Synergistic antifungal indolecarbazoles from Streptomyces sp. CNS-42 associated with traditional Chinese medicine Alisma orientale

The Journal of Antibiotics
2017.0

Abstract

Multi-drug resistance of pathogenic microorganisms is a serious threat to human health, especially Candida albicans, the most common opportunistic clinical fungal pathogen causing systemic infections with high mortality. Widespread and repeated use of azoles has led to rapid antifungal drug resistance, highlighting the need for new therapeutic strategies such as synergistic drugs. A high-throughput synergy screening (HTSS) method was developed to identify microbial natural products that synergize with low-dose ketoconazole (KTC) against fungal pathogens. Screening of a microbial natural product library from endophytic bacteria associated with traditional Chinese medicine Alisma orientale led to the identification of an extract from endophytic actinomycete Streptomyces sp. CNS-42 with synergistic antifungal activity. Bioassay-directed fractionation of a large-scale (42 L) culture of CNS-42 yielded four known indolecarbazoles (1–4). Compounds 1 (N-formyl-staurosporine) and 2 (N-acetyl-staurosporine) showed potent synergistic antifungal activities with MIC values of 6.25 and 0.78 μg ml⁻¹, respectively, when combined with 25% of the MIC of KTC against C. albicans, but weak or no antifungal activity (MIC ≥ 100 μg ml⁻¹) when tested singly. This study reports the new synergistic antifungal activity of indolecarbazoles, providing a basis for their further pharmaceutical application.

Knowledge Graph

Similar Paper

Synergistic antifungal indolecarbazoles from Streptomyces sp. CNS-42 associated with traditional Chinese medicine Alisma orientale
The Journal of Antibiotics 2017.0
Synergistic antifungal indolecarbazoles from Streptomyces sp. CNS-42 associated with traditional Chinese medicine Alisma orientale
The Journal of Antibiotics 2017.0
High-throughput synergy screening identifies microbial metabolites as combination agents for the treatment of fungal infections
Proceedings of the National Academy of Sciences 2007.0
Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
Marine Drugs 2019.0
Antiamoebic Activities of Indolocarbazole Metabolites Isolated from Streptomyces sanyensis Cultures
Marine Drugs 2019.0
Design of new antifungal agents: synthesis and evaluation of 1-[(1H-indol-5-ylmethyl)amino]-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols
Bioorganic & Medicinal Chemistry Letters 2009.0
Expanding the Chemical Repertoire of the Endophyte <i>Streptomyces albospinus</i> RLe7 Reveals Amphotericin B as an Inducer of a Fungal Phenotype
Journal of Natural Products 2017.0
Expanding the Chemical Repertoire of the Endophyte <i>Streptomyces albospinus</i> RLe7 Reveals Amphotericin B as an Inducer of a Fungal Phenotype
Journal of Natural Products 2017.0
An efficient synthesis and antifungal evaluation of natural product streptochlorin and its analogues
Fitoterapia 2018.0
Synthesis and biological evaluations of a series of calycanthaceous analogues as antifungal agents
Natural Product Research 2021.0