Cytotoxic Potential of the Monoterpene Isoespintanol against Human Tumor Cell Lines.

Cancer is a disease that encompasses multiple and different malignant conditions and is among the leading causes of death in the world. Therefore, the search for new pharmacotherapeutic options and potential candidates that can be used as treatments or adjuvants to control this disease is urgent. Natural products, especially those obtained from plants, have played an important role as a source of specialized metabolites with recognized pharmacological properties against cancer, therefore, they are an excellent alternative to be used. The objective of this research was to evaluate the action of the monoterpene isoespintanol (ISO) against the human tumor cell lines MDA-MB-231, A549, DU145, A2780, A2780-cis and the non-tumor line MRC-5. Experiments with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and fluorescence with propidium iodide (PI), 4',6-diamidino-2-phenylindole dilactate (DAPI) and green plasma revealed the cytotoxicity of ISO against these cells; furthermore, morphological and chromogenic studies revealed the action of ISO on cell morphology and the inhibitory capacity on reproductive viability to form colonies in MDA-MB-231 cells. Likewise, 3D experiments validated the damage in these cells caused by this monoterpene. These results serve as a basis for progress in studies of the mechanisms of action of these compounds and the development of derivatives or synthetic analogues with a better antitumor profile.

N-Methyl-2-(1-methyl-3-phenyl-prop-2-en-1-yl-idene)hydrazinecarbo-thio-amide.

In the title compound, C12H15N3S, the mol-ecule deviates slightly from planarity, with a maximum deviation from the mean plane of the non-H atoms of 0.2756 (6) Šfor the S atom and a torsion angle for the N-N-C-N fragment of -7.04 (16)°. In the crystal, mol-ecules are linked by N-H⋯S hydrogen-bond inter-actions, forming centrosymmetric dimers. Additionally, one weak intra-molecular N-H⋯N hydrogen-bond inter-action is observed. The crystal packing shows a herringbone arrangement viewed along the c axis.

Role of Cathepsin B in Cancer Progression: A Potential Target for Coordination Compounds.

A member of cathepsin enzymes called Cathepsin B is a cysteine-protease enzyme that plays significant role in metalloproteinase regulation. Cathepsin B stands out amidst other members of cathepsin because of its role in both normal body physiology and pathophysiology. Being an antiapoptotic and a pro-apoptotic agent, Cathepsin B has been reported to have deleterious effects, especially when its expression, activities, and distribution are outrageous. The over-expression of cathepsin B is traceable to dysregulation of one or more regulated steps involved in its synthesis. Consequently, the over-expression of cathepsin B contributes to the pathogenesis of different types of cancers - a global menace. Interestingly, the synthesis of this enzyme has been reported to be inhibited by several metal compounds, thus, curbing its involvement in carcinogenesis. In this review, the synthesis, structure, localization, and roles of cathepsin B in carcinogenesis were explored. Likewise, we also discussed the capacity of metallic compounds to inhibit this enzyme. Metals such as gold, ruthenium, palladium, Iridium, and Tellurium demonstrated remarkable activity toward cathepsin B of different modes. A relationship between cytotoxicity and inhibition constants was observed.

Crystal structure of (E)-2-[4-(4-hy-droxy-phen-yl)butan-2-yl-idene]hydrazine-1-carbo-thio-amide.

The title compound, C11H15N3OS, is a thio-semicarbazone derivative of the raspberry ketone rheosmin [systematic name: 4-(4-hy-droxy-phen-yl)butane-2-one]. The mol-ecule deviates from planarity, with the bridging C-C-C=N torsion angle equal to -101.3 (2)°. The maximum deviation from the mean plane of the non-H atoms of the thio-semicarbazone fragment [C=N-N-C(= S)-N] is 0.085 (5) Šfor the Schiff base N atom, and the dihedral angle between this mean plane and the aromatic ring is 50.31 (8)°. In the crystal, mol-ecules are linked by N-H⋯O, N-H⋯S and O-H⋯S hydrogen bonds, forming a three-dimensional structure, with the mol-ecules stacked along [011].