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苏拉明

苏拉明用途

Suramin是具有各种生物活性的多磺化萘脲。Suramin是DNA topoisomerase II抑制剂,IC50值为5 μM。

苏拉明名称

[ CAS 号 ]:
145-63-1

[ 中文名 ]:
苏拉明

[ 英文名 ]:
Suramin

[英文别名 ]:

Naphuride
EINECS 205-658-4
Naganin
Farma
Antrypol
Germanin
Fourneau
Suramine
Belganyl
Naganol

苏拉明生物活性

[ 描述 ]:

Suramin是具有各种生物活性的多磺化萘脲。Suramin是DNA topoisomerase II抑制剂,IC50值为5 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> P2Y受体

研究领域 >> 癌症

[ 靶点 ]

IC50: 5 μM (DNA topoisomerase II)[3]

[体外研究]

苏拉明抑制培养的HeLa细胞中的细胞增殖和DNA合成。通过40μM苏拉明完全消除SV40 DNA的复制。 DNA聚合酶α对较低浓度的苏拉明敏感(IC50 =8μM)比DNA聚合酶δ(IC50 =36μM)敏感,而DNA聚合酶β对药物相对不敏感(IC50为90μM)[1]。苏拉明是细菌RecA蛋白的DNA链交换和ATP酶活性的有效抑制剂。苏拉明抑制RecA催化的LexA阻遏蛋白水解切割。苏拉明这种抑制作用的机制涉及其拆解RecA-单链DNA细丝的能力[2]。苏拉明是核酶DNA拓扑异构酶II的有效抑制剂。苏拉明抑制纯化的酵母拓扑异构酶II,IC50约为5μM[3]。

[体内研究]

与对照大鼠相比,苏拉明治疗在第21天显示出较低的肺动脉压,右心室肥大和远端血管肌肉化值。苏拉明治疗抑制PA-SMC增殖并减弱炎症反应和胶原沉积[4]。

[激酶实验]

ATP酶测定在10μL反应混合物中进行，所述反应混合物含有20mM Tris-HCl（pH 7.5），1mM DTT，8mM MgCl2,5μMM13环状ssDNA，来自指定细菌物种的2.5μMRecA和增加浓度的苏拉明。通过加入2mM [α-32P] ATP引发反应，在37℃温育30分钟并通过加入25mM EDTA终止反应[2]。

[动物实验]

大鼠：为了评估苏拉明的潜在预防和疗效，在MCT注射后将大鼠随机分成4组。在预防策略中，治疗在第一天开始，并且一组每周两次静脉内接受10mg / kg苏拉明，持续3周，而第二组在相同时间点仅接受载体。为了评估苏拉明的潜在疗效，给予大鼠MCT并且不进行处理21天，然后将其随机分成两组，随后从第21天至第42天（包括苏拉明或载体）用苏拉明或载体治疗。从MCT注射的第21天到对应于治疗期的第42天评估苏拉明对存活的影响[4]。

[参考文献]

[1]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7.

[2]. Nautiyal A, et al. Suramin is a potent and selective inhibitor of Mycobacterium tuberculosis RecA protein and the SOS response: RecA as a potential target for antibacterial drug discovery. J Antimicrob Chemother. 2014 Jul;69(7):1834-43.

[3]. Bojanowski K, et al. Suramin is an inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcomacells. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.

[4]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.

[相关活性小分子]

苏拉明物理化学性质

[ 分子式 ]:
C₅₁H₄₀N₆O₂₃S₆

[ 分子量 ]:
1297.28000

[ 精确质量 ]:
1296.05000

[ PSA ]:
534.03000

[ LogP ]:
13.66600

[ 折射率 ]:
1.777

[ 储存条件 ]:
通风低温干燥

苏拉明毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QM6900000

CHEMICAL NAME :: 1,3,5-Naphthylenetrisulfonic acid, 8,8'-(ureylenebis(m-phenylenecarbonylimino(4-methyl- m-phenylene)carbonylimino))di-

CAS REGISTRY NUMBER :: 145-63-1

BEILSTEIN REFERENCE NO. :: 3230873

LAST UPDATED :: 199710

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C51-H40-N6-O23-S6

MOLECULAR WEIGHT :: 1297.33

WISWESSER LINE NOTATION :: L66J BSWQ DSWQ GSWQ JMVR D1 CMVR CMVMR CVMR B1 EVM- JL66J BSWQ DSWQ GSWQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 46 mg/kg/5W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified

REFERENCE :: NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928- Volume(issue)/page/year: 314,1455,1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 620 mg/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

REFERENCE :: AVPCAQ Advances in Pharmacology and Chemotherapy. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.7-20, 1969-84. Volume(issue)/page/year: 15,289,1978 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3 gm/kg/16W-I

TOXIC EFFECTS :: Liver - other changes Liver - changes in liver weight Endocrine - changes in spleen weight

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 19,266,1991 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 300 mg/kg

SEX/DURATION :: female 7-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CRSBAW Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1849- Volume(issue)/page/year: 167,1518,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 250 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: CBINA8 Chemico-Biological Interactions. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1969- Volume(issue)/page/year: 58,149,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 150 mg/kg

SEX/DURATION :: female 9-11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: CRSBAW Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1849- Volume(issue)/page/year: 167,1518,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 195 mg/kg

SEX/DURATION :: female 9-11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

REFERENCE :: CRSBAW Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1849- Volume(issue)/page/year: 167,1518,1973

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 195 mg/kg

SEX/DURATION :: female 9-11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

REFERENCE :: CRSBAW Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1849- Volume(issue)/page/year: 167,1717,1973

苏拉明