JP6810814B2 - 抗腫瘍薬の調製におけるスペルミン及びその誘導体の使用 - Google Patents
抗腫瘍薬の調製におけるスペルミン及びその誘導体の使用 Download PDFInfo
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- JP6810814B2 JP6810814B2 JP2019551698A JP2019551698A JP6810814B2 JP 6810814 B2 JP6810814 B2 JP 6810814B2 JP 2019551698 A JP2019551698 A JP 2019551698A JP 2019551698 A JP2019551698 A JP 2019551698A JP 6810814 B2 JP6810814 B2 JP 6810814B2
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- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
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Description
上記化合物のうちの少なくとも2つを組み合わせて使用することにより、より良い腫瘍の治療又は改善効果が得られることが期待される。
さらなる生化学的酵素実験、細胞生物学実験により、SAICARの蓄積に対する化合物スペルミンの抑制率が71.1%に達することができ、PAICS活性を抑制することにより、毒性化合物SAICARの蓄積が減少することが確認された。
さらなる細胞生物学実験、ウエスタンブロット(Western Blot)実験により、化合物スペルミンが癌遺伝子mycに対して顕著な発現抑制役割を果たすことができ、これにより、癌遺伝子mycの発現量が明らかに減少する(ウェスタンブロット実現結果が図4に示すように)ことが確認された。
さらなる細胞生物学実験により、化合物スペルミンが肺癌細胞株A549、肺癌細胞株H1299、乳癌細胞株MD468、乳癌細胞株MD231に対していずれも効果的な抑制役割(薬物が48時間投与される場合のIC50値が次の表に示される)を果たすことができ、抗がん効果が非常に顕著であることが確認された。
Claims (4)
- 腫瘍を治療又は緩和するための組成物であって、その活性成分がスペルミン又はその薬学的に許容される誘導体のうちの少なくとも一つから選択され、
前記腫瘍が、ホスホリボシルアミノイミダゾールスクシノカルボキサミド合成酵素/ホスホリボシルアミノイミダゾールカルボキシラーゼ(phosphoribosylaminoimidazole succinocarboxamide synthetase /phosphoribosylaminoimidazole carboxylase:PAICS)の高発現および/またはサクシニル-5-アミノイミダゾール-4-カルボキサミド-1-リボース-5-ホスフェート(succinyl-5-aminoimidazole-4-carboxamide-1-ribose-5-phosphate:SAICAR)の過度蓄積の存在を特性として有する腫瘍であり、
前記の薬学的に許容される誘導体が、スペルミンと、炭素原子数1〜6のカルボン酸、炭素原子数1〜6のアルコール又は炭素原子数1〜6のアミンとの縮合反応によって得られる、低級エステル、低級エーテル、低級アルキル基置換物、薬用塩、低級アミドであることを特徴とする、腫瘍の治療又は緩和用組成物。 - 前記組成物はさらに少なくとも一種の既存の腫瘍を治療するための活性成分を含むことを特徴とする、請求項1に記載の腫瘍の治療又は緩和用組成物。
- 組成物はさらに薬学的又は食品に許容される補助材料を含むことを特徴とする、請求項1又は2に記載の腫瘍の治療又は緩和用組成物。
- 前記腫瘍が、腫瘍は急性リンパ性白血病、肺癌、神経膠腫、前立腺癌、結腸直腸癌、胃癌、肝癌、食道癌、大腸癌、悪性リンパ腫、子宮頸癌、鼻咽頭癌、乳癌、皮膚癌、膀胱癌から選択され、
前記腫瘍は、PAICSの高発現および/またはSAICARの過度蓄積の存在を特性として有する、請求項1〜3のいずれか1項に記載の腫瘍の治療又は緩和用組成物。
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