• 제목/요약/키워드: 2,4,6-TCP

검색결과 85건 처리시간 0.023초

1-Methyl Substituent and Stereochemical Effects of 2-Phenylcyclopropylamines on the Inhibition of Rat Brain Mitochondrial Monoamine Oxidase A and B

  • Kang, Gun-Il;Hong, Suk-Kil;Choi, Hee-Kyung
    • Archives of Pharmacal Research
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    • 제10권1호
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    • pp.50-59
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    • 1987
  • (E)-2-Phenylcyclopropylamine ((E)-TCP), (Z)-2-Phenylacyclopropylamine ((Z)-TCP), (E)-1-methyl-2-phenylcyclopropylamine ((E)-MTCP), and (Z)-1-methyl-2-phenylcyclopropylamine ((Z)-MTCP) were synthesized and used to determine to what extent 1-methylsubstitution and stereochemistry of 2-phenycyclopropylamines affect inhibition of monoamine oxidase (MAO). Inhibition of rat brain mitochondrial MAO-A and B by the compounds were measured using serotonin and benzylamine as the substrate, respectively and $IC_{50}$ values obtianed with 95% confidence limits by the method of computation. For the inhibition of MAO-A, (E)-MTPC ($IC_{50}$ = 6.2 * $10^{-8}$M) was found to be 37 times more potent than (Z)-MTCP ($IC_{50}$ = 7.8 * $10^{-8}$M), was 7 times more potent than (Z)-MTCP($IC_{50}$= 4.7 * $10^{-7}$M) and (E)-TCP($IC_{50}$ =7.8 * $10^{-8}$M),0.6 times as potent as (Z)- TCP ($IC_{50}$ = 4.4 * $10^{-8}$M). The results suggested that while without 1-methyl group, potency of a (Z)-isomer was comparable to that of (E)-isomer, the methyl group in its (Z)-position was very unfavorable to the inhibition of MAO and that in its (E)-position, the methyl group contributed positively to the potency as found by the fact that (E)-MTCP was 1-5 times more potent than (E)-TCP. In view of the selective inhibition of MAO-A- or B over MAO-A and 1-methyl substitution as well as the stereochemical factors did not significantly influence the selectivity.

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Adverse effects of pesticide/metabolites on boar spermatozoa

  • Wijesooriya Mudhiyanselage Nadeema Dissanayake;Jung Min Heo;Young-Joo Yi
    • 농업과학연구
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    • 제50권4호
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    • pp.941-952
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    • 2023
  • The metabolites of agrichemicals, such as organophosphorus pesticides, are known to be more hazardous than their parent pesticides. 3,5,6-trichloro-2-pyridinol (TCP) is a major degradation product of chlorpyrifos, one of the organophosphate insecticides widely used in agriculture. In vivo or in vitro exposure to chlorpyrifos has been known to interfere with male reproductive functions, leading to reduced fertility in mammals. Therefore, this study was performed to examine the changes in the fertilization competence of boar spermatozoa exposed to TCP. Sperm samples were subjected to varying concentrations of TCP (10, 50, 100, 200 µM) and different periods of incubation. Sperm motility, motion kinematics, viability, acrosome integrity, intracellular reactive oxygen species (ROS) production, and gene expression levels (ODf2, ZPBP2, AKAP3 and AKAP4) were evaluated after exposure of the sperm to TCP. A significant dose-dependent reduction in motility was observed in sperm samples incubated with TCP compared to the controls after both incubation periods. Sperm viability was significantly decreased in samples incubated with 50, 100, and 200 µM TCP in both incubation periods. A significantly lower percentage of normal acrosomes and gene expression levels were observed in sperm samples exposed to 50, 100, and 200 µM TCP after both incubation periods, compared to the controls. There was a significant increase in the ROS production in spermatozoa incubated with 100 - 200 µM TCP after both incubation periods. Consequently, the direct exposure of boar spermatozoa to TCP interferes with sperm functions and leads to decreased fertilization. In order to identify and address the various causes of reproductive decline, the impact of chemical metabolites needs to be discussed in depth.

가토 두개골 결손부에 이식된 ${\beta}$-TCP의 골치유과정에서 맥동전자기장의 영향에 관한 연구 (THE EFFECT OF PULSED ELECTROMAGNETIC FIELDS ON ${\beta}$-TCP GRAFT IN RABBIT CRANIAL BONE DEFECT)

  • 김상우;황경균;임병섭;박창주;정일혁;백승삼;심광섭
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제32권4호
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    • pp.360-373
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    • 2006
  • The purpose of this research was to investigate whether pulsed electromagnetic field (PEMF) stimulation applied to the rabbit cranial defects grafted with ${\beta}$-tricalcium phosphate (${\beta}$-TCP) could affect the new bone formation. With 16 New Zealand white rabbits under the same condition, bilateral calvarial bone defects were formed around the sagittal suture line. The defect on the left side was grafted with ${\beta}$-TCP, while on the right side was grafted by harvested autogenous bone. PEMF was applied to 8 rabbits for 8 hours per day. The bony specimen were divided into 3 groups, the group 1 was autogenous bone grafted specimen, the group 2 was ${\beta}$-TCP grafted with PEMF, and the group 3 was ${\beta}$-TCP grafted without PEMF. We investigated the bone regeneration & growth factor expression at 2, 4, 6, and 8 weeks. As a result, BMP 2 was expressed in the group 1 from 2 weeks, the group 2 from 4 weeks, and the group 3 from 6 weeks. BMP 4 was expressed in the group 1 from 2 weeks, in the group 2 and the group 3 from 4 weeks. 4. There was no significant difference in expression pattern of BMP 7, PDGF, VEGF, and TGF-${\beta}$1 during grafted bone regeneration in group 1, 2, and 3. According to our results, PEMF stimulation could be effective on the new bome formation in animal study, and have a feasibility of clinical use.

Hydroxyapatite와 Al2O3 혼합분말의 상압소결에 의한 TCP/Al2O3 및 Fluorapatite/Al2O3 복합재료의 In-Situ 제조 (In-Situ Fabrication of TCP/Al2O3 and Fluorapatite/Al2O3 Composites by Normal Sintering of Hydroxyapatite and Al2O3 Powder Mixtures)

  • 하정수;한유정
    • 한국재료학회지
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    • 제29권2호
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    • pp.129-135
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    • 2019
  • A powder mixture of 70 wt% $Al_2O_3$ and 30 wt% hydroxyapatite (HA) is sintered at $1300^{\circ}C$ or $1350^{\circ}C$ for 2 h at normal pressure. An $MgF_2$-added composition to make HA into fluorapatite (FA) is also prepared for comparison. The samples without $MgF_2$ show ${\alpha}$ & ${\beta}$-tricalcium phosphates (TCPs) and $Al_2O_3$ phases with no HA at either of the sintering temperatures. In the case of $1,350^{\circ}C$, a $CaAl_4O_7$ phase is also found. Densification values are 69 and 78 %, and strengths are 156 and 104 MPa for 1,300 and $1,350^{\circ}C$, respectively. Because the decomposition of HA produces a $H_2O$ vapor, fewer large pores of $5-6{\mu}m$ form at $1,300^{\circ}C$. The $MgF_2$-added samples show FA and $Al_2O_3$ phases with no TCP. Densification values are 79 and 87 %, and strengths are 104 and 143 MPa for 1,300 and $1,350^{\circ}C$, respectively. No large pores are observed, and the grain size of FA ($1-2{\mu}m$) is bigger than that of TCP ($0.7{\mu}m{\geq}$) in the samples without $MgF_2$. The resulting $TCP/Al_2O_3$ and $FA/Al_2O_3$ composites fabricated in situ exhibit strengths 6-10 times higher than monolithic TCP and HA.

Improved Injection Behavior with the Addition of Granulated β-Tricalcium Phosphate in Brushite Bone Cement

  • Jo, Hyun-Ho;Oh, Kyung-Sik
    • 한국세라믹학회지
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    • 제55권6호
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    • pp.590-596
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    • 2018
  • To improve the injection behavior of brushite cement, dense ${\beta}-Ca_3(PO_4)_2$ (${\beta}-TCP$) granules were added to the starting material. The spherical ${\beta}-TCP$ granules prepared by spray-drying and subsequent sintering at $1000{\sim}1200^{\circ}C$ accounted for fractions of from 0.5 to 0.7 of the total ${\beta}-TCP$. The injection behavior was evaluated by measuring the injected mass divided by the loaded mass of paste in the syringe pump. The injected amount was increased with the increase in the fraction and sintering temperature of ${\beta}-TCP$ granules, except at $1200^{\circ}C$. The increase in the fraction of ${\beta}-TCP$ and its sintering temperature resulted in a decrease in the plastic limit, which is the volume of water required to liquefy the compact. The rest water could be utilized in the cement with the reduced plastic limit for improved injectability. The amounts of rest water assigned for powdery phase were estimated, and correlated with the injectability of paste.

수직골 증대술에서 $\beta$-Tricalciumphosphate/Hydroxyapatite 골 이식재 입자 크기의 영향 (Effects of different sizes of Hydroxyapatite/$\beta$-Tricalcium phosphate particles on vertical bone augmentation)

  • 허중보;정동희;김지선;신상완
    • 대한치과보철학회지
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    • 제48권4호
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    • pp.259-265
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    • 2010
  • 연구 목적: $\beta$-Tricalcium phosphate/Hydroxyapatite ($\beta$-TCP/HA) 입자가 혼합된 합성 골 이식재의 particle size가 토끼의 두개골에서 타이타늄 메쉬를 이용해 시행된 골유도 재생술의 결과에 미치는 영향을 평가하고자 하였다. 연구 재료 및 방법: 여섯 마리의 수컷 뉴질랜드 산 백토끼 (5 kg)를 이용하여 실험 하였다. 토끼 두개골의 정 중앙을 절개하고 전층 판막을 형성하여 박리하였다. 두개골의 네 부위에 6 mm 직경의 트레핀 바 (XTP 5406; Dentium, Seoul, Korea)로 원형의 홈을 형성한 후 blood supply를 위해 원형의 홈안에 1 mm 직경의 라운드 바로 다섯 개의 작은 구멍을 형성하였다. 형성된 네 개의 홈 위에 표준화되어 맞춤 제작된 반구형 타이타늄 메쉬 (높이 3 mm, 직경 6 mm; Dentium, Seoul, Korea)를 위치시키고 세 개의 2 mm 길이의 티타늄 핀 (Dentium, Seoul, Korea)을 이용하여 고정하였다. 대조군은 이식재를 포함시키지 않았고 나머지 타이타늄 메쉬들은 실험군으로서 서로 다른 세 가지 크기의 이식재를 각각 담아서 고정하였다. 이식재 ($Osteon^{(R)}$, Dentium, Seoul, Korea)의 성분은 HA와 $\beta$-TCP ($\beta$-TCP/HA)가 혼합되어 있는 합성골 이식재이며 실험군으로 사용한 이식재의 크기는 각각 small (0.3 - 0.5 mm), medium (0.5 - 1.0 mm), large (1.0 - 2.0 mm) size 였다. 8주의 치유기간 후에 토끼를 희생시킨 후 조직 표본을 제작하고 CCD 카메라 (Polaroid DMC2 digital Microscope Camera (Polaroid Corporation, Cambridge, MA 02139, USA))가 부착되어 있는 광학 현미경 (Olympus BX, Tokyo, Japan)을 이용하여 두 가지 배율 (12.5배, 40배)로 조직학적 소견을 관찰하였다. 신생 골부위와 남은 골이식재 부위의 넓이를 측정하여 타이타늄 메쉬 내부 공간에서 차지하는 면적의 비율(%)을 구하였다. 그 수치들을 Mann-Whitney U-test와 Wilcoxon signed rank-test를 이용하여 통계 분석하였다 ($\alpha$ = .05). 결과: 대조군과 $\beta$-TCP/HA를 이식한 나머지 세 군의 신생골 형성을 비교하면 통계적으로 유의하게 $\beta$-TCP/HA를 이식한 군에서 신생골 형성이 더 많았다 (P = .003). 서로 다른 particle size 간 비교에서는 신생골 형성에 있어서 통계적으로 유의한 차이는 없었다. 하지만 형성된 수직골 총량 (신생골과 이식골의 면적의 합)을 각 그룹 간에 비교해 보면 대조군보다 $\beta$-TCP/HA를 이식한 군이 통계적으로 더 많은 비율을 나타내었고 (P = .001), 특히 $\beta$-TCP/HA 이식 군간 비교에서는 medium size 군이 large particle size 군보다 통계적으로 더 큰 면적을 나타내었다 (P = .039). 그러나 large particle size 군과 small particle size 군 사이 그리고 medium size 군과 small particle size 군 사이에는 통계적으로 유의한 차이를 보이지 않았다 (P> .05). 결론: 티타늄 메쉬를 이용한 수직골 증대술에서 $\beta$-TCP/HA 합성골을 사용하는 경우 수직골 형성에 기여하며 특히 medium size (0.5 - 1.0 mm)의 $\beta$-TCP/HA 이식재가 large size 이식재 보다 더 우수한 수직골 형성의 결과를 보였다.

Evaluation of the regenerative capacity of stem cells combined with bone graft material and collagen matrix using a rabbit calvarial defect model

  • Jun-Beom Park;InSoo Kim;Won Lee;Heesung Kim
    • Journal of Periodontal and Implant Science
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    • 제53권6호
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    • pp.467-477
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    • 2023
  • Purpose: The purpose of this study was to evaluate the regenerative capacity of stem cells combined with bone graft material and a collagen matrix in rabbit calvarial defect models according to the type and form of the scaffolds, which included type I collagen matrix and synthetic bone. Methods: Mesenchymal stem cells (MSCs) were obtained from the periosteum of participants. Four symmetrical 6-mm-diameter circular defects were made in New Zealand white rabbits using a trephine drill. The defects were grafted with (1) group 1: synthetic bone (β-tricalcium phosphate/hydroxyapatite [β-TCP/HA]) and 1×105 MSCs; (2) group 2: collagen matrix and 1×105 MSCs; (3) group 3: β-TCP/HA, collagen matrix covering β-TCP/HA, and 1×105 MSCs; or (4) group 4: β-TCP/HA, chipped collagen matrix mixed with β-TCP/HA, and 1×105 MSCs. Cellular viability and cell migration rates were analyzed. Results: Uneventful healing was achieved in all areas where the defects were made at 4 weeks, and no signs of infection were identified during the healing period or at the time of retrieval. New bone formation was more evident in groups 3 and 4 than in the other groups. A densitometric analysis of the calvarium at 8 weeks post-surgery showed the highest values in group 3. Conclusions: This study showed that the highest regeneration was found when the stem cells were applied to synthetic bone along with a collagen matrix.

가토 상악동에 이식된 ${\beta}$-TCP의 골치유에 관한 실험적 연구 (THE EXPERIMENTAL STUDY OF THE BONE REGENERATION ON RABBIT MAXILLARY SINUS GRAFTING WITH ${\beta}$-TCP)

  • 박정하;황경균;박창주;최용수;마평수;백승삼;심광섭
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제32권2호
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    • pp.107-116
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    • 2006
  • Purpose:Maxillay sinus grafting is an effective treatment procedure to improve bone height in the posterior maxillar area for implant installation. Beta-tricalciumphosphate(${\beta}$-TCP) was introduced to be grafting substitute material, providing a reasonable bio-degradation time, no need for harvesting procedure. The purpose of this study is to evaluate bone healing & regeneration phase using histomorphometric and immunohistochemical analysis. Material & Methods:Sixteen rabbits were divided into 4 groups. Bi-lateral maxillary sinus membranes were elevated at each rabbits, ${\beta}$-TCP was augmented in left sinus, autogenous bone was augmented in right sinus. The rabbits were sacrificed at 2, 4, 8 and 12 weeks. We investigated the bone regeneration & growth factor expression. Results: 1. The mean new bone volume formation was 28.99${\pm}$6.55%, 49.54${\pm}$5.47%, 69.09${\pm}$8.90% in autogenous grafted area, and 22.86${\pm}$5.56%, 24.00${\pm}$4.09%, 34.11${\pm}$3.37% in ${\beta}$-TCP area at 4, 8, 12 weeks. Therefore, new bone formation in autogenous bone was significantly higher than ${\beta}$-TCP (p<0.05). 2. The BMP 2/4 expression in autogenous bone grafted area was higher at 4, 8 weeks. 3. There was no difference in expression pattern of BMP-7/PDGF/VEGF during grafted bone regeneration. Conclusion:The authors we conclude that the autogenous bone graft was faster than ${\beta}$-TCP in bone regeneration, and the BMP 2/4 were more important in graft bone regeneration.

수산화아파타이트 분말의 열처리가 유사생체용액 내 용해거동에 미치는 영향 (Influence of thermal treatment on the dissolution of hydroxyapatite powders in simulated body fluid)

  • 송대성;서동석;이종국
    • 한국결정성장학회지
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    • 제15권2호
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    • pp.79-85
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    • 2005
  • 수산화아파타이트 상용분말을 $1000{\sim}1350^{\circ}C$ 온도범위에서 2시간 동안 공기 중에서 하소한 다음, pH 7.4인 유사 생체용액에 넣고 $37^{\circ}C$에서 3일 또는 7일간 침적실험을 행하였다. 열분해에 따른 수산화아파타이트 분말의 용해 거동은 XRD, FTIR, TEM을 이용해 비교분석 하였다. $1200^{\circ}C$에서 하소된 수산화아파타이트 분말은 격자 내 $OH^-$ 이온들의 탈수로 인하여 OHAP(oxyhydroxyapatite, ($Ca_{10}(PO_4)_6O_x(OH)_{2-2x}$)로 전이하였다. $1350^{\circ}C$에서 수산화아파타이트 분말 일부가 ${\alpha}-TCP$(${\alpha}-tricalcium$ phosphate)와 TTCP (tetracalcium phosphate)로 열분해 되었다. 수산화아파타이트 분말의 열분해로 인해 생성된 ${\alpha}-TCP$, TTCP 및 비화학양론조성의 OHAP 조성들이 수산화아파타이트 분말의 표면용해를 진전시켰다.

토끼의 하악골에서 $\beta-TCP$ 와 rhBMP-2의 골형성 효과에 대한 형태계측학적 연구 (Morphometric analysis on bone formation effect of $\beta-TCP$ and rhBMP-2 in rabbit mandible)

  • 김규남;양정은;장재원;사시카라 바라라만;왕붕;김일규
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제36권3호
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    • pp.161-171
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    • 2010
  • Introduction: This study was to assess the effectiveness of new bone formation and regeneration by using a rhBMP-2 and $\beta-TCP$ as a carrier in rabbits’mandible. Materials and Methods: The mandibles of 36 rabbits were exposed and cortical bone was penetrated for this study. The experimental subjects were divided into 3 groups each 12 rabbits ; control group, experimental group 1, and experimental group 2. Control group had the defect itself without any treatment, in the experimental group 1, $\beta-TCP$P only was grafted, and in the experimental group 2, rhBMP-2 soaked in $\beta-TCP$ was grafted. The rabbits were sacrificed after 1, 2, 3, 4, 6, and 8weeks, and new bone formation area was examined and measured for bone quantitative and qualitative analysis with light, fluorescent and polarized microscopy. Results: In the experimental group 1, new bone formation from the adjacent host bone was made by osteoconduction, and in the experimental group 2, direct new bone formation by osteoinduction of rhBMP-2 as well as new bone formation by osteoconduction of $\beta-TCP$ were observed. Conclusion: rhBMP-2 of experimental group 2 is very effective in the bone formation in early 2weeks and bone remodelling from 3weeks.