Seselin

Seselin is an anticancer, antinociceptive, anti-inflammatory and antifungal agent. Seselin is orally active[1][2][3].

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Fungal

Research Areas >> Inflammation/Immunology

Seselin 对 P-388 和 HT-29 细胞有毒性，ED50 分别为 8.66 和 9.94 μg/mL [1]。 Seselin (5-20 μM; 0.5-24 h) 抑制 LPS 和 IFN-γ 刺激的巨噬细胞的细胞因子输出[3]。 Seselin (5-20 μM; 12 h) 抑制 BMDMs 中促炎巨噬细胞标志物 (iNOS、phagocytosis、CD11c) 的表达[3]。 Seselin (5-20 μM; 0.5-6 h) 阻断 STAT1 信号通路[3]。 RT-PCR[3] Cell Line: Bone marrow-derived macrophages (BMDMs) Concentration: 5, 10 and 20 μM Incubation Time: 6 h Result: Reduced the mRNA for cytokines (IL-1β, IL-6, Tnf-α and IL-23) and chemokines (Ccl3, Ccl7, Cxcl9 and Cxcl11) concentration-dependently in BMDMs. Western Blot Analysis[3] Cell Line: BMDMs Concentration: 5, 10 and 20 μM Incubation Time: 0.5, 1.5, 3 and 6 h Result: Suppressed expression of p-STAT1 and p-p65 both concentration and time dependently.

Seselin (0.5-40.5 mg/kg; s.c.; once) 在小鼠中显示外周抗炎和抗伤感受活性[2]。 Seselin (3-30 mg/kg; i.g.; once) 改善小鼠盲肠结扎和穿刺引起的脓毒症[3]。 Animal Model: Male Swiss mice[2] Dosage: 0.5, 4.5 or 40.5 mg/kg Administration: Subcutaneous injection; once Result: Inhibited the writhing response induced by acetic acid in a significant and dose-dependent manner, by 19.5%, 26.2% and 41.4% at dose of 0.5, 4.5 or 40.5 mg/kg, respectively. Elicited a significant inhibition of formalin response during the second phase (inflammatory), by 90.3%, 97.8% and 95.3%, respectively. Animal Model: C57BL/6 mice, caecal ligation and puncture (CLP) induced sepsis model[3] Dosage: 3, 10 and 30 mg/kg Administration: Intragastric administration, once Result: Ameliorated lung injury and decreased JAK2 phosphorylation level in lung tissue during sepsis. Reduced the immune cell counts in BALF induced by CLP.

[1]. Chou HC, et al. Cytotoxic and anti-platelet aggregation constituents from the root wood of Melicope semecarpifolia. Planta Med. 2005 Nov;71(11):1078-81.  

[2]. Lima V, et al. Antinociceptive activity of the pyranocoumarin seselin in mice. Fitoterapia. 2006 Dec;77(7-8):574-8.Lima V, et al. Antinociceptive activity of the pyranocoumarin seselin in mice. Fitoterapia. 2006 Dec;77(7-8):574-8.Lima V, et al. Antinociceptive activity of the pyranocoumarin seselin in mice. Fitoterapia. 2006 Dec;77(7-8):574-8.  

[3]. Feng L, et al. Seselin ameliorates inflammation via targeting Jak2 to suppress the proinflammatory phenotype of macrophages. Br J Pharmacol. 2019 Jan;176(2):317-333.