Abstract

Strain 12A35 was isolated from a deep-sea sediment collected from the South China Sea and showed promising antibacterial activities. It was identified as Streptomyces sp. by the 16S rDNA sequence analysis. Bioassay-guided fractionation using HP20 adsorption, flash chromatography over silica gel and octadecylsilyl (ODS) and semi-preparative HPLC, led to the isolation and purification of five metabolites from the fermentation culture of 12A35. Two new spirotetronate antibiotics, lobophorins H (1) and I (2), along with three known analogues, O-β-kijanosyl-(1→17)-kijanolide (3), lobophorins B (4) and F (5) were characterized by 1D, 2D-NMR and MS data. These compounds exhibited significant inhibitory activities against Bacillus subtilis. Compounds 1 and 5 exhibited moderate activities against Staphylococcus aureus. In particular, the new compound lobophorin H (1) showed similar antibacterial activities against B. subtilis CMCC63501 to ampicillin.

Highlights

  • Infectious disease is one of the most deadly diseases threatening public health

  • Natural products from marine-derived microorganisms have been an important source of novel lead structures for drug discovery

  • Marinisporolides A and B were polyene macrolides isolated from the culture of an actinomycete from a new genus Marinispora

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Summary

Introduction

Infectious disease is one of the most deadly diseases threatening public health. drug-resistant bacteria are steadily rising, increasing the difficulty of treatment. Natural products from marine-derived microorganisms have been an important source of novel lead structures for drug discovery. Marine actinomycetes are one of the most efficient groups of secondary metabolite producers. Many intriguing compounds with potent and various bioactivities have been found from marine microbes for lead compounds [1]. Marinisporolides A and B were polyene macrolides isolated from the culture of an actinomycete from a new genus Marinispora. During our continuous screening for new antibiotics, the organic extract of the fermentation broth of a deep-sea-derived actinobacterial strain 12A35 showed potent antibacterial activities. Five spirotetronate antibiotics were isolated from an actinomycete 12A35 as a member of the genus. The new compound lobophorin H (1) showed similar antibacterial activities against Bacillus subtilis to ampicillin as a positive control drug

Taxonomy of the Strain 12A35
Structure Determination
Antimicrobial Activity of Compounds 1–5
General Experimental Procedures
Microorganisms and Fermentation Conditions
Bioactivity-Guided Isolation and Purification
Conclusions
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