JP2007230888A - Supplement containing serenoa repens extract and carcinogenesis prophylactic agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a highly safe new supplement for the complementary therapy in preventing androgen-nondependent cancer, and to provide an androgen-nondependent cancer prophylactic agent. <P>SOLUTION: The new supplement for the complementary therapy in preventing androgen-nondependent cancer contains a plant-derived Serenoa repens extract. The androgen-nondependent cancer prophylactic agent comprises the Serenoa repens extract. The above supplement and the agent prevent developing androgen-nondependent cancer, especially cutaneous cancer and lung caner. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to a nutritional supplement for supplemental therapy in the prevention of male hormone-independent cancer and a male hormone-independent cancer preventive agent, which contains a plant-derived component, in particular, a saw palmetto extract.

The number of cancer deaths in our country exceeds 300,000 annually, and is the leading cause of death, and establishment of preventive and therapeutic methods is required. There are three main cancer treatment methods: surgical treatment, chemotherapy with anticancer agents, and radiation therapy, although it varies depending on the site of cancer. Although these treatments are combined for treatment, no effective treatment has yet been established.
On the other hand, in order to reduce death from cancer, the idea that prevention of cancer is important is being established. It has been found that about 80% of cancers are caused by familiar environmental factors. Benzpyrenes contained in exhaust gases such as ultraviolet rays and automobiles are examples of carcinogenic factors in the environment. In addition, as carcinogens in the diet, components contained in the burns of meat and fish, compounds such as aflatoxin produced by mold, nitrosamines produced by the reaction of nitrite and amino compounds contained in vegetables, etc. are known. ing.
In addition to improving lifestyle habits, methods for daily intake of effective ingredients that antagonize these carcinogenic factors have been proposed for cancer prevention.
Saw palmetto (Serenoa repens) is a plant belonging to the family of Palmoae, native to North America, and its fruit extract has been known to be effective for prostate enlargement. The development of benign prostatic hyperplasia involves dihydrotestosterone, which is produced by the action of testosterone under the action of 5-α-reductase, and saw palmetto extract inhibits 5-α-reductase to inhibit or treat prostatic hypertrophy. (For example, Non-Patent Document 1). In addition, male hormone-dependent cancers such as prostate cancer require male hormones for their growth, and dihydrotestosterone has a stronger growth stimulating effect than testosterone, so saw palmetto extract suppresses androgen-dependent cancers It is expected that.

  However, the effect of saw palmetto extract on male hormone-independent cancer such as skin cancer or lung cancer has not been known so far. The use of substances that antagonize the carcinogenic factors present in the environment and foods and have a preventive effect on the onset of male hormone-independent cancer has been desired to be useful in the prevention and treatment of such cancers. Furthermore, it has been desired to be useful as a complementary therapy in the prevention of male hormone-independent cancer by easily ingesting it as a dietary supplement containing a substance having such a preventive effect.

Thus, as a result of intensive studies, the present inventors have newly found the fact that a saw palmetto extract has a remarkable suppressive action on male hormone-independent cancer and completed the present invention.
That is, one aspect of the present invention relates to a dietary supplement for complementary therapy in the prevention of male hormone-independent cancer, particularly skin cancer or lung cancer, which contains a saw palmetto extract.
The second aspect of the present invention relates to an androgen-independent cancer preventive agent containing a saw palmetto extract. Among them, the male hormone-independent cancer preventive agent preferably prevents skin cancer and lung cancer.

Since the dietary supplement of the present invention contains a saw palmetto extract, it is useful as a complementary therapy in the prevention of male hormone-independent cancer, particularly skin cancer or lung cancer. On the other hand, the male hormone-independent cancer preventive agent of the present invention can effectively prevent carcinogenesis of these cancers. Furthermore, since the extract from saw palmetto is an experienced plant, the dietary supplement and cancer preventive agent of the present invention containing the extract are highly safe and can be taken daily.

The present invention is described in detail below.
It is not clear what mechanism the saw palmetto extract is involved in the prevention of carcinogenesis. For example, when the cancer preventive agent of the present invention is administered, the cancer preventive agent is not administered. Compared to the case, the incidence of lung cancer can be effectively reduced. Further, for example, when the cancer preventive agent of the present invention is applied to the skin in advance, the incidence of skin cancer can be effectively reduced as compared with the skin to which the cancer preventive agent is not applied. The dosage of the nutritional supplement and the cancer preventive agent of the present invention is suitably an amount of about 100 to 1000 mg per day as a saw palmetto extract. Thereby, the male hormone-independent cancer preventive agent of the present invention can exhibit an excellent carcinogenic effect. Of course, it goes without saying that the nutritional supplement of the present invention containing a saw palmetto extract is also expected to have a carcinogenic effect. It is also possible to use the nutritional supplement of the present invention and a cancer preventive agent in combination.

  As the saw palmetto extract in the present invention, a commercially available one or one extracted directly from the saw palmetto is used. The raw material for extraction can be appropriately selected from any part of the saw palm, but a saw palm fruit is particularly preferable. The saw palmetto extract can be obtained from the extraction raw material by a method generally used for extraction of plant extracts. The saw palmetto extract is, for example, a saw palm fruit as it is or after being dried, and then pulverized as it is or using a crusher, and any extraction solvent such as water or alcohols (methanol, ethanol, butanol, isopropyl alcohol, etc.) , Refluxing from room temperature using polyhydric alcohols (glycerin, propylene glycol, ethylene glycol, etc.), organic solvents such as acetone, ethyl acetate, chloroform, toluene, diethyl ether, hexane, and mixtures of two or more thereof Below, it can extract using arbitrary apparatuses according to the kind and extraction scale of a solvent. Specifically, saw palm fruit as an extraction raw material is put into a treatment tank filled with an extraction solvent, and is sometimes stirred to elute soluble components. Then, a saw palmetto extract can be obtained by filtering and removing an extraction residue, concentrating and drying the obtained extract. The extraction conditions are usually about 30 minutes to 2 hours at 50 to 90 ° C. when water is used as the extraction solvent. When a mixed solvent of water and ethanol is used as the extraction solvent, it is usually about 30 minutes to 2 hours at 40 to 80 ° C. The obtained saw palmetto extract can be purified for the purpose of decolorization, deodorization, activity improvement and the like. Further, the saw palmetto extract may be one obtained by supercritical extraction with carbon dioxide. As a commercially available saw palmetto extract, the brand name Sabal Select (produced by the supercritical extraction method) of Indena Co. (Italy) and the like can be mentioned.

The saw palmetto extract thus extracted is formulated into various dosage forms that can be usually used together with various other components, for example, solid preparations, semi-solid preparations, liquid preparations, etc., depending on the use in the present invention. The Specific dosage forms include, for example, tablets (including orally disintegrating tablets, chewable tablets, effervescent tablets, troches, jelly-like drops, etc.), granules, fine granules, powders, hard capsules, soft capsules Capsule, dry syrup, liquid (including drink, suspension, syrup), gel, liposome, extract, tincture, limonade, jelly, paste and the like. Among these, solid agents such as tablets, granules, fine granules, powders, hard capsules, soft capsules, and liquid agents are suitable. As the dietary supplement, hard capsules or soft capsules that are easy to swallow with water without having to worry about the taste or smell of the content components are particularly preferable. As the cancer preventive agent, a liquid agent that can be employed as an internal preparation, an external preparation, or an injection is particularly preferable.

In addition to the saw palmetto extract, the nutritional supplement and cancer preventive agent of the present invention are usually used in foods, health foods, health supplements, cosmetics, quasi-drugs, and pharmaceuticals depending on the respective use or dosage form. Of course, the components to be added can be appropriately blended.
Examples of food ingredients that can be blended include soybean isoflavones, ginseng, echinacea, ganoderma, agaricus, mesicacob, lactic acid bacteria, yeast, fungi such as koji molds, black beans, rahan fruit, seven ginsengs, licorice, western cabbage, hemp, Egg yolk oil, chamomile, pine needle extract, valerian, oyster meat extract, hub tea, kale, loquat leaf, pearl barley, horsetail, cod sprout, rabu hemp tea, amachazul, mugwort, ginkgo biloba extract, jewel, perilla, nucleic acid, turmeric Shark Fin Cartilage, Royal Jelly, Noni, Aloe, Sockeye, Ginseng, Suppon, Kale, Spirulina, Dokudami, Chamomile, Pechy Tea, Fucoidan, Lemon Balm, Propolis, Gadju, Honey, Chlorella, Kefir, Deep Sea Agate Extract, Cranberry, Gaukurua , Acerola, collagen, wood vinegar, placenta Prunes, maca, mugwort, pomegranate, wolfberry, radish, root comb, oligosaccharide, plum meat, psyllium, bittern, soy milk, dextrin, ginger pepper, gymnema, banaba tea, maitake, lipoic acid, morohaya, cordyceps, pine pollen, siberia Ginseng, Himematsutake, Nihonsan Ginseng, Pual Tea, Guava Tea, Natto, Garlic, Blueberry, Brown Rice, Oyster Leaf, Mulberry Leaf, Chitin, Rice Germ, Root Comb, Tochu Tea, Dokudami, Gajutsu, Barley Wakaba Extract, Apple cider vinegar, Yamasuko, purple ipe, etc., and extracts from these, vitamins such as retinol, carotenoids, tocopherol, ascorbic acid, minerals such as zinc and selenium, polyphenols such as catechin, omega such as EPA, DHA 3 fatty acids, L-carnitine, psyllium, coenzyme, mu Polysaccharides, rutin, chondroitin, lycopene, AHCC, hyaluronic acid, flavonoids, and the like.
Examples of pharmaceutical components that can be incorporated include anticancer agents, antibiotics, anti-inflammatory agents such as aspirin, and cytokines such as interferon. Various additives that can be used for formulation can also be used.

The dietary supplement or cancer preventive agent of the present invention can be produced, for example, by the method described below.
Granules / fine granules / powder: Obtained by drying a saw palmetto extract with an excipient if necessary using a spray dryer.
Tablet: For example, it can be obtained by mixing the granule, fine granule and powder obtained by the above-mentioned method with a binder or the like, if necessary, and tableting into a predetermined shape.
Hard capsule / soft capsule: For example, a content component containing a saw palmetto extract can be obtained by encapsulating with a gelatin film using an automatic rotary capsule filling machine or the like.
Solution: For example, a saw palmetto extract is obtained by dissolving in water or other solvent using an emulsifier if necessary. If intended for oral administration, the ingredients used are selected from those that are pharmaceutically or food acceptable.

It is also possible to include a saw palmetto extract in common foods or cosmetics. Examples of such foods include general foods such as ice cream, strawberries, gums, confectionery, bread, noodles, and soft drinks such as alcoholic beverages, carbonated beverages, fruit juice beverages, lactic acid bacteria beverages, coffee, and tea. In addition, the saw palmetto extract can be ingested as a form of the above-mentioned dosage form or the like as a health supplement, a food for specified health use, or a nutritional functional food.
On the other hand, examples of cosmetics that can contain a saw palmetto extract include skin cosmetics such as soaps, facial cleansers, creams, emulsions, lotions, powders, perfumes, lipsticks, and cosmetics for baths, and hair such as shampoos and rinses. For cosmetics.

  EXAMPLES Hereinafter, although an Example demonstrates this invention in more detail, this invention is not limited to these.

Example 1: Nutritional supplement (soft capsule 1)
After weighing each component according to the formulation shown in Table 1 below, ganoderma extract, saw palmetto extract (commercial product; trade name: Saval Select; manufactured by Indena (Italy)), perilla oil, beeswax and glycerin fatty acid ester are mixed homogeneously. did. Thereafter, the mixed solution was encapsulated with a gelatin and glycerin film using an automatic rotary capsule filling machine as a content solution, and after drying, dietary supplement 1 (soft capsule) of the present invention was obtained.

Example 2: Nutritional supplement (soft capsule 2)
After weighing each component according to the formulation in Table 2 below, encapsulate with gelatin and glycerin film using an automatic rotary capsule filling machine with saw palmetto extract, soy isoflavone, yeast extract, ascorbic acid and zinc gluconate as the contents liquid After molding and drying, the nutritional supplement of the present invention (soft capsule 2) was obtained.

Example 3: Nutritional supplement (soft capsule 3)
After weighing each component in accordance with the composition shown in Table 3 below, it is encapsulated with a gelatin and glycerin film using an automatic rotary capsule filling machine with saw palmetto extract, catechin, royal jelly and hyaluronic acid as the contents liquid, dried, An inventive nutritional supplement (soft capsule 3) was obtained.

Example 4: Nutritional supplement (liquid)
Each component was weighed in accordance with the formulation shown in Table 4 below and mixed in a mixer until homogeneous, to obtain a dietary supplement (liquid preparation) of the present invention.

Example 5: Dietary supplement (tablets)
In accordance with the composition shown in Table 5 below, a commercially available saw palmetto extract and other additives are weighed, mixed in a fluid bed granulator for several minutes, granulated while spraying the granulation liquid, and dried at an air temperature of about 80 ° C. did. Thereafter, the obtained granule was tableted using a tableting machine to obtain a dietary supplement (tablet) of the present invention.

Example 6: Dietary supplement (granule)
Each component was weighed and mixed according to the formulation shown in Table 6 below. Next, the mixture is granulated using an extrusion granulator, dried using a hot air dryer at 45 ° C. so that the loss on drying is 7% or less, and then a male hormone-independent cancer preventive agent ( Granules) were obtained.

Example 7: Cancer preventive agent (semi-solid agent (ointment))
Each component was weighed according to the formulation shown in Table 7 below and mixed in a mixer until homogeneous, to obtain a cancer preventive agent (semi-solid agent (ointment)) of the present invention.

Example 8: Cancer preventive agent (solution (for oral administration))
Each component was weighed in accordance with the formulation shown in Table 8 below and mixed until homogenous in a mixer to obtain a male hormone-independent cancer preventive agent (solution (for oral administration)) of the present invention.

Example 9: Cancer preventive agent (tablet)
In accordance with the composition shown in Table 9 below, a commercially available saw palmetto extract and other additives are weighed, mixed in a fluid bed granulator for several minutes, granulated while spraying the granulation liquid, and dried at an air temperature of about 80 ° C. did. Thereafter, the obtained granule was tableted using a tableting machine to obtain the cancer preventive agent (tablet) of the present invention.

Example 10: Cancer preventive agent (granule)
Each component was weighed and mixed according to the formulation shown in Table 10 below. Next, the mixture is granulated using an extrusion granulator, dried using a hot air dryer at 45 ° C. so that the loss on drying is 7% or less, and then a male hormone-independent cancer preventive agent ( Granules) were obtained.

上記表１１及び図１の結果より、乳頭腫の発生率を見ると、対照群においては、ＴＰＡ塗布開始６週間後から乳頭腫の発生が確認され、そして１０週間後にはすべてのマウスに乳頭腫の発生が確認された。これに対して、実施例群においては、乳頭腫の発生が８週間後にまで抑制され、そして１０週間後においてもわずか１３．３％の発生率に抑制されていた。また、乳頭腫数を見ると、対照群においては、２０週間後には１匹当り平均９．１個もの乳頭腫が発生したのに対し、実施例群においては２０週間後においてもわずか平均４．０個にまで抑制された。 [Test Example 1: Skin cancer inhibitory effect of male hormone-independent prophylactic agent of the present invention]
The back of a 6 week old female ICR mouse was shaved and 100 μg DMBA was applied. Then, the cancer preventive agent of Example 7 was apply | coated to this DMBA application | coating site | part in the quantity used as 50 micrograms of saw palmetto extract. 1 hour later, in order to induce skin papilloma, 1 μg of phorbol ester (TPA) was applied to the DMBA application site, and then 50 μg of saw palmetto extract and 1 μg of TPA were similarly applied twice a week for 20 weeks. Subsequently, these mouse groups were designated as example groups. In addition, the mouse | mouth group which apply | coated the phorbol ester directly with respect to the DMBA application site | part without applying the cancer preventive agent of Example 7 was made into the control group. In each of the Example group and the control, after the second TPA application every week, the proportion of mice with papillomas (occurrence rate%) relative to all mice was determined, and it occurred at the DMBA application site per mouse. The average number of papillomas was determined. The results are shown in Table 11 below and FIG. 1 and FIG.

From the results shown in Table 11 and FIG. 1, when the incidence of papillomas is observed, in the control group, the occurrence of papillomas was confirmed after 6 weeks from the start of TPA application, and after 10 weeks all mice had papillomas. The occurrence of was confirmed. In contrast, in the example group, the occurrence of papillomas was suppressed up to 8 weeks later, and even after 10 weeks, the incidence was suppressed to only 13.3%. In addition, in terms of the number of papillomas, in the control group, an average of 9.1 papillomas per mouse occurred after 20 weeks, whereas in the example group, only an average of 4. It was suppressed to zero.

表１２を見ると、対照群においては、９３．３％（１５匹中１４匹）という非常に高い確率で肺腺腫が発生し、１個体当りの肺腺腫数は３．２個であった。これに対し、実施例群においては、肺腺腫が発生したマウスは５３．３％（１５匹中８匹）に抑制され、１個体当りの肺腺腫数もわずか０．８個であった。以上より、実施例群は肺腺腫の発生が効果的に予防されたことが判る。 [Test Example 2: Inhibition of carcinogenesis of lung cancer by male hormone-independent prophylactic agent of the present invention]
The back of 6 week old female ICR mice was injected with 4NQO at 10 mg / kg.
Five weeks later, a group of mice that were allowed to drink freely every day after mixing the male hormone-independent cancer preventive agent of Example 8 with glycerol mixed at a concentration of 8% by mass, and raised for another 25 weeks. Grouped. In addition, the mouse | mouth group which orally administered similarly the 8% glycerol aqueous solution which does not contain the male hormone independent cancer preventive agent was made into the control group. In each of the Example group and the Control group, 15 mice were tested, necropsied after completion of administration, the lungs were formalin-fixed, the total number of lung adenomas that occurred, the number of lung adenomas per individual, and mice that had lung adenomas The ratio (%) was obtained. The results are shown in Table 12 below.

Referring to Table 12, in the control group, lung adenomas occurred with a very high probability of 93.3% (14 of 15 animals), and the number of lung adenomas per animal was 3.2. On the other hand, in the Example group, 53.3% (8/15) of mice with lung adenoma were suppressed, and the number of lung adenoma per animal was only 0.8. From the above, it can be seen that the example group effectively prevented the occurrence of lung adenoma.

[Summary]
From the above results, it can be seen that the male hormone-independent cancer preventive agent of the present invention containing a saw palmetto extract can effectively prevent carcinogenesis. Furthermore, since the nutritional supplement of the present invention similarly contains a saw palmetto extract, it can be expected to prevent carcinogenesis.

The vertical axis shows the incidence (%) of papillomas, the horizontal axis shows the elapsed time (weeks) from the start of the test, the broken line connecting the triangles in the figure shows the test results of the examples, and the rectangles are connected The broken line is a graph showing the test results of the control. The vertical axis shows the number of tumors (pieces / mouse), the horizontal axis shows the elapsed time (weeks) from the start of the test, the broken line connecting the triangles in the figure shows the test results of the examples, and the broken line connecting the rectangular marks Is a graph showing the test results of controls.

Claims (6)

A dietary supplement for complementary therapy in the prevention of male hormone-independent cancer, which contains a saw palmetto extract. The dietary supplement according to claim 1, wherein the male hormone-independent cancer is skin cancer. The dietary supplement according to claim 1, wherein the male hormone-independent cancer is lung cancer. A male hormone-independent cancer preventive agent containing a saw palmetto extract. The said androgen-independent cancer preventive agent according to claim 4, wherein the androgen-independent cancer preventive agent prevents skin cancer. The said androgen-independent cancer preventive agent according to claim 4, wherein the androgen-independent cancer preventive agent prevents lung cancer.

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