Structural Characterization, Antimicrobial, Antibiofilm, Antioxidant, Anticancer and Acute Toxicity Properties of N-(2-hydroxyphenyl)-2-phenazinamine From Nocardiopsis exhalans (KP149558)

Abstract

The present study aimed to isolate and identify potential drugs from marine actinomycete Nocardiopsis exhalans and screen them for biomedical applications. The cell-free culture of N. exhalans was extracted with ethyl acetate and the solvent extract showed six fractions in thin-layer chromatography. The fractions were subjected to column chromatography for purification and evaluated for activity against human clinical pathogens. Fraction 4 showed significant activity and was identified as N-(2-hydroxyphenyl)-2-phenazinamine (NHP) using spectral analyses. Further, NHP showed excellent biofilm inhibitory activity against human clinical pathogens Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. The in vitro antioxidant activity confirmed that NHP is scavenging the oxidative stress-enhancing molecules. The anti-proliferative activity of NHP against human breast cancer cells showed significant activity at 300 µg/ml and less cytotoxic activity against normal cells. Additionally, the toxicity assessment against zebrafish revealed that NHP does not cause any toxicity in the important organs. The results highlight N. exhalans as a promising candidate for the development of antibiotics with potential therapeutic applications.

Resistomycin Suppresses Prostate Cancer Cell Growth by Instigating Oxidative Stress, Mitochondrial Apoptosis, and Cell Cycle Arrest

“…In another study, marine actinomycete Nocardiopsis exhalan-derived metabolite significantly repressed the proliferation of MCF-7 cancer cells in a concentration-dependent manner related to doxorubicin (standard anticancer agent). This was achieved through an imbalance of ROS and by causing oxidative-stress-mediated apoptosis [44]. Therefore, we speculated that resistomycin-induced ROS underlies the cytotoxic effect and cell death of PC3 cells.…”

“…One-electron reductions are the most common under aerobic conditions, and they produce free radical intermediates [46]. The detoxifying enzyme cytochrome P450 reductase and other flavoprotein enzymes are primarily responsible for carrying them out [44]. An alternate mechanism for the activation involves two-electron reductions, which are then followed by inactivation by glucuronidation, sulfation, or transformation into an alkylating intermediate.…”

Recent advances in therapeutic targets identification and development of treatment strategies towards Pseudomonas aeruginosa infections

“…Excellent biofilm inhibitory activity [77] the peptidase inhibitor sitagliptin, as permeators efficiently crossing the epithelial barrier and permeabilizing bacterial membranes [78].…”