| Description: |
Fucosterol possesses anti-oxidant, hepatoprotective, cytotoxic, antihistaminic, anticholinergic and antiviral activities. Fucosterol exhibits anti-inflammatory activity which might attribute to inhibition of NO and ROS generation and suppression of the NF-κB pathway. Fucosterol also has anti-diabetic activity in vivo, it exhibits an inhibition of sorbitol accumulations in the lenses and causes an inhibition of blood glucose level and glycogen degradation. Fucosterol is a dual-LXR agonist that regulates the expression of key genes in cholesterol homeostasis in multiple cell lines without inducing hepatic triglyceride accumulation; it could as an anti-obesity agent, it can inhibit expression of PPARγ and C/EBPα, resulting in a decrease of lipid accumulation in 3T3-L1 pre-adipocytes.
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| In vitro: |
| Pharmacogn Mag. 2012 Jan;8(29):60-4. | | Cytotoxicity of fucosterol containing fraction of marine algae against breast and colon carcinoma cell line.[Pubmed: 22438665] | Marine algae produce different secondary metabolites with a wide range of biological activities. Many studies have been achieved on the screening of biological effects of marine organisms and a lot of active compounds were isolated and characterized.
In an attempt to find cytotoxic compound of hexane fraction, isolation, identification, and cytotoxicity of active compound of this fraction were performed.
METHODS AND RESULTS:
In this study, total methanolic (70%) extract and partition fractions of hexane, chloroform (CHCl(3)), ethyl acetate (EtOAc), and MeOH-H(2)O of Sargassum angustifolium, Chondria dasyphylla, and Ulva flexuosa, collected from coastlines of the Persian Gulf in south of Iran, were studied against colon carcinoma (HT-29), colorectal adenocarcinoma (Caco-2), breast ductal carcinoma (T47D), and Swiss mouse embryo fibroblast (NIH 3T3) cell lines by MTT assay.
IC(50) (median growth inhibitory concentration) values were calculated by Sigmaplot (10) software.
Hexane fraction of Chondria dasyphylla (IC(50) 82.26 ± 4.09 μg/ml) and MeOH-H(2)O fraction of Ulva flexuosa (IC(50) 116.92 ± 8.58 μg/ml) showed cytotoxic activity against proliferation of T47D cells. Hexane fraction of Sargassum angustifolium was also observed for cytotoxicity against T47D and HT-29 cell lines (IC(50) 166.42 ± 26.7 and 190.24 ± 52.8 μg/ml), respectively. An investigation of a component from the hexane fraction of Sargassum angustifolium yielded a steroidal metabolite, Fucosterol, with cytotoxicity in T47D and HT29 (IC(50) 27.94 ± 9.3 and 70.41 ± 7.5 μg/ml).
CONCLUSIONS:
These results indicated that Fucosterol, the most abundant phytosterol in brown algae, is responsible for cytotoxic effect of this extract against breast and colon carcinoma cell lines. | | Pharmacologyonline, 2009, 1(1):1104-1112. | | Antihistaminic, Anticholinergic and Antiviral activities of Fucosterol from Turbinaria conoides (J.Agardh) Kutzing[Reference: WebLink] | Fucosterol (Stigmasta-5,24(28)-dien-3-ol) was isolated from cyclohexane extract of Turbinaria conoides (J.Agardh) Kutzing. The structure was identified by comparing with the reported physical and spectral data of the compound.
METHODS AND RESULTS:
The antihistaminic and anticholinergic activities have been evaluated using in vitro standard animal models in comparison to chlorpheniramine maleate and pancuronium respectively. Evaluation of the potency (EC50), affinity (pA2) of the Fucosterol and the maximal response (Emax) to the Histamine and acetylcholine were determined in the absence and presence of Fucosterol. Antiviral activity and cytotoxicity were performed in human embryonic lung, human epithelial and Vero cells. Fucosterol showed antiviral activity against tested viruses with EC50 values ranging from >4 μg/mL to >20 μg/mL in the cells. Fucosterol inhibited histamine (97%) and acetylcholine (94%) induced contractions at 20 μg/mL, which were comparable to that of 10 μg/mL of chlorpheniramine maleate and pancuronium respectively.
CONCLUSIONS:
Thus Fucosterol springs up to be potent antihistaminic and anticholinergic compound. | | Arch Pharm Res. 2014 Jun;37(6):713-20. | | Anti-adipogenic activity of the edible brown alga Ecklonia stolonifera and its constituent fucosterol in 3T3-L1 adipocytes.[Pubmed: 24014306 ] | Fucosterol is a sterol metabolite of brown algae and regulates genes involved with cholesterol homeostasis. As a part of our continuous search for anti-obesity agents from natural marine sources, the anti-adipogenic activities of Ecklonia stolonifera and its sterol, Fucosterol, were evaluated for the inhibition of adipocyte differentiation and lipid formation.
METHODS AND RESULTS:
Oil Red O staining was used to evaluate triglyceride contents in 3T3-L1 pre-adipocytes primed by differentiation medium (DM) I and DM II. The methanolic extract of E. stolonifera showed strong anti-adipogenic activity, and was thus fractionated with several solvents. Among the tested fractions, the dichloromethane (CH2Cl2) fraction was found to be the most active fraction, with significant inhibition (40.5 %) of intracellular lipid accumulation at a non-toxic concentration, followed by the ethyl acetate fraction (30.2 %) at the same concentration, while the n-butanol and water fractions did not show inhibitory activity within the tested concentrations. The strong anti-adipogenic CH2Cl2-soluble fraction was further purified by a repeated chromatography to yield Fucosterol. Fucosterol reduced lipid contents in a concentration-dependent manner without showing any cytotoxicity. Fucosterol treatment also yielded a decrease in the expression of the adipocyte marker proteins peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα) in a concentration-dependent manner.
CONCLUSIONS:
Taken together, these results suggest that Fucosterol inhibits expression of PPARγ and C/EBPα, resulting in a decrease of lipid accumulation in 3T3-L1 pre-adipocytes, indicating that the potential use of E. stolonifera and its bioactive Fucosterol as an anti-obesity agent. |
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