• Journal of Pharmacopuncture
• /
• v.25 no.3
• /
• pp.209-215
• /
• 2022

Objectives: Aqueous leaf extract of Tridax procumbens (ALETP) has potent relaxant activity. However, this relaxant activity in respiratory smooth muscle remains uninvestigated. This study investigates the effect of ALETP on the contractile activity of tracheal smooth muscle (TSM) in adult male Wistar rats. Methods: Twelve male Wistar rats divided into 2 groups and were treated with either 100 mg/kg of ALETP (ALETP treatment group) or vehicle (distilled water; control group) through oral gavage for 4 weeks. Dose responses of TSM from the 2 groups to acetylcholine (10^-9 to 10^-5 M), phenylephrine (10^-9 to 10^-5 M), and potassium chloride (KCl; 10^-9 to 10^-4 M) were determined cumulatively. Furthermore, cumulative dose responses to acetylcholine (10^-9 to 10^-5 M) after pre-incubation of TSM with atropine (10^-5 M), L-NAME (10^-4 M), indomethacin (10^-4 M), and nifedipine (10^-4 M), were determined. Results: Treatment with ALETP substantially inhibited TSM contraction stimulated by cumulative doses of acetylcholine, phenylephrine, and KCl. Furthermore, preincubation of TSM from the 2 groups in atropine significantly inhibited contractility in TSM. Incubation in L-NAME and indomethacin also significantly inhibited contractility in TSM of ALETP-treated rats compared to that of controls. Contractile activity of the TSM was also inhibited significantly with incubation in nifedipine in ALETP-treated rats. Conclusion: ALETP enhanced relaxant activity in rat TSM primarily by blocking the L-type calcium channel and promoting endothelial nitric oxide release. ALETP contains agents that may be useful in disorders of the respiratory tract.

• Biomolecules & Therapeutics
• /
• v.16 no.2
• /
• pp.147-160
• /
• 2008

The present study was designed to examine effects of polyphenolic compounds isolated from red wine (PCRW) on the release of catecholamines (CA) from the isolated perfused model of the rat adrenal medulla, and to clarify its mechanism of action. PCRW (20${\sim}$180 ${\mu}$g/mL), given into an adrenal vein for 90 min, caused inhibition of the CA secretory responses evoked by ACh (5.32 mM), high $K^+$ (a direct membrane-depolarizer, 56 mM), DMPP (a selective neuronal nicotinic $N_N$ receptor agonist, 100 ${\mu}$M) and McN-A-343 (a selective muscarinic $M_1$ receptor agonist, 100 ${\mu}$M) in dose- and time-dependent fashion. PCRW itself did not affect basal CA secretion (data not shown). Following the perfusion of PCRW (60 ${\mu}$g/mL), the secretory responses of CA evoked by Bay-K-8644 (a L-type dihydropyridine $Ca^{2+}$ channel activator, 10 ${\mu}$M), cyclopiazonic acid (a cytoplasmic $Ca^{2+}$-ATPase inhibitor, 10 ${\mu}$M) and veratridine (an activator of voltage-dependent $Na^+$ channels, 10 ${\mu}$M) were also markedly blocked, respectively. Interestingly, in the simultaneous presence of PCRW (60 ${\mu}$g/mL) and L-NAME (a selective inhibitor of NO synthase, 30 ${\mu}$M), the inhibitory responses of PCRW on the CA secretion evoked by ACh, high $K^+$, DMPP, McN-A-343, Bay-K-8644 and cyclpiazonic acid were recovered to considerable level of the corresponding control release compared with those effects of PCRW-treatment alone. Practically, the amount of NO released from adrenal medulla after loading of PCRW (180 ${\mu}$g/mL) was significantly increased in comparison to the corresponding basal released level. Collectively, these results obtained here demonstrate that PCRW inhibits the CA secretory responses evoked by stimulation of cholinergic (both muscarinic and nicotinic) receptors as well as by direct membrane-depolarization from the isolated perfused adrenal gland of the normotensive rats. It seems that this inhibitory effect of PCRW is mediated by blocking the influx of both ions through $Na^+$ and $Ca^+{2$} channels into the rat adrenomedullary chromaffin cells as well as by inhibiting the release of $Ca^{2+}$ from the cytoplasmic calcium store, which are due at least partly to the increased NO production through the activation of nitric oxide synthase. Based on these data, it is also thought that PCRW may be beneficial to prevent or alleviate the cardiovascular diseases, such as hypertension and angina pectoris.

• Journal of Korean Traditional Oncology
• /
• v.16 no.2
• /
• pp.25-34
• /
• 2011

Objectives : Citrus is the fruit that is readily available around us. Therefore, we investigated the anti-inflammatory effects of fraction isolated from the Citrus hassaku pericarp in RAW264.7 macrophage cells. Methods : The effects of fraction from Citrus hassaku pericarp on cell viability on RAW264.7 cells were measured by the MTT assay. The mRNA levels of iNOS and COX-2, its protein level by fraction of Citrus hassaku pericarp treatment in RAW264.7 macrophage cells were investigated by RT-PCR and immunoblots. Nitrite accumulation in the culture was measured colorimetrically by the Griess reaction using a Griess reagent. The amount of IL-6 and TNF-${\alpha}$ production was determined using an enzyme-linked immunosorbent assay (ELISA) kit. Results : The results indicated that the fraction of Citrus hassaku pericarp concentration highly suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) and IL-6 productions without a cytotoxic effect on RAW264.7 cells. fraction of Citrus hassaku pericarp inhibited the expressions of LPS-induced iNOS and COX-2 protein and their mRNA in a dose-dependent manner. Particularly, fraction of Citrus hassaku pericarp suppressed the level of nuclear factor-${\kappa}B$ (NF-${\kappa}B$) activity, which was linked with the suppression of LPS-induced phosphorylation of p65 at serine 276 and p65 translocation into nuclei, but not MAPK signaling. In addition, treatment with fraction of Citrus hassaku pericarp inhibited the production of IL-6 and TNF-${\alpha}$ in LPS-stimulated RAW264.7 cells. Conclusion : Our results indicate that fraction of Citrus hassaku pericarp potentially inhibits the biomarkers related to inflammation through the blocking of NF-${\kappa}B$ p65 activation, and it may be a potential therapeutic candidate for the treatment of inflammatory diseases.

• ALGAE
• /
• v.29 no.4
• /
• pp.343-353
• /
• 2014

Despite the extensive literature on marine algae over the past few decades, a paucity of published research and studies exists on red algae. The purpose of this study was to evaluate the potential therapeutic properties of the ethanol extract of the red alga Callophyllis japonica against lipopolysaccharide (LPS)-stimulated macrophage inflammation. The C. japonica extract (CJE) significantly inhibited the nitric oxide (NO) production and the induced dose-dependent reduction of the protein and mRNA levels of inducible nitric oxide synthase and cyclooxygenase-2. Additionally, the CJE reduced the mRNA levels of inflammatory cytokines, including tumor necrosis factor-${\alpha}$, interleukin (IL)-$1{\beta}$, and IL-6. We investigated the mechanism by which the CJE inhibits NO by examining the level of mitogen-activated protein kinases (MAPKs) activation, which is an inflammation-induced signaling pathway in macrophages. The CJE significantly suppressed the LPS-induced phosphorylation of c-Jun N-terminal kinase, extracellular signal-regulated kinase and p38 MAPK. Taken together, the results of this study demonstrate that the CJE inhibits LPS-induced inflammation by blocking the MAPK pathway in macrophages.

• The Korean Journal of Physiology and Pharmacology
• /
• v.12 no.4
• /
• pp.155-164
• /
• 2008

Resveratrol has been known to possess various potent cardiovascular effects in animal, but there is little information on its functional effect on the secretion of catecholamines (CA) from the perfused model of the adrenal medulla. Therefore, the aim of the present study was to determine the effect of resveratrol on the CA secretion from the isolated perfused model of the normotensive rat adrenal gland, and to elucidate its mechanism of action. Resveratrol (10${\sim}100{\mu}$M) during perfusion into an adrenal vein for 90 min inhibited the CA secretory responses evoked by ACh (5.32 mM), high $K^+$ (a direct membrane-depolarizer, 56 mM), DMPP (a selective neuronal nicotinic $N_n$ receptor agonist, 100${\mu}$M) and McN-A-343 (a selective muscarinic $M_1$ receptor agonist, 100${\mu}$M) in both a time- and dose- dependent fashion. Also, in the presence of resveratrol (30${\mu}$M), the secretory responses of CA evoked by veratridine 8644 (an activator of voltage-dependent$Na^+$ channels, 100${\mu}$M), Bay-K-8644 (a L-type dihydropyridine $Ca^{2+}$ channel activator, 10${\mu}$M), and cyc1opiazonic acid (a cytoplasmic $Ca^{2+}$-ATPase inhibitor, 10${\mu}$M) were significantly reduced. In the simultaneous presence of resveratrol (30${\mu}$M) and L-NAME (an inhibitor of NO synthase, 30${\mu}$M), the CA secretory evoked by ACh, high $K^+$, DMPP, McN-A-343, Bay-K-8644 and cyc1opiazonic acid were recovered to a considerable extent of the corresponding control secretion compared with the inhibitory effect of resveratrol alone. Interestingly, the amount of nitric oxide (NO) released from the adrenal medulla was greatly increased in comparison to its basal release. Taken together, these experimental results demonstrate that resveratrol can inhibit the CA secretory responses evoked by stimulation of cholinergic nicotinic receptors, as well as by direct membrane-depolarization in the isolated perfused model of the rat adrenal gland. It seems that this inhibitory effect of resveratrol is exerted by inhibiting an influx of both ions through $Na^+$ and $Ca^{2+}$ channels into the adrenomedullary cells as well as by blocking the release of $Ca^{2+}$ from the cytoplasmic calcium store, which are mediated at least partly by the increased NO production due to the activation of NO synthase.

• Korean Journal of Ecology and Environment
• /
• v.34 no.4 s.96
• /
• pp.261-266
• /
• 2001

Effects of elevated carbon dioxide ($CO_2$) on soil microbial processes were studied in a northern peatland. Intact peat cores with surface vegetation were collected from a northern Welsh fen, and incubated either under elevated carbon dioxide (700 ppm) or ambient carbon dioxide (350 ppm) conditions for 4 months. Higher algal biomass was found under the elevated $CO_2$ condition, suggesting $CO_2$ fertilization effect on primary production, At the end of the incubation, trace gas production and consumption were analyzed using chemical inhibitors. For methane ($CH_4$ ), methyl fluoride ($CH_3F$) was applied to determine methane oxidation rates, while acetylene ($C_2H_2$) blocking method were applied to determine nitrification and denitrification rates. First, we have adopted those methods to optimize the reaction conditions for the wetland samples. Secondly, the methods were applied to the samples incubated under two levels of $CO_2$. The results exhibited that elevated carbon dioxide increased both methane production (210 vs. $100\;ng\;CH_4 g^{-1}\;hr^{-1}$) and oxidation (128 vs. $15\;ng\;CH_4 g^{-1}\;hr^{-1}$), resulting in no net increase in methane flux. For nitrous oxide ($N_2O$) , elevated carbon dioxide enhanced nitrous oxide emission probably from activation of nitrification process rather than denitrification rates. All of these changes seemed to be substantially influenced by higher oxygen diffusion from enhanced algal productivity under elevated $CO_2$.

• Economic and Environmental Geology
• /
• v.41 no.3
• /
• pp.327-334
• /
• 2008

Understanding the chemical characteristics of sediments and the nutrient diffusion from sediments to the water body is important in the management of surface water quality. Changes in chemical properties and nutrient concentration of a submerged soil were monitored for 6 months using a microcosm with the thickness of 30cm for upland soil and 15cm of water thickness above the soil. The soil color changed from yellowish red to grey and an oxygenated layer was formed on the soil surface after 5 week flooding. The redox potential and the pH of the pore water in the microcosm decreased during the flooding. The nitrate concentration of the surface water was continuously increased up to $8\;mg\;l^{-1}$ but its phosphate concentration decreased from $2\;mg\;l^{-1}$ to $0.1\;mg\;l^{-1}$ during flooding. However, the concentrations of $NH_4^+$, $PO_4^{3-}$, Fe and Mn in the pore water were increased by the flooding during this period. The increased $NO_3^-$ in the surface water was due to the migration of $NH_4^+$ formed in the soil column and the oxidation to $NO_3^-$ in the surface water. The increased phosphate concentration in the pore water was due to the reductive dissolution of Fe-oxide and Mn-oxide, which scavenged phosphate from the soil solution. The oxygenated layer played a role blocking the migration of phosphate from the pore water to the water body.

• Journal of Life Science
• /
• v.23 no.8
• /
• pp.963-969
• /
• 2013

Although it is popularly believed that vitamin C protects cells from various genotoxicants, the degrees and mechanisms of itsprotective actions are not fully understood. In this study, vitamin C's protective effects against various genotoxicants were quantified, together with subsequent analyses on the mechanisms of these protective effects. Comet assay was employed to measure the degree of DNA damage in Chinese hamster ovary cells (CHO-K1) exposed to five genotoxicants, $H_2O_2$, $HgCl_2$, N-methyl-N-nitro-N-nitrosoguanidine (MNNG), 4-nitroquinoline-1-oxide (4NQO), and UV-irradiation. In cases cells were treated with $H_2O_2$, $HgCl_2$, and 4NQO together with vitamin C, the damage to DNA decreased to the level of the control group. In cases of UV-irradiation, the protective effect of vitamin C appeared, but did not reach the control levels. Interestingly, vitamin C did not have protective effects against the genotoxicity of MNNG. The degrees of DNA damage of cells treated with vitamin C prior to exposure togenotoxicants were 28~49% lower than those of cells treated with vitamin C after being exposed to genotoxicants. In conclusion, vitamin C had strong antioxidanteffects against genotoxicants by being a primary antioxidant blocking genotoxicity reaching the cells, rather than being a secondary antioxidant acting on post-exposure DNA repair processes. However, vitamin C's protective effects appearto be limited, as there are genotoxicants, such as MNNG, whosegenotoxicityis not affected by vitamin C. Therefore, the results of this study warrant furtherstudies on toxic mechanisms of genotoxicants and their interactions with protective mechanisms of vitamin C.

• Archives of Pharmacal Research
• /
• v.29 no.7
• /
• pp.591-597
• /
• 2006

Aerial parts of Artemisia asiatica (Compositae) have been traditionally used as an oriental medicine for the treatment of inflammatory and ulcerogenic diseases. In the present study, artemisolide was isolated as a nuclear factor $(NF)-{\kappa}B$ inhibitor from A. asiatica by activity-guided fractionation. Artemisolide inhibited $NF-{\kappa}B$ transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $5.8\;{\mu}M$. The compound was also effective in blocking $NF-{\kappa}B$ transcriptional activities elicited by the expression vector encoding the $NF-{\kappa}B$ p65 or p50 subunits bypassing the inhibitory kB degradation signaling $NF-{\kappa}B$ activation. The macrophages markedly increased their $PGE_2$ and NO production upon exposure to LPS alone. Artemisolide inhibited LPS-induced $PGE_2$ and NO production with $IC_{50}$ values of $8.7\;{\mu}M$ and $6.4\;{\mu}M$, respectively, but also suppressed LPS-induced synthesis of cyclooxygenase (COX)-2 or inducible NO synthase (iNOS). Taken together, artemisolide is a $NF-{\kappa}B$ inhibitor that attenuates LPS-induced production of $PGE_2$ or NO via down-regulation of COX-2 or iNOS expression in macrophages RAW 264.7. Therefore, artemisolide could represent and provide the anti-inflammatory principle associated with the traditional medicine, A. asiatica.

• Journal of the Korean Applied Science and Technology
• /
• v.37 no.6
• /
• pp.1517-1527
• /
• 2020

This study is about the UV protection effect and water resistance of a multiple emulsion (W/O/W) sunblock cream applied with emotional engineering and reports an actual industrial case. Multiple emulsion system of sunblock cream has the characteristics of changing to a W/O type that is soft and moist when applied, and has excellent water resistance after absorption. Multiple emulsion cream is a highly functional sunblock cream that has both moisture and water resistance. It is a stable milky white cream with a viscosity of 36,000 cps. The organic sunscreen used for the sunscreen was ethylhexylmethoxycinnamate and bisethylhexyloxyphenolmethoxyphenyltriazine. Hexagonal zinc oxide and titanium dioxide that block both UVB and UVA were used. As a result of measuring the UV protection effect by the in-vitro method, the UV protection effect (SPF) is 78.9 for multiple emulsion cream, 76.7 for W/O cream, and 71.3 for O/W cream. It was found that the blocking effect was different. This obtained the highest effect value in the multiple emulsion. As a clinical (in-vivo) result of the UV protection effect, the SPF value representing the UV protection effect of the sunblock cream developed with a multiple emulsion system was 85.7, and the PA-value that blocks the UVA area was 26.5, and ++++. It was found that it has a corresponding high blocking effect. As a result of the water resistance test, the W/O/W formulation had a high waterproofing resistance of 93.8% even after 4 hours, W/O had 75.4%, and O/W had a low water resistance of 25.3%. In the results of the HUT test, it was found in the order of multiple emulsion sun block cream > hydrophilic cream > lipophilic cream. Based on the research results of this multiple emulsion, it is expected to be highly active as a sunblock cream dedicated to outdoor activities by improving the feeling of use, UV protection index, and water resistance. Therefore, in this study, a multiple emulsion system of sunblock cream is developed and has a characteristic that changes to a W/O type that has a soft and moist feeling when applied, and has excellent water resistance after absorption.