JP5956036B2 - 冷メントール受容体trpm8の低分子量モジュレーターの検出および使用 - Google Patents
冷メントール受容体trpm8の低分子量モジュレーターの検出および使用 Download PDFInfo
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- JP5956036B2 JP5956036B2 JP2015158967A JP2015158967A JP5956036B2 JP 5956036 B2 JP5956036 B2 JP 5956036B2 JP 2015158967 A JP2015158967 A JP 2015158967A JP 2015158967 A JP2015158967 A JP 2015158967A JP 5956036 B2 JP5956036 B2 JP 5956036B2
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Description
1. 一般用語の定義:
文献中には、「TRPM8」の各種同義語:TRPP8、LTRPC6、CMR1、MGC2849、一過性受容体電位カチオンチャネル、サブファミリーM、メンバー8がある。本発明においては全ての名称が包含される。また、特にスプライス変異体、アイソフォーム(例えばTRPM8 CRA_a、TRPM8 CRA_bなど)のようなこの受容体の全ての機能的改変、およびヒト、マウス、ラットなどの様々な生物に由来する全ての類似の受容体も包含される。各種受容体のヌクレオチド配列およびアミノ酸配列はそれ自体公知であり、配列データベースにリストされている。このように、例えばhTRPM8の配列情報は、番号NM_024080で登録されている。
本発明は、第1に、冷メントール受容体TRMP8の(特にヒトTRPM8受容体)のin-vitroまたはin-vivoモジュレーション方法であって、該受容体を、ヒトTRPM8受容体を組換え発現する細胞を用いた(特に標準条件下における)細胞活性試験においてCa2+イオンに対するこれらの細胞の透過性をモジュレートする多核有機化合物から選択される少なくとも1種の化合物と接触させる、上記方法に関する。
化合物1(CAS番号:99602-94-5(3R-cis形態))
化合物2(CAS番号:165753-08-2)
化合物3(CAS番号:338771-57-6)
化合物4(CAS番号:878942-21-3)
化合物5(CAS番号:748783-13-3)
上記の改変形態または誘導体は、これらが所望の生物学的活性(受容体TRPM8モジュレーティング)をさらに示す場合、機能的類似体または機能的等価化合物とも呼ばれる。
a) 抗癌剤組成物、膀胱疾患の治療用の組成物、鎮痛剤などの医薬組成物、
b) アイスクリーム、ムース、クリーム、飲料、菓子などの食品、
c) 歯磨剤、マウスウォッシュ、チューインガム、ブレスフレッシュナーなどの口腔ケア組成物、
d) サンクリーム、サンバーンクリーム、ローション、シャンプー、プラスター、マウスウォッシュ、ローション、シェービングクリーム、コンディショナー、フェイスクレンザー、石鹸、バスオイルおよびバスフォーム、制汗剤、デオドラントなどのスキンケアまたはヘアケア組成物、
e) 昆虫忌避剤、殺虫剤
から選択される。
実施例1-ヒトTRPM8のクローニング
ヒトTRPM8受容体のクローニングの出発点は、LnCaP cDNAライブラリーである。このライブラリーは、例えば市販されており(例えばBioChain, Hayward, USA)、またはアンドロゲン感受性ヒト前立腺癌細胞株LnCaP(例えばATCC、CRL1740またはECACC、89110211)から、標準的なキットを使用して作成することができる。
http://www.ncbi.nlm.nih.gov/entrez/viewer.fcgi?db=nuccore&id=109689694を参照)は、PCR増幅し、標準的な方法を用いてクローン化することができる。この方法で単離したヒトTRPM8遺伝子は、プラスミドpInd_M8を作成するために使用した。プラスミドpInd_M8の構造は、図2に記載のプラスミドマップによって示される。
試験細胞系として、ヒトTRPM8 DNA(上記のプラスミドpInd-M8を参照)で安定にトランスフェクトしたHEK293細胞株を作成する。ここで好ましいのは、導入されたプラスミドを介して、テトラサイクリンによるTRPM8発現の誘導という選択肢を与えるHEK293である。
Behrendt H.J.ら, Br. J. Pharmacol. 141, 2004, 737-745による文献に既述された試験と同等の試験を行う。これらの受容体のアゴニスト化またはアンタゴニスト化は、Ca2+感受性色素(例えばFURA、Fluo-4等)を用いて定量化することができる。それら自身で、アゴニストはCa2+シグナルの増加をもらし;アンタゴニストは、例えばメントールの存在下でCa2+シグナルの低下をもたらす(いずれの場合も、Ca2+の結果として異なる蛍光特性を有する色素Fluo-4によって検出される)。
最初に細胞培養フラスコ中で、形質転換したHEK細胞の新鮮な培養物を、それ自体公知の方法で調製する。この試験細胞HEK293-TRPM8細胞を、細胞培養フラスコからトリプシンを用いて剥離し、40,000細胞/ウェルを、100μlの培地と共に96ウェルプレート(ポリ-D-リシンでコーティングしたGreiner # 655948)に播種した。受容体TRPM8を誘導するため、テトラサイクリンを成長培地(DMEM/HG、10% FCSテトラサイクリン非含有、4mM L-グルタミン、15μg/ml ブラストサイジン、100μg/ml ハイグロマイシンB、1μg/ml テトラサイクリン)に加える。翌日、細胞にFluo-4AM色素を負荷し、試験を行う。この試験手順は以下のとおりである:
- いずれの場合も、100μl/ウェルの色素溶液Ca-4キット(RB 141(Molecular Devices社))を、100μlの培地(DMEM/HG、10% FCSテトラサイクリン非含有、4 mM L-グルタミン、15μg/ml ブラストサイジン、100μg/ml ハイグロマイシンB、1μg/ml テトラサイクリン)に添加する
- ハッチングキャビネット中で、30分間/37℃/5% CO2、30分間/室温(RT)でインキュベーションする
- 試験物質(200μlのHBSSバッファー中で各種濃度)、ならびに陽性対照(200μlのHBSSバッファー中で各種濃度のメントール、イシリンおよびイオノマイシン)および陰性対照(200μlのHBSSバッファーのみ)も調製する
- 50μl/ウェル量の試験物質を添加し、(例えば、アッセイ装置FLIPR(Molecular Devices社)またはNovoStar(BMG社)中で)485nm励起、520nm発光で蛍光の変化を測定し、様々な物質/濃度の有効性を評価し、EC50値を測定する。
下記の組成のマウスウォッシュを調製する:
エタノール 95% 177ml
ソルビトール 70% 250g
表2に記載のTRPM8アゴニスト
(エタノール中の1%溶液として) 50ml
ハッカ油 0.30g
サリチル酸メチル 0.64g
オイカリプトール 0.922g
チモール 0.639g
安息香酸 1.50g
Pluronic(登録商標)F127
非イオン性界面活性剤 5.00g
サッカリンナトリウム 0.60g
クエン酸ナトリウム 0.30g
クエン酸 0.10g
水 適量1リットル
マウスウォッシュを調製するため、上記の成分を記載の量で一緒に混合する。
[1] 冷メントール受容体TRMP8のin-vitroまたはin-vivoモジュレーション方法であって、該受容体を、ヒトTRPM8受容体を組換え発現する細胞を用いた細胞活性試験においてCa 2+ イオンに対するこれらの細胞の透過性をモジュレートする多核有機化合物から選択される少なくとも1種の化合物と接触させる、前記方法。
[2] モジュレーティング化合物が、互いに独立して単環もしくは多環の炭素環または複素環である少なくとも2個の4〜7員環を有し、且つこれらの環の少なくとも2個が場合により縮合していてもよい、1に記載の方法。
[3] モジュレーターが、細胞のCa 2+ イオン透過性に対するアゴニストまたはアンタゴニスト作用を有する、1または2に記載の方法。
[4] モジュレーターが、以下の式1〜19:
で表される化合物から選択される化合物である、1〜3のいずれかに記載の方法。
[5] ヒトおよび/または動物において冷感を誘発するための、1〜4のいずれかに定義されるTRPM8受容体モジュレーターの使用。
[6] 医薬組成物の活性成分としての、1〜4のいずれかに定義されるTRPM8受容体モジュレーターの使用。
[7] 前立腺癌の治療のための、膀胱虚弱の治療のための、または疼痛治療における、1〜4のいずれかに定義されるTRPM8受容体モジュレーターの使用。
[8] 昆虫忌避剤または殺虫剤としての、1〜4のいずれかに定義されるTRPM8受容体モジュレーターの使用。
[9] 包装において冷感を誘発するための、1〜4のいずれかに定義されるTRPM8受容体モジュレーターの使用。
[10] 織物において冷感を誘発するための、1〜4のいずれかに定義されるTRPM8受容体モジュレーターの使用。
[11] TRPM8受容体のメディエーターとして使用するための、1〜4のいずれかに定義される物質。
[12] 少なくとも1種の1〜4のいずれかに定義される化合物を含む組成物。
[13] 以下:
a) 抗癌剤、膀胱疾患の治療用薬剤、鎮痛剤などの医薬組成物、
b) アイスクリーム、ムース、クリーム、飲料、菓子などの食品、
c) 歯磨剤、マウスウォッシュ、チューインガムなどの口腔ケア組成物、
d) サンクリーム、サンバーンクリーム、ローション、シャンプー、プラスターなどのスキンケアまたはヘアケア組成物、
e) 昆虫忌避剤、殺虫剤
から選択される、12に記載の組成物。
[14] 少なくとも1種の1〜4のいずれかに定義される化合物で仕上げられた、例えばシャツ、ズボン、ソックス、タオルなどの織物製品。
[15] 少なくとも1種の1〜4のいずれかに定義される化合物を結合させた包装材。
Claims (11)
- ヒトおよび/または動物において冷感を誘発するための、請求項1に記載の組成物。
- 医薬組成物の活性成分としての、請求項1に記載の組成物。
- 前立腺癌の治療のための、膀胱虚弱の治療のための、または疼痛治療のための、請求項1に記載の組成物。
- 昆虫忌避剤または殺虫剤としての、請求項1に記載の組成物。
- 包装において冷感を誘発するための、請求項1に記載の組成物。
- 織物において冷感を誘発するための、請求項1に記載の組成物。
- 請求項1に記載のいずれかの化合物をTRPM8受容体のメディエーターとして使用するための、請求項1に記載の組成物。
- 以下:
a)医薬組成物、
b)食品、
c)口腔ケア組成物、
d)スキンケアまたはヘアケア組成物、あるいは
e) 昆虫忌避剤、殺虫剤
のためのものである、請求項1に記載の組成物。 - 請求項1に記載の組成物で仕上げられた、織物製品。
- 請求項1に記載の組成物を結合させた包装材。
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