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Induction of apoptosis in COLO 320 DM. Human colon cancer cell lines (COLO 320 DM) cells were treated 120 or 240 μM β-sitosterol. The anti-proliferative effect is shown in (a), flow cytometric analysis for the determination of pro-apoptotic/apoptotic/necrotic cells is given in (b), and fluorescent staining of nuclei by Hoechst 33258 at 20× is seen in (c).
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Asclepias curassavica Linn. is a traditional medicinal plant used by tribal people in the western ghats, India, to treat piles, gonorrhoea, roundworm infestation and abdominal tumours. We have determined the protective effect of beta-sitosterol isolated from A. curassavica in colon cancer, using in vitro and in vivo models.
The active molecule was...
Contexts in source publication
Context 1
... had anti-radical activity, with an IC 50 of 389.5 μM and 448.2 μM for DPPH and NO scavenging assays, respectively (Figure 2A &2B). β-sitosterol was noticeably inhibitory within 24 h at 30 μM and significantly more so at 240 μM (P < 0.05; Figure 3A), with minimal toxicity in non-cancerous cells (VERO). IC 50 values were 266.2 μM for COLO 320 cells and >1 mM for VERO cells. ...Context 2
... increased number of COLO 320 DM cells treated with 240 μM β-sitosterol stained with Annexin FITC + / PI + , with a lower percentage of necrotic or propidium iodide stained cells after 24 h incubation ( Figure 3B). β- sitosterol induced DNA fragmentation even at a 15 μM; increased DNA fragmentation and DNA tailing also ocurred in cancer cells treated with 120 μM β-sitosterol ( Figure 3C). ...Context 3
... increased number of COLO 320 DM cells treated with 240 μM β-sitosterol stained with Annexin FITC + / PI + , with a lower percentage of necrotic or propidium iodide stained cells after 24 h incubation ( Figure 3B). β- sitosterol induced DNA fragmentation even at a 15 μM; increased DNA fragmentation and DNA tailing also ocurred in cancer cells treated with 120 μM β-sitosterol ( Figure 3C). DCF fluorescence in COLO 320 DM cells indicates enhanced free radical generation in living cells ( Figure 4A). ...Citations
... Two constituents of dichloromethane extract of wheatgrass are β-sitosterol and galactolipids [58]. β-sitosterol was shown to inhibit cancer development in a renal cancer model [59] and possess an anti-proliferative as well as a pro-apoptotic potential through induction of cell cycle arrest and cell demise [60]. Moreover, β-sitosterol and β-sitosterol glycoside complexes derived from plant origins act by targeting certain T-helper lymphocytes and augmenting lymphocyte production and natural killer cell action [61]. ...
The etiology of colon cancer is either genetic in nature or results from inflammatory bowel diseases such as ulcerative colitis and Crohn’s disease; nevertheless, dietary habits play a crucial role in the disease. Wheatgrass is a dietary supplement that is rich in vitamins, minerals, and antioxidants which contribute to health promotion in cardiovascular diseases, liver disease, blood diseases, diabetes, and inflammatory bowel diseases, as well as in several types of cancers, such as oral squamous cell cancer, cervical cancer, and breast cancer. In colorectal cancer (CRC), the prospect that wheatgrass possesses anti-inflammatory, antioxidant, and anticancer properties, and its use as an adjunctive therapy, have been minimally investigated and evidence is still limited. In this review, we compiled the available evidence pertaining to wheatgrass and its likely impact on CRC, described the pathways of inflammation in which wheatgrass could possibly play a role, and identified future research needs on the subject.
... Studies on nutraceutical foods have shown that the ingestion of βsitosterol, one of the main phytosterols found in the Arachis genus, inhibits intestinal cholesterol absorption, prevents cardiovascular disease (Li et al., 2022), and reduces the risk of lung, breast, stomach, esophageal, prostate, colon, rectum, endometrial, and ovarian cancers (Bin Sayeed and Ameen, 2015). In addition to prevention, cytotoxic activity against colon (Baskar et al., 2010), prostate (Awad et al., 2000), and breast (Awad et al., 2007) tumors has been demonstrated. In Arachis seeds, the types and content of phytosterols vary according to the species and genotypes (Awad et al., 2000;Grosso et al., 2000). ...
... The same study, among others, was conducted on an in vitro model using human adenocarcinoma cells and measuring proliferating cell nuclear antigen (PCNA) in human colon cancer cell lines (COLO 320 DM). The results showed inhibition of PCNA antigens and dose-dependent growth inhibition of COLO 320 cell lines, where the IC50 was 266.2 µM [64]. Moreover, β-sitosterol attenuated β-catenin and proliferating cell nuclear antigen expression. ...
Phytosterols are a large group of substances belonging to sterols—compounds naturally occurring in the tissues of plants, animals, and humans. The most well-known animal sterol is cholesterol. Among phytosterols, the most significant compounds are β-sitosterol, stigmasterol, and campesterol. At present, they are mainly employed in functional food products designed to counteract cardiovascular disorders by lowering levels of ‘bad’ cholesterol, which stands as their most extensively studied purpose. It is currently understood that phytosterols may also alleviate conditions associated with the gastrointestinal system. Their beneficial pharmacological properties in relation to gastrointestinal tract include anti-inflammatory and hepatoprotective activity. Also, the anti-cancer properties as well as the impact on the gut microbiome could be a very interesting area of research, which might potentially lead to the discovery of their new application. This article provides consolidated knowledge on a new potential use of phytosterols, namely the treatment or prevention of gastrointestinal diseases. The cited studies indicate high therapeutic efficacy in conditions such as peptic ulcer disease, IBD or liver failure caused by hepatotoxic xenobiotics, however, these are mainly in vitro or in vivo studies. Nevertheless, studies to date indicate their therapeutic potential as adjunctive treatments to conventional therapies, which often exhibit unsatisfactory efficacy or serious side effects. Unfortunately, at this point there is a lack of significant clinical study data to use phytosterols in clinical practice in this area.
... The proliferation of COLO 320 DM cells is inhibited dosedependently by β-sitosterol (IC50 266.2 microM), which also scavenges reactive oxygen species to cause apoptosis and suppresses the expression of β-catenin and proliferating cell nuclear antigen in human colon cancer cells (Baskar et al., 2010). Adding β-sitosterol to colon cancer cell lines prevents them from growing without changing the overall amount of phospholipids in the membrane. ...
sitosterol is waxy substance, white in color distributed in a variety of natural plant sources cereals, pulses, legumes, vegetables, fruits, and herbs. Several clinical and preclinical investigations indicate that β-sitosterol has a wide range of important health advantages. It prevents many types of malignancies, lowers levels of low density lipoprotein (LDL), lowers the risk of coronary artery disease, heart attacks, and atherosclerosis, and supports the body’s natural healing process. It is found to have cancer-protective properties and has the potency to be beneficial against breast, prostate, colon, lung, stomach, and leukemia. The present review provides a complete analysis and examines the literature on β-sitosterol from different dietary sources, with a focus on its toxicological characteristics and nutraceutical qualities. It lays down the theoretical basis and justification for directing the future planning and execution of clinical studies intended to confirm the importance and possible toxicity of β-sitosterol.
... In non-1,2-dimethylhydrazine (DMH) treated rats, supplementation of β-sitosterol did not induce ACF in colonic mucosa. In DMH-treated rats, a substantial reduction in the count of the aberrant crypt and its multiplicity was observed when exposed to β-sitosterol for 16 weeks [92]. ...
Cancer remains one of the major causes of morbidity and mortality worldwide. Scientists from different fields are working to devise an efficient treatment strategy in order to reduce the global burden of cancer. Commonly used treatment approaches for cancer treatment include chemotherapy, immunotherapy, photodynamic therapy, radiation, surgery, etc. These treatment procedures have several pitfalls, such as toxicity, limited bioavailability, rapid elimination, poor specificity, and high cost. On the other side, plant-derived anticancer compounds exhibit several advantages and can overcome these shortcomings. Plant-based anticancer compounds are safer, potent, easily available, and comparatively cost-effective. The current review discusses pure plant- based compounds that are used as a therapeutic remedy for anticancer application. The proposed mechanisms of action, through which these compounds inhibit cancer cell growth, tumor growth, angiogenesis, instigate apoptosis, cytotoxicity, mitochondrial membrane degradation, and reduce cell viability as well as cell cycle progression, are also reviewed. These naturally occurring compounds exhibit great therapeutic potential and could be used as candidate drugs in clinical applications.
... Phytosterols have been found to have a protective effect against various types of cancer such as breast (30), prostate (34), lung (14), liver and stomach (35), and ovary and colon cancers (36). In vivo studies have demonstrated that diets enriched with phytosterols (2%, w/w) helped improve lipid profiles and reduced atherosclerotic lesions in apolipoprotein E-knockout (apo E-KO) mice (14,37). ...
Background: Consuming a diet rich in natural foods that include oilseed products containing minor bioactive compounds and a diverse array of fatty acids is not just a dietary choice; it is a critical element of maintaining human health. Objective: This paper aims to review the current state of knowledge on minor bioactive compounds in plant cold pressed oils, these are substances that are found in small amounts in plant cold pressed oils. Methods: This review provides a comprehensive analysis of the current state of the art, using data from peer-reviewed articles sourced from various databases. Results and Discussion: Cold-pressed oils extracted from various plant sources have emerged as vital allies in the battle against inflammation-related diseases, offering a versatile range of valuable compounds. These compounds contribute to the oils' multifaceted properties, which encompass potent anti-inflammatory, antioxidant, and anticancer effects, greatly enhancing their nutritional significance. This brief review delves deep into the intricate composition of cold-pressed oils, with a specific focus on the often overlooked but highly influential minor bioactive compounds, including phytosterols, phospholipids, tocols, phenols, squalene and pigments. Conclusion: This paper highlights the importance of cold-pressed oils as a source of various minor bioactive compounds that have the potential to promote human health and prevent or manage a range of diseases. The findings presented in this paper serve as a valuable resource for medical professionals in the field of integrative medicine, nutrition, and dietetics, as well as for consumers looking to make informed choices about their dietary and health needs.
... Due to its promising safety profile, low toxicity, and efficacy, β-sitosterol has garnered significant attention in recent research. Extensive pharmacological studies have confirmed its considerable anti-cancer activity, indicating its potential as a therapeutic agent for various cancers (Baskar et al., 2010). ...
... colon cancer (COLO 320 DM) cells in a dose-dependent manner, further causing apoptosis by scavenging reactive oxygen species (ROS), inhibiting the β-catenin expression and proliferating cell nuclear antigen (PCNA) antigens. In in vivo model of colon cancer, β-sitosterol supplementation has reduced the amount of aberrant crypt and crypt multiplicity in a concentration-dependent manner(Baskar et al., 2010). β-sitosterol decreased HCT116 cell growth and induced an early apoptosis(Alvarez-Sala et al., 2019).The addition of β-sitosterol to colorectal HT-29 cancer cells resulted in the suppression of cell proliferation without affecting the total concentration of membrane phospholipids. ...
Sterols, including β-sitosterol, are essential components of cellular membranes in both plant and animal cells. Despite being a major phytosterol in various plant materials, comprehensive scientific knowledge regarding the properties of β-sitosterol and its potential applications is essential for scholarly pursuits and utilization purposes. β-sitosterol shares similar chemical characteristics with cholesterol and exhibits several pharmacological activities without major toxicity. This study aims to bridge the gap between phytochemistry and current pharmacological evidence of β-sitosterol, focusing on its anticancer activity and other biomedical properties. The goal is to provide a comprehensive understanding of β-sitosterol's potential for future translational approaches. A thorough examination of the literature was conducted to gather relevant information on the biological properties of β-sitosterol, particularly its anticancer therapeutic potential. Various databases were searched, including PubMed/MedLine, Scopus, Google Scholar, and Web of Science using appropriate keywords. Studies investigating the effects of β-sitosterol on different types of cancer were analyzed, focusing on mechanisms of action, pharmacological screening, and chemosensitizing properties. Modern pharmacological screening studies have revealed the potential anticancer therapeutic properties of β-sitosterol against various types of cancer, including leukemia, lung, stomach, breast, colon, ovarian, and prostate cancer. β-sitosterol has demonstrated chemosensitizing effects on cancer cells, interfering with multiple cell signaling pathways involved in proliferation, cell cycle arrest, apoptosis, survival, metastasis invasion, angiogenesis, and inflammation. Structural derivatives of β-sitosterol have also shown anti-cancer effects. However, research in the field of drug delivery and the detailed mode of action of β-sitosterol-mediated anticancer activities remains limited. β-sitosterol, as a non-toxic compound with significant pharmacological potential, exhibits promising anticancer effects against various cancer types. Despite being relatively less potent than conventional cancer chemotherapeutics, β-sitosterol holds potential as a safe and effective nutraceutical against cancer. Further comprehensive studies are recommended to explore the biological properties of β-sitosterol, including its mode of action, and develop novel formulations for its potential use in cancer treatment. This review provides a foundation for future investigations and highlights the need for further research on β-sitosterol as a potent superfood in combating cancer.
... But plants can also deal with factors that promote oxidative stress, inflammation, and hyperglycemia thereby making conditions unconducive for malignant cells to grow and spread. [9][10][11][12] Numerous intracellular signal-transduction pathways converge with the activation of the transcription factors NF-κB and AP1, which act independently or coordinately to regulate target-gene expression. 7,8 Atypical activation of NF-κB has been associated with protection against apoptosis and stimulation of proliferation in malignant cells, 7,8 and overexpression of NF-κB is causally linked to the phenotypic changes that are characteristic of neoplastic transformations. ...
... 8 Many chemo preventive phytochemicals that are derived from the diet have been shown to suppress constitutive NF-κB activation in malignant cells or NF-κB activation induced by the external tumour promoter phorbol 12-myristate 13-acetate (PMA) or tumour-necrosis factor-α (TNF-α). 9,13 The conventional approach to cancer treatment is based on drugs that retard the proliferation of abnormal cells (cytostatic) or that can kill the abnormal cells (cytotoxic). The mechanisms of actions employed by these drugs includes the inhibition of cell division or by the killing of neoplastic cells by the induction of apoptosis (suicide by cells). ...
... β-Sitosterol plays an important role in the prevention and treatment of cancers. It can inhibit proliferation and induce apoptosis in cancer cells [15]. Recent studies have shown that β-sitosterol can exhibit anti-pancreatic cancer activity by modulating apoptosis and inhibiting epithelial-mesenchymal transition (EMT) by deactivating Akt/GSK-3β signaling [16]. ...
Glioma is characterized by rapid cell proliferation, aggressive invasion, altered apoptosis and a poor prognosis. β-Sitosterol, a kind of phytosterol, has been shown to possess anticancer activities. Our current study aims to investigate the effects of β-sitosterol on gliomas and reveal the underlying mechanisms. Our results show that β-sitosterol effectively inhibits the growth of U87 cells by inhibiting proliferation and inducing G2/M phase arrest and apoptosis. In addition, β-sitosterol inhibits migration by downregulating markers of epithelial-mesenchymal transition (EMT). Mechanistically, network pharmacology and transcriptomics approaches illustrate that the EGFR/MAPK signaling pathway may be responsible for the inhibitory effect of β-sitosterol on glioma. Afterward, the results show that β-sitosterol effectively suppresses the EGFR/MAPK signaling pathway. Moreover, β-sitosterol significantly inhibits tumor growth in a U87 xenograft nude mouse model. β-Sitosterol inhibits U87 cell proliferation and migration and induces apoptosis and cell cycle arrest in U87 cells by blocking the EGFR/MAPK signaling pathway. These results suggest that β-sitosterol may be a promising therapeutic agent for the treatment of glioma.
... β-Sitosterol (5b) also displayed several biological activities like antipyretic, antioxidant, antimicrobial, antidiabetic, antiinflammatory, antihypercholesterolemic, antiarthritic, antipulmonary tuberculosis, immune modulation and anti-HIV and anticancerogenic activities [37]. Compound 5b reduced β-catenin and PCNA regulation, which hypothetically could be considered as an adjuvant in colon cancer treatment [38] and showed promising results in 1,2-dimethylhydrazine (DMH) stimulated colonic preneoplastic progression in Wistar rats as demonstrated by the observed radical scavenging ability [39]. ...
The chemical analysis of dichloromethane (DCM) extract of Macaranga grandifolia (Blanco) Merr. resulted in the isolation and identification of several compounds. From the leaves, vedelianin (1), squalene (2), β-carotene (3) and polyprenol (4) were isolated. The barks contained a mixture of stigmasterol (5a) and β-sitosterol (5b). Additionally, the fruits yielded saturated fatty acid (6). The elucidation of structure 1 was accomplished through the utilization of comprehensive 1D and 2D NMR spectroscopic techniques. The identification of the structures of compounds 2-6 was achieved through a comparative analysis of their nuclear magnetic resonance (NMR) data with the literature data.
