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博来霉素

具有抗肿瘤特性的抗生素

产品号 #(选择产品)

产品号 #100-0550_C

具有抗肿瘤特性的抗生素

总览

博莱霉素是一种从细菌中分离出来的糖肽类抗生素链霉菌属verticillus它能导致DNA链断裂,并对鳞状细胞癌和恶性淋巴瘤具有抗肿瘤作用(Galm et al.)。博莱霉素会导致肺损伤,引发急性炎症反应和肺纤维化(Kulkarni et al.)。本品是博来霉素A2和博来霉素B2的混合物,以硫酸盐形式供应。

别名
布洛芬;硫酸博来霉素(盐)
 
细胞类型
癌细胞及细胞系
 
研究领域
癌症,疾病建模
 
CAS 编号
9041-93-4 (for A2),9060-10-0 (for B2)
 
化学式
C55H84N17O21S3 • XHSO4 (for A2),C55H84N20O21S2 (for B2)
 
分子量
1415.6 克/摩尔(用于 A2),1425.5 克/摩尔(用于 B2)
 
纯度
≥ 95%(A2和B2混合物)
 

产品说明书及文档

请在《产品说明书》中查找相关支持信息和使用说明,或浏览下方更多实验方案。

Document Type
Product Name
Catalog #
Lot #
Language
Catalog #
100-0550
Lot #
All
Language
English
Document Type
Safety Data Sheet
Catalog #
100-0550
Lot #
All
Language
English

相关材料与文献

技术资料 (3)

文献 (3)

The triterpenoid CDDO-Me inhibits bleomycin-induced lung inflammation and fibrosis. A. A. Kulkarni et al. PloS one 2013

Abstract

Pulmonary Fibrosis (PF) is a devastating progressive disease in which normal lung structure and function is compromised by scarring. Lung fibrosis can be caused by thoracic radiation, injury from chemotherapy and systemic diseases such as rheumatoid arthritis that involve inflammatory responses. CDDO-Me (Methyl 2-cyano-3,12-dioxooleana-1,9(11)dien-28-oate, Bardoxolone methyl) is a novel triterpenoid with anti-fibrotic and anti-inflammatory properties as shown by our in vitro studies. Based on this evidence, we hypothesized that CDDO-Me would reduce lung inflammation, fibrosis and lung function impairment in a bleomycin model of lung injury and fibrosis. To test this hypothesis, mice received bleomycin via oropharyngeal aspiration (OA) on day zero and CDDO-Me during the inflammatory phase from days -1 to 9 every other day. Bronchoalveolar lavage fluid (BALF) and lung tissue were harvested on day 7 to evaluate inflammation, while fibrosis and lung function were evaluated on day 21. On day 7, CDDO-Me reduced total BALF protein by 50{\%}, alveolar macrophage infiltration by 40{\%}, neutrophil infiltration by 90{\%} (p≤0.01), inhibited production of the inflammatory cytokines KC and IL-6 by over 90{\%} (p≤0.001), and excess production of the pro-fibrotic cytokine TGF$\beta$ by 50{\%}. CDDO-Me also inhibited $\alpha$-smooth muscle actin and fibronectin mRNA by 50{\%} (p≤0.05). On day 21, CDDO-Me treatment reduced histological fibrosis, collagen deposition and $\alpha$SMA production. Lung function was significantly improved at day 21 by treatment with CDDO-Me, as demonstrated by respiratory rate and dynamic compliance. These new findings reveal that CDDO-Me exhibits potent anti-fibrotic and anti-inflammatory properties in vivo. CDDO-Me is a potential new class of drugs to arrest inflammation and ameliorate fibrosis in patients who are predisposed to lung injury and fibrosis incited by cancer treatments (e.g. chemotherapy and radiation) and by systemic autoimmune diseases.
Antitumor antibiotics: bleomycin, enediynes, and mitomycin. U. Galm et al. Chemical reviews 2005 feb
Bleomycin: new perspectives on the mechanism of action. S. M. Hecht Journal of natural products 2000 jan

Abstract

The bleomycin group antitumor antibiotics have long been of interest as a consequence of their efficacy in the treatment of certain tumors, not to mention their unique structures and properties in mediating dioxygen activation and sequence selective degradation of DNA. At a chemical level, the structure originally assigned to bleomycin was subsequently reassigned and the new structure has been confirmed by total synthesis. Through the elaboration of structurally modified bleomycin congeners and fragments, synthetic efforts have also facilitated an understanding of the contribution of individual structural domains in bleomycin to sequence selective DNA binding and cleavage, and have also provided insights into the nature of the chemical processes by which DNA degradation takes place. Within the last several years, it has also become apparent that bleomycin can mediate the oxidative degradation of all major classes of cellular RNAs; it seems entirely plausible that RNA may also represent an important locus of action for this class of antitumor agent. In parallel with ongoing synthetic and mechanistic efforts using classical methods, the study of bleomycins attached to solid supports has been shown to provide important mechanistic insights, and the actual elaboration of modified bleomycins by solid phase synthesis constitutes a logical extension of such efforts.

更多信息

更多信息
Molecular Weight 1415.6 g/mol (for A2), 1425.5 g/mol (for B2)
Alternative Names Blenoxane; Bleomycin sulfate (salt)
Cas Number 9041-93-4 (for A2), 9060-10-0 (for B2)
Chemical Formula C55H84N17O21S3 • XHSO4 (for A2), C55H84N20O21S2 (for B2)
纯度 ≥ 95% (mixture of A2 and B2)
质量保证:

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