Mechanism of action of(AMB This kind of antifungal agents act against sensitive fungal by combining with membrane ergosterols with subsequent aeration in permeability and loss of essential organic and inorganic cell constituents In mammalian cell membranes, the principal sterol is chloesterol(Ha 甾醇), AMB binds approximately times more tightly to vesicles(醇囊) containing ergosterol rather than to those containing chloesterol Side-effects The most serious are hypokalemia and distal tubular acidosis. the Nephrotoxicity has been lessened to some extent by lipid complexed formulations
Mechanism of Action of (AMB) This kind of antifungal agents act against sensitive fungal by combining with membrane ergosterols with subsequent aleration in permeability and loss of essential organic and inorganic cell constituents. In mammalian cell membranes, the principal sterol is chloesterol(胆 甾醇), AMB binds approximately times more tightly to vesicles (醇囊) containing ergoesterol rather than to those containing chloesterol. Side-effects The most serious are hypokalemia and distal tubular acidosis. the Nephrotoxicity has been lessened to some extent by lipidcomplexed formulations
Some lipid-complexed formulation of aMB in market and R&D (1)两性霉素B脂质体剂型( AmBisome是用脂质体将两性霉 素B包裹而成已在欧洲和美国上市多年 (2两性霉素B脂质体复合物(ABLC)商品名Abee是脂质体 与两性霉素B交织而成近来已在美国上市 3)两性霉素B胶体分散剂(ABCD.商品名 Amphocil和 Δ mphotec是用等量的硫酸胆固醇与等量的两性霉素混合包 裹现正在欧洲和美国使用 (4)聚乙二醇AMB,AMB/ polethelne glyco- phospholipid脂质, 临床前研究
Some lipid-complexed formulation of AMB in market and R&D (1)两性霉素B脂质体剂型(AmBisome),是用脂质体将两性霉 素 B包裹而成.已在欧洲和美国上市多年. (2)两性霉素B脂质体复合物(ABLC),商品名Abelcet是脂质体 与两性霉素B交织而成,近来已在美国上市. (3)两性霉素B胶体分散剂(ABCD),商品名Amphocil和 Amphotec,是用等量的硫酸胆固醇与等量的两性霉素混合包 裹,现正在欧洲和美国使用. (4)聚乙二醇—AMB, AMB/polethelne glyco-phospholipid脂质, 临床前研究
522 Nystain(NYS)(制霉菌素) OH O OHOH OH OH OH HOOC H' CH3 NH OH OH Deriving from AMB, developed by aronex and in preclinic phase NYS is recommended for treatment of oral thrush or esophagitis caused by Candida albicans in AIDS
5.2.2 Nystain (NYS)(制霉菌素) O O O OH H HOOC OH OH OH OH OH OH OH O O CH3 OH NH2 OH Deriving from AMB,developed by Aronex and in preclinic phase. NYS is recommended for treatment of oral thrush or esophagitis caused by Candida albicans in AIDS
52.3 Griseofulvin(灰黄霉素) OCH3 O OCH3 ≥O CH3O O CH3 Griseofulvin as marked in 1958, the primary site of action of it involves Binding to RNA. Manifestations include inhibition of hyphal cell-wall synthesis and cytoplasmic microtubules. Mainly used to treat the skin fungal infections. The side effects are gastrointestinal, allergic, and more frequently, moderate increase in fecal protoporphyrin
5.2.3 Griseofulvin(灰黄霉素) OCH3 CH3O Cl O O O OCH3 CH3 Griseofulvin as marked in 1958, the primary site of action of it involves Binding to RNA. Manifestations include inhibition of hyphal cell-wall synthesis and cytoplasmic microtubules. Mainly used to treat the skin fungal infections. The side effects are: gastrointestinal, allergic,and more frequently, moderate increase in fecal protoporphyrin
5.2, 4 Others 脂肽类抗生素 Echinocandin OH HO CH3 CH3 NH O(CH2)4CH3 OH HO OH OH 真菌细胞壁具有许多杀真局菌活性的靶位参与真菌细胞壁 的合成的许多合成酶是真菌特有的如1,3-葡聚糖合成酶聚 乙酰氨基葡糖合成酶等
5.2.4 Others OH OH NH NH O HO O CH3 HO O N CH3 HO NH O N OH O OH OH NH O NH CH3 CH3 O O(CH2 )4CH3 脂肽类抗生素 Echinocandin 真菌细胞壁具有许多杀真局菌活性的靶位.参与真菌细胞壁 的合成的许多合成酶是真菌特有的,如1,3-葡聚糖合成酶;聚 乙酰氨基葡糖合成酶等