Pulchranin A: First report of isolation from an endophytic fungus and its inhibitory activity on cyclin dependent kinases. Issue 19 (1st October 2020)

• Record Type: Journal Article
• Authors: Moussa, Ashaimaa Y.; Mostafa, Nada M.; Singab, Abdel Nasser B.
• Is Part Of: Natural product research. Volume 34:Issue 19(2020)
• Page Start: 2715
• Page End: 2722
• Publication Date: 2020-10-01
• Subjects: Aspergillus -- cytotoxic effect -- Tabebuia -- molecular docking -- cyclin-dependent kinase inhibitor; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2019.1585846
• Languages: English
• ISSNs: 1478-6419

Abstract

Abstract: Fungal factories emerge as a promising source for the production of bioactive natural products. This study reports the isolation and structure elucidation of pulchranin A, for the first time, from an endophytic fungus ( Aspergillus TRL1 ), which was cultured from Tabebuia rosea (Bignoniaceae) stems and identified by DNA ITS sequencing. Pulchranin A showed promising in-vitro cytotoxic effects against breast (MCF-7), liver (Hep-G2) and colorectal (HCT) cell lines, with IC50 values of 63, 80 and 91 µg/mL, respectively. In addition, it inhibited three cyclin-dependent kinases (CDK1, CDK2 and CDK4) in MCF-7 cells with IC50 values of 9.82, 15.6 and 2.7 µg/mL, respectively. Results were further supported by in-silico molecular docking of pulchranin A to CDK1, CDK2, and CDK4 crystal structures, where it demonstrated good interactions by H-bonding, hydrophobic and Pi-Pi interactions with different amino acid residues of these enzymes. Pulchranin A might be a potential CDK inhibitor in human breast cancer cells.