期刊
MARINE DRUGS
卷 17, 期 4, 页码 -出版社
MDPI
DOI: 10.3390/md17040229
关键词
zebrafish Nile red fat metabolism assay; anti-obesity drugs; chlorophyll derivatives; murine pre-adipocytes; PPAR
资金
- European ERA-NET Marine Biotechnology project CYANOBESITY [ERA-MBT/0001/2015]
- national funds through FCT (Foundation for Science and Technology, Portugal)
- project INNOVMAR-Innovation and Sustainability in the Management and Exploitation of Marine Resources [NORTE-01-0145-FEDER-000035]
- North Portugal Regional Operational Program
- European Regional Development Fund (ERDF)
- FCT strategic fund [UID/Multi/04423/2019, SFRH/BPD/112287/2015, IF/01358/2014, SFRH/BD/108314/2015, SFRH/BD/116009/2016]
- Fundação para a Ciência e a Tecnologia [ERA-MBT/0001/2015] Funding Source: FCT
Marine organisms, particularly cyanobacteria, are important resources for the production of bioactive secondary metabolites for the treatment of human diseases. In this study, a bioassay-guided approach was used to discover metabolites with lipid-reducing activity. Two chlorophyll derivatives were successfully isolated, the previously described 13(2)-hydroxy-pheophytin a (1) and the new compound 13(2)-hydroxy-pheofarnesin a (2). The structure elucidation of the new compound 2 was established based on one- and two-dimensional (1D and 2D) NMR spectroscopy and mass spectrometry. Compounds 1 and 2 showed significant neutral lipid-reducing activity in the zebrafish Nile red fat metabolism assay after 48 h of exposure with a half maximal effective concentration (EC50) of 8.9 +/- 0.4 mu M for 1 and 15.5 +/- 1.3 mu M for 2. Both compounds additionally reduced neutral lipid accumulation in 3T3-L1 multicellular spheroids of murine preadipocytes. Molecular profiling of mRNA expression of some target genes was evaluated for the higher potent compound 1, which indicated altered peroxisome proliferator activated receptor gamma (PPAR) mRNA expression. Lipolysis was not affected. Different food materials (Spirulina, Chlorella, spinach, and cabbage) were evaluated for the presence of 1, and the cyanobacterium Spirulina, with GRAS (generally regarded as safe) status for human consumption, contained high amounts of 1. In summary, known and novel chlorophyll derivatives were discovered from marine cyanobacteria with relevant lipid-reducing activities, which in the future may be developed into nutraceuticals.
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