マイトマイシンC

解説マイトマイシンC，Streptomyces caespitosusが産生する抗腫瘍抗生物質．青紫色の結晶．融点360 ℃．UV(メタノール)λmax 216，360，560 nm(ε 24800，24800，2)．水，エタノールに難溶，ジエチルエーテルに不溶．グラム陽性菌，グラム陰性菌，結核菌などに強い抗菌力をもつ．内服または注射で，慢性リンパ性白血病，慢性骨髄性白血病，胃がん，肝がん，結腸·直腸がん，肺がん，子宮頸がん，子宮体がん，乳がんなどのがんの治療に単独あるいは併用で用いられる．作用機序は，がん細胞内で還元された活性化体が，二本鎖DNAのグアニン残基に結合して架橋し，DNAの複製を阻害することである．LD50 4 mg/kg(マウス，静注)．

用途DNA のグアニンと結合して架 橋切断を起し、DNA 生合成阻害作用を示しま す。

用途制癌作用研究用。

説明Mitomycin C is naturally produced by Streptomyces caespitosus, an Actinobacteria found in soil. Mitomycin C has antibiotic and antitumor activities and has been studied extensively since the 1950s. A unique feature of this drug is strong bioreductive alkylation under hypoxic conditions. Oxygen-poor cells internal to solid tumors provide an environment in which this drug is highly activated. As an antitumor agent, it has shown efficacy in a wide variety of cancers, including gastric cancer, pancreatic cancer, breast cancer, non-small-cell lung cancer, cervical cancer, prostate cancer, and bladder cancer. The sideeffect profile is large, which prohibits its widespread use. Mitomycin C is antibacterial to gram-positive, gram-negative, and acid-fast bacilli.

使用Mitomycin C is the most studied of a family of highly distinctive blue/purple metabolites produced by several Streptomyces species. Mitomyin C exhibits potent antibacterial and antitumour activity and inhibits DNA synthesis by intercalation, blocking nuclear division with the induction of apoptosis in cancer cells.

一般的な説明Blue-violet crystals. Used as an anti-tumor antibiotic complex.

純化方法Mitomycin C forms blue-violet crystals from *C6H6/pet ether. It is soluble in Me2CO, MeOH and H2O, moderately soluble in *C6H6, CCl4 and Et2O but insoluble in pet ether. It has UV max at 216, 360 and a weak peak at 560nm in MeOH. [Stevens et al. J Med Chem 8 1 1965, Shirahata & Hirayama J Am Chem Soc 105 7199 1983, Beilstein 25 III/IV 516.]