WO2016062288A1 - 代谢性疾病药物用于制备抑制癌症的医药组合物的用途 - Google Patents
代谢性疾病药物用于制备抑制癌症的医药组合物的用途 Download PDFInfo
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- WO2016062288A1 WO2016062288A1 PCT/CN2015/092779 CN2015092779W WO2016062288A1 WO 2016062288 A1 WO2016062288 A1 WO 2016062288A1 CN 2015092779 W CN2015092779 W CN 2015092779W WO 2016062288 A1 WO2016062288 A1 WO 2016062288A1
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Definitions
- the present invention is a novel indication for a variety of metabolic disease drugs, in particular, the plurality of drugs are approved drugs marketed by the Department of Health and have the use of inhibiting various cancers.
- Cancer has long been the leading cause of death worldwide, and the number of cancer patients has increased year by year. Therefore, treating cancer has become an important issue.
- the treatment of cancer can be divided into surgical treatment, radiation therapy, chemotherapy and target treatment.
- cancer drug treatment is intended to prevent cancer cells from replicating and dividing to block the spread and spread of tumors.
- chemotherapy chemotherapy or target treatment
- cancer drug treatment is intended to prevent cancer cells from replicating and dividing to block the spread and spread of tumors.
- chemotherapeutic drugs and target treatment hoping to kill cancer cells by different mechanisms to improve the therapeutic effect, but in fact, patients often react to the treatment of drugs Not good.
- many cancer cells successively develop drug resistance, which greatly reduces the effectiveness of drug use, and ultimately leads to failure of cancer treatment.
- the present invention aims at the development of new indications for a variety of drugs that have undergone clinical trials and have no adverse reactions to the human body, and achieves the goal of new use of old drugs.
- cancer cells have different performance traits, type differences, or changes in function, compared to normal cells, and each cancer cell is located at a different location and is mutated.
- the state is related to the environment in which it is located, and therefore the inventors believe that cancer cells can also be regarded as another cell having abnormal metabolism, and propose an inventive concept of inhibiting cancer cells using a metabolic disease drug and carry out an experiment.
- the present invention provides a use of a medicament for a metabolic disease for the preparation of a pharmaceutical composition for inhibiting cancer, wherein the pharmaceutical composition is an effective dose of a metabolic disease drug and a pharmaceutically acceptable salt.
- the metabolic disease drug of the present invention is an FDA-approved drug and has been used in human or animal body for decades, and has a large amount of data on drug transfer and human research results. Therefore, if applied to cancer, this new drug Development will save time, reduce costs, and can be combined with other treatments to improve results.
- the cost of cancer drugs today is tens of thousands to millions of dollars, and the metabolic disease drugs of the present invention have therapeutic effects on cancer cells, so for patients who cannot afford expensive treatment, these inexpensive and long-established drugs will Bring new hopes.
- the drug system for obtaining a metabolic disease is selected from the group consisting of a hypoglycemic agent, a strong liver agent, a gout therapeutic agent, a kidney dialysis drug, an antidote, an enzyme preparation, and other drugs for metabolic diseases.
- the hypoglycemic agent of the invention is a commercially available oral hypoglycemic agent, which can be divided into six categories: 1. Sulfonylurea: stimulates the secretion of a large amount of insulin in the pancreas, and has a good blood sugar lowering effect; 2. a biguanide: inhibition The absorption of sugar and amino acids in the small intestine inhibits the production of glucose in the liver; 3. The oxazolidinedione: reduces insulin resistance, also known as insulin sensitizer; 4. Meglitos: stimulates the secretion of insulin from the pancreas, characterized by Fast drug effect, short duration of action, mainly for liver metabolism; 5.
- Alpha-type disaccharide decomposition inhibitor inhibits the decomposition of carbohydrates in the intestine and reduces the absorption of sugar, mainly used to control the blood sugar concentration after meals;
- Peptide protein Hydrolase inhibitors promote the action of gut hormones, less likely to cause hypoglycemia, and control blood sugar after meals.
- the hypoglycemic agent is selected from the group consisting of Glibenclamide, Minidiab, Diamicron, Acarbose, and Glimepiride. , Glucophage, oral isotretinoin, Omeprazole (Priosec), Avandia, Novonorm, Januvia , sugar release film (Starlix), Glucobay (Glucobay), Orlistat (Alli, Xenical), Amiloride hydrochloride (Midamor), Aspartame, Pioglitazone hydrochloride (Actos), Roxithromycin, Phenformin hydrochloride, Vildagliptin, A drug consisting of one or more of Gliquidone, Voglibose, Cysteamine HCl, Cepharanthine, and Tolaszamide.
- the strong liver drug is selected from the group consisting of Malotilate, SILYMARIN, GLUTATHION REDUCED, Vitamin B12, and Venopine ( A drug consisting of one or more of Vinorelbine (Navelbine), Monobenzone (Benoquin), Niacin (Nicotinic acid), L-Glutamine, Captopril (Capoten), Balofloxacin, and Tolvaptan.
- the gout therapeutic agent is a drug selected from the group consisting of one or more of Wuzhou Tonglian Capsule (ACEO), Benzbromarone and Benemid.
- the drug for renal dialysis is a drug selected from the group consisting of one or more of ARTIFICIAL, Gemcitabine (Gemzar), Ranitidine (Zantac), Xylose, and Levosimendan.
- the antidote agent is selected from the group consisting of sodium bicarbonate, chlorophosphorus, and pamidronate.
- a drug consisting of one or more of Disodium) and Ribavirin.
- the enzyme preparation drug is a drug selected from the group consisting of one or more of AMBEZIM, Nizatidine, Vitamin B12, Lisinopril, Bezafibrate, and Doxofylline.
- the other metabolic diseases are selected from the group consisting of Ristronate sodium, Pralatrexate (Folotyn), Alendronate (Fosamax), and bear diol ( A drug consisting of one or more of Ursodiol (Actigal Urso), Ristronic acid (Actonel), Mecarbinate, Licofelone, Manidipine, Allylthiourea, Tolcapone, and Chlorzoxazone.
- the cancer is one or more selected from the group consisting of lung cancer, intestinal cancer, colorectal cancer, prostate cancer, bladder cancer, cervical cancer, breast cancer, and blood cancer.
- the effective dose is 20-500 mg/kg/day.
- Fig. 1 shows the results of analysis of the application of the metabolic disease drug of the present invention to inhibit various cancer cells.
- the cell lines of different cancer types were subcultured, and after counting the number of cells, 2 ⁇ 10 6 cells were placed in a culture dish, and then the culture medium in which the cell strain was cultured was added to a volume of 10 ml, and the culture was continued. 2-3 days. The cells were then counted and dispensed into 96-well plates where the number of cells per well was fixed at 3000 and the volume was 100 ul.
- the original culture solution in the 96-well plate was aspirated, and a commercially available metabolic disease drug having a concentration of 10 ⁇ M and a volume of 100 ul was added to each well. After 72 hours, 100 ul of diluted WST-1 reagent was added to each well. The dilution ratio was The volume ratio of the culture solution to the WST-1 stock solution is 9:1, and finally the total volume of each well plate is 200 ul, and then the 96-well plate is placed at 37 ° C for 30-90 minutes, using Elisa reader (ELISA) The absorbance was detected at OD450 and the survival rate of each cancer cell line was calculated.
- ELISA Elisa reader
- Drugs for metabolic diseases are used to inhibit cancer cell analysis results
- the metabolic disease medication according to the present invention can be classified into a hypoglycemic agent, a strong liver agent, a gout therapeutic agent, a kidney dialysis drug, an antidote agent, an enzyme preparation, and other drugs for metabolic diseases according to the type of disease to be treated.
- lung cancer cell lines H1650, A549, gastric cancer cell lines (AGS, MKN-45), liver cancer cell lines (HepG2), rectal cancer cell lines (HCT116, LoVo), skin cancer cell lines (A375), cervical cancer Growth of cell line (HeLa), prostate cancer cell line (PC3), bladder cancer cell line (TSGH-8301), breast cancer cell line (MCF7), and blood cancer cell line (HL-60).
- Metabolic disease medication Inhibition of cancer cell line effects Pamidronate Disodium 0 Ranitidine (Zantac) 0 Licofelone 0 Ribavirin (Copegus) 0 Roxithromycin (Roxl-150) 0 Tolvaptan (OPC-41061) 0 Rivaroxaban (Xarelto) 0 Mepivacaine HCl 0 Clofibric acid 0
- the other drugs for metabolic diseases have different inhibitory effects on various cancer cells. As shown in Table 3 below, the values in Table 3 are expressed as IC50 (half maximal inhibitory concentration), and the gray mark indicates the metabolism. The disease drug has a significant inhibitory effect on the cell line.
- Pralatrexate (Folotyn) (Platinosa), Vinorelbine (Navelbine), Ursodiol (Actigal Urso), Monobenzone (Benoquin) (Monobenzone), Nizatidine (Nizatidine), Vitamin B12, Pioglitazone hydrochloride ( Actos) (Pioglitazone Hydrochloride), Captopril (Capoten) (Captopril), Balofloxacin (Barofloxacin), Mecarbinate (Mikamate), Lisinopril (Zestril) (Linopril), Donepezil HCl (Aricept) (Donepezil hydrochloride), Doxycycline HCl (doxycycline hydrochloride), Allylthiourea (allylthiourea), Sodium Picosulfate (sodium pyridoxine), Tolcapone (Tocame), Probenecid (Benemid), probenecid Ch
- the metabolic drugs include Acarbose, Ristronate sodium, Risedronate sodium, Pralatrexate (Folotyn), Vinolerbine (Navelbine), Ursodiol. (Actigal Urso), Monobenzone (Benoquin), Gemcitabine (Gemzar), Balofloxacin, Mecarbinate, Lisinopril (Zestril), Bazedoxifene HCl, Donepezil HCl (Aricept), Phenformin hydrochloride, Probenecid (Benemid), Chlorzoxazone, Bezafibrate, Doxofylline, Cepharanthine for different Types of cancer cells have significant inhibitory effects.
- the results of the experimental design show that the metabolic disease drugs have no or only minimal toxicity to normal cells, but whether the metabolic disease drugs have selective effects between normal cells and tumor cells remains to be further studied. Not all metabolic diseases can effectively inhibit tumor cells under the same conditions.
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Abstract
代谢性疾病药物在制备抑制癌症的医药组合物中的应用,所述代谢性疾病药物选自降血糖剂、强肝剂、痛风治疗剂、肾脏透析用药、解毒剂、酵素制剂及其他代谢性疾病用药中的一种或多种。
Description
本发明为多种代谢性疾病药物的新适应症的应用,尤其该多种药物为卫生署核准上市的药物且具有抑制多种癌症的用途。
癌症长期高居全球死因之首,且罹患癌症人数更是逐年攀升,因此治疗癌症俨然成为重要的课题。癌症的治疗可区分为手术治疗、放射线治疗、化学治疗及标靶治疗。
一般来说,癌症药物治疗无论是化学治疗或标靶治疗,目的多是让癌细胞无法复制、分裂,来阻断肿瘤的蔓延扩张。在临床治疗选择上,通常会结合一到数种化疗药物以及标靶治疗,希望能藉由不同机制来杀死癌细胞以提高治疗效果,但事实上,还是常遇到患者对于治疗药物的反应不佳。进一步,许多癌细胞相继产生抗药性,使药物的使用成效大幅降低,最终导致癌症治疗失败。
尽管如此,癌症药物开发依然是重要的医学议题,开发过程必须经过繁复的临床前试验才能进入临床试验。根据统计,平均每一万个新药约只有五个能够进入第一期临床试验。此外,除了药物本身是否能大量制造的难题外,还需克服药物安全性、病人筛选、试用剂量等问题,即便药物已经通过FDA的核准并上市,亦有可能因上市后于人体发现不良反应而强制下架回收,由此可见药物开发具有一定的困难程度。
发明内容
有鉴于此,本发明针对通过临床实验且对人体无不良反应的多种药物进行新适应症的研发,而达到老药新用的目标。
发明人依据长年的研究经验,证实癌症细胞与正常细胞相比,具有不同的表现性状、型态上的差异或是作用机转的变化,而每一种癌症细胞所在的位置不同、变异的状态又与所处的环境有关,因此发明人认为癌细胞亦可视为另一种代谢异常的细胞,而提出使用代谢性疾病药物抑制癌症细胞的发明概念并且进行实验。
本发明提供一种代谢性疾病药物用于制备抑制癌症的医药组合物的用途,其中所述医药组合物是包含有效剂量的代谢性疾病药物及药学上可接受的盐类。
本发明所述代谢性疾病药物是FDA所认可的用药,且于人体或动物体中使用数十年,具有大量药物机转及人体研究成果的数据,因此,若应用在癌症方面,这项新发展会更省时、减少成本,也能和其他治疗方式结合来提高效果。此外,现今癌症药物费用动辄上万至数百万元,而本发明所述代谢性疾病药物对癌症细胞具有治疗功效,因此对于无法负担昂贵治疗的患者们,这些便宜而历史悠久的药物,会带来新希望。
本发明一实施例中,其中得到代谢性疾病药物系是选自由降血糖剂、强肝剂、痛风治疗剂、肾脏透析用药、解毒剂、酵素制剂及其他代谢性疾病用药等药物。
本发明所述降血糖剂系为市售的口服降血糖药,可区分为六类:一、磺酰尿素类:刺激胰脏分泌较多量的胰岛素,降血糖效果佳;二、双胍类:抑制小肠对糖及氨基酸的吸收,抑制肝脏制造葡萄糖;三、唑烷二酮类:降低胰岛素阻抗性,又称为胰岛素增敏剂;四、美格替耐类:刺激胰脏分泌胰岛素,特点是药效快,作用时间短,主要为肝代谢;五、α型双糖分解脢抑制剂:抑制肠道内糖类分解,减少糖类的吸收,主要用来控制饭后血糖浓度;六、双胜肽蛋白
水解酶抑制剂:促进肠泌素激素作用,较不易引起低血糖,控制饭后血糖效果佳。
本发明一实施例中,其中所述降血糖剂是选自由血糖平(Glibenclamide)、灭糖尿(Minidiab)、岱蜜克龙(Diamicron)、醣禄锭(Acarbose)、玛尔胰锭(Glimepiride)、库鲁化锭(Glucophage)、口服维他命A酸(Isotretinoin)、奥美拉唑(Omeprazole(Prilosec))、梵蒂雅锭(Avandia)、诺和隆锭(Novonorm)、佳糖维(Januvia)、使糖立释膜衣锭(Starlix)、糖禄锭(Glucobay)、Orlistat(Alli、Xenical)、Amiloride hydrochloride(Midamor)、Aspartame、吡格列酮(Pioglitazone hydrochloride(Actos))、Roxithromycin、Phenformin hydrochloride、Vildagliptin、Gliquidone、Voglibose、Cysteamine HCl、Cepharanthine及Tolazamide中的一种或多种所组成的药物。
本发明一实施例中,其中所述强肝剂药物是选自由马洛替酯片(Malotilate)、思利马林胶囊本(SILYMARIN)、GLUTATHION REDUCED、维他命B12(Vitamin B12)、温诺平(Vinorelbine(Navelbine))、Monobenzone(Benoquin)、Niacin(Nicotinic acid)、L-Glutamine、Captopril(Capoten)、Balofloxacin及Tolvaptan中的一种或多种所组成的药物。
本发明一实施例中,其中所述痛风治疗剂是选自由五洲痛立安胶囊(ACEO)、优诺锭(Benzbromarone)及Benemid中的一种或多种所组成的药物。
本发明一实施例中,其中所述肾脏透析用药物是选自由ARTIFICIAL、Gemcitabine(Gemzar)、Ranitidine(Zantac)、Xylose及Levosimendan中的一种或多种所组成的药物。
本发明一实施例中,其中所述解毒剂药物是选自由碳酸氢钠锭(Sodium bicarbonate)、氯磷锭(PRALIDOXIME CHLORIDE)、帕米膦酸盐(Pamidronate
Disodium)及Ribavirin中的一种或多种所组成的药物。
本发明一实施例中,其中所述酵素制剂药物是选自由安病疾锭(AMBEZIM)、Nizatidine、维他命B12(Vitamin B12)、Lisinopril、Bezafibrate及Doxofylline中的一种或多种所组成的药物。
本发明一实施例中,其中所述其他代谢性疾病用药是选自由升骨卓(Risedronate sodium)、服瘤停注射剂(Pralatrexate(Folotyn))、福善美(Alendronate(Fosamax))、熊二醇(Ursodiol(ActigalUrso))、Risedronic acid(Actonel)、Mecarbinate、Licofelone、Manidipine、Allylthiourea、Tolcapone及Chlorzoxazone中的一种或多种所组成的药物。
本发明一实施例中,其中所述癌症是选自由肺癌、肠道癌、大肠直肠癌、前列腺癌、膀胱癌、子宫颈癌、乳癌及血癌中的一种或多种。
本发明一实施例中,其中所述有效剂量系为20-500mg/kg/天。
图1为本发明代谢性疾病用药应用于抑制各种癌细胞的分析结果。
建立细胞株
参照表一,将不同癌症类型的细胞株进行继代培养,计算细胞数目后,将2×106细胞数置入培养皿,然后加入培养该细胞株的培养液补至体积为10ml,继续培养2-3天。之后将细胞计数,并分装至96孔盘,其中每孔的细胞数目固定为3000个,且体积为100ul。
表一、细胞株及其培养所用的培养液
细胞存活分析方法
将96孔盘中原有的培养液吸掉,每孔加入浓度10μM、体积100ul的市售代谢性疾病用药,放置72小时后,每孔再加入100ul已稀释的WST-1试剂,该稀释比例为培养液与WST-1原液的体积比为9:1,最后每个孔盘的总体积为200ul,然后将96孔盘放置于37℃,30~90分钟,利用Elisa reader(酶联免疫检测仪)于OD450侦测吸光值,并计算各癌症细胞株的存活率。
代谢性疾病用药物应用于抑制癌细胞分析结果
本发明所述代谢性疾病用药可依据治疗的疾病种类,分为降血糖剂、强肝剂、痛风治疗剂、肾脏透析用药、解毒剂、酵素制剂及其他代谢性疾病用药等药物。
请参照表二,实验结果显示Pamidronate Disodium、Ranitidine(Zantac)、Licofelone、Ribavirin(Copegus)、Roxithromycin(Roxl-150)、Tolvaptan(OPC-41061)、Rivaroxaban(Xarelto)、Mepivacaine HCl、Clofibric acid并无法有效的抑制肺癌细胞株(H1650、A549)、胃癌细胞株(AGS、MKN-45)、肝癌细胞株(HepG2)、直肠癌细胞株(HCT116、LoVo)、皮肤癌细胞株(A375)、子宫颈癌细胞株(HeLa)、前列腺癌细胞株(PC3)、膀胱癌细胞株(TSGH-8301)、乳癌细胞株(MCF7)及血癌细胞株(HL-60)的生长。
表二、对癌症细胞株无抑制效果之代谢性疾病用药
代谢性疾病用药 | 抑制癌症细胞株效果 |
Pamidronate Disodium | 0 |
Ranitidine(Zantac) | 0 |
Licofelone | 0 |
Ribavirin(Copegus) | 0 |
Roxithromycin(Roxl-150) | 0 |
Tolvaptan(OPC-41061) | 0 |
Rivaroxaban(Xarelto) | 0 |
Mepivacaine HCl | 0 |
Clofibric acid | 0 |
而其他代谢性疾病用药对于各种癌症细胞的抑制效果也不尽相同,如下表三所示,表三中的数值是以IC50(半抑制浓度,half maximal inhibitory concentration)表示,灰色标记表示该代谢性疾病药物对于该细胞株有明显抑制的功效。
实验结果证实Malotilate(马洛替酯)、Leucovorin Calcium(亚叶酸钙)、Acarbose(拜唐苹(阿卡波糖))、Glimepiride(格列美脲)、Isotretinoin(异维甲酸)、Omeprazole(Prilosec)(奥美拉唑)、Risedronate sodium(利塞膦酸钠)、Pralatrexate(Folotyn)(普拉曲沙)、Vinorelbine(Navelbine)长春瑞滨)、Ursodiol(Actigal Urso)(熊脱氧胆酸)、Monobenzone(Benoquin)(莫诺苯宗)、Gemcitabine(Gemzar)(吉西他滨)、Niacin(Nicotinic acid)(烟酸)、L-Glutamine(L-谷氨酰胺)、Vitamin B12(维他命B12)、Aspartame(阿斯巴甜)、Pioglitazone hydrochloride(Actos)(盐酸吡格列酮)、Captopril(Capoten)(卡托普利)、Balofloxacin(巴洛沙星)、Mecarbinate(美卡比酯)、Lisinopril(Zestril)(赖诺普利)、Bazedoxifene HCl(盐酸巴多昔芬)、Donepezil HCl(Aricept)(盐酸多奈哌齐)、Phenformin hydrochloride(盐酸苯乙双胍)、Scopine(东莨菪醇)、Mifepristone(Mifeprex)(米非司酮)、Noradrenaline bitartrate monohydrate(Levophed)(重酒石酸左旋去甲肾上腺素)、Vildagliptin(LAF-237)(维格列汀)、Pravastatin sodium(普伐他汀钠)、Flumequine(氟甲喹)、Probenecid(Benemid)(丙磺舒)、Amprolium HCl(氨基喹啉)、Chlorzoxazone(氯若沙宗)、Bezafibrate(苯扎贝特)、Doxofylline(多索茶碱)、Cepharanthine(西法安生)等药物对于肺癌症细胞有明显的抑制效果。
实验结果证实Leucovorin Calcium(亚叶酸钙)、Acarbose(拜唐苹(阿卡波糖))、Omeprazole(Prilosec)(奥美拉挫)、Risedronate sodium(利塞膦酸钠)、Pralatrexate(Folotyn)(普拉曲沙)、Vinorelbine(Navelbine)(长春瑞滨)、Alendronate(Fosamax)(阿仑唑奈)、Orlistat(Alli,Xenical)(奥利司他)、Ursodiol(Actigal Urso)(熊脱氧胆酸)、Monobenzone(Benoquin)(莫诺苯宗)、Gemcitabine(Gemzar)(吉西他滨)、Amiloride hydrochloride(Midamor)(盐酸
阿米洛利)、Risedronic acid(Actonel)(利塞膦酸)、Balofloxacin(巴洛沙星)、Mecarbinate(美卡比酯)、Lisinopril(Zestril)(赖诺普利)、Xylose(戊醛糖)、Bazedoxifene HCl(盐酸巴多昔芬)、Levosimendan(左西孟旦)、Donepezil HCl(Aricept)(盐酸多奈哌齐)、Vildagliptin(LAF-237)(维格列汀)、Pravastatin sodium(普伐他汀钠)、Flumequine(氟甲喹)、Allylthiourea(烯丙基硫脲)、Tolcapone(托卡朋)、Probenecid(Benemid)(丙磺舒)、Amprolium HCl、Chlorzoxazone(氯唑沙宗)、Bezafibrate(苯扎贝特)、Doxofylline(多索茶碱)、Cepharanthine(西法安生)等药物对于胃癌症细胞有明显的抑制效果。
实验结果证实Probenecid(Benemid)(丙磺舒)药物对于肝癌症细胞有明显的抑制效果。
实验结果证实Glimepiride(格列美脲)、Pralatrexate(Folotyn)(普拉曲沙)、Vinorelbine(Navelbine)、Monobenzone(Benoquin)(莫诺苯宗)、Risedronic acid(Actonel)(利塞膦酸)、Pioglitazone hydrochloride(Actos)(吡格列酮)、Captopril(Capoten)(卡托普利)、Balofloxacin(巴洛沙星)、Mecarbinate(美卡比酯)、Lisinopril(Zestril)(赖诺普利)、Donepezil HCl(Aricept)(盐酸多奈哌齐)、Gliquidone、Flumequine、Clodronate Disodium、氯唑沙宗(Chlorzoxazone)、Bezafibrate(苯扎贝特)、Doxofylline(多索茶碱)等药物对于结肠癌症细胞有明显的抑制效果。
实验结果证实Glimepiride(格列美脲)、Omeprazole(Prilosec)(奥美拉唑)、Risedronate sodium(利塞膦酸钠)、Pralatrexate(Folotyn)(普拉曲沙)、Vinorelbine(Navelbine)、Monobenzone(Benoquin)(莫诺苯宗)、Gemcitabine(Gemzar)(吉西他滨)、Bazedoxifene HCl(盐酸巴多昔芬)、Donepezil HCl(Aricept)(盐酸多奈哌齐)、Mifepristone(Mifeprex)(米非司酮)、Noradrenaline bitartrate
monohydrate(Levophed)(重酒石酸左旋去甲肾上腺素)、Bufexamac(丁苯羟酸)、Vildagliptin(LAF-237)(维格列汀)、Sodium Picosulfate(吡苯氧磺钠)、Tolcapone(托卡朋)、Probenecid(Benemid)(丙磺舒)、Chlorzoxazone(氯唑沙宗)、Bezafibrate(苯扎贝特)、Doxofylline(多索茶碱)、Cepharanthine(西法安生)等药物对于皮肤癌症细胞有明显的抑制效果。
实验结果证实代谢性疾病药物Monobenzone(Benoquin)(莫诺苯宗)、L-Glutamine(L-谷氨酰胺)、Balofloxacin(巴洛沙星)、Mecarbinate(美卡比酯)、Lisinopril(Zestril)(赖诺普利)、Bazedoxifene HCl(盐酸巴多昔芬)、Levosimendan(左西孟旦)、Donepezil HCl(Aricept)(盐酸多奈哌齐)、Phenytoin sodium(Dilantin)(苯妥英钠)、Chlorzoxazone(氯唑沙宗)、Doxofylline(多索茶碱)、Cepharanthine等药物对于子宫颈癌症细胞有明显的抑制效果。
实验结果证实Pralatrexate(Folotyn)(普拉曲沙)、Vinorelbine(Navelbine)、Ursodiol(Actigal Urso)、Monobenzone(Benoquin)(莫诺苯宗)、Nizatidine(尼扎替丁)、Vitamin B12、Pioglitazone hydrochloride(Actos)(盐酸吡格列酮)、Captopril(Capoten)(卡托普利)、Balofloxacin(巴洛沙星)、Mecarbinate(美卡比酯)、Lisinopril(Zestril)(赖诺普利)、Donepezil HCl(Aricept)(盐酸多奈哌齐)、Doxycycline HCl(盐酸强力霉素)、Allylthiourea(烯丙基硫脲)、Sodium Picosulfate(吡苯氧磺钠)、Tolcapone(托卡朋)、Probenecid(Benemid)(丙磺舒)、Chlorzoxazone(氯唑沙宗)、Bezafibrate(苯扎贝特)、Doxofylline、Cepharanthine等药物对于前列腺癌症细胞有明显的抑制效果。
实验结果证实Leucovorin Calcium、Acarbose、Pralatrexate(Folotyn)(普拉曲沙)、Vinorelbine(Navelbine)、Alendronate(Fosamax)(阿仑唑奈)、Orlistat(Alli,Xenical)(奥利斯特)、Ursodiol(Actigal Urso)、Monobenzone(Benoquin)(莫
诺苯宗)、Gemcitabine(Gemzar)、Balofloxacin(巴洛沙星)、Mecarbinate(美卡比酯)、Lisinopril(Zestril)(赖诺普利)、Xylose(木糖,戊醛糖)、Levosimendan(左西孟旦)、Donepezil HCl(Aricept)(盐酸多奈哌齐)、Manidipine(Manyper)(盐酸马尼地平)、Phenformin hydrochloride(盐酸苯乙双胍)、Scopine(东莨菪醇)、Tolcapone(托卡朋)、Probenecid(Benemid)、Chlorzoxazone(氯唑沙宗)、Bezafibrate(苯扎贝特)、Doxofylline(多索茶碱)、Cepharanthine(西法安生)等药物对于膀胱癌症细胞有明显的抑制效果。
实验结果证实Acarbose(拜糖平)、Risedronate sodium(利塞膦酸钠)、Alendronate(Fosamax)(阿仑唑奈)、Orlistat(Alli,Xenical)(奥利斯特)、Ursodiol(Actigal Urso)、Monobenzone(Benoquin)(莫诺苯宗)、Niacin(Nicotinic acid)、L-Glutamine、Nizatidine(尼扎替丁)、Vitamin B12、Aspartame、Pioglitazone hydrochloride(Actos)(盐酸吡格列酮)、Captopril(Capoten)(卡托普利)、Balofloxacin(巴洛沙星)、Mecarbinate(美卡比酯)、Lisinopril(Zestril)(赖诺普利)、Bazedoxifene HCl(盐酸巴多昔芬)、Flumequine(氟甲喹)、Voglibose(伏格列波糖)、Clodronate Disodium(氯甲双磷酸二钠)、Chlorzoxazone(氯若沙宗)、Bezafibrate(苯扎贝特)、Doxofylline(多索茶碱)、Cepharanthine(千金藤素)、Amprolium HCl等药物对于乳腺癌症细胞有明显的抑制效果。
实验结果证实代谢性疾病药物Vinorelbine(Navelbine)(长春瑞滨)、Gemcitabine(Gemzar)(吉西他滨)、Bazedoxifene HCl(盐酸巴多昔芬)、Manidipine(Manyper)(盐酸马尼地平)、Phenformin hydrochloride(盐酸苯乙双胍)等药物对于白血病细胞有明显的抑制效果。
请参考图一,由实验结果可知,代谢性药物包括Acarbose、Risedronate sodium、Risedronate sodium、Pralatrexate(Folotyn)、Vinorelbine(Navelbine)、Ursodiol
(Actigal Urso)、Monobenzone(Benoquin)、Gemcitabine(Gemzar)、Balofloxacin、Mecarbinate、Lisinopril(Zestril)、Bazedoxifene HCl、Donepezil HCl(Aricept)、Phenformin hydrochloride、Probenecid(Benemid)、Chlorzoxazone、Bezafibrate、Doxofylline、Cepharanthine对于不同类型的癌症细胞均有明显的抑制效果。
重复性实验
依据表三所示结果,针对癌症细胞株有效的药物进行重复性实验,其结果如表四所示。
而实验设计的结果显示代谢性疾病药物对正常细胞没有或仅有微小的毒性,但至于代谢性疾病用药在正常细胞与肿瘤细胞之间是否具有选择性的影响,还待更多的研究厘清,且并非所有的代谢性疾病用药在相同的条件下均能有效的抑制肿瘤细胞。
上列详细说明是针对本发明的可行实施例的具体说明,惟该实施例并非用以限制本发明的专利范围,凡未脱离本发明技艺精神所为的等效实施或变更,均应包含于本发明的专利范围中。
Claims (11)
- 一种代谢性疾病药物用于制备抑制癌症的医药组合物的用途,其特征是,所述医药组合物是包含有效剂量的代谢性疾病药物及药学上可接受的盐类所组成。
- 如权利要求1所述的用途,其特征是,所述代谢性疾病药物是选自由降血糖剂、强肝剂、痛风治疗剂、肾脏透析用药、解毒剂、酵素制剂及其他代谢性疾病用药中的一种或多种所组成的药物。
- 如权利要求2所述的用途,其特征是,所述降血糖剂药物是选自由血糖平(Glibenclamide)、灭糖尿(Minidiab)、岱蜜克龙(Diamicron)、醣禄锭(Acarbose)、玛尔胰锭(Glimepiride)、库鲁化锭(Glucophage)、口服维他命A酸(Isotretinoin)、奥美拉唑(Omeprazole(Prilosec))、梵蒂雅锭(Avandia)、诺和隆锭(Novonorm)、佳糖维(Januvia)、使糖立释膜衣锭(Starlix)、糖禄锭(Glucobay)、Orlistat(Alli、Xenical)、Amiloride hydrochloride(Midamor)、Aspartame、吡格列酮(Pioglitazone hydrochloride(Actos))、Roxithromycin、Phenformin hydrochloride、Vildagliptin、Gliquidone、Voglibose、Cysteamine HCl、Cepharanthine及Tolazamide中的一种或多种所组成的药物。
- 如权利要求2所述的用途,其特征是,所述强肝剂药物是选自由马洛替酯片(Malotilate)、思利马林胶囊本(SILYMARIN)、GLUTATHION REDUCED、维他命B12(Vitamin B12)、温诺平(Vinorelbine(Navelbine))、Monobenzone(Benoquin)、Niacin(Nicotinic acid)、L-Glutamine、Captopril(Capoten)、Balofloxacin及Tolvaptan中的一种或多种所组成的药物。
- 如权利要求2所述的用途,其特征是,所述痛风治疗剂药物是选自由五洲痛立 安胶囊(ACEO)、优诺锭(Benzbromarone)及Benemid中的一种或多种所组成的药物。
- 如权利要求2所述的用途,其特征是,所述肾脏透析用药药物是选自由ARTIFICIAL、Gemcitabine(Gemzar)、Ranitidine(Zantac)、Xylose及Levosimendan中的一种或多种所组成的药物。
- 如权利要求2所述的用途,其特征是,所述解毒剂药物是选自由碳酸氢钠锭(Sodium bicarbonate)、氯磷锭(PRALIDOXIME CHLORIDE)、帕米膦酸盐(Pamidronate Disodium)及Ribavirin中的一种或多种所组成的药物。
- 如权利要求2所述的用途,其特征是,所述酵素制剂药物是选自由安病疾锭(AMBEZIM)、Nizatidine、维他命B12(Vitamin B12)、Lisinopril、Bezafibrate及Doxofylline中的一种或多种所组成的药物。
- 如权利要求2所述的用途,其特征是,所述其他代谢性疾病用药是选自由升骨卓(Risedronate sodium)、服瘤停注射剂(Pralatrexate(Folotyn))、福善美(Alendronate(Fosamax))、熊二醇(Ursodiol(ActigalUrso))、Risedronic acid(Actonel)、Mecarbinate、Licofelone、Manidipine、Allylthiourea、Tolcapone及Chlorzoxazone中的一种或多种所组成的药物。
- 如权利要求1所述的用途,其特征是,所述癌症是选自由肺癌、肠道癌、大肠直肠癌、前列腺癌、膀胱癌、子宫颈癌、乳癌、血癌中的一种或多种。
- 如权利要求1所述的用途,其特征是,所述有效剂量为20-500mg/kg/天。
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