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ABSTRACT: Saposhnikovia divaricata Schischk. belongs to the family Umbelliferae and grows in the eastern Siberia and northern Asia. 1 The roots of S. divaricata have been used for the treatment of rheumatism, headache, convulsion and nerve paralysis in China and Korea. 1 Previous study for this plant led to the identification of chemical constituents such as chromones, coumarins, lignans, polyacetylenes, and sterols, 2 as well as biological activities including analgesic, 3 anti-proliferative, 4 antioxidant, 4 and iNOS inhibitory activities. 5 As a part of our search for anti-inflammatory constituents of plant origin, 6,7 this plant was selected for further follow-up isolation work. In the present study, we described the isolation and structures elucidation of a new compound and 13 known compounds (Fig. 1), and the evaluation of their Figure 1. Structures of Compounds 1-14.
Bull. Korean Chem. Soc. 01/2132; 32326.
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ABSTRACT: Two triterpenoidal saponins were isolated from the seeds of Momordica cochinchinensis Sprenger (Cucurbitaceae). Identification of chemical structures has been performed by (1)H- and (13)C-NMR spectroscopy and gas chromatography (GC). One of the saponins is a new gypsogenin glycoside, named as gypsogenin 3-O-β-D-galactopyranosyl(1→2)-[α-L-rhamnopyranosyl(1→3)]-β-D-glucuronopyranoside (compound 1), which is reported for the first time from natural resources. The other saponin is a quillaic acid glycoside (compound 2), which showed anti-inflammatory activities in RAW 264.7 cells. The mechanistic understanding of anti-inflammatory activities demonstrates that compound 2 inhibits lipopolysaccharide-induced expression of nitric oxide and IL-6 via NF-κB pathway.
Immunopharmacology and Immunotoxicology 08/2012; · 1.83 Impact Factor
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ABSTRACT: Cinnamomum cambodianum has been used as a traditional medicine in Cambodia. Its effect on the bone marrow-derived mast cells (BMMCs) mediated allergic response remains unknown. In this study, a chloroform-soluble extract of C. cambodianum was evaluated for its effect on allergic mediators, including prostaglandin D₂ (PGD₂), leukotriene C₄ (LTC₄), β-hexosaminidase and cyclooxygenase-2 (COX-2) protein, in phorbol 12-myristate 13-acetate (PMA) plus calcimycin-stimulated BMMCs. The results revealed that the chloroform-soluble extract inhibited the production of interleukin-6, PGD₂ and LTC₄, and the expression of COX-2 in PMA plus calcimycin-stimulated BMMCs, implying a potential benefit of C. cambodianum in the treatment of allergy.
Immunopharmacology and Immunotoxicology 01/2012; 34(4):639-44. · 1.83 Impact Factor
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ABSTRACT: In this study, the anti-inflammatory and anti-allergic effects of the chloroform-soluble extract of Agaricus blazei in mouse bone marrow-derived mast cells (BMMCs) were investigated. The chloroform-soluble extract inhibited IL-6 production in PMA plus A23187-stimulated BMMCs, and down-regulated the phosphorylation of Akt. In addition, this extract demonstrated inhibition of the degranulation of β-hexosaminidase and the production of IL-6, prostaglandin D(2) and leukotriene C(4) in PMA plus A23187-induced BMMCs. In conclusion, the chloroform-soluble extract of Agaricus blazei exerted anti-inflammatory and anti-allergic activities mediated by influencing IL-6, prostaglandin D(2), leukotriene C(4), and the phosphorylation of Akt.
The American Journal of Chinese Medicine 01/2012; 40(5):1073-84. · 1.98 Impact Factor
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ABSTRACT: Lambertianic acid is a bioactive diterpene found in the leaves of Thuja orientalis. Its effect on the bone marrow-derived mast cell (BMMC) mediated allergy and inflammation mechanism remains unknown. In this study, lambertianic acid was evaluated for its effect on the allergic mediators, including prostaglandin D(2) (PGD(2)), leukotriene C(4) (LTC(4)), β-hexosaminidase (β-Hex) and cyclooxygenase-2 (COX-2) protein, in phorbol 12-myristate 13-acetate (PMA) plus calcimycin-stimulated BMMCs. The results revealed that lambertianic acid inhibited the production of interleukin-6 (IL-6), PGD(2) and LTC(4), the expression of COX-2 and the degranulation of β-hexosaminidase in the PMA plus calcimycin-induced BMMCs. Taken together, these findings implied that lambertianic acid may possess the potential in the treatment of allergy.
Immunopharmacology and Immunotoxicology 08/2011; 34(2):250-5. · 1.83 Impact Factor
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Hee-Sung Chae,
Ok-Hwa Kang,
You-Chang Oh,
Jang-Gi Choi,
Joon-Ho Keum,
Sung-Bae Kim,
Yong-Sik Kim,
Su-Hyun Mun,
Dong-Won Shin,
Sin-Hee Han,
Dong-Yeul Kwon
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ABSTRACT: Gomisin N is a bioactive compound and a prominent anti-allergic agent found in the fruits of tree Schizandra chinensis. However, its effects on the bone marrow-derived mast cell (BMMC)-mediated allergy and inflammation mechanism remain unknown. In this study, the biological effects of gomisin were evaluated while focusing on its effects on the allergic mediator in PMA + A23187-stimulated BMMCs. The anti-allergic effect of gomisin has shown that inhibited PMA + A23187-induced interleukin-6 (IL-6) production. An investigation was also conducted to determine its effects on the production of several allergic mediators including prostaglandin D(2) (PGD(2)), leukotriene C(4) (LTC(4)), β-hexosaminidase (β-Hex), and cyclooxygenase-2 (COX-2) protein. The results revealed that gomisin inhibited the PMA + A23187-induced production of IL-6, PGD(2), LTC(4), β-Hex, and COX-2 protein. Taken together, these findings indicate that gomisin N has the potential for use in the treatment of allergy.
Immunopharmacology and Immunotoxicology 03/2011; 33(4):709-13. · 1.83 Impact Factor
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ABSTRACT: Bioactivity-guided isolation on a n-hexane-soluble fraction of Thyrsanthera suborbicularis led to the isolation of a new rosane-type diterpene, 19-hydroxy-1(10), 15-rosadiene (1), along with three known compounds, taraxerol, acetyl aleuritolic acid, and spathulenol. The structures of isolated compounds were determined by interpretation of NMR spectroscopic data and mass spectrometry. Compound 1 demonstrated significantly inhibitory activity on nitric oxide production in RAW264.7 lipopolysaccharide (LPS)-activated mouse macrophages with an IC(50) value of 2.91 µg/ml via the suppression of inducible nitric oxide synthase (iNOS) mRNA expression.
Chemical & pharmaceutical bulletin 01/2011; 59(3):382-4. · 1.70 Impact Factor
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ABSTRACT: To determine the anti-inflammatory and analgesic activities of methyl gallate (MG) isolated from Galla Rhois, MG was studied in vivo for its analgesic activities using the writhing response in mice. Anti-inflammatory activity of MG was evaluated for NO and IL-6 production in RAW 264.7 cells. MG inhibited LPS-induced NO and IL-6 production. Consistent with these observations, the protein and mRNA expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) were inhibited by MG. Moreover, MG suppressed the phosphorylation of ERK1/2 in LPS-induced RAW 264.7 cells in a dose-dependent manner. Taken together, the results of this study indicate that MG has anti-inflammatory effects.
The American Journal of Chinese Medicine 01/2010; 38(5):973-83. · 1.98 Impact Factor
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Jang-Gi Choi,
Ok-Hwa Kang,
Obiang-Obounou Brice,
Young-Seob Lee, Hee-Sung Chae,
You-Chang Oh,
Dong-Hwan Sohn,
Hyun Park,
Han-Gil Choi,
Se-Gun Kim,
Dong-Won Shin,
Dong-Yeul Kwon
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ABSTRACT: Ecklonia cava is a brown alga (Laminariales, Phaeophyta) growing on the subtidal rocky shores of Korea. It has antioxidant, antidiarrhea, and anticoagulant effects. In this study, the antimicrobial activity of E. cava EtOH extract and its fractions (n-hexane, CH2Cl2, EtOAc, n-BuOH, and H2O) were investigated against methicillin-resistant Staphylococcus aureus and Salmonella spp. The E. cava EtOAc fraction showed good antibacterial activity against all bacteria. Eckol isolated from E. cava EtOAc fraction showed antimicrobial activity against all the tested strains. The minimum inhibitory concentration of eckol against S. aureus strains ranged from 125 to 250 microg/mL and 125 to 250 microg/mL for Salmonella strains. The fraction inhibitory concentration index of eckol in combination with ampicillin ranged from 0.31 to 0.5, indicating remarkable synergism against S. aureus. However, against Salmonella gallinarum ATCC 9184 and Salmonella typhimurium, it ranges from 0.75 to 1.0. The combinations of eckol + ampicillin exhibited improved inhibition of S. aureus and Salmonella with synergy or additive effect. We suggest that eckol ingredients of the E. cava against S. aureus and Salmonella have antibacterial activity.
Foodborne Pathogens and Disease 12/2009; 7(4):435-41. · 2.26 Impact Factor
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Jang-Gi Choi,
Ok-Hwa Kang,
Young-Seob Lee, Hee-Sung Chae,
You-Chang Oh,
Obiang-Obounou Brice,
Min-San Kim,
Dong-Hwan Sohn,
Hun-Soo Kim,
Hyun Park,
Dong-Won Shin,
Jung-Rae Rho,
Dong-Yeul Kwon
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ABSTRACT: Punica granatum is commonly used in Korea as a traditional medicine for the treatment of pathogenic bacteria. In this study, we investigated the in vitro and in vivo antimicrobial activity of P. granatum peel EtOH extract (PGPE) against 16 strains of Salmonella. The minimal inhibitory concentrations of PGPE were in the range of 62.5-1000 x03BCg mL(-1). In addition, the in vivo antibacterial activity of the PGPE extract was examined in a S. typhimurium infection mouse model. Mice were initially infected with S. typhimurium and then with PGPE. The extract was found to have significant effects on mortality and the numbers of viable S. typhimurium recovered from feces. Although clinical signs and histological damage were rarely observed in the treated mice, the untreated controls showed signs of lethargy and histological damage in the liver and spleen. Taken together, the results of this study indicate that PGPE has the potential to provide an effective treatment for salmonellosis.
Evidence-based Complementary and Alternative Medicine 09/2009; 2011:690518. · 4.77 Impact Factor
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Jang-Gi Choi,
Ok-Hwa Kang, Hee-Sung Chae,
Brice Obiang-Obounou,
Young-Seob Lee,
You-Chang Oh,
Min-San Kim,
Dong-Won Shin,
Jeong-Ah Kim,
Young-Ho Kim,
Dong-Yeul Kwon
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ABSTRACT: Methicillin-resistant Staphylococcus aureus (MRSA) is serious clinical urgent problems worldwide. In the present study, the antibacterial activity of Hylomecon hylomeconoides was investigated. The EtOH extract and its fraction (n-hexane, CH(2)Cl(2), EtOAc, and H(2)O) were investigated against MRSA. The most active extract (CH(2)Cl(2)) led to the isolation of 6-methoxydihydrosanguinarine (6-MS), 6-acetonylhydrosanguinarine, and dihydrosanguinarine. These compounds were very active against MRSA strains with minimum inhibitory concentrations (MICs) ranging from 1.95 to 250 microg/ml. Our study did however focus on 6-MS as it appeared to be the most active with MICs in the range of 1.9 to 3.9 microg/ml. These results encourage us to think that 6-MS can be used as a natural antibacterial agent.
Applied biochemistry and biotechnology 08/2009; 160(8):2467-74. · 1.94 Impact Factor
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Ok-Hwa Kang,
Hye-Jin Jang, Hee-Sung Chae,
You-Chang Oh,
Jang-Gi Choi,
Young-Seob Lee,
Jong-Hak Kim,
Youn Chul Kim,
Dong Hwan Sohn,
Hyun Park,
Dong-Yeul Kwon
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ABSTRACT: Resveratrol is a phytoalexin polyphenolic compound found in various plants, including grapes, berries, and peanuts. Recently, studies have documented various health benefits of resveratrol including cardiovascular and cancer-chemopreventive properties. The aim of the present study was to demonstrate the effects of resveratrol on the expression of pro-inflammatory cytokines, as well as to elucidate its mechanism of action in the human mast cell line (HMC-1). Cells were stimulated with phorbol 12-myristate 13-acetate (PMA) plus A23187 in the presence or absence of resveratrol. To study the possible effects of resveratrol, ELISA, RT-PCR, real-time RT-PCR, Western blot analysis, fluorescence, and luciferase activity assays were used in this study. Resveratrol significantly inhibited the PMA plus A23187-induction of inflammatory cytokines such as tumour necrosis factor (TNF)-alpha, interleukin (IL)-6 and IL-8. Moreover, resveratrol attenuated cyclooxygenase (COX)-2 expression and intracellular Ca2+ levels. In activated HMC-1 cells, phosphorylation of extra-signal response kinase (ERK) 1/2 decreased after treatment with resveratrol. Resveratrol inhibited PMA plus A23187-induced nuclear factor (NF)-kappaB activation, IkappaB degradation, and luciferase activity. Resveratrol suppressed the expression of TNF-alpha, IL-6, IL-8 and COX-2 through a decrease in the intracellular levels of Ca2+ and ERK 1/2, as well as activation of NF-kappaB. These results indicated that resveratrol exerted a regulatory effect on inflammatory reactions mediated by mast cells.
Pharmacological Research 06/2009; 59(5):330-7. · 4.44 Impact Factor
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Hee-Sung Chae,
Ok-Hwa Kang,
Jang-Gi Choi,
You-Chang Oh,
Young-Seob Lee,
Hye-Jin Jang,
Jong Hak Kim,
Hyun Park,
Kyu Yong Jung,
Dong Hwan Sohn,
Dong-Yeul Kwon
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ABSTRACT: In this study, we evaluated the effect of 5-hydroxytryptophan on anti-inflammatory and analgesic activity in RAW 264.7 cells. Cells were treated with different concentrations of 5-hydroxytryptophan for either 1 h or for 24 h. The anti-inflammatory effect was then analyzed by enzyme-linked immunosorbent assay (ELISA), Western blotting and reverse transcription polymerase chain reaction (RT-PCR). In addition, the analgesic activity was evaluated by measuring the acetic acid-induced writhing response. We found that 5-hydroxytryptophan significantly reduced the acetic acid-induced writhing response. Moreover we evaluated the effects of 5-hydroxytryptophan on the release of several inflammatory mediators including nitric oxide (NO) and interleukin-6 (IL-6). Our results demonstrated that 5-hydroxytryptophan inhibited the lipopolysaccharide (LPS)-induced expression of NO and IL-6. Furthermore, we found that 5-hydroxytryptophan played a role in LPS induced inducible nitric oxide synthase (iNOS), cyclo oxygenase-2 (COX-2) and extracellular-signal regulated protein kinase (ERK) activation. Taken together, these results indicate that 5-hydroxytryptophan has the potential for use in the treatment of inflammatory disease and as an analgesic.
Biological & Pharmaceutical Bulletin 05/2009; 32(4):553-7. · 1.66 Impact Factor
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ABSTRACT: We evaluated the in vivo anti-inflammatory and analgesic activities of orally administered paeonol in mice, and also investigated the anti-inflammatory activity of paeonol in a cell line. Paeonol significantly reduced the edema induced by arachidonic acid in rats. The analgesic effects were assayed using 2 different models, i.e., by acetic acid-induced writhing response and by formalin induced licking and biting time. Moreover, we examined the effects of paeonol on the release of inflammatory mediators such as NO, PGE(2) and IL-6. Our results demonstrated that paeonol inhibited LPS induced expression of NO, PGE(2) and IL-6. Paeonol prevented LPS induced iNOS, COX-2 and ERK activation. Therefore, paeonol appears to have potential as a treatment for inflammatory disease and analgesic.
The American Journal of Chinese Medicine 02/2009; 37(1):181-94. · 1.98 Impact Factor
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ABSTRACT: Methyl gallate is a major component of Galla Rhois, as carvacrol is of oregano essential oils. Both have shown good antibacterial activity against intestinal bacteria. This study investigated the antibacterial activities of nalidixic acid in combination with methyl gallate and carvacrol against nalidixic acid resistant bacteria. The combined effect of nalidixic acid with methyl gallate and carvacrol was evaluated using the checkerboard method to obtain a fractional inhibitory concentration index. The results showed that the combinations of nalidixic acid + methyl gallate/carvacrol improved nalidixic acid resistant pathogenic bacteria inhibition with synergy or partial synergy activity. Thus, a strong bactericidal effect of the drug combinations was observed. In vitro data thus suggested that nalidixic acid combined with methyl gallate and carvacrol may be microbiologically beneficial, rather than antagonists.
Molecules 02/2009; 14(5):1773-80. · 2.39 Impact Factor
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ABSTRACT: Resveratrol is a polyphenol compound and prominent anti-inflammatory agent found in plants, including the fruits of Morus alba. However, the therapeutic mechanisms of resveratrol remain largely unclear. To gain insight into the biological effects of resveratrol, we examined its influence on LPS-induced IL-8 production in the human monocytic cell line, THP-1. In inflammatory diseases, IL-8 plays a central role in the initiation and maintenance of inflammatory response. In the present study, IL-8 production was measured by ELISA and RT-PCR, while MAPK activation, IkappaBalpha degradation, nuclear factor (NF)-kappaB activation and cyclooxygenase (COX)-2 expression were determined by Western blot analysis. Resveratrol inhibited LPS-induced IL-8 production in a dose-dependent manner. Furthermore, resveratrol inhibited extracellular signal-regulated kinase (ERK) and p38 MAPK phosphorylation, IkappaBalpha degradation, NF-kappaB activation and cyclooxygenase (COX)-2 expression, which suggest that resveratrol inhibits IL-8 secretion by blocking MAPK phosphorylation and NF-kappaB activation. Taken together, these findings may help elucidate the mechanism by which resveratrol modulates THP-1 cell activation under inflammatory conditions.
The American Journal of Chinese Medicine 01/2009; 37(6):1203-14. · 1.98 Impact Factor
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Jang-Gi Choi,
Ok-Hwa Kang,
Young-Seob Lee,
You-Chang Oh, Hee-Sung Chae,
Hye-Jin Jang,
Jong Hak Kim,
Dong-Hwan Sohn,
Dong-Won Shin,
Hyun Park,
Dong-Yeul Kwon
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ABSTRACT: Salmonella remains a primary cause of food poisoning worldwide, and massive outbreaks have been witnessed in recent years. Therefore, this study investigated the antimicrobial activity of methyl gallate (MG), which exhibited good antibacterial activity (MIC=3.9-125 mg/ml) against all the bacterial strains tested. In a checkerboard dilution test, MG markedly lowered the MICs of ciprofloxacin (CPFX) against Salmonella. The combined activity of CPFX and MG against Salmonella resulted in fractional inhibitory concentrations (FICs) ranging from 0.0037 to 0.015 and from 0.24 to 7.8 mg/ml, respectively. Meanwhile, the FIC index ranged from 0.31-0.37, indicating a marked synergistic relationship between CPFX and MG against Salmonella. Time-kill assays also showed a decrease in the CFU/ml between the combination and the more active compound. Therefore, this study demonstrated that MG and CPFX can act synergistically in inhibiting Salmonella in vitro.
Journal of Microbiology and Biotechnology 12/2008; 18(11):1848-52. · 1.38 Impact Factor
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Ok-Hwa Kang, Hee-Sung Chae,
Jang-Gi Choi,
Yoo-Chang Oh,
Young-Seob Lee,
Jong-Hak Kim,
Man-Jun Seung,
Hye-Jin Jang,
Ki-Hwan Bae,
John-Hwa Lee,
Dong-Won Shin,
Dong Yeul Kwon
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ABSTRACT: Macrophages play central roles in the innate immune system. The roots of Aralia cordata are widely used in Oriental medicine as a remedy for arthritis. During our program to screen medicinal plants for potential anti-inflammatory compounds, ent-pimara-8(14), 15-dien-19-oic acid (pimaradienoic acid; PA) was isolated from the roots of A. cordata. We examined the effect of PA on pro-inflammatory mediators in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. PA was found to significantly inhibit the production of nitric oxide (NO), prostaglandin E(2) (PGE(2)), and interleukin-6 (IL-6), as well as the expressions of inducible NO synthase (iNOS), cyclooxygenase-2 (COX-2), and IL-6. Furthermore, we examined whether mitogen-activated protein kinases (MAPKs) and phosphatidylinositol 3-kinase (PI3K) signaling pathways are involved in LPS-induced RAW 264.7 cells. We found that a p38 inhibitor (SB203580) and an ERK 1/2 inhibitor (PD98059) significantly affected LPS-induced IL-6 production. In contrast, a JNK 1/2 inhibitor (SP600125) and PI3K inhibitor (wortmannin or LY294002) did not block the induction of IL-6 production by LPS. The LPS-induced phosphorylation of p38 MAPK and extracellular signal-regulated kinase 1/2 (ERK1/2) was inhibited by PA, but not the phosphorylation of JNK 1/2 and AKT (Ser473). Moreover, PA suppressed I kappaB alpha degradation, NF-kappaB activation and luciferase activity. These results suggest that PA isolated from A. cordata has a potential regulatory effect on inflammatory iNOS, COX-2 and IL-6 expression through blockade of the phosphorylation of MAPKs following I kappaB alpha degradation and NF-kappaB activation.
European journal of pharmacology 11/2008; 601(1-3):179-85. · 2.59 Impact Factor
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ABSTRACT: The antimicrobial killing activity toward methicillin-resistant Staphylococcus aureus (MRSA) has been a serious emerging global issue. New effective antimicrobials and/or new approaches to settle this issue are urgently needed. The oriental herb, Alpinia officinarum, has been used in Korea for several hundreds of years to treat various infectious diseases. As it is well known, one of the active constituents of Alpinia officinarum is galangin. Against the 17 strains, the minimum inhibitory concentrations (MICs) of galangin (GAL) were in the range of 62.5 ~ 125 microg/ml, and the MICs of gentamicin (GEN) ranged from 1.9 microg/ml to 2,000 microg/ml. The fractional inhibitory concentrations (FICs) of GAL, in combination with GEN, against 3 test strains were 0.4, 3.9, and 250 microg/ml, and were all 15.62 microg/ml in GEN. The FIC index showed marked synergism in the value range of 0.19 to 0.25. By determining time-kill curves, also confirmed the low synergism of the GAL and GEN combination against 4 h, 8 h, 12 h, and 24 h cultured MRSA. The time-kill study results indicated a low synergistic effect against 3 test strains. Thus, the mixture of GAL and GEN could lead to the development of new combination antibiotics against MRSA infection.
The Journal of Microbiology 07/2008; 46(3):283-8. · 1.10 Impact Factor
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Ok-Hwa Kang, Hee-Sung Chae,
You-Chang Oh,
Jang-Gi Choi,
Young-Seob Lee,
Hye-Jin Jang,
Jong-Hak Kim,
Youn Chul Kim,
Dong Hwan Sohn,
Hyun Park,
Dong-Yeul Kwon
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ABSTRACT: The extract of Angelicae dahuricae radix has traditionally been used as an anti-noceptive remedy in China. In this study, the methanol extract of Angelicae dahuricae radix (MEAD) was evaluated to determine if it has anti-noceptive and anti-inflammatory action. The anti-nociceptive activities of MEAD were evaluated by determining the writhing response and sleeping time, as well as by a formalin test. In addition, the anti-inflammatory activities of MEAD were evaluated by a vascular permeability test as well as by measuring the carrageenan-induced paw edema and conducting a myeloperoxidase (MPO) assay. MEAD (600 and 1200 mg/kg) exhibited anti-inflammatory effects on acetic acid-induced vascular permeability, carrageenan-induced paw edema, and MPO activity. Moreover, the results of the formalin test, the acetic acid-induced writhing response and the pentobarbital-induced sleeping time indicated that MEAD had anti-nociceptive effects that occurred in a concentration-dependent manner. To determine the mechanism by which MEAD exerted its effects on the expression of inducible nitric oxide synthase (iNOS) and the production of nitric oxide (NO) by treated murine macrophage RAW 264.7 cells was evaluated. Similar to the in vivo activities, both the iNOS expression and NO production were significantly suppressed by MEAD in a dose-dependent manner. Furthermore, MEAD inhibited the activating phosphorylation of ERK1/2. These results provide a scientific basis that explains the mechanism by which Angelicae dahuricae radix relieves inflammatory pain.
The American Journal of Chinese Medicine 02/2008; 36(5):913-28. · 1.98 Impact Factor
