• Biomolecules & Therapeutics
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• v.24 no.6
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• pp.595-603
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• 2016

(E)-3-Phenyl-1-(2-pyrrolyl)-2-propenone (PPP) is a pyrrole derivative of chalcone, in which the B-ring of chalcone linked to ${\beta}$-carbon is replaced by pyrrole group. While pyrrole has been studied for possible Src inhibition activity, chalcone, especially the substituents on the B-ring, has shown pharmaceutical, anti-inflammatory, and anti-oxidant properties via inhibition of NF-${\kappa}B$ activity. Our study is aimed to investigate whether this novel synthetic compound retains or enhances the pharmaceutically beneficial activities from the both structures. For this purpose, inflammatory responses of lipopolysaccharide (LPS)-treated RAW264.7 cells were analyzed. Nitric oxide (NO) production, inducible NO synthase (iNOS) and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) mRNA expression, and the intracellular inflammatory signaling cascade were measured. Interestingly, PPP strongly inhibited NO release in a dose-dependent manner. To further investigate this anti-inflammatory activity, we identified molecular pathways by immunoblot analyses of nuclear fractions and whole cell lysates prepared from LPS-stimulated RAW264.7 cells with or without PPP pretreatment. The nuclear levels of p50, c-Jun, and c-Fos were significantly inhibited when cells were exposed to PPP. Moreover, according to the luciferase reporter gene assay after cotransfection with either TRIF or MyD88 in HEK293 cells, NF-${\kappa}B$-mediated luciferase activity dose-dependently diminished. Additionally, it was confirmed that PPP dampens the upstream signaling cascade of NF-${\kappa}B$ and AP-1 activation. Thus, PPP inhibited Syk, Src, and TAK1 activities induced by LPS or induced by overexpression of these genes. Therefore, our results suggest that PPP displays anti-inflammatory activity via inhibition of Syk, Src, and TAK1 activity, which may be developed as a novel anti-inflammatory drug.

• Journal of the Korean Applied Science and Technology
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• v.35 no.1
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• pp.254-262
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• 2018

It was intended to check a possibility of activity of Psidium guajava leaf extract as anti-oxidant and anti-inflammatory material. Total polyphenol and total flavonoid content of Psidium guajava leaf extract was checked. Cream having inhibitory effect on inflammation through toxicity and NO production inhibition in RAW 264.7 cell was manufactured, and skin safety was evaluated. It was confirmen that total polyphenol and flavonoid content of Psidium guajava leaf extract was 126.4 mg/g and 223.17 mg/g respectively, which was high content. According to the results of checking toxicity through cell viability in RAW 264.7 cell, cytotoxicity was not shown. And NO production indicating inflammatory disease was inhibited concentration-dependently. According to the results of carrying out single patch test after manufacturing the cream containing the Psidium guajava leaf extract, skin irritation did not occur for 24 h to put patch on skin or for 24 h after removing the patch. Putting these results together, it was verified that there was possibility of application as raw materials for cosmetics, which would have anti-oxidant activity owing to the high polyphenol and flavonoid content of Psidium guajava leaf extract and anti-inflammatory material through NO production inhibition.

• Microbiology and Biotechnology Letters
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• v.38 no.4
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• pp.434-441
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• 2010

The Plants and their extracts containing polyphenol have been shown to be associated with decreased the cause of aging and variety of disease such as reaction oxygen species (ROS) and reactive nitrogen species (RNS) in several recent studies. We conducted to investigate whether the extracts and fractionation isolated from Aster glehni Fr. Schm. has an inhibitory effect association with oxidation or inflammation. The Aster glehni Fr. Schm. 70% aq. MeOH was fractioned according to polarity with n-hexane layer, EtOAc layer, n-BuOH layer and water layer. The electron donating ability of EtOAc, n-BuOH solvent fraction from Aster glehni Fr. Schm. was about 58.0%, 46.4% at $50\;{\mu}g/mL$, respectively. The superoxide anion radical inhibitory effect of EtOAc extracts was about 64.65% at $50\;{\mu}g/mL$, and n-BuOH extracts was 35.66% at $50\;{\mu}g/mL$. EtOAc layer to the inhibition activity of hyaluronidase and lipoxygenase were inhibited about 24.37%, 29.5% at $5\;{\mu}g/mL$. In the anti-inflammation effect of EtOAc layer inhibited the generation of nitric oxide. also, these results showed that EtOAc extract inhibited 81.5% at $50\;{\mu}g/mL$ on the expressions of iNOS protein in Raw264.7 cell line.

• Natural Product Sciences
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• v.13 no.3
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• pp.220-224
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• 2007

To search of more selective vasculogenic relaxation activity, the antioxidant activity of silkworm male pupae was determined by measuring its radical scavenging effect on 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radicals, and anticoagulant activity of them was measured clotting time in both activated partial thromboplastin time (aPTT). Because, most of cGMP-enhancing agent such as, sildenafil, promotes thrombin-induced platelet aggregation, developed unexplained thrombic conditions including heart attack. To search more suitable and safe drug for vasculogenic relaxation, we purified silkworm pupae male extract. The ethyl acetate extract of silkworm male pupae showed strong scavenging activity in both DPPH and aPTT anticoagulant activity. The antioxidant activity potential of the individual fraction was in order of ethyl acetate > n-butanol > chloroform > n-hexane. The ethyl acetate soluble fraction exhibiting strong anti-oxidant and anticoagulant activity was further purified by repeated silica gel and Sephadex LH-20 column chromatography. Cholesterol was isolated as one of the active principles from ethyl acetate fraction, together with, minor portion, ${\beta}-sitosterol$.

• Korean Journal of Pharmacognosy
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• v.37 no.4 s.147
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• pp.235-240
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• 2006

We investigated the antioxidant activities such as DPPH radical scavenging capacity, xanthine oxidase inhibitory activity, and superoxide radical scavenging capacity of the aqueous EtOH extract and its solvent fractions of Artemisia scoparia. The ethyl acetate fraction showed high antioxidant activity, compared to positive controls such as ascorbic acid, butylated hydroxy anisole (BHA), trolox, and allopurinol in these assay systems. Moreover, we examined the inhibitory effect of solvent fractions of A. scoparia on the production of pro-inflammatory factors that the nitric oxide (NO), inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and prostaglandin E2 $(PGE_2)$ production activated with LPS $(1{\mu}g/ml)$ in murine macrophage cell line RAW264.7. The amounts of protein levels were determined by immunoblottting. Tn the sequential fractions of hexane and dichloromethane inhibited the NO and $PGE_2$ production and the protein level of iNOS and COX-2. These results suggest that A. scoparia may have anti-inflammatory activity through the antioxidant activity and inhibition of pro-inflammatory factors.

• Korean Journal of Oriental Medicine
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• v.14 no.1
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• pp.123-128
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• 2008

Glehnia littoralis (Umbelliferae), a perennial herb distributed along the coastline of northern Pacific countries, is the medicinal plant used traditionally for treatment of various diseases. This review focuses on the various pharmacological activities of Glehnia littoralis for understanding about its traditional medicinal applications, medicinal uses in the modern society, and potentials for drug development Glehnia littoralis was reported to have anti-oxidant, anti-tumor, anti-amnesic, blood circulation-promoting, immunomodulatory, anti-microbial, and allelopathic activities. However, their mechanisms remain to be clarified. Because Glehnia littoralis has been prescribed in traditional Oriental medicine as a tonic herb, Glehnia littoralis can be better than other chemical drugs and medicines which exert the equal pharmacological activities. Although the activities of Glehnia littoralis are not specifically high-potent with unique mode of action, it may turn out that it can be beneficial to exert multiple pharmacological activities. In view of low toxicity, relative cheapness, presence in the diet, and occurrence in various herbal remedies of Glehnia littoralis, it needs to be prudent to evaluate its properties and applications further.

• Fisheries and Aquatic Sciences
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• v.17 no.3
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• pp.305-311
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• 2014

Dieckol is a polyphenol compound isolated from brown algae that has anti-oxidant, anti-inflammatory, and anti-tumor activity. We examined the anti-angiogenic effects of dieckol in endothelial cells under hypoxic conditions. Treatment with $CoCl_2$, a hypoxic mimetic agent, increased proliferation, adhesion, migration, and tube formation in HUVECs, as well as vessel sprouting in rat aortic rings, which correlated well with increased expression of hypoxia-inducible factor 1-alpha ($HIF1{\alpha}$) and ${\beta}1$-integrin. Dieckol suppressed $CoCl_2$-induced adhesion, migration, and tube formation in HUVECs and vessel sprouting in rat aortic rings. Dieckol treatment decreased $CoCl_2$-induced overexpression of $HIF1{\alpha}$ and its downstream signaling molecules, including ${\beta}1$-integrin/Fak, Akt/eNOS, and p38 MAPK. These results suggest that dieckol is a novel angiogenesis inhibitor and a potential treatment for angiogenesis-dependent diseases in humans, such as malignant tumors.

• Journal of Pharmacopuncture
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• v.20 no.3
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• pp.158-172
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• 2017

Nigella sativa (N. sativa, family Ranunculaceae) is a medicinal plant that has been widely used for centuries throughout the world as a natural remedy. A wide range of chemical compounds found in N. sativa expresses its vast therapeutic effects. Thymoquinone (TQ) is the main component (up to 50%) in the essential oil of N. sativa. Also, pinene (up to 15%), p-cymene (40%), thymohydroquinone (THQ), thymol (THY), and dithymoquinone (DTQ) are other pharmacologically active compounds of its oil. Other terpenoid compounds, such as carvacrol, carvone, 4-terpineol, limonenes, and citronellol, are also found in small quantities in its oil. The main pharmacological characteristics of this plant are immune system stimulatory, anti-inflammatory, hypotensive, hepatoprotective, antioxidant, anti-cancer, hypoglycemic, anti-tussive, milk production, uricosuric, choleretic, anti-fertility, and spasmolytic properties. In this regard, we have searched the scientific databases PubMed, Web of Science, and Google Scholar with keywords of N. sativa, anti-cancer, apoptotic effect, antitumor, antioxidant, and malignancy over the period from 2000 to 2017. The effectiveness of N. sativa against cancer in the blood system, kidneys, lungs, prostate, liver, and breast and on many malignant cell lines has been shown in many studies, but the molecular mechanisms behind that anti-cancer role are still not clearly understood. From among the many effects of N. sativa, including its anti-proliferative effect, cell cycle arrest, apoptosis induction, ROS generation, anti-metastasis/anti-angiogenesis effects, Akt pathway control, modulation of multiple molecular targets, including p53, p73, STAT-3, PTEN, and $PPAR-{\gamma}$, and activation of caspases, the main suggestive anti-cancer mechanisms of N. sativa are its free radical scavenger activity and the preservation of various anti-oxidant enzyme activities, such as glutathione peroxidase, catalase, and glutathione-S-transferase. In this review, we highlight the molecular mechanisms of apoptosis and the anti-cancer effects of N. sativa, with a focus on its molecular targets in apoptosis pathways.

• Korean Journal of Food Science and Technology
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• v.25 no.2
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• pp.160-164
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• 1993

The antioxidant activity of ethanol extracts from defatted perilla flour was investigated by measuring peroxide value of perilla oil during storage at $45^{\circ}C$. The antioxidant activity of ethanol extracts was also compared with BHA, BHT and tocopherol. Anti-oxidant activity of ethanol extracts was also examined in corn oil and lard. The ethanol extracts contents of defatted perilla flour and the original perilla seed were 7.69 and 4.56% respectively. The antioxidant activity of ethanol extracts was superior to that of 0.02% BHT, BHA and tocopherol in the perilla oil substrate, merely in concentration of one-twentieth as much as that contained in original perilla oil seeds. The fractions of non-polar solvent (hexane and chloroform) obtained from silicic acid column chromatography are less effective than that of polar solvent as an antioxidant. Antioxidant activity of partially purified ethanol fraction is slightly inferior to that of original crude ethanol extracts. Ethanol extracts were also effective in corn oil and lard almost same as in perilla oil. The total phenolic compound contents of crude ethanol extracts and partially purified ethanol fraction were 9.3, 6.4%, respectively.

• Korean Journal of Pharmacognosy
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• v.42 no.2
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• pp.195-200
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• 2011

In this study, we investigated on antioxidative activity, tyrosinase inhibitory activity and nitric oxide(NO) production inhibitory activity in the hot water extract of Taraxacum coreanum and its fractions. The total polyphenol and flavonoid contents of the extract were found to be 65.42 mg/g and 9.83 mg/g, respectively. And the total polyphenol and flavonoid contents of the ethyl acetate fraction were found to be 168.23 mg/g and 31.92 mg/g, respectively. In DPPH radical scavenging ability, $SC_{50}$ values of the ethyl acetate and butanol fraction were exhibited 64.65 ${\mu}g/ml$ and 277.42 ${\mu}g/ml$, respectively. Moreover, ethyl acetate fraction showed higher inhibitory activity than other samples in tyrosinase inhibitory activity. In NO production inhibitory activity, the extract and its fractions showed NO production inhibitory effect. Especially, the ethyl acetate, chloroform and butanol fraction was exhibited higher NO production inhibitory activity than other samples. As a result, the ethyl acetate and butanol fraction from the water extract of T. coreanum could be applicable to functional materials for skin-related fields.