Large-Scale Production of Bioactive Terrein by Aspergillus terreus Strain S020 Isolated from the Saudi Coast of the Red Sea

Abstract

The diversity of symbiotic fungi derived from two marine sponges and sediment collected off Obhur, Jeddah (Saudi Arabia), was investigated in the current study. A total of 23 isolates were purified using a culture-dependent approach. Using the morphological properties combined with internal transcribed spacer-rDNA (ITS-rDNA) sequences, 23 fungal strains (in the majority Penicillium and Aspergillus) were identified from these samples. The biological screening (cytotoxic and antimicrobial activities) of small-scale cultures of these fungi yielded several target fungal strains which produced bioactive secondary metabolites. Amongst these isolates, the crude extract of Aspergillus terreus strain S020, which was cultured in fermentation static broth, 21 L, for 40 days at room temperature on potato dextrose broth, displayed strong antimicrobial activities against Pseudomonas aeruginosa and Staphylococcus aureus and significant antiproliferative effects on human carcinoma cells. Chromatographic separation of the crude extract by silica gel column chromatography indicated that the S020 isolate could produce a series of chemical compounds. Among these, pure crystalline terrein was separated with a high yield of 537.26 ± 23.42 g/kg extract, which represents the highest fermentation production of terrein to date. Its chemical structure was elucidated on the basis of high-resolution electrospray ionization mass spectrometry (HRESIMS) or high-resolution mass spectrometry (HRMS), 1D, and 2D NMR spectroscopic analyses and by comparison with reported data. The compound showed strong cytotoxic activity against colorectal carcinoma cells (HCT-116) and hepatocellular carcinoma cells (HepG2), with IC50 values of 12.13 and 22.53 µM, respectively. Our study highlights the potential of A. terreus strain S020 for the industrial production of bioactive terrein on a large scale and the importance of future investigations of these strains to identify the bioactive leads in these fungal extracts.

Efficient Production of the Potent Antimicrobial Metabolite “Terrein” From the Fungus Aspergillus terreus

“…Recently, co-culture techniques of endophytic fungi A. terreus EN-539 and Paecilomyces lilacinus EN-531 induced the production of the new derivative asperterrein and a known dihydroterrein having a multibacterial inhibitory effect. 28 In the present study, we describe the improved strategy for the production of pure terrein in a more economical way which leads to higher accessibility to consumers. We discuss the improved production of pure terrein (crystallized form) directly from the modified SDB.…”

Antibiotics from Extremophilic Micromycetes

“…The study of some isolates of marine micromycetes allowed to identify a producer of the well-known antibiotic terrein (248) [131,225], with high productivity [226]. The selection of strains was based on the screening of the antimicrobial and cytotoxic activities of isolates.…”

LAMA-1: A Cerebroside Isolated from the Deep-Sea-Derived Fungus Penicillium chrysogenum

“…The fungus Penicillium chrysogenum strain S003 ( Figure 3) was cultured from deep-sea sediment from the Red Sea, and the fungal strain was identified based on a previously described method [26]. 16.95, 13.6; and 2.89, 3.07 µM, respectively, while they were inactive against HeLa cells.…”

“…In the course of our ongoing efforts to isolate and identify drug leads from marine metabolites [22][23][24][25][26][27], we have investigated the extract of the Red Sea deep-sediment isolated fungus Penicillium chrysogenum strain S003.…”