Cepharanthine千金藤碱,481-49-2

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Cepharanthine

CAS No. : 481-49-2

MCE 国际站：Cepharanthine

产品活性：Cepharanthine 是一种可以从植物 Stephania cephalantha  Hayata中分离出来的天然产物。Cepharanthine 具有抗SARS-CoV-2 的活性。Cepharanthine 对病毒增殖有良好的抑制作用 (半数最大 (50%) 抑制浓度 (IC₅₀) 和 90% 抑制浓度 (IC₉₀) 值为 1.90 和 4.46 µM。Cepharanthine 还能有效逆转 K562 细胞中 P-gp 介导的多重耐药性，并增强异种移植小鼠模型中抗癌药物的敏感性。Cepharanthine 对人肝细胞色素 P450 酶 CYP3A4，CYP2E1 和 CYP2C9具有抑制作用。Cepharanthine 具有抗肿瘤、抗炎和镇痛效果。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：SARS-CoV  |  Cytochrome P450  |  Apoptosis  |  Parasite

In Vitro: Cepharanthine (CEP) (2 μM, 48 h) inhibits cell viability and colony formation and induces apoptosis via the mitochondrial pathway in human TNBC cells.
Cepharanthine (2 μM, 48 h) Combinates with Epirubicin (HY-13624) impairs mitochondrial function and causes mitochondrial fission and apoptosis in MDA-MB-231 cells.
Cepharanthine (5 μM, 24 h) potently enhances the sensitivity of anticancer agents Doxorubicin (HY-15142A) and Vincristine (HY-N0488) and enhanced apoptosis induced by anticancer agents in K562 cells.
Cepharanthine (10-50 μM, 0.5-1 h) changes the distribution of Doxorubicin (HY-15142A) from cytoplasmic vesicles to nucleoplasm in K562 cells by inhibiting the acidification of cytoplasmic organellesin.
Cepharanthine (0-50 μM, 30 min) shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4,CYP2E1 and CYP2C9in vitro.
Cepharanthine(0-4 μM, 48 hours) blocks P. falciparum development in ring stage with IC₅₀s of 3.059, 0.927, 2.276, and 1.803 μM for FCM29, W2, 3D7 and K1, respectively.

In Vivo: Cepharanthine (12 mg/kg, i.p., once daily for 36 days) enhances the therapeutic efficacy of Epirubicin (HY-13624) in MDA-MB-231 cell xenografts.
Cepharanthine (10 mg/kg, i.p., single dose) prevents LPS-induced pulmonary vascular injury in rats by inhibiting leukocyte activation.
Cepharanthine (CE)(10 mg/kg, i.p., single dose) exerts anti-inflammatory effects via NF-kB inhibition in a LPS-induced rat model of systemic inflammation.
Cepharanthine (20-180 mg/kg, i.p.) results in a dose-dependent antinociceptive effect with an ED₅₀ value of 24.5 mg/kg in mice pain models.

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