リンコマイシン 化学特性,用途語,生産方法
解説
リンコマイシン
C18H34N2O6S(406.54).Streptomyces lincolnensisの産生する抗生物質.培養液から pH 10でn-ブタノールにより抽出される.不定形の白色粉末.+158°(水).pKa 7.5.水に微溶,アルコール類,酢酸エチル,アセトン,クロロホルムに可溶.塩酸塩のC18H35ClN2O6S・0.5H2O(452.01)はより安定な白色の斜方晶系.融点146~148 ℃.+137°(水).水,アルコール類に可溶,炭化水素以外の有機溶媒に易溶.1水和塩(融点156~158 ℃,+143°(水))も知られている.1963年にアメリカで放線菌の一種 Streptomyces lincolnensisの培養ろ液から発見されたマクロライド系抗生物質。グラム陽性菌 (ブドウ球菌,レンサ球菌,肺炎球菌,髄膜炎菌など) ならびに一部の陰性菌に有効。抗菌スペクトルはマクロライド抗生物質に近似しており,グラム陽性菌,グラム陰性球菌,とくに根粒菌Bacteroidesなどの嫌気性菌に有効である.作用機作はタンパク質合成阻害で,細菌リボソームの50 Sサブユニットに結合して,ペプチド転移反応を阻害する.副作用として肝障害がある.LD50 4000 mg/kg(ラット,経口).1000 mg/kg(マウス,腹腔).
効能
抗生物質, タンパク質合成阻害薬
説明
Lincomycin is an antibiotic active against grampositive
bacteria. Occupational exposure occurs in
poultry and pig breeders.
化学的特性
White Crystalline Solid
使用
Lincomycin is a polar, water soluble, broad spectrum antibiotic first isolated from Streptomyces licolnensis by researchers at Upjohn in 1962. Lincomycin was the first of a unique structural class, the lincosamides, containing a rare amino acid, 4-propyl-N-methylproline, coupled to an equally rare aminomethylthio-octopyranoside sugar. Lincomycin and semi-synthetic analogues are often incorrectly considered to be aminoglycosides but share little or no structural similarity. Lincomycin is a broad spectrum antibiotic with activity against anaerobic bacteria and protozoans. Lincomycin acts by binding to the 23S ribosomal subunit, blocking protein synthesis. Lincomycin has been extensively studied with over 7,000 literature citations.
定義
ChEBI: A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis.
抗菌性
Lincomycin has an antibacterial effect with respect to Gram-positive microorganisms
(staphylococci, streptococci, pneumococci, diphtheria bacillus, and clostridia). It is used
for serious bacterial infections: sepsis, osteomyelitis, septic endocarditis, pneumonia, pulmonary abscess, infected wounds, and purulent meningitis. Lincomycin is a reserve drug
for infections caused by strains of staphylococci and other Gram-positive microorganisms
that are resistant to penicillin and other antibiotics. Synonyms of this drug are lincocin,
mycivin, albiotic, and others.
一般的な説明
Lincomycin was found in the culture broth of Streptomyces lincolnensis var. lincolnensis by the Upjohn Co. in 1962. It shows antibacterial activity similar to that of the macrolide antibiotics and also shows excellent activity against anaerobic bacteria. Lincomycin is used clinically in combination with other classes of antibiotics for postoperative, gynecological, urinary tract, ear and nose, and other infections.
接触アレルゲン
Lincomycin is an antibiotic of the lincosanide group,active against Gram-positive bacteria. Occupational
exposure occurs in poultry and pig breeders
臨床応用
Lincomycin is a natural product isolated from fermentations of Streptomyces lincolnensisvar. lincolnensis. It
is active against Gram-positive organisms, including some anaerobes. It is indicated for the treatment of
serious infections caused by sensitive strains of streptococci, pneumococci, and staphylococci. It generally
is reserved for patients who are allergic to penicillin because of the increased risk of pseudomembranous
colitis. It also serves as the starting material for the synthesis of clindamycin (by a SN-2
reaction that inverts the R stereochemistry of the C-7 hydroxyl to a C-7 S-chloride).
リンコマイシン 上流と下流の製品情報
原材料
準備製品