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(bay-ta seato-stair-ol)
CategoryDHT reducer

Parameter Effect Result on hair growth
5a-reductases UNKNOWN



Beta-sitosterol is a substance found in plants and is also called a “plant sterol ester.” A natural substance found in all types of fruits, vegetables, nuts, and seeds. These include flax, soy, peanuts, olive oil among others. Often used to treat high cholesterol. It has been shown to be effective in combination with Saw Palmetto to treat of BHP (benign prostatic hyperplasia). It has also been used in the treatment of skin wounds.

Some studies have shown it to have anti-inflammatory properties.

Typical Results N/A
Typical Dosages N/A
Significant Side Effects N/A
Dissolves inN/A
Pharmacology Pharmacodynamics N/A

Clinical Studies

Clinical StudiesAbstract
Inhibition of inflammatory gene expression in keratinocytes using a composition containing carnitine, thioctic Acid and saw palmetto extract. Chronic inflammation of the hair follicle (HF) is considered a contributing factor in the pathogenesis of androgenetic alopecia (AGA). Previously, we clinically tested liposterolic extract of Serenoa repens (LSESr) and its glycoside, β-sitosterol, in subjects with AGA and showed a highly positive response to treatment. In this study, we sought to determine whether blockade of inflammation using a composition containing LSESr as well as two anti-inflammatory agents (carnitine and thioctic acid) could alter the expression of molecular markers of inflammation in a well-established in vitro system. Using a well-validated assay representative of HF keratinocytes, specifically, stimulation of cultured human keratinocyte cells in vitro, we measured changes in gene expression of a spectrum of well-known inflammatory markers. Lipopolysaccharide (LPS) provided an inflammatory stimulus. In particular, we found that the composition effectively suppressed LPS-activated gene expression of chemokines, including CCL17, CXCL6 and LTB(4) associated with pathways involved in inflammation and apoptosis. Our data support the hypothesis that the test compound exhibits anti-inflammatory characteristics in a well-established in vitro assay representing HF keratinocyte gene expression. These findings suggest that 5-alpha reductase inhibitors combined with blockade of inflammatory processes could represent a novel two-pronged approach in the treatment of AGA with improved efficacy over current modalities.
Link to Full Study
Chemical constituents, anti-inflammatory and antioxidant activities of bark extracts from Prunus tucumanensis Lillo. The anti-inflammatory, antioxidant, antimicrobial and cytotoxic activities of the hexane (HE), chloroform (CE) and methanol (ME) extracts obtained from the bark of Prunus tucumanensis Lillo were investigated. Both ME and CE extracts displayed a significant in vitro anti-inflammatory activity similar to dexamethasone and to a commercial formulation (Pygeum) used for the treatment of benign prostatic hyperplasia (BPH). ME exhibited powerful antioxidant (67.6% relative to BHT) and free radical scavenging (RC(50) = 5 ppm) activities, antimicrobial activities against Staphylococcus aureus and Mycobacterium smegmatis and did not show any cytotoxic effect on human-derived macrophage cells. Chemical analyses showed that (2 R,3 R)-3,5,7,3',5'-pentahydroxyflavan, β-sitosterol and β-sitosterol-3-O-β-D-glucopyranoside (daucosterol) are relevant components of ME.
Dietary supplements for benign prostatic hyperplasia: An overview of systematic reviews. Benign prostatic hyperplasia (BPH) is a common chronic condition in older men. The aim of this overview of systematic reviews (SRs) is to summarise the current evidence on the efficacy and adverse effects of dietary supplements for treating BPH with lower urinary tract symptoms. We searched 5 electronic databases and relevant overviews without limitations on language or publication status. Six SRs of 195 articles were included in this overview. Serenoa repens was reviewed in 3 studies and no specific effect on BPH symptoms and urinary flow measures was observed. However, β-sitosterol, Pygeum africannum and Cernilton were reviewed in one study each, and significant improvement was observed for all three. All the included compounds have mild and infrequent adverse effects. SRs on β-sitosterol, Pygeum africannum and Cernilton have not been updated since 2000, thus an update of reviews on these compounds will be necessary in the future.
Link to Full Study
Randomized trial of a combination of natural products (cernitin, saw palmetto, B-sitosterol, vitamin E) on symptoms of benign prostatic hyperplasia (BPH). Because benign prostatic hyperplasia (BPH) is relatively common, it is important to discover safe and effective means to treat this often debilitating perturbation. Accordingly, we examined the effectiveness of a combination of natural products (cernitin, saw palmetto, B-sitosterol, vitamin E) in treating symptoms of BPH. We undertook a randomized, placebo-controlled, double-blind study. Patients were enrolled from 3 urological practices in the USA. 144 subjects were randomized for study. 17 subjects eventually withdrew, leaving 70 patients in the test group and 57 in the placebo group to complete the study. Inclusion criteria consisted of a diagnosis of BPH, no evidence of cancer, and a maximal urinary flow rate between 5 and 15 ml/second. Patients received either placebo or the combined natural products for 3 months. Evaluations were performed via the American Urological Association (AUA) Symptom Index score, urinary flow rate, PSA measurement, and residual bladder volume. Nocturia showed a markedly significant decrease in severity in patients receiving the combined natural products compared to those taking placebo (p < 0.001). Daytime frequency was also lessened significantly (p < 0.04). When the average individual total AUA Symptom Index score in the test group was compared to that in the placebo group at the end of the study, the difference proved highly significant (p < 0.014). PSA measurements, maximal and average urinary flow rates, and residual volumes showed no statistically significant differences. When taken for 3 months, a combination of natural products (cernitin, saw palmetto, B-sitosterol, vitamin E) compared to placebo can significantly lessen nocturia and frequency and diminish overall symptomatology of BPH as indicated by an improvement in the total AUA Symptom Index score. The combination of natural products caused no significant adverse side effects.
Effect of beta-sitosterol on transforming growth factor-beta-1 expression and translocation protein kinase C alpha in human prostate stromal cells in vitro. BACKGROUND: Today, plant extracts are widely used in the treatment of benign prostatic hyperplasia (BPH). However, the complete mode of action of the active substance, beta-sitosterol, is under investigation. The purpose of this study was to investigate the effect of beta-sitosterol on the expression of transforming growth factor beta 1 (TGF-beta1) and the activity of protein kinase C alpha (PKC-alpha) in primary prostate stromal cell cultures in vitro. METHODS: Tissue samples for primary cell cultures were obtained from patients undergoing transurethral resection of the prostate (TURP). TGF-beta1 levels in stromal cell conditioned media following a culture with beta-sitosterol were detected in a TGF-beta1 specific ELISA assay. Following different incubation periods with beta-sitosterol, cells were lysed and fractionated into a Triton-soluble membrane fraction and a cytosol fraction. PKC-alpha protein was detected using immunoblot analysis. RESULTS: Beta-sitosterol was able to induce the expression and secretion of TGF-beta1 significantly between 1.26- and 1.86-fold compared to a cholesterol and the nonsupplemented control in 6 of 8 individual cultures. The total amount of secreted TGF-beta1 varied in cells from different patients. Based on its presence in both membrane fraction and cytosol, PKC-alpha appeared to be constitutively expressed in stromal cells. In the absence of beta-sitosterol PKC-alpha was predominantly found in its membrane-associated active form. Following a culture with beta-sitosterol, a translocation of PKC-alpha from the membrane to the cytosol was observed. This effect was specific for beta-sitosterol as compared to cholesterol. CONCLUSION: This study describes the effect of beta-sitosterol on the expression of a multifunctional growth factor (TGF-beta1) and the activity of PKC-alpha membrane in stromal cells of the human prostate in vitro.
Chemical constituents of the root of Dystaenia takeshimana and their anti-inflammatory activity.. In our ongoing search for bioactive compounds originating from the endemic species in Korea, we found that the hexane and EtOAc fractions of the MeOH extract from the root of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin D2 (PGD2) and leukotriene C4 (LTC4) in mouse bone marrow-derived mast cells. By activity-guided fractionation, five coumarins, viz. psoralen (2), xanthotoxin (3), scopoletin (4), umbelliferone (5), and (+)-marmesin (6), together with beta-sitosterol (1), were isolated from the hexane fraction, and two phenethyl alcohol derivatives, viz. 2-methoxy-2-(4'-hydroxyphenyl)ethanol (7) and 2-hydroxy-2-(4'-hydroxyphenyl)ethanol (8), three flavonoids, viz. apigenin (9), luteolin (10), and cynaroside (11), as well as daucosterol (12) were isolated from the EtOAc fraction using silica gel column chromatography. In addition, D-mannitol (13) was isolated from the BuOH fraction by recrystallization. Two of the coumarins, scopoletin (4) and (+)-marmesin (6), the two phenethyl alcohol derivatives (7, 8) and the three flavonoids (9-11) were isolated for the first time from this plant. Among the compounds isolated from this plant, the five coumarins as well as the three flavonoids showed COX-2/5-LOX dual inhibitory activity. These results suggest that the anti-inflammatory activity of D. takeshimana might in part occur via the inhibition of the generation of eicosanoids.
Effect of resveratrol, tyrosol and beta-sitosterol on oxidised low-density lipoprotein-stimulated oxidative stress, arachidonic acid release and prostaglandin E2 synthesis by RAW 264.7 macrophages. Oxidation of LDL is hypothesised as an early and critical event in atherogenesis. Oxidised LDL (oxLDL) favour the transformation of macrophages into foam cells, an important cell involved in atherosclerosis. Furthermore, oxLDL cause multiple changes in macrophage functions. Thus, oxLDL induces certain genes, suppresses others and alters cell lipid metabolism. Consumption of a Mediterranean diet is associated with a low incidence of atherosclerotic disease, but data about the specific dietary constituents involved and mechanisms conferring cardioprotection are still sparse. The aim of the present study was to determine the effect of representative minor components of wine and olive oil on reactive oxygen species and eicosanoid synthesis induced by oxLDL-stimulated macrophages. We observed that exposure to non-toxic oxLDL concentrations leads to the production of H2O2 by RAW 264.7 macrophages and this effect was reverted by apocynin, a NADPH oxidase inhibitor. Moreover, oxLDL induced arachidonic acid (AA) release, cyclo-oxygenase-2 overexpression and subsequent PGE2 release. We observed that resveratrol and tyrosol revert H2O2 production induced by oxLDL as well as AA release and PGE2 synthesis and that these effects were not as a consequence of these compounds interfering with the oxLDL binding to their receptors. Interestingly, beta-sitosterol presence enhances these polyphenol actions. Thus, we found a synergistic action of polyphenols of olive oil and wine and beta-sitosterol of olive oil led to the modulation of the effects of oxLDL on oxidative stress and PGE2 synthesis.
Effect of resveratrol and beta-sitosterol in combination on reactive oxygen species and prostaglandin release by PC-3 cells.. The objective of this project was to identify some possible mechanisms by which two common phytochemicals, resveratrol and beta-sitosterol, inhibit the growth of human prostate cancer PC-3 cells. These mechanisms include the effect of the phytochemicals on apoptosis, cell cycle progression, prostaglandin synthesis and the production of reactive oxygen species (ROS). Prostaglandins have been known to play a role in regulating cell growth and apoptosis. PC-3 cells were supplemented with 50 microM resveratrol or 16 microM beta-sitosterol alone or in combination for up to 5 days. Phytochemical supplementation resulted in inhibition in cell growth. beta-Sitosterol was more potent than resveratrol and the combination of the two resulted in greater inhibition than supplementation with either alone. Long-term supplementation with resveratrol or beta-sitosterol elevated basal prostaglandin release but beta-sitosterol was much more potent than resveratrol in this regard. beta-Sitosterol was more effective than resveratrol in inducing apoptosis and the combination had an intermediate effect after 1 day of supplementation. Cells supplemented with resveratrol were arrested at the G1 phase and at the G2/M phase in the case of beta-sitosterol while the combination resulted in cell arrest at the two phases of the cell cycle. beta-Sitosterol increased ROS production while resveratrol decreased ROS production. The combination of the two phytochemicals resulted in an intermediate level of ROS. The observed changes in prostaglandin levels and ROS production by these two phytochemicals may suggest their mediation in the growth inhibition. The reduction in ROS level and increase by resveratrol supplementation in PC-3 cells reflects the antioxidant properties of resveratrol. It was concluded that these phytochemicals may induce the inhibition of tumor growth by stimulating apoptosis and arresting cells at different locations in the cell cycle and the mechanism may involve alterations in ROS and prostaglandin production.
Effect of olive oil minor components on oxidative stress and arachidonic acid mobilization and metabolism by macrophages RAW 264.7. Minor components of virgin olive oil may explain the healthy effects of the Mediterranean diet on the cardiovascular system and cancer development. The uncontrolled production of reactive oxygen species (ROS) and arachidonic acid (AA) metabolites contributes to the pathogenesis of cardiovascular disease and cancer, and inflammatory cells infiltrated in the atheroma plaque or tumor are a major source of ROS and eicosanoids. We aimed to determine the effects of squalene, beta-sitosterol, and tyrosol, which are representative of the hydrocarbons, sterols, and polyphenols of olive oil, respectively, on superoxide anion (O2(-)), hydrogen peroxide (H2O2), and nitric oxide (*NO) levels. We also studied AA release and eicosanoid production by phorbol esters (PMA)-stimulated macrophages RAW 264.7. beta-Sitosterol and tyrosol decreased the O2(-) and H2O2 production induced by PMA, and tyrosol scavenged the O2(-) released by a ROS generating system. These effects were correlated with the impairment of [3H]AA release, cyclooxygenase-2 (COX-2) expression, and prostaglandin E(2)/leukotriene B(4) synthesis in RAW 264.7 cultures stimulated by PMA. beta-Sitosterol exerted its effects after 3-6 h of preincubation. Tyrosol inhibited the [3H]AA release induced by exogenous ROS. beta-Sitosterol and tyrosol also reduced the *NO release induced by PMA, which was correlated with the impairment of inducible nitric oxide synthase (iNOS) levels. This may be correlated with the modulation of NF-kappaB activation. Further studies are required to gain more insight into the potential healthy effects of minor components of extra virgin olive oil.
Inhibitory effect of β-sitosterol on TNBS-induced colitis in mice. beta-Sitosterol, a common sterol in herbal medicines, exhibits anti-inflammatory effects beneficial in the treatment of lung inflammation, asthma, and bronchospasm. To evaluate whether β-sitosterol also has anticolitic benefits, we tested the effect of β-sitosterol on 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in mice. β-Sitosterol inhibited colon shortening and led to lowered macroscopic scores and myeloperoxidase activity in TNBS-treated colitic mice. β-Sitosterol also inhibited the expression of proinflammatory cytokines TNF-α, IL-1β, and IL-6, and an inflammatory enzyme, cyclooxygenase (COX)-2, in the colons of TNBS-induced colitic mice, as well as the activation of NF-κB. Based on these findings, β-sitosterol may ameliorate colitis by inhibiting the NF-κB pathway.


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