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ABSTRACT: In this study the potent scavenging activity of "Lycopi Herba" (LH) extract was studied using the following: evaluation of the total phenolics, measuring the antioxidant activity by Trolox equivalent antioxidant concentration, measuring the scavenging effects on reactive oxygen species, on reactive nitrogen species, and measuring the inhibitory effect on Cu(2+) induced human low-density lipoprotein oxidation in vitro. The ethyl acetate fraction from the LH extracts were found to have a potent scavenging activity against all of the reactive species tested, as well as an inhibitory effect on LDL oxidation. Therefore, we isolated and identified luteolin-7-O-beta-D-glucuronide methyl ester as the major compound from the ethyl acetate fraction of LH and their antioxidant activities were evaluated.
Journal of Enzyme Inhibition and Medicinal Chemistry 10/2010; 25(5):702-7. · 1.62 Impact Factor
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ABSTRACT: The antioxidant activity of extracts from Caesalpinia sappan L. (CSL) was studied in vitro by evaluating the total phenolics, measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) and on reactive nitrogen species (RNS), and measuring the inhibitory effect on Cu(2+)-induced human low-density lipoprotein (LDL) oxidation. The CSL extracts were found to have a potent scavenging activity against all of the reactive species tested, as well as an inhibitory effect on LDL oxidation, especially in the ethyl acetate (EA) fraction. Therefore, we isolated and identified benzylchroman derivatives sappanchalcone (1) and 3'-deoxy-4-O-methylepisappanol (2) from the EA fraction of CSL and their antioxidant activities were evaluated. The studied CSL extracts and the compounds 1 and 2 were revealed to be very effective against the evaluated pro-oxidant species, including ROS and RNS.
Journal of Enzyme Inhibition and Medicinal Chemistry 10/2010; 25(5):608-14. · 1.62 Impact Factor
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ABSTRACT: We observed that an aqueous extract of this medicinal plant exhibited significant neuroprotection against glutamate-induced toxicity in primary cultured rat cortical cells from methanol extracts of the seeds of P. tobira. To further clarify the underlying neuroprotective mechanism(s) of this observed effect, we isolated and identified various active fractions and components. By using such fractionation procedures, four known carotenoids compounds--tobiraxanthins A1, A2, A3, and B--were isolated from the n-hexane fraction of methanol extracts from the seeds of P. tobira. Among these four compounds, tobiraxanthins B exhibited significant neuroprotective activity against glutamate-induced neurotoxicity, as indicated by a cell viability of approximately 50%, at concentrations ranging from 0.1 microM to 10 microM. These findings indicate that, the neuroprotective effects of P. tobira might be due to the inhibition of glutamate-induced toxicity by carotenoids present in the plant.
Phytotherapy Research 04/2010; 24(4):625-8. · 2.09 Impact Factor
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ABSTRACT: Oxidative stress and inflammatory mediators were measured in the plasma and livers of C57BL/6 mice fed a high-cholesterol diet for 14 weeks and in cultured human umbilical vein endothelial cells (HUVECs). Some of the mice fed with the atherogenic diet received drinking water supplemented with 0.01 g of a 70% ethanol extract of Caesalpinia sappan L. (CSLE) per 20 g of body weight. Numerous parameters were determined: concentrations of total, high-, and low-density cholesterol; atherogenic index; plasma trolox equivalent antioxidant capacity (TEAC); levels of hepatic thiobarbituric acid reactive substances (TBARS) and protein carbonyls; and the activities of hepatic antioxidant enzymes, including Cu·Zn-SOD, Mn-SOD, glutathione peroxidase, glutathione reductase, and catalase. HUVECs were stimulated with tumor necrosis factor α (TNFα) and the expression of intracellular reactive oxygen species (ROS), lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1), adhesion molecules, inhibitory κBα (IκBα), and nuclear factor κB (NFκB) were measured. Compared to mice fed a hypercholesterolemic diet alone, mice fed a hypercholesterolemic diet supplemented with CSLE exhibited decreased total plasma cholesterol and increased high-density lipoprotein cholesterol, and thus a lower atherogenic index. Furthermore, plasma TEAC and levels of hepatic TBARS and protein carbonyls were significantly decreased in CSLE-supplemented mice (P < 0.05), whereas all hepatic antioxidative indicators were significantly elevated (P < 0.05). In HUVECs stimulated with TNFα, CSLE significantly decreased the expression of intracellular ROS, LOX-1, and adhesion molecules; the degradation of IκBα; and the nuclear translocation of NFκB; in contrast, CSLE induced the expression of Nrf2 and HO-1 (P < 0.05 for all results).
Immunopharmacology and Immunotoxicology 03/2010; 32(4):671-9. · 1.83 Impact Factor
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ABSTRACT: The proliferation of vascular smooth muscle cells (VSMCs) plays a key role in the development of atherosclerosis. Abnormal VSMC proliferation induces vascular dysfunction and several other pathological processes. The present study investigated the apoptotic effects of genistein on tumor necrosis factor-alpha (TNF-alpha)-induced proliferation in human aortic smooth muscle cells (HASMCs). The apoptotic effects of genistein were assessed to determine the mechanism(s) of its antiproliferative activity, including MTT, LDH assay, morphological change of cell, DNA fragmentation, and expression levels of pro- or anti-apoptotic molecules by RT-PCR and Western blots. The results show that genistein significantly reduced cell proliferation in TNF-alpha-induced HASMCs. Genistein also reduced intracellular nuclei staining with DAPI in a dose-dependent manner. In addition, genistein increased nucleosomal DNA fragmentation, increased the expression levels of Bax and c-Myc, and decreased the expression levels of Bcl-2 and Bcl-xL in TNF-alpha-induced HASMCs. Taken together, these findings indicate that genistein regulates the activation of apoptosis-related molecules in TNF-alpha-induced HASMCs, leading to the suppression of proliferation and induction of apoptosis.
Journal of Agricultural and Food Chemistry 02/2010; 58(3):2015-9. · 2.82 Impact Factor
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ABSTRACT: In Leonurus sibiricus herb extract (LHE)-supplemented animals, plasma cholesterol decreased and high-density lipoprotein-cholesterol increased, resulting in a lowered atherogenic index. The plasma trolox equivalent antioxidant capacity, levels of hepatic thiobarbituric acid-reactive substances, and protein carbonyl values decreased significantly in LHE-supplemented mice (p<0.05), whereas the hepatic antioxidant indicators were all significantly elevated (p<0.05). In human umbilical vein endothelial cells stimulated with tumor necrosis factor alpha, LHE significantly suppressed intracellular reactive oxygen species, LOX-1, and adhesion molecules. LHE supplementation may modulate the lipoprotein composition and attenuate oxidative stress by elevated antioxidant processes, thus suppressing the activation of inflammatory mediators. This is a possible mechanism of the anti-atherogenic effect.
Bioscience Biotechnology and Biochemistry 02/2010; 74(2):279-84. · 1.28 Impact Factor
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ABSTRACT: In this study, the anti-oxidative activities of 70% ethanol extract from Curcuma aromatica Salisb. (CAS) and curcumin (CUR) were studied. The CAS extracts and CUR were both found to have a potent scavenging activity against the reactive species tested, as well as an inhibitory effect on LDL oxidation. Cultured human umbilical vein endothelial cells (HUVECs) were stimulated with tumour necrosis factor alpha (TNFalpha), expression of intracellular reactive oxygen species (ROS), nitric oxide (NO), endothelial nitric oxide synthase (eNOS), lectin-like oxidised LDL receptor-1 (LOX-1), adhesion molecules, inhibitory kappa Balpha (IkappaBalpha) and nuclear factor kappa B (NFkappaB) were measured. In HUVECs stimulated with TNFalpha, CUR significantly suppressed expression of the intracellular ROS, LOX-1 and adhesion molecules, degradation of IkappaBalpha and translocation of NFkappaB, while inducing production of NO by phosphorylation of eNOS (p <0.05). In conclusion, CAS and CUR may modulate lipoprotein composition and attenuate oxidative stress by elevated antioxidant processes.
Journal of Enzyme Inhibition and Medicinal Chemistry 02/2010; 25(5):720-9. · 1.62 Impact Factor
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ABSTRACT: Inflammation plays a critical role in the development of atherosclerosis and TNF-alpha, a major inflammatory cytokine, induces inflammatory responses by enhancing the expression of adhesion molecules and the secretion of inflammatory mediators. Indirubin is an active compound of Polygonum tinctorium Lour (P. tinctorium) that has the ability to suppress inflammation. Previously, we described the novel indirubin derivative, 5'-nitro-indirubinoxime (5'-NIO), and demonstrated that it has potent anti-proliferative activity against various human cancer cells. In this study, we examined the effect of 5'-NIO on the TNF-alpha induced inflammatory conditions of human umbilical vein endothelial cells (HUVECs). We found that 5'-NIO inhibited TNF-alpha induced MCP-1 and IL-8 expression at the RNA and protein levels in HUVECs. Specifically, 5'-NIO significantly inhibited the TNF-alpha stimulated release of MCP-1 and IL-8, with levels that were only 19.8% and 30.9% of those of untreated control cells, respectively. Furthermore, 5'-NIO largely inhibited the adhesion of U937 cells to HUVECs by decreasing the expression level of ICAM-1 and VCAM-1. Overall, these observations suggest that 5'-NIO has the potential for use as an anti-atherosclerotic agent.
Atherosclerosis 02/2010; 211(1):77-83. · 3.79 Impact Factor
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ABSTRACT: Essential oil obtained from the leaves of Pittosporum tobira was extracted and its chemical composition and larvicidal effects were studied. Analyses were conducted by gas chromatography and mass spectroscopy (GC-MS) to determine the primary constituents of the essential oil of P. tobira. The yield of P. tobira essential oil (PTEO) was 0.1%, and GC-MS analysis identified its major constituents as undecane (31.11%), 4-methyl-1,3-pentadiene (11.34%), (1,3-dimethyl-2-butenyl)benzene (5.45%), and L-limonene (14.08%). The essential oil had a significant toxic effect against early fourth-stage larvae of Aedes aegypti (L.), with an LC(50) value of 58.92 ppm and an LC(90) value of 111.31 ppm. Finally, the LC(50) and LC(90) values of L-limonene were 39.7 ppm and 78.11 ppm. These results could be useful for seeking newer, safer, and more effective natural larvicidal agents against A. aegypti.
Journal of Enzyme Inhibition and Medicinal Chemistry 10/2009; 25(3):391-3. · 1.62 Impact Factor
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ABSTRACT: In Korea, Dendropanax morbifera Leveille (Araliaceae) is commonly used in traditional medicines for various diseases. We evaluated the hypolipidemic activity of D. morbifera essential oil (DMEO) in male Wistar rats (weight, 160 +/- 15 g) maintained on a high-cholesterol diet. DMEO was extracted by hydrodistillation and analyzed using gas chromatography/mass spectroscopy (GC/MS). The DMEO yield was 3.5%, and GC/MS analysis revealed that its major constituents were gamma-elemene (18.59%), tetramethyltricyclo hydrocarbons (10.82%), beta-zingiberene (10.52%), and beta-selinene (10.41%). Rats were orally administered DMEO at doses of 50, 100, and 200 mg kg(-1) d(-1) for 2 weeks. DMEO significantly and dose-dependently reduced the total cholesterol, triglyceride, and low-density lipoprotein cholesterol levels and significantly increased the high-density lipoprotein cholesterol levels. We conclude that D. morbifera has significant lipid-lowering effects and is a promising agent that should be considered in studies seeking new, safe, and effective natural cardioprotective agents.
Pharmazie 08/2009; 64(8):547-9. · 1.01 Impact Factor
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ABSTRACT: The whole plants of Carpesium divaricatum are used in traditional medicine as an antipyretic, analgesic and vermifugic, including a topical application for sores and inflammation. In a previous paper, the isolation and structural elucidation of isolated ineupatorolides A from methanol extracts of C. rosulatum (Compositae) were reported. The present paper deals with the isolation and identification of antiplasmodial compounds from C. divaricatum in Carpesium spp. Five compounds, 1 beta,6 alpha-dihydroxy-4(15)-eudesmene [1], beta-dictyopterol [2], 2-isopropenyl-6-acetyl-8-methoxy-1,3-benzodioxin-4-one [3], (3E,6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyl-3,6,10,14,18,22-tetracosahexaen-2-ol [4] and neophytadiene [5], were isolated from the whole plants of C. divaricatum. The in vitro activity against P. falciparum strain D10 was assessed using the parasite lactate dehydrogenase assay method. The main antiplasmodial principle, 2-isopropenyl-6-acetyl-8-methoxy-1,3-benzodioxin-4-one [3], has been isolated from C. divaricatum for the first time. Compound 3 exhibited an antiplasmodial activity with IC(50) values of 2.3 +/- 0.3 microm. This is the first report on the antiplasmodial activity of the compounds from C. divaricatum.
Phytotherapy Research 05/2009; 24(3):451-3. · 2.09 Impact Factor
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ABSTRACT: Diabetes is one of the major risk factors for cataract. Aldose reductase has been reported to play an important role in sugar-induced cataract. In this study, we conducted pharmacological investigations upon experimental rat lenses using extracts of the fruits of Litchi chinensis (Sapindaceae). Of the extracts and organic fractions of L. chinensis tested, a MeOH extract and an EtOAc fraction were found to be potent inhibitors of rat lens aldose reductase (RLAR) in vitro--their IC(50) values being 3.6 and 0.3 microg/mL, respectively. From the active EtOAc fraction, four minor compounds with diverse structural moieties were isolated and identified as D-mannitol (1), 2,5-dihydroxybenzoic acid (2), delphinidin 3-O-beta-galactopyranoside-39,59-di-O-beta-glucopyranoside (3), and delphinidin 3-O-beta- galactopyranoside-39-O-beta-glucopyranoside (4). Among these, 4 was found to be the most potent RLAR inhibitor (IC(50) = 0.23 microg/mL), and may be useful in the prevention and/or treatment of diabetic complications.
Journal of Enzyme Inhibition and Medicinal Chemistry 05/2009; 24(4):957-9. · 1.62 Impact Factor
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ABSTRACT: Oligonol is a polyphenol formulation enriched with catechin-type oligomers. As an initial approach to assess the chemopreventive potential of Oligonol, the study investigated the effects of Oligonol on the inhibition of lung metastasis induced by B16F-10 melanoma cells in C57BL/6 mice. Oligonol, which is abundantly found in plants, vegetables and fruits, was found to possess antimetastatic activity against B16F-10 melanoma cells. Continued consumption of Oligonol, even at high doses, for long periods does not seem to cause any toxic symptoms because excess Oligonol is stored in adipose tissue rather than in the liver. However, the mechanism by which Oligonol exerts its antimetastatic activity remains unclear. Further investigations are required to clarify the exact role of Oligonol in such B16F-10 melanoma regulation.
Phytotherapy Research 04/2009; 23(7):1043-6. · 2.09 Impact Factor
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ABSTRACT: Dendropanax morbifera Leveille (Araliaceae) is well known in Korea traditional medicine for a variety of diseases. The methanol extract of the lower stem parts of D. morbifera was investigated for its activity against chloroquine-sensitive strains of Plasmodium falciparum using the parasite lactate dehydrogenase assay method. Two cycloartane-type glycosides oleifoliosides A (1) and B (2), and dendropanoxide (3), beta-amyrin (4), alpha-amyrin (5) have been isolated from the stem parts of D. morbifera. All five compounds were evaluated for in vitro antiplasmodial activities as well as their cytotoxic potential on SK-OV-3 cancer cell lines. Compounds 2 and 3 showed notable growth inhibitory activity against chloroquine-sensitive strains of Plasmodium falciparum with IC(50) values of 6.2 and 5.3 microm. This compound showed no significant cytotoxicity (IC(50) > 150 microm) evaluated using SK-OV-3 cancer cell lines. This is the first report on the antiplasmodial activity of the compounds from D. morbifera.
Phytotherapy Research 04/2009; 23(11):1634-7. · 2.09 Impact Factor
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ABSTRACT: A series of benzamide-containing stilbene derivatives was synthesized through the incorporation of short basic side-chains in the B-ring hydroxy position of resveratrol. Their antiplasmodial activity was evaluated in vitro against the chloroquine resistant Plasmodium falciparum D10 strain, showing IC(50) values between 1.5 and 80 microM, while their cytotoxicity was assessed using an human myeloid leukemia (U-937) cell line. With a selectivity ratio of > 51.02, the most selective of these derivatives, 29, also had the most lowest cytotoxic activity of the series.
Chemical Biology & Drug Design 03/2009; 73(3):346-54. · 2.28 Impact Factor
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ABSTRACT: Petroleum ether extracts of Viola websteri Hemsl (Violaceae) were reported to have anti-plasmodial activity against Plasmodium falciparum in vitro, with this activity being largely attributable to 6-(8'Z-pentadecenyl)-salicylic acid (6-SA).
The schizontocidal activity of 6-SA on early Plasmodium berghei infections was evaluated in a four-day test. The possible 'repository' activity of 6-SA was assessed using the method described by Peters. The median lethal dose (LD50) of 6-SA, when given intraperitoneally, was also determined using uninfected ICR mice and the method of Lorke.
In the present study, 6-SA was found to have anti-malarial activity in vivo, when tested against P. berghei in mice. 6-SA at 5, 10 and 25 mg/kg x day exhibited a significant blood schizontocidal activity in four-day early infections, repository evaluations and established infections with a significant mean survival time comparable to that of the standard drug, chloroquine (5 mg/kg.day).
6-SA possesses a moderate anti-malarial activity that could be exploited for malaria therapy.
Malaria Journal 02/2009; 8:151. · 3.19 Impact Factor
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ABSTRACT: Motherwort (MW), a Korean folk medicine, has been applied to treat inflammatory disease. However, its effect on inflammatory cytokine release from mast cells is not well known. We investigated the anti- inflammatory effect of MW on the secretion of inflammatory cytokine such as tumor necrosis factor (TNF)-alpha and interleukin (IL)-6 and IL-8 in human mast cell line (HMC-1). MW was treated in vitro before activation of HMC-1 cells with phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore A23187. MW had no cytotoxic effects on HMC-1 cell viability. MW (1 mg/ml) inhibited PMA plus A23187-stimulated gene expression and production of TNF-alpha, IL-6, and IL-8. Stimulation with PMA plus A23187 induced NF-kappaB activation in HMC-1 cells, which was inhibited by MW (1 mg/ml). MW inhibited secretion of TNF-alpha, IL-6, and IL-8 possibly by inhibiting NF-kappaB activation. These results indicate that MW may be helpful in regulating inflammatory diseases.
Immunopharmacology and Immunotoxicology 02/2009; 31(2):209-13. · 1.83 Impact Factor
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ABSTRACT: Leaves of Eriobotrya japonica Lindl. (Rosaceae) (LEJL) have been used as traditional medicines for inflammatory diseases and chronic bronchitis. However, its effect on mast cell-mediated anaphylactic reaction is not known. The anaphylactic allergic reaction is involved in many allergic diseases such as asthma and allergic rhinitis. In this report, we investigate the effect of LEJL on the anaphylactic allergic reaction and studied its possible mechanisms of action. LEJL inhibited compound 48/80-induced systemic anaphylactic reactions and serum histamine release in mice. LEJL dose-dependently decreased the IgE-mediated passive cutaneous anaphylaxis and histamine release from mast cells. Furthermore, LEJL decreased the production of tumor necrosis factor-alpha in phorbol 12-myristate 13-acetate and A23187-stimulated human mast cells. These findings provide evidence that LEJL could be a candidate as an anti-allergic agent.
Immunopharmacology and Immunotoxicology 02/2009; 31(2):314-9. · 1.83 Impact Factor
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ABSTRACT: Vascular smooth-muscle cell proliferation plays an important role in atherosclerosis and restenosis. Rhein is an active component extracted from rhubarb. In this study, rhein was found to exert potent inhibitory effects against tumor necrosis factor (TNF)-alpha-induced human aortic smooth-muscle cells (HASMCs) proliferation.
These effects were associated with induced apoptosis, including the induction of Annexin V-positive cells, the cleavage of poly(ADP-ribose)polymerase (PARP), and caspases 3, 8 and 9.
Inhibitors of caspases 3, 8 and 9 were efficiently blocked by rhein-induced apoptosis in TNF-alpha-treated HASMCs. In addition, treatment with rhein resulted in the release of cytochrome c into the cytosol, a loss of mitochondrial membrane potential (DeltaPsi(m)), a decrease in Bcl-2 and Bcl-xL and an increase in Bax and Bak expression. However, rhein-mediated apoptosis was blocked by a mitochondrial membrane depolarization inhibitor. These findings indicate that rhein-induced apoptosis occurred via a mitochondrial pathway. Furthermore, the inhibition of mitochondrial membrane depolarization was efficiently blocked by rhein-induced caspase-9 activity, which indicates that the rhein-induced caspase activation signal was downstream of the mitochondrial pathway. Taken together, the results of this study show that rhein inhibits TNF-alpha-induced HASMC proliferation via mitochondria-dependent apoptosis and that rhein has the potential to act as an anti-atherosclerosis agent.
Journal of Vascular Research 02/2009; 46(4):375-86. · 2.65 Impact Factor
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ABSTRACT: The mast cell-mediated immediate-type allergic reaction is involved in many allergic diseases such as asthma, allergic rhinitis, and sinusitis. Stimulation of mast cells starts the process of degranulation resulting in release of mediators such as histamine and an array of inflammatory cytokines. In this report, we investigated the effect of aqueous extract of Teucrium japonicum Houttuyn (Labiatae) (AXTJ) on the mast cell-mediated allergy model and studied its possible mechanisms of action. AXTJ inhibited compound 48/80-induced systemic reactions and serum histamine release in mice. AXTJ decreased immunoglobulin E-mediated passive cutaneous anaphylaxis reaction. AXTJ reduced histamine release and intracellular calcium from rat peritoneal mast cells activated by compound 48/80. In addition, AXTJ attenuated activation of nuclear factor (NF)-kappaB, and downstream tumor necrosis factor (TNF)-alpha expression in phorbol 12-myristate 13-acetate and calcium ionophore A23187-stimulated human mast cells. Our findings provide evidence that AXTJ inhibits mast cell-derived allergic reactions and involvement of intracellular calcium, TNF-alpha, and NF-kappaB in these effects.
Food and chemical toxicology: an international journal published for the British Industrial Biological Research Association 01/2009; 47(2):398-403. · 2.99 Impact Factor
