• Title/Summary/Keyword: e-Ring

Search Result 669, Processing Time 0.031 seconds

Effects of Cyclobuxine E on Two Distinct Types of Potassium-Activated Calcium Channels in an Intestinal Smooth Muscle (흰쥐 장관에 있어 칼륨에 의해 활성화되는 칼슘 채널에 대한 Cyclobuxine E의 영향)

  • Lee, Jong-Hwoa;Kwon, Jun-Tack;Cho, Byung-Heon;Choi, Kyu-Hong;Kim, Yu-Jae;Kim, Jong-Bae;Kim, Chun-Sook;Cha, Young-Deog;Kim, Young-Suk
    • The Korean Journal of Pharmacology
    • /
    • v.25 no.1
    • /
    • pp.53-58
    • /
    • 1989
  • For several years, we investigated the pharmacological action of several substances isolated from Buxus microphylla var koreana Nakai, which had been used as folk remedies of malaria and venereal disease. Cyclobuxine $D(C_{25}H_{42}ON_2)$, a steroidal alkaloid, exerted an antiinflammatory action, hypotensive and bradycardic effects in rats. In the present study, we isolated alkaloid from the acetone-insoluble fraction of the strong bases of this plants. This alkaloid $(C_{25}H_{38}ON_2)$ was identified as a steroidal alkaloid contained a cyclopropane ring by physical and chemical methods. It is a derivative of cyclobuxine D and named cyclobuxine E. We examined the effect of cyclobuxine E on the contractile response induced by acetylcholine and two distinct types of potassium-activated calcium channels in an intestinal smooth muscle of the rat. Cyclobuxine E inhibited significantly the Ach-induced contraction. The isolated longitudinal muscle from the rat duodenum was immersed calcium-depleted potassium depolarizing solution. Ten minutes after, 1.8 mM $CaCl_2$ was added to muscle bath and elicited a biphasic increase in muscle tension. Cyclobuxine E produced an appreciable inhibition of both components of the mechanical response. In addition, Cyclobuxine E introduced at a point when the tonic response had reached its maximum level, caused the muscle to exhibit a rapid loss of tension. Based on these experimental results, we proposed the possibility that the inhibitory action of cyclobuxine E on the isolated rat duodenum may be due to inhibiting the transmembrane fluxes of calcium ion in potassium-activated calcium channels.

  • PDF

Influence of substituted phenoxy group on the fungicidal activities of 2-N-benzyl-5-phenoxy-3-isothiazolone derivatives (2-N-benzyl-5-phenoxy-3-isothiazolone 유도체의 살균활성에 미치는 치환-phenoxy기의 영향)

  • Sung, Nack-Do;Kim, Ki-Hyun
    • The Korean Journal of Pesticide Science
    • /
    • v.5 no.3
    • /
    • pp.36-40
    • /
    • 2001
  • A series of new 2-N-benzyl-5-phenoxy-3-isothiazolone derivatives were synthesized and their in vitro antifungal activities against resistant Phytophthora capsici (RPC) & sensitive Phytophthora capsici (SPC) with metalaxyl fungicide have been measured. In addition, influence of substituted 5-phenoxy group on the -antifungal activities ($pI_{50}$) and the reactivity of substrates were investigated. From the results, reactivity of none substituted substrate showed tendency displaying orbital-controlled reaction. The substituents on the 5-phenoxy ring showed selective fungicidal activity between SPC and RPC. Especially, the 4-fluoro substituent, 6 in the RPC and 4-nitro substituent, 3 in SPC exhibited strongly selective antifungal activity among them. The activities on the SPC would depend largely on the optimal molar refractivity ($MR_{(opt.)}=7.37cm^3/mol$) whereas the activities on the RPC would depend largely on the optimal highest occupied molecular orbital energy ($HOMO_{(opt.)}=-9.2137e.v.$) and weak electron donating (${\sigma}<0$) group. And Free-Wilson analyses revealed that the antifungal activity against RPC depends on the methoxy and bromo-substituent and all of the substituents contribute to antifungal activities against SPC.

  • PDF

Quantification of Pediatric Cervical Spine Growth at the Cranio-Vertebral Junction

  • Lee, Ho Jin;Kim, Jong Tae;Shin, Myoung Hoon;Choi, Doo Yong;Hong, Jae Taek
    • Journal of Korean Neurosurgical Society
    • /
    • v.57 no.4
    • /
    • pp.276-282
    • /
    • 2015
  • Objective : The purpose of this study was to investigate morphological change at the craniovertebral junction (CVJ) region using computed tomography. Methods : A total of 238 patients were included in this study, and mean age was $47.8{\pm}21.3months$. Spinal canal diameter, Power's ratio, McRae line, antero-posterior C1 ring height, atlantoaxial joint space, C2 growth, epidural space from the dens (M-PB-C2) and longitudinal distance (basion to C2 lower margin, B-C2) were measured. The mean value of each parameter was assessed for individual age groups. The cohorts were then divided into three larger age groups : infancy (I) (${\leq}2years$), very early (VE) childhood (2-5 years) and early (E) childhood ($5{\geq}years$). Results : Spinal canal diameter increased with age; however, this value did not increase with statistical significance after VE age. A significant age-related difference was found for all C2 body and odontoid parameters (p<0.05). Mean McRae line was 8.5, 8, and 7.5 mm in the I, VE, and E groups, respectively. The M-PB-C2 line showed up-and-down dynamic change during early pediatric periods. Conclusion : Expansion of the spinal canal was restricted to the very early childhood period (less than 5 years) in the CVJ region; however, the C2 body and odontoid process increased continuously with age. The above results induced a dynamic change in the M-PB-C2 line. Although C2 longitudinal growth continued with age, the McRae line showed relatively little change.

Surface Structures and Thermal Desorption Behaviors of Cyclopentanethiol Self-Assembled Monolayers on Au(111)

  • Kang, Hun-Gu;Kim, You-Young;Park, Tae-Sun;Park, Joon-B.;Ito, Eisuke;Hara, Masahiko;Noh, Jae-Geun
    • Bulletin of the Korean Chemical Society
    • /
    • v.32 no.4
    • /
    • pp.1253-1257
    • /
    • 2011
  • The surface structures, adsorption conditions, and thermal desorption behaviors of cyclopentanethiol (CPT) self-assembled monolayers (SAMs) on Au(111) were investigated by scanning tunneling microscopy (STM), X-ray photoelectron spectroscopy (XPS), and thermal desorption spectroscopy (TDS). STM imaging revealed that although the adsorption of CPT on Au(111) at room temperature generates disordered SAMs, CPT molecules at $50^{\circ}C$ formed well-ordered SAMs with a $(2{\surd}3{\times}{\surd}5)R41^{\circ}$ packing structure. XPS measurements showed that CPT SAMs at room temperature were formed via chemical reactions between the sulfur atoms and gold surfaces. TDS measurements showed two dominant TD peaks for the decomposed fragments ($C_5H_9^+$, m/e = 69) generated via C-S bond cleavage and the parent molecular species ($C_5H_9SH^+$, m/e = 102) derived from a recombination of the chemisorbed thiolates and hydrogen atoms near 440 K. Interestingly, dimerization of sulfur atoms in n-alkanethiol SAMs usually occurs during thermal desorption and the same reaction did not happen for CPT SAMs, which may be due to the steric hindrance of cyclic rings of the CPT molecules. In this study, we demonstrated that the alicyclic ring of organic thiols strongly affected the surface structure and thermal desorption behavior of SAMs, thus providing a good method for controlling chemical and physical properties of organic thiol SAMs.

Kinematics and Geometrical Structure of the Planetary Nebula NGC 6881 (행성상 성운 NGC 6881의 운동학적 특성과 기하학적 구조)

  • Lee, Sang-Min;Hyung, Siek
    • Journal of the Korean earth science society
    • /
    • v.28 no.7
    • /
    • pp.847-856
    • /
    • 2007
  • The Planetary nebula NGC 6881 displays quadrupole morphology and it also has a jet feature in its image. We investigated the line profiles of the optical region spectral emission lines, using the Hamilton Echelle Spectrograph (HES) at the Lick observatory. The HES data obtained in this study was the radiation coming from the inner region within the diameter of 4 second of arc. Expansion velocity was obtained, based on the strong emission line profiles of e.g. H, Hel, Hell, [OIII], [NII], [ArIII], [SII], and [SIII}, using the IRAF and StarLink/Dipso reduction packages. The HI recombination lines showed one single peak profile, while the He and forbidden strong lines displayed double peaks. The results of this study show that the outflow velocity of gas increases radially outwards due to the central stellar radiation pressure. It was concluded that three central rings appeared in the HST image are the result of a combined structure of bipolar cones (seen in e.g. HI lines) and a ring (seen in He, [SIII] lines) in projection.

Construction of ELISA System for the Detection of Indian citrus ringspot virus (Indian citrus ringspot virus의 ELISA 진단 시스템 구축)

  • Shin, Myeung-Ju;Kwon, Young-Chul;Ro, Hyeon-Su;Lee, Hyun-Sook
    • Research in Plant Disease
    • /
    • v.18 no.3
    • /
    • pp.231-235
    • /
    • 2012
  • Indian citrus ring spot virus (ICRSV) is known to cause a serious disease to citrus, especially to Kinnow mandarin, the popular cultivated citrus species in India. In this study, we developed diagnostic systems based on enzyme-linked immunosorbent assay (ELISA). In order to generate antibodies against ICRSV coat protein, we overexpressed the coat protein in Escherichia coli using the pET15b expression vector containing an optimized ICRSV coat protein gene. The recombinant ICRSV coat protein was overexpressed as soluble form at $37^{\circ}C$ upon IPTG induction. The protein was purified to 95% in purity by Ni-NTA column chromatography. The purified protein was immunized to rabbit for the generation of polyclonal antibody (PAb). The PAb showed a specific immunoreaction to recombinant ICRSV coat protein in western blot analysis and ELISA. Diluted rabbit antisera (10,000 fold) could detect less than 10 ng and 5 ng of the target protein in western blot and ELISA analysis, respectively.

Fungicidal Activity of 3-(X-Sub. phenyl)-1-(2-furyl)propenone Derivatives (3-(치환(X)-phenyl)-1-(2-furyl)propenone 유도체의 항균활성)

  • Sung, Nack-Do;Kang, Hee-Deog;Maeng, Joo-Yang;Shin, Dong-Rin
    • Applied Biological Chemistry
    • /
    • v.37 no.4
    • /
    • pp.287-294
    • /
    • 1994
  • New 3-phenyl-1-(2-furyl)propenones, 1 and 3-phenyl-1-(2-furyl)-3-thiophenyl-propanone, 2 derivatives were synthesized, and their fungicidal activities in vitro against Botrytis cineria (BC), Valsa ceratosperma (VC), Scelerotium cepivorum (SC) and Phytophthora capsici (PC) were investigated using a generalized structure-activity relationship (SAR). The activity of 1 was superior to those of 2, and nonsubstituent, 1a and chloro group substituent, 1d of E (Syn) conformer were the most effective $(EC_{50}=10{\sim}12\;ppm)$ compound to BC. Antifungal activities were able to predict to depend essentially on the ${\beta}$ carbon and their positive charge from the results that the good correlation $(r^2=0.90)$ was observed between hydrolysis rate constant (logk) of 1 and the electronic parameter $({\sigma})$ of X-substituent on the ${\beta}-phenyl$ ring.

  • PDF

Quantitative Structure-Activity Relationships in MAO-Inhibitor~' 2-Phenylcyclopropylarnines: Insights into the Topography of MAO-A and MAO-B

  • Kang, Gun-Il;Hong, Suk-Kil
    • Archives of Pharmacal Research
    • /
    • v.13 no.1
    • /
    • pp.82-96
    • /
    • 1990
  • Ten (E)-and (Z)-isomers of 2-phenylcyclopropylamine (PCA), 1-Me PCA, 2-Me-PCA, N-Me-PCA, and N, N-diMe PCA and fifteen o-. m-, p- isomers of (E) PCA with substituents of Me, Cl, F, OMe, OH were synthesized in this laboratory and tested for the inhibition of rat brain mitochondrial MAO-A and MAO-B. The effects of substituents, their positions, and stereochemistry on the inhibition were assessed for the compounds with substituents at cyclopropyl and amino groups and QSAR analyses were performed using the potency data of ring-substituted compounds. The best correlated QSAR equations are as follows : pI$_{50}$ = 0.804 $\pi^2$-0.834 Blo-1.069 Blm + 0.334 Lp-1.709 HDp +7.897 (r = 0.945, s =0.211, F = 16.691, p = 0.000) for the inhibition of MAO-A;PI$_{50}$= 1.815$\pi$-0.825 $\pi^2$-1.203R + 0.900 Es$^2$ + 0.869 Es$^3$ + 0.796 Es$^4$-0.992 HDp + 0.562 HAo + 3.893 (r = 0.982, s =0.178, F = 23.351, p = 0.000) for the inhibition of MAO-B. Based on the potency difference between stereoisomers of cyclopropylamine-modified compounds and an QSAR cavity near para position, two hydrophobic carities interacting with Me group, a hydrophobic site near para position, and an amino group binding site and that in addition to the same two hydrophotic cavities, hydrophotic area, steric boundaries, hydrogen-acceptor site, and amino group binding site, another steric boundary near para position and a hydrogen donating site near ortho position constitute active sites of MAO-B.

  • PDF

Trend Complex Analysis of Exercise Content on the Rings Final in the Korea Cup 2014 (2014 코리아컵 국제체조대회 링 경기 복합연기내용 분석)

  • Song, Joo-Ho;Park, Jong-Hoon;Min, A-Young
    • Journal of Digital Convergence
    • /
    • v.13 no.4
    • /
    • pp.377-385
    • /
    • 2015
  • The purpose of the study was to perform trend analysis of the exercise content i.e. element difficulty distribution scores, element group distribution scores obtained by the athletes during 2014 Korea Cup International Gymnastic finals. The conclusion drawn from the analysis are as follows: Firstly in terms of tournament technical difficulty value, Korean athletes showed characteristics of reliance on swing element rather than strength hold element which could actually secure higher difficulty scores. Secondly, skill acquisition of higher difficulty value is demanded by taking advantage of familiar characteristics from the swing element i.e. Jonasson and Roll bwd. Slowly with str. arms and body to swallow (2s.). Thirdly, development of sensory training and strengthening exercise program are essential to enhance strength hold technique.

Expression Profiling of WSSV ORF 199 and Shrimp Ubiquitin Conjugating Enzyme in WSSV Infected Penaeus monodon

  • Jeena, K.;Prasad, K. Pani;Pathan, Mujahid Khan;Babu, P. Gireesh
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.25 no.8
    • /
    • pp.1184-1189
    • /
    • 2012
  • White spot syndrome virus (WSSV) is one of the major viral pathogens affecting shrimp aquaculture. Four proteins, WSSV199, WSSV 222, WSSV 249 and WSSV 403, from WSSV are predicted to encode a RING-H2 domain, which in presence of ubiquitin conjugating enzyme (E2) in shrimp can function as viral E3 ligase and modulate the host ubiquitin proteasome pathway. Modulation of host ubiquitin proteasome pathway by viral proteins is implicated in viral pathogenesis. In the present study, a time course expression profile analysis of WSSV Open Reading Frame (ORF) 199 and Penaeus monodon ubiquitin conjugating enzyme (PmUbc) was carried out at 0, 3, 6, 12, 24, 48 and 72 h post WSSV challenge by semi-quantitative RT-PCR as well as Real Time PCR. EF1${\alpha}$ was used as reference control to normalize the expression levels. A significant increase in PmUbc expression at 24 h post infection (h.p.i) was observed followed by a decline till 72 h.p.i. Expression of WSSV199 was observed at 24 h.p.i in WSSV infected P. monodon. Since the up-regulation of PmUbc was observed at 24 h.p.i where WSSV199 expression was detected, it can be speculated that these proteins might interact with host ubiquitination pathway for viral pathogenesis. However, further studies need to be carried out to unfold the molecular mechanism of interaction between host and virus to devise efficient control strategies for this chaos in the shrimp culture industry.