Aeroplysinin 1

Aeroplysinin 1用途

Aeroplysinin 1 ((+)-Aeroplysinin-1),从海洋海绵中分离出的次生代谢产物,对革兰氏阳性细菌 (bacteria) 显示出有效的抗生素作用,并具有针对 HIV-1 的抗病毒活性 (IC50=14.6 μM)。Aeroplysinin 1 具有抗炎,抗血管生成和抗肿瘤活性。Aeroplysinin 1诱导内皮细胞凋亡 (apoptosis)。

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Aeroplysinin 1名称

[ CAS 号 ]:
28656-91-9

[ 英文名 ]:
Aeroplysinin(Aeroplysinin-1)

[英文别名 ]:

AEROPLYSININ,APLYSINA AEROPHOBA
aeroplysinin 1
AEROPLYSININ
Aeroplysinin I

Aeroplysinin 1生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 抗感染 >> HIV

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Bacterial

HIV-1:14.6 μM (IC50)

Apoptosis

[体外研究]

气溶素1对肿瘤细胞(HT-1080、HTC-116、HeLa、THP-1、NOMO-1和HL-60细胞)具有抗增殖作用,其ic50在2.3~17μM之间[1]。Aeroplysin-1还表现出对HIV-1的抗病毒活性,这是由于其逆转录酶活性受到抑制所致[1]。Aeroplysinin 1可抑制P.phosphoreum、C.wailesii、P.minimum和HIV,IC50分别为3.5、5.6、7.0和14.6μM[1]。气溶素1抑制人内皮细胞(EVLC-2、HMEC、RF-24和HUVEC细胞),其ic50在2.6到4.7μM之间[2]。(+)-aeroplysin-1(0.25-0.5μM)可阻断MCF-7和ZR-75-1人乳腺癌细胞的EGF依赖性增殖,并抑制配体诱导的EGF受体内吞作用[3]。

[参考文献]

[1]. García-Vilas JA, et al. Aeroplysinin-1, a Sponge-Derived Multi-Targeted Bioactive Marine Drug. Mar Drugs. 2015;14(1):1. Published 2015 Dec 22.

[2]. Martínez-Poveda B, et al. The brominated compound aeroplysinin-1 inhibits proliferation and the expression of key pro- inflammatory molecules in human endothelial and monocyte cells. PLoS One. 2013;8(1):e55203.

[3]. Kreuter MH, et al. Inhibition of intrinsic protein tyrosine kinase activity of EGF-receptor kinase complex from human breast cancer cells by the marine sponge metabolite (+)-aeroplysinin-1. Comp Biochem Physiol B. 1990;97(1):151‐158.

Aeroplysinin 1物理化学性质

[ 密度 ]:
2.01g/cm3

[ 沸点 ]:
479.6ºC at 760 mmHg

[ 分子式 ]:
C₉H₉Br₂NO₃

[ 分子量 ]:
338.98100

[ 闪点 ]:
243.8ºC

[ 精确质量 ]:
336.89500

[ PSA ]:
73.48000

[ LogP ]:
1.53738

[ 蒸汽压 ]:
3.27E-11mmHg at 25°C

[ 折射率 ]:
1.645

[ 储存条件 ]:
-20°C，密闭，干燥

Aeroplysinin 1毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GU4735000

CHEMICAL NAME :: 2,4-Cyclohexadiene-1-acetonitrile, 3,5-dibromo-1,6-dihydroxy-4-methoxy-, (1S-trans)-

CAS REGISTRY NUMBER :: 28656-91-9

LAST UPDATED :: 199204

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C9-H9-Br2-N-O3

MOLECULAR WEIGHT :: 339.01

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 202 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ZNCBDA Zeitschrift fuer Naturforschung, Section C: Biosciences. (Verlag der Zeitschrift fuer Naturforschung, Postfach 2645, D-7400 Tuebingen, Fed. Rep. Ger.) V.29- 1974- Volume(issue)/page/year: 44,680,1989