Bleomycin hydrochloride

产品活性：Bleomycin hydrochloride 是一种 DNA 损伤剂，抑制 DNA 合成。Bleomycin hydrochloride 是一种抗肿瘤抗生素 (antibiotic)。

研究领域：Cell Cycle/DNA Damage | Anti-infection

作用靶点：DNA/RNA Synthesis | Antibiotic

In Vitro: Bleomycin hydrochloride is chosen as the best-studied micronucleus inducers in human lymphocytes with different mechanisms of genotoxicity. The most frequent Bleomycin-induced DNA lesions are single and double strand breaks and single apuinic/apyrimidinic sites. At the same time Bleomycin is true radiomimetic compound, resembling almost completely the genetic effect of ionizing radiation.
The IC₅₀ value of Bleomycin hydrochloride for UT-SCC-19A cell line is 4.0±1.3 nM. UT-SCC-12A and UT-SCC-12B are both more resistant to Bleomycin; IC₅₀ values are 14.2±2.8 nM and 13.0±1.1 nM, respectively.
Bleomycin hydrochloride (50, 100 μM; for 24, 48 h) induce pulmonary fibrosis in RLE-6TN cell (50 μM) and A549 cell (100 μM).

In Vivo: Bleomycin hydrochloride can be used in animal modeling to construct animal models of pulmonary fibrosis. Bleomycin hydrochloride treatment (3.5-4.0 mg/kg; intra-tracheal) on day 0, body weights decreases by day 4 then increases by Day 7 through the end of the study.
Bleomycin hydrochloride (3.5-4.0 mg/kg; intra-tracheal) produces a statistically significant increase in lung hydroxyproline levels, and also increases right caudal lung lobe mass.
Bleomycin hydrochloride (intratracheal instillation; 5.0 mg/kg/day) induces pulmonary fibrosis in eighty 8-week-old male BALB/c mice with weight about 20-30 g. Bleomycin induces the expression levels of α-SMA and collagen I.
Bleomycin hydrochloride (intratracheally; 2.5 mg/kg; 1.25 mg/ml, approximately 50 μl per mouse) induces pulmonary fibrosis in male C57BL/6 mice (8 weeks old, average weight approximately 24.5 g).
Bleomycin sulfate is quickly absorbed following intramuscular, subcutaneous, intraperitoneal, or intrapleural administration and reaches peak plasma concentrations in approximately 60 min. Less than 1% of the drug given intravenously binds to plasma proteins, leading to high bioavailability. Additionally, a mean plasma drug clearance approaching 70 mL/min/m² has been calculated for Bleomycin sulfate. Bleomycin sulfate possesses a high plasma elimination rate and high urinary excretion rate.
Bleomycin sulfate can be used to construct model of pulmonary fibrosis.

Induction of Pulmonary Fibrosis

Background

Bleomycin sulfate can lead to lung patchy parenchymal inflammation, epithelial cell injury with reactive hyperplasia, epithelial-mesenchymal transition, activation and differentiation of fibroblasts to myofibroblasts, and basement membrane and alveolar epithelium injures. The experimental use of Bleomycin sulfate is to induce pulmonary fibrosis animal models.

Specific Mmodeling Methods

Mice: C57BL/6 • 12-week-old
Administration: 3-5 mg/kg • intratracheal administration • sprays on day one

Note

The mice were housed in separate stainless-steel cages (six mice per cage) in a temperature-controlled environment (20-24°C) on 12 h light-dark cycles with unrestricted access to food and water.

Modeling Record

Body quality changes: The appetite activity is reduced, with the fur less shiny, the spirits being lethargic, and the bodyweight decreasing. Showed shortness of breath, coughing, and noisy.
Lung changes: Increased fibrotic consolidations, non-aerated lung area, and high-density lung area. Pulmonary function decreased.
Molecular changes: Increased indicators: TGF-β1, TNF-α, IL-6, and GM-CSF in bronchoalveolar lavage fluid.

Correlated Product(s): Bleomycin hydrochloride (HY-17565A)

Neotuberostemonine (HY-N3196)

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