Thiamphenicol
(Synonyms: 甲砜霉素; Thiophenicol; Dextrosulphenidol) 目录号 : GC17076
Thiamphenicol是Chloramphenicol的甲砜基衍生物，是一种广谱抗菌抗生素。
Cas No.:15318-45-3
Sample solution is provided at 25 µL, 10mM.
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Thiamphenicol, a methyl-sulfonyl derivative of Chloramphenicol, is a broad-spectrum antimicrobial antibiotic[1]. Thiamphenicol acts by binding to the 50S ribosomal subunit, leading to inhibition of protein synthesis and bacteriostatic effect[2]. Thiamphenicol exhibits inhibitory activity against Gram-positive bacteria, Gram-negative aerobes, and anaerobes, and is commonly employed in studies of bacterial infection mechanisms and the mode of action of antibacterial agents[3][4].
In vitro, in agar culture system, Thiamphenicol (36μg/mL; 8 or 24h) reversibly suppresses mouse bone marrow CFC proliferation and markedly reduces colony formation via inhibition of mitochondrial protein synthesis, while simultaneously skewing CFC differentiation toward macrophage colonies (97–100% versus 20–50% in controls) and reducing granulocytic colonies to<5%[5].
In vivo, Thiamphenicol (216mg/kg; i.p.) administered 1h before LPS challenge and maintained for 12h significantly decreased the lung wet-to-dry ratio in LPS-induced ALI mice, reduced neutrophil and total cell counts in bronchoalveolar lavage fluid, suppressed IL-6 and IL-1β mRNA expression in lung tissue, and reversed LPS-induced ultrastructural damage to the alveolar–capillary barrier and degradation of VE-cadherin protein[6]. Thiamphenicol (250mg/kg; subcutaneously implanted dialysis bag; 7 days) significantly reduced peripheral reticulocyte counts and caused a decline in total red blood cell numbers in normal rabbits; in phlebotomized anaemic rabbits, this dosage markedly suppressed the proliferation and differentiation of erythroid progenitor cells in the marrow, decreasing the erythroid precursor fraction from 75% to 0%, while also lowering reticulocyte haemoglobin synthesis rate and ribosomal content without affecting plasma erythropoietin levels[7].
References:
[1] Mariani L. Cloramfenicolo e tiamfenicolo [Chloramphenicol and thiamphenicol]. Clin Ter. 1978;86(3):195-218.
[2] Marchese A, Debbia EA, Tonoli E, Gualco L, Schito AM. In vitro activity of thiamphenicol against multiresistant Streptococcus pneumoniae, Haemophilus influenzae and Staphylococcus aureus in Italy. J Chemother. 2002;14(6):554-561.
[3] Dinos GP, Athanassopoulos CM, Missiri DA, et al. Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions. Antibiotics (Basel). 2016;5(2):20.
[4] Raymond J, Boutros N, Bergeret M. Place du thiamphénicol dans le traitement des pneumopathies communautaires [Role of thiamphenicol in the treatment of community-acquired lung infections]. Med Trop (Mars). 2004;64(1):33-38.
[5] Ratzan RJ, Moore MA, Yunis AA. Effect of chloramphenicol and thiamphenicol on the in vitro colony-forming cell. Blood. 1974;43(3):363-369.
[6] Zhang Z , Xie J , Shan N ,et al.Discovery of the specific inhibitory effect of thiamphenicol on LPS-induced acute lung injury (ALI) in mice through virtual screening and biological evaluation.Journal of Molecular Structure. 2022, 1257:132638.
[7] Nijhof W, Wierenga PK, Kardaun S. The effect of thiamphenicol on the production of immature red blood cells under anaemic conditions. Br J Haematol. 1977;36(1):29-40.
Thiamphenicol是Chloramphenicol的甲砜基衍生物，是一种广谱抗菌抗生素[1]。Thiamphenicol通过与50S核糖体亚基结合，抑制蛋白质合成，从而发挥抑菌作用[2]。Thiamphenicol对革兰氏阳性菌、革兰氏阴性需氧菌及厌氧菌均具有抑制作用，常用于细菌感染机制及抗菌药作用模式的研究[3][4]。
体外实验中，在琼脂培养体系中，Thiamphenicol（36μg/mL；作用8或24小时）通过抑制线粒体蛋白质合成，可逆性抑制小鼠骨髓集落形成细胞（CFC）的增殖并显著减少集落形成，同时使CFC向巨噬细胞集落分化比例从20–50%升高至97–100%，粒细胞集落比例降至<5%[5]。
体内实验中，Thiamphenicol（216mg/kg；腹腔注射）于LPS刺激前1小时给药并持续12小时，可显著降低LPS诱导的急性肺损伤（ALI）小鼠肺湿干比，减少支气管肺泡灌洗液中的中性粒细胞及总细胞数，抑制肺组织IL-6和IL-1β mRNA表达，并逆转LPS引起的肺泡–毛细血管屏障超微结构损伤及VE-钙黏蛋白降解[6]。Thiamphenicol（250mg/kg；皮下植入透析袋给药；7天）在正常兔中显著减少外周血网织红细胞数量并导致红细胞总数下降；在放血性贫血兔中，该剂量显著抑制骨髓红系祖细胞的增殖与分化，使红细胞前体比例自75%降至0%，同时降低网织红细胞血红蛋白合成速率及核糖体含量，而不影响血浆促红细胞生成素水平[7]。
| Cell experiment [1]: | |
Cell lines | mouse marrow cells |
Preparation Method | Media were prepared as follows: Dulbecco’s modified Eagle’s powder medium 2.7g, NaHCO3 0.74g, penicillin-streptomycin (10,000U-10,000μg/ml) 0.1ml, fetal calf serum 22.4ml, horse serum 6ml, and double-distilled water65.6ml (final volume 94.1ml). Medium thus prepared will be designated DME when serum is omitted and DME-S when serum is included. The final agar-medium mixture was prepared immediately before use as follows: double-strength DME-S 40ml, 3% trypticase soy broth in water 10ml, DEAE-dextran (50mg/mI) 0.15ml, L-asparagine (6.6mg/mI) 0.3ml, and 0.6% agar 50ml. To study CFC survival, mouse marrow cells were suspended in medium (1:1 mixture of double-strength DME-S: water) at a concentration of 1.75×l05 cells/mI. Two-milliliter aliquots were distributed in sterile culture tubes, and these were divided into three sets of six tubes each. One set received 0.05ml of BSS per tube, the second and third set received 0.05ml of CAP (final concentration 40μg/ml) and Thiamphenicol (final concentration 45μg/ml), respectively. The tubes were incubated under the same condition described above for agar plates. At times 0, 8, and 24 hr, two tubes from each set were centrifuged at 700g for 15 min and the cell pellet were washed twice in 1ml BSS. To each cell pellet was added 3.5ml of DME-S-agar mixture, and the suspension was mixed thoroughly and plated in 1mI aliquots in triplicate (100,000 cells per plate). Then colony counting were performed. |
Reaction Conditions | 45μg/ml; 8 or 24h |
Applications | Thiamphenicol reversibly suppresses mouse bone marrow CFC proliferation and markedly reduces colony formation. |
| Animal experiment [2]: | |
Animal models | male ICR mice |
Preparation Method | Forty-eight male ICR mice weighing 18–22g were housed in an environment at 22±2°C with free access to food and water on a 12h light/dark cycle. All mice were randomly divided into 8 groups according to body weight: control group, LPS group, Thiamphenicol treatment group (2.67, 8, 24, 72, 216mg/kg) and Dexamethasone (DEX) treatment group (5mg/kg) for each group of 6 mice. One hour before LPS challenge (3 mg/kg, intratracheal instillation), Thiamphenicol or DEX was administered intraperitoneally. At 12h after ALI modeling, the right lung was separated from the thorax, and the surface mucus and blood were removed with filter paper. Then, the wet weight was determined. Subsequently, the lungs were dried at 60°C for 72h to a constant weight. Finally, the dry weight was measured and the lung wet-to-dry ratio was measured by dividing the wet weight by the dry weight. |
Dosage form | 2.67, 8, 24, 72, 216mg/kg; i.p. |
Applications | Thiamphenicol(216mg/kg) significantly decreased the lung wet-to-dry ratio in LPS-induced ALI mice. |
References: | |
| Cas No. | 15318-45-3 | SDF | |
| 别名 | 甲砜霉素; Thiophenicol; Dextrosulphenidol | ||
| 化学名 | 2,2-dichloro-N-[(1R,2R)-1,3-dihydroxy-1-(4-methylsulfonylphenyl)propan-2-yl]acetamide | ||
| Canonical SMILES | CS(=O)(=O)C1=CC=C(C=C1)C(C(CO)NC(=O)C(Cl)Cl)O | ||
| 分子式 | C12H15Cl2NO5S | 分子量 | 356.22 |
| 溶解度 | ≥ 15.55mg/mL in DMSO | 储存条件 | Store at RT |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8073 mL | 14.0363 mL | 28.0725 mL |
| 5 mM | 0.5615 mL | 2.8073 mL | 5.6145 mL |
| 10 mM | 0.2807 mL | 1.4036 mL | 2.8073 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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