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Biomedicine & Pharmacotherapy =... Nov 2020Phytosterols are bioactive compounds that are naturally present in plant cell membranes with chemical structure similar to the mammalian cell- derived cholesterol. They... (Review)
Review
Phytosterols are bioactive compounds that are naturally present in plant cell membranes with chemical structure similar to the mammalian cell- derived cholesterol. They are highly present in lipid-rich plant foods such as nuts, seed, legumes and olive oil. Among various phytosterols, β-sitosterol (SIT) is the major compound, found plentiful in plants. It has been evidenced in many in-vitro and in-vivo studies that SIT possesses various biological actions such as anxiolytic & sedative effects, analgesic, immunomodulatory, antimicrobial, anticancer, anti - inflammatory, lipid lowering effect, hepatoprotective, protective effect against NAFLD and respiratory diseases, wound healing effect, antioxidant and anti-diabetic activities. In this review, in order to compile the sources, characterization, biosynthesis, pharmacokinetics, antioxidant and anti-diabetic activities of SIT, classical and online-literature were studied which includes the electronic search (Sci Finder, Pubmed, Google Scholar, Scopus, and Web of Science etc) and books on photochemistry. The experimental studies on SIT gives a clear evidence that the potential phytosterol can be used as supplements to fight against life threatening diseases. High potential of this compound, classifies it as the notable drug of the future. Therefore, immense researches regarding its action at molecular level on life threatening diseases in humans are highly endorsed.
Topics: Animals; Antioxidants; Diabetes Mellitus; Dietary Supplements; Humans; Sitosterols
PubMed: 32882583
DOI: 10.1016/j.biopha.2020.110702 -
Nutrients Jul 2022Sarcopenia refers to a decline in muscle mass and strength with age, causing significant impairment in the ability to carry out normal daily functions and increased risk...
Sarcopenia refers to a decline in muscle mass and strength with age, causing significant impairment in the ability to carry out normal daily functions and increased risk of falls and fractures, eventually leading to loss of independence. Maintaining protein homeostasis is an important factor in preventing muscle loss, and the decrease in muscle mass is caused by an imbalance between anabolism and catabolism of muscle proteins. Although β-sitosterol has various effects such as anti-inflammatory, protective effect against nonalcoholic fatty liver disease (NAFLD), antioxidant, and antidiabetic activity, the mechanism of β-sitosterol effect on the catabolic pathway was not well known. β-sitosterol was assessed in vitro and in vivo using a dexamethasone-induced muscle atrophy mice model and C2C12 myoblasts. β-sitosterol protected mice from dexamethasone-induced muscle mass loss. The thickness of gastrocnemius muscle myofibers was increased in dexamethasone with the β-sitosterol treatment group (DS). Grip strength and creatine kinase (CK) activity were also recovered when β-sitosterol was treated. The muscle loss inhibitory efficacy of β-sitosterol in dexamethasone-induced muscle atrophy in C2C12 myotube was also verified in C2C12 myoblast. β-sitosterol also recovered the width of myotubes. The protein expression of muscle atrophy F-box (MAFbx) was increased in dexamethasone-treated animal models and C2C12 myoblast, but it was reduced when β-sitosterol was treated. MuRF1 also showed similar results to MAFbx in the mRNA level of C2C12 myotubes. In addition, in the gastrocnemius and tibialis anterior muscles of mouse models, Forkhead Box O1 (FoxO1) protein was increased in the dexamethasone-treated group (Dexa) compared with the control group and reduced in the DS group. Therefore, β-sitosterol would be a potential treatment agent for aging sarcopenia.
Topics: Animals; Dexamethasone; Disease Models, Animal; Forkhead Box Protein O1; Forkhead Transcription Factors; Mice; Muscle Fibers, Skeletal; Muscle, Skeletal; Muscular Atrophy; Sarcopenia; Sitosterols; Ubiquitin-Protein Ligases
PubMed: 35889851
DOI: 10.3390/nu14142894 -
BMC Urology Jul 2020The present clinical trial was conducted to evaluate the efficacy and tolerability of a standardized saw palmetto oil containing 3% β-sitosterol in the treatment of... (Comparative Study)
Comparative Study Randomized Controlled Trial
A double blind, placebo-controlled randomized comparative study on the efficacy of phytosterol-enriched and conventional saw palmetto oil in mitigating benign prostate hyperplasia and androgen deficiency.
BACKGROUND
The present clinical trial was conducted to evaluate the efficacy and tolerability of a standardized saw palmetto oil containing 3% β-sitosterol in the treatment of benign prostate hyperplasia (BPH) and androgen deficiency.
METHODS
Subjects aged 40-65 years with symptomatic BPH were randomized to 12-week double-blind treatment with 500 mg doses of β-sitosterol enriched saw palmetto oil, conventional saw palmetto oil and placebo orally in the form of capsules (n = 33 in each group). BPH severity was determined using the International Prostate Symptom Score (IPSS), uroflowmetry, serum measurement of prostate specific antigen (PSA), testosterone and 5α-reductase. During the trial, the androgen deficiency was evaluated using Aging Male Symptoms (AMS) scale, the Androgen Deficiency in the Aging Male (ADAM) questionnaire, serum levels of free testosterone.
RESULTS
Subjects treated with β-sitosterol enriched saw palmetto oil showed significant decrease in IPSS, AMS and ADAM scores along with reduced postvoiding residual volume (p < 0.001), PSA (p < 0.01) and 5α-reductase from baseline to end of 12-week treatment as compared to placebo. There was also a significant increment in the maximum and average urine flow rate (p < 0.001), and serum free testosterone level of subjects treated with enriched saw palmetto oil as compared to placebo.
CONCLUSION
This study demonstrates the efficacy of β-sitosterol enriched saw palmetto oil superior to conventional oil thus extending the scope of effective BPH and androgen deficiency treatment with improved quality of life through the intake of functional ingredients.
TRIAL REGISTRATION
CTRI/2018/12/016724 dated 19/12/2018 prospectively registered. URL: http://ctri.nic.in/Clinicaltrials/advsearch.php.
Topics: Adult; Aged; Androgens; Double-Blind Method; Humans; Male; Middle Aged; Phytosterols; Phytotherapy; Plant Extracts; Plant Oils; Prostatic Hyperplasia; Serenoa; Sitosterols; Treatment Outcome; Urological Agents
PubMed: 32620155
DOI: 10.1186/s12894-020-00648-9 -
Journal of Lipid Research Jul 1992Sitosterolemia is a rare inherited lipid storage disease characterized chemically by the accumulation of plant sterols and 5 alpha-saturated stanols in plasma and... (Review)
Review
Sitosterolemia is a rare inherited lipid storage disease characterized chemically by the accumulation of plant sterols and 5 alpha-saturated stanols in plasma and tissues. Very low cholesterol synthesis due to a deficiency of HMG-CoA reductase associated with increased intestinal plant sterol absorption and slow hepatic sterol removal are major biochemical features. Because cholesterol synthesis cannot up-regulate, bile acid malabsorption mobilizes body sterols for bile acid synthesis and dramatically lowers plasma and monocyte sterol concentrations and may halt the progression of the atherosclerotic process.
Topics: Cholesterol; Humans; Lipid Metabolism, Inborn Errors; Sitosterols
PubMed: 1431587
DOI: No ID Found -
The Cochrane Database of Systematic... 2000This systematic review aimed to assess the effects of beta-sitosterols (B-sitosterol) on urinary symptoms and flow measures in men with of benign prostatic hyperplasia... (Review)
Review
OBJECTIVES
This systematic review aimed to assess the effects of beta-sitosterols (B-sitosterol) on urinary symptoms and flow measures in men with of benign prostatic hyperplasia (BPH).
SEARCH STRATEGY
Trials were searched in computerized general and specialized databases (MEDLINE, EMBASE, Cochrane Library, Phytodok), by checking bibliographies, and by contacting manufacturers and researchers.
SELECTION CRITERIA
Trials were eligible for inclusion provided they (1) randomized men with BPH to receive B-sitosterol preparations in comparison to placebo or other BPH medications, and (2) included clinical outcomes such as urologic symptom scales, symptoms, or urodynamic measurements.
DATA COLLECTION AND ANALYSIS
Information on patients, interventions, and outcomes was extracted by at least two independent reviewers using a standard form. Main outcome measure for comparing the effectiveness of B-sitosterols with placebo and standard BPH medications was the change in urologic symptom scale scores. Secondary outcomes included changes in nocturia as well as urodynamic measures (peak and mean urine flow, residual volume, prostate size). Main outcome measure for side effects was the number of men reporting side effects.
MAIN RESULTS
519 men from 4 randomized, placebo-controlled, double-blind trials, (lasting 4 to 26 weeks) were assessed. 3 trials used non-glucosidic B-sitosterols and one utilized a preparation that contained 100% B-sitosteryl-B-D-glucoside. B-Sitosterols improved urinary symptom scores and flow measures. The weighted mean difference (WMD) for the IPSS was -4.9 IPSS points (95%CI = -6.3 to -3.5, n = 2 studies). The WMD for peak urine flow was 3.91 ml/sec (95%CI = 0.91 to 6.90, n = 4 studies) and the WMD for residual volume was -28.62 ml (95%CI = -41. 42 to -15.83, n = 4 studies). The trial using 100% B-sitosteryl-B-D-glucoside (WA184) show improvement in urinary flow measures. B-sitosterols did not reduce prostate size. Withdrawal rates for men assigned to B-sitosterol and placebo were 7.8% and 8. 0%, respectively.
REVIEWER'S CONCLUSIONS
The evidence suggests non-glucosidic B-sitosterols improve urinary symptoms and flow measures. Their long term effectiveness, safety and ability to prevent BPH complications are not known.
Topics: Humans; Male; Phytotherapy; Prostatic Hyperplasia; Sitosterols; Urodynamics
PubMed: 10796740
DOI: 10.1002/14651858.CD001043 -
International Journal of Molecular... Nov 2021Phytosterols constitute a class of natural products that are an important component of diet and have vast applications in foods, cosmetics, and herbal medicines. With... (Review)
Review
Phytosterols constitute a class of natural products that are an important component of diet and have vast applications in foods, cosmetics, and herbal medicines. With many and diverse isolated structures in nature, they exhibit a broad range of biological and pharmacological activities. Among over 200 types of phytosterols, stigmasterol and β-sitosterol were ubiquitous in many plant species, exhibiting important aspects of activities related to neurodegenerative diseases. Hence, this mini-review presented an overview of the reported studies on selected phytosterols related to neurodegenerative diseases. It covered the major phytosterols based on biosynthetic considerations, including other phytosterols with significant in vitro and in vivo biological activities.
Topics: Brain; Humans; Molecular Structure; Neurodegenerative Diseases; Neuroprotective Agents; Phytosterols; Phytotherapy; Plants, Medicinal; Sitosterols; Stigmasterol
PubMed: 34830148
DOI: 10.3390/ijms222212255 -
Journal of Atherosclerosis and... Sep 2018Sitosterolemia is a rare inherited disease characterized by increased levels of plant sterols, such as sitosterol. The cause of this disease is ATP-binding cassette... (Review)
Review
Sitosterolemia is a rare inherited disease characterized by increased levels of plant sterols, such as sitosterol. The cause of this disease is ATP-binding cassette (ABC) subfamily G member 5 or member 8 (ABCG5 or ABCG8, respectively) gene mutations. Recent advances in genetics have revealed that the prevalence of subjects with deleterious mutations in ABCG5 and/or ABCG8 genes could be more than 1 in ~200,000 individuals among the general population. Furthermore, accumulated evidence, including infantile cases exhibiting progression/regression of systemic xanthomas associated with LDL cholesterol levels, have shown that the elevation of LDL cholesterol seems to be the major cause of development of atherosclerosis and not the elevation of sitosterol. Regarding therapies, LDL apheresis, as well as proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, could be useful for sitosterolemia, in addition to ezetimibe and/or colestimide. In this study, we provide the current understanding and future perspectives of sitosterolemia, which is currently considered an extremely rare disorder but is expected to be much more prevalent in clinical settings.
Topics: ATP Binding Cassette Transporter, Subfamily G, Member 5; ATP Binding Cassette Transporter, Subfamily G, Member 8; Coronary Artery Disease; Heterozygote; Humans; Hypercholesterolemia; Intestinal Diseases; Lipid Metabolism, Inborn Errors; Lipoproteins; Mutation; Phenotype; Phytosterols; Polymorphism, Genetic; Proprotein Convertase 9; Sitosterols
PubMed: 30033951
DOI: 10.5551/jat.RV17024 -
Current Opinion in Lipidology Apr 2001The molecular mechanisms regulating the amount of dietary cholesterol retained by the body, as well as the body's ability to exclude other dietary sterols selectively,... (Review)
Review
The molecular mechanisms regulating the amount of dietary cholesterol retained by the body, as well as the body's ability to exclude other dietary sterols selectively, are poorly understood. An average Western diet will contain approximately 250-500 mg of dietary cholesterol and approximately 200-400 mg of non-cholesterol sterols, of which plant sterols are the major constituents. Approximately 50-60% of dietary cholesterol is absorbed and retained by the normal human body, but less than 1% of the non-cholesterol sterols are retained. There thus exists a subtle mechanism that allows the body to distinguish between cholesterol and non-cholesterol sterols. In sitosterolemia, a rare autosomal recessive disorder, affected individuals hyperabsorb and retain not only cholesterol but also all other sterols, including plant and shellfish sterols from the intestine. Consequently, patients with this disease have very high levels of plant sterols in the plasma, and develop tendon and tuberous xanthomas, accelerated atherosclerosis, and premature coronary artery disease. The STSL locus has been mapped to human chromosome 2p21. Mutations in two tandem ABC genes, ABCG5 and ABCG8, encoding sterolin-1 and -2, respectively, are now known to be mutant in sitosterolemia. The identification of these genes should now lead to a better understanding of the molecular mechanism(s) governing the highly selective absorption and retention of cholesterol by the body. Indeed, it is the very existence of this disease that has given credence to the hypothesis that there is a molecular pathway that regulates dietary cholesterol absorption and sterol excretion by the body.
Topics: ATP-Binding Cassette Transporters; Cholesterol; Chromosomes, Human, Pair 2; Female; Homozygote; Humans; Lipid Metabolism, Inborn Errors; Male; Mutation; Pedigree; Sitosterols
PubMed: 11264985
DOI: 10.1097/00041433-200104000-00007 -
Advances in Nutrition (Bethesda, Md.) Sep 2023Cancer is one of the primary causes of death worldwide, and its incidence continues to increase yearly. Despite significant advances in research, the search for... (Review)
Review
Cancer is one of the primary causes of death worldwide, and its incidence continues to increase yearly. Despite significant advances in research, the search for effective and nontoxic preventive and therapeutic agents remains greatly important. Cancer is a multimodal disease, where various mechanisms play significant roles in its occurrence and progression. This highlights the need for multitargeted approaches that are not only safe and inexpensive but also provide effective alternatives for current therapeutic regimens. β-Sitosterol (SIT), the most abundant phytosterol found in various plant foods, represents such an option. Preclinical evidence over the past few decades has overwhelmingly shown that SIT exhibits multiple anticancer activities against varied cancers, such as liver, cervical, colon, stomach, breast, lung, pancreatic, and prostate cancers, in addition to leukemia, multiple myeloma, melanoma, and fibrosarcoma. In this article, we present the latest advances and perspectives on SIT-systematically summarizing its antitumor mechanisms of action into 7 main sections and combining current challenges and prospects-for its use as a promising agent for cancer prevention and treatment. In particular, SIT plays a role in cancer prevention and treatment mainly by enhancing apoptosis, inducing cell cycle arrest, bidirectionally regulating oxidative stress, improving metabolic reprogramming, inhibiting invasion and metastasis, modulating immunity and inflammation, and combating drug resistance. Although SIT holds such great promise, the poor aqueous solubility and bioavailability coupled with low targeting efficacy limit its therapeutic efficacy and clinical application. Further research on novel drug delivery systems may improve these deficiencies. Overall, through complex and pleiotropic mechanisms, SIT has good potential for tumor chemoprevention and chemotherapy. However, no clinical trials have yet proven this potential. This review provides theoretical basis and rationality for the further design and conduct of clinical trials to confirm the anticancer activity of SIT.
Topics: Male; Humans; Antineoplastic Agents; Sitosterols; Prostatic Neoplasms; Chemoprevention
PubMed: 37247842
DOI: 10.1016/j.advnut.2023.05.013 -
Journal of Atherosclerosis and... Sep 2023
Topics: Humans; Cholesterol; Hypercholesterolemia; Intestinal Absorption; Sitosterols
PubMed: 36642538
DOI: 10.5551/jat.ED221