low-polarity ginsenosides. 5、按照权利要求1和2所述具有抗衰老活性的药物，其特征在于：所述低极性人参皂苷与任何法定药用配合剂和赋形剂制成各种药用剂型的制剂。5. The drug with anti-aging activity according to claims 1 and 2, characterized in that the low-polarity ginsenoside is prepared into various pharmaceutical dosage forms with any legal pharmaceutical compounding agents and excipients. 6、按照权利要求5所述具有抗衰老活性的药物，其特征在于：所述低极性人参皂苷与目前市场上用于抗衰老的激素类和抑制前列腺增生的药物制成复方制剂。6. The drug with anti-aging activity according to claim 5, characterized in that: the low-polarity ginsenoside is prepared into a compound preparation with anti-aging hormones and drugs for inhibiting benign prostatic hyperplasia currently on the market. 7、按照权利要求6所述具有抗衰老活性的药物，其特征在于：所述剂型为口服、注射或局部用药剂型的任何一种。7. The drug with anti-aging activity according to claim 6, wherein the dosage form is any one of oral, injection or topical dosage form. 8、按照权利要求6所述具有抗衰老活性的药物，其特征在于：所述口服剂型包括片剂、粉剂、悬浊液、乳浊液、胶囊、颗粒剂、糖衣片、药丸、液体、醑剂、糖浆、柠檬水剂。8. According to claim 6, the medicine with anti-aging activity is characterized in that: said oral dosage forms include tablets, powders, suspensions, emulsions, capsules, granules, sugar-coated tablets, pills, liquids, spirits Elixir, Syrup, Lemonade. 9、按照权利要求6所述具有抗衰老活性的药物，其特征在于：所述注射剂型包括水剂、悬浊液、脂质体溶液。9. The medicine with anti-aging activity according to claim 6, characterized in that: said injection dosage forms include water, suspension and liposome solution. 10、按照权利要求6所述具有抗衰老活性的药物，其特征在于：所述局部用药剂型包括软膏、固体、悬浊液、水剂、醑剂、粉剂、糊剂、栓剂、气溶胶、泥敷剂、涂抹剂、洗剂、灌肠剂、乳剂。10. The medicine with anti-aging activity according to claim 6, characterized in that: said topical dosage forms include ointment, solid, suspension, water, spirit, powder, paste, suppository, aerosol, mud Dressings, smears, lotions, enemas, creams.
CNA2004101004542A 2004-12-23 2004-12-23 Medication possessing activity of fighting against senium Pending CN1795868A (en)

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Cited By (6)

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WO2008110050A1 (en) * 2007-03-12 2008-09-18 Institute Of Materia Medica, Chinese Academy Of Medical Sciences THE USE OF GINSENOSIDE Rg1, ITS METABOLITES GINSENOSIDE Rh1 AND PpT
CN102481303A (en) * 2009-06-30 2012-05-30 狮王株式会社 Sugar metabolism-improving agent and sugar metabolism-improving composition
CN103239398A (en) * 2012-02-02 2013-08-14 天马药业(集团)股份有限公司 Dammarane sapogenin suspension, and preparation method and application thereof
WO2015069086A1 (en) * 2013-11-11 2015-05-14 서울대학교산학협력단 Composition containing fraction of panax ginseng or ginsenoside separated therefrom for preventing or treating disease treated by activation of sirtuins
CN109689020A (en) * 2016-09-08 2019-04-26 株式会社爱茉莉太平洋 For skin anti-aging, composition comprising dehydroabietic acid and compound K
US11633413B2 (en) 2019-09-27 2023-04-25 Amorepacific Corporation Composition for preventing or improving menopausal symptom comprising novel ginsenoside

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013256519A (en) * 2007-03-12 2013-12-26 Inst Of Materia Medica Chinese Academy Of Medical Sciences USE OF GINSENOSIDE Rg1, ITS METABOLITES GINSENOSIDE Rh1 AND/OR Ppt
JP2010520894A (en) * 2007-03-12 2010-06-17 インスティテュート オブ マテリア メディカ， チャイニーズ アカデミー オブ メディカル サイエンスィズ Use of ginsenoside Rg1, its metabolite ginsenoside Rh1 and / or Ppt
US8765695B2 (en) 2007-03-12 2014-07-01 Jecui Health Industry Corp. Ltd. Use of ginsenoside RG1, its metabolites ginsenoside RH1 and/or PPT
WO2008110050A1 (en) * 2007-03-12 2008-09-18 Institute Of Materia Medica, Chinese Academy Of Medical Sciences THE USE OF GINSENOSIDE Rg1, ITS METABOLITES GINSENOSIDE Rh1 AND PpT
CN102481303B (en) * 2009-06-30 2013-08-14 狮王株式会社 Sugar metabolism improving agent and sugar metabolism improving composition
CN102481303A (en) * 2009-06-30 2012-05-30 狮王株式会社 Sugar metabolism-improving agent and sugar metabolism-improving composition
CN103239398A (en) * 2012-02-02 2013-08-14 天马药业(集团)股份有限公司 Dammarane sapogenin suspension, and preparation method and application thereof
CN103239398B (en) * 2012-02-02 2014-07-16 天马药业(集团)股份有限公司 Dammarane sapogenin suspension, and preparation method and application thereof
WO2015069086A1 (en) * 2013-11-11 2015-05-14 서울대학교산학협력단 Composition containing fraction of panax ginseng or ginsenoside separated therefrom for preventing or treating disease treated by activation of sirtuins
KR101548605B1 (en) * 2013-11-11 2015-09-01 서울대학교산학협력단 Compositions comprising fractions of Panax ginseng or ginsenosides isolated therefrom for prevention or treatment of disease through activation of sirtuins
CN109689020A (en) * 2016-09-08 2019-04-26 株式会社爱茉莉太平洋 For skin anti-aging, composition comprising dehydroabietic acid and compound K
CN109689020B (en) * 2016-09-08 2022-06-21 株式会社爱茉莉太平洋 Composition containing dehydroabietic acid and compound K for resisting skin aging
US11633413B2 (en) 2019-09-27 2023-04-25 Amorepacific Corporation Composition for preventing or improving menopausal symptom comprising novel ginsenoside

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