• YAKHAK HOEJI
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• v.27 no.3
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• pp.207-213
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• 1983

Chloramphenicol (CAF) was esterified with aspirin, naproxen and acetaminophen in order to develop new prodrugs which have double effect-antibiotic activity and antipyretic effect. Chloramphenicol acetylsalicylate (CAF-ASP), chloramphenicol naproxenate (CAF-NAX), and chloramphenicol acetaminophen succinate (CAF-SUC-ACET) were synthesized by using dicyclohoxylcarbodiimidc (D.C.C.) because of two hydroxyl group of chloramphenicol. Three synthetic prodrugs did not show bitterness and antibiotic activity in vitro, and were hydrolyzed in liver homogenate, but weren't in acid.

• YAKHAK HOEJI
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• v.29 no.1
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• pp.50-54
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• 1985

Seven different sorbents were evaluated for their adsorptivity and desorptivity of antibiotic, chloramphenicol. Among the sorbents studied, Carbopak B was found to be the most efficient in enriching the chloramphenicol from dilute aqueous solution. Interfering components in the milk matrix could be washed off by water and petroleum ether from Carbopak B column, while the chloramphenicol was retained on the surface of Carbopak B. The method of simple and efficient purification and enrichment of chloramphenicol using Carbopak B, followed by quantitative analysis employing $C_{18}$ reversed phase high performance liquid chromatography has been applied to the determination of chloramphenicol in milk.

• Journal of Pharmaceutical Investigation
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• v.7 no.1_4
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• pp.38-50
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• 1977

A study on the mechanism of biliary and urinary excretion of chloramphenicol has been performed in the dog. 1) Chloramphenicol administered intravenously to dogs with ligated renal pedicle, readily appeared in bile greater than in plasma. 6.9% of a 50mg /kg i. v. dose of chloramphenicol were excreted into bile within 100 minutes. During the same periods of above experiment, the bile/plasma concentration ratios(B/P ratios) were 46 to 87. 2) Chloramphenicol injected into the vein of dog was rapidly excreted into urine. 18% of the administered dose were excreted into urine within 70 minutes. In the same periods of this experiment, Ccm/Ccr ratios were greater than 1.0 in most cases. 3) In experiment of simultaneous measurement of biliary and urinary excretion of chloramphenicol, Ccm/Ccr ratios were less than 1.0 and B/P ratios were 50 to 52. 4) In experiment measured simultaneously biliary and urinary excretion both Ccm/Ccr and $C^Hcm$(hepatic clearance) were significantly declined by probenecid, but not affected by 2,4-DNP and aminophylline although 2,4-DNP increased only bile flow and aminophylline both bile and urine volume. 5) Ccm/Ccr and $C^Hcm$ were increased in proportion to increment of plasma concentration ranging from 3.3 to 30 mg% of chloramphenicol. But when plasma concentration were increased to 70mg %, Ccm/Ccr were not increased and $C_Hcm$ were reduced about 30% in comparison with values obtajned at 30mg% of chloramphenicol. 6) Free/Bound(free to bouid from) ratios ranging from 1.0 to 90.0mg% of chloramphenicol were 76.2+3.72% $(mean{\pm}S.E.)$ Above results suggest that chloramphenicol is excreted into bile by a process of active trasport, that excretion of chloramphenicol into urine was made up with dual process, reabsorption and secretion, and that renal secretion was attained by active trasport process although renal reabsorption process could not understand.

• Journal of Microbiology and Biotechnology
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• v.15 no.5
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• pp.913-918
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• 2005

Chloramphenicol is a broad-spectrum antimicrobial agent against Gram (+) and Gram (-) bacteria. Its clinical application has recently been limited, due to severe side effects such as bone marrow suppression and aplastic anemia. In the present study, the cytotoxic effects of chloramphenicol were investigated in vitro using chronic myelogenous leukemia K562 cells. Chloramphenicol inhibited the growth of K562 cells in a dose-dependent manner, but their growth was restored after the cessation of chloramphenicol, indicating reversible cytotoxic effects. The expression of cell cycle regulatory molecules, including E2F-1 and cyclin D1, was decreased at the translational and/or transcriptional level after being treated with a therapeutic blood level ($20{\mu}g/ml$) of chloramphenicol. Chloramphenicol also induced apoptotic cell death through a caspase-dependent pathway, which was verified by Western blot analysis and the enzymatic activity of caspase-3. These results demonstrated that chloramphenicol inhibited the cell growth through arresting the transition of the cell cycle, and induced apoptotic cell death through a caspase-dependent pathway at therapeutic concentrations.

• Journal of Pharmaceutical Investigation
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• v.14 no.2
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• pp.76-85
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• 1984

Antibiotic activity and antipyretic effect of three synthetic prodrugs, chloramphenicol acetylsalicylate (CAF-ASP), chloramphenicol naproxenate(CAF-NAX) and chloramphenicol acetaminophen succinate (CAF-SUC-ACET), were studied in vitro and in vivo. In the experimental results, the CAF-NAX showed the moat rapid absorption and the highest blood levels, and the CAF-SUC-ACET and CAF-ASP also were more rapid absorption and higher blood levels than controls, chloramphenicol and chloramphenicol palmitate. The synthetic prodrugs also showed the antipyretic effect by modified Roszkowski method using endotoxin.

• Journal of Veterinary Clinics
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• v.15 no.2
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• pp.378-385
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• 1998

Chloramphenicol주사에 의한 좌골신경손상을 유발한 후 Prednisolone을 이용한 약물처치군, 전침군 및 전침과 약물을 병용한 군에서 각각 회복속도를 비교하였다. 정상보행 횟수, pinching을 통한 감각신경의 통감반응,그리고 병리조직소견 등을 죠사한 결과를 요약 하면 다음과 같다. Enrofloxacin, cefazolin, cephalexin, penicillin 등의 좌골신경주위 주사게 서는 신경마비가 관찰되지 않았으나 chloramphenicol을 주사할 경우에는 좌골신경손상으로 인한 편측성 후지마비가 유발되어 knuckling 반응을 보였다. Chloramphenicol을 투여한후 좌골신경손상에 대한 각 처치에서 정상보행 횟수는 8-12주까지는 침술처치군이 약간 중가하 였으나, 처리군간 유의성은 관찰되지 않았다. 실험기간동안 chloramphenicol 에 의한 신경손 상에 대한 각 처치군별 병리조직 소견은 호전양상이 관찰되지 아니하였다.

• YAKHAK HOEJI
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• v.29 no.2
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• pp.55-61
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• 1985

The effect of dietary fat on the immunotoxicity of chloramphenicol was investigated in mice, sensitized and challenged with sheep red blood cells. Chloramphenicol suppressed more cell-mediated immunity than humoral immunity. The saturated fat diet elevated humoral and cell-mediated immunotoxicity, whereas the unsaturated fat diet decreased humoral immunotoxicity, but elevated cell-mediated immunotoxicity of chloramphenicol. Especially, the normal diet in saturated and unsaturated fat restored immunosuppressive effect of chloramphenicol compared to the saturated fat diet and the unsaturated fat diet.

• The Korean Journal of Mycology
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• v.15 no.2
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• pp.87-91
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• 1987

The in vitro interactions between antibiotics(ampicillin, kanamycin, cephalexin, oxytetracycline and chloramphenicol) and ginseng saponin were studied by the chessboard method against bacteria(Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Mycobacterium smegmatis). Ampicillin, kanamycin, oxytetracycline and chloramphenicol against Bacillus subtilis, and ampicillin and cephalexin against Staphylococcus aureus were synergistic in the presence of gi­nseng saponin. Whereas kanamycin, oxytetracycline and chloramphenicol against Staphylococcus aureus, and ampicillin, Kanamycin, cephalexin, oxytetracycline and chlorampheniol against Escherichia coli, and ampicillin, kanamycin, and chloramphenicol against Pseudomonas aer­uginosa, and ampicillin and chloramphenicol against Mycobacterium smegmatis were indiffer­ent in the presence of ginseng saponin. Antagonisms between antibiotics and ginseng saponin were not observed in this study.

• Bulletin of the Korean Chemical Society
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• v.34 no.6
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• pp.1839-1844
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• 2013

Molecularly imprinted microsphere for chloramphenicol (CAP) with high adsorption capacity and excellent selectivity is prepared by aqueous suspension polymerization, in which chloramphenicol is used as template molecule and ethyl acetate as porogen. The CAP-imprinted microspheres are used as high performance liquid chromatography (HPLC) stationary phase and packed into stainless steel column ($150mm{\times}4.6mm$ i.d.) for selective separation of chloramphenicol. HPLC analysis suggests that chloramphenicol can be distinguished from not only its structural analogs but also other broad-spectrum antibiotic such as erythromycin and tetracycline. In addition, the binding experiments of CAP-imprinted microspheres are carried out in ethanol/water (1:4, V:V), the results indicate that the maximum apparent static binding capacity of molecularly imprinted microspheres is up to 66.64 mg $g^{-1}$ according to scatchard model.

• Journal of the Korean Chemical Society
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• v.36 no.4
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• pp.552-557
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• 1992

Chloramphenicol was studied by differential pulse polarography (DDP). A reduction peak which is dependent on pH of the solution appeared in the voltage range between zero and -1.50 volt vs. Ag/AgCl (sat. KCl) reference electrode. A plot of peak potentials (Ep) measured at room temperature (20$^{\circ}C$) vs. pH of the chloramphenicol solutions showed linear relationship changing slope (Ep/pH) at pH 8.9. The slope was -59.7 mV/pH in pH 2.7∼8.9 and -24.3 mV/pH in pH 8.9∼11.2, respectively. A log plot of peak currents (ip) vs. concentrations showed a linearity at the concentrations between 4.8 ${\times}$ 10$^{-7}$ M and 6.2 ${\times}$ 10$^{-5}$ M (0.16 ppm∼20 ppm) chloramphenicol in pH 8.0 ammonium buffer. Between the DPP method and the reference method measuring absorbance at 278 nm, the correlation coefficient was 0.996, which means an excellent linearity. The DPP method was able to detect degradation products of chloramphenicol in mild alkaline solution (pH = 8.0) more distinctly than the spectrophotometric method.