Echinocandin B is the key antifungal antibiotic, which is mainly derived from the secondary metabolites of Aspergillus nidulans [1]. Due to the structure of the linoleoyl side chain, Echinocandin B shows a strong hemolytic activity[2]. Echinocandin B is a non-competitive inhibitor of β-1, 3-Glucan synthetase, which restricts the synthesis of Glucan, a key component of the cell wall[3]. Echinocandin B has been widely used as a lead compound to synthesize a series of derivatives to inhibit Candida activity[4].
In vitro, Echinocandin B treatment for 2 days inhibited a variety of Candida species activity, with IC50 values of 0.24μg/ml for Candida albicans FP578, 0.16μg/ml for Candida albicans FP582, and 0.12μg/ml for Candida albicans FP633, respectively [5].
In vivo, Echinocandin B treatment via subcutaneous injection at a dose of 10mg/kg/day for 3 days showed a potent anti-Candida activity in ICR mice infected with C. albicans FP633[5].
References:
[1] Wiederhold N P, Lewis R E. The echinocandin antifungals: an overview of the pharmacology, spectrum and clinical efficacy[J]. Expert opinion on investigational drugs, 2003, 12(8): 1313-1333.
[2] Niu K, Qi Y X, Cai H W, et al. Investigation of the enhancement for Echinocandin B fermentation with methyl oleate from transcription level[J]. Bioprocess and Biosystems Engineering, 2023, 46(7): 1045-1052.
[3] Kumari V, Kumar V, Kaushal M, et al. Curcumin epigenetically represses histone acetylation of echinocandin B producing Emericella rugulosa[J]. Physiologia, 2023, 3(2): 221-232.
[4] Cacho R A, Jiang W, Chooi Y H, et al. Identification and characterization of the echinocandin B biosynthetic gene cluster from Emericella rugulosa NRRL 11440[J]. Journal of the American Chemical Society, 2012, 134(40): 16781-16790.
[5] Iwamoto T, Fujie A, Sakamoto K, et al. WF11899A, B and C, novel antifungal lipopeptides I. Taxonomy, fermentation, isolation and physico-chemical properties[J]. The Journal of antibiotics, 1994, 47(10): 1084-1091.
Echinocandin B是一种关键抗真菌抗生素，主要来源于Aspergillus nidulans的次级代谢产物[1]。由于亚油酰侧链的结构，Echinocandin B表现出较强的溶血活性[2]。作为β-1,3-葡聚糖合成酶的非竞争性抑制剂，Echinocandin B可通过限制细胞壁关键组分葡聚糖的合成发挥抗真菌作用[3]。Echinocandin B并已被广泛作为先导化合物用于合成一系列抑制念珠菌活性的衍生物[4]。
在体外，Echinocandin B处理2天可抑制多种念珠菌活性，对白色念珠菌FP578、FP582和FP633的IC50值分别为0.24μg/ml、0.16μg/ml和0.12μg/ml[5]。
在体内，感染白色念珠菌FP633的ICR小鼠每日皮下注射Echinocandin B（10mg/kg/day；持续3天）显示出强效抗念珠菌活性[5]。