Dianemycin
(Synonyms: Nanchangmycin free acid) 目录号 : GC35857Dianemycin (Nanchangmycin free acid) 由 Streptomyces nanchangensis NS3226 产生的,抑制革兰氏阳性菌。Dianemycin 也是一种抗 Zika 病毒的广谱抗病毒药物。
Cas No.:35865-33-9
Sample solution is provided at 25 µL, 10mM.
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Dianemycin (Nanchangmycin free acid), produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria[1]. Dianemycin is a broad spectrum antiviral active against Zika virus[2]. Bacteria[1] Zika virus[2]
Dianemycin (Nanchangmycin) can be used as a growth promotant in poultry and to cure coccidiosis in chickens. Dianemycin is active against drug resistant strains of malaria[1]. Dianemycin (Nanchangmycin) as a potent inhibitor of Zika virus (ZIKV) entry across all cell types tested including physiologically relevant primary cells. Dianemycin potently reduces infection of all three strains of ZIKV across all three cell types. The IC50s for infection are between 0.1 and 0.4 μM while Dianemycin has low toxicity in these ranges. In addition, DENV is inhibited by Dianemycin across cell types[2].
[1]. Liu T, et al. Mechanism of thioesterase-catalyzed chain release in the biosynthesis of the polyether antibiotic Nanchangmycin. Chem Biol. 2008 May;15(5):449-58. [2]. Rausch K, et al. Screening Bioactives Reveals Nanchangmycin as a Broad Spectrum Antiviral Active against Zika Virus. Cell Rep. 2017 Jan 17;18(3):804-815.
Cas No. | 35865-33-9 | SDF | |
别名 | Nanchangmycin free acid | ||
Canonical SMILES | C[C@H]1[C@@]2(O[C@]([C@@]3([H])O[C@](O)([C@H](C)C[C@@H]3C)CO)([H])C[C@@H]2C)O[C@]([C@]4(O[C@]5(O[C@]([C@H](C)[C@@H](O)C5)([H])[C@@H](C)/C=C(C)/C([C@H](C)C[C@H](C)C(O)=O)=O)CC4)C)([H])C[C@@H]1O[C@@]6([H])O[C@@H]([C@@H](OC)CC6)C | ||
分子式 | C47H78O14 | 分子量 | 867.11 |
溶解度 | DMSO: 155 mg/mL (178.75 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.1533 mL | 5.7663 mL | 11.5326 mL |
5 mM | 0.2307 mL | 1.1533 mL | 2.3065 mL |
10 mM | 0.1153 mL | 0.5766 mL | 1.1533 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Topical anti-inflammatory activity of Dianemycin isolated fromStreptomyces sp. MT 2705-4
Arch Pharm Res 1997 Aug;20(4):372-4.PMID:18975182DOI:10.1007/BF02976203.
In order to develop new anti-inflammatory agents having different action mechanisms compared with nonsteroidal and steroidal anti-inflammatory drugs, the culture broths of various actinomycetes isolated from soil were screened using anin vivo mouse ear edma assay and one strain (Streptomyces sp. MT 2705-4: KCTC 8651P) was selected. Activity-guided purification led to the isolation of a polyether compound, Dianemycin. Topically, Dianemycin showed a potent anti-inflammatory activity in mouse ear edema induced by croton-oil or arachidonic acid. ED(50) value of Dianemycin was found to be 0.8 mg/ear compared to 0.4 mg/ear of prednisolone in croton-oil ear edema. However, Dianemycin did not show the inhibitory activity in UV-erythema and delayed hypersensitivity reaction. These results indicate that Dianemycin is a potential topical anti-inflammatory agent.
Studies on the ionophorous antibiotics. XXV. The assignments of the 13C-NMR spectra of Dianemycin and lenoremycin
J Antibiot (Tokyo) 1980 Feb;33(2):144-56.PMID:7380725DOI:10.7164/antibiotics.33.144.
All the resonances observed in the 13C-NMR spectra of polyether antibiotics, Dianemycin and lenoremycin (Ro 21-6150) have been assigned by the aid of selective proton decoupling experiments, T1 value measurements and biosynthetic methods as well as comparison to model compounds such as monensin, nigericin, etheromycin and carriomycin.
CP-60,993, a new dianemycin-like ionophore produced by Streptomyces hygroscopicus ATCC 39305: fermentation, isolation and characterization
J Ind Microbiol 1990 Aug;5(6):365-74.PMID:1366760DOI:10.1007/BF01578095.
CP-60,993, 19-epi-dianemycin, is a novel polycyclic ether antibiotic produced by Streptomyces hygroscopicus ATCC 39305. Fermentation recovery, purification and crystallization were achieved using standard procedures. CP-60,993 was characterized as a monocarboxylic acid. Elemental analysis suggested a molecular formula of C47H78O14 for the free acid and C47H77O14 Na for the sodium salt. Crystalline from CP-60,993 sodium salt shows the following properties: m.p. 193-205 degrees C, E1%(1 cm) = 157 at 232 nm, [alpha]25 degrees C(D) + 11.0 (c 1, methanol). The structure, determined by MS, PMR and CMR, differs from Dianemycin only in the stereochemistry at position 19. This was confirmed by X-ray crystallography carried out on the rubidium salt of CP-60,993. It exhibited activity in vitro against Gram-positive and anaerobic bacteria, efficacy against Eimeria coccidia in vivo in poultry, and stimulation in vitro of rumen propionic acid production.
Antibiotic A-130, isolation and characterization
J Antibiot (Tokyo) 1975 Dec;28(12):931-4.PMID:1206005DOI:10.7164/antibiotics.28.931.
An antibiotic, A-130, was isolated from a strain identified as Streptomyces hygroscopicus, strain A-130. The antibiotic belongs to the nigericin group and like Dianemycin, has an alpha, beta-unsaturated ketone chromophore in its molecule. A-130 is active against gram-positive organisms.
Studies on the ionophorous antibiotics. XXIV. Leuseramycin, a new polyether antibiotic produced by Streptomyces hygroscopicus
J Antibiot (Tokyo) 1980 Feb;33(2):137-43.PMID:7380724DOI:10.7164/antibiotics.33.137.
A new antibiotic leuseramycin has been isolated from the cultured mycelium of the strain of Streptomyces hygroscopicus TM-531. Physicochemical data, in particular those of 1H- and 13C-NMR spectra, revealed that leuseramycin is closely related to Dianemycin in its structure, the former having a methyl group in place of the hydroxymethyl group at C-30. It is active against Gram-positive bacteria, some phytopathogenic fungi and some protozoa.