• Title/Summary/Keyword: $\mu$ synthesis

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Stimulatory Effect of Ginsenosides on $pp60^{c-src}$ Protein Tyrosine Kinase

  • Hong, Hee-Youn;Park, Seon-Yang;Lee, Seung-Ki;Yoo, Gyurng-Soo;Choi, Jung-Kap
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.114-117
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    • 1993
  • Ginsenosides present in the roots of panax ginseng C.A. Meyer were shown to induce a stimulatory effect on the overexpressed cellular chicken c-src protein tyrossine kinase in NH3T3 cells. Among 4 ginsenosides studied $(G-Rb_2,\;G-Rc,\;G-Re\;and\;G-Rg_1),\;G-Rg_1$ showed the most stimulatory effect at $16.7\mu{g/ml}$ ginsenoside concentration increasing the activity by 2-4 times. Inhibitors of either protein synthesis or RNA synthesis blocked the activation of c-src proein tyrosine kinase. These results suggest that the csrc kinase activation apprars to involve an increase in the amount of protein of the kinase by transcriptional control mechanism rather than an increase in the kinase activity.

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Inhibitory effects of Thalictrum rochebrunianum var. grandisepalum on tyrosinase in IBMX-induced B16F10 melanoma cells

  • Jang, Tae-Won;Choi, Ji-Soo;Mun, Jeong-Yun;Im, Jong-Yun;Nam, Su-Hwan;Kim, Do-Wan;Lee, Seung-Hyun;Park, Jae-Ho
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2019.04a
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    • pp.116-116
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    • 2019
  • Thalictrum rochebrunianum var. grandisepalum (TRG) is a Korean endemic plant, and it is widely used for edible, medicinal, landscape materials. In this study, we examined the protein and mRNA expression levels of MITF, tyrosinase, TRP-1 and TRP-2 by TRG extract (TRGE) in IBMX-treated melanocytes to evaluate the possibility of using TRG as a whitening material. IBMX were reported as melanin synthesis enhancers. It could increase intracellular melanin synthesis by activation of the microphthalmia-associated transcription factor (MITF) signaling pathway. TRGE did not show cytotoxicity at concentrations below $100{\mu}g/ml$ in B16F10 cells. TREG dose-dependently inhibited protein and mRNA levels of MITF, tyrosinase, TRP-1 and TRP-2. Therefore, we suggest that TRGE is an important natural resource for cosmetic raw materials for whitening function.

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Synthesis and COX-2 Inhibitory Properties of Luotonin A Homologues

  • Park, Jae-Gyu;Kim, Dong-Hyun;Rahaman-A.F.M.Motiur;Chang, Hyeun-Wook;Lee, Eung-Seok;Jahng, Yurng-Dong
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.172.1-172.1
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    • 2003
  • Luotonin A was isolated from Peganum nigellastrum Bunge (Zygophyllaceae) which was named Luo-Tuo-Hao in China and used as a Chinese traditional medicine for the treatment of rheumatism, abscess, and inflammation. The basic fractions of P. nigellastrum showed antitumor activtity, and the origin of such an activity was recently revealed by identifying its constituent luotonin A which inhibited the growth of leukemia P-388 cells ($IC_50$ = 1.8 $\mu$g/mL). Such an intriguing properties of luotonin A led developments of efficient methods for total synthesis. (omitted)

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Synthesis of Benzo[c]phenanthridine Derivatives and their in Vitro Antitumor Activities

  • Cho, Won-Jea;Yoo, Su-Jeong;Chung, Byung-Ho;Choi, Bo-Gil;Cheon, Seung-Hoon;Whang, Soon-Ho;Kim, Sin-Kyu;Kang, Boo-Hyon;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.19 no.4
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    • pp.321-325
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    • 1996
  • Aiming at the development of anticancer agents by modification of phenolic benzo[c]phenanthridine alkaloid, additional hydroxyl group was put on C10 position of fagaridine (1) by a biomimetic synthetic procedure to afford 10-hydroxyfagaridine (12). All of the synthetic intermediates were also screened in vitro antitumor activities against five different cell lines as well as 12. Among them the representative cytotoxic results are shown as follows; P-quinone (11) $[ED_50;(A549=0.22; {\mu}g/ml)$, $(HCT;15=0.21 {\mu}g/ml)$, fagaridine (1) $(HCT;15=0.41 {\mu}g/ml)$, olefin (6) $(HCT; 15=0.06 {\mu}g/ml)$, acetal (7) $(SKMEL-2=0.07 {\mu}g/ml)$, dihydrofagaridne (10) $(A549=0.38 {\mu}g/ml)$, 10-hydroxyfagaridine (12) $(A 549=0.45{\mu}g/mi)$. From these observation three main remarks can be drawn; (i) the iminium part of benzo[c]phenanthridine is not essential for showing acitvities, (ii) the additional hydroxyl group did not contribute to enhance the cytotoxicity, (iii) the 3-arylisoquinolin-1(2H)-one derivatives were found to display significant in vitro antitumor activity.

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Effects of Nicotine on mineralization in human fetal osteoblasts (니코틴이 사람태아골모세포의 광물화 과정에 미치는 영향)

  • Lim, Sung-Woo;Han, Sang-Heon;Lee, Seong-Jin;You, Suk-Joo;Shin, Hyung-Shik;You, Hyung-Keun
    • Journal of Periodontal and Implant Science
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    • v.33 no.4
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    • pp.729-738
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    • 2003
  • Nicotine is one of the major components of cigarette smoking which causes various systemic and local diseases to human body. The purpose of the present study was to investigate the effects of nicotine on bone mineralization in human fetal osteoblasts cell line(hFOB1). To compare the alkaline ph-osphatase(ALP) synthesis, hFOBl were cultured with DMEM/F-12 1:1 Mixture and 100 pg/ml, 1 ng/ml, 10 ng/ml, 100 ng/ml, 1 ${\mu}g$/ml, 10 ${\mu}g$/ml, 100 ${\mu}g$/ml of nicotine. And to compare the calcium accumulation, hFOB1 cultured for 23 days were quantified and photographed. ALP activity of hFOB1 exposed to nicotine was not significantly changed at a lower concentrations of nicotine, but was significantly decreased at a higher concentrations (10 ${\mu}g$/ml, 100 ${\mu}g$/ml) of nicotine (p<0.05). A quantified calcium acculation in hFOB1 was significantly decreased at 1,10, and 100${\mu}g$/ml of nicotine (p<0.05). Significantly decreased calcium deposition was observed at 1, 10, and 100${\mu}$/ml of nicotine. These results indicate that a higher concentration of nicotine show a negative effects on mineralization of hFOB1.

Characterization and Electron Microscopic Visualization of the Plasmid and the Gene Expression in the Escherichia coli (E. coli의 유전자 발현 및 플라스미드 DNA 구조의 특성에 관한 연구)

  • Kim, Sung-Jun;Park, Yeal;Lee, Sook-Young;Kim, Hong-Seob;Kim, Woo-Kap
    • Applied Microscopy
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    • v.20 no.2
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    • pp.57-70
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    • 1990
  • Characterization and electron microscopic visualization of the plasmid and the gene expression of Escherichia coli were carried out. Transcriptional units of active structural genes were observed after lysis of Escherichia coli cells. The ribosomes attached to the E. coli genome on mRNA molecule as polyribosomes. From this gradient of polyribosome length, we estimated location of mRNA synthesis initiation site. In this experiment, a granule is ofen present which may correspond to a RNA polymerase at the promoter site. pOX1, pOX7, pOX7A, $pOX7{\Delta}1$, pSTP36, pSTP21, pBR322, and pJH12 were visualized by way of electron microscope, and their estimated sizes were determined to be $5.70{\pm}0.08{\mu}m,\;2.15{\pm}0.10{\mu}m,\;2.14{\pm}0.12{\mu}m,\;7.39{\pm}0.08{\mu}m,\;4.03{\pm}0.04{\mu}m,\;1.50{\pm}0.03{\mu}m\;and\;1.25{\pm}0.09{\mu}m$ respectively. One micrometer of measured length corresponded to about 3.0 Kb. Mica-press adsorption method that allows selectivs visualization of the plasmid DNA released in situ from the bacterial cell is rapid and useful for visualization of plasmids. The released plasmid DNA was adsorbed preferently on mica in a divalent cation-free solution. Miller chromatin-spreading method was useful to observe the plasmid and transcripts. BAC method and cytochrome C monolayer were useful to observe the plasmid DNA. Our ability to visualize ultrastructural aspects of the expression of E. coli has given us a unique tool with which to study the regulation the level of an individual gene.

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Anti-Proliferation Effects of Benzimidazole Derivatives on HCT-116 Colon Cancer and MCF-7 Breast Cancer Cell Lines

  • Al-Douh, Mohammed Hadi;Sahib, Hayder B.;Osman, Hasnah;Hamid, Shafida Abd;Salhimi, Salizawati M.
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.8
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    • pp.4075-4079
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    • 2012
  • Benzimidazoles 1-4 were obtained using modified synthesis methods and studied for their ability to inhibit cell proliferation of colon cancer cell HCT-116 and breast cancer cell MCF-7 using MTT assays. In the HCT-116 cell line, benzimidazole 2 was found to have an $IC_{50}$ value of $16.2{\pm}3.85{\mu}g/mL$ and benzimidazole 1 a value of $28.5{\pm}2.91{\mu}g/mL$, while that for benzimidazole 4 was $24.08{\pm}0.31{\mu}g/mL$. In the MCF-7 cell line, benzimidazole 4 had an $IC_{50}$ value of $8.86{\pm}1.10{\mu}g/mL$, benzimidazole 2 a value of $30.29{\pm}6.39{\mu}g/mL$, and benzimidazole 1 a value of $31.2{\pm}4.49{\mu}g/mL$. Benzimidazole 3 exerted no cytotoxity in either of the cell lines, with $IC_{50}$ values $>50{\mu}g/mL$. The results suggest that benzimidazoles derivatives may have chemotherapeutic potential for treatment of both colon and breast cancers.

Regulation of Inflammatory Cytokine Production by Bee Venom in Rat Chondrocytes

  • Kim, Eun-Jung;Kim, Gye-Yeop
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.25 no.1
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    • pp.132-137
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    • 2011
  • Bee venom acupuncture (BVA), as a kind of herbal acupuncture, involved injecting diluted bee venom into acupoints and is used for pain, osteoarthritis and rheumatoid arthritis patients. BVA is growing in popularity, especially in Korea, and is used primarily for pain relief in many kinds of diseases. However, the effect of bee venom anti-inflammatory related action in lipopolysaccharide (LPS) induced chondrocyte stress have not been reported yet. The aim of this study was to investigate the effect of bee venom of cell viability and inflammatory cytokine in rat articular chondrocyte cultures stimulated with lipopolysaccharide. Inflammation was induced in rat chondrocytes by treatment with $10{\mu}g/m{\ell}$ LPS. The change of cell viability were decreased in chondrocytes after treatment with lipopolysaccharide. The cell viability revealed that BV exerted no significant cytotoxicity in the rat chondrocyte. Bee venom inhibited decreased cell viability in the presence of lipopolysaccharide ($10{\mu}g/m{\ell}$) in a dose dependent manner(0.1, 0.5, 1.0 and $5.0{\mu}g/m{\ell}$) at bee venom(p<0.05). Tumor necrosis factor (TNF)-${\alpha}$ production in the presence of lipopolysaccharide($1{\mu}g/m{\ell}$) was also inhibited in a dose dependent manner (p<0.05 from bee venom $0.1{\mu}g/m{\ell}$). Interleukin (IL)-6 production in the presence of lipopolysaccharide ($10{\mu}g/m{\ell}$) was inhibited as well (p<0.05 at bee venom 0.1, 0.5, 1.0 and $5.0{\mu}g/m{\ell}$, respectively). Our results demonstrate that bee venom was a anti-inflammatory agent of chondrocytes. Bee venom may exert its anti inflammatory effects through inhibition of TNF-${\alpha}$ and IL-6 synthesis, and may then pain relief and reduce the articular destruction.

Synthesis of Novel Kojic Acid Derivative and Its Anti-pigmentation Effect

  • Kim, K. H.;Kim, K. S.;Kim, J. G.;Park, S. H.;E. K. Yang;Park, S. N.
    • Proceedings of the SCSK Conference
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    • 2003.09a
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    • pp.719-732
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    • 2003
  • A kojic acid derivative, kojic acid 7-O-$\beta$-D-tetraacetylglucopyranoside(KTG) was synthesized. Regio-and stereo-selective glycosylation at 7-postion in kojic acid with $\beta$-D-pentaacetylglucose was achieved with high yield(80%) by the use of Lewis acid and organic base in nonpolar solvent. KTG was hydrolyzed in methanol by the aid of sodium methoxide to give kojic acid 7-O-$\beta$-D-glucopyranoside(KGP). KGP is freely soluble in water and soluble in methanol and ethanol. Its structure was comfirmed by $^1$H-NMR and $^{13}$ C-NMR. Tyrosinase activity inhibition of KGP was measured with mushroom tyrosinase compared with ascorbic acid, kojic acid and arbutin. KGP showed higher tyrosinase inhibition activity($IC_{50}$/=33.3 $\mu\textrm{g}$/ml) than ascorbic acid(63.2 $\mu\textrm{g}$/ml) and arbutin(91.8 $\mu\textrm{g}$/ml) but lower inhibition activity than kojic acid(8.3 $\mu\textrm{g}$/ml). To test free-radical scavenging activity, we used 1, 1-diphenyl-2-picrylhydrazyl(DPPH) as a free-radical source. Free-radical scavenging activity of KGP was very low($SC_{50}$/>1000 $\mu\textrm{g}$/ml) compared with ascorbic acid($SC_{50}$/=2.68 $\mu\textrm{g}$/ml) and arbutin($SC_{50}$/=180$\mu\textrm{g}$/ml). Melanin formation inhibition of KGP was measured in B16 melanoma, compared with kojic acid, arbutin and Vitamin C. Inhibition activity of KGP for melanin formation was not found within test concentrations.

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Effect of Pine (Pinus densiflora) Needle Extracts on Synthesis of Collagen in Osteoblastic MC3T3-E1 Cells (적송잎 추출물이 조골세포의 collagen 합성에 미치는 영향)

  • Jeon, Min-Hee;Kim, Young-Kyoung;Park, Yong-Soo;Hwang, Hyun-Jung;Kim, Sung-Gu;Lee, Sang-Hyeon;Choi, In-Soon;Kim, Mi-Hyang
    • Journal of Life Science
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    • v.20 no.4
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    • pp.607-613
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    • 2010
  • Osteoporosis is a disease involving a decrease in bone mineral density and an increased risk of fractures. The MC3T3-E1 pre-osteoblastic cell line is a well-accepted model of osteogenesis in vitro. Pine needles have long been used as a traditional health-promoting medicinal food in Korea. In this study, MTT assay, the alkaline phosphatase (ALP) activity and collagen synthesis of osteoblast cells were investigated to determine the effects of pine needle extracts on cell proliferation and differentiation. Pine needle extracts were prepared using hexane, ethanol and water. The effects of the pine needle extracts were examined by comparing the results with those of commercial agents, such as proanthocyanidin. The MC3T3-E1 cells exposed to proanthocyanidin showed increased proliferation in a concentration-dependent manner. The cells exposed to the hexane extract showed a similar increase in proliferation to that observed with proanthocyanidin. The hexane extract showed the highest ALP activity. Moreover, a supplement of pine needle extracts induced collagen synthesis in MC3T3-E1 cells. The pine needle extract produced the highest level of collagen synthesis at concentrations of $10{\sim}50\;{\mu}g/ml$. These results indicate that pine needle extracts have an anabolic effect on bone by promoting osteoblastic differentiation, and may be used in the treatment of common metabolic bone diseases.