Vitamin K1 (Phylloquinone)

Vitamin K1 (Phylloquinone) is a fat-soluble, plant-derived natural vitamin. Vitamin K1 serves as an essential cofactor for γ-glutamyl carboxylase (GGCX) to promote the γ-carboxylation of coagulation factors II, VII, IX, and X, enabling them to bind calcium ions and exert normal coagulation function. Vitamin K1 reduces oxidative stress and cellular damage by inhibiting 12-lipoxygenase (12-LOX) activation. Vitamin K1 can be used in research related to bleeding disorders, cancer, and other diseases^[1-4].

In vitro, Vitamin K1 (6–24μM) was used to treat PLC/PRF/5, HLF, and Hep3B human hepatocellular carcinoma cells for 72 hours. Vitamin K1 significantly inhibited cell migration while causing a reduction in polymerized F-actin and its perinuclear redistribution^[5]. Vitamin K1 (10–200μM) was used to treat Caco-2, HT-29, and SW480 human colon cancer cell lines for 24–72 hours. Vitamin K1 significantly inhibited cell proliferation, induced apoptosis, and concurrently reduced polyamine biosynthesis^[6].

In vivo, Vitamin K1 (1–3mg/kg) was administered by gavage once daily for one week as pretreatment, followed by an intraperitoneal injection of acetaminophen (APAP; 200mg/kg) on the final day in Albino mice. Vitamin K1 dose-dependently attenuated APAP-induced liver injury^[7]. Vitamin K1 (1mg/kg; single dose) was administered by gavage to C57BL/6 mice that received an intraperitoneal injection of LPS (15mg/kg). Vitamin K1 ameliorated LPS-triggered skeletal muscle injury^[8].

References:
[1] Halder M, Petsophonsakul P, Akbulut AC, et al. Vitamin K: Double Bonds beyond Coagulation Insights into Differences between Vitamin K1 and K2 in Health and Disease. Int J Mol Sci. 2019 Feb 19;20(4):896.
[3] Basset GJ, Latimer S, Fatihi A, et al. Phylloquinone (Vitamin K1): Occurrence, Biosynthesis and Functions. Mini Rev Med Chem. 2017;17(12):1028-1038.
[4] Britt RB, Brown JN. Characterizing the Severe Reactions of Parenteral Vitamin K1. Clin Appl Thromb Hemost. 2018 Jan;24(1):5-12.
[5] D'Alessandro R, Refolo MG, Lippolis C, et al. Strong enhancement by IGF1-R antagonists of hepatocellular carcinoma cell migration inhibition by Sorafenib and/or vitamin K1. Cell Oncol (Dordr). 2018 Jun;41(3):283-296.
[6] Orlando A, Linsalata M, Tutino V, et al. Vitamin K1 exerts antiproliferative effects and induces apoptosis in three differently graded human colon cancer cell lines. Biomed Res Int. 2015;2015:296721.
[7] Abass SA, Mohamed AA, El-Slam AHA, et al. Vitamin K1 attenuates acetaminophen-induced ferroptotic hepatic damage in mice via targeting keap1/Nrf2/HO-1 pathway. Naunyn Schmiedebergs Arch Pharmacol. 2026 Feb;399(3):3699-3713.
[8] Xiao Y, Feng J, Jia J, et al. Vitamin K1 ameliorates lipopolysaccharide-triggered skeletal muscle damage revealed by faecal bacteria transplantation. J Cachexia Sarcopenia Muscle. 2024 Feb;15(1):81-97.

Vitamin K1 (Phylloquinone) 是一种脂溶性的、来源于植物的天然维生素。Vitamin K1可作为γ-谷氨酰羧化酶(GGCX)的必需辅因子来促进凝血因子II、VII、IX、X的γ-羧基化，使其能够结合钙离子并发挥正常的凝血功能。Vitamin K1通过抑制12-脂氧合酶（12-LOX）激活以减少氧化应激和细胞损伤。Vitamin K1可用于出血性疾病、癌症等疾病的相关研究^[1-4]。

在体外，Vitamin K1（6–24μM）处理PLC/PRF/5、HLF和Hep3B人肝细胞癌细胞72小时。Vitamin K1显著抑制细胞迁移，同时引起聚合F-actin减少和核周重新分布^[5]。Vitamin K1（10–200μM）处理Caco-2、HT-29和SW480人结肠癌细胞系24–72小时。Vitamin K1显著抑制细胞增殖，诱导细胞凋亡，同时降低多胺生物合成^[6]。

在体内，Vitamin K1（1–3mg/kg）每天一次灌胃预处理一周，随后在最后一天腹腔注射Acetaminophen（200mg/kg）处理Albino小鼠。Vitamin K1剂量依赖性地减轻了APAP诱导的肝损伤^[7]。Vitamin K1（1mg/kg/kg；单次）灌胃于腹腔注射LPS（15mg/kg）的C57BL/6小鼠。Vitamin K1改善了LPS触发的骨骼肌损伤^[8]。