CN1816344A - 用于治疗和预防前列腺病症的植物组合物 - Google Patents
用于治疗和预防前列腺病症的植物组合物 Download PDFInfo
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Abstract
本发明公开了包含以下成分的组合物:a)游离形式或与磷脂复合的水飞蓟素或其组分;b)纯形式或番茄(Lycoperisicum aesculentum)提取物形式的番茄红素;c)月桂酸或其非毒性的酯或盐或锯齿棕(Serenoa repens)的亲脂性提取物;d)任选地,锌盐和/或硒化合物。
Description
发明领域
本发明涉及植物来源的天然化合物和(可能的话)微量元素(oligoelement)的组合物,其用于治疗前列腺肥大和预防前列腺癌。
发明背景
已知当通过局部或全身途径施用时,水飞蓟素和尤其是水飞蓟宾是具有抗肝毒性活性(Reinhard S.等.Drugs,2001,61,2035-2063)和抗炎活性(Gupta P.O.等.Phytomedicine,2000,7,21)的化合物;已知该分子还对雌激素受体具有亲和性(Scambia G.等.European J.of Cancer,1996,32A,878)。几十年来水飞蓟素已经被用于治疗各种肝脏疾病并用于治疗α-鹅膏菌素和毒伞素中毒。US 5714473也描述了水飞蓟素和水飞蓟宾在调控或降低肿瘤药物如顺铂和蒽环类化合物的毒性中的应用。WO 96/37209要求保护与磷脂的复合物形式的水飞蓟宾,其抑制激素依赖型卵巢和乳腺肿瘤的增生,并与顺铂复合物具有协同作用。该分子对雌激素受体的亲和性使得其可在异常表达雌激素受体的位点蓄积,发挥其对过表达雌激素受体的器官的特定的抗氧化、抗炎和抗增生作用。这些抗炎和抗增生作用在非激素依赖型前列腺肿瘤的治疗和预防中是尤为重要的,原因如下所述。
在体外,水飞蓟素和特别是水飞蓟宾抑制独立的产雄激素性前列腺癌细胞增生,从而阻碍G1期的细胞周期。
番茄红素是一种亲脂性抗氧化剂,众所周知它对前列腺癌的发生具有预防作用。在流行病学水平上,番茄红素血浆水平与前列腺肿瘤之间存在负相关,其原因迄今未充分阐明;该类胡萝卜素前体(procarotenoid)在体内不会产生维生素A,它进入脂蛋白,在其中它抑制胆固醇的氧化,并且所述的抑制作用可影响甾类激素的合成和代谢。在用患有局部前列腺癌等待手术根除的患者进行的实验中,番茄红素被作为饮食的一部分以每天28毫克的剂量使用三周后,其可降低血浆PSA(前列腺特异性抗原)水平,并大大降低对术后活组织检查组织的DNA的氧化损伤(J Natl Cancer Inst2001,93,1872-79)。
最后,锯齿棕(Serenoa repens)的亲脂性提取物被用于治疗良性前列腺肥大已经有一段时间。
发明内容
现已令人惊奇地发现a、b、c、d的组合物可减少细胞增殖、前列腺增生、PSA和对DNA的氧化损伤,其减少程度远大于单独使用这些成分:
a.游离形式或与磷脂复合的水飞蓟素或其组分;
b.以纯的形式或以番茄(Lycoperisicum aesculentum)提取物形式使用的番茄红素;
c.月桂酸或其非毒性的酯或盐或锯齿棕的亲脂性提取物;
d.和任选地,锌盐和/或硒化合物。
由水飞蓟(Silybum marianum)提取的水飞蓟素或它的主要组分(水飞蓟宾、水飞蓟宁(silidianin)和水飞蓟丁(silichristin),尤其是水飞蓟宾)可以以原形或以与磷脂的复合物形式使用,如EP 0209038中所公开的那样。
特别优选水飞蓟宾与磷脂酰胆碱的复合物。
番茄提取物可以如EP 0818225、PCT/EP03/02749中所述进行制备,而锯齿棕提取物可以如EP 0250953中所公开的那样进行制备。
月桂酸优选为甲酯或乙酯或锌盐的形式。
为了施用5至20微克硒,可以将硒与不同非毒性载体的加合物用作硒的来源。特别优选甲基硒代半胱氨酸。
各种成分优选用适当的赋形剂配制成片剂、硬或软明胶胶囊剂或可饮用的剂型。
各种成分的平均日剂量是:水飞蓟宾100毫克至1克,优选150-300毫克;番茄红素2至30毫克,优选7.5毫克;月桂酸或它的非毒性的酯或盐20至80毫克,优选40毫克;锌的施用量是8至16毫克,优选12毫克;甲基硒代半胱氨酸形式的硒每天用量为5至20微克,优选10微克。
在使用水飞蓟宾或水飞蓟素的磷脂复合物的情况下,所述剂量是指活性成分的含量。
一个优选的组合物含有160毫克与磷脂酰胆碱复合的水飞蓟宾、7.5毫克番茄红素、22毫克月桂酸锌和12微克甲基硒代半胱氨酸。
各种成分用适当的赋形剂稀释,所述赋形剂应确保整个制剂具有可接受的吸收。使用这些组合物,良性前列腺增生症状如排尿困难、日间和夜间尿频以及前列腺增大的进程在前列腺患者中均得到减轻。在患有非激素依赖型前列腺癌的患者中,该组合降低血浆PSA值,表明它对细胞增殖具有直接作用。
下述实施例详细阐述了本发明。
实施例1
胶囊剂,其含有:
水飞蓟素与磷脂酰胆碱的复合物 240毫克
锯齿棕提取物 200毫克
含有10%番茄红素的番茄提取物 50毫克
实施例2
胶囊剂,其含有:
水飞蓟素与磷脂酰胆碱的复合物 160毫克
番茄红素 20毫克
月桂酸锌 30毫克
甲基硒代半胱氨酸 0.01毫克
Claims (7)
1.组合物,其包含:
a.游离形式或与磷脂复合的水飞蓟素或其组分;
b.纯形式或番茄(Lycoperisicum aesculentum)提取物形式的番茄红素;
c.月桂酸或其非毒性的酯或盐或锯齿棕(Serenoa repens)的亲脂性提取物;
d.任选地,锌盐和/或硒化合物。
2.权利要求1中所述的组合物,其中组分a.为与磷脂酰胆碱复合的水飞蓟素。
3.权利要求1或2中所述的组合物,其中组分c.为月桂酸的甲酯或乙酯或其锌盐。
4.以上权利要求中任一项所述的组合物,其中硒化合物为甲基硒代半胱氨酸。
5.以上权利要求中任一项所述的组合物,其含有日剂量为100毫克至1克的水飞蓟素或水飞蓟素或相当量的相应的磷脂复合物;2至30毫克番茄红素;20至80毫克月桂酸或它的酯或盐;8至16毫克锌和5至20微克甲基硒代半胱氨酸形式的硒。
6.权利要求5中所述的组合物,其含有160毫克与磷脂酰胆碱复合的水飞蓟素;7.5毫克番茄红素;22毫克月桂酸锌和12微克甲基硒代半胱氨酸。
7.以下成分的组合在制备药物或营养物中的用途:
a.游离形式或与磷脂复合的水飞蓟素或其组分;
b.纯形式或番茄提取物形式的番茄红素;
c.月桂酸或其非毒性的酯或盐或锯齿棕的亲脂性提取物;
d.任选地,锌盐和/或硒化合物,
所述药物或营养物用于治疗良性前列腺增生和用于治疗和预防非激素依赖型前列腺癌。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT001388A ITMI20031388A1 (it) | 2003-07-08 | 2003-07-08 | Formulazioni per il trattamento e la prevenzione di patologie della prostata. |
ITMI2003A001388 | 2003-07-08 |
Publications (1)
Publication Number | Publication Date |
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CN1816344A true CN1816344A (zh) | 2006-08-09 |
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Application Number | Title | Priority Date | Filing Date |
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CNA200480019235XA Pending CN1816344A (zh) | 2003-07-08 | 2004-06-17 | 用于治疗和预防前列腺病症的植物组合物 |
Country Status (12)
Country | Link |
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US (1) | US20060246153A1 (zh) |
EP (1) | EP1641478A1 (zh) |
JP (1) | JP2007528361A (zh) |
KR (1) | KR20060032996A (zh) |
CN (1) | CN1816344A (zh) |
AU (1) | AU2004255405A1 (zh) |
BR (1) | BRPI0412295A (zh) |
CA (1) | CA2531417A1 (zh) |
IT (1) | ITMI20031388A1 (zh) |
NO (1) | NO20060058L (zh) |
RU (1) | RU2006103631A (zh) |
WO (1) | WO2005004889A1 (zh) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101703158B (zh) * | 2009-11-26 | 2012-04-11 | 浙江汇能动物药品有限公司 | 一种含有番茄红素的畜禽肉质改良剂及其制备和应用 |
CN105106520A (zh) * | 2015-10-06 | 2015-12-02 | 常州亚当生物技术有限公司 | 一种保健品 |
CN111295199A (zh) * | 2017-11-01 | 2020-06-16 | 卡罗琳·西姆斯 | 包含植物性脂肪酸源的膳食组合物 |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
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US8221803B1 (en) | 2007-06-25 | 2012-07-17 | OncoNatural Solutions, Inc. | Composition for prostate health |
ITMI20080283A1 (it) * | 2008-02-22 | 2009-08-23 | Indena Spa | Composizioni per il trattamento di ipertrofia prostatica benigna, prostatiti, prostatosi e carcinoma prostatico |
DE102008012988A1 (de) | 2008-03-07 | 2009-09-10 | S.W. Patentverwertungs Ltd. | Zusammensetzung und Verwendungen zur Beeinflussung des Haarwachstums |
ITMI20130807A1 (it) * | 2013-05-16 | 2014-11-17 | Indena Spa | Combinazioni di estratti di serenoa repens e di estratti lipofili di zingiber officinalis e di echinacea angustifolia, loro uso e formulazioni che li contengono |
ITUB20150330A1 (it) * | 2015-02-05 | 2016-08-05 | Novamont Spa | Processo per il frazionamento di semi di piante oleaginose. |
JP2017214342A (ja) * | 2016-06-02 | 2017-12-07 | 日清オイリオグループ株式会社 | 排尿障害の予防用又は改善用組成物 |
IT201600081379A1 (it) * | 2016-08-03 | 2018-02-03 | Neilos S R L | Composizione farmaceutica per uso nel trattamento delle patologie prostatiche. |
Family Cites Families (10)
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IT1215291B (it) * | 1985-07-17 | 1990-01-31 | Inverni Della Beffa Spa | Complessi di flavanolignani con fosfolipidi, loro preparazione e relative composizioni farmaceutiche. |
IT1265312B1 (it) * | 1993-12-21 | 1996-10-31 | Indena Spa | Formulazioni contenenti carotenoidi e procarotenoidi associati a polifenoli nella prevenzione dei danni da abnorme produzione di |
US5895652A (en) * | 1996-07-29 | 1999-04-20 | Longevity Institute International | Method of metabolic adjuvanation and cellular repair |
EP1056464A1 (en) * | 1998-02-27 | 2000-12-06 | Nutramax Laboratories, Inc. | L-ergothioneine, milk thistle, and s-adenosylmethionine for the prevention, treatment and repair of liver damage |
US20030083383A1 (en) * | 1999-08-16 | 2003-05-01 | Spallholz Julian E. | Method of using synthetic L-Se-methylselenocysteine as a nutriceutical and a method of its synthesis |
ATE298233T1 (de) * | 2000-02-19 | 2005-07-15 | Goldschmidt Gmbh | Kosmetische und pharmazeutische öl-in-wasser- emulsionen von polyethermodifizierten polysiloxanen |
US6300377B1 (en) * | 2001-02-22 | 2001-10-09 | Raj K. Chopra | Coenzyme Q products exhibiting high dissolution qualities |
FR2829022B1 (fr) * | 2001-09-03 | 2004-09-24 | Oreal | Composition de fond de teint comprenant des pigments interferentiels |
US20030054053A1 (en) * | 2001-09-20 | 2003-03-20 | Charles Young | Methods and compositions for inhibiting the proliferation of prostate cancer cells |
EP1314438A1 (en) * | 2001-11-23 | 2003-05-28 | Nutricia N.V. | Anti-proliferative composition |
-
2003
- 2003-07-08 IT IT001388A patent/ITMI20031388A1/it unknown
-
2004
- 2004-06-17 BR BRPI0412295-0A patent/BRPI0412295A/pt not_active Application Discontinuation
- 2004-06-17 CN CNA200480019235XA patent/CN1816344A/zh active Pending
- 2004-06-17 RU RU2006103631/15A patent/RU2006103631A/ru not_active Application Discontinuation
- 2004-06-17 CA CA002531417A patent/CA2531417A1/en not_active Abandoned
- 2004-06-17 AU AU2004255405A patent/AU2004255405A1/en not_active Abandoned
- 2004-06-17 EP EP04740008A patent/EP1641478A1/en not_active Withdrawn
- 2004-06-17 WO PCT/EP2004/006550 patent/WO2005004889A1/en not_active Application Discontinuation
- 2004-06-17 JP JP2006518006A patent/JP2007528361A/ja active Pending
- 2004-06-17 US US10/563,380 patent/US20060246153A1/en not_active Abandoned
- 2004-06-17 KR KR1020067000215A patent/KR20060032996A/ko not_active Application Discontinuation
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2006
- 2006-01-05 NO NO20060058A patent/NO20060058L/no not_active Application Discontinuation
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101703158B (zh) * | 2009-11-26 | 2012-04-11 | 浙江汇能动物药品有限公司 | 一种含有番茄红素的畜禽肉质改良剂及其制备和应用 |
CN105106520A (zh) * | 2015-10-06 | 2015-12-02 | 常州亚当生物技术有限公司 | 一种保健品 |
CN111295199A (zh) * | 2017-11-01 | 2020-06-16 | 卡罗琳·西姆斯 | 包含植物性脂肪酸源的膳食组合物 |
Also Published As
Publication number | Publication date |
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ITMI20031388A1 (it) | 2005-01-09 |
EP1641478A1 (en) | 2006-04-05 |
JP2007528361A (ja) | 2007-10-11 |
BRPI0412295A (pt) | 2006-09-19 |
RU2006103631A (ru) | 2006-06-10 |
AU2004255405A1 (en) | 2005-01-20 |
US20060246153A1 (en) | 2006-11-02 |
WO2005004889A1 (en) | 2005-01-20 |
NO20060058L (no) | 2006-01-05 |
CA2531417A1 (en) | 2005-01-20 |
KR20060032996A (ko) | 2006-04-18 |
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