• Title/Summary/Keyword: inhibitory compounds

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Effect of Evodiae fructus Methanol Extract on Virulence-Related Genes' Expression of Helicobacter pylori (오수유 메탄올 추출물이 Helicobacter pylori 병원성 관련 유전자 발현에 미치는 영향)

  • Yang, Ji Yeong;Lee, Pyeongjae;Kim, Jong-Bae
    • Korean Journal of Clinical Laboratory Science
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    • v.51 no.3
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    • pp.316-322
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    • 2019
  • Helicobacter pylori, a gram-negative bacterium, is one of the risk factors that induces gastritis and gastric cancer. Therefore, much attention has been paid to the compounds that inhibit bacterial growth or eradicate bacteria. Evodiae fructus (EF), the fruit of Evodia rutaecarpa, has been used for treating diarrhea and abdominal pain. EF extract was already found to inhibit the growth of H. pylori. However, to the best of our knowledge, the effect of EF on the virulence factors of H. pylori has not been reported. In this study, when comparing the minimum inhibitory concentration (MIC) of the different methanol concentration extracts, the 95% methanol extract (EF95) showed the lowest MIC value. EF95 extract suppressed the expressions of cagA, vacA and ureB, but interestingly, it up-regulated the expression of ureA. A decrease in production of ammonia in the culture medium and the cell lysates indicated that EF95 inhibited the urease activity in H. pylori, which was the result of EF95 inhibiting the ureB expression. Although the mechanism by which EF95 extract regulates the virulence factors in H. pylori needs further study, EF95 could be used for treatment of gastric troubles induced by H. pylori.

Antioxidative Effect of Phrymaleptostachyavar. Asiatica HARA Extract on the Neurotoxicity of Aluminum Sulfate, Environmental Pollutant (환경오염물질인 황산알루미늄의 신경독성에 대한 파리풀 추출물의 항산화 효과)

  • Yoo, Sun-Mi;Lee, Jun-Hee
    • Korean Journal of Clinical Laboratory Science
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    • v.51 no.2
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    • pp.235-244
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    • 2019
  • This study examined the neurotoxicity of aluminum sulfate (AS), an environmental pollutant, and the protective effect of Phrymaleptostachya var. asiatica HARA (PLVAH) extract on the neurotoxicity induced by AS in the cultured C6 glioma cells. For this study, the cell viability and antioxidative effects, such as electron donating (ED) activity, lipid peroxidation (LP) activity, and superoxide anion-radical (SAR) scavenging activity, were analyzed. AS decreased the cell viability significantly in a dose-dependent manner and the $XTT_{50}$ value was measured at $120.0{\mu}M$ of AS. The neurotoxicity of AS was determined to be mid-toxic by Borenfreund and Puerner's toxic criteria. In addition, the catalase (CAT), antioxidant enzyme remarkably increased the cell viability injured by AS-induced neurotoxicity in these cultures. Regarding the protective effect of the PLVAH extract on AS-induced neurotoxicity, PLVAH extract significantly increased the ED ability, and the inhibitory ability of the LP and SAR scavenging ability. These findings suggest that oxidative stress is involved in the cytotoxicity of AS, and the PLVAH extract effectively protected against AS-induced neurotoxicity by its antioxidative effects. Natural resources, such as the PLVAH extract may be a putative therapeutic agent for the treatment of the toxicity induced by heavy metallic compounds, such as AS correlated with the oxidative stress.

Immunomodulatory Effects of Euglena gracilis Extracts (Euglena gracilis 추출물의 면역조절 및 생리활성 분석)

  • Yu, Sun Nyoung;Park, Bo Bae;Kim, Ji Won;Hwang, You Lim;Kim, Sang Hun;Kim, Sunah;Lee, Taeho;Ahn, Soon Cheol
    • Journal of Life Science
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    • v.31 no.2
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    • pp.183-191
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    • 2021
  • Euglena gracilis is a microalga of great biotechnological interest that can create high levels of bioactive compounds, such as tocopherol, paramylon, and folic acid. The objective of this study was to investigate the biological activities of extracts from E. gracilis, especially those focused on immunological activity. E. gracilis biomass was extracted with hot water (HWE) and the remaining pellet was continuously extracted with methanol (HWME). First, we examined the effect of two extracts from E. gracilis on the production of nitric oxide (NO) and the expression of pro-inflammation cytokines, including IL-1β, IL-6, and TNF-α in murine macrophage RAW 264.7 cells. HWE treatment dose-dependently increased the production of IL-1β and TNF-α. On the other hand, treatment with HWME significantly decreased the generation of NO and pro-inflammatory cytokines (IL-6 and TNF-α) in lipopolysaccharide (LPS)-stimulated macrophage cells. In addition, other biological activities of the extracts were further analyzed: α-glucosidase inhibition, protein tyrosine phosphatase (PTP1B) inhibition, tyrosinase inhibition, xanthine oxidase (XO) inhibition, and angiotensin-converting enzyme (ACE) inhibition. Analysis of these biological activities showed that HWE has more inhibitory effects than HWME against α-glucosidase, tyrosinase, and XO agents. However, the inhibition of PTP1B and ACE with HWME were higher than with HWE. Taken together, the results suggested that E. gracilis possesses various biological activities―especially immunological capabilities―through regulation of cytokine production. Therefore, E. gracilis extract may be potentially useful for food material with immune-regulating effects.

Gossypii Semen oil alleviates memory dysfunction in scopolamine-treated mice (면화자 정유의 기억력 손상 완화 효과)

  • Lee, Jihye;Jung, Eun Mi;Lee, Eunhong;Jang, Gwi Yeong;Seo, Kyung Hye;Kim, Mi Ryeo;Jung, Ji Wook
    • The Korea Journal of Herbology
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    • v.36 no.2
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    • pp.1-9
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    • 2021
  • Objectives : Gossypium arboreum (cotton) is traditionally used to treat various health disorders. However, anti-amnesic effect of G. arboreum has not been reported. The objective of this study was to investigate in-vivo the anti-amnesic effects along with in vitro antioxidant and acetylcholinesterase (AChE) inhibition potential in G. arboreum seed essential oil. Methods : The essential oil of G. arboreum obtained by solid phase microextraction (SPME) techniques were identified by gas chromatography-mass spectroscopy (GC-MS). 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay were performed to determine the antioxidant activity at various concentrations (312.5, 625, 1250, 2500, 5000, 10000 ㎍/㎖. Y-maze, passive avoidance and Morris water maze tests were carried out to evaluate improved effect on scopolamine (1 mg/kg)-induced memory dysfunction at the dose level of 50, 100 and 200 mg/kg. Donepezil (5 mg/kg) was used as a positive drug control. We performed acetylcholinesterase (AChE) activity assay in ex vivo. Results : Five volatile compounds were identified in G. arboreum. The assays of DPPH and ABTS revealed that G. arboreum increased antioxidant activity in a dose-dependent manner. G. arboreum ameliorated the percent of spontaneous alternation in the Y-maze test, shortened step-through latency in the passive avoidance test, and increased swimming time in the target zone in the Morris water maze test. In addition, G. arboreum inhibited the AChE activity. Conclusions : Based on these findings, G. arboreum may aid in the prevention and treatment of learning and memory-deficit disorders through antioxidant and AChE inhibitory activities.

Comparison of Antioxidant and Anti-inflammatory Activity of Korean Houttuynia cordata Thunb. Extracts (국내산 어성초(Houttuynia cordata Thunb.)추출물의 항산화 및 항염증 활성 비교)

  • Lim, Hyun-Ji;Lee, Hea-Jin;Lim, Mi-Hye
    • Journal of the Korean Applied Science and Technology
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    • v.38 no.1
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    • pp.217-227
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    • 2021
  • In this study, Korean-cultivated Houttuynia cordata Thunb. (HC) was extracted anti-inflammatory effects of extracts were compared in order to confirm the possibility of natural cosmetics as a raw material. HPLC pattern analysis, cell viability assay, total phenolic contents, ABTS/DPPH radical scavenging analysis, measurement of ROS production, griess reagent assay, and luminex technique. The content of quercetin was higher in fresh Houttuynia cordata (HC-F) than in dried Houttuynia cordata (HC-D). Also, content of HC extracts shows a difference in the content of the two representative compounds (polyphenol and flavonoid) according to the stored differently. ROS production showed higher inhibitory rates at HC-F. The anti-inflammatory activity of HC-D was shown higher than that of HC-F. But, in the measurement of the reduction in inflammatory cytokines, IL-1β showed that HC-D had a relatively high reduction effect, and IL-6 and TNF-α showed a high reduction effect. And these results will be a basis for the development of cosmetology in skin care and improvement of skin problem.

Anti-oxidation and Anti-thrombosis Activities of Polyphenol-enriched Fraction of Acorn Pollen Extract (도토리 화분 추출물의 폴리페놀 고함유 분획물의 항산화 및 항혈전 활성)

  • Lee, Yun-Jin;Kang, Deok-Gyeong;Pyo, Su-Jin;Sohn, Ho-Yong
    • Journal of Life Science
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    • v.32 no.7
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    • pp.501-509
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    • 2022
  • Pollen corrected from Quercus species is abundant in Korea and has been used to treat anemia and inflammation of the prostate gland. It is also used for hemostasis in oriental medicine. In this study, the ethanol extract of the acorn pollen and its subsequent organic solvent fractions using hexane, ethylacetate, butanol, and water residue were prepared, and their antioxidant, anti-thrombosis, and hemolysis activities were evaluated. The ethylacetate fraction of acorn pollen (EF-AP) showed the highest polyphenol content (225.0 mg/g) and strong antioxidant activity among the solvent fractions. The RC50 of EF-AP against DPPH, ABTS, and nitrite radicals was 72.2, 27.7, and 62.6 ㎍/ml, respectively. The blood coagulation activities of the all-solvent fractions determined by thrombin time, prothrombin time, and activated partial thromboplastin time were negligible up to 5 mg/ml. Platelet aggregation inhibitory activities were observed in the EF-AP, butanol fraction, and water residue, whereas hexane fraction induced strong platelet aggregation. The EF-AP has no hemolysis activity against human RBC up to 1 mg/ml. UPLC/MS/MS analysis of the EF-AP revealed that rutin, isoquercitrin, and astragalin are major compounds for antioxidant and anti-thrombosis activities. Our results suggest that EF-AP could be developed as a noble antioxidant and anti-thrombosis agent.

Production of PMA-induced MMP-2 and MMP-9 in the HT-1080 Fibrosarcoma Cell Line is Inhibited by Corydalis heterocarpa via the MAPK-related Pathway (PMA로 자극된 HT-1080 세포에서 염주괴불주머니 추출물의 MAPK 경로를 통한 MMP-2, MMP-9 발현 억제 효과)

  • Yu, Ga Hyun;Karadeniz, Fatih;Oh, Jung Hwan;Kong, Chang-Suk
    • Journal of Life Science
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    • v.32 no.1
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    • pp.51-55
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    • 2022
  • Matrix metalloproteinase (MMP) enzymes are responsible for the degradation and formation of the extracellular matrix (ECM), and overproduction of MMPs is observed in several diseases, such as cancer and asthma, that progress with metastatic characteristics. Natural products, especially phytochemicals, have been an important source of MMP inhibitors with reduced side effects. Although the majority of phytochemicals inhibit the enzymatic activity of MMPs, some suppress MMP production. In this context, the current study evaluated the potential of Corydalis heterocarpa, a halophyte with reported bioactivities, to inhibit MMP expression in PMA-stimulated HT-1080 cells. A crude C. heterocarpa extract was shown to decrease the mRNA and protein expression of MMP-2 and MMP-9 while increasing the endogenous MMP inhibitors TIMP-1 and TIMP-2 which regulate MMP expression in healthy tissues. In addition, our results show that the inhibitory effects of C. heterocarpa might occur through suppression of the phosphorylation of MAPK signaling, the upstream activator of MMP overexpression. In conclusion, C. heterocarpa is a potential source of antimetastatic compounds that might serve as lead molecules to develop novel MMP inhibitors.

Anti-inflammatory Effects of Epimedii Herba Water Extract through Inhibition of Nuclear Factor-κB in RAW 264.7 Cells (RAW 264.7 세포에서 음양곽(淫羊藿) 물 추출물의 nuclear factor-κB 억제를 통한 항염증 효과)

  • Jung, Ji Yun;Byun, Sung Hui;Park, Chung A;Cho, Il Je;Kim, Sang Chan
    • The Korea Journal of Herbology
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    • v.33 no.2
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    • pp.19-28
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    • 2018
  • Objectives : Epimedii Herba has been frequently used in Korean Traditional Medicine to treat impotence, spermatorrhoea, exophthalmos, and forgetfulness. Present study investigated anti-inflammatory effects of Epimedii Herba water extract (EWE) and attempted to elucidate molecular mechanisms involved. Methods : To explore anti-inflammatory effects of EWE, RAW 264.7 cells, a murine macrophage cell line, were pretreated with $10-100{\mu}g/m{\ell}$ of EWE, and then subsequently exposed to $1{\mu}g/m{\ell}$ of lipopolysaccharide (LPS). Levels of nitric oxide (NO), interleukin-6, $interleukin-1{\beta}$, and tumor necrosis $factor-{\alpha}$ were monitored in the medium. Expression levels of inducible nitric oxide synthase and cyclooxygenase-2 were determined by immunoblot and real-time PCR analyses. Signaling pathways related with nuclear $factor-{\kappa}B$ ($NF-{\kappa}B$) and mitogen-activated protein kinases were monitored to elucidate molecular mechanisms involved. Finally, the role of three flavonoid compounds in EWE on LPS-mediated NO production were investigated. Results : In conditioned medium, pretreatment of EWE ($100{\mu}g/m{\ell}$) significantly inhibited LPS-stimulated NO and pro-inflammatory cytokine production. In addition, EWE attenuated the expressions of inducible nitric oxide synthase and cyclooxygenase-2 by LPS. EWE prevented the phosphorylation and degradation of inhibitory ${\kappa}B{\alpha}$, nuclear translocation of $NF-{\kappa}B$, and DNA binding of $NF-{\kappa}B$, while EWE did not change the phosphorylation of mitogen-activated protein kinases by LPS. Moreover, icariin, icaritin, and quercetin partly, but significantly, inhibited the LPS-stimulated NO production. Conclusions : These results suggest that EWE has an ability to prevent inflammation in macrophages through inhibition of $NF-{\kappa}B$ signaling pathway.

Depigmenting Effects of Mistletoe (Viscum album var. coloratum) Extracts (겨우살이 추출물의 미백 효과)

  • Hah, Young-Sool;Kim, Eun-Ji;Goo, Young Min;Kil, Young Sook;Sin, Seung Mi;Kim, Sang Gon;Kang, Ha Eun;Yoon, Tae-Jin
    • Journal of Life Science
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    • v.32 no.5
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    • pp.355-361
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    • 2022
  • Melanin pigments are the main cause of skin color. They are produced in melanocytes and then transferred to keratinocytes, which eventually gives the skin surface a variety of colors. Although many skin-lightening or depigmenting agents have been developed, the demand for materials to reduce pig- mentation is still increasing. Here, we tried to find materials for skin-lightening or depigmentation using natural compounds and found that mistletoe (Viscum album var. coloratum) extracts (ME) had an inhibitory effect on tyrosinase activity. As a result, ME significantly reduced pigmentation in human primary melanocytes. In addition, a promoter reporter assay revealed that ME inhibited the transcription of microphthalmia-associated transcription factor (MITF), melanophilin (MLPH), tyrosinase-related protein-2 (TRP-2), and tyrosinase (TYR) genes in HM3KO melanoma cells. In addition, ME decreased the protein level for pigmentation-related molecules, such as TYR and TRP-1. Furthermore, it markedly inhibited the melanogenesis of zebrafish embryos, an in vivo evaluation model for pigmentation. To elucidate the action mechanism of ME, we investigated its effects on intracellular signaling. Eventually, the ME dramatically decreased the phosphorylation of the cAMP responsive element binding protein (CREB), AKT, and ERK. The data suggest that ME may inhibit the melanogenesis pathway by regulating the signaling pathway related to pigmentation. Taken together, these data propose that ME can be developed as a depigmenting or skin-lightening agent.

Synthesis of 1,2-Dodecylaminopropanediol and Its Mixing Effect with 1,2-Alkanediols as Preservatives (보존제로서 1,2-도데실아미노프로판디올의 합성 및 1,2-알칸디올 화합물의 혼합 효과)

  • Cha, Kyung-On;Kwak, Sang-Woon;Jeong, Kook-In;Kim, Young-Ho
    • Applied Chemistry for Engineering
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    • v.33 no.2
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    • pp.179-187
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    • 2022
  • In this study, the synthesis of 1,2-dodecylaminopropanediol (1,2-DDAP) having a 12 carbon chain length and an amine group was designed to improve the preservation and hydrophilicity of 1,2-alkanediol-based compounds. 1,2-DDAP was prepared by reacting dodecylamine (DDA) with 3-monochloro-1,2-propanediol (3-MCPD) in an ethanol solvent at 40 ℃, and its yield and purity were about 56% and 98%, respectively, under a reaction condition of 2 h and a DDA:3-MCPD molar ratio of 1:0.8. The antimicrobial effect of 1,2-DDAP showed the values of the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against microorganisms at concentrations of 10 to 100 times lower than those of 1,2-octanediol(1,2-ODIOL) or 1,2-decanediol (1,2-DDIOL). Based on the hydrophilic properties of 1,2-DDAP, mixed preservatives were prepared by adding small amounts of 1,2-ODIOL or 1,2-DDIOL, which are poorly soluble in water, with 1,2-DDAP. Mixed preservatives exhibited an effect of inhibiting microorganisms equal to or greater than that of 1,2-DDAP alone in antimicrobial activity tests. As a result of confirming the preservation effect in lotion (cosmetic formulation) for application, 1,2-DDAP showed similar antimicrobial activity at concentrations of 0.3 to 0.6 times lower than that of 1,2-ODIOL or 1,2-DDIOL. Therefore, it is considered that the use of 1,2-DDAP alone and the mixed use with small amounts of 1,2-ODIOL or 1,2-DDIOL can be a good alternative to preservatives in the product.