Thymoquinone is an orally active natural product isolated from Nigella glandulifera. Thymoquinone downregulates the VEGFR2-PI3K-Akt pathway, inhibits the expression of NF-κB and MMP-9, downregulates TWIST1 expression, and activates the Nrf2 pathway to exert various biological activities. Thymoquinone can be used in research related to Alzheimer's disease, cancer, cardiovascular diseases, infectious diseases, and inflammation[1-4].
In vitro, Thymoquinone (25–100μM) was used to treat the human breast cancer cell line MCF-7 for 12–72 hours. Thymoquinone significantly inhibited cell proliferation, induced apoptosis, and caused S-phase and G2-phase cell cycle arrest[5]. Thymoquinone (20μM) was used to treat the colorectal cancer cell lines RKO and SW1116 for 24 hours. In RKO cells, Thymoquinone significantly induced DNA fragmentation, caspase activation, and upregulation of pro-apoptotic genes. In SW1116 cells, Thymoquinone significantly inhibited caspase activity and induced caspase-independent necrotic cell death[6].
In vivo, Thymoquinone (100mg/kg/day) was administered by gavage to LDL-R-/- mice for 8 weeks. Thymoquinone significantly alleviated hyperlipidemia-induced liver injury[7]. Thymoquinone (20mg/kg and 40mg/kg; three times per week) was administered via intraperitoneal injection to C57BL/6J mice for one month. Thymoquinone (40mg/kg) significantly improved age-related hearing loss[8].
References:
[1] Zeinvand-Lorestani H, Nili-Ahmadabadi A, Balak F, et al. Protective role of thymoquinone against paraquat-induced hepatotoxicity in mice. Pestic Biochem Physiol. 2018 Jun;148:16-21.
[2] Nagi MN, Mansour MA. Protective effect of thymoquinone against doxorubicin-induced cardiotoxicity in rats: a possible mechanism of protection. Pharmacol Res. 2000 Mar;41(3):283-9.
[3] Elibol B, Beker M, Terzioglu-Usak S, et al. Thymoquinone administration ameliorates Alzheimer's disease-like phenotype by promoting cell survival in the hippocampus of amyloid beta1-42 infused rat model. Phytomedicine. 2020 Dec;79:153324.
[4] Su X, Ren Y, Yu N, et al. Thymoquinone inhibits inflammation, neoangiogenesis and vascular remodeling in asthma mice. Int Immunopharmacol. 2016 Sep;38:70-80.
[5] Motaghed M, Al-Hassan FM, Hamid SS. Cellular responses with thymoquinone treatment in human breast cancer cell line MCF-7. Pharmacognosy Res. 2013 Jul;5(3):200-6.
[6] Kurowska N, Książek M, Borkowska P, et al. Cell Line-Dependent Cell Death Pathways Induced by Thymoquinone in Colorectal Cancer Cells. Molecules. 2026 Feb 2;31(3):512.
[7] Wang F, Yao W, Yu D, et al. Protective role of thymoquinone in hyperlipidemia-induced liver injury in LDL-R-/-mice. BMC Gastroenterol. 2023 Aug 11;23(1):276.
[8] Salam SA, Mostafa F, Alnamshan MM, et al. Thymoquinone ameliorates age-related hearing loss in C57BL/6J mice by modulating Sirt1 activity and Bak1 expression. Biomed Pharmacother. 2021 Nov;143:112149.
Thymoquinone是一种从黑种草籽中分离得到的口服活性天然产物。Thymoquinone可下调VEGFR2-PI3K-Akt通路、抑制NF-κB和MMP-9的表达、下调TWIST1表达并激活Nrf2通路以发挥多种生物活性。Thymoquinone可用于阿尔茨海默病、癌症、心血管疾病、感染病和炎症等方面的相关研究[1-4]。
在体外，Thymoquinone（25–100μM）处理人类乳腺癌细胞系MCF-7 12–72小时。Thymoquinone显著抑制细胞增殖，诱导细胞凋亡，并导致S期和G2期细胞周期阻滞[5]。Thymoquinone（20μM）处理结直肠癌细胞系RKO和SW1116，24小时。在RKO细胞中，Thymoquinone显著诱导DNA片段化、caspase激活和促凋亡基因上调。在SW1116细胞中，Thymoquinone显著抑制caspase活性并诱导caspase非依赖性坏死性细胞死亡[6]。
在体内，Thymoquinone（100mg/kg/day）通过灌胃给药，用于处理LDL-R-/-小鼠，持续8周。Thymoquinone显著减轻了高血脂引起的肝损伤[7]。Thymoquinone（20mg/kg和40mg/kg；每周三次）腹腔注射C57BL/6J小鼠，持续一个月。Thymoquinone（40mg/kg）显著改善了年龄相关性听力损失[8]。