• Title/Summary/Keyword: C18 modification

Search Result 106, Processing Time 0.036 seconds

Effects of Atorvastatin on the Pharmacokinetics of Nicardipine after Oral and Intravenous Administration in Rats

  • Choi, Jun-Shik;Ha, Sung-Il;Choi, Dong-Hyun
    • Biomolecules & Therapeutics
    • /
    • v.18 no.2
    • /
    • pp.226-232
    • /
    • 2010
  • The aim of this study was to investigate the effect of atrovasatatin on the pharmacokinetics of nicardipine after oral and intravenous administration of nicardipine to rats. Nicardipine was administered orally (12 mg/kg) or intravenously (i.v., 4 mg/kg) without or with oral administration of atrovasatatin (0.3 or 1.0 mg/kg) to rats. The effect of atorvastatin on the P-glycoprotein (P-gp) as well as CYP3A4 activity was also evaluated. Atorvastatin inhibited CYP3A4 enzyme activity in a concentration-dependent manner with 50% inhibition concentration ($IC_{50}$) of 48 ${\mu}M$. Compared to the controls (nicardipine alone), the area under the plasma concentration-time curve (AUC) of nicardipine was significantly (1.0 mg/kg, p<0.05) greater by 16.8-45.4%, and the peak plasma concentration ($C_{max}$) was significantly (1.0 mg/kg, p<0.05) higher by 28.0% after oral administration of nicardipine with atorvastatin, respectively. Consequently, the relative bioavailability (R.B.) of nicardipine was increased by 1.17- to 1.45-fold and the absolute bioavailability (A.B.) of nicardipine with atrovasatatin was significantly greater by 16.7-20.9% compared to that of the controls (14.3%). Compared to the i.v. control, atrovasatatin did not significantly change pharmacokinetic parameters of i.v. administration nicardipine. The enhanced oral bioavailability of nicardipine by atorvastatin suggests that CYP3A subfamily-mediated metabolism were inhibited in the intestine and/or in the liver rather than P-gp-mediated efflux of nicardipine. Based on these results, modification of nicardipine of dosage regimen is required in the patients. Human studies are required to prove the above hypothesis.

A Detection of Novel Habitats of Abies Koreana by Using Species Distribution Models(SDMs) and Its Application for Plant Conservation (종 분포 모형을 활용한 새로운 구상나무 서식지 탐색, 그리고 식물보전 활용)

  • Kim, Nam-Shin;Han, DongUk;Cha, Jin-Yeol;Park, Yong-Su;Cho, Hyeun-Je;Kwon, Hye-Jin;Cho, Yong-Chan;Oh, Seung-Hwan;Lee, Chang-Seok
    • Journal of the Korean Society of Environmental Restoration Technology
    • /
    • v.18 no.6
    • /
    • pp.135-149
    • /
    • 2015
  • Korean fir(Abies koreana E.H.Wilson 1920), endemic tree species of Korean peninsula, is considered as vulnerable and endangered species to recent rapid environmental changes such as land use and climate change. There are limited activities and efforts to find natural habitats of Korean fir for conservation of the species and habitats. In this study, by applying SDMs (Species Distribution Models) based on climate and topographic factors of Korean fir, we developed Korean fir's predicted distribution model and explored novel natural habitats. In Mt. Shinbulsan, Youngnam region and Mt. Songnisan, we could find korean fir's two novel habitat and the former was the warmest($13^{\circ}C$ in annual mean temperature), the driest(1,200mm~1,600mm in annual rainfall) and relatively low altitude environment among Korean fir's habitats in Korea. The result of SDMs did not include mountain areas of Gangwon-do as habitats of A. nephrolepis, because there were different contributions of key habitat environment factors, summer rainfall, winter mean temperature and winter rainfall, between A. koreana and A. nephrolepis. Our results raise modification of other distribution models on Korean fir. Novel habitat of Korean fir in Mt. Shinbulsan revealed similar habitat affinity of the species, ridgy and rocky site, with other habitats in Korea. Our results also suggest potential areas for creation of Korea fir's alternative habitats through species reintroduction in landscape and ecosystem level.

Improvement of HACCP Verification Checklist in School Foodservices - A Case Study on Cooked Squid with Seasoned Fresh Vegetable - (학교급식 HACCP 검증 체크리스트 개선 - 오징어채소무침을 중심으로 -)

  • Kim, Yang-Sook;Moon, Hye-Kyung;Jeong, Hye-Jin
    • Journal of the Korean Dietetic Association
    • /
    • v.18 no.3
    • /
    • pp.222-233
    • /
    • 2012
  • The purpose of this study was the improvement and modification of the HACCP verification checklist in school foodservices. For this, the HACCP verification checklist was modified on the basis of an existing school foodservice format. The modified checklist was composed of 28 items, including CCPs (critical control points), microbial test, and other components of the HACCP system than CCPs. To confirm the suitability of the modified checklist, comparisons were made based on the microbiological quality of cooked foods, utensils, and number of aerial microbes in the working area. In this study, the applicability of the modified checklist was determined by focusing on cooked squid with seasoned fresh vegetables (Ojingeochaesomoochim). The following results were obtained from 14 schools in Changwon. The checklist scores for maintaining hot foods over $60^{\circ}C$ or serving within 2 hours, microbial tests of drinking water, food contact surfaces and cooking utensils, monitoring tools, and usage of suitable sanitizers were 2 points each (The possible highest score is 2 points). On the contrary, the checklist score for microbial test of cooked foods was the lowest of all the items. The correlation coefficient (r) between the improved checklist and microbiological quality of cooked foods was 0.699 (P<0.01), whereas that between the improved checklist and microbiological quality of cooking utensils was 0.612 (P<0.05). The correlation coefficient between the improved checklist and aerial plate count in the working area was -0.556 (P<0.05). Our results indicate the potential possibility of using the HACCP verification checklist in school foodservices.

Study on Polymer-Modified Self-Healing Asphalt (고분자를 이용한 자가치유 아스팔트에 관한 연구)

  • Yang, Dong-Geon;Yoo, Pyeong-Jun;Hong, Young-Keun
    • Elastomers and Composites
    • /
    • v.49 no.2
    • /
    • pp.134-143
    • /
    • 2014
  • Polymers are introduced to neat asphalt to prepare self-healing asphalt. The polymers are Surlyn, Nylon and polyethyleneterephtalate(PET). Since they are known as having high intermolecular force, they have high processing temperature. Therefore they are hardly introduced into the asphalt as bulk state. So in this study, they are introduced as solutions. Polymer-modified asphalts showed excellent modification effect and also healing effect. 5% polymer added asphalt showed more than 18% increased tensile strength. This tensile strength increment can be explained by polymer's intermolecular forces. Especially Surlyn interacts with asphalt molecules by hydrogen bonding and also with metals in asphalt by ionic bonding. When it comes to healing aspect the healing efficiency of Surlyn increased to 138% based on tensile strength. That of PET increased to 141% based on complex modulus and in case of Nylon it increased to 131% based on impact strength. This tells that in dealing with healing efficiency the important considering factors are not only the intermolecular forces of the polymers but also the interaction between the polymer and asphalt molecules.

Application Study on Skin Beauty Culture, Green Laver Culture and Synthesis of ${\alpha},{\beta}$-Dichloro Substituted Chitosan Succinic Acid Derivatives (${\alpha},{\beta}$-Dichloro 치환기를 갖는 Chitosan Succinic Acid 유도체 합성과 피부미용 및 해태 김 양식 응용에 관한 연구)

  • Ryu, Soung-Ryual
    • Journal of the Korean Applied Science and Technology
    • /
    • v.29 no.3
    • /
    • pp.503-515
    • /
    • 2012
  • ${\alpha},{\beta}$-Dichlorosuccinic acid was synthesized through the reaction of maleic anhydride with $Cl_2$(g) and ultra violet(200~300nm) wavelength in the presence of $CCl_4$. The second reaction of N-(${\alpha},{\beta}$-dichloro)succinic acid contained glucosamine derivatives(I) was accomplished by a modification of the general acylation using excess ${\alpha},{\beta}$-dichlorosuccinic anhydride in the presence of 2% acetic acid with methanol as a solvent at elevated temperature($70^{\circ}C$). We considered organic acid derivatives were useful especially of treatment for the cultivating porphyra and skin beauty culture.

On the Pyrolysis of Polymers I. Thermogravimetric Analysis of Polymers (高分子物質의 熱分解에 關한 硏究 (第1報) 熱天秤에 依한 硏究)

  • Chwa-Kyung Sung
    • Journal of the Korean Chemical Society
    • /
    • v.7 no.2
    • /
    • pp.96-105
    • /
    • 1963
  • The weight decrease curves of 18 kinds of polymers have been measured by thermobalance at the same condition where temperature is increased $1^{\circ}C$ per minutes under nitrogen or air atmosphere. The curves are further differentiated to obtain rate curve of weight decrease. Those curve offer a method to compare relative thermal stability, effects of oxygen or modes of thermal degradation of polymers qualitatively. The curves could be classified into following four types: Polystyrene, polymethylmethacrylate and acetal polymer belong to the first type. Those polymers depolymerize mainly into corresponding monomers, weight decrease curves are steepy up to perfect vaporization of polymers and rate curves show a relatively sharp peak. (Type I) Polyvinyl chloride represents the second type. This polymer decomposes with splitting off of hydrogen chloride. The thermogravimetric curve rises rapidly at first, then level off at the moderate weight decrease and gradually rises. Polyvinyl acetate also belongs to this class. (Type II) The modification of the second type is represented by polyester. The curve at the early stage is less steep, the leveling off at the next stage is less clear and the final rising of the curve is steeper than the normal second type. Polyamide, polyurethane, and polycarbonate belong to this type. (Type II') The thermal decomposition of the third type polymers is more complex than that of others. Various irregular chain scissions including side chain splitting and depolymerization to monomers occur simultaneously. The weight of the polymer decreases gradually and the rate curve does not show sharp peaks. Polyvinyl alcohol and diene polymers belong to this type. (Type III) Generally, polycondensation polymers are more stable toward heat than addition polymers and polymers having aromatic nucleus show good thermal stability. Polymers having tertiary carbon atoms such as polystyrene or polypropylene and acetal resin start decomposition under airatmosphere at the temprature below $50^{\circ}C$ or more of the temperature where the polymers start decomposition under nitrogen atmosphere.

  • PDF

Evidence for a Common Molecular Basis for Sequence Recognition of N3-Guanine and N3-Adenine DNA Adducts Involving the Covalent Bonding Reaction of (+)-CC-1065

  • Park, Hyun-Ju
    • Archives of Pharmacal Research
    • /
    • v.25 no.1
    • /
    • pp.11-24
    • /
    • 2002
  • The antitumor antibiotic (+)-CC-1065 can alkylate N3 of guanine in certain sequences. A previous high-field $^1H$ NMR study on the$(+)-CC-1065d[GCGCAATTG*CGC]_2$ adduct ($^*$ indicates the drug alkylation site) showed that drag modification on N3 of guanine results in protonation of the cross-strand cytosine [Park, H-J.; Hurley, L. H. J. Am. Chem. Soc.1997, 119,629]. In this contribution we describe a further analysis of the NMR data sets together with restrained molecular dynamics. This study provides not only a solution structure of the (+)-CC-1065(N3- guanine) DNA duplex adduct but also new insight into the molecular basis for the sequence- specific interaction between (+)-CC-1065 and N3-guanine in the DNA duplex. On the basis of NOESY data, we propose that the narrow minor groove at the 7T8T step and conformational kinks at the junctions of 16C17A and 18A19T are both related to DNA bending in the drugDNA adduct. Analysis of the one-dimensional $^1H$ NMR (in $H_2O$) data and rMD trajectories strongly suggests that hydrogen bonding linkages between the 8-OH group of the (+)-CC-1065 A-sub-unit and the 9G10C phosphate via a water molecule are present. All the phenomena observed here in the (+)-CC-1065(N3-guanine) adduct at 5'$-AATTG^*$are reminiscent of those obtained from the studies on the (+)-CC-1065(N3-adenine) adduct at $5'-AGTTA^*$, suggesting that (+)-CC-1065 takes advantage of the conformational flexibility of the 5'-TPu step to entrap the bent structure required for the covalent bonding reaction. This study reveals a common molecular basis for (+)-CC-1065 alkylation at both $5'-TTG^*$ and $5'-TTA^*$, which involves a trapping out of sequence-dependent DNA conformational flexibility as well as sequence-dependent general acid and general base catalysis by duplex DNA.

Selective Detection of Campylobacter sp. and Campylobacter jejuni in Meat Food by Polymerase Chain Reaction (PCR을 이용한 육류 내 Campylobacter sp. 및 Campylobacter jejuni의 분리 검출)

  • Joo, Jong-Won;Hong, Kyung-Pyo;Kim, Yong-Hui;Cho, Sang-Buem
    • Journal of the East Asian Society of Dietary Life
    • /
    • v.18 no.5
    • /
    • pp.753-759
    • /
    • 2008
  • The principal objective of this study was to develop the optimum oligonucleotide primers for the simple detection of Campylobacter in food samples. In order to achieve this goal, a variety of oligonucleotide primers were designed via the modification of 16S rDNA, ceuE and mapA sequences of Campylobacter. Through the subsequent analysis of the specificity and sensitivity of primers, two types of oligonucleotide primers, CB4 and CJ1, were selected for Campylobacter genus-specific and C. jejuni species-specific primers, respectively. The detection limit was found to be $10^0{\sim}10^1$ cells per reaction with the prepared cell suspension, however, the sensitivity in the meat samples was less, at $10^1{\sim}10^2$. We suggested that PCR inhibitors such as hemoglobin or immunoglobulin in pork or beef influenced.

  • PDF

The Rate and Morphology of Mycorrhizal Infection in the Wild Ginseng (Panax ginseng C.A. Meyer) Collected from Various Locations in Korea (한국내 각지에서 채집된 산삼의 균근(菌根) 형태와 감염율)

  • Lee, Kyu-Hwa;Lee, Kyung-Joon;Park, Hoon;Budi Sri Wilarso
    • Journal of Ginseng Research
    • /
    • v.30 no.4
    • /
    • pp.206-211
    • /
    • 2006
  • To investigate mycorrhizal infection by arbuscular mycorrhizal fungi(AMF), samples of fine lateral roots were taken from the wild ginseng(Panax ginseng C.A. Meyer) naturally growing at various locations in Korea. Mycorrhiazal infections were studied by cleaning the root samples and staining fungal hyphae with frypan blue. Wild ginsengs for this study were graded by an appraisal committee consisting of 12 experts of Korea Mountain Ginseng Association. Following five quality groups were recognized: Heaven group(pure natural), Earth group (from seeding of wild ginseng), Man group(from seeding or seedlings of wild ginseng with slight environmental modification), unmarketable, and imported wild ginseng. Morphology of AMF was typical Paris-type which shows intracellular hyphal coils with rare vesicles and lack of arbuscules. Average infection rate of individual wild ginsengs was 58.3% and showed no differences among five quality groups. When portions of fine roots were quantified for mycorrhizal infection, 18.7% of the total length of the primary and secondary roots were infected by AMF. Wild ginsengs from Gyeonggi Province(84.2%), and from mountains lower than 1,200 meters above sea level(about 70%) showed higher infection rate, while the ginseng from Gyeongbuk Province(27.8%) had lower rate. Wild ginsengs at older age showed lower infection rates.

Improving Initial Abstraction Method of NRCS-CN for Estimating Effective Rainfall (유효우량 산정을 위한 NRCS-CN 모형의 초기손실량 산정방법 개선)

  • Park, Dong-Hyeok;Ajmal, Muhammad;Ahn, Jae-Hyun;Kim, Tae-Woong
    • Journal of Korea Water Resources Association
    • /
    • v.48 no.6
    • /
    • pp.491-500
    • /
    • 2015
  • In order to improve the runoff estimation accuracy of the Natural Resources Conservation Service (NRCS) curve number (CN) model, this study incorporated rainfall and maximum potential retention as contributors for initial abstraction. The modification was proposed based on 658 rank-order data of rainfall and subsequent runoff from 15 watersheds. The NRCS-CN model (M1), one of its inspired modified model (M2), and the proposed model (M3) were analyzed employing different CN approaches. Using tabulated, calculated and least squares fitted CNs ($CN_T$, $CN_C$, $CN_{LSF}$, respectively), the models' performances were evaluated based on Root Mean Square Error (RMSE), Nash-Sutcliffe Efficiency (NSE), and Percent Bias (PBIAS). Applications of model M1, M2, and M3, respectively exhibited watershed cumulative mean [RMSE (23.60, 18.12, 16.04), NSE (0.54, 0.73, 0.79), and PBIAS (36.54, 20.25, 12.00)]. Similarly, using CNC (for M1 and M2 model) and $CN_{LSF}$ (for M3 model), the performance of three models respectively were assessed based on watershed cumulative mean [RMSE (17.17, 15.88, 13.82), NSE (0.76, 0.80, 0.85), and PBIAS (3.06, 4.47, 0.11)]. The proposed model (M3) that linked all of the NRCS-CN variants showed more statistically significant agreement between the observed and estimated data.