Omanische Heilpflanze im Fokus der Phytochemie IPB-Wissenschaftler und Partner aus Dhofar haben jüngst die omanische Heilpflanze Terminalia dhofarica unter die phytochemische Lupe genommen. Die Pflanze ist reich an…
Geschmack ist vorhersagbar: Mit FlavorMiner. FlavorMiner heißt das Tool, das IPB-Chemiker und Partner aus Kolumbien jüngst entwickelt haben. Das Programm kann, basierend auf maschinellem Lernen (KI), anhand der…
Smolková, R.; Smolko, L.; Samoľová, E.; Morgan, I.; Rennert, R.; Kaluđerović, G. N.;Novel Zn(ii), Co(ii) and Cu(ii) diflunisalato complexes with neocuproine and their exceptional antiproliferative activity against cancer cell linesDalton Trans.5317595-17607(2024)DOI: 10.1039/d4dt01736f
Three novel complexes of deprotonated diflunisal (dif) with neocuproine (neo) were synthesized and characterized via elemental, spectral (UV-vis, FTIR, fluorescence, and mass spectrometry), and single-crystal X-ray diffraction analyses. Although the compounds shared a similar composition of [MCl(dif)(neo)], where M represents Zn(II) (1), Co(II) (2) and Cu(II) (3), only 1 and 2 were isostructural, while 3 differed in both the molecular and supramolecular structures. In all three complex molecules, the central atom is coordinated by two nitrogen atoms of neo in a bidentate chelate mode, and one chlorido ligand and dif is bonded in either a monodentate mode via one oxygen atom of the carboxylate in 1 and 2 or in a bidentate chelate mode via both carboxylate oxygen atoms in 3. All three compounds demonstrated remarkable antiproliferative activity against human prostate (PC-3), colon (HCT116) and breast (MDA-MB-468) cancer cell lines with IC50 values in the nanomolar range, with the lowest values observed in the case of PC-3 and MDA-MB-468 with 2 (20.0 nM) and 3 (31.1 nM), respectively. Moreover, complex 2, as the most active, was further investigated for its potential to induce perturbations in the cell cycle of PC-3 cells. The results indicated an induction of caspase-independent apoptosis. The interaction of the complexes with genomic DNA isolated from the respective cancer cell lines was evaluated for the intercalative mode, with binding strength correlated with the antiproliferative activity against PC-3 and MDA-MB-468 cancer cell lines.
Publikation
Predarska, I.; Saoud, M.; Morgan, I.; Eichhorn, T.; Kaluđerović, G. N.; Hey-Hawkins, E.;Cisplatin−cyclooxygenase inhibitor conjugates, free and immobilised in mesoporous silica SBA-15, prove highly potent against triple-negative MDA-MB-468 breast cancer cell lineDalton Trans.51857–869(2022)DOI: 10.1039/d1dt03265h
For the development of anticancer drugs with higher activity and reduced
toxicity, two approaches were combined: preparation of platinum(IV) complexes exhibiting higher stability compared to their platinum(II)
counterparts and loading them into mesoporous silica SBA-15 with the
aim to utilise the passive enhanced permeability and retention (EPR)
effect of nanoparticles for accumulation in tumour tissues. Three
conjugates based on a cisplatin scaffold bearing the anti-inflammatory
drugs naproxen, ibuprofen or flurbiprofen in the axial positions (1, 2 and 3, respectively) were synthesised and loaded into SBA-15 to afford the mesoporous silica nanoparticles (MSNs) SBA-15|1, SBA-15|2 and SBA-15|3.
Superior antiproliferative activity of both free and immobilised
conjugates in a panel of four breast cancer cell lines (MDA-MB-468,
HCC1937, MCF-7 and BT-474) with markedly increased cytotoxicity with
respect to cisplatin was demonstrated. All compounds exhibit highest
activity against the triple-negative cell line MDA-MB-468, with
conjugate 1 being the most potent. However, against MCF-7 and BT-474 cell lines, the most notable improvement was found, with IC50
values up to 240-fold lower than cisplatin. Flow cytometry assays
clearly show that all compounds induce apoptotic cell death elevating
the levels of both early and late apoptotic cells. Furthermore,
autophagy as well as formation of reactive oxygen species (ROS) and
nitric oxide (NO) were elevated to a similar or greater extent than with
cisplatin.
Bücher und Buchkapitel
Restrepo, S.; Samper, C.; di Palma, F.; Hodson, E.; Torres, M.; Reol, E. M.; Eddi, M.; Wessjohann, L.; Jaramillo, G. P.; et al., .;Colombia hacia una sociedad
del conocimiento. Reflexiones
y propuestas1-450(2020)ISBN:978-958-5135-12-3
Medicago truncatula, owing to its small diploid genome (∼500 Mbp), short life cycle, and high natural diversity makes it a good model plant and has opened the door of opportunities for scientists interested in studying legume biology. But over the years, challenges are also being faced for genetic manipulation of this plant. Many genetic manipulation protocols have been published involving Agrobacterium tumefaciens, a pathogen causing tumor disease in plants. These protocols apart from being difficult to achieve, are also time consuming. Nowadays, an easy, less time consuming and highly reproducible Agrobacterium rhizogenes based method is in use by many research groups. This method generates composite plants having transformed roots on a wild‐type shoot. Here, stable transformed lines that can be propagated over time are not achieved by this method, but for root‐development or root–microbe interaction studies this method has proven to be a useful tool for the community. In addition, transformed roots can be propagated by root organ cultures (ROCs), wherein transformed roots are propagated on sucrose containing media without any shoot part. Occasionally, even stable transgenic plants can be regenerated from transgenic roots. In this chapter, developments and improvements of various transformation protocols are discussed. The suitability of composite plants is highlighted by a study on mycorrhization of transformed and non‐transformed roots, which did not show differences in the mycorrhization rate and developmental stages of the arbuscular mycorrhizal (AM) fungus inside the roots as well as in transcript accumulation and metabolite levels of roots. Finally, applications of the A. rhizogenes based transformation method are discussed.