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Doxorubicinol hydrochloride

Doxorubicinol hydrochloride用途

盐酸阿霉素(13-二氢阿霉素盐酸盐)是阿霉素的次级醇代谢产物[1]。

Doxorubicinol hydrochloride名称

[ CAS 号 ]:
63950-05-0

[ 英文名 ]:
Doxorubicinol hydrochloride

Doxorubicinol hydrochloride生物活性

[ 描述 ]:

盐酸阿霉素(13-二氢阿霉素盐酸盐)是阿霉素的次级醇代谢产物[1]。

[ 相关类别 ]:

研究领域 >> 癌症

[体外研究]

盐酸阿霉素是由阿霉素侧链羰基(C13)双电子NADPH依赖性还原为仲醇[1]生成的。与阿霉素相比,盐酸阿霉素具有显著较低的DNA结合活性。此外,虽然盐酸阿霉素保留在细胞质或溶酶体中,但阿霉素主要积聚在细胞核中[1]。

[体内研究]

在体内,在荷瘤小鼠中,尼罗替尼作为ABCB1抑制剂,被发现可增加癌组织中阿霉素和盐酸阿霉素的积累。这意味着盐酸阿霉素较弱的抗癌活性可能与其增加对ABC转运体的亲和力有关,从而导致该药物的细胞内浓度降低[1]。与野生型小鼠相比,mdr1a(-/-)小鼠的阿霉素终末半衰期和血浆浓度-时间曲线下面积分别高出1.6倍和1.2倍。阿霉素及其代谢物盐酸阿霉素在mdr1a(-/-)小鼠心脏中的滞留时间显著延长[2]。

[参考文献]

[1]. Kamil Piska, et al. Metabolic carbonyl reduction of anthracyclines - role in cardiotoxicity and cancer resistance. Reducing enzymes as putative targets for novel cardioprotective and chemosensitizing agents. Invest New Drugs. 2017 Jun;35(3):375-385.

[2]. J van Asperen, et al. Increased accumulation of doxorubicin and doxorubicinol in cardiac tissue of mice lacking mdr1a P-glycoprotein. Br J Cancer. 1999 Jan;79(1):108-13.

Doxorubicinol hydrochloride物理化学性质

[ 密度 ]:
1.61g/cm3

[ 沸点 ]:
828.7ºC at 760 mmHg

[ 熔点 ]:
188-192ºC

[ 分子式 ]:
C₂₇H₃₂ClNO₁₁

[ 分子量 ]:
581.99600

[ 闪点 ]:
455ºC

[ 精确质量 ]:
581.16600

[ PSA ]:
209.23000

[ LogP ]:
1.29540

[ 折射率 ]:
1.716

Doxorubicinol hydrochloride毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QI9295800

CHEMICAL NAME :: 5,12-Naphthacenedione, 10-((3-amino-2,3,6-trideoxy-alpha-L-lyxo-hexopyranosy l)oxy)-8-(1,2- dihydroxyethyl)-7,8,9,10-tetrahydro-6,8,11-trihydroxy -1-methoxy-, hydrochloride

CAS REGISTRY NUMBER :: 63950-05-0

LAST UPDATED :: 198406

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C27-H31-N-O11.Cl-H

MOLECULAR WEIGHT :: 582.05

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Mammal - species unspecified Lymphocyte

DOSE/DURATION :: 52 umol/L

REFERENCE :: FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 32,315,1977