BIOACTIVE METABOLITE FROM MARINE SPONGEDERIVED FUNGUS Cochliobolus geniculatus WR12

Abstract

This study aims to find bioactive metabolites from fungus, which was isolated from marine sponge Haliclona fascigera. The fungus was identified molecularly as C. geniculatus WR12. The isolation of the bioactive compound was achieved by column chromatography with step gradient polarity (SGP) method and purification by recrystallization. The structure was determined based on spectroscopic analyses (UV, IR, HR-MS, 1 H and 13 C NMR). The antibacterial activity of the compound was tested against Methicillin-Resistant Staphylococcus Aureus (MRSA) by using the agar diffusion method. The Cytotoxicity of the compound was tested on the cancer cell lines by using the microculture tetrazolium (MTT) assay. The results of this study were obtained a pure compound (1). The compound was identified as radicinin based on 1D and 2D NMR and HRESIMS data. This compound showed cytotoxic activity with IC 50 values of 60.68, 30.89, and 87.89 µg/mL against WiDr, T47D, and Hela cell lines, respectively, but not toxic against Vero cell (IC 50 value of 607.31 µg/mL). Radicinin showed higher cytotoxic activity against T47D cells (IC 50 = 25.01 ppm) compared with doxorubicin (IC 50 = 33.49 ppm). The result of the antibacterial activity of radicinin showed the minimum inhibitory concentration (MIC) of 125 µg/disc against MRSA. Based on these results, it can be concluded that radicinin could be considered as a potential candidate for future anticancer and anti-MRSA drug.

In Vitro Effects of Fungal Phytotoxins on Cancer Cell Viability: First Insight into Structure Activity Relationship of a Potent Metabolite of Cochliobolus australiensis Radicinin

“…These may be optimized through formulation, allowing highly toxic compounds be approved for marketing, as is, for example maytansin, that is now used in the clinic thanks to its conjugation to trastuzumab. It is worthy of note that radicinin was shown to have less pronounced effects on the viability of a non-cancerous cell line [37]. Nevertheless, no clear conclusion on benefits in tumor bearing mice could be reached after analyzing the experiments conducted by the National Cancer Institute.…”

Antimicrobial Natural Products from Plant Pathogenic Fungi

“…Secondary metabolites from the fungal plant pathogens Alternaria radicina , Cercospora beticola , D. macrodidyma , D. torresensis , I. europaea , and I. liriodendra have been reported to exhibit a variety of bioactivities including antimicrobial, anti-proliferative, antimalarial, and phytotoxic activities and as inhibitors of acetylcholinesterase [ 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 ].…”

Cochliobolus, Drechslera, Bipolaris, Curvularia different nomenclature for one potent fungus

“…Cochliobolus metabolites showed also promising anticancer activities. Radicinin isolated from Cochliobolus geniculatus WR12 exhibited high cytotoxic activity against T47D cells recording IC50 of 25.01 ppm [41]. The same compound showed also anti-MRSA activity with minimum inhibitory concentration (MIC) of 125 µg/disc against tested MRSA [42].…”