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Actinonin

抑制氨肽酶的拟肽类抗生素，Actinonin ((-)-Actinonin) 是一种由放线菌产生的天然抗菌剂。Actinonin 抑制氨肽酶 M，氨肽酶 N 和亮氨酸氨肽酶。Actinonin 是一种有效的可逆肽去甲酰基酶 (PDF) 抑制剂，Ki 为 0.28 nM。Actinonin 还抑制 MMP-1，MMP-3，MMP-8，MMP-9 和 hmeprin α 的 Ki 值分别为 300 nM，1,700 nM，190 nM，330 nM 和 20 nM。Actinonin 是一种凋亡诱导剂，具有抗

目录号: PC13003 纯度: ≥98%

CAS No. :13434-13-4

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中文名称

Actinonin

中文别名

放线酰胺素;(-)-放线酰胺素;(±)-6,6-二溴-1,1-二-2-萘酚

英文名称

Actinonin

英文别名

(R)-N4-Hydroxy-N1-((S)-1-((S)-2-(hydroxymethyl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-yl)-2-pentylsuccinamide;(-)-Actinonin;ACTINONIN;Actinonin;Butanediamide,N4-hydroxy-N1-[(1S)-1-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]carbonyl]-2-methyl...;Butanediamide,N4-hydroxy-N1-[(1S)-1-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]carbonyl]-2-methylpropyl]-2-pentyl-,(2R)-;Actinonine;3-[[1-[(2-(Hydroxymethyl)-1-pyrrolidinyl)carbonyl]-2-methylpropyl]carbamoyl]octanohydroxamic acid;octanohydroxamicacid,3-((1-((2-(hydroxymethyl)-1-pyrrolidinyl)carbonyl)-2-met;3-[[1-[[2-(HYDROXYMETHYL)-1-PYRROLIDINYL]CARBONYL]-2-METHYL-PROPYL]CARBAMOYL]OCTANOHYDROXAMIC ACID;N'-Hydroxy-N-[1-[[2-(hydroxymethyl)-1-pyrrolidinyl]carbonyl]-2-methylpropyl]-2-pentylbutanediamide;3-[[1-[[2-(HYDROXYMETHYL)-1-PYRROLIDINYL]-CARBONYL]-2-METHYLPROPYL]-CARBAMOYL]-OCTONOHYDROXAMIC ACID;N4-HYDROXY-N1-[(1S)-1[[(2S)-2-(HYDROXYMETHYL)-1-PYRROLDINYL]CARBONYL]-2-METHYLPROPYL]-2-PENTYL-,(2R)-(9CI);Butanediamide, N4-hydroxy-N1-(1S)-1-(2S)-2-(hydroxymethyl)-1-pyrrolidinylcarbonyl-2-methylpropyl-2-pentyl-, (2R)-;hylpropyl)carbamoyl)-

Cas No.

13434-13-4

分子式

C₁₉H₃₅N₃O₅

分子量

385.50

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a K_i of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with K_i values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.

性状

Solid

IC50 & Target[1][2]

Ki: 0.28 nM (Peptide deformylase (PDF)), 300 nM (MMP-1), 1,700 nM (MMP-3), 190 nM (MMP-8), 330 nM (MMP-9), and 20 nM (hmeprin α)
Apoptosis
Aminopeptidase M, Aminopeptidase N and Leucine aminopeptidase

体外研究(In Vitro)

Actinonin inhibits cell growth in various human tumor cell lines. The IC₅₀ of 4, 6.9, 12.8, 16.6, 27.4, 15.7 and 49.3 μM for Raji cells, MDA-MB-468 cells,PC3 cells, SK-LC-19 cells, Hela cells, HT-1080 cells and AL67 cells, respectively.
HsPDF is a critical target of actinonin and that the inhibition of this protein in the mitochondria leads to cell death in tumor cells. Actinonin treatment of cells led to a tumor-specific mitochondrial membrane depolarization and ATP depletion in a time- and dose-dependent manner.
Actinonin is a potent inhibitor of all three forms (Zn-, Ni-, and Fe-) of peptide deformylases from both S. aureus and E. coli bacteria. Under the assay conditions, the IC₅₀ values for Actinonin are 90, 3, 0.8, and 11 nM for Zn-PDF (E. coli), Ni-PDF (E. coli), Fe-PDF (E. coli), and Ni-PDF (S. aureus), respectively.
Actinonin is active against Gram-positive bacteria, including S. aureus (MIC value of 8-16 μg/mL), Streptococcus pyogenes (MIC value of 8 μg/mL) and Streptococcus epidermidis (MIC value of 2-4 μg/mL). Actinonin is also active against fastidious Gramne-gative bacteria, such as H. influenzae (MIC value of 1-2 μg/mL), Moraxella catarrhalis (MIC value of 0.5 μg/mL), and Neisseria gonorrheae (MIC value of 1-4 μg/mL). Actinonin is very active against the H. influenzae acr (MIC value of 0.13 μg/mL) and E. coli acr (MIC value of 0.25 μg/mL) efflux pump mutants.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Actinonin has been safely administered to mice as an antibiotic at doses up to 400 mg/kg. Actinonin does not appear to have significant toxicity to normal tissues, despite its antitumor activity 体外研究. Remarkably, Actinonin exhibits significant antitumor activity when given i.p. or orally in a CWR22 human prostate tumor xenograft model in nude mice. During treatment, the animals show no signs of toxicity.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

结构分类

Others

来源

actinomycete

参考文献

[1]. Lee MD, et al. Human mitochondrial peptide deformylase, a new anticancer target of actinonin-based antibiotics. J Clin Invest. 2004 Oct;114(8):1107-16. [Information]

[2]. Chen DZ, et al. Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor. Biochemistry. 2000 Feb 15;39(6):1256-62. [Information]

[3]. Wahl, R.C., et al. Hydroxamate inhibitors of human gelatinase B (92 kDa). Bioorganic & Medicinal Chemistry Letters 5(4), 349-352 (1995).

[4]. Duke SO, et al. Modes of action of microbially-produced phytotoxins. Toxins (Basel). 2011 Aug;3(8):1038-64. [Information]

[5]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (129.70 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5940 mL	12.9702 mL	25.9403 mL
5 mM	0.5188 mL	2.5940 mL	5.1881 mL
10 mM	0.2594 mL	1.2970 mL	2.5940 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (12.97 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (12.97 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 5 mg/mL (12.97 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (12.97 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (12.97 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (12.97 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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