Immunosuppressive properties of flavonoids isolated from Boerhaavia diffusa Linn

Department of Immunology, Sanjay Gandhi Post-Graduate Institute of Medical Sciences, Lucknow 226 014, India.
International Immunopharmacology (Impact Factor: 2.47). 04/2005; 5(3):541-53. DOI: 10.1016/j.intimp.2004.11.001
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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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    • "It decreased the production of IL-2 and TNF-α in human PBMCs and repressed NF-κB and AP-1, thereby depressing activation and proliferation of T cells. The author suggested specific potential of eupalitin-3-O-β-D-galactopyranoside for immunosuppression [14]. "
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    ABSTRACT: Unlabelled: Boerhavia diffusa (BD) is a plant of rasayana category as per ayurvedic claims. It is reported to possess antiaging, disease prevention, and life strengthening activities which hold enormous influence in disease burden and affordability/availability of healthcare in the world. Objective. This paper has been compiled to comment on the studies reported for BD to highlight its chemical and therapeutic potential along with its ethnopharmacological considerations. Methods: In the present paper, a detailed account of chemical constituents and pharmacological activities has been presented. All the findings were correlated with modern pharmacological activities to appraise the value of BD. Results: Chemical analysis of BD gives a wide variety of chemical constituents, namely, rotenoids, flavonoids, xanthones, purine nucleoside, lignans, and steroids. Various ethnopharmacological reports emphasize its role in disorders of reproductive system, gastrointestinal system, respiratory system, urinary system, hepatic system/jaundice, cardiovascular system, and cancer. Conclusions: The studies on the therapeutic activities of BD range from studies on crude extracts to isolated compounds; however some of the studies require sophistication and validated results. BD is a plant of enormous importance in the purview of its chemical and therapeutic properties.
    BioMed Research International 05/2014; 2014(5):808302. DOI:10.1155/2014/808302 · 3.17 Impact Factor
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    • "Ursolic acid is reported to possess cardioprotective potential via inducing uncoupling of mitochondrial oxidative phosphorylation and reducing mitochondrial H2O2 production [60]. Eupalitin-3-O-â-D-galactopyranoside is reported to possess immunosuppressive properties and it inhibits the nuclear translocation of NF-êB [61]. Kaempferol is also reported to possess cardioprotective potential and boeravinone G is another antioxidant and genoprotective compound in B.diffusa [62], [63]. "
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    ABSTRACT: Mitochondrial dysfunction plays a critical role in the development of cardiac hypertrophy and heart failure. So mitochondria are emerging as one of the important druggable targets in the management of cardiac hypertrophy and other associated complications. In the present study, effects of ethanolic extract of Boerhaavia diffusa (BDE), a green leafy vegetable against mitochondrial dysfunction in angiotensin II (Ang II) induced hypertrophy in H9c2 cardiomyoblasts was evaluated. H9c2 cells challenged with Ang II exhibited pathological hypertrophic responses and mitochondrial dysfunction which was evident from increment in cell volume (49.09±1.13%), protein content (55.17±1.19%), LDH leakage (58.74±1.87%), increased intracellular ROS production (26.25±0.91%), mitochondrial superoxide generation (65.06±2.27%), alteration in mitochondrial transmembrane potential (ΔΨm), opening of mitochondrial permeability transition pore (mPTP) and mitochondrial swelling. In addition, activities of mitochondrial respiratory chain complexes (I-IV), aconitase, NADPH oxidase, thioredoxin reductase, oxygen consumption rate and calcium homeostasis were evaluated. Treatment with BDE significantly prevented the generation of intracellular ROS and mitochondrial superoxide radicals and protected the mitochondria by preventing dissipation of ΔΨm, opening of mPTP, mitochondrial swelling and enhanced the activities of respiratory chain complexes and oxygen consumption rate in H9c2 cells. Activities of aconitase and thioredoxin reductase which was lowered (33.77±0.68% & 45.81±0.71% respectively) due to hypertrophy, were increased in BDE treated cells (P≤0.05). Moreover, BDE also reduced the intracellular calcium overload in Ang II treated cells. Overall results revealed the protective effects of B. diffusa against mitochondrial dysfunction in hypertrophy in H9c2 cells and the present findings may shed new light on the therapeutic potential of B. diffusa in addition to its nutraceutical potentials.
    PLoS ONE 04/2014; 9(4):e96220. DOI:10.1371/journal.pone.0096220 · 3.23 Impact Factor
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    • "Pharmacological studies have demonstrated that B. diffusa known to possess anticonvulsant [4] , diuretic, anti-inflammatory, antifibrinolytic [9] , antibacterial [10] , anti-hepatotoxic, anthelmintic, febrifuge, anti-leprosy, antiasthmatic, antiurethritis, antilymphoproliferative [11] , antimetastatic [12] , immunosuppressive [13] , antidiabetic, antioxidant [14] , immune-modulation [15] , hepatoprotective [16] , anti-nociceptive, nephroprotective [17] , bacteria induced ulcer & diarrhea [18] and antiurolithiatic [19] activities. "
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    ABSTRACT: To investigate the bioactivities of crude n-hexane, ethyl acetate and methanol extracts of aerial part of Boerhavia diffusa Linn. (B. diffusa) and its phytochemical analysis. The identification of phytoconstituents and assay of antioxidant, thrombolytic, cytotoxic, antimicrobial activities were conducted using specific standard in vitro procedures. The results showed that the plant extracts were a rich source of phytoconstituents. Methanol extract showed higher antioxidant, thrombolytic activity and less cytotoxic activity than those of n-hexane and ethyl acetate extracts of B. diffusa. Among the bioactivities, antioxidant activity was the most notable compared to the positive control and thus could be a potential rich source of natural antioxidant. In case of antimicrobial screening, crude extracts of the plant showed remarkable antibacterial activity against tested microorganisms. All the extracts showed significant inhibitory activity against Candida albicuns, at a concentration of 1000 µg/disc. The present findings suggest that, the plant widely available in Bangladesh, could be a prominent source of medicinally important natural compounds.
    Asian Pacific Journal of Tropical Biomedicine 09/2012; 2(9):673-8. DOI:10.1016/S2221-1691(12)60208-1
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