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      Critical Analysis on Characterization, Systemic Effect, and Therapeutic Potential of Beta-Sitosterol: A Plant-Derived Orphan Phytosterol

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          Abstract

          Beta-sitosterol (BS) is a phytosterol, widely distributed throughout the plant kingdom and known to be involved in the stabilization of cell membranes. To compile the sources, physical and chemical properties, spectral and chromatographic analytical methods, synthesis, systemic effects, pharmacokinetics, therapeutic potentials, toxicity, drug delivery and finally, to suggest future research with BS, classical as well as on-line literature were studied. Classical literature includes classical books on ethnomedicine and phytochemistry, and the electronic search included Pubmed, SciFinder, Scopus, the Web of Science, Google Scholar, and others. BS could be obtained from different plants, but the total biosynthetic pathway, as well as its exact physiological and structural function in plants, have not been fully understood. Different pharmacological effects have been studied, but most of the mechanisms of action have not been studied in detail. Clinical trials with BS have shown beneficial effects in different diseases, but long-term study results are not available. These have contributed to its current status as an “orphan phytosterol”. Therefore, extensive research regarding its effect at cellular and molecular level in humans as well as addressing the claims made by commercial manufacturers such as the cholesterol lowering ability, immunological activity etc. are highly recommended.

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          Phytosterols, phytostanols, and their conjugates in foods: structural diversity, quantitative analysis, and health-promoting uses.

          Phytosterols (plant sterols) are triterpenes that are important structural components of plant membranes, and free phytosterols serve to stabilize phospholipid bilayers in plant cell membranes just as cholesterol does in animal cell membranes. Most phytosterols contain 28 or 29 carbons and one or two carbon-carbon double bonds, typically one in the sterol nucleus and sometimes a second in the alkyl side chain. Phytostanols are a fully-saturated subgroup of phytosterols (contain no double bonds). Phytostanols occur in trace levels in many plant species and they occur in high levels in tissues of only in a few cereal species. Phytosterols can be converted to phytostanols by chemical hydrogenation. More than 200 different types of phytosterols have been reported in plant species. In addition to the free form, phytosterols occur as four types of "conjugates," in which the 3beta-OH group is esterified to a fatty acid or a hydroxycinnamic acid, or glycosylated with a hexose (usually glucose) or a 6-fatty-acyl hexose. The most popular methods for phytosterol analysis involve hydrolysis of the esters (and sometimes the glycosides) and capillary GLC of the total phytosterols, either in the free form or as TMS or acetylated derivatives. Several alternative methods have been reported for analysis of free phytosterols and intact phytosteryl conjugates. Phytosterols and phytostanols have received much attention in the last five years because of their cholesterol-lowering properties. Early phytosterol-enriched products contained free phytosterols and relatively large dosages were required to significantly lower serum cholesterol. In the last several years two spreads, one containing phytostanyl fatty-acid esters and the other phytosteryl fatty-acid esters, have been commercialized and were shown to significantly lower serum cholesterol at dosages of 1-3 g per day. The popularity of these products has caused the medical and biochemical community to focus much attention on phytosterols and consequently research activity on phytosterols has increased dramatically.
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            Plant-based foods and prevention of cardiovascular disease: an overview.

            Frank Hu (2003)
            Evidence from prospective cohort studies indicates that a high consumption of plant-based foods such as fruit and vegetables, nuts, and whole grains is associated with a significantly lower risk of coronary artery disease and stroke. The protective effects of these foods are probably mediated through multiple beneficial nutrients contained in these foods, including mono- and polyunsaturated fatty acids, n-3 fatty acids, antioxidant vitamins, minerals, phytochemicals, fiber, and plant protein. In dietary practice, healthy plant-based diets do not necessarily have to be low in fat. Instead, these diets should include unsaturated fats as the predominant form of dietary fat (eg, fats from natural liquid vegetable oils and nuts), whole grains as the main form of carbohydrate, an abundance of fruit and vegetables, and adequate n-3 fatty acids. Such diets, which also have many other health benefits, deserve more emphasis in dietary recommendations to prevent chronic diseases.
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              Antidiabetic and antioxidant potential of β-sitosterol in streptozotocin-induced experimental hyperglycemia.

              Oxidative stress, produced under diabetic conditions, may cause tissue damage. Although several drugs are currently available for the treatment of diabetes, their continued use may cause unwanted side effects. The aim of the present study was to evaluate the antioxidant potential of β-sitosterol (BS), a phytosterol from Solanum surattense, using an experimental model for diabetes-induced oxidative damage. The effects of 21 days treatment with BS (10, 15 and 20 mg/kg, p.o.) on blood, serum, and tissue biochemical parameters were evaluated in control and streptozotocin-induced diabetic rats. Nine experimental groups, including a control group, a diabetic group, and BS- and glibenclamide-treated diabetic groups, were evaluated. All three dose levels dose dependently resulted in decreases in glycated hemoglobin, serum glucose, and nitric oxide, with concomitant increases in serum insulin levels. Furthermore, treatment with BS doses also increased pancreatic antioxidant levels, with a concomitant decrease in thiobarbituric acid-reactive substances. β-Sitosterol has promising antidiabetic as well as antioxidant effects and may be considered in clinical studies for drug development. © 2011 Ruijin Hospital, Shanghai Jiaotong University School of Medicine and Blackwell Publishing Asia Pty Ltd.
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Medicines (Basel)
                Medicines (Basel)
                medicines
                Medicines
                MDPI
                2305-6320
                15 November 2016
                December 2016
                : 3
                : 4
                : 29
                Affiliations
                [1 ]Department of Clinical Pharmacy and Pharmacology, University of Dhaka, Dhaka-1000, Bangladesh
                [2 ]Department of Pharmacy, Daffodil International University, Dhaka-1207, Bangladesh; smroney46@ 123456gmail.com
                [3 ]Department of Pharmaceutical Chemistry, University of Dhaka, Dhaka-1000, Bangladesh; tasnuva.phr.du@ 123456gmail.com
                [4 ]Department of Biochemistry and Molecular, Biology, University of Dhaka, Dhaka-1000, Bangladesh; monzurmorshed.du@ 123456gmail.com
                Author notes
                [* ]Correspondence: shahdaat2013@ 123456du.ac.bd ; Tel.: +880-2966-4953 or +880-171-3459-747; Fax: +880-2966-4950
                Article
                medicines-03-00029
                10.3390/medicines3040029
                5456237
                28930139
                4b0bc12b-bf45-4598-a1ea-4b65698bbf6c
                © 2016 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 17 May 2016
                : 07 November 2016
                Categories
                Review

                beta-sitosterol,orphan phytosterol,characterization,therapeutic potential,drug delivery

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