Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc^{[1][2][3][4][5][6][7][8][9][10]}.

Beta-Sitosterol (0-40 µM, 24 h) decreases cell viability with concentrations exceeding 5 µM in MAC-T cells ^[1].
Beta-Sitosterol (1 µM, 24 h) increases the levels of CAT, GSH, T-AOC, T-SOD and decreases the level of ROS, TNF-α, IL-1β, NF-κB p65 in LPS (HY-D1056)-induced MAC‐T cells^[1].
Beta-Sitosterol (1 µM, 24 h) inhibits apoptosis, attenuates the expression levels of caspase-3 and Bax, increases the levels of Bcl-2 and Bcl-2/Bax radio in LPS-induced MAC‐T cells^[1].
Beta-Sitosterol (1 µM, 24 h) restores HIF-1α/mTOR signaling pathway viability and the expression of fat synthesis-related Genes (SCD, PSMA5, FASN, SREBP1) in LPS-induced MAC-T cells^[1].
Beta-Sitosterol (25-200 µM, 24-72 h) affectes the growth of A549 cells, with an IC₅₀ of 24.7 μM at 72 h, increases the release of LDH in A549 cells, affects the viability of NCI-H460 cells, but does not affect the growth and viability of normal human lung, PBMC cells and NCI-H23 cells^[2].
Beta-Sitosterol (25-200 µM, 24-72 h) induces cell cycle arrest at Sub-G1 phase, reduces the expression of Cyclin D1 and CDK2 in A549 cells^[2].
Beta-Sitosterol (25-200 µM, 0-72 h) induces apoptosis occurred via mitochondrial dysfunction and ROS mediated DNA damage in A549 cells^[2].
Beta-Sitosterol (25-200 µM, 0-72 h) elevates the expression levels of caspase-3, caspase-9, cleavage PARP, Bax, p53 and pSer15-p53, suppresses the expression levels of Bcl-2 in A549 cells^[2].
Beta-Sitosterol (25-200 µM, 72 h) induces apoptosis occurred via the activation of p53 in NCI-H460 cells^[2].
Beta-Sitosterol decreases the expression of both TrxR1 and Trx1 in A549 and NCI-H460 cells^[2].
Beta-Sitosterol (5-50 µM, 24 h) blocks M1 but promotes M2 macrophage polarization in IFN-γ/IL-4-stimulated BMBMs^[3].
Beta-Sitosterol (1-150 μM/L, 5 days) increases MCF-7 cells proliferation^[5].
Beta-Sitosterol (8-16 μM, 5 days) causes a significant reduction in cell growth, alters composition of cell membranes in MCF-7 and MDA-MB-231 cells^[6].
Beta-Sitosterol (16 μM, 1-3 days) increases caspase-8 activity and Fas protein levels in MCF-7 and MDA-MB-231 cells^[6].
Beta-Sitosterol (0.1-100 μM, 18 h) reduces VCAM-1 and ICAM-1 expression, attenuates phosphorylation of NFkB p65 in TNF-α- stimulated HAEC, inhibits binding of U937 cells to TNF-α-stimulated HAEC^[7].
Beta-Sitosterol (50 μM, 1-6 h) reverts the enhancement of GSSG levels and the impairment of GSH levels or the GSH/total glutathione ratio induced by PMA (HY-18739) in RAW 264.7 cells^[8].
Beta-Sitosterol (50 μM, 1-6 h) increases GPx and Mn SOD activities, and decreases catalase activity in RAW 264.7 cells^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Beta-Sitosterol (20-50  mg/kg, i.p., every 2 days, 31 days; 2 × 10⁶ BMDMs treating with 25 μM BS, i.v., once) inhibits pathological changes by suppressing humoral and cellular immune responsesin, in part, through IL-10 transfer in Collagen (HY-NP003)-induced arthritis (CIA) mice model^[3].
Beta-Sitosterol (2-5 mg/20 g mouse, i.p., once) plays an analgesic role in Acetic acid (HY-Y0319)-induced Swiss Webster albino mice model^[4].
Beta-Sitosterol (2 mg/20 g mouse, i.p., once) plays an anti-inflammatory role in Carrageenan (HY-125474)-induced mouse paw oedema model^[4].
Beta-Sitosterol (9.8 g/kg diet, o.p., 18 weeks) inhibits the growth of estrogen-responsive breast cancer cells of MCF-7 tumors implanted in ovariectomized athymic mice^[5].
Beta-Sitosterol (10-20 mg/kg, o.p., once a day, 21 days) has antidiabetic as well as antioxidant effects in Streptozotocin (HY-13753)-induced diabetes Wistar rats model^[9].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

414.71

C₂₉H₅₀O

83-46-5

Solid

White to off-white

CC[C@@H](C(C)C)CC[C@@H](C)[C@H]1CC[C@@]2(09)[C@]3(09)CC=C4C[C@@H](O)CC[C@]4(C)[C@@]3(09)CC[C@]12C

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Fan Y, et al. β-Sitosterol Suppresses Lipopolysaccharide-Induced Inflammation and Lipogenesis Disorder in Bovine Mammary Epithelial Cells. Int J Mol Sci. 2023 Sep 27;24(19):14644.  [Content Brief]

  [2]. Rajavel T, et al. β-Sitosterol targets Trx/Trx1 reductase to induce apoptosis in A549 cells via ROS mediated mitochondrial dysregulation and p53 activation. Sci Rep. 2018 Feb 1;8(1):2071.  [Content Brief]

  [3]. Liu R, et al. β-Sitosterol modulates macrophage polarization and attenuates rheumatoid inflammation in mice. Pharm Biol. 2019 Dec;57(1):161-168.  [Content Brief]

  [4]. Villaseñor IM, et al. Bioactivity studies on beta-sitosterol and its glucoside. Phytother Res. 2002 Aug;16(5):417-21.  [Content Brief]

  [5]. Ju YH, et al. beta-Sitosterol, beta-Sitosterol Glucoside, and a Mixture of beta-Sitosterol and beta-Sitosterol Glucoside Modulate the Growth of Estrogen-Responsive Breast Cancer Cells In Vitro and in Ovariectomized Athymic Mice. J Nutr. 2004 May;134(5):1145-51.  [Content Brief]

  [6]. Awad AB, et al. beta-Sitosterol activates Fas signaling in human breast cancer cells. Phytomedicine. 2007 Nov;14(11):747-54.  [Content Brief]

  [7]. Loizou S, et al. Beta-sitosterol exhibits anti-inflammatory activity in human aortic endothelial cells. Mol Nutr Food Res. 2010 Apr;54(4):551-8.  [Content Brief]

  [8]. Vivancos M, et al. beta-Sitosterol modulates antioxidant enzyme response in RAW 264.7 macrophages. Free Radic Biol Med. 2005 Jul 1;39(1):91-7.  [Content Brief]

  [9]. Gupta R, et al. Antidiabetic and antioxidant potential of β-sitosterol in streptozotocin-induced experimental hyperglycemia. J Diabetes. 2011 Mar;3(1):29-37.  [Content Brief]

  [10]. Anwar R, et al. Antimicrobial Activity of β-Sitosterol Isolated from Kalanchoe tomentosa Leaves Against Staphylococcus aureus and Klebsiella pneumonia. Pak J Biol Sci. 2022 Jun;25(7):602-607.  [Content Brief]