β-Sitosterol is a natural sterol derived from plants that has a variety of biological activities such as inhibiting cancer development[1]. β-Sitosterol is also commonly used to study its effects on cardiovascular health[2]. β-Sitosterol is commonly used to study its effects on cardiovascular health. β-Sitosterol can help lower blood cholesterol levels by modulating cholesterol metabolism, thereby playing a positive role in the prevention of cardiovascular diseases[3]. β-Sitosterol also has anti-inflammatory activity, allowingβ-Sitosterol to participate in the body's inflammatory regulation process and help alleviate some inflammation-related symptoms[4].
In vitro, treatment of human ovarian cancer cell lines ES2 and OV90 with β-Sitosterol (10, 25, 50µg/mL) for 48 hours induces apoptosis, inhibits cell proliferation, reduces mitochondrial membrane potential, increases reactive oxygen species (ROS) and calcium influx, alters intracellular signaling pathways, inhibits cell aggregation, growth, and migration. When used in combination with standard anticancer drugs such as cisplatin (20μM) or paclitaxel (20μM), β-Sitosterol demonstrates synergistic anticancer effects[5]. Treatment of human hepatocellular carcinoma cell lines Huh-7 and HCCLM3 with β-Sitosterol (5, 10, 20µg/mL) for 24–72 hours significantly inhibits cell proliferation, migration, and invasion, induces apoptosis, inhibits epithelial-mesenchymal transition (EMT), and reduces GSK3B expression. Additionally, when used in combination with the GSK3B inhibitor (CHIR-98014; 50nM), β-Sitosterol further enhances the inhibitory effects on hepatocellular carcinoma cell proliferation and invasion[6].
In vivo, oral administration of β-Sitosterol (200mg/kg) once daily, in combination with intraperitoneal injection of dexamethasone (20mg/kg) once daily, was used to treat 6-week-old C57BL/6 mice for 3 weeks. β-Sitosterol significantly alleviated dexamethasone-induced muscle atrophy in mice, through the regulation of FoxO1-dependent signaling pathways[7]. Intraperitoneal injection of β-Sitosterol (100mg/kg) in C57BL/6J mice significantly reduced anxiety-like behaviors. β-Sitosterol demonstrated synergistic anxiolytic effects when used in combination with fluoxetine (5mg/kg; i.p.)[8].
References:
[1] Arivarasu L. In-Vitro Antioxidant Potential of Beta-Sitosterol: A Preface. Cureus. 2023 Sep 20;15(9):e45617.
[2] Bao X, Zhang Y, Zhang H, et al. Molecular Mechanism of β-Sitosterol and its Derivatives in Tumor Progression. Front Oncol. 2022 Jun 8;12:926975.
[3] Babu S, Jayaraman S. An update on β-sitosterol: A potential herbal nutraceutical for diabetic management. Biomed Pharmacother. 2020 Nov;131:110702.
[4] Rossi A, Bragonzi A, Medede M, et al. β-sitosterol ameliorates inflammation and Pseudomonas aeruginosa lung infection in a mouse model. J Cyst Fibros. 2023 Jan;22(1):156-160.
[5] Bae H, Park S, Ham J, et al. ER-Mitochondria Calcium Flux by β-Sitosterol Promotes Cell Death in Ovarian Cancer. Antioxidants (Basel). 2021 Oct 8;10(10):1583.
[6] Wang R, Tang D, Ou L, et al. β-Sitosterol alleviates the malignant phenotype of hepatocellular carcinoma cells via inhibiting GSK3B expression. Hum Cell. 2024 Jul;37(4):1156-1169.
[7] Hah YS, Lee WK, Lee S, et al. β-Sitosterol Attenuates Dexamethasone-Induced Muscle Atrophy via Regulating FoxO1-Dependent Signaling in C2C12 Cell and Mice Model. Nutrients. 2022 Jul 14;14(14):2894.
[8] Panayotis N, Freund PA, Marvaldi L, et al. β-sitosterol reduces anxiety and synergizes with established anxiolytic drugs in mice. Cell Rep Med. 2021 May 18;2(5):100281.
β-Sitosterol是一种来源于植物的天然甾醇，具有抑制癌症发展等多种生物活性[1]。β-Sitosterol也常被用于研究对心血管健康的影响[2]。β-Sitosterol能够通过调节胆固醇的代谢，有助于降低血液中胆固醇水平，进而对心血管疾病的预防等方面起到积极作用[3]。β-Sitosterol具有一定的抗炎活性，可参与到机体的炎症调节过程中，辅助缓解一些炎症相关症状[4]。
在体外，β-Sitosterol（10、25、50µg/mL）处理人卵巢癌细胞系ES2和OV90 48h，可诱导细胞凋亡，抑制细胞增殖，降低线粒体膜电位，增加活性氧（ROS）和钙离子流入，改变细胞内信号通路，抑制细胞聚集、生长和迁移。与顺铂（20μM）或紫杉醇（20μM）等标准抗癌药物联合使用时，β-Sitosterol展现出协同抗癌效果[5]。β-Sitosterol（5、10、20µg/mL）处理人肝细胞癌细胞系Huh-7和HCCLM3 24-72h，β-Sitosterol显著抑制细胞增殖、迁移和侵袭，诱导细胞凋亡，抑制上皮-间质转化（EMT），降低GSK3B表达。与GSK3B抑制剂（CHIR-98014；50nM）联合使用时，β-Sitosterol进一步增强了对肝细胞癌细胞增殖和侵袭的抑制效果[6]。
在体内，β-Sitosterol（200mg/kg）每天一次口服给药，联合地塞米松（20mg/kg）每天一次腹腔注射，用于处理6周龄的C57BL/6小鼠，连续3周。β-Sitosterol通过调节FoxO1依赖性信号通路，显著减轻了地塞米松诱导的小鼠肌肉萎缩[7]。β-Sitosterol（100mg/kg）通过腹腔注射给药C57BL/6J小鼠，β-Sitosterol显著降低小鼠的焦虑行为，并且与氟西汀（5mg/kg；i.p.）联合使用时表现出协同抗焦虑效果[8]。