Immunosuppressive properties of flavonoids isolated from Boerhaavia diffusa Linn.
ABSTRACT Plant extracts have been widely evaluated for possible immunomodulatory properties. We have earlier reported that ethanolic extract of Boerhaavia diffusa root, a plant used in Indian traditional medicine, has significant immunomodulatory potential. B. diffusa hexane, chloroform and ethanol extracts, and two pure compounds Bd-I (eupalitin-3-O-beta-D-galactopyranoside) and Bd-II (eupalitin) were evaluated in vitro for their effect on T cell mitogen (phytohemagglutinin; PHA) stimulated proliferation of human peripheral blood mononuclear cell (PBMC), mixed lymphocyte culture, lipopolysaccharide (LPS) stimulated nitric oxide production by RAW 264.7, PHA and LPS induced IL-2 and TNF-alpha production, in human PBMCs, superoxide production in neutrophils, human natural killer (NK) cell cytotoxicity and nuclear translocation of nuclear factor-(kappa)B and AP-1 in PHA stimulated PBMCs. The chloroform and ethanol extracts inhibited PHA stimulated proliferation of peripheral blood mononuclear cells, two-way MLR, NK cell cytotoxicity as well as LPS induced NO production by RAW 264.7; the hexane extract showed no activity. Bd-I purified from the ethanolic extract at equivalent dose, inhibited PHA-stimulated proliferation of peripheral blood mononuclear cells, two-way MLR and NK cell cytotoxicity as well as LPS induced NO production by RAW 264.7 equally or more effectively than the parent ethanolic extract. Bd-I inhibited production of PHA stimulated IL-2 at the protein and mRNA transcript levels and LPS stimulated TNF-alpha production in human PBMCs; it also blocked the activation of DNA binding of nuclear factor-(kappa)B and AP-1, two major transcription factors centrally involved in expression of the IL-2 and IL-2R gene, which are necessary for T cell activation and proliferation. Our results report selective immunosuppressive activity of B. diffusa leaf extracts and that this activity lies in eupalitin-3-O-beta-D-galactopyranoside (Bd-I) isolated and purified from the ethnaolic extract. Thus, Bd-I could be a candidate for development as an immunosuppressive agent.
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ABSTRACT: The present study is initially intended to evaluate antioxidant and β-hydroxy-β-methylglutaryl-CoA reductase (HMGR) inhibitory property of Ficus virens Ait., first by in vitro analyses followed by a corroboratory molecular informatics study. Our results show that of all the sequentially extracted fraction of F. virens bark and leaves extract, F. virens bark methanol extract exhibits strong radical scavenging, antioxidant and oxidative DNA damage protective activity, which is well correlated with its total phenolic content. In addition, F. virens bark methanol extract, which is non-cytotoxic, significantly and non-covalently inhibit the HMGR activity (IC50 = 3.45 ± 0.45 µg/ml) in comparison with other extracts. The mechanistic aspect of this inhibition activity is authenticated by molecular docking study of bioactive compounds as revealed from gas chromatography-mass spectrometry data, with HMGR. The analysis for the first time indicates that quinic acid (ΔG: -8.11 kcal/mol) and paravastatin (ΔG: -8.22 kcal/mol) exhibit almost same binding energy, while other compounds also showed good binding energy, suggesting that quinic acid alone or in combination with other major bioactive compound is probably responsible for HMGR inhibitory property of the extract and plausibly can be used in in vivo system for the management, prevention, and alleviation of hypercholesterolemia as well as hypercholesterolemia-induced oxidative stress. Copyright © 2013 John Wiley & Sons, Ltd.Phytotherapy Research 06/2014; 28(6). DOI:10.1002/ptr.5077 · 2.40 Impact Factor
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ABSTRACT: Boerhaavia diffusa Linn. has been shown to exhibit a wide range of medicinal properties for the treatment of diabetes, inflammation, stress, hepatotoxicity, jaundice and heart failure. The extraordinary antioxidant, hepatoprotective, antibiotic, antidiabetic and anticarcinogenic properties of B. diffusa have attracted pioneers in the field of science and medicine. Moreover, the therapeutic importance of this plant, which is due to presence of polyphenols and flavanoids, makes this plant medically more important to be exploited by clinicians and scientists to gain more insight into its biological and medicinal properties. The present review on B. diffusa focuses over the chemical compositions and its ethno-medicinal uses, linked from ancient times to the present with a scope of development in future. Furthermore, a recent update on mechanistic approaches of B. diffusa has also been discussed, which could be helpful for the researchers working in this field. Eventually, based on its antioxidant and antidiabetic characteristics, it is hypothesized that B. diffusa might exhibit antiglycating properties as well.
- 01/2011; LAP LAMBERT Academic Publishing (December 5, 2011)., ISBN: 978-3846517437