• Title/Summary/Keyword: semisynthetic

Search Result 42, Processing Time 0.03 seconds

Teratogenicity Study of KTC-1, a New Semisynthetic Rifamycin Derivative, in Rats (새로운 반합성 Rifamycin 유도체 KTC-1의 랫트 최기형 시험)

  • 김종춘;정문구;박종일;한상섭
    • Toxicological Research
    • /
    • v.11 no.1
    • /
    • pp.81-89
    • /
    • 1995
  • A teratogenicity study of KTC-1, a new semisynthetic rifamycin antituberculous drug, was conducted in Sprague-Dawley rats. Dosages of KTC-1 0, 7, 21, and 63 mg/kg/day were administered to darns orally gayage from day 7 to day 17 of gestation. Two-third of dams per group were subjected to cesarean section on day 21 of pregnancy for examination of their fetuses, and the remaining one-third of darns per group were allowed to deliver naturally for postnatal examination of their offspring. At 21 mg/kg/day, an increase in the skeletal variations of F1 fetuses and a decrease in the body weight of F1 offspring were seen. At 63 mg/kg/day, a loss in body weight was observed in darns. An increase in fetal death rate, a decrease in litter size and body weight, and an increase in the incidence of visceral malforrnations and skeletal variations were found in F1 fetuses. In particular, lumar rib occurred at an incidence of 31%. In addition, an increase in the dead newborns at birth and neonatal deaths during the lactation period, a loss in body weight, and a decrease in spleen weight were observed in F1 offspring. There were no signs of maternal toxicity or embryotoxicity at 7 mg/kg/day. The results suggest that the no-effect dose level(NOEL)for dams is 21 mg/kg/day, and NOELs for F1 fetuses and offspring are 7 mg/kg/day.

  • PDF

Validation of an Extraction Method for the Determination of Airborne MWFs using Alternative Solvents (대체용매를 이용한 금속가공유 측정방법 타당성 평가)

  • Jeong, Jee Yeon;Baek, Nam Won
    • Journal of Korean Society of Occupational and Environmental Hygiene
    • /
    • v.16 no.2
    • /
    • pp.91-100
    • /
    • 2006
  • The purpose of this study was to validate alternative method by using non-carcinogenic, and less toxic solvents than NIOSH analytical method 5524 for measuring the airborne MWFs in workplaces. In laboratory tests, the ETM solvents(mixture of same volume for ethyl ether, toluene, and ethanol) were selected. The alternative method of analyzing MWFs, referred to as the ETM solvent extraction method, showed 0.04 mg/sample as LOD, and 0.15 mg/sample as LOQ. The analytical precision (pooled CV, coefficient of variation) of the ETM solvent extraction method for analyzing the straight, soluble, semisynthetic, and synthetic metalworking fluid was 1.5%, 2.0%, 2.6%, 1.6%, respectively, which was similar to the precision (2.6%) of NIOSH analytical method (NIOSH 0500) for total dust. The analytical accuracy by recovery test, spiked mass calculated as extractable mass, was almost 100%. As the result of storage stability test, metalworking fluid samples should be stored in refrigerated condition, and be analyzed in two weeks after sampling. The 95% confidence limit of the estimated total standard error for the ETM solvent extraction method for analyzing the straight, soluble, semisynthetic, and synthetic metalworking fluid was ${\pm}12.6%$, ${\pm}12.5%$, ${\pm}14.0%$, and ${\pm}13.6%$, respectively, which satisfied the OSHA sampling and analytical criteria.

Fertility Study of KTC-1, a New Semisynthetic Rifamycin Derivative, in Rats. (새로운 반합성 Rifamucin 유도체 KTC-1의 랫트 수태능력 시험)

  • 김종춘;정문구;노정구
    • Toxicological Research
    • /
    • v.12 no.1
    • /
    • pp.93-99
    • /
    • 1996
  • The effect of KTC-1, a new semisynthetic rifamycin antituberculous drug, on general toxicity, reproductive capability and fetal development was investigated in Sprague-Dawley rats. Male rats were administered KTC-1 with mashed feed from 63 days before mating to the end of mating period, and female rats were given from 14 days before mating to day 7 of gestation at dose levels of 0, 375, 750, and 1,500 ppm. The females were sacrificed on day 21 of gestation for examination of their fetuses. At 1,500 ppm, a reduction in body weight gain and testis atrophy were observed in male rats. Histological examination revealed testicular atrophy, absence or decrease of germinal cells, and vacuolization of Sertoli cells in testis. A reduction in body weight gain, a decrease in food consumption were found in female rats. In addition, decreases in the number of corpora lutea, iraplantations, and the litter size of live fetuses were seen. Mating, fertility, and pregnancy performances were also affected. There were no external abnormalities observed by examination of fetuses. At 750 ppm, a reduction in the body weight gain of male and female rats and decreases in the number of implantations and litter size were found. At 375 ppm, no treatment-related effects were observed. The results suggest that the no-effect dose levels (NOELs) of KTC-1 are 375 ppm for males and females on general toxicity, 750 ppm for males and females on reproductive capability, and 375 ppm for fetuses on embryonic development.

  • PDF

Taxol Production in Taxus spp. Cell Culture : Semisynthesis of Taxol from Baccatin III in Cell Cultures of Taxus baccta Pendula (주목 세포배양에 의한 Taxol 생산 : 유럽 주목의 세포배양에서 추출한 Baccatin III로부터 Taxol의 반합성)

  • 전정욱;조병관
    • KSBB Journal
    • /
    • v.11 no.3
    • /
    • pp.263-269
    • /
    • 1996
  • Anticancer agent taxol was synthesized from baccatin III which was extracted from cell cultures of European yew, Taxus baccata Pendula. Callus and suspension cultures of T. baccata Pendula showed the formation baccatin III. The content of baccatin III in cell cultures reached 0.015% (w/w) on dry weight basis. The semisynthetic approaches were made with baccatin III and taxol side chain. To prepare taxol side chain, (-)-N-((S)-2-hydroxy-1-phenylethyl) benzamide was synthesized first from (S)-(+)-phenylglycine. Then (-)-N-((IS,2S)-2-hydroxy-1-phenyl-3-butenyl) benzamide was synthesized with vinyl magnesium bromide. The synthesis of (2R, 3S)-(-)-2-(1-ethoxyethoxy)-3-phenyl-3-(phenylmethanamido) propanoic acid with RuCl3, catalyst was the final step to prepare taxol side chain. The semisynthetic reactions yielded 0.0002% taxol, 0.0005% 7-epi-10-deacetyltaxol, and unidentified taxanes on dry weight basis. It is suggested that the semisynthesis of taxol from baccatin III could be an alternative source of taxol and related taxanes.

  • PDF

The Effect of Choline Deficiency on Lipid Metabolism in Chicks (콜린 결핍이 병아리의 지질대사에 미치는 영향)

  • Lim, Hyeon-Sook;Park, Jeong-Ro;B-H Simon Cho
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.21 no.3
    • /
    • pp.247-254
    • /
    • 1992
  • In the experiment in which young chicks were fed the semisynthetic diet devoid of choline or the same diet with butanolamine supplementation, the weight gain was decreased significantly accompanied by the reduction of feed consumption in choline deficient chicks as compared to control chicks. However, the overall effects of choline deficiency on the relative liver weight, lipid contents of liver, and plasma lipid and lipoprotein levels were not observed, nor was the response to choline deficiency on the incorporation of $^{14}$ C-oleic acid into lipids in the liver microsomes. When hyperlipidemia was induced by estrogen treatment, the liver lipids, as well as relative liver weight, showed a tendency to be increased only in the chicks fed the semisynthetic diet devoid of choline with butanolamine supple-mentation. And the magnitude of elevation of VLDL lipids by estrogen treatment was the lowest in the above group. These results indicated that young chicks were not able to synthesize considerable choline for normal growth ; nevertheless, the release of VLDL by hepatocytes was performed normally. But it was also implied that there might be some problems of VLDL release under the condition of hyperlipidemia in chicks in choline deficiency accelerated by butanolamine supplementation.

  • PDF

Computational Approach for Biosynthetic Engineering of Post-PKS Tailoring Enzymes

  • Kim, Ki-Bong;Park, Kie-Jung
    • Genomics & Informatics
    • /
    • v.6 no.4
    • /
    • pp.227-230
    • /
    • 2008
  • Compounds of polyketide origin possess a wealth of pharmacological effects, including antibacterial, antifungal, antiparasitic, anticancer and immunosuppressive activities. Many of these compounds and their semisynthetic derivatives are used today in the clinic. Most of the gene clusters encoding commercially important drugs have also been cloned and sequenced and their biosynthetic mechanisms studied in great detail. The area of biosynthetic engineering of the enzymes involved in polyketide biosynthesis has recently advanced and been transferred into the industrial arena. In this work, we introduce a computational system to provide the user with a wealth of information that can be utilized for biosynthetic engineering of enzymes involved in post-PKS tailoring steps. Post-PKS tailoring steps are necessary to add functional groups essential for the biological activity and are therefore important in polyketide biosynthesis.

METHICILLIN RESISTANT STAPHYLOCOCCAL INFECTION;REPORT OF 2 CASES (Methicillin Resistant Staphylococcal Infection;증례보고)

  • Kim, In-Soo;Kim, Young-Kyun
    • Maxillofacial Plastic and Reconstructive Surgery
    • /
    • v.23 no.2
    • /
    • pp.180-184
    • /
    • 2001
  • MRSI is the staphylococcal infection having resistance to the methicillin which is semisynthetic penicillinase-resistant agents against penicillinase. These infections are very difficult to treat because they have resistance to almost every antibiotics except for vancomycin. We experienced MRSE(methicilline-resistant staphylococcal epidermis) infected 56 years old man who developed 2 months after arthroplasty for TMJ ankylosis and MRSA(methicilline-resistant staphylococcal aureus) infected 59 years old man who was performed arthroplasty far traumatic TMJ disc displacement.

  • PDF

Inhibition of NF-kB/Rel by Paclitaxel in Mouse Macrophages

  • Lim, Jin-Soo;Lee, Seog-Ki;Jeon, Young-Jin
    • Toxicological Research
    • /
    • v.23 no.1
    • /
    • pp.19-24
    • /
    • 2007
  • We demonstrate that paclitaxel, an antitumor agent derived from yew tree, inhibits LPS- and $IFN-{\gamma}$-induced NF-kB/Rel activation in RAW 264.7 cells. Previously, paclitaxel ($>10{\mu}M$) has been known to induce iNOS gene expression in macrophages. However, in the previous report we described that the pretreatment of macrophages with low concentration of paclitaxel ($0.1{\mu}M$) for 8 h inhibited LPS-induced iNOS gene expression. Pretreatment of RAW 264.7 cells with paclitaxel significantly inhibited NF-kB/Rel transcriptional activation. Electrophoretic mobility shift assay further confirmed that pretreatment of macrophages with paclitaxel inhibited NF-kB/Rel DNA binding. Taxotere, a semisynthetic analog of paclitaxel, also inhibited LPS- and $IFN-{\gamma}$-induced iNOS gene expression. Collectively, these series of experiments indicate that paclitaxel inhibits iNOS gene expression by blocking NF-kB/Rel activation.

Enumeration and Recovery of Bacterial Isolates from Ruminants Fed with Different Dietary Regimes and Their Antibacterial Activity

  • Pattnaik, P.;Grover, Sunita;Batish, V.K.
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.14 no.6
    • /
    • pp.811-815
    • /
    • 2001
  • The study evaluated different synthetic and semisynthetic media for maximal recovery of rumen bacteria and expression of their antibacterial activity. Rumen Glucose Cellobiose Agar (RGCA) medium was found to be the best for recovery of rumen bacteria. However, L-10 medium was the best for expression of antibacterial activity of ruminal isolates followed by Easy, M-10, RGCA and M-98-5 medium. The present study recommends the use of L-10 medium as the medium of choice for screening of antibacterial activity of ruminal isolates. Comparative evaluation of bacterial counts on different dietary regimes indicated significant difference between different growth media on a specific diet and between diets on specific growth media within a species. However, there is no overall significant difference between total bacterial counts obtained from rumen liquor of cattle and buffalo with respect to either the feeding regime or growth media. Feeding straw based diet to the animal is the best for high recovery of rumen bacteria.

Isolation and Characterization of a Cephalosporin C Resistant and 7-Aminocephalosporanic Acid Sensitive Strain (Cephalosporin C 내성과 7-Aminocephalosporanic Acid 감수성을 지닌 균주의 선발 및 특성)

  • Kim, Ook-Hyun;Park, Yong-Chjun;Lim, Jai-Yun;Kim, Young-Chang
    • Microbiology and Biotechnology Letters
    • /
    • v.23 no.5
    • /
    • pp.556-558
    • /
    • 1995
  • A strain which showed cephalosporin C resistance and 7-aminocephalosporanic acid sensitivity was isolated from nature. Among the isolates, SS5 was sensitive to cephalosporin C, penicillin G, ampicillin, 7-aminocephalosporanic acid, 6-aminopenicillanic acid, and 7-aminodeacetoxy cephatosporanic acid at concentrations of 1,000 $\mu $g/ml, 2,000 $\mu $g/ml, 3,000 $\mu $g/ml, 30 $\mu $g/ml 100 $\mu $g/ml and 100 $\mu $g/ml, respectively. But SS5 was sensitive at very low concentration of chloramphenicol, kanamycin, neomycin, streptomycin and tetracycline. Since SS5 was sensitive to 7-ACA (30 $\mu $g/ml) and didn't have $\beta $-lactamase activity on the cephalosporin C, SS5 could be useful as an indicator strain for the production of 7-ACA, which is an important precursor for the synthesis of many semisynthetic cephalosporins.

  • PDF