Metallodrugs form a large family of therapeutic agents against cancer, among which is cisplatin, a paradigmatic member. Therapeutic resistance and undesired side effects to Pt(II) related drugs, prompts research on different metal–ligand combinations with potentially enhanced biological activity. We present the synthesis and biological tests of novel palladium(II) complexes containing bisdemethoxycurcumin (BDMC) 1 and 2. Complexes were fully characterized and their structures were determined by X-ray diffraction. Their biological activity was assessed for several selected human tumor cell lines: Jurkat (human leukaemic T-cell lymphoma), HCT-116 (human colorectal carcinoma), HeLa (human cervix epitheloid carcinoma), MCF-7 (human breast adenocarcinoma), MDA-MB-231 (human mammary gland adenocarcinoma), A549 (human alveolar adenocarcinoma), Caco-2 (human colorectal carcinoma), and for non-cancerous 3T3 cells (murine fibroblasts). The cytotoxicity of 1 is comparable to that of cisplatin, and superior to that of 2 in all cell lines. It is a correlation between IC₅₀ values of 1 and 2 in the eight studied cell types, promising a potential use as anti-proliferative drugs. Moreover, for Jurkat cell line, complexes 1 and 2, show an enhanced activity. DFT and docking calculations on the NF-κB protein, Human Serum Albumin (HSA), and DNA were performed for 1 and 2 to correlate with their biological activities.

So far, the polyphenolic components of turmeric have shown a significant pharmacological preventative activity for a wide spectrum of diseases, including oncological disorders. This type of natural product could be of great interest for the inhibition of cancer cell proliferation, displaying less side effects in comparison to classical chemotherapeutics. The poor bioavailability and quick metabolism of such natural compounds require new investigative methods to improve their stability in the organisms. A synthetic approach to increase the efficiency of curcuminoids is to coordinate them to metals through the beta-dicarbonyl moiety. We report the synthesis and the biological attempts on human ovarian carcinoma A2780 of ruthenium(II) complexes 1–4, containing curcuminoid ligands. The cytotoxicity of complexes 1–4 proves their antiproliferative capability, and a correlation between the IC₅₀ values and NF-κB transcription factor, FGF-2, and MMP-9 levels was figured out through the principal component analysis (PCA).

Bacterial resistance to antibiotics in use represents a critical threat to public health. The treatment of nosocomial, often life-threatening infections is often challenging and requires the search for new antibacterial compounds. In this study a series of phosphonium salts derived from bis(bibenzyl) isoperrottetin A were studied. Bis(bibenzyls) are compounds unique for liverworts. Phosphonium salts were prepared by an eight-step synthesis. The key steps in its preparation were the Ullmann reaction and the Wittig reaction. Ten phosphonium salts were prepared. Isoperrottetin A and its phosphonium salts were tested for antibacterial activity. Some of the compounds exhibit significant biological activity. Most of the prepared derivatives are more potent than the original isoperrottetin A. Compounds were evaluated for the antibacterial activity against selected Gram-positive bacteria such as Staphylococcus aureus, methicillin sensitive and resistant, Enterococcus faecalis and vancomycin sensitive and resistant and Gram-negative bacteria such as Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae. Mycobacterium smegmatis and Mycobacterium marinum belonging to the genus Mycobacterium were also tested. Besides antibacterial activity, the compounds inhibit cell breathing and show cytotoxic activity against melanoma cells, retinal and epithelial cells. The results of antibacterial tests showed that the most effective compound is 5,5',5'',5'''-[1,7(1),4,5(1,3)-tetrabenzenaoctaphane-1³,4⁴,5⁶,8³-tetrayltetrakis(oxy)]tetrakis(5-oxo-P,P,P-triphenylpentane-1-phosphonium) tetrabromide (4P). The values of minimum bactericidal concentration (MBC) against S. aureus methicillin sensitive and resistant and E. faecalis vancomycin sensitive and resistant were < 1 µM. At the same time, the compound does not involve damaging the cell wall, as is known for cationic amphiphilic compounds, and showed favorable safety profiles at MBC values. These findings highlight the potential of compounds found in liverworts as active agents against sensitive and resistant bacterial strains. Chemical modification of bis(bibenzyls) with a phosphonium cation is promising in preparation of potent microbicidal compounds.