• Title/Summary/Keyword: natural inhibitor

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Corrosion Inhibition of Steel by Addition of Birch Sap in Chloride Solution (염화물 수용액에서 자작나무 수액을 이용한 철강의 부식 억제)

  • Park, Tae-Jun;Kim, Ki Ae;Lee, Ji Yi;Jang, HeeJin
    • Corrosion Science and Technology
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    • v.17 no.5
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    • pp.225-230
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    • 2018
  • The effects of birch sap, a possible natural corrosion inhibitor, on the corrosion behavior of steel in chloride solution were investigated. The corrosion rate was significantly reduced by the addition of 1~5 mL of birch sap to 500 mL of 3wt% NaCl or 3wt% $CaCl_2$ solution. A remarkable increase in the pitting potential in NaCl solution was observed by the addition of birch sap although it was almost constant in $CaCl_2$ solution. The corrosion rate of steel in both NaCl and $CaCl_2$ birch sap solution without addition of water was higher compared to that of aqueous solution without birch sap as the pH of the birch sap was 4.0. The presence of organic compounds like, fructose, galactose, glucose, and palmitic acid in the birch sap are thought to be adsorbed effectively on the metal surface, which provided corrosion protection. However, the inorganic elements including Na, Ca, K, Mg, Mn, S, etc. present in the birch sap exhibited no role in corrosion inhibition.

Hesperidin Suppresses Melanosome Transport by Blocking the Interaction of Rab27A-Melanophilin

  • Kim, Bora;Lee, Jee-Young;Lee, Ha-Yeon;Nam, Ky-Youb;Park, JongIl;Lee, Su Min;Kim, Jin Eun;Lee, Joo Dong;Hwang, Jae Sung
    • Biomolecules & Therapeutics
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    • v.21 no.5
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    • pp.343-348
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    • 2013
  • We investigated the inhibitory effects of hesperidin on melanogenesis. To find melanosome transport inhibitor from natural products, we collected the structural information of natural products from Korea Food and Drug Administration (KFDA) and performed pharmacophore-based in silico screening for Rab27A and melanophilin (MLPH). Hesperidin did not inhibit melanin production in B16F10 murine melanoma cells stimulated with ${\alpha}$-melanocyte stimulating hormone (${\alpha}$-MSH), and also did not affect the catalytic activity of tyrosinase. But, hesperidin inhibited melanosome transport in melanocyte and showed skin lightening effect in pigmented reconstructed epidermis model. Therefore, we suggest that hesperidin is a useful inhibitor of melanosome transport and it might be applied to whitening agent.

Intravenous administration of piceatannol, an arginase inhibitor, improves endothelial dysfunction in aged mice

  • Nguyen, Minh Cong;Ryoo, Sungwoo
    • The Korean Journal of Physiology and Pharmacology
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    • v.21 no.1
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    • pp.83-90
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    • 2017
  • Advanced age is one of the risk factors for vascular diseases that are mainly caused by impaired nitric oxide (NO) production. It has been demonstrated that endothelial arginase constrains the activity of endothelial nitric oxide synthase (eNOS) and limits NO generation. Hence, arginase inhibition is suggested to be vasoprotective in aging. In this study, we examined the effects of intravenous injection of Piceatannol, an arginase inhibitor, on aged mice. Our results show that Piceatannol administration reduced the blood pressure in aged mice by inhibiting arginase activity, which was associated with NO production and reactive oxygen species generation. In addition, Piceatannol administration recovered $Ca^{2+}$/calmodulin-dependent protein kinase II phosphorylation, eNOS phosphorylation and eNOS dimer stability in the aged mice. The improved NO signaling was shown to be effective in attenuating the phenylephrine-dependent contractile response and in enhancing the acetylcholine-dependent vasorelaxation response in aortic rings from the aged mice. These data suggest Piceatannol as a potential treatment for vascular disease.

Hepatoprotective Activity of Chungpesagan-tang is Related to the Inhibition of ${\beta}-Glucuronidase$

  • Kim, Jae-Kwan;Bae, Hyung-Sup;Kim, Young-Suk;Cho, Ki-Ho;Lee, Kyung-Sup;Lee, Hae-Ung;Kim, Dong-Hyun
    • Natural Product Sciences
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    • v.7 no.3
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    • pp.63-67
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    • 2001
  • ${\beta}-Glucuronidase-inhibitory$ and hepatoprotective effects of Chungpesagan-tang, which has been used for liver diseases and stroke, on $CCl_4-induced$ hepatotoxicity of rats was investigated. Chungpesagan-tang potently inhibited ${\beta}-glucuronidases$. Serum AST, ALT and LDH levels of the $CCl_4$ group orally treated with Chungpesagan-tang (100 mg/kg) were lowered to 47, 28 and 58% of the $CCl_4-treated$ group, respectively. Among the ingredients of Chungpesagan-tang, Puerariae Radix, Scutellariae Radix and Rhei Rhizoma potently inhibited the ${\beta}-glucuronidase$ and protected $CCl_4-induced$ liver injury. The hepatoprotective activity of Puerariae Radix was affected by ingredients of Chungpesagan-tang: Scutellariae Radix had the synergistic activity, but Angelicae Tenussimae Radix exhibited the antagonistic activity. These results suggest that the ${\beta}-glucuronidase$ inhibitor of herbal medicines may protect $CCl_4-induced$ liver injury and puerarin should be a natural prodrug for the hepatoprotective effect.

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SYNTHETIC DEVELOPMENT OF NEW 1$\beta$-SUBSTITUTED CARBAPENEMS

  • Nagao, Yoshimitsu
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.34-35
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    • 1993
  • The Development of new asymmetric induction methods useful for syntheses of biologically active natural products and drugs, using C4-chiral 1,3-th-iazolidine-2-thiones, has been a recent focus of interest. 1-8) The present account describes the significance of particular heterocycles in the synthetic development of new 1${\beta}$-substituted carbapenems. A fungal metabolite, (+)-thienamycin (1) has attracted one's attention as a hopeful candidate for new-generation antibiotic drugs because of its strong antimicrobial activities and wide antimicrobial spectra due to the extensive inhibition against various ${\beta}$-lactamases. However, it has been serious problems toward a practically useful drug that (+)-thienamycin is fairly labile in the solution and can be metabolized by renal dehydropept- idase-I (DHP-I). Recently, a Merck Sharp & Dohme research group exploited a non-natural ${\beta}$-lactam, imipenem (2) which has been appeared in the drug market as the first carbapenem-type antibiotic drug. 9) However 2 must be used with a DHP-I inhibitor, cilastatin sodium (3).9) Thus, a 1,${\beta}$-methyl- carbapenem derivative 4 has been disclosed by the same group. 10) It seems to be more hopeful candidate as a new-generation antibiotic because it can directly resist against metabolism by the renal DHP-1 without an enzyme inhibitor 3. 10)

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Effect of Staurosporine on the Long-term Secretion of Catecholamines Induced by Various Secretagogues in Cultured Bovine Adrenal Medullary Chromaffin Cells

  • Choi, Seong-Soo;Suh, Hong-Won
    • The Korean Journal of Physiology and Pharmacology
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    • v.5 no.6
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    • pp.503-510
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    • 2001
  • Long-term treatment of cultured bovine adrenal medullary chromaffin (BAMC) cells with arachidonic acid $(100\;{\mu}M),$ angiotesnin II (100 nM), prostaglandin $E_2\;(PGE_2;\;10\;{\mu}M),$ veratridine $(2\;{\mu}M)$ or KCl (55 mM) for 24 hrs increased both norepinephrine and epinephrine levels in the supernatant. Pretreatment with staurosporine (10 nM), a protein kinase C (PKC) inhibitor, completely blocked increases of norepinephrine and epinephrine secretion induced by arachidonic acid, angiotensin II, $PGE_2,$ veratridine or KCl. In addition, K252a, another PKC inhibitor whose structure is similar to that of staurosporine, effectively attenuated both norepinephrine and epinephrine secretion induced by arachidonic acid. However, K252a did not affect the catecholamine secretion induced by angiotensin II, $PGE_2,$ veratridine or KCl. Our results suggest that staurosporine may inhibit long-term catecholamine secretion induced by various secretagogues in a mechanism other than inhibiting PKC signaling. Furthermore, long-term secretion of catecholamines induced by arachidonic acid may be dependent on PKC pathway.

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An Electrochemical Study on the Effect of Salt Affecting to Corrosion Behavior of Concrete Reinforced Steel in Natural Sea Water (천연해수에 침지된 콘크리트 내부의 철근부식거동에 미치는 염분의 영향에 관한 전기화학적 연구)

  • 김광근;류보현;점성종;김기준;문경만
    • Journal of Ocean Engineering and Technology
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    • v.14 no.4
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    • pp.23-29
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    • 2000
  • When the concrete structures were being made with sand containing chloride ion it was knows that corrosion rate of reinforced steel embedded in concrete with chloride ion was higher than that of concrete with on chloride ion. In this study, the operation of Friedel salts affecting the corrosion behavior of reinforced steel embedded in cement mortar was investigated with electrochemical view. Corrosion potential of reinforced steel embedded in cement mortar with sand containing chloride ion was shifted noble direction than that of cement mortar with no chloride ion after immersed 5 month in natural sea water and also corrosion current density decreased with shifting corrosion potential to noble direction. However Friedel salts appeared from surface to 2.5cm of inside direction of mortar specimen, which is located at 11.5$\circ$(2$\theta$) in XRD analysis and the amount of Ca(OH)2 by SEM photograph in cement mortar with chloride ion was larger than that of cement mortar with mo chloride ion. Eventually it is suggested that Friedel salts was resulted from chloride ion and it acted as the corrosion inhibitor.

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Phenotypic Alterations in Transgenic Tobacco Plants that Overproduce Cytokinins (Cytokinins overproduction에 따른 담배형질전환체의 변화)

  • Chung, Yong-Yoon
    • The Journal of Natural Sciences
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    • v.10 no.1
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    • pp.33-37
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    • 1998
  • Cytokinin is one of major growth regulators in plants. In this study, the gene isopentenyl transferase (jpt) which encodes a key enzyme involved in the biosynthesis of the growth regulator cytokinin isolated from Agrobacterium tumefaciens was introduced ito tobacco plant via Agrobacterium-mediated transformation. The jpt gene was modulated using the proteinase inhibitor II (PI-IIK) promotor. In general, this promoterlipt gene fusion resulted in overproduction of cytokinins throughout the transgenic plants. The overproduction of cytokinin caused dramatic changes in morphology of the plant, including stem thickness and reduced root development. The studies reported in this paper were initiated to examine the consequences of overproduction of cytokinin in plant.

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Free fatty acid-induced histone acetyltransferase activity accelerates lipid accumulation in HepG2 cells

  • Chung, Sangwon;Hwang, Jin-Taek;Park, Jae Ho;Choi, Hyo-Kyoung
    • Nutrition Research and Practice
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    • v.13 no.3
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    • pp.196-204
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    • 2019
  • BACKGROUND/OBJECTIVES: Non-alcoholic fatty liver disease (NAFLD) is a common metabolic disease triggered by epigenetic alterations, including lysine acetylation at histone or non-histone proteins, affecting the stability or transcription of lipogenic genes. Although various natural dietary compounds have anti-lipogenic effects, their effects on the acetylation status and lipid metabolism in the liver have not been thoroughly investigated. MATERIALS/METHODS: Following oleic-palmitic acid (OPA)-induced lipid accumulation in HepG2 cells, the acetylation status of histone and non-histone proteins, HAT activity, and mRNA expression of representative lipogenic genes, including $PPAR{\gamma}$, SREBP-1c, ACLY, and FASN, were evaluated. Furthermore, correlations between lipid accumulation and HAT activity for 22 representative natural food extracts (NExs) were evaluated. RESULTS: Non-histone protein acetylation increased following OPA treatment and the acetylation of histones H3K9, H4K8, and H4K16 was accelerated, accompanied by an increase in HAT activity. OPA-induced increases in the mRNA expression of lipogenic genes were down-regulated by C-646, a p300/CBP-specific inhibitor. Finally, we detected a positive correlation between HAT activity and lipid accumulation (Pearson's correlation coefficient = 0.604) using 22 NExs. CONCLUSIONS: Our results suggest that NExs have novel applications as nutraceutical agents with HAT inhibitor activity for the prevention and treatment of NAFLD.

A Tubulin Inhibitor, N-(5-Benzyl-1,3-thiazol-2-yl)-3-(furan-2-yl)prop-2-enamide, Induces Anti-inflammatory Innate Immune Responses to Attenuate LPS-mediated Septic Shock

  • Park, Hyun Jung;Lee, Sung Won;Park, Hwangseo;Park, Se-Ho;Hong, Seokmann
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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    • pp.3307-3312
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    • 2014
  • The anti-inflammatory effect of a tubulin inhibitor, N-(5-benzyl-1,3-thiazol-2-yl)-3-(furan-2-yl)prop-2-enamide (1), on innate immune responses remains unclear. Thus, we investigated the effect of 1 on the immune responses mediated by lipopolysaccharide (LPS). The in vitro addition of 1 to dendritic cells and macrophages dose-dependently reduced tumor necrosis factor alpha production elicited by LPS stimulation. Additionally, the stimulation of natural killer (NK) and natural killer T (NKT) cells with 1 resulted in the decrease of interferon gamma ($IFN{\gamma}$) induced by LPS treatment. Moreover, 1 substantially reduced interleukin 12 in dendritic cells (DC) as well as $IFN{\gamma}$ in NKDCs induced by LPS in vitro. Furthermore, the in vivo administration of 1 ameliorated LPS/D-galactosamine-induced endotoxic lethality in mice. Taken together, our results demonstrate for the first time that 1 possesses anti-inflammatory properties, most notably by modulating LPS-induced innate immune responses. Therefore, 1 might have therapeutic potential for the treatment of inflammation-mediated diseases such as sepsis.