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TWI873094B - Compositions for inhibiting proliferation of cancer cells, anticancer compositions, compositions for inhibiting canceration of normal cells, compositions for inhibiting the onset of cancer, and compositions for inducing cancer cell death - Google Patents

Compositions for inhibiting proliferation of cancer cells, anticancer compositions, compositions for inhibiting canceration of normal cells, compositions for inhibiting the onset of cancer, and compositions for inducing cancer cell death Download PDF

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TWI873094B
TWI873094B TW108115978A TW108115978A TWI873094B TW I873094 B TWI873094 B TW I873094B TW 108115978 A TW108115978 A TW 108115978A TW 108115978 A TW108115978 A TW 108115978A TW I873094 B TWI873094 B TW I873094B
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flavonol
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TW202003435A (en
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花房知夏
不破有沙
內尾隆正
川﨑健吾
室山幸太郎
室﨑伸二
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日商好侍健康食品股份有限公司
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Abstract

本發明之課題在於抑制細胞之癌化及癌症之惡化發展即癌症之發病、或誘導癌細胞之細胞死亡。 本發明提供一種含有薑黃酮醇A及薑黃酮醇B之至少1種作為有效成分之癌細胞之增殖抑制用組合物、抗癌用組合物、正常細胞之癌化抑制用組合物、癌症發病抑制用組合物、及癌細胞死亡誘導用組合物。The subject of the present invention is to inhibit the canceration of cells and the deterioration of cancer, i.e. the onset of cancer, or to induce cell death of cancer cells. The present invention provides a composition for inhibiting the proliferation of cancer cells, an anti-cancer composition, a composition for inhibiting the canceration of normal cells, a composition for inhibiting the onset of cancer, and a composition for inducing cancer cell death, which contains at least one of curcuminol A and curcuminol B as an effective ingredient.

Description

癌細胞之增殖抑制用組合物、抗癌用組合物、正常細胞之癌化抑制用組合物、癌症發病抑制用組合物、及癌細胞死亡誘導用組合物Compositions for inhibiting proliferation of cancer cells, anticancer compositions, compositions for inhibiting canceration of normal cells, compositions for inhibiting the onset of cancer, and compositions for inducing cancer cell death

本發明係關於一種癌細胞之增殖抑制用組合物、抗癌用組合物、正常細胞之癌化抑制用組合物、癌症發病抑制用組合物、及癌細胞死亡誘導用組合物。The present invention relates to a composition for inhibiting the proliferation of cancer cells, an anti-cancer composition, a composition for inhibiting the canceration of normal cells, a composition for inhibiting the onset of cancer, and a composition for inducing cancer cell death.

因癌症以致死亡之過程迄今為止被詳細解析而逐漸明瞭。目前,提出有被稱為多階段致癌之癌症之發展過程,其係指因化學物質、輻射、病毒之暴露導致基因受損,癌基因或癌抑制基因等複數種基因發生變異,細胞因該異常之累積而癌化,於獲得細胞增殖等各種異常性質之後,獲得浸潤、轉移及復發等能力而惡性度進一步增加(惡化發展)以致死亡。因此,認為抑制因化學物質、輻射、病毒誘導性之基因變異所引發之細胞癌化對於預防癌症發生較為重要,而抑制癌細胞之增殖、浸潤、轉移則對於抑制癌症惡化發展較為重要。The process of death from cancer has been analyzed in detail and gradually clarified. Currently, a process of cancer development called multi-stage carcinogenesis is proposed, which refers to the accumulation of abnormalities in cells, which lead to gene damage due to exposure to chemicals, radiation, and viruses, and mutations in multiple genes such as oncogenes or tumor suppressor genes. After acquiring various abnormal properties such as cell proliferation, the cancer acquires the ability to invade, metastasize, and relapse, and its malignancy further increases (malignant development) and leads to death. Therefore, it is believed that inhibiting cell carcinogenesis caused by chemical, radiation, and virus-induced gene mutations is more important for preventing cancer, while inhibiting the proliferation, infiltration, and metastasis of cancer cells is more important for inhibiting the progression of cancer malignancy.

專利文獻1中記載有一種將自薑黃之根莖單離出之蛋白結合多糖體作為有效成分之抗腫瘤劑。Patent document 1 describes an anti-tumor agent having a protein-bound polysaccharide isolated from the rhizome of turmeric as an active ingredient.

另一方面,薑黃酮醇(Turmeronol)A及薑黃酮醇B係自薑黃單離且結構已確定之已知成分(非專利文獻1)。非專利文獻1中報告稱薑黃酮醇A具有抑制大豆脂肪加氧酶之酵素活性之作用與抗氧化作用。 [先前技術文獻] [專利文獻]On the other hand, turmeronol A and turmeronol B are known components isolated from turmeric and their structures have been determined (non-patent document 1). Non-patent document 1 reports that turmeronol A has the effect of inhibiting the enzymatic activity of soybean lipoxygenase and has an antioxidant effect. [Prior technical document] [Patent document]

專利文獻1:日本專利特開昭60-67428號公報 [非專利文獻]Patent document 1: Japanese Patent Publication No. 60-67428 [Non-patent document]

非專利文獻1:Agric Biol Chem. 1990; 54 (9): 2367-71Non-patent literature 1: Agric Biol Chem. 1990; 54 (9): 2367-71

[發明所欲解決之問題][The problem the invention is trying to solve]

專利文獻1中對自薑黃之根莖單離出之蛋白結合多糖體之作用進行了記載,非專利文獻1中對薑黃酮醇A之抗氧化作用進行了記載,但該等文獻中並未對源自薑黃之薑黃酮醇A及薑黃酮醇B抑制細胞之癌化及癌症之惡化發展即癌症之發病、或誘導癌細胞死亡之情況進行記載。Patent document 1 describes the effects of protein-bound polysaccharides isolated from the rhizome of turmeric, and non-patent document 1 describes the antioxidant effects of turmeric flavonol A. However, these documents do not describe the effects of turmeric flavonol A and turmeric flavonol B derived from turmeric on inhibiting cell carcinogenesis and cancer metastasis, i.e., the onset of cancer, or inducing cancer cell death.

因此,本發明提供一種用以抑制細胞之癌化及癌症之惡化發展即癌症之發病之方法、或用以誘導癌細胞死亡之方法。 [解決問題之技術手段]Therefore, the present invention provides a method for inhibiting the canceration of cells and the deterioration of cancer, i.e. the onset of cancer, or a method for inducing cancer cell death. [Technical means for solving the problem]

本發明人等發現,薑黃酮醇A及薑黃酮醇B可抑制細胞之癌化及癌症之惡化發展即癌症之發病,或可誘導癌細胞死亡,從而完成了以下之本發明。 (1)一種癌細胞之增殖抑制用組合物,其含有薑黃酮醇A及薑黃酮醇B之至少1種作為有效成分。 (2)如(1)所記載之癌細胞之增殖抑制用組合物,其中上述癌細胞係大腸癌細胞。 (3)一種抗癌用組合物,其含有薑黃酮醇A及薑黃酮醇B之至少1種作為有效成分。 (4)如(3)所記載之抗癌用組合物,其係針對大腸癌之抗癌用組合物。 (5)一種正常細胞之癌化抑制用組合物,其含有薑黃酮醇A及薑黃酮醇B之至少1種作為有效成分。 (6)如(5)所記載之正常細胞之癌化抑制用組合物,其抑制正常細胞向大腸癌之癌化。 (7)一種癌症發病抑制用組合物,其含有薑黃酮醇A及薑黃酮醇B之至少1種作為有效成分。 (8)如(7)所記載之癌症發病抑制用組合物,其係針對大腸癌之癌症發病抑制用組合物。 (9)一種癌細胞死亡誘導用組合物,其含有薑黃酮醇A及薑黃酮醇B之至少1種作為有效成分。 (10)如(9)所記載之癌細胞死亡誘導用組合物,其中上述癌細胞係大腸癌細胞。The inventors of the present invention have found that curcuminol A and curcuminol B can inhibit the carcinogenesis of cells and the deterioration of cancer, i.e. the onset of cancer, or can induce cancer cell death, thereby completing the following present invention. (1) A composition for inhibiting the proliferation of cancer cells, which contains at least one of curcuminol A and curcuminol B as an active ingredient. (2) A composition for inhibiting the proliferation of cancer cells as described in (1), wherein the cancer cells are colorectal cancer cells. (3) An anticancer composition, which contains at least one of curcuminol A and curcuminol B as an active ingredient. (4) The anticancer composition as described in (3), which is an anticancer composition for colorectal cancer. (5) A composition for inhibiting the carcinogenesis of normal cells, which contains at least one of curcuminol A and curcuminol B as an active ingredient. (6) A composition for inhibiting the carcinogenesis of normal cells as described in (5), which inhibits the carcinogenesis of normal cells into colorectal cancer. (7) A composition for inhibiting the onset of cancer, which contains at least one of curcuminol A and curcuminol B as an active ingredient. (8) A composition for inhibiting the onset of cancer as described in (7), which is a composition for inhibiting the onset of cancer for colorectal cancer. (9) A composition for inducing cancer cell death, which contains at least one of curcuminol A and curcuminol B as an active ingredient. (10) The cancer cell death-inducing composition as described in (9), wherein the cancer cells are colorectal cancer cells.

(11)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造癌細胞之增殖抑制用組合物。 (12)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造癌細胞之增殖抑制用醫藥。 (13)一種抑制癌細胞之增殖之方法,其包括: 將薑黃酮醇A及薑黃酮醇B之至少1種於生物體內或生物體外投予至癌細胞;及 抑制上述癌細胞之增殖。 (14)一種薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其用以於生物體內或生物體外抑制癌細胞之增殖。 (15)如(11)所記載之用途、如(12)所記載之用途、如(13)所記載之方法、或如(14)所記載之薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其中上述癌細胞係大腸癌細胞。(11) A use of at least one of turmeric flavonol A and turmeric flavonol B, wherein at least one of turmeric flavonol A and turmeric flavonol B is used to produce a composition for inhibiting the proliferation of cancer cells. (12) A use of at least one of turmeric flavonol A and turmeric flavonol B, wherein at least one of turmeric flavonol A and turmeric flavonol B is used to produce a drug for inhibiting the proliferation of cancer cells. (13) A method for inhibiting the proliferation of cancer cells, comprising: administering at least one of turmeric flavonol A and turmeric flavonol B to cancer cells in vivo or in vitro; and inhibiting the proliferation of the above cancer cells. (14) A turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B, which is used to inhibit the proliferation of cancer cells in vivo or in vitro. (15) The use described in (11), the use described in (12), the method described in (13), or the turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B described in (14), wherein the cancer cells are colorectal cancer cells.

(16)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造抗癌用組合物。 (17)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造抗癌用醫藥。 (18)一種治療癌症之方法,其包括: 將薑黃酮醇A及薑黃酮醇B之至少1種投予至需要癌症治療之患者;及 於上述患者中治療癌症。 (19)一種薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其係用以於需要癌症治療之患者中治療癌症。 (20)如(16)所記載之用途、如(17)所記載之用途、如(18)所記載之方法、或如(19)所記載之薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其中上述癌係大腸癌。(16) A use of at least one of turmeric flavonol A and turmeric flavonol B, which is to use at least one of turmeric flavonol A and turmeric flavonol B to prepare an anti-cancer composition. (17) A use of at least one of turmeric flavonol A and turmeric flavonol B, which is to use at least one of turmeric flavonol A and turmeric flavonol B to prepare an anti-cancer drug. (18) A method for treating cancer, comprising: Administering at least one of turmeric flavonol A and turmeric flavonol B to a patient in need of cancer treatment; and Treatment of cancer in the above patient. (19) A turmericflavonol A, turmericflavonol B, or a mixture of turmericflavonol A and turmericflavonol B, which is used to treat cancer in a patient in need of cancer treatment. (20) The use described in (16), the use described in (17), the method described in (18), or the turmericflavonol A, turmericflavonol B, or a mixture of turmericflavonol A and turmericflavonol B described in (19), wherein the above-mentioned cancer is colorectal cancer.

(21)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造正常細胞之癌化抑制用組合物。 (22)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造正常細胞之癌化抑制用醫藥。 (23)一種抑制正常細胞之癌化之方法,其包括: 將薑黃酮醇A及薑黃酮醇B之至少1種於生物體內或生物體外投予至正常細胞;及 抑制上述正常細胞之癌化。 (24)一種薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其係用以於生物體內或生物體外抑制正常細胞之癌化。 (25)如(21)所記載之用途、如(22)所記載之用途、如(23)所記載之方法、或如(24)所記載之薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其中上述癌化係向大腸癌之癌化。(21) A use of at least one of turmeric flavonol A and turmeric flavonol B, wherein at least one of turmeric flavonol A and turmeric flavonol B is used to produce a composition for inhibiting the carcinogenesis of normal cells. (22) A use of at least one of turmeric flavonol A and turmeric flavonol B, wherein at least one of turmeric flavonol A and turmeric flavonol B is used to produce a drug for inhibiting the carcinogenesis of normal cells. (23) A method for inhibiting the carcinogenesis of normal cells, comprising: administering at least one of turmeric flavonol A and turmeric flavonol B to normal cells in vivo or in vitro; and inhibiting the carcinogenesis of the above normal cells. (24) A turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B, which is used to inhibit the carcinogenesis of normal cells in vivo or in vitro. (25) The use described in (21), the use described in (22), the method described in (23), or the turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B described in (24), wherein the above-mentioned carcinogenesis is carcinogenesis of colorectal cancer.

(26)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造癌症發病抑制用組合物。 (27)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造癌症發病抑制用醫藥。 (28)一種抑制癌症發病之方法,其包括: 將薑黃酮醇A及薑黃酮醇B之至少1種投予至需要抑制癌症發病之患者;及 於上述患者中抑制癌症發病。 (29)一種薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其係用以於需要抑制癌症發病之患者中抑制癌症發病。 (30)如(26)所記載之用途、如(27)所記載之用途、如(28)所記載之方法、或如(29)所記載之薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其中上述癌係大腸癌。(26) A use of at least one of turmeric flavonol A and turmeric flavonol B, which is to use at least one of turmeric flavonol A and turmeric flavonol B to produce a composition for inhibiting the onset of cancer. (27) A use of at least one of turmeric flavonol A and turmeric flavonol B, which is to use at least one of turmeric flavonol A and turmeric flavonol B to produce a drug for inhibiting the onset of cancer. (28) A method for inhibiting the onset of cancer, comprising: Administering at least one of turmeric flavonol A and turmeric flavonol B to a patient who needs to inhibit the onset of cancer; and Inhibiting the onset of cancer in the above patient. (29) A turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B, which is used to inhibit the onset of cancer in a patient in need of inhibiting the onset of cancer. (30) The use described in (26), the use described in (27), the method described in (28), or the turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B described in (29), wherein the above-mentioned cancer is colorectal cancer.

(31)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造癌細胞死亡誘導用組合物。 (32)一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係將薑黃酮醇A及薑黃酮醇B之至少1種用於製造癌細胞死亡誘導用醫藥。 (33)一種誘導癌細胞之細胞死亡之方法,其包括: 將薑黃酮醇A及薑黃酮醇B之至少1種於生物體內或生物體外投予至癌細胞;及 誘導上述癌細胞之細胞死亡。 (34)一種薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其係用以於生物體內或生物體外誘導癌細胞之細胞死亡。 (35)如(31)所記載之用途、如(32)所記載之用途、如(33)所記載之方法、或如(34)所記載之薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其中上述癌細胞係大腸癌細胞。(31) A use of at least one of turmeric flavonol A and turmeric flavonol B, wherein at least one of turmeric flavonol A and turmeric flavonol B is used to produce a composition for inducing cancer cell death. (32) A use of at least one of turmeric flavonol A and turmeric flavonol B, wherein at least one of turmeric flavonol A and turmeric flavonol B is used to produce a drug for inducing cancer cell death. (33) A method for inducing cell death of cancer cells, comprising: administering at least one of turmeric flavonol A and turmeric flavonol B to cancer cells in vivo or in vitro; and inducing cell death of the above cancer cells. (34) A turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B, which is used to induce cell death of cancer cells in vivo or in vitro. (35) The use described in (31), the use described in (32), the method described in (33), or the turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B described in (34), wherein the cancer cells are colorectal cancer cells.

本說明書包含成為本申請案之優先權之基礎之日本專利申請編號2018-093848號之揭示內容。 [發明之效果]This specification contains the disclosure contents of Japanese Patent Application No. 2018-093848, which is the basis for the priority of this application. [Effect of the invention]

本發明提供一種將薑黃酮醇A及薑黃酮醇B之至少1種作為有效成分之癌細胞之增殖抑制用組合物、抗癌用組合物、正常細胞之癌化抑制用組合物、癌症發病抑制用組合物、及癌細胞死亡誘導用組合物。The present invention provides a composition for inhibiting the proliferation of cancer cells, an anti-cancer composition, a composition for inhibiting the cancerization of normal cells, a composition for inhibiting the onset of cancer, and a composition for inducing cancer cell death, which contains at least one of curcuminol A and curcuminol B as an active ingredient.

<有效成分> 薑黃酮醇A及薑黃酮醇B係分別具有以下之平面結構之化合物。<Active ingredients> Turmeric flavonol A and turmeric flavonol B are compounds with the following planar structures.

[化1] [Chemistry 1]

[化2] [Chemistry 2]

眾所周知,自薑黃分離出之天然之薑黃酮醇A、薑黃酮醇B分別於2-甲基-2-庚烯-4-酮之部分結構中之碳6位置之立體組態係S型。然而,本發明中可使用之薑黃酮醇A、薑黃酮醇B只要係分別具有上述平面結構者即可,並不限於源自薑黃之立體結構之薑黃酮醇A、薑黃酮醇B,較佳為源自薑黃之立體結構之薑黃酮醇A、薑黃酮醇B。於本發明中,可使用鹽、水合物等各種形態之薑黃酮醇A、薑黃酮醇B。作為鹽之形態之薑黃酮醇A、薑黃酮醇B,只要為藥學上容許之鹽則並無特別限定,例如可列舉鈉鹽(酚性羥基之鈉鹽)。As is well known, the stereo configuration of natural turmeric flavonol A and turmeric flavonol B separated from turmeric is S-type at the carbon 6 position in the partial structure of 2-methyl-2-heptene-4-one. However, the turmeric flavonol A and turmeric flavonol B that can be used in the present invention can be any turmeric flavonol A and turmeric flavonol B as long as they have the above-mentioned planar structure, and are not limited to the turmeric flavonol A and turmeric flavonol B derived from the stereo structure of turmeric, and preferably the turmeric flavonol A and turmeric flavonol B derived from the stereo structure of turmeric. In the present invention, turmeric flavonol A and turmeric flavonol B in various forms such as salts and hydrates can be used. The salt form of curcuminol A and curcuminol B is not particularly limited as long as it is a pharmaceutically acceptable salt, and an example thereof is sodium salt (sodium salt of phenolic hydroxyl group).

於本發明之各態樣中,有效成分係薑黃酮醇A及薑黃酮醇B之至少1種。即,上述有效成分可為僅由薑黃酮醇A構成者,可為僅由薑黃酮醇B構成者,亦可為薑黃酮醇A與薑黃酮醇B之混合物。In each aspect of the present invention, the active ingredient is at least one of turmeric flavonol A and turmeric flavonol B. That is, the active ingredient may be composed of only turmeric flavonol A, may be composed of only turmeric flavonol B, or may be a mixture of turmeric flavonol A and turmeric flavonol B.

本發明中所使用之有效成分可為源自植物者,亦可為人工合成者。例如光學活性之(+)-薑黃酮醇A可藉由Biosci Biotechnol Biochem.1993;57(7):1137-40所記載之方法合成。The active ingredients used in the present invention may be derived from plants or may be artificially synthesized. For example, optically active (+)-curcuminol A can be synthesized by the method described in Biosci Biotechnol Biochem. 1993; 57(7): 1137-40.

本發明中所使用之有效成分更佳為源自植物原料者,更佳為源自薑科薑黃屬植物者。作為薑科薑黃屬植物,可列舉薑黃(Curcuma longa)、郁金(Curcuma aromatica)、莪術(Curcuma zedoaria)、蓬莪術(Curcuma phaeocaulis)、廣西莪術(Curcuma kwangsiensis)、溫郁金(Curcuma wenyujin)、黃紅薑黃(Curcuma xanthorrhiza),尤佳為薑黃(Curcuma longa)。可自薑科薑黃屬植物之根莖等部位獲取薑黃酮醇A及薑黃酮醇B。根莖可使用采自土中者,亦可使用將根莖之適當部位保持原型、或截斷為適當之尺寸或形狀者,或製成粉碎物之形態者。植物原料亦可為經適宜乾燥者。The active ingredients used in the present invention are preferably derived from plant materials, and more preferably from plants of the genus Curcuma in the family Curcumae. Examples of plants of the genus Curcuma in the family Curcumae include Curcuma longa, Curcuma aromatica, Curcuma zedoaria, Curcuma phaeocaulis, Curcuma kwangsiensis, Curcuma wenyujin, and Curcuma xanthorrhiza, and Curcuma longa is particularly preferred. Curcuma flavonol A and curcuma flavonol B can be obtained from the rhizome and other parts of plants of the genus Curcuma in the family Curcumae. The rhizomes may be collected from the soil, or the appropriate parts of the rhizomes may be kept in their original form, or cut into appropriate sizes or shapes, or made into a powdered form. The plant material may also be suitably dried.

本發明中所使用之選自薑黃酮醇A及薑黃酮醇B中之至少1種化合物可為含有其之植物或植物加工品之形態、自植物或植物加工品中提取之提取物之形態、由上述提取物製備之提高了上述化合物之純度之區分的形態、自上述提取物或區分中單離之上述化合物之形態等任意形態。At least one compound selected from curcuminol A and curcuminol B used in the present invention may be in any form, such as a plant or plant processed product containing the compound, an extract extracted from the plant or plant processed product, a fraction prepared from the extract with improved purity of the compound, or a compound isolated from the extract or fraction.

作為包含選自源自植物或植物加工品之薑黃酮醇A及薑黃酮醇B中之至少1種之提取物之製備中所使用之提取溶劑,可例示選自由水、極性有機溶劑及非極性有機溶劑所組成之群中之至少1種、或超臨界二氧化碳等超臨界流體。作為選自由水、極性有機溶劑及非極性有機溶劑所組成之群中之至少1種提取溶劑,可列舉水、極性有機溶劑、水與極性有機溶劑之混合溶劑、非極性有機溶劑等。極性有機溶劑亦可為複數種極性有機溶劑之混合溶劑。非極性有機溶劑亦可為複數種非極性有機溶劑之混合溶劑。所謂「水」亦包含熱水。作為熱水,例如可使用95℃以上之熱水。作為極性有機溶劑,可列舉至少1種醇(亦可為複數種醇之混合溶劑),作為醇,並無特別限定,較佳為甲醇、乙醇。於將醇與水之混合溶劑用作提取溶劑之情形時之混合比並無特別限定,例如以重量比計較佳為10:90~90:10之範圍,更佳為20:80~50:50之範圍。選自源自植物或植物加工品之薑黃酮醇A及薑黃酮醇B中之至少1種之提取方法並無特別限定。包含選自薑黃酮醇A及薑黃酮醇B中之至少1種之提取物根據需要使提取溶劑揮發去除後使用。As an extraction solvent used in the preparation of an extract containing at least one selected from turmeric flavonol A and turmeric flavonol B derived from plants or plant processed products, at least one selected from the group consisting of water, polar organic solvents and non-polar organic solvents, or a supercritical fluid such as supercritical carbon dioxide can be exemplified. As at least one extraction solvent selected from the group consisting of water, polar organic solvents and non-polar organic solvents, water, polar organic solvents, mixed solvents of water and polar organic solvents, non-polar organic solvents, etc. can be listed. The polar organic solvent can also be a mixed solvent of a plurality of polar organic solvents. The non-polar organic solvent may also be a mixed solvent of a plurality of non-polar organic solvents. The so-called "water" also includes hot water. As hot water, for example, hot water above 95°C may be used. As the polar organic solvent, at least one alcohol (or a mixed solvent of a plurality of alcohols) may be cited. As the alcohol, there is no particular limitation, and methanol and ethanol are preferred. When a mixed solvent of alcohol and water is used as an extraction solvent, the mixing ratio is not particularly limited. For example, the weight ratio is preferably in the range of 10:90 to 90:10, and more preferably in the range of 20:80 to 50:50. The extraction method of at least one of turmeric flavonol A and turmeric flavonol B selected from plants or plant processed products is not particularly limited. The extract containing at least one selected from turmeric flavonol A and turmeric flavonol B is used after the extraction solvent is evaporated and removed as needed.

由上述提取物製備提高了選自薑黃酮醇A及薑黃酮醇B中之至少1種之純度之區分的方法並無特別限定,例如可例示:將包含選自薑黃酮醇A及薑黃酮醇B中之至少1種化合物之提取物供於乙酸乙酯/水之液-液分佈,於乙酸乙酯區分中將上述化合物高純度化之方法;將上述提取物或區分供於管柱層析法等層析法而將上述化合物高純度化之方法。作為層析法,可使用逆相管柱層析法、正相薄層層析法等。The method for preparing a fraction having a higher purity of at least one compound selected from turmeric flavonol A and turmeric flavonol B from the extract is not particularly limited, and examples thereof include: subjecting the extract containing at least one compound selected from turmeric flavonol A and turmeric flavonol B to liquid-liquid separation of ethyl acetate/water, and purifying the compound to a higher degree in ethyl acetate fractionation; and subjecting the extract or fraction to a chromatography method such as column chromatography to purify the compound to a higher degree. As the chromatography method, reverse phase column chromatography, normal phase thin layer chromatography, etc. can be used.

自上述提取物或區分中單離選自薑黃酮醇A及薑黃酮醇B中之至少1種化合物之方法並無特別限定,可使用利用層析法等方法單離上述化合物之方法。The method for isolating at least one compound selected from curcuminol A and curcuminol B from the extract or fraction is not particularly limited, and a method for isolating the compound by chromatography or the like can be used.

選自薑黃酮醇A及薑黃酮醇B中之至少1種化合物、包含上述化合物之植物或植物加工品、或者包含上述化合物之植物或植物加工品之提取物或區分亦可為藉由常規方法,實施乾燥、粉末化、顆粒化、溶液化等加工而成者。At least one compound selected from curcuminol A and curcuminol B, a plant or plant processed product containing the above compound, or an extract or fraction of a plant or plant processed product containing the above compound can also be processed by drying, powdering, granulating, solubilizing, etc. by conventional methods.

<癌細胞之增殖抑制用組合物、抗癌用組合物、正常細胞之癌化抑制用組合物、癌症發病抑制用組合物、癌細胞死亡誘導用組合物> 本發明之第一態樣係關於一種癌細胞之增殖抑制用組合物,其含有選自薑黃酮醇A及薑黃酮醇B中之至少1種作為有效成分。本發明之癌細胞之增殖抑制用組合物較佳為大腸癌細胞之增殖抑制用組合物。又,本發明之第一態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造癌細胞之增殖抑制用組合物。又,本發明之第一態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造癌細胞之增殖抑制用醫藥。又,本發明之第一態樣係關於一種抑制癌細胞之增殖之方法,其包括:將選自薑黃酮醇A及薑黃酮醇B中之至少1種於生物體內或生物體外投予至癌細胞;及抑制上述癌細胞之增殖。又,本發明之第一態樣係關於一種薑黃酮醇A、薑黃酮醇B、或薑黃酮醇A與薑黃酮醇B之混合物,其係用以於生物體內或生物體外抑制癌細胞之增殖。<Composition for inhibiting proliferation of cancer cells, anti-cancer composition, composition for inhibiting canceration of normal cells, composition for inhibiting the onset of cancer, composition for inducing cancer cell death> The first aspect of the present invention is a composition for inhibiting proliferation of cancer cells, which contains at least one selected from turmeric flavonol A and turmeric flavonol B as an active ingredient. The composition for inhibiting proliferation of cancer cells of the present invention is preferably a composition for inhibiting proliferation of colorectal cancer cells. In addition, the first aspect of the present invention is a use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a composition for inhibiting proliferation of cancer cells. Furthermore, the first aspect of the present invention is related to a use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a drug for inhibiting the proliferation of cancer cells. Furthermore, the first aspect of the present invention is related to a method for inhibiting the proliferation of cancer cells, which comprises: administering at least one selected from turmeric flavonol A and turmeric flavonol B to cancer cells in vivo or in vitro; and inhibiting the proliferation of the above cancer cells. Furthermore, the first aspect of the present invention is related to a turmeric flavonol A, turmeric flavonol B, or a mixture of turmeric flavonol A and turmeric flavonol B, which is used to inhibit the proliferation of cancer cells in vivo or in vitro.

本發明之第二態樣係關於一種抗癌用組合物,其含有選自薑黃酮醇A及薑黃酮醇B中之至少1種作為有效成分。本發明之抗癌用組合物較佳為針對大腸癌之抗癌用組合物。又,本發明之第二態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造抗癌用組合物。又,本發明之第二態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造抗癌用醫藥。又,本發明之第二態樣係關於一種治療癌症之方法,其包括:將選自薑黃酮醇A及薑黃酮醇B中之至少1種投予至需要癌症治療之患者;及於上述患者中治療癌症。又,本發明之第二態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種,其係用以於需要癌症治療之患者中治療癌症。The second aspect of the present invention is related to an anticancer composition, which contains at least one selected from turmeric flavonol A and turmeric flavonol B as an active ingredient. The anticancer composition of the present invention is preferably an anticancer composition for colorectal cancer. In addition, the second aspect of the present invention is related to the use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to prepare an anticancer composition. In addition, the second aspect of the present invention is related to the use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to prepare an anticancer drug. In addition, the second aspect of the present invention is related to a method for treating cancer, comprising: administering at least one selected from turmeric flavonol A and turmeric flavonol B to a patient in need of cancer treatment; and treating cancer in the patient. In addition, the second aspect of the present invention is related to at least one selected from turmeric flavonol A and turmeric flavonol B, which is used to treat cancer in a patient in need of cancer treatment.

本發明之第三態樣係關於一種正常細胞之癌化抑制用組合物,其含有選自薑黃酮醇A及薑黃酮醇B中之至少1種作為有效成分。本發明之正常細胞之癌化抑制用組合物較佳為抑制正常細胞向大腸癌之癌化。又,本發明之第三態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造正常細胞之癌化抑制用組合物。又,本發明之第三態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造正常細胞之癌化抑制用醫藥。又,本發明之第三態樣係關於一種抑制正常細胞之癌化之方法,其包括:將選自薑黃酮醇A及薑黃酮醇B中之至少1種於生物體內或生物體外投予至正常細胞;及抑制上述正常細胞之癌化。又,本發明之第三態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種,其係用以於生物體內或生物體外抑制正常細胞之癌化。The third aspect of the present invention is a composition for inhibiting the canceration of normal cells, which contains at least one selected from turmeric flavonol A and turmeric flavonol B as an active ingredient. The composition for inhibiting the canceration of normal cells of the present invention is preferably used to inhibit the canceration of normal cells into colorectal cancer. In addition, the third aspect of the present invention is a use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a composition for inhibiting the canceration of normal cells. Furthermore, the third aspect of the present invention is related to a use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a drug for inhibiting the canceration of normal cells. Furthermore, the third aspect of the present invention is related to a method for inhibiting the canceration of normal cells, which comprises: administering at least one selected from turmeric flavonol A and turmeric flavonol B to normal cells in vivo or in vitro; and inhibiting the canceration of the above normal cells. Furthermore, the third aspect of the present invention is related to at least one selected from turmeric flavonol A and turmeric flavonol B, which is used to inhibit the canceration of normal cells in vivo or in vitro.

本發明之第四態樣係關於一種癌症發病抑制用組合物,其含有選自薑黃酮醇A及薑黃酮醇B中之至少1種作為有效成分。本發明之癌症發病抑制用組合物較佳為針對大腸癌之癌症發病抑制用組合物。又,本發明之第四態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造癌症發病抑制用組合物。又,本發明之第四態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造癌症發病抑制用醫藥。又,本發明之第四態樣係關於一種抑制癌症發病之方法,其包括:將選自薑黃酮醇A及薑黃酮醇B中之至少1種投予至需要抑制癌症發病之患者;及於上述患者中抑制癌症發病。又,本發明之第四態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種,其係用以於需要抑制癌症發病之患者中抑制癌症發病。The fourth aspect of the present invention is related to a composition for inhibiting the onset of cancer, which contains at least one selected from turmeric flavonol A and turmeric flavonol B as an active ingredient. The composition for inhibiting the onset of cancer of the present invention is preferably a composition for inhibiting the onset of cancer for colorectal cancer. In addition, the fourth aspect of the present invention is related to the use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a composition for inhibiting the onset of cancer. In addition, the fourth aspect of the present invention is related to the use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a medicine for inhibiting the onset of cancer. In addition, the fourth aspect of the present invention is related to a method for inhibiting the onset of cancer, which comprises: administering at least one selected from turmeric flavonol A and turmeric flavonol B to a patient in need of inhibiting the onset of cancer; and inhibiting the onset of cancer in the patient. In addition, the fourth aspect of the present invention is related to at least one selected from turmeric flavonol A and turmeric flavonol B, which is used to inhibit the onset of cancer in a patient in need of inhibiting the onset of cancer.

本發明之第五態樣係關於一種癌細胞死亡誘導用組合物,其含有選自薑黃酮醇A及薑黃酮醇B中之至少1種作為有效成分。本發明之癌細胞死亡誘導用組合物較佳為大腸癌細胞之細胞死亡誘導用組合物。又,本發明之第五態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造癌細胞死亡誘導用組合物。又,本發明之第五態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種之用途,其係將選自薑黃酮醇A及薑黃酮醇B中之至少1種用於製造癌細胞死亡誘導用醫藥。又,本發明之第五態樣係關於一種誘導癌細胞之細胞死亡之方法,其包括:將選自薑黃酮醇A及薑黃酮醇B中之至少1種於生物體內或生物體外投予至癌細胞;及誘導上述癌細胞之細胞死亡。又,本發明之第五態樣係關於一種選自薑黃酮醇A及薑黃酮醇B中之至少1種,其係用以於生物體內或生物體外誘導癌細胞之細胞死亡。The fifth aspect of the present invention is related to a cancer cell death-inducing composition, which contains at least one selected from turmeric flavonol A and turmeric flavonol B as an active ingredient. The cancer cell death-inducing composition of the present invention is preferably a cell death-inducing composition for colorectal cancer cells. In addition, the fifth aspect of the present invention is related to a use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a cancer cell death-inducing composition. Furthermore, the fifth aspect of the present invention is related to a use of at least one selected from turmeric flavonol A and turmeric flavonol B, which is to use at least one selected from turmeric flavonol A and turmeric flavonol B to produce a drug for inducing cancer cell death. Furthermore, the fifth aspect of the present invention is related to a method for inducing cell death of cancer cells, which comprises: administering at least one selected from turmeric flavonol A and turmeric flavonol B to cancer cells in vivo or in vitro; and inducing cell death of the above cancer cells. Furthermore, the fifth aspect of the present invention is related to at least one selected from turmeric flavonol A and turmeric flavonol B, which is used to induce cell death of cancer cells in vivo or in vitro.

本發明中所使用之上述有效成分或含有其之組合物或醫藥可為醫藥品、飲食品、飼料、食品添加劑、飼料添加劑等各形態之組合物,更佳為醫藥品或飲食品。飲食品亦包含功能性表示食品、特定保健用食品、用於營養補充之補充品等形態者。本發明中所使用之含有上述有效成分之組合物或醫藥較佳為藉由經口或經鼻攝取或投予之組合物之形態,更佳為藉由經口攝取或投予之組合物之形態。The above-mentioned active ingredients or compositions or drugs containing the same used in the present invention may be compositions in various forms such as pharmaceuticals, beverages, feeds, food additives, feed additives, etc., and are more preferably pharmaceuticals or beverages. Beverages also include functional foods, specific health foods, and supplements for nutritional supplements. The compositions or drugs containing the above-mentioned active ingredients used in the present invention are preferably in the form of compositions that are taken orally or nasally, and are more preferably in the form of compositions that are taken orally.

本發明之一實施形態之包含上述化合物之組合物或醫藥每1日之攝取或投予量較佳為針對1人、尤其是針對1成人之每1日之攝取或投予量以薑黃酮醇A及薑黃酮醇B之合計量成為100 μg以上之方式含有選自薑黃酮醇A及薑黃酮醇B中之至少1種。本發明之另一實施形態之包含上述有效成分之組合物或醫藥每1日之攝取或投予量較佳為針對1人、尤其是針對1成人之每1日之攝取或投予量以薑黃酮醇A成為80 μg以上、及/或薑黃酮醇B成為20 μg以上之方式,更佳為以薑黃酮醇A成為80 μg以上、及薑黃酮醇B成為20 μg以上之方式含有選自薑黃酮醇A及薑黃酮醇B中之至少1種。根據該等實施形態,可有效地獲得癌細胞增殖抑制作用、抗癌作用、正常細胞之癌化抑制作用、癌症發病抑制作用、或癌細胞死亡誘導作用。此處所謂「1日之攝取或投予量」係指於藉由經口或經鼻、較佳為藉由經口攝取或投予之情形時,典型而言以本發明之組合物之量計為0.1 g~500 g。本發明中所使用之上述有效成分或含有其之組合物或醫藥可連續地攝取或投予,亦可於必要時攝取或投予而使用。The composition or medicine containing the above-mentioned compound in one embodiment of the present invention preferably contains at least one selected from turmeric flavonol A and turmeric flavonol B in a daily intake or administration amount for one person, especially for one adult, such that the total amount of turmeric flavonol A and turmeric flavonol B is 100 μg or more. In another embodiment of the present invention, the composition or medicine containing the above-mentioned active ingredient is preferably taken or administered in a daily amount for one person, especially for one adult, such that turmeric flavonol A becomes 80 μg or more and/or turmeric flavonol B becomes 20 μg or more, and more preferably, turmeric flavonol A becomes 80 μg or more and turmeric flavonol B becomes 20 μg or more, and contains at least one selected from turmeric flavonol A and turmeric flavonol B. According to these embodiments, cancer cell proliferation inhibition, anti-cancer effect, normal cell cancerization inhibition, cancer pathogenesis inhibition, or cancer cell death induction effect can be effectively obtained. The "daily intake or administration amount" referred to herein refers to the amount of the composition of the present invention, typically 0.1 g to 500 g, when taken or administered orally or nasally, preferably orally. The above-mentioned active ingredient or the composition or medicine containing the same used in the present invention can be taken or administered continuously or when necessary.

本發明中所使用之上述有效成分或含有其之組合物或醫藥可為上述有效成分本身,亦可為包含上述有效成分與至少1種其他成分者。於本發明中所使用之上述有效成分或含有其之組合物或醫藥包含上述有效成分與至少1種其他成分之情形時,可為將上述有效成分與至少1種其他成分混合而成之組合物,可為利用適當之方法將上述有效成分與至少1種其他成分製劑化而成之組合物,亦可為將上述有效成分與至少1種其他成分製劑化而成之組合物進而與其他成分混合而成之組合物。The above-mentioned active ingredient or the composition or medicine containing the same used in the present invention may be the above-mentioned active ingredient itself, or may be a composition containing the above-mentioned active ingredient and at least one other ingredient. When the above-mentioned active ingredient or the composition or medicine containing the same used in the present invention contains the above-mentioned active ingredient and at least one other ingredient, it may be a composition in which the above-mentioned active ingredient and at least one other ingredient are mixed, it may be a composition in which the above-mentioned active ingredient and at least one other ingredient are formulated by an appropriate method, or it may be a composition in which the above-mentioned active ingredient and at least one other ingredient are formulated and then mixed with other ingredients.

本發明中所使用之上述有效成分或含有其之組合物或醫藥之形狀並無特別限定,例如可為液體狀、流動狀、凝膠狀、半固體形狀、或固體形狀等任一形狀。The shape of the active ingredient or the composition or medicine containing the active ingredient used in the present invention is not particularly limited, and may be in any shape such as liquid, fluid, gel, semi-solid, or solid.

作為本發明中所使用之上述有效成分或含有其之組合物或醫藥可包含之至少1種其他成分,並無特別限定,可較佳地例示醫藥品、飲食品、飼料、食品添加劑、飼料添加劑等最終形態中所容許,且可經口攝取之成分。The at least one other ingredient that can be contained in the above-mentioned active ingredient or the composition or medicine containing the same used in the present invention is not particularly limited, and preferably includes ingredients that are permitted in the final form of medicines, drinks, feeds, food additives, feed additives, etc. and can be orally ingested.

作為此種其他成分,例如可列舉甜味料、酸味料、維生素類、礦物類、增黏劑、乳化劑、抗氧化劑、水等。又,視需要,亦可添加色素、香料、保存料、防腐劑、防黴劑、其他之生理活性物質等。Examples of such other ingredients include sweeteners, acidulants, vitamins, minerals, thickeners, emulsifiers, antioxidants, water, etc. Furthermore, pigments, flavorings, preservatives, antiseptics, anti-mold agents, and other physiologically active substances may be added as needed.

作為甜味料,可列舉葡萄糖、果糖、蔗糖、乳糖、麥芽糖、巴拉金糖、海藻糖、木糖等單糖或二糖,異構化糖(葡萄糖果糖液糖、果糖葡萄糖液糖、砂糖混合異構化糖等)、糖醇(赤藻糖醇、木糖醇、乳糖醇、異麥芽糖醇、山梨糖醇、還原飴糖等)、蜂蜜、高甜度甜味料(蔗糖素、乙醯磺胺酸鉀、索馬甜、甜菊、阿斯巴甜等)等。As sweeteners, there may be mentioned monosaccharides or disaccharides such as glucose, fructose, sucrose, lactose, maltose, palatinose, trehalose, and xylose, isomerized sugars (glucose-fructose syrup, fructose-glucose syrup, mixed isomerized sugars of granulated sugar, etc.), sugar alcohols (erythritol, xylitol, lactitol, isomalt, sorbitol, reduced syrup, etc.), honey, and high-intensity sweeteners (sucralose, acesulfame potassium, thaumatin, stevia, aspartame, etc.), etc.

作為酸味料,有檸檬酸、蘋果酸、葡萄糖酸、酒石酸、乳酸、磷酸、或該等之鹽等,可利用該等中之1種或2種以上。As the acidulant, there are citric acid, apple acid, gluconic acid, tartaric acid, lactic acid, phosphoric acid, or salts thereof, and one or more of them can be used.

作為維生素類,可列舉維生素A、維生素B1、維生素B2、維生素B6、維生素E、菸鹼酸、肌醇等。As vitamins, there are vitamin A, vitamin B1, vitamin B2, vitamin B6, vitamin E, niacin, inositol, etc.

作為礦物類,可列舉鈣、鎂、鋅、鐵等。Minerals include calcium, magnesium, zinc, iron, etc.

作為增黏劑,可列舉角叉菜膠、結冷膠、三仙膠、阿拉伯膠、羅望子膠、瓜爾膠、刺槐豆膠、刺梧桐樹膠、瓊脂、明膠、果膠、大豆多糖類、羧甲基纖維素(CMC)等。As thickeners, carrageenan, gellan gum, samson gum, gum arabic, tamarind gum, guar gum, locust bean gum, karaya gum, agar, gelatin, pectin, soybean polysaccharides, carboxymethyl cellulose (CMC), etc. can be listed.

作為乳化劑,可列舉甘油脂肪酸酯、蔗糖脂肪酸酯、山梨醇酐脂肪酸酯、卵磷脂、植物性固醇、皂苷等。As emulsifiers, there can be mentioned glycerol fatty acid esters, sucrose fatty acid esters, sorbitan fatty acid esters, lecithin, plant sterols, saponins, and the like.

作為抗氧化劑,可列舉維生素C、生育酚(維生素E)、酵素改性芸香苷、兒茶素等。As antioxidants, vitamin C, tocopherol (vitamin E), enzyme-modified rutin, catechins, etc. can be listed.

上述其他成分可分別以業者於飲食品、醫藥品等組合物中通常採用之範圍內之量適宜地調配。The above-mentioned other ingredients can be appropriately formulated in amounts within the ranges commonly used by the industry in compositions such as beverages and pharmaceuticals.

利用適當之方法將本發明中所使用之上述有效成分與至少1種其他成分製劑化而成之組合物或醫藥之形態可為粉末、顆粒、膠囊劑、錠劑(包括糖衣錠等包衣錠或多層錠、口中崩解劑、咀嚼錠等)等固體組合物之形態,亦可為溶液劑等液體組合物之形態。 [實施例]The composition or medicine prepared by preparing the above-mentioned active ingredient and at least one other ingredient in the present invention by an appropriate method can be in the form of solid compositions such as powder, granules, capsules, tablets (including coated tablets such as sugar-coated tablets or multi-layer tablets, orally disintegrating tablets, chewable tablets, etc.), or in the form of liquid compositions such as solutions. [Examples]

1.抗癌作用之評價 將薑黃酮醇A(Tumeronol A)及薑黃酮醇B(Tumeronol B)(均為來自Nagara Science股份有限公司之市售品)溶解於二甲基亞碸中用於以下之試驗。1. Evaluation of anticancer effect Tumeronol A and Tumeronol B (both commercially available from Nagara Science Co., Ltd.) were dissolved in dimethyl sulfoxide and used in the following test.

將作為人大腸癌之細胞株之HT-29細胞懸浮於RPMI1640培養基(含10%FBS(Fetal Bovine Serum,胎牛血清))中,以每個孔中細胞數為3.0×103 個之方式播種於96孔微盤中,並於37℃且5%CO2 之條件下培養24小時。如此將96孔盤中培養之HT-29細胞,於以12.5 μM、25 μM、50 μM、100 μM之量包含薑黃酮醇A與薑黃酮醇B之任一者之RPMI1640培養基(含2.5%FBS)中培養72小時。培養結束前2小時添加WST-1試劑,2小時後用讀板儀測定吸光度(細胞之代謝活性)。將除使用不含檢體(薑黃酮醇A、薑黃酮醇B)之RPMI1640培養基外按同樣之程序培養所得之HT-29細胞之代謝活性設為100%,求出包含各濃度之檢體之RPMI1640培養基中培養之HT-29細胞之代謝活性之變化率。此處所謂細胞之代謝活性係意指包含細胞之增殖活動、及過度之活性化之生命維持活動。HT-29 cells, a cell line of human colorectal cancer, were suspended in RPMI1640 medium (containing 10% FBS (Fetal Bovine Serum)), seeded in a 96-well microplate at a cell number of 3.0×10 3 per well, and cultured for 24 hours at 37°C and 5% CO 2. The HT-29 cells cultured in the 96-well plate were cultured for 72 hours in RPMI1640 medium (containing 2.5% FBS) containing either 12.5 μM, 25 μM, 50 μM, or 100 μM of turmeric flavonol A or turmeric flavonol B. WST-1 reagent was added 2 hours before the end of the culture, and the absorbance (cell metabolic activity) was measured with a plate reader 2 hours later. The metabolic activity of HT-29 cells cultured in the same manner except that RPMI1640 medium without the sample (curcuminol A, curcuminol B) was set as 100%, and the change rate of metabolic activity of HT-29 cells cultured in RPMI1640 medium containing the sample at each concentration was calculated. The cell metabolic activity here refers to the cell proliferation activity and the over-activated life-sustaining activity.

分別將薑黃酮醇A相關結果示於圖1,將薑黃酮醇B相關結果示於圖2。圖1表明藉由用薑黃酮醇A處理HT-29細胞,細胞之代謝活性劑量依賴性地顯著降低。同樣地,圖2表明藉由用薑黃酮醇B處理HT-29細胞,細胞之代謝活性劑量依賴性地顯著降低。該等結果表明,薑黃酮醇A及薑黃酮醇B均抑制大腸癌細胞之代謝活性。此處所謂癌細胞之代謝活性之抑制係意指癌細胞之增殖抑制、癌化抑制、癌細胞死亡誘導。The results related to turmeric flavonol A are shown in FIG1 , and the results related to turmeric flavonol B are shown in FIG2 . FIG1 shows that by treating HT-29 cells with turmeric flavonol A, the metabolic activity of the cells is significantly reduced in a dose-dependent manner. Similarly, FIG2 shows that by treating HT-29 cells with turmeric flavonol B, the metabolic activity of the cells is significantly reduced in a dose-dependent manner. These results show that both turmeric flavonol A and turmeric flavonol B inhibit the metabolic activity of colorectal cancer cells. The inhibition of the metabolic activity of cancer cells here refers to the inhibition of cancer cell proliferation, inhibition of cancerization, and induction of cancer cell death.

本說明書中所引用之所有出版物、專利及專利申請案直接藉由引用而併入至本說明書中。All publications, patents, and patent applications cited in this specification are directly incorporated into this specification by reference.

圖1表示薑黃酮醇A(Tumeronol A)對作為人大腸癌之細胞株之HT-29細胞之代謝活性之抑制能力的測定結果。 圖2表示薑黃酮醇B(Tumeronol B)對HT-29細胞之代謝活性之抑制能力的測定結果。Figure 1 shows the results of the determination of the inhibitory ability of tumeronol A on the metabolic activity of HT-29 cells, which is a cell line of human colorectal cancer. Figure 2 shows the results of the determination of the inhibitory ability of tumeronol B on the metabolic activity of HT-29 cells.

Claims (5)

一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係用於製造大腸癌細胞之增殖抑制用組合物。 A use of at least one of turmeric flavonol A and turmeric flavonol B for preparing a composition for inhibiting the proliferation of colorectal cancer cells. 一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係用於製造針對大腸癌之抗癌用組合物。 A use of at least one of turmeric flavonol A and turmeric flavonol B for preparing an anticancer composition for colorectal cancer. 一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係用於製造正常細胞向大腸癌之癌化抑制用組合物。 A use of at least one of turmeric flavonol A and turmeric flavonol B for preparing a composition for inhibiting the transformation of normal cells into colorectal cancer. 一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係用於製造針對大腸癌之癌症發病抑制用組合物。 A use of at least one of turmeric flavonol A and turmeric flavonol B for preparing a composition for inhibiting the onset of colorectal cancer. 一種薑黃酮醇A及薑黃酮醇B之至少1種之用途,其係用於製造大腸癌細胞死亡誘導用組合物。 A use of at least one of turmeric flavonol A and turmeric flavonol B for preparing a composition for inducing colorectal cancer cell death.
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