Atraric acid (Methyl atrarate) 是一种特异的雄激素受体 (androgen receptor) 拮抗剂，具有抗炎和抗癌作用。Atraric acid 抑制 LNCaP 和 C4-2 细胞中内源性前列腺特异性抗原基因的表达。Atraric acid 还能抑制NO和细胞因子的合成，抑制MAPK-NFκB信号通路。Atraric acid 可用于前列腺疾病和炎症性疾病的研究。
| 生物活性 | Atraric acid (Methyl atrarate) is a specificandrogen receptor(AR)antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis ofNOand cytokine, and suppress theMAPK-NFκBsignaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases[1][2]. |
| IC50& Target | Androgen receptor, NO synthesis, MAPK-NFκB pathway[1][2] |
体外研究
(In Vitro) | Atraric acid (10 μM; CV1 cells) represses the transactivation function mediated by Dihydrotestosterone-induced human AR[1].
Atraric acid (10 μM; PCa cells) inhibits the expression of the PSA gene in both androgen-dependent and androgen-independent PCa cells[1].
Atraric acid (1-300 μM; 24 h) dose-dependently inhibits pro-inflammatory cytokine, nitric oxide, prostaglandin E2 in LPS-stimulated RAW264.7 cells, but does not influence the cell viability[2].
Atraric acid (100 and 300 μM; 18 h or 4 h) downregulates the expression of phosphorylated IκB, extracellular signal-regulated kinases (ERK) and nuclear factor kappa B (NFκB) signaling pathway to exhibit anti-inflammatory effects in LPS-stimulated RAW264.7 cells[2].
Cell Viability Assay[2] | Cell Line: | RAW264.7 cells | | Concentration: | 1-300 μM | | Incubation Time: | 24 h | | Result: | Did not influence the cell viability. |
Western Blot Analysis[2] | Cell Line: | RAW264.7 cells | | Concentration: | 100 and 300 μM | | Incubation Time: | 18 h or 4 h | | Result: | Inhibited LPS-Induced expression of iNOS and COX-2 in a dose-dependent manner.
Suppressed LPS-stimulated phosphorylation of the Nfκb signaling pathway. |
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体内研究
(In Vivo) | Atraric acid (10, 30 mg/kg; i.p.; single dosage) inhibits the production of pro-inflammatory cytokines and reduces pathological damages in LPS-induced endotoxin shock mice[2].
| Animal Model: | Female BALB/c mice (7 weeks old, 17-20 g; LPS-induced endotoxin shock)[2] | | Dosage: | 10, 30 mg/kg | | Administration: | i.p.; single dosage | | Result: | Inhibited the production of pro-inflammatory cytokines.
Reduced pathological damages such as vasodilation and bleeding. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
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