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Background: Marine actinomycetes are among indispensable sources of natural bioactive compounds with unique antimicrobial and anti-cancer activities., Objective: Herein, it was aimed to elucidate the bioactive potential of a marine-derived Streptomyces ovatisporus S4702T, isolated previously., Methods: Streptomyces ovatisporus S4702 T was cultured in N-Z Amine broth, and extraction was carried out using different organic solvents. Bioassay-guided purification was followed by chemical characterization using NMR and LC-MS/MS. The compound was then evaluated for its antibacterial, antioxidant and cytotoxic activities., Results: Etyl acetate extracts gave the highest antibacterial activity, and chemical characterization of this extract indicated the formula as C15H29O5N3 and the corresponding possible molecular structure as 4H-chromen-4-one derivative. It was found highly potent against Bacillus subtilis ATCC 6633 (MIC: 0.25 μg ml -1 ) and Micrococcus luteus ATCC 9341 (MBC: 0.5 μg ml -1 ). It has no remarkable antioxidant activity, but a higher EC50 value and less cytotoxicity against normal cells. The EC50 values of this chromen derivative were found as 9.68 μg ml-1 for human colon carcinoma, 9.93 μg ml -1 for human prostate adenocarcinoma and 25.5 μg ml -1 for human embryonic kidney cells., Conclusion: Overall, the presented 4H-chromen-4-one derivative is a remarkable bioactive compound with potent antibacterial and cytotoxic activity. With its high bioactive potential, it is proposed as a good candidate in medicine., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Indole-based heterocyclic compounds play important roles in pharmaceutical chemistry due to their unexpected biological and pharmacological properties., Objective: Herein, we describe novel biological properties (antioxidant, antimicrobial and anti-cancer) of 3- bromo-1-ethyl-1H-indole (BEI) structure., Methods: BEI was synthesized from 1-Methyl-2-phenylindole and N-bromosuccinimide and was characterized by using 1H and 13C NMR. Cytotoxicity was determined by MTT assay. Apoptosis analysis of BEI was determined by Arthur™ image-based Cytometer. Different methods were applied to assess the antioxidant activity of BEI. Molecular docking studies were conducted to determine the interactions of bonding between GST isozymes and BEI., Results: According to the antioxidant and antimicrobial activity assays, BEI compound showed reduced total antioxidant activity compared to the Trolox standard, whereas it showed moderate antimicrobial activity against Aspergillus niger and Phytophora eryhtrospora. Notably, the BEI compound demonstrated substantial selective cytotoxicity for the first time towards cancer cell lines, and there existed a significant decrease in the percentage of live cells treated with BEI, in comparison to the control ones. Interestingly, BEI exhibited a promising glutathione S-transferase isozymes inhibition., Conclusion: The results of this study suggest that BEI seems to be a promising molecule to be used in the design of new anti-cancer agents that provide superiority to present commercial anti-cancer drugs., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Anthocephalus cadamba is used in traditional and folklore medicinal system., Objectives: In order to validate its traditional medicinal claim, the present study was designed to assess antioxidant, antigenotoxic and cytotoxic activity of fractions from Anthocephalus cadamba bark and to identify their active phytoconstituents., Methods: The four fractions viz. hexane (HACB), chloroform (CACB), ethylacetate (EACB) and nbutanol (NACB) were fractionated from the crude methanol extract from bark of A. cadamba. All fractions were evaluated for antiradical efficacy using various in vitro antioxidant assays and for antigenotoxicity by SOS chromotest using E. coli PQ37 tester strain. Cytotoxic potential was checked using MTT assay., Results: Among the four fractions, EACB and NACB exhibited promising radical quenching potential in DPPH, ABTS, superoxide anion radical scavenging and pBR322 plasmid DNA nicking assays. All the fractions were evaluated for genotoxic and antigenotoxic activity in SOS chromotest using E. coli PQ37 tester strain. Results revealed that fractions were non-genotoxic and have potential to suppress the genotoxicity induced by 4NQO (4-nitroquinoline-1-oxide) and AFB1 (aflatoxin B1). NACB was found to inhibit the growth of colon (COLO 205) cancer cells with GI50 of 54.36 µg/ml. To identify bioactive principles in the active fractions, NACB and EACB were subjected to UPLC-electrospray-ionization-quadrupole time-of-flight mass spectrometry which revealed the presence of 3β-isodihyrocadambine-oxide, cadambine, phelasin A/B, 3β- dihydrocadambine and 3'-O-caffeoylsweroside like compounds., Conclusions: Overall results revealed that A. cadamba is a rich source of antioxidant, antigenotoxic and cytotoxic constituents which may find their significance in various food and pharmaceutical products., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)

Background: Natural products and their derivatives are widely used to treat cancer and other diseases associated with ROS- and RNS-induced damages., Methods: A series of paramagnetic modified curcumin analogs and 3,5-diarylidene-piperidones (DAP) have been designed, synthesized, and characterized on their anti-proliferative and antioxidant activity., Results: Biological characterization of the new compounds supported the earlier results that incorporation of a nitroxide moiety or its precursor into curcumin or diarylidenylpiperidone (DAP) scaffolds resulted in anti-proliferative effect toward cancerous cell-lines in case of aryl hydroxy and/or methoxy substituent containing derivatives, suggesting their potential for targeted therapeutic applications. In case of basic side chain derivatives, nitroxide incorporation gave unambiguous results, however in tendency the more accessible DAP derivatives had stronger anti-proliferative effect. In most cases, the nitroxide incorporation increased the TEAC value (proton and electron donation capability) of DAP derivatives., Conclusions: Among the compounds synthesized and investigated the spin-labeled curcumin and 3,5-bis(4-hydroxy-3-methoxybenzylidene)piperidin-4-one derivatives were the most effective antiproliferative and antioxidant derivatives., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)

The present study evaluated the levels of total phenolics, flavonoids, tannins and anthocyanins from Peganum harmala L. seeds and determined their antioxidant, antiplasmodial and anticancer potentials. Antioxidant activity was determined by DPPH and ABTS assays. Extracts of P. harmala seeds from Oudref and Djerba (two places in Tunisia) were obtained by successive extraction solvents: petroleum ether, chloroform, ethyl acetate, ethanol and water. Their composition was evaluated for phenolics (gallic acid equivalent 2.48 to 72.52 g/kg), tannins (catechin equivalent 0 to 25.27 g/kg), anthocyanins (cyanidin equivalent 0 to 20.56 mg/kg) and flavonoids (quercetin equivalent 0 to 3.12 g/kg). Ethanolic extract exerted the highest activities against a chloroquine-resistant strain of Plasmodium falciparum (IC₅₀=23 mg/L), against human breast cancer cells MCF7 (IC₅₀=32 mg/L) and against free radical (IC₅₀=19.09±3.07 mg/L). Correlations were studied between each chemical family and the three activities. Total phenolics content exhibited the highest correlation with antiplasmodial activity (R²=0.92) and with anticancer activity (R²=0.86), respectively.