• Title/Summary/Keyword: Drug transfer

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A Stereoselective Asymmetric Synthesis of Antibiotic (-)-Fumagillol Using Claisen Rearrangement and Intramolecular Ester Enolate Alkylation as Key Steps

  • Kim Deukjoon;Ahn Soon Kil;Bae Hoon;Kim Hak Sung
    • Archives of Pharmacal Research
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    • v.28 no.2
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    • pp.129-141
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    • 2005
  • (-)-Fumagillol (1), a hydrolysis product of fumagillin, has been synthesized by several group from commercially available 1,2:5,6-di-O-isopropylidene-${\alpha}$-D-allofuranose in a highly stereoselective manner. Chiral centers on C5 and C6 came from D-allofuranose and the asymmetric center on C4 was accomplished by 1,3-chirality transfer using the Claisen rearrangement on a chiral allyl alcohol. Chirality, which is necessary on an epoxide consisting of the spiro-ring system, was diastereoselectively constructed by the well-known reaction, intramolecular ester enolate alkylation (IEEA), which showed that this reaction can be applied to the alpha-alkoxy ester system. The epoxide on the side chain was regioselectively introduced by the difference between the number of substituents on the vinyl groups. This accomplishment proved that IEEA can be a useful tool for the synthesis of complex molecules.

Drug Resistance and R Plasmids of Escherichia coli in Patients and Healthy Individuals in Korea (한국(韓國)의 환자(患者) 및 건강인(健康人)에서 분리(分離)한 E.coli의 약제내성(藥劑耐性) 및 R Plasmids)

  • Seol, Sung-Yong
    • The Journal of the Korean Society for Microbiology
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    • v.12 no.1
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    • pp.11-18
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    • 1977
  • A total of 665 strains of Escherichia coli isolated in Korea from stools of patients who were treated with antimicrobial drugs, doctors, and students were tested for the drug resistance and distribution of R plasmids. Approximately 25 to 41% of isolates were resistant to chloramphenicol, tetracycline, streptomycin, sulfisemidine and ampicillin(AP), and 9.5% were resistant to kanamycin. Nalidixic acid-resistant strains were only rarely encountered. The prevalence of resistant strains was significantly higher among patients than doctors and students. Strains multiply resistant to four or more drugs were significantly more prevalent among patient isolates than those from doctors and students, while no difference on the incidence of strains resistant to three or less drugs was noted among isolates from the three groups. The persons carrying strains resistant to four or more drugs were more frequently found among patients than doctors and students. Quite large proportions of drug-resistant strains transferred their resistance to drug-sensitive E. coli, with frequent transfer of whole resistance and AP resistance. Strains having higher multiplicity of resistance showed a tendency toward higher incidence of resistance transfer, irrespective of the origins of strains.

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Preparation of Chitosan-Gold and Chitosan-Silver Nanodrug Carrier Using QDs (QDs를 이용한 키토산-골드와 키토산-실버 나노약물전달체 제조)

  • Lee, Yong-Choon;Kang, Ik-Joong
    • Korean Chemical Engineering Research
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    • v.54 no.2
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    • pp.200-205
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    • 2016
  • A drug transport carrier could be used for safe send of drugs to the affected region in a human body. The chitosan is adequate for the drug delivery carrier because of adaptable to living body. The gold, a metallic nanoparticles, tends to form a nano complex at rapidly when it combined with chitosan because of its negative charge. having energy from the other, outer gold nano-complex make heat due to its property to release the contained drugs to the target area. Silver could be also formed an useful biocompatible nano-composites with chitosan which should be used as an useful drug transfer carrier because its special ability to protect microbial contamination. Being one of the oxidized nano metals, $Fe_3O_4$ is nontoxic and has been used for its magnetic characteristics. In this study, the control of catalyst, reducing agent, and solvent amount. The chitosan-$Fe_3O_4$-gold & silver nanoshell have been changed to form about 100 nm size by ionic bond between the amine group, an end group of chitosan, and the metal. It was observed the change in order to seek for its optimum reaction condition as a drug transfer carrier.

DIFFERENTIAL INDUCTION OF RAT LIVER MICROSOMAL CYTOCHROME-DEPENDENT MONOOXYGENASE AND UDP-GLUCURONOSYLTRANSFERASE ACTIVITIES BY VARIOUS NARCOTIC DRUGS

  • Hong, Young-Sook;Pae, Young-Sook
    • Toxicological Research
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    • v.5 no.1
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    • pp.17-25
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    • 1989
  • Chronic adminstraction of morphine to adult male rats has long been known to lower hepatic cytochrome p-450 content and its dependent mixed-function oxidase activity. Following the treatment of adult male rats with morphine, pethidine pentazocine and codeine and also by concomitant adminstration of naloxone activities of microsomal electron transfer in the adult male rats were examined. In present study, the acute treatment of mature male rats with a dose of narcotic drugs higher than that used chronically also reduces their hepatic cytochrome p-450.

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Current Status of Gene Therapy as a New Drug Delivery System (신약전달기술체계인 유전자 치료의 현재까지의 개발동향)

  • Bae, Yun-Sung;Cho, Jung-Yoon;Ji, Sang-Mi;Lee, Young-Joo
    • Journal of Pharmaceutical Investigation
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    • v.32 no.3
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    • pp.153-159
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    • 2002
  • Gene therapy is fundamentally a sophisticated drug delivery technology to cure a disease by the transfer of genetic material to modify living cells. In other words, the gene is used as a therapeutic drug much like a chemical compound is employed in chemotherapy. Currently almost 600 clinical trials are underway worldwide since the first clinical trials carried out in 1990 to treat adenosine deaminase deficiency using retroviral vectors. Despite the great progress still is there no gene therapy product being approved as a new drug. This is partly due to a lack of an ideal gene delivery system that is safe and can provide stable, optimal level production of the therapeutic proteins in the cell. This review covers the current status of several different biological and physico-chemical agents that are being developed as gene delivery vehicles. Although gene therapy promises great hopes toward the cure of a broad spectrum of genetic and acquired diseases, the success of gene therapy heavily asks for the development of vector systems for safe and efficient application in humans.

Comparison of Embryo Production Performance and Conception Rate after Embryo Transfer between Mongolian Cattle and Korean Native Cattle

  • Chuluundorj, Gantugs;Lee, Ho-Jun;Son, Dong-Soo;Ganbaatar, Enkhmanlai;Tumur, Baldan;Yoon, Jong-Taek
    • Journal of Embryo Transfer
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    • v.32 no.4
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    • pp.319-324
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    • 2017
  • This study is to compare the effect of estrus synchronization and embryo transfer between Korean and Mongolian cattle. Embryos were collected from 9 donors housed in Asan city in South Chungcheong Province, South Korea. Embryos were collected 9 donors from Khushaat sum, Selenge province and Bayanchandmani sum, Tov province in Mongolia. Follicle Stimulating Hormone (FSH), Controlled Internal Drug Release (CIDR) and Prostaglandin (PG) were used for superovulation. Subsequently, Artificial Insemination (AI) was done for donor cow and embryo was collected after 7 and 8 days. Collected embryos were compared between Mongolian and Korean cattle. Finally, good quality and fresh embryos were transferred to 50 and 22 recipients of cows in Korea and Mongolia respectively. The findings show that Korean native cattle each donor cow produced on an average 16.9 embryos and, 10.9 embryos were found transferable. But in case of Mongolia the average production of embryos per donor cow was 8.6 embryos and, 6.2 embryos were found transferable. Embryo collection after 7 and 8 days was not difference in embryo production in Korea. But, in Mongolia embryo production after 8 days was found more efficient than the 7 days. Korean native recipient's cows (74.6%) and Mongolian recipient's cows (71.0%) respectively were found transferable ovarian stage. The result suggested that efficiency of embryo production from the superovulation method treated of Korean cow were higher than the Mongolian cow. The pregnancy rate of Korea native cattle was 72%, which was about 10% higher than that of Mongolia cattle.

Optimization of In Vivo Embryo Production and Pregnancy following Embryo Transfer in Hanwoo Cattle

  • Jeon, Soon-Hong;Jung, Kyoung Sub;Choi, Jae-Won;Heo, Young-Tae;Xu, Yong-Nan;Kim, Nam-Hyung
    • Journal of Embryo Transfer
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    • v.28 no.4
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    • pp.307-314
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    • 2013
  • Embryos formed in vivo were collected from 171 donors housed in Chung Cheong Buk-Do Institute of Livestock and Veterinary Research of the Chungbuk community during the years 2009~2012. We evaluated annual embryo collection, effect of follicle stimulating hormone (FSH), controlled internal drug release (CIDR) and prostaglandin (PG) administration to the donor for superovulation and controlling the estrus cycle, seasonal effects of embryo collection and compared the number of embryos recovered as per the collection days and pregnancy rate. In all, 1,243 embryos were collected from 118 donors with an average of $7.31{\pm}5.35$ embryos per donor, out of which 69.4% were transferable. Dosages of FSH required for inducing superovulation in various donors were compared. Average number of embryos collected from donors administered with 30 AU of FSH ($7.13{\pm}5.74$ per donor) was not significantly different from that of donors who were given an injection of 24 AU of FSH ($7.53{\pm}4.91$ per donor). However, the percentage of transferable embryos in the 30AU FSH-administered group (63.2 %, 449 of 711) was higher than that in the 24AU FSH-administered group (77.8%, 414 of 532). In the group of donors under a natural estrus cycle, the FSH dose administered did not influence the number of transferable embryos produced ($7.49{\pm}6.25$ per donor for 30 AU of FSH vs $7.49{\pm}4.92$ per donor for 24 AU of FSH). However, in donors administered with CIDR and PG for controlling the estrus cycle, the FSH dose affected the average number of transferable embryos collected ($4.25{\pm}2.87$ per donor for 30 AU of FSH vs $8.50{\pm}6.36$ per donor for 24 AU of FSH). We collected embryos from donors 6, 7 or 8 days after artificial insemination (AI). Results showed that the percentage of transferable embryos among those collected 8 days after AI was significantly higher than that among embryos collected 6 or 7 days after AI. Seasonal variations did not affect number of recovered embryos and pregnancy rates in natural estrus cycle and CIDR treatment groups (48.28% and 42.55%) but higher than pregnancy rate of frozen embryos (19.63%). These results indicated that administration of FSH beyond a threshold dose (at least 24 AU) has no beneficial effect on the production embryos and that collection of embryos 7~8 days after AI is optimal for embryo recovery. CIDR treatment induced superovulation in short term and had no influence on the natural estrus cycle. Finally, although good-quality embryos were transferred, freezing significantly reduced the pregnancy rates after transfer.

Isolation of antibiotic resistant Lactobacillus spp from fermented milk and starters, and detection of transmissible R plasmids (유산균 발효유 및 starter에서 항생제내성 유산균 분리 및 전달성 R plasmids 분포조사)

  • Baek Kui-Jeong;Seo Heyng-Seok;Roh Young-Sun;Yang Hae-Dong;Hur Boo-Hong;Seo Lee-Won;Joung Dong-Suk;Song Hee-Jong
    • Korean Journal of Veterinary Service
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    • v.29 no.3
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    • pp.277-285
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    • 2006
  • Plasmids are covalently closed circular molecules of DNA that are stably inherited and replicate somewhat independently of the bacterial chromosome. Genes carried on plasmids can mediate a wide variety of important functions, including antibiotics (R plasmids) and heavy metals resistance, toxins production, cell penetration, iron chelation, complement resistance, and metabolic characteristics such as sucrose and lactose fermentation. Fifty strains of lactobacilli were isolated from 26 staters and 29 fermented milk products. They were classified 27 strains as Lactobacillus paracasei subsp paracasei, 11 stains as Lactococcus lactis subsp cremoris, 6 strains as L delbrueckii subsp lactis, 4 strains as L acidophius, and 2 strains as L delbrueckii subsp bulgaricus. All of these strains were examined for drug resistance and transferability of R plasmids. All of the isolates were sensitive to Am, C, CF, E, NB, P, T, and Te. But resistant to SXT 94% (47 strains), K 66% (33 strains), S 56% (28 strains), ENR 50% (25 strains), NOR 38% (19 strains) CIP 38% (19 strains), GM 16% (8 strains), and N 14% (7 strains), in order. And 32 different resistant patterns were found. The most frequently encountered patterns were CIP-ENR-K-NOR-S-SXT (5 strains). In vitro R plasmids transfer experiment, 57 antibiotic resistant strains which were not transfer to the recipient 2 Escherichia coli strains by conjugation, These results indicate that Lactobacillus in internal trade market' stater recognize R factor but transmissible R plasmid is not existed.

Comparison of Methods for Detection of Escherichia coli O157:H7 in Ground Beef and Radish Sprouts

  • Lee, Jae-Hoon;Hyeon, Ji-Yeon;Heo, Seok;Hwang, In-Gyun;Kwak, Hyo-Sun;Choi, In-Soo;Park, Chan-Kyu;Seo, Kun-Ho
    • Food Science of Animal Resources
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    • v.30 no.2
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    • pp.179-184
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    • 2010
  • Escherichia coli O157:H7 is a food-borne pathogen that causes bloody diarrhea, hemorrhagic colitis, and hemolytic uremic syndrome (HUS). We compared three selective media and evaluated the performance of immunomagnetic separation (IMS) for the detection of low levels of E. coli O157:H7 in ground beef and radish sprouts with different levels of background flora. Bulk food samples (500 g for each trial) were artificially inoculated with nalidixic acid-resistant E. coli O157:H7 at the lowest dose that would generate 20 partial-positive samples of 25 g each. All samples were homogenized in mTSB (225 mL) and incubated overnight at $37^{\circ}C$. IMS was performed using the enriched mTSB samples (1 mL) along with conventional spreads plated onto three different selective media: Sorbitol MacConkey agar (SMAC), Sorbitol MacConkey agar with cefixime and tellulite (CT-SMAC), and Sorbitol MacConkey agar with nalidixic acid (NAL-SMAC) as the gold standard. Two suspicious colonies from each medium were selected and confirmed usinga serological test after transfer to tryptic soy broth with yeast extract (TSAYE). CT-SMAC was better than SMAC for detecting E. coli O157:H7 in all food types. Although there was no statistical difference in the number of positive samples when using IMS vs. non-IMS techniques, more positive samples were detected when IMS was used in both ground beef and radish sprouts. It appears that the improvement was more significant in radish sprouts, which had a higher level of background flora than ground beef. The results also suggest that the combination of CT-SMAC and IMS is sufficient to recover low levels of E. coli O157:H7 in high background flora food samples.