• Title/Summary/Keyword: Analogs

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Inhibitory effects of resveratrol analogs on lipopolysaccharide-induced cyclooxygenase-2 activity in RAW264.7 cells

  • Park, Eun-Jung;Min, Hye-Young;Park, Jae-Eun;Kim, Sang-Hee;Lee, Sang-Kook
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.245.1-245.1
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    • 2002
  • It has been known that resveratrol, a phytoalexin present in grapes mainly, has antioxidant. anti-inflammatory, and cancer chemopreventive activity. One mechanism of its anti-inflammation and cancer prevention is considered to modulate cyclooxygense-2 (COX-2) activity. Since COX-2 plays an important role in inflammation and carcinogenesis, the potential COX-2 inhibitors have been considered as anti-inflammatory or cancer chemopreventive agents. (omitted)

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CONVERGENCE THEOREMS FOR TWO NONLINEAR MAPPINGS IN CAT(0) SPACES

  • Sokhuma, Kritsana;Sokhuma, Kasinee
    • Nonlinear Functional Analysis and Applications
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    • v.27 no.3
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    • pp.499-512
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    • 2022
  • In this paper, we construct an iteration scheme involving a hybrid pair of the Suzuki generalized nonexpansive single-valued and multi-valued mappings in a complete CAT(0) space. In process, we remove a restricted condition (called end-point condition) in Akkasriworn and Sokhuma's results [2] in Banach spaces and utilize the same to prove some convergence theorems. The results in this paper, are analogs of the results of Akkasriworn et al. [3] in Banach spaces.

Heat and mass transfer processes at the most heat-stressed areas of the surface of the descent module

  • Oleg A., Pashkov;Boris A., Garibyan
    • Advances in aircraft and spacecraft science
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    • v.9 no.6
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    • pp.493-506
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    • 2022
  • The study presents the results of the research of heat and heat exchange processes on the heat-stressed elements of the structure of an advanced TsAGI descent vehicle. The studies were carried out using a mathematical model based on solving discrete analogs of continuum mechanics equations. Conclusions were drawn about the correctness of the model and the dependence of the intensity of heat and mass transfer processes on the most heat-stressed sections of the apparatus surface on its geometry and the catalytic activity of the surface.

9-Meric Peptide Analogs of Defensin-like Antimicrobial Peptide Coprisin with Potent Antibacterial Activities with Bacterial Sell Selectivites

  • Shin, Areum;Lee, Eunjung;Kim, Jin-Kyoung;Bang, Jeong-Kyu;Kim, Yangmee
    • Bulletin of the Korean Chemical Society
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    • v.35 no.9
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    • pp.2809-2812
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    • 2014
  • The 43-residue defensin-like peptide coprisin, which is isolated from dung bettle, Copris tripartitus, is a potent antimicrobial peptide. In our previous work, we determined the tertiary structure of coprisin and found that alpha helical region of coprisin from residue 19 to residue 30 is important for its antimicrobial activities. Here, we designed cop12mer and cop9mer analogs of coprisin based on the tertiary structure of coprisin. To investigate the relationship between hydrophobicity and antimicrobial activities and develop the potent peptide antibiotics, we designed cop9mer-1 with substitution of $His^2$ with Trp in cop9mer. The results showed that cop9mer-1 has higher toxicities as well as improved antimicrobial activities compared to cop9mer. In order to reduce the toxicity of cop9mer-1, we designed cop9mer-2 and cop9mer-3 with substitution of $Cys^3$ with Lys or Ser. Substitution of $Cys^3$ with these hydrophilic amino acids results in lower cytotoxicities compared to cop9mer-1. Cop9mer-2 with substitution of $Cys^3$ with Lys in Cop9mer-1 showed high antibacterial activities against drug resistant bacteria without cytotoxicity. Antibiotic action of cop9mer-1 analog appears to involve permeabilization of the bacterial cell membrane while cop9mer-2 and cop9mer-3 may have different mechanism of action. These results imply that that optimum balance in hydrophobicity and hydrophilicity in these 9-meric peptides plays key roles in their antimicrobial activities as well as cytotoxicities.

Long-term effects of gonadotropin-releasing hormone analogs in girls with central precocious puberty

  • Kim, Eun Young
    • Clinical and Experimental Pediatrics
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    • v.58 no.1
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    • pp.1-7
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    • 2015
  • Gonadotropin-releasing hormone analogs (GnRHa) are widely used to treat central precocious puberty (CPP). The efficacy and safety of GnRHa treatment are known, but concerns regarding long-term complications are increasing. Follow-up observation results after GnRHa treatment cessation in female CPP patients up to adulthood showed that treatment (especially <6 years) was beneficial for final adult height relative to that of pretreated or untreated patients. Puberty was recovered within 1 year after GnRHa treatment discontinuation, and there were no abnormalities in reproductive function. CPP patients had a relatively high body mass index (BMI) at the time of CPP diagnosis, but BMI standard deviation score maintenance during GnRHa treatment seemed to prevent the aggravation of obesity in many cases. Bone mineral density decreases during GnRHa treatment but recovers to normal afterwards, and peak bone mass formation through bone mineral accretion during puberty is not affected. Recent studies reported a high prevalence of polycystic ovarian syndrome in CPP patients after GnRHa treatment, but it remains unclear whether the cause is the reproductive mechanism of CPP or GnRHa treatment itself. Studies of the psychosocial effects on CPP patients after GnRHa treatment are very limited. Some studies have reported decreases in psychosocial problems after GnRHa treatment. Overall, GnRHa seems effective and safe for CPP patients, based on long-term follow-up studies. There have been only a few long-term studies on GnRHa treatment in CPP patients in Korea; therefore, additional long-term follow-up investigations are needed to establish the efficacy and safety of GnRHa in the Korean population.

Growth Inhibition and G2/M Phase Cell Cycle Arrest by 3,4,5-Trimethoxy-4'-bromo-cis-stilbene in Human Colon Cancer Cells

  • Heo, Yeon-Hoi;Min, Hye-Young;Kim, Sang-Hee;Lee, Sang-Kook
    • Biomolecules & Therapeutics
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    • v.15 no.2
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    • pp.95-101
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    • 2007
  • Resveratrol (3,5,4’-trihydroxy-trans-stilbene), a naturally occurring phytoallexin abundant in grapes and several plants, has been shown to be active in inhibiting proliferation and inducing apoptosis in several human cancer cell lines. On the line of the biological activity of resveratrol, a variety of resveratrol analogs were synthesized and evaluated for their growth inhibitory effects against several human cancer cell lines. In the present study, we found that one of the resveratrol analogs, 3,4,5-trimethoxy-4’-bromo-cis-stilbene, markedly suppressed human colon cancer cell proliferation (EC$_{50}$ = 0.01 ${\mu}$g/ml), and the inhibitory activity was superior to its corresponding trans-isomer (EC$_{50}$ = 1.6 ${\mu}$g/ml) and resveratrol (EC$_{50}$ = 18.7 ${\mu}$g/ml). Prompted by the strong growth inhibitory activity in cultured human colon cancer cells (Col2), we investigated its mechanism of action. 3,4,5-Trimethoxy-4’-bromo-cis-stilbene induced arrest of cell cycle progression at G2/M phase and increased at sub-G1 phase DNA contents of the cell cycle in a time- and dose-dependent manner. Colony formation was also inhibited in a dose-dependent manner, indicating the inhibitory activity of the compound on cell proliferation. Moreover, the morphological changes and condensation of the cellular DNA by the treatment of the compound were well correlated with the induction of apoptosis. These data suggest the potential of 3,4,5-trimethoxy-4’-bromo-cis-stilbene might serve as a cancer chemotherapeutic or chemopreventive agent by virtue of arresting the cell cycle and inducing apoptosis for the human colon cancer cells.

Instructional Effects of Multiple Analogies on Conceptual Understanding and Learning Motivation (다중 비유를 사용한 수업이 개념 이해 및 학습 동기에 미치는 효과)

  • Kwon, Hyeok Soon;Noh, Tae Hee
    • Journal of the Korean Chemical Society
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    • v.45 no.2
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    • pp.177-182
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    • 2001
  • An instructional model using multiple analogies according to component process (MACP) was designed on the vasis of schema theory and comornent process theory in analogical reasoning. This model has ? phases: introducting multiple analsgs, extracting multiple analogs, extracting common attributes of analogs, introducing target conanother context. Te instructional effects of this model upon students' conceptual understanding and learning motivation were compared with those of the Teaching-With-Analogy (TWA) and non-analogy instructions. Three classes of 8th grade were randomly assigned to MACP, TWA, and control group, respectively, Subjects were taught about chemical changes and reactions for 10 class hours. The ANCOVA results indicated that the scores of the conceptions test for the MACP group were significantly higher than for the control graup. However, no significant differences were found among the three groups in the test scores of learning motivation.

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Immobilization of ATP on Bovine $\beta$- Caseins by Using Transglutaminase (효소법에 의한 ATP의 Bovine $\beta$-Casein에의 고정화)

  • 윤세억;박선영김명곤
    • KSBB Journal
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    • v.5 no.3
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    • pp.241-246
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    • 1990
  • ATP analogs were immobilized or bovine caseins by the action of transglutaminase. The ATP analogs immobilized on the caseins were enzymatically active and interconverten by kinases. The immobilized ATP was dephosphorylated to the corresponding ADP by hexokinase and rephosphorylated to the ATP in solid form by acetate kinase. Under the conditions chosen, about 55% of the immobilized ATP was dephosphorylated and about 80% of the resulted ADP was rephosphorylated. Bovine $\beta$-casein was more useful than $\alpha$sf-casein as a carrier and C8-substituted ATP analognwas more effective than N6-substituted one in immobilization. Michaelis constant of C8-substituted ATP analog immobilized on $\beta$-casein was similar to that of free form of ATP and that of ATP analog. The immobilized ATP was much more stable than free ATP and its analog, while maximum velocity was reduced to 37% of the free ATP analog. The immobilized ATP was recovered almost completely by calcium precipitation.

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A COMPARISON OF ACCURACY BETWEEN FIXTURE IMPRESSION AND ABUTMENT IMPRESSION FOR DENTAL IMPLANTS (치과 임플랜트용 고정체 인상법과 지대원주 인상법간의 정확성 비교)

  • Choi, Hyun-Sik;Yim, Soon-Ho;Cho, In-Ho
    • The Journal of Korean Academy of Prosthodontics
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    • v.35 no.4
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    • pp.662-673
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    • 1997
  • The purpose of this study was to compare the accuracy between future impression and abutment impression using strain gauges. The master model used in this study was a partially edentulous mandibular metal cast with two fixture analogs on both sides. On the left, two future analogs were parallel, whereas right side, posterior future analog exhibiting a 15-degree lingual inclination. From master cast, 10 impressions were made for each of the three impression methods. The master frameworks was fabricated on the master model, and two-element strain gauge was attached to a master framework. The master framework was seated on each cast, and gold screws were tightened to 10 Ncm using a torque controller AI-1600 strain measurement system was used for strain measuring. Impression methods studied were : Group 1:abutment impression Group 2:fixture impression Group 3:combined impression (anterior:fixture impression, posterior:abutment impression) The results were as followed. 1. The strain values on X-axis and Y-axis according to the three impression methods showed no significant difference. 2. The strain values on parallel and angulated groups according to the three impression methods showed no significant difference. 3. The parallel group exhibited significantly higher accuracy in adaptation than angulated group for all experimental groups (p<0.05). In conclusion, it is considered that accuracy of implant prostheses is more affected by implant angulation than impression methods.

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Synthesis of Two Nitro Analogs of Tranylcypromine: Relations of Aromatic Substitution of Nitro Groups to MAO-Inhibitory Activity

  • Kang, Gun-Il;Hong, Suk-Kil
    • Archives of Pharmacal Research
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    • v.11 no.1
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    • pp.33-40
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    • 1988
  • Two new nitro analogs of tranylcypromine, (E)-2-(p-nitrophenyl)cyclopropylamine ((E)-p-NTCP) and (E)-2-(m-nitrophenyl)cyclopropylamine ((E)-m-NTCP) were synthesized in order to examine the effect of aromatic nitro substitution on the MAO-inhibitory activity of 2-phenylcyclopropylamines. The compounds were obtained by treating t-butyl (E)-2-(p-nitrophenyl) cyclopropanecarbamate and t-butyl (E)-2-(m-nitrophenyl)cyclopropanecarbamate with p-toluenesulfonic acid in $CH_3$CN. Inhibitions of rat brain mitochondrial MAO-A and B by the compounds were examined using serotonin and benzylamine as the substrate at both in vitro and ex vivo levels. It was found from in vitro measurements that (E)-p-NTCP at $6.0{\times}10^{-5}M$ elicited merely 22.5% inhibition against MAO-B without any effect on MAO-A. In contrast, (E)-m-NTCP showed fair degrees of inhibitions of MAO-A and B with $IC_{50}$ values, $2.5{\times}10^{-7}M\;and\;1.4{\times}10^{-6}M$, respectively. It was also noted from (E)-m-NTCP that m-nitro substitution caused a shift of selectivity of the inhibition toward MAO-A. According to ex vivo measurements at 1.5, 3, 6, and 12 hr following the administration of a dose of 0.015 mmol/kg, i.p. to the rats, the inhibition percents of MAO-A by (E)-m-NTCP were 58.6, 63.7 63.6, and 46.6%, slightly lower than those observed by tranylcypromine. Whereas, (E)-m-NTCP at the same dose level did not show significant inhibitions against both MAO-A and MAO-B. Possible reasons for the difference in potencies between (E)-m-NTCP and (E)-p-NTCP were sought in relation to differing electron withdrawing effects of m- and p-substituents which will influence electron density of the side chain amino functions and the partitions.

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