JP2009514901A - 化合物の医薬品的使用 - Google Patents
化合物の医薬品的使用 Download PDFInfo
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- JP2009514901A JP2009514901A JP2008539185A JP2008539185A JP2009514901A JP 2009514901 A JP2009514901 A JP 2009514901A JP 2008539185 A JP2008539185 A JP 2008539185A JP 2008539185 A JP2008539185 A JP 2008539185A JP 2009514901 A JP2009514901 A JP 2009514901A
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- psidium
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- guajava
- cattleianum
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- 239000000284 extract Substances 0.000 claims abstract description 32
- 241000508269 Psidium Species 0.000 claims abstract description 26
- 235000013929 Psidium pyriferum Nutrition 0.000 claims abstract description 21
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- 230000000694 effects Effects 0.000 claims abstract description 18
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Abstract
Description
Psidium guajavaの葉から抽出物を調製する製造プロセスは以下の工程により記述される:
−Psidium guajavaの葉を細かい粉末に粉砕する
−エタノールで抽出する
−抽出液を減圧し、エタノールが蒸発するまで濃縮する
−遠心により不溶性の不純物を除去し、浄化された液体を得る
−浄化された液体をマクロ多孔性樹脂を充填したクロマトグラフィーのカラムにロードし、水によりさらに不純物を取り除き、その後エタノールにより脱着してエタノール性溶出液を集める
−抽出液を乾燥させ、Psidium guajava抽出物を得る。
細かく砕いた原料(生のPsidium guajavaの果実)500gが計量され、80%エタノール2000mL中に移される(三口丸底フラスコ)。混合物は60℃にて2時間穏やかに混合される。溶液をろ過する。ろ液を集め、同様の条件下、80%エタノール2000mLを用いて抽出を繰り返す。溶液は再びろ過され、両方のろ液を合わせる。
粉砕されたPsidium guajavaの葉の粉末20kgが計量されて250Lのボイラーに入れられ、その後80%エタノール160Lが添加され、混合物は60℃にて2時間混合される。溶液がろ過され、再び80%エタノール160Lが残渣に注がれる。混合物はさらに60℃にて2時間抽出、ろ過され、その後二つの抽出工程のろ液は一緒に混合される。60℃減圧下でエタノールがほとんどなくなるまで、得られた混合物は濃縮される。真空度は−0.09MPaである。得られた混合物は遠心される。遠心後、水40Lを使用して残渣を洗浄し、ろ液は一緒に混合される。合わせられたろ液は、マクロクロスリンクしたマクロ多孔性樹脂(Type Amberlite XAD4)を通して分離される。まず、水160Lを用いて吸着後の樹脂が洗浄され、それにより不純物の一部を取り除くことができる。次に80%エタノール350Lが脱着工程のために使用される。黄褐色の脱着された液体が集められる。脱着された液体は、60℃減圧下で濃縮される。その後、真空乾燥機中で5時間乾燥される。
方法:
DP−IVの活性は、比色分析によって測定された。
実施例3に従って得られたPsidium guajava抽出物は、攪拌条件下、45℃で24時間、蒸留水に抽出された。その後、抽出物は、遠心(15000rpm、15分)、ろ過(シリンジフィルター、0.45μM)により浄化され、適切に希釈されて試験アッセイにかけられた。
結果は、阻害剤を加えていない試料において得られた試験結果を、阻害剤またはPsidium guajava抽出物(どちらも濃度をふって)を加えた試料において得られた試験結果と比較して得られた%阻害として表される。
アッセイはよく知られた通常の手順を用いて、較正された。
以下において別段の指示がない限り、使用した原料および方法は、実施例4の原料および方法と同じであった。
グアヤベリンはHEPESバッファーに溶解され(20分。超音波処理に続いて室温にて2時間振とう)、適切に希釈されて試験アッセイにかけられた。希釈液はHEPESバッファーの添加により調製された。試験された濃度は、70から280μg/mL試験アッセイの間であった。
結果は、陽性対照試料(阻害剤なし)において得られた試験結果を、グアヤベリンを異なる濃度で加えた試料において得られた試験結果と比較して得られた%活性として表される。
図3および4に示されるように、グアヤベリンは、DP−IVの明確な用量依存性阻害をもたらす。選択された試験アッセイシステムにおいて、140から210μg/mL試験アッセイ(100から150μg/アッセイ体積)間の濃度が、約50%のDP−IV阻害をもたらした。
Claims (10)
- DP−IVまたはDP−IV様の酵素の活性に関連するおよび/またはそれにより引き起こされる病気および/または疾患の治療用薬剤の製造のための、Psidium cattleianum、Psidium cattleianum ssp. Lucidum、Psidium guajava、Psidium guineense、Psidium littorale、Psidium molleおよびPsidium schiedeanumからなるグループから選択される植物の抽出物の使用。
- 植物がPsidium guajavaである、請求項1に記載の使用。
- 抽出物が葉、果実および/または植物の樹皮の抽出物である、請求項1または2に記載の使用。
- 抽出物が、水、メタノール、エタノール、アセトン、酢酸エチル、およびそれらの混合物のグループから選択される溶媒を用いて調製された抽出物である、請求項1−3のいずれかに記載の使用。
- 抽出物が固体の形である、請求項1−4のいずれかに記載の使用。
- グアヤベリンを0.5重量%またはそれ以上、好ましくは10から50重量%まで含むことを特徴とする、請求項1−5のいずれかに記載の使用。
- DP−IVまたはDP−IV様の酵素の活性に関連するまたはそれにより引き起こされる病気または疾患の治療用の薬剤の製造のための、グアヤベリンおよび/またはそれらの薬学的に許容される塩またはエステルの使用。
- 病気および/または疾患が糖尿病、肥満、および/またはアテローム性動脈硬化症などのようなグルコース代謝疾患である、請求項1−7のいずれかに記載の使用。
- 薬剤として使用するための、Psidium cattleianum、Psidium cattleianum ssp. Lucidum、Psidium guajava、Psidium guineense、Psidium littorale、Psidium molleおよびPsidium schiedeanumからなるグループから選択される植物の抽出物。
- 栄養成分として、例えば機能食品の組成物としてソフトドリンク中に、または化粧品中に成分として、グアヤベリンおよび/またはそれらの薬学的に許容される塩またはエステルの使用、および/またはPsidium cattleianum、Psidium cattleianum ssp. Lucidum、Psidium guajava、Psidium guineense、Psidium littorale、Psidium molleおよびPsidium schiedeanumからなるグループから選択される植物の抽出物の使用。
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AT0183305A AT502717A1 (de) | 2005-11-09 | 2005-11-09 | Pharmazeutische verwendung einer verbindung |
ATA1833/2005 | 2005-11-09 | ||
PCT/AT2006/000454 WO2007053865A1 (en) | 2005-11-09 | 2006-11-08 | Pharmaceutical use of a compound |
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US20080293644A1 (en) * | 2007-04-27 | 2008-11-27 | Thomas Eidenberger | Guava extract |
JP2010105922A (ja) * | 2008-10-28 | 2010-05-13 | Uha Mikakuto Co Ltd | Lox−1アンタゴニスト作用剤 |
CA2823534C (en) | 2010-12-28 | 2018-09-11 | Mary Kay Inc. | Topical composition comprising a psidium guajava extract and a kunzea ericoides extract for providing sebum control and treating acne |
US8877259B2 (en) | 2012-02-09 | 2014-11-04 | Mary Kay Inc. | Cosmetic formulation |
CN103565928A (zh) * | 2013-11-01 | 2014-02-12 | 华南农业大学 | 一种番石榴降糖活性组分、制备方法及用途 |
CN104173975A (zh) * | 2014-08-25 | 2014-12-03 | 河南科技大学第一附属医院 | 一种用于治疗糖尿病的中药组合物 |
EA201791982A1 (ru) | 2015-03-09 | 2020-02-17 | Интекрин Терапьютикс, Инк. | Способы лечения неалкогольной жировой болезни печени и/или липодистрофии |
DE102016102271A1 (de) | 2016-02-10 | 2017-08-10 | Pm-International Ag | Zusammensetzung zur Reduzierung und/oder Hemmung einer intestinalen Glucose-Resorption, Nahrungsergänzungsmittel, Verwendung der Zusammensetzung und Verfahren zur Herstellung des Nahrungsergänzungsmittels |
DE102016102265A1 (de) | 2016-02-10 | 2017-08-10 | Pm-International Ag | Zusammensetzung zur Reduzierung und/oder Hemmung einer intestinalen Glucose-Resorption, Nahrungsergänzungsmittel, Verwendung der Zusammensetzung und Verfahren zur Herstellung des Nahrungsergänzungsmittels |
CN108882742A (zh) * | 2016-02-10 | 2018-11-23 | Pm国际股份公司 | 用以减少和/或阻止肠道葡萄糖吸收的含有番石榴苷的组合物、膳食补充剂、组合物的用途和膳食补充剂的制备方法 |
CA3058806A1 (en) | 2017-04-03 | 2018-10-11 | Coherus Biosciences Inc. | Ppar.gamma. agonist for treatment of progressive supranuclear palsy |
WO2020025137A1 (de) * | 2018-08-02 | 2020-02-06 | Pm-International Ag | Gänseblümchenextrakt |
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AT502717A1 (de) | 2007-05-15 |
WO2007053865A9 (en) | 2007-07-12 |
JP5717317B2 (ja) | 2015-05-13 |
US20090186110A1 (en) | 2009-07-23 |
WO2007053865A1 (en) | 2007-05-18 |
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