Epimedokoreanin B

Names

[ Name ]:
Epimedokoreanin B

[Synonym ]:
2-(3,4-Dihydroxy-5-((E)-3-methyl-but-2-enyl)-phenyl)-5,7-dihydroxy-8-(3-methyl-but-2-enyl)-1-benzopyran-4-one
2-[3,4-Dihydroxy-5-(3-methyl-2-buten-1-yl)phenyl]-5,7-dihydroxy-8-(3-methyl-2-buten-1-yl)-4H-chromen-4-one
2-[3,4-Dihydroxy-5-((E)-3-methyl-but-2-enyl)-phenyl]-5,7-dihydroxy-8-(3-methyl-but-2-enyl)-1-benzopyran-4-one
4H-1-Benzopyran-4-one, 2-[3,4-dihydroxy-5-(3-methyl-2-buten-1-yl)phenyl]-5,7-dihydroxy-8-(3-methyl-2-buten-1-yl)-

Biological Activity

[Description]:

Epimedokoreanin B is a natural flavonoid with anticancer, anti-inflammatory and antibacterial effects. Epimedokoreanin B inhibits the growth of lung cancer cells through endoplasmic reticulum stress-mediated Apoptosis accompanied by autophagosome accumulation. Epimedokoreanin B is an anti-periodontitis agent that inhibits gingipains and Porphyromonas gingivalis growth and biofilm formation[1][2][3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Infection

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Epimedokoreanin B (compound6; 3.13-25 μM; 48 hours) 对肺癌细胞 A549、Calu1 和 H1299 的增殖显示出显着的抑制作用。Epimedokoreanin B 对人支气管上皮细胞 BEAS-2B 无毒性[1]。 Epimedokoreanin B 处理抑制 A549 和 NCI-H292 细胞中伴随细胞质空泡形成的细胞增殖和迁移。Epimedokoreanin B 处理的细胞中观察到自噬体聚集并伴有自噬通量阻断，这与内质网应激的发生相符[2]。 Epimedokoreanin B（5 μM；24 小时）抑制 CD163 表达和 IL-10 的产生，这是已知的 M2 标记，表明 Epimedokoreanin B 抑制人单核细胞衍生巨噬细胞 (HMDM) 中的 M2 极化。Epimedokoreanin B 抑制 HMDMs 中的 STAT3 激活[4]。 Cell Cytotoxicity Assay[1] Cell Line: A549, Calu1 and H1299 cells Concentration: 3.13 μM, 6.25 μM, 12.5 μM and 25.0 μM Incubation Time: 48 hours Result: Showed significate inhibitory effect on proliferation against lung cancer cell A549, Calu1 and H1299. Western Blot Analysis[4] Cell Line: Human monocyte-derived macrophages (HMDMs) Concentration: 5 μM Incubation Time: 24 hours Result: Significantly suppressed IL-10-induced JAK1/STAT3 activation.and H1299.

[In Vivo]

Epimedokoreanin B（20 mg/kg；口服；每周三次；持续 17 天）抑制 LM8 荷瘤鼠模型中的肿瘤生长[4]。 Animal Model: Female C3H mice (8-10 weeks old) injected with LM8 cells[4] Dosage: 20 mg/kg Administration: Oral administration; thrice a week; for 17 days Result: Inhibited tumor growth.

[References]

[1]. Huaran Zhang, et al. Flavonoids from the leaves of Epimedium Koreanum Nakai and their potential cytotoxic activities. Nat Prod Res. 2020 May;34(9):1256-1263.

[2]. Hao Zheng, et al. Epimedokoreanin B inhibits the growth of lung cancer cells through endoplasmic reticulum stress-mediated paraptosis accompanied by autophagosome accumulation. Chem Biol Interact. 2022 Oct 1;366:110125.

[3]. T Kariu, et al. Inhibition of gingipains and Porphyromonas gingivalis growth and biofilm formation by prenyl flavonoids. J Periodontal Res. 2017 Feb;52(1):89-96.

[4]. Cheng Pan , et al. Flavonoid Compounds Contained in Epimedii Herba Inhibit Tumor Progression by Suppressing STAT3 Activation in the Tumor Microenvironment. Front Pharmacol. 2020 Mar 18;11:262.