CN116211907A - Volatile oil and its use for treating or improving male sexual dysfunction - Google Patents
Volatile oil and its use for treating or improving male sexual dysfunction Download PDFInfo
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- CN116211907A CN116211907A CN202310026501.6A CN202310026501A CN116211907A CN 116211907 A CN116211907 A CN 116211907A CN 202310026501 A CN202310026501 A CN 202310026501A CN 116211907 A CN116211907 A CN 116211907A
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- China
- Prior art keywords
- volatile oil
- weight
- ginseng
- guaiacene
- eucalyptol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 206010057672 Male sexual dysfunction Diseases 0.000 title abstract description 12
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Abstract
The present application relates to volatile oils and their use for treating or ameliorating male sexual dysfunction. The volatile oil comprises the following components: 60-75wt% of ginseng alkynol based on the total weight of the volatile oil; and 9wt% to 15wt% of a terpenoid; and wherein the terpenoid is selected from the group consisting of amycins, β -cyclic olefins, neocaryophyllene, rhynchophylline, trans-caryophyllene, eucalyptol, elemene, calamine, α -gulene, andrographolide, eucalyptol, validol, β -sirtuin Lin Xi, champignon, longifolene, cedrene, citrus limonene, α -guaiacene, β -guaiacene, trans-nerol, and β -Ma Lanxi, and any combination thereof.
Description
Technical Field
The present application relates to the use of volatile oils, in particular essential oils derived from ginseng, for the treatment of male sexual dysfunction.
Background
Male Erectile Dysfunction (MED), also known as male erectile dysfunction, is defined as the penile erection required to fail to achieve and/or maintain satisfactory sexual activity. It is estimated that the prevalence of Erectile Dysfunction (ED) (mild, moderate and complete impotence) is 52% in men 40 to 70 years old, with a higher proportion in the population over 70 years old (Melman et al 1999). The disease has a significant negative impact on the quality of life of the individual and his partner, often resulting in increased anxiety and stress, causing depression and reduced self-esteem.
There are a number of MED therapies, of which sildenafil citrate is the better therapeutic oral drug, currently representing the most preferred therapy. However, there is also a need to find new methods of treating male sexual dysfunction, in particular MED.
The ginseng is dried root and rhizome of ginseng (panax ginseng C.A. Meyer) which is a plant of Araliaceae, is a traditional rare Chinese medicinal material, and has very high medicinal value and edible value. The ginseng has the effects of reinforcing primordial qi, restoring pulse, relieving depletion, tonifying spleen, benefiting lung, promoting fluid production, nourishing blood, soothing nerves and promoting intelligence, and is used for treating body deficiency, aphasia, limb coldness, weak spleen deficiency, anorexia, lung deficiency, asthma and cough, body fluid deficiency, thirst, internal heat diabetes, deficiency of qi and blood, deficiency of long-term illness, deficiency of both qi and blood, palpitation, insomnia, impotence and cold womb. However, ginseng is used in clinical practice in traditional Chinese medicine for oral preparation. These oral formulations are typically decocted in water and the resulting decoction is administered to the patient. Alternatively, the extract obtained after concentrating or drying the soup is prepared into syrup, pill or other solid preparation for oral administration. In this conventional manner, only the water-soluble components of ginseng are generally utilized. However, ginseng also contains volatile oil components which are poorly water-soluble or insoluble and which are dissipated during the decoction process.
Recently, researches on ginseng at home and abroad have been focused on water-soluble components (e.g., ginsenoside components and saccharide components) of ginseng, but ginseng volatile oil is not much studied due to its special properties. Therefore, the application value of the volatile oil component in ginseng is still insufficient. The existing researches show that the chemical components of ginseng volatile oil mainly comprise terpenes, alcohols, fatty acids and esters, ketones, aldehydes, phenols, heterocycles, alkanes and other compounds. Terpenes include, but are not limited to, β -patchoulene, α -farnesene, β -farnesene, amyrin, β -cyclic ene, trans-caryophyllene, neocaryophyllene, rhynchophylline, trans-caryophyllene, eucalyptol, elemene, calamine, α -ginseng, β -ginseng, α -gulene, β -gulene, α -apirene, β -apirene, γ -apirene, apigenin, andrographolide, eugenol, validol, β -sirtuin, caryophyllene, longifolene, cedrene, bergamotene, α -guaiacene, β -guaiacene, trans-nerol, β -Ma Lanxi, and the like. Alcohol compounds include, but are not limited to, ginseng neoterpene alcohol, stigmasterol, gamma-sitosterol, ginseng alkynol, ginseng epoxyalkynol, ginseng alkyndiol, ginseng alkyntriol, tertiary hexadecylthiol, campesterol, etc., wherein ginseng alkynol, ginseng epoxyalkynol, ginseng alkyndiol and ginseng alkyntriol are important compounds in the fat-soluble components of ginseng. The fatty acid and its ester compound mainly comprise oleic acid, linoleic acid, linolenic acid, stearic acid, etc. Pharmacological studies show that the ginseng volatile oil has the pharmacological effects of resisting inflammation, relieving cough and fatigue, reducing blood fat, dispelling alcohol, preventing drunk, exciting central nervous system, inhibiting tumor and the like.
There remains a need to study and develop new pharmacological actions and therapeutic uses of ginseng volatile oils.
Disclosure of Invention
The studies conducted by the inventors have revealed that the volatile oil of the present invention, particularly the volatile oil (essential oil) derived from ginseng, is effective in treating sexual dysfunction in male individuals, and has a therapeutic effect superior to that of ginseng extract extracted by conventional methods (e.g., by aqueous extraction, alcohol extraction, or aqueous alcohol extraction) and orally administered. The study also shows that the volatile oils of the invention have a good ameliorating effect on male sexual dysfunction, whether administered by the oral or (incense) inhalation route.
In one aspect, the present application provides the essential oils of the present invention.
In another aspect, the present application provides a pharmaceutical or nutraceutical composition comprising the volatile oils of the present invention.
In another aspect, the present application provides the use of the volatile oil of the present invention in the manufacture of a medicament or health care product for treating sexual dysfunction in a male individual.
In another aspect, the present application provides a method for treating or ameliorating sexual dysfunction in a male subject comprising administering to the subject an effective amount of a volatile oil, a pharmaceutical or nutraceutical composition, or a medicament or nutraceutical of the present invention.
The volatile oils of the present invention are defined below, which may be synthetic or formulated, or preferably may be derived from plants, preferably ginseng.
Brief description of the drawings
Fig. 1 shows the mating behavior of male SD rats: (A) capturing; (B) sniffing yin; (C) riding; (D) mating; and (E) licking the vagina after mating.
Detailed Description
Unless otherwise defined, technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this application belongs.
The term "volatile oil" is used interchangeably herein with "essential oil" to mean a combination or mixture of two or more volatile components, either synthetic or formulated, or extracted from a plant (e.g., flowers, leaves, stems, roots, or fruits). Methods for extraction include, but are not limited to, steam distillation, cold compaction, liposuction, and solvent extraction (e.g., CO 2 Extraction method).
In this context, the components of the volatile oil may be selected from (but are not limited to): panaxynol (CAS No. 21852-80-2), linoleic acid (CAS No. 60-33-3), sitosterol (CAS No. 83-47-6), palmitic acid (CAS No. 57-10-3), amyrene (CAS No. 25246-27-9), beta-cyclic alkene (CAS No. 28973-97-9), stigmasterol (CAS No. 83-48-7), neocaryophyllene (CAS No. 4545-68-0), rhynchophylline (CAS No. 6753-98-6), trans-caryophyllene (CAS No. 87-44-5), eucalyptol (CAS No. 6750-3), elemene (CAS No. 29873-99-2) calamine (CASNo.17334-55-3), alpha-gulene (CAS No. 489-40-7), eucalyptol (CAS No. 489-41-8), andrographolide (CAS No. 5508-58-7), validol (CAS No. 6892-80-4), beta-sirtuin Lin Xi (CAS No. 17066-67-0), gan Xiangxi (CAS No. 3242-08-8), longifolene (CAS No. 475-20-7), bergamotene (CAS No. 489-39-4), alpha-guaiacene (CAS No. 3691-12-1), beta-guaiacene (CAS No. 88-84-6), trans-nerolidol (CASNo.40716-66-3) or beta-Ma Lanxi (CAS No. 489-29-2), and combinations or mixtures of any two or more thereof.
Herein, the term "ginseng" means dried roots and rhizomes of ginseng (panax ginseng c.a. meyer) of the araliaceae family.
Erectile dysfunction (erectile dysfunction, ED) as used herein is the most common male sexual dysfunction, meaning that the penis is unable to achieve and/or maintain an adequate erection to accomplish satisfactory sexual activity. "erectile dysfunction" is used interchangeably herein with "impotence".
The term "treatment" as used herein refers to complete or partial cure of a disease, including but not limited to one, or a combination of two or more effects selected from the group consisting of: reducing or eliminating the etiology of the disease or disorder; improving or eliminating its pathological changes; alleviating or eliminating one or more symptoms thereof; delay or arrest its progress; lessening the severity thereof; reducing the incidence rate of the disease; reducing recurrence thereof; improving its prognosis.
The terms "comprising," "including," "having," "containing," or "involving," and other variations thereof herein, are inclusive or open-ended and do not exclude additional unrecited elements or method steps, although not necessarily present (i.e., the terms also encompass the terms "consisting essentially of … …" and "consisting of … …").
Herein, the term "wt%" refers to weight percent.
The term "about" or "approximately" means within + -10%, preferably within + -5%, more preferably within + -2% of the stated value.
In a first aspect, the present application provides a volatile oil, wherein the volatile oil comprises the following components:
based on the total weight of the volatile oil,
60-75wt% of ginseng alkynol; and
9-15 wt% of terpenoid.
In some embodiments, the ginseng alkynol is present in an amount of 60wt%, 61wt%, 62wt%, 63wt%, 64wt%, 65wt%, 66wt%, 67wt%, 68wt%, 69wt%, 70wt%, 71wt%, 72wt%, 73wt%, 74wt% or 75wt%, or a subrange between any two of the above values, e.g., 62wt% to 72wt%, particularly 64wt% to 70wt%, based on the total weight of the volatile oil.
In a particular embodiment, the panaxynol is present in an amount of 66wt% to 69wt%, in particular 67wt% to 68wt%, for example 67.8wt%, based on the total weight of the volatile oil.
Panaxynol is the highest content component in the volatile oil of the invention. The known panaxynol has anticancer, antibacterial, antifungal, tranquilizing, analgesic, blood pressure lowering, antiinflammatory, and nerve cell protecting effects. There is no report on the treatment or improvement of male sexual dysfunction with ginseng alkynol.
In some embodiments, the terpenoid is present in an amount of 9wt%, 10wt%, 11wt%, 12wt%, 13wt%, 14wt% or 15wt%, or a subrange between any two of the above values, e.g., 10wt% to 14wt%, particularly 11wt% to 13wt%, more particularly 12wt% to 13wt%, e.g., 12.3wt% to 12.8wt%, based on the total weight of the volatile oil.
In some embodiments, the terpenoid is selected from the group consisting of amycene, β -cyclic ene, neocaryophyllene, rhynchophylline, trans-caryophyllene, eucalyptol, elemene, calamine, α -gulene, andrographolide, eucalyptol, validol, β -siraitia Lin Xi, ganbergamotene, longifolene, cedrene, citrus limonene, α -guaiacene, β -guaiacene, trans-nerol, and β -Ma Lanxi, and any combination thereof.
No report is seen about the treatment or improvement of male sexual dysfunction by terpenoids in ginseng volatile oil.
In some of the above-described embodiments, the terpenoid comprises:
based on the total weight of the volatile oil,
1.2wt% to 2.2wt%, preferably 1.4wt% to 2.0wt%, more preferably 1.6wt% to 1.8wt% of amycin;
1.0wt% to 2.0wt%, preferably 1.2wt% to 1.8wt%, more preferably 1.4wt% to 1.6wt% of β -cyclic alkene;
0.8wt% to 1.6wt%, preferably 1.0wt% to 1.4wt%, more preferably 1.1wt% to 1.3wt% of neo-syringtricycloalkene;
0.8wt% to 1.6wt%, preferably 0.9wt% to 1.4wt%, more preferably 1.0wt% to 1.2wt% of rhythmene;
from 0.8% to 1.5%, preferably from 0.9% to 1.3%, more preferably from 1.0% to 1.2% by weight of trans-caryophyllene;
from 0.8% to 1.5%, preferably from 0.9% to 1.3%, more preferably from 1.0% to 1.2% by weight eucalyptol; and
0.6wt% to 1.3wt%, preferably 0.8wt% to 1.2wt%, more preferably 0.9wt% to 1.1wt% of elemene.
In a particular embodiment, the terpenoid comprises:
based on the total weight of the volatile oil,
1.7% by weight of amycin,
1.5% by weight of beta-cyclic olefins,
1.2% by weight of neo-syringtricycloalkene,
1.1% by weight of a rhythmic graphene,
1.1% by weight of trans-caryophyllene,
1.0wt% eucalyptol; and
1.0wt% of elemene.
In some of the above-described embodiments, the terpenoid comprises:
based on the total weight of the volatile oil,
0.4wt% to 1.0wt%, preferably 0.5wt% to 0.9wt%, more preferably 0.6wt% to 0.8wt% of calamine;
0.3wt% to 0.9wt%, preferably 0.4wt% to 0.8wt%, more preferably 0.5wt% to 0.7wt% of alpha-gulene;
0.3wt% to 0.8wt%, preferably 0.3wt% to 0.7wt%, more preferably 0.4wt% to 0.6wt% of eucalyptol; and
0.3wt% to 0.7wt%, preferably 0.3wt% to 0.6wt%, more preferably 0.4wt% to 0.5wt% of the valproic acid.
In some such embodiments, the terpenoid comprises:
based on the total weight of the volatile oil,
0.7wt% calamine;
0.6wt% of alpha-gulene;
0.5wt% eucalyptol; and
0.4wt% of the wifery alcohol.
In some of the above-described embodiments, the volatile oil comprises or consists essentially of:
67.8wt% of ginseng alkynol;
1.7% by weight of amycin,
1.5% by weight of beta-cyclic olefins,
1.2% by weight of neo-syringtricycloalkene,
1.1% by weight of a rhythmic graphene,
1.1% by weight of trans-caryophyllene,
1.0wt% eucalyptol;
1.0wt% of elemene;
0.7wt% calamine;
0.6wt% of alpha-gulene;
0.5wt% eucalyptol; and
0.4wt% of the wifery alcohol.
In some of the above-described embodiments, the volatile oil comprises from 1.0wt% to 2.0wt%, preferably from 1.2wt% to 1.8wt%, more preferably from 1.4wt% to 1.6wt% (e.g., 1.5 wt%) of a mixture of the following other terpenoids, based on the total weight of the volatile oil: beta-sec Lin Xi, chamaerene, longifolene, cedrene, bergamotene, alpha-guaiacene and beta-guaiacene.
In some such embodiments, the mixture of other terpenoids comprises:
based on the total weight of the volatile oil,
0.15wt% to 0.45wt%, preferably 0.2wt% to 0.4wt%, more preferably 0.25wt% to 0.35wt% (e.g., 0.3 wt%) of β -ray Lin Xi;
from 0.15wt% to 0.45wt%, preferably from 0.2wt% to 0.4wt%, more preferably from 0.25wt% to 0.35wt% (e.g., 0.28 wt%) Gan Xiangxi;
0.15wt% to 0.45wt%, preferably 0.2wt% to 0.4wt%, more preferably 0.25wt% to 0.35wt% (e.g. 0.27 wt%) longifolene;
0.1wt% to 0.3wt%, preferably 0.12wt% to 0.26wt%, more preferably 0.16wt% to 0.22wt% (e.g., 0.2 wt%) cedrene;
0.08wt% to 0.2wt%, preferably 0.1wt% to 0.18wt%, more preferably 0.12wt% to 0.16wt% (e.g. 0.15 wt%) of bergamotene;
0.08wt% to 0.18wt%, preferably 0.1wt% to 0.16wt%, more preferably 0.11wt% to 0.14wt% (e.g. 0.11 wt%) of α -guaiacene; and
from 0.08wt% to 0.18wt%, preferably from 0.1wt% to 0.16wt%, more preferably from 0.11wt% to 0.14wt% (e.g. 0.12 wt%) of β -guaiacene.
In a particular embodiment, the mixture of other terpenoids comprises:
based on the total weight of the volatile oil,
0.3wt% of beta-sirtuin Lin Xi;
0.28wt% Gan Xiangxi;
0.27wt% longifolene;
0.2wt% cedrene;
0.15wt% of bergamotene;
0.11wt% of α -guaiacene; and
0.12wt% of beta-guaiacene.
In some of the above-described embodiments, the volatile oil comprises:
based on the total weight of the volatile oil,
from 0.04% to 0.1% by weight, preferably from 0.06% to 0.08% by weight (e.g. 0.07% by weight) of trans-nerolidol; and
from 0.03wt% to 0.08wt%, preferably from 0.04wt% to 0.06wt% (e.g. 0.05 wt%) of β -Ma Lan ene.
In some of the above-described embodiments, the volatile oil comprises 0.3wt% to 0.8wt%, preferably 0.3wt% to 0.6wt%, more preferably 0.4wt% to 0.5wt% (e.g., 0.46 wt%) andrographolide, based on the total weight of the volatile oil.
Andrographolide is known to have antibacterial and antiinflammatory pharmacological effects. There is no report on andrographolide treatment or improvement of male sexual dysfunction.
In some of the above-described embodiments, the volatile oil further comprises:
based on the total weight of the volatile oil,
3.0wt% to 6.0wt%, preferably 3.5wt% to 5.0wt%, more preferably 4.0wt% to 4.5wt% (e.g. 4.3 wt%) sitosterol; and
1.0wt% to 2.0wt%, preferably 1.2wt% to 1.8wt%, more preferably 1.4wt% to 1.6wt% (e.g. 1.5 wt%) stigmasterol.
Sitosterol, a drug, has the effect of reducing serum cholesterol. Sitosterol is a plant sterol and is mainly used as a raw material for synthesizing steroid hormone. No report of Guan Gu sterols or stigmasterols for treating or ameliorating male sexual dysfunction was seen.
In some further embodiments, the volatile oil further comprises:
based on the total weight of the volatile oil,
5-15 wt% of linoleic acid; and
2.5wt% to 8.0wt% of palmitic acid.
In some embodiments, the linoleic acid is present in an amount of 5wt%, 6wt%, 7wt%, 8wt%, 9wt%, 10wt%, 11wt%, 12wt%, 13wt%, 14wt% or 15wt%, or a subrange between any two of the above values, e.g., 7wt% to 13wt%, especially 9wt% to 11wt%, e.g., 10wt%, based on the total weight of the volatile oil.
In some embodiments, the palmitic acid is present in an amount of 2.5wt%, 3.0wt%, 3.5wt%, 4.0wt%, 4.5wt%, 5.0wt%, 5.5wt%, 6.0wt%, 6.5wt%, 7.0wt%, 7.5wt% or 8.0wt%, or a subrange between any two of the above, e.g., 3.0wt% to 6.0wt%, particularly 3.5wt% to 4.0wt%, e.g., 3.7wt%, based on the total weight of the volatile oil.
No report of Guan Ya oleic or palmitic acid treatment or improvement of male sexual dysfunction was seen.
In some of the above-described embodiments, the volatile oil comprises the components shown in table 1:
TABLE 1
In some embodiments, each of the volatile oil components described above, as well as the volatile oil, may be synthetic, and the volatile oil may be formulated from various components.
In other embodiments, the volatile oils described above may be derived from plants, preferably ginseng (i.e., ginseng essential oil). In some such embodiments, the volatile oil is waterSteam distillation, cold pressing, fat absorption, and solvent extraction (e.g., CO 2 Extraction method) is obtained from ginseng. In some embodiments, the volatile oil is obtained from ginseng by steam distillation. The steam distillation method may include the steps of: pulverizing Ginseng radix, pulverizing, steam distilling, and collecting volatile oil to obtain the volatile oil.
In a second aspect, the present application provides a pharmaceutical or nutraceutical composition comprising a volatile oil of the invention as described above, and optionally one or more physiologically or pharmaceutically acceptable additives, carriers and/or excipients.
The studies conducted by the inventors have revealed that the volatile oil of the present invention has an effect of treating or improving sexual dysfunction in male individuals. In particular, it was surprisingly shown that the volatile oils of the present invention, administered either orally or by inhalation (incense), significantly shorten the penile erection and lengthen the ejaculation latency of model animals and are superior to the ginseng extract extracted by aqueous ethanol extraction and administered orally. The study also shows that the administration of the volatile oils of the invention by the (incense) inhalation route has an effect comparable to oral administration, even in some respects significantly better than low doses of volatile oils.
In a third aspect, the present application provides a volatile oil or a pharmaceutical or nutraceutical composition of the invention as described above for use in the treatment or amelioration of sexual dysfunction in a male individual.
In a fourth aspect, the present application also provides the use of the volatile oil or the pharmaceutical or health care composition of the invention as described above in the manufacture of a medicament or health care product for treating or ameliorating sexual dysfunction in a male individual.
In a fifth aspect, the present application also provides a method for treating sexual dysfunction in a male subject, comprising administering to a subject in need thereof an effective amount of a volatile oil, pharmaceutical or nutraceutical composition, medicament or nutraceutical as described above.
In some embodiments, the sexual dysfunction is erectile dysfunction. In other embodiments, the sexual dysfunction is premature ejaculation. In other embodiments, the sexual dysfunction is lack of libido. In some embodiments, the sexual dysfunction described above is of kidney-yang deficiency type, e.g., liver depression and kidney deficiency type.
The pharmaceutical or nutraceutical compositions, medicaments or nutraceuticals of the present invention can comprise one or more physiologically or pharmaceutically acceptable additives, carriers and/or excipients, such as flavoring agents, fragrances, preservatives, inclusion agents (e.g., cyclodextrins), propellants and combinations thereof.
The pharmaceutical or nutraceutical composition, medicament or nutraceutical may be administered by inhalation, topically, transdermally or orally. In some preferred embodiments, the composition, medicament or nutraceutical is administered by inhalation.
The pharmaceutical or nutraceutical composition, medicament or nutraceutical may be in solid, semi-solid, liquid or gaseous form, for example in the form of a spray, aerosol, fragrance, aromatherapy, sachet, syrup, elixir or soft capsule. Preferred dosage forms include sprays, aerosols, fragrances, aromatherapy agents or sachets, more preferably fragrances or aromatherapy agents.
An "effective amount" of the volatile oil, pharmaceutical or nutraceutical composition, medicament or nutraceutical of the present invention may be about 0.1 to 5.0ml of the volatile oil, e.g., about 0.3 to 4.9ml, about 0.5 to 4.7ml, about 1.0 to 4.5ml, about 1.5 to 4.0ml, about 2.0 to 3.5ml or about 2.5 to 3.0ml, per single dose, based on the volume of the volatile oil. The effective amount will generally depend on a variety of factors including the sex, age, weight, general health, severity of the disorder or condition of the individual being treated, the rate of administration and the discretion of the prescribing physician and thus can vary.
The volatile oil, pharmaceutical or health care composition, medicament or health care product of the present invention may be administered once, twice, three times or more daily, preferably once daily.
Preferably, the volatile oil, pharmaceutical or nutraceutical composition, medicament or nutraceutical of the present invention may be administered prior to the occurrence of sexual activity, for example about 120 to 5 minutes, preferably about 120 to 30 minutes, for example about 90 to 30 minutes, or about 60 to 45 minutes, prior to the occurrence of sexual activity.
Advantageous effects
The volatile oil of the present invention can significantly shorten the penile erection latency and lengthen the ejaculation latency of the impotence-model rats, and has an effect superior to that of ginseng extract extracted by conventional methods (e.g., aqueous ethanol extraction) and orally administered. The volatile oils of the present invention are administered by the (incense) inhalation route with comparable effects to oral administration, even in some respects significantly better than low dose oral volatile oils.
Examples
The invention is illustrated in more detail by the following examples, which are not to be construed as limiting the invention in any way, the scope of which is defined solely by the appended claims.
Example 1: pharmacodynamics research of ginseng essential oil in impotence model rat
A compound emotion modeling method is used for establishing a rat liver depression and kidney deficiency impotence model, and a series of animal behavior indexes such as riding latency, inserting latency, ejaculation latency, riding times, inserting times and the like of a male rat are observed to evaluate the efficacy effect of the male rat.
1. Experimental materials
1) Ginseng essential oil: supplied by the Hunan noniming Bioengineering Co., ltd., lot number: 1903008.
the composition of ginseng essential oil is shown in table 2 below:
TABLE 2
The ginseng essential oil can be obtained by a preparation process mainly comprising the following steps: pulverizing Ginseng radix, pulverizing, steam distilling, and collecting essential oil to obtain Ginseng radix essential oil.
2) Ginseng extract: supplied by the Hunan noniming Bioengineering Co., ltd., lot number: yu20200514, which contains 10% ginsenoside.
The preparation process of the ginseng extract comprises the following steps: pulverizing Ginseng radix, adding 50% -80% ethanol water solution (10 ml/g Ginseng radix) at 80deg.C for 2 times (1.5 hr/time), concentrating the extractive solution, purifying the concentrated solution with D101 macroporous resin, spray drying, and collecting powder to obtain Ginseng radix extract.
3) Sildenafil citrate tablet (0.05 g/tablet): lot number, produced by the company limited in the biochemical pharmaceutical industry (Jiangsu) in Changzhou: 190806.
2. test method
75 male SPF-grade SD rats (Si Bei Fu (Beijing) biotechnology Co., ltd.) qualified for quarantine and 200.3-312.8 g weight were selected and randomly divided into normal groups (10) and model groups (65) according to the weight. The model rats were subjected to one of the following daily stimulations using a compound emotion modeling method: soaking in ice water (soaking in plastic barrel at 4deg.C for 25 cm), soaking in water for 5min, keeping out water for 24 hr, binding (fixing the rat in steel binding barrel for 4 hr), keeping out food for 24 hr, and clamping tail (clamping long tail ticket of 25cm at 1cm from tail end for 30 min). One stimulus per day for 28 consecutive days. To achieve unpredictability, the stimulation was selected using a piecewise non-repeating random digital method, in the order shown in table 3. The normal group did not apply any emotional stimulus. The success or failure of modeling is confirmed by observing the riding latency, the inserting latency, the ejaculation latency, the riding times and the inserting times.
TABLE 3 stimulation order
Model rats were selected for 60 animals, weighing 311.6-388.7 g, and randomly dividing into a model control group, a positive control group (sildenafil citrate tablet, 9mg/kg, gastric lavage), a ginseng extract group (0.09 mg/kg, gastric lavage), a ginseng essential oil low dose group (0.09 mg/kg, gastric lavage), a ginseng essential oil high dose group (0.18 mg/kg, gastric lavage) and a ginseng essential oil aromatherapy group (0.3 ml, by continuous 30min aromatherapy administration), each group of 10 animals. Each group of animals subjected to gastric lavage is provided with a liquid medicine with corresponding concentration according to 10 mL/kg; the aromatherapy group is dosed for 30min by an aromatherapy machine under the condition of incomplete transparent sealing; the normal control group and the model control group were lavaged with equal volumes of pure water. The administration was carried out 1 time per day for 7 days. At 30min after the last administration, 20 μg of estradiol benzoate (Sichuan Jin Ke medical industry Co., lot: 20190301) and 500 μg of progesterone (Zhejiang Xian pharmaceutical Co., lot: 171107) were injected subcutaneously with oestrus-good female mice (24 h and 3h before mating) at 1:1 cage, and the mating behavior of each group of male mice within 30min was recorded by using a video monitoring system, and a series of animal behavior indexes such as penile erection latency, riding latency, insertion latency, ejaculation latency, riding number, insertion number, etc. were observed.
Observation index
(1) Riding latency: observing the time from the beginning of the test to the 1 st riding of the male mouse for 30min when no riding occurs; (2) mating latency: the time from the beginning of the test to the completion of mating of the male mouse 1 st time (with insertion behavior) is counted for 30min when no mating behavior occurs within 30min; (3) number of rides: total number of riding events occurring within 30min; (4) number of mating: total number of mating actions occurring within 30min; (5) insertion rate: mating number/(riding number + mating number); (6) number of captures: the number of female mice captured within 30 min.
3. Experimental results
(1) Effects on penile erection
After pure water is given to the normal control group rats, the rats do not have obvious abnormality in autonomous activity and mental state, lie on one side of a mating cage firstly, and after about 30 minutes, penis erection occurs and licking hair occurs; after the model control group male mice and female mice are in a cage, the male mice lie on one side of the mating cage, and penis erection does not occur, and meanwhile, the autonomous activity is obviously reduced compared with that of the normal control group; after the positive control group is dosed, penile erection occurs after about 9-18 min, activity is increased, net climbing action is carried out, and the times of licking behavior are obviously increased. As shown in table 4; the penis erection latency of the rats is respectively about 17-28 min, 10-26 min, 9-16 min and 7-21 min, and the independent activities are increased to different degrees, wherein the rats in the ginseng essential oil high-dose group and the ginseng essential oil aromatherapy group are more vigorous and have stronger activity. The penile erection latency was significantly prolonged in model control animals compared to normal control (p < 0.01); compared with the model control group, the positive control group, the ginseng extract and the ginseng essential oil perfuse the stomach and the aromatherapy group have obviously shortened penile erection latency (p < 0.01); compared with the positive control group, the penis erection latency of the rats in the low dosage group of the ginseng extract and the ginseng essential oil is obviously prolonged (p < 0.01); compared with ginseng extract, the penile erection latency of the low-dose and high-dose group of ginseng essential oil rats is obviously shortened (p <0.05 or p < 0.01) and the positive correlation level of the dosage is shown; the high dosage group of the ginseng essential oil is basically equivalent to the rat penis erection latency period of the ginseng essential oil aromatherapy group.
TABLE 4 Effect of Ginseng radix extract and essential oils on penis erection latency in impotence model rats
Note that: in comparison with the normal control group, ++ p<0.01; in comparison with the control group of the model, ** p<0.01; in comparison with the positive control group, ## p<0.01; in comparison with the group of ginseng extracts, Δ p<0.05, ΔΔ p<0.01。
(2) Effects on mating behavior
The mating behavior of the rats is shown in fig. 1. As shown in tables 5 and 6, the model control rats had significantly longer mating latency (p < 0.01), significantly reduced number of rides, mating number and insertion rate (p <0.05 or p < 0.01) compared to the normal control, and no significant difference between the number of catches and riding latency. Compared with the model control group, the mating latency of rats in each administration group is obviously shortened (p <0.05 or p < 0.01), and the capturing times, riding times, mating times and insertion rate are obviously increased (p <0.05 or p < 0.01); the mating latency of rats in the low dose group of ginseng extract and ginseng essential oil is significantly shortened (p < 0.01), the mating frequency of rats in the low dose group of ginseng extract, ginseng essential oil, high dose group and ginseng essential oil aromatherapy group is significantly reduced (p <0.05 or p < 0.01), and the capturing frequency, riding latency and riding frequency of rats in the ginseng extract group are significantly reduced (p <0.05 or p < 0.01); compared with the ginseng extract group, the mating latency and riding latency of the ginseng essential oil high-dose group and the ginseng essential oil aromatherapy group rats are remarkably shortened (p <0.05 or p < 0.01), the mating times are remarkably increased (p <0.05 or p < 0.01), and the capturing times and riding times of the ginseng essential oil aromatherapy group are remarkably increased (p < 0.01).
TABLE 5 influence of Ginseng radix extract and essential oils on mating behavior of impotence model rats
Note that: in comparison with the normal control group, + p<0.05, ++ p<0.01; in comparison with the control group of the model, * p<0.05, ** p<0.01; in comparison with the positive control group, # p<0.05, ## p<0.01; in comparison with the group of ginseng extracts, Δ p<0.05, ΔΔ p<0.01。
TABLE 6 influence of Ginseng radix extract and essential oils on mating behavior of impotence model rats/>
Note that: in comparison with the normal control group, + p<0.05, ++ p<0.01; in comparison with the control group of the model, * p<0.05, ** p<0.01; in comparison with the positive control group, # p<0.05, ## p<0.01; in comparison with the group of ginseng extracts, Δ p<0.05, ΔΔ p<0.01。
4. conclusion(s)
The ginseng extract (oral administration) and the ginseng essential oil (oral administration and aromatherapy) have remarkable improving effects on impotence, wherein the improving effect of the ginseng essential oil in oral administration with low dosage is better than that of the ginseng extract (oral administration) with equal dosage, so that the improving effect of the ginseng essential oil is better. The effect of the ginseng essential oil aromatherapy group is equivalent to that of the ginseng essential oil oral high-dose group, and is obviously superior to that of the ginseng essential oil oral low-dose group in some aspects.
Various modifications of the invention, in addition to those described herein, will be apparent to those skilled in the art from the foregoing description. Such modifications are also intended to fall within the scope of the appended claims. Each reference cited in this application (including all patents, patent applications, journal articles, books, and any other publications) is incorporated herein by reference in its entirety.
Claims (10)
1. A volatile oil, wherein the volatile oil comprises the following components:
based on the total weight of the volatile oil,
60wt% to 75wt%, preferably 62wt% to 72wt%, more preferably 64wt% to 70wt%, for example 66wt% to 69wt% or 67wt% to 68wt% of ginseng alkynol; and
9wt% to 15wt%, preferably 10wt% to 14wt%, more preferably 11wt% to 13wt% of terpenoid; and is also provided with
Wherein the terpenoid is selected from the group consisting of amycins, β -cyclic olefins, neocaryophyllene, rhynchophylline, trans-caryophyllene, eucalyptol, elemene, calamine, α -gulene, andrographolide, eucalyptol, validol, β -sirtuin Lin Xi, champignon, longifolene, cedrene, bergamotene, α -guaiacene, β -guaiacene, trans-nerol, and β -Ma Lanxi, and any combination thereof.
2. The volatile oil of claim 1, wherein the terpenoid comprises:
based on the total weight of the volatile oil,
1.2wt% to 2.2wt%, preferably 1.4wt% to 2.0wt%, more preferably 1.6wt% to 1.8wt% of amycin;
1.0wt% to 2.0wt%, preferably 1.2wt% to 1.8wt%, more preferably 1.4wt% to 1.6wt% of β -cyclic alkene;
0.8wt% to 1.6wt%, preferably 1.0wt% to 1.4wt%, more preferably 1.1wt% to 1.3wt% of neo-syringtricycloalkene;
0.8wt% to 1.6wt%, preferably 0.9wt% to 1.4wt%, more preferably 1.0wt% to 1.2wt% of rhythmene;
from 0.8% to 1.5%, preferably from 0.9% to 1.3%, more preferably from 1.0% to 1.2% by weight of trans-caryophyllene;
from 0.8% to 1.5%, preferably from 0.9% to 1.3%, more preferably from 1.0% to 1.2% by weight eucalyptol; and
0.6wt% to 1.3wt%, preferably 0.8wt% to 1.2wt%, more preferably 0.9wt% to 1.1wt% elemene;
preferably, the terpenoid comprises:
based on the total weight of the volatile oil,
1.7% by weight of amycin,
1.5% by weight of beta-cyclic olefins,
1.2% by weight of neo-syringtricycloalkene,
1.1% by weight of a rhythmic graphene,
1.1% by weight of trans-caryophyllene,
1.0wt% eucalyptol; and
1.0wt% of elemene.
3. The volatile oil of claim 1 or 2, wherein the terpenoid comprises:
based on the total weight of the volatile oil,
0.4wt% to 1.0wt%, preferably 0.5wt% to 0.9wt%, more preferably 0.6wt% to 0.8wt% of calamine;
0.3wt% to 0.9wt%, preferably 0.4wt% to 0.8wt%, more preferably 0.5wt% to 0.7wt% of alpha-gulene;
0.3wt% to 0.8wt%, preferably 0.3wt% to 0.7wt%, more preferably 0.4wt% to 0.6wt% of eucalyptol; and
0.3wt% to 0.7wt%, preferably 0.3wt% to 0.6wt%, more preferably 0.4wt% to 0.5wt% of the valproic acid;
preferably, the terpenoid comprises:
based on the total weight of the volatile oil,
0.7wt% calamine;
0.6wt% of alpha-gulene;
0.5wt% eucalyptol; and
0.4wt% of the wifery alcohol.
4. A volatile oil according to any one of claims 1 to 3, wherein the volatile oil comprises or consists essentially of:
67.8wt% of ginseng alkynol;
1.7% by weight of amycin,
1.5% by weight of beta-cyclic olefins,
1.2% by weight of neo-syringtricycloalkene,
1.1% by weight of a rhythmic graphene,
1.1% by weight of trans-caryophyllene,
1.0wt% eucalyptol;
1.0wt% of elemene;
0.7wt% calamine;
0.6wt% of alpha-gulene;
0.5wt% eucalyptol; and
0.4wt% of the wifery alcohol.
5. The volatile oil of any one of claims 1 to 4, wherein the volatile oil comprises 1.0wt% to 2.0wt%, preferably 1.2wt% to 1.8wt%, more preferably 1.4wt% to 1.6wt% of a mixture comprising the following other terpenoids, based on the total weight of the volatile oil: beta-sec Lin Xi, chamaerene, longifolene, cedrene, bergamotene, alpha-guaiacene and beta-guaiacene;
preferably, the mixture of other terpenoids comprises:
based on the total weight of the volatile oil,
0.15wt% to 0.45wt%, preferably 0.2wt% to 0.4wt%, more preferably 0.25wt% to 0.35wt% of β -sirtuin Lin Xi;
from 0.15wt% to 0.45wt%, preferably from 0.2wt% to 0.4wt%, more preferably from 0.25wt% to 0.35wt% Gan Xiangxi;
0.15wt% to 0.45wt%, preferably 0.2wt% to 0.4wt%, more preferably 0.25wt% to 0.35wt% longifolene;
0.1wt% to 0.3wt%, preferably 0.12wt% to 0.26wt%, more preferably 0.16wt% to 0.22wt% cedrene;
0.08wt% to 0.2wt%, preferably 0.1wt% to 0.18wt%, more preferably 0.12wt% to 0.16wt% of bergamotene;
0.08wt% to 0.18wt%, preferably 0.1wt% to 0.16wt%, more preferably 0.11wt% to 0.14wt% of α -guaiacene; and
from 0.08% to 0.18%, preferably from 0.1% to 0.16%, more preferably from 0.11% to 0.14% by weight of β -guaiacene;
more preferably, the mixture of other terpenoids comprises:
based on the total weight of the volatile oil,
0.3wt% of beta-sirtuin Lin Xi;
0.28wt% Gan Xiangxi;
0.27wt% longifolene;
0.2wt% cedrene;
0.15wt% of bergamotene;
0.11wt% of α -guaiacene; and
0.12wt% of beta-guaiacene.
6. The volatile oil of any one of claims 1 to 5, wherein the volatile oil comprises:
based on the total weight of the volatile oil,
from 0.04% to 0.1% by weight, preferably from 0.06% to 0.08% by weight, of trans-nerolidol, and
0.03wt% to 0.08wt%, preferably 0.04wt% to 0.06wt% of beta-Ma Lanxi;
and/or
0.3wt% to 0.8wt%, preferably 0.3wt% to 0.6wt%, more preferably 0.4wt% to 0.5wt% of andrographolide;
and/or
3.0wt% to 6.0wt%, preferably 3.5wt% to 5.0wt%, more preferably 4.0wt% to 4.5wt% sitosterol;
and/or
1.0wt% to 2.0wt%, preferably 1.2wt% to 1.8wt%, more preferably 1.4wt% to 1.6wt% stigmasterol;
and/or
5wt% to 15wt%, preferably 7wt% to 13wt%, more preferably 9wt% to 11wt% linoleic acid;
and/or
2.5wt% to 8.0wt%, preferably 3.0wt% to 6.0wt%, more preferably 3.5wt% to 4.0wt% of palmitic acid.
7. The volatile oil of any one of claims 1 to 6, wherein the volatile oil comprises the components shown in table 1 or table 2.
8. The volatile oil according to any one of claims 1 to 7, wherein the volatile oil may be synthetic or formulated, preferably obtainable from plants, more preferably from ginseng.
9. A pharmaceutical or nutraceutical composition comprising the volatile oil of any one of claims 1 to 7, and optionally one or more physiologically or pharmaceutically acceptable additives, carriers and/or excipients.
10. Use of the volatile oil of any one of claims 1 to 9 or the pharmaceutical or health care composition of claim 9 in the manufacture of a medicament or health care product for treating or ameliorating sexual dysfunction in a male individual;
preferably, the sexual dysfunction is selected from erectile dysfunction, premature ejaculation and lack of libido;
and/or
Preferably, the sexual dysfunction is of kidney-yang deficiency type, for example liver depression and kidney deficiency type.
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Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
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KR20020071326A (en) * | 2001-03-06 | 2002-09-12 | 팍스바이오젠 주식회사 | Composition for improving erectile dysfunction and foods containing the same |
CN112043754A (en) * | 2020-09-25 | 2020-12-08 | 李庆远(广州)养生生物科技有限公司 | Medicinal essential oil for men |
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Publication number | Priority date | Publication date | Assignee | Title |
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KR20020071326A (en) * | 2001-03-06 | 2002-09-12 | 팍스바이오젠 주식회사 | Composition for improving erectile dysfunction and foods containing the same |
CN112043754A (en) * | 2020-09-25 | 2020-12-08 | 李庆远(广州)养生生物科技有限公司 | Medicinal essential oil for men |
Non-Patent Citations (1)
Title |
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赵岩等: "人参挥发油化学成分及其主要活性成分聚乙炔醇类药理作用研究进展", 中国药房, vol. 28, no. 13, pages 1856 - 1859 * |
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