Ginseng contains three active components: ginsenosides, gintonin, and polysaccharides. After the separation of 1 of the 3 ingredient fractions, other fractions are usually discarded as waste. In this ...study, we developed a simple and effective method, called the ginpolin protocol, to separate gintonin-enriched fraction (GEF), ginseng polysaccharide fraction (GPF), and crude ginseng saponin fraction (cGSF).
Dried ginseng (1 kg) was extracted using 70% ethanol (EtOH). The extract was water fractionated to obtain a water-insoluble precipitate (GEF). The upper layer after GEF separation was precipitated with 80% EtOH for GPF preparation, and the remaining upper layer was vacuum dried to obtain cGSF.
The yields of GEF, GPF, and cGSF were 14.8, 54.2, and 185.3 g, respectively, from 333 g EtOH extract. We quantified the active ingredients of 3 fractions: L-arginine, galacturonic acid, ginsenosides, glucuronic acid, lysophosphatidic acid (LPA), phosphatidic acid (PA), and polyphenols. The order of the LPA, PA, and polyphenol content was GEF > cGSF > GPF. The order of L-arginine and galacturonic acid was GPF >> GEF = cGSF. Interestingly, GEF contained a high amount of ginsenoside Rb1, whereas cGSF contained more ginsenoside Rg1. GEF and cGSF, but not GPF, induced intracellular Ca2+i transient with antiplatelet activity. The order of antioxidant activity was GPF > GEF = cGSF. Immunological activities (related to nitric oxide production, phagocytosis, and IL-6 and TNF-α release) were, in order, GPF > GEF = cGSF. The neuroprotective ability (against reactive oxygen species) order was GEF > cGSP > GPF.
We developed a novel ginpolin protocol to isolate 3 fractions in batches and determined that each fraction has distinct biological effects.
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Cardiovascular diseases prevail among modern societies and underdeveloped countries, and a high mortality rate has also been reported by the World Health Organization affecting millions of people ...worldwide. Hyperactive platelets are the major culprits in thrombotic disorders. A group of drugs is available to deal with such platelet-related disorders; however, sometimes, side effects and complications caused by these drugs outweigh their benefits. Ginseng and its nutraceuticals have been reported to reduce the impact of thrombotic conditions and improve cardiovascular health by antiplatelet mechanisms. This review provides (1) a comprehensive insight into the available pharmacological options from ginseng and ginsenosides (saponin and nonsaponin fractions) for platelet-originated cardiovascular disorders; (2) a discussion on the impact of specific functional groups on the modulation of platelet functions and how structural modifications among ginsenosides affect platelet activation, which may further provide a basis for drug design, optimization, and the development of ginsenoside scaffolds as pharmacological antiplatelet agents; (3) an insight into the synergistic effects of ginsenosides on platelet functions; and (4) a perspective on future research and the development of ginseng and ginsenosides as super nutraceuticals.
Cardiovascular diseases are a rapidly growing epidemic with high morbidity and mortality. There is an urgent need to develop nutraceutical-based therapy with minimum side effects to reduce ...cardiovascular risk. Panax ginseng occupies a prominent status in herbal medicine for its various therapeutic effects against inflammation, allergy, diabetes, cardiovascular diseases, and even cancer, with positive, beneficial, and restorative effects. The active components found in most P. ginseng varieties are known to include ginsenosides, polysaccharides, peptides, alkaloids, polyacetylene, and phenolic compounds, which are considered to be the main pharmacologically active constituents in ginseng. P. ginseng is an adaptogen. That is, it supports living organisms to maintain optimal homeostasis by exerting effects that counteract physiological changes caused by physical, chemical, or biological stressors. P. ginseng possesses immunomodulatory (including both immunostimulatory and immunosuppressive), neuromodulatory, and cardioprotective effects; suppresses anxiety; and balances vascular tone. P. ginseng has an antihypertensive effect that has been explained by its vasorelaxant action, and paradoxically, it is also known to increase blood pressure by vasoconstriction and help maintain cardiovascular health. Here, we discuss the potential adaptogenic effects of P. ginseng on the cardiovascular system and outline a future research perspective in this area.
Inflammation is a natural host defensive process that is largely regulated by macrophages during the innate immune response. Mitogen-activated protein kinases (MAPKs) are proline-directed serine and ...threonine protein kinases that regulate many physiological and pathophysiological cell responses. p38 MAPKs are key MAPKs involved in the production of inflammatory mediators, including tumor necrosis factor-α (TNF-α) and cyclooxygenase-2 (COX-2). p38 MAPK signaling plays an essential role in regulating cellular processes, especially inflammation. In this paper, we summarize the characteristics of p38 signaling in macrophage-mediated inflammation. In addition, we discuss the potential of using inhibitors targeting p38 expression in macrophages to treat inflammatory diseases.
BAY 11-7082 (BAY) is an inhibitor of κB kinase (IKK) that has pharmacological activities that include anticancer, neuroprotective, and anti-inflammatory effects. In this study, BAY-pharmacological ...target pathways were further characterized to determine how this compound simultaneously suppresses various responses. Primary and cancerous (RAW264.7 cells) macrophages were activated by lipopolysaccharide, a ligand of toll-like receptor 4. As reported previously, BAY strongly suppressed the production of nitric oxide, prostaglandin E2, and tumor necrosis factor-α and reduced the translocation of p65, major subunit of nuclear factor-κB, and its upstream signaling events such as phosphorylation of IκBα, IKK, and Akt. In addition, BAY also suppressed the translocation and activation of activator protein-1, interferon regulatory factor-3, and signal transducer and activator of transcription-1 by inhibiting the phosphorylation or activation of extracellular signal-related kinase, p38, TANK-binding protein, and Janus kinase-2. These data strongly suggest that BAY is an inhibitor with multiple targets and could serve as a lead compound in developing strong anti-inflammatory drugs with multiple targets in inflammatory responses.
It has been reported that red ginseng acidic polysaccharide (RGAP), isolated from Korean red ginseng, displays immunostimulatory and anti-tumor activities. In a follow-up study, we have carried out a ...study on the anti-hyperlipidemic effects of RGAP using hyperlipidemic rats acutely induced by Triton WR1339 or corn oil intravenously injected. Oral administration of RGAP (100 to 1000 mg/kg) dose-dependently reduced the serum levels of triglyceride (TG) up-regulated by Triton WR1339, an inducer of endogenous model hyperlipidemia. Moreover, RGAP treatment was shown to significantly decrease the levels of non-esterified fatty acid (NEFA) concomitant with TG reduction. However, such reduction effects were not observed in cases of total cholesterol (TC) and phospholipid levels increased under the same conditions, although there was an inhibitory tendency. Similar suppressive patterns were also seen in hepatic parameters (total lipids and TG) under the same conditions. The exogenous hyperlipidemic rat condition triggered by corn oil also supported the anti-hyperlipidemic activity of RGAP in serum and hepatic parameters of TG and NEFA. Interestingly, RGAP significantly enhanced the serum activity of lipoprotein lipase, a key hydrolytic enzyme of lipid molecules in lipoprotein, in a dose-dependent manner up to 80%, implying potential involvement of this enzyme in lowering TG and NEFA by RGAP. Therefore, our data suggest that RGAP may play an additional role in reducing hyperlipidemic conditions, which can be used as a valuable neutraceutical application for the treatment of hyperlipidemia.
Ginseng is a vastly used herbal supplement in Southeast Asian countries. Red ginseng extract enriched with Rg3 (Rg3-RGE) is a formula that has been extensively studied owing to its various biological ...properties.
(PT), belonging to the
family, has also been reported for its anti-inflammatory properties. Ulcerative colitis (UC) is inflammation of the large intestine, particularly in the colon. This disease is increasingly common and has high probability of relapse. We investigated, separately and in combination, the effects of Rg3-RGE and PT using murine exemplary of UC induced by DSS (Dextran Sulfate Sodium). For in vitro and in vivo experiments, nitric oxide assay, qRT-Polymerase Chain Reaction (PCR), Western blot, ulcerative colitis introduced by DSS, Enzyme Linked Immunosorbent Assay (ELISA), and flow cytometry analysis were performed. The results obtained demonstrate that treatment with Rg3-RGE + PT showed synergism to suppress inflammation (in vitro) in RAW 264.7 cells via mitogen-activated protein kinase and nuclear factor κB pathways. Moreover, in C57BL/6 mice, this mixture exhibits strong anti-inflammatory effects in restoring colon length, histopathological damage, pro-inflammatory mediators, and cytokines amount, and decreasing levels of
inflammasome (in vivo). Our results recommend that this mixture can be used for the prevention of UC as a prophylactic/therapeutic supplement.
Dieckol is a phlorotannin that can be found in seaweeds, particularly in Eisenia bicyclis (brown algae) and is known to have anti-oxidant, anti-inflammatory, and anti-microbial properties. It also ...possesses anti-thrombotic and pro-fibrinolytic activities; however, the mechanistic aspects of anti-platelet and anti-thrombotic activity are yet to be explored.
We investigated the pharmacological effects of dieckol on the modulation of platelet functions using human, rat, and mice models. Inhibitory effects of dieckol on platelet aggregation were assessed using platelet-rich plasma and washed platelets, followed by measurement of dense granule secretions, fibrinogen binding to integrin αIIbβ3, fibronectin adhesion assay, platelet spreading on immobilized fibrinogen, and clot retraction. Cyclic nucleotide signaling events were evaluated, such as cyclic-AMP production followed by vasodilator-stimulated phosphoprotein (VASP) stimulation. The in vivo anti-thrombotic potential was evaluated in mice using an acute pulmonary thromboembolism model and tail bleeding assay.
Dieckol markedly inhibited platelet aggregation and granule secretion; furthermore, it down-regulated integrin αIIbβ3–mediated inside-out and outside-in signaling events, including platelet adhesion, spreading, and clot retraction, whereas it upregulated the cAMP–PKA–VASP pathway. Dieckol-treated mice significantly survived the thrombosis than vehicle treated mice, without affecting hemostasis. Histological examinations of lungs revealed minimum occluded vasculature in dieckol-treated mice.
Dieckol possesses strong anti-platelet and anti-thrombotic properties and is a potential therapeutic drug candidate to treat and prevent platelet-related cardiovascular disorders.
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•Impaired hemostasis is a common complication of anti-platelet drugs while dealing with thrombotic events.•Surface integrins especially αIIbβ3 play critical role in modulation of platelet functions and thormbus formation.•Dieckol inhibits platelet thrombus formation without affecting hemostasis by regulating integrin αIIbβ3 and cAMP signaling.•Dieckol can be a potential candidate to treat and prevent platelet-related cardiovascular disorders.
•Differential identification of Anaplasma spp. in 1219 South Korean cattle by PCR and RFLP.•Anaplasma bovis and A. capra were detected in 1.0% and 0.4% using 16S rRNA and multilocus genes.•This study ...suggests the potential of cattle to serve as reservoirs of A. capra.•The occurrence of a new emerging A. capra strain with public health and veterinary significance in Korean cattle.
Bovine anaplasmosis is a tick-borne, infectious, non-contagious disease caused by Anaplasma marginale, A. centrale, A. bovis, and zoonotic A. phagocytophilum. Recently, Anaplasma capra detected in goats was identified as a novel zoonotic pathogen. To determine whether A. capra can infect bovines, we used PCR to differentially diagnose Anaplasma spp. in 1219 South Korean cattle by performing multilocus gene typing and restriction fragment length polymorphism (RFLP). Nucleotide sequencing and phylogenetic analysis detected the 16S rRNA gene of A. bovis and four genes from A. capra in 12 (1.0%) and five (0.4%) cattle, respectively. Supplementary discrimination between A. bovis and A. capra was accomplished by RFLP. The 16S rRNA, msp4, groEL, and gltA genes of A. capra identified in this study had much lower degrees of identity to those in A. centrale and other Anaplasma spp. A. phagocytophilum was not detected in any of the tested cattle. Although the prevalence was low, this study suggests the potential of cattle to serve as reservoirs of A. capra. Thus, further studies are needed to clarify the pathogenesis of A. capra in cattle and its possible involvement in transmission to humans.
The purpose of this study was to assess tick-borne pathogenic infections in 42 wild Korean water deer (KWD) and 26 farmed elk in the Gyeongbuk and Gangwon Provinces of Korea. Among the 42 wild KWD ...tested, the eighteen (42.9%) and five (11.9%) samples tested positive for Anaplasma phagocytophilum and A. bovis, respectively, by PCR and DNA sequencing. All positive samples were only from wild KWD. All samples were negative for other tick-borne pathogens tested. Detected 16S rRNA sequences of A. phagocytophilum and A. bovis showed 98.6–99.8% and 94.4–100% identity to those of sequences in GenBank, respectively. Because few studies have examined tick-borne pathogens in wild animals, appropriate control programs and studies are needed to prevent pathogen transmission.