Green synthesized pyridazinone derivatives as promising biologically active and anticancer drugs

2021 ◽  
Vol 0 (0) ◽  
pp. 0-0
Author(s):  
Amal Selim ◽  
fathy yassin ◽  
Ahmed Salama
Keyword(s):  
Anticancer Drugs ◽  
Biologically Active ◽  
Pyridazinone Derivatives

scholarly journals Anticancer Drugs from Marine Flora: An Overview

2010 ◽  
Vol 2010 ◽  
pp. 1-18 ◽  
Author(s):  
N. Sithranga Boopathy ◽  
K. Kathiresan
Keyword(s):  
Anticancer Drugs ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Sulphated Polysaccharides ◽  
Lead Compounds ◽  
Present Context ◽  
Baseline Information ◽  
Marine Flora ◽  
New Anticancer Drugs ◽  
Great Scope

Marine floras, such as bacteria, actinobacteria, cyanobacteria, fungi, microalgae, seaweeds, mangroves, and other halophytes are extremely important oceanic resources, constituting over 90% of the oceanic biomass. They are taxonomically diverse, largely productive, biologically active, and chemically unique offering a great scope for discovery of new anticancer drugs. The marine floras are rich in medicinally potent chemicals predominantly belonging to polyphenols and sulphated polysaccharides. The chemicals have displayed an array of pharmacological properties especially antioxidant, immunostimulatory, and antitumour activities. The phytochemicals possibly activate macrophages, induce apoptosis, and prevent oxidative damage of DNA, thereby controlling carcinogenesis. In spite of vast resources enriched with chemicals, the marine floras are largely unexplored for anticancer lead compounds. Hence, this paper reviews the works so far conducted on this aspect with a view to provide a baseline information for promoting the marine flora-based anticancer research in the present context of increasing cancer incidence, deprived of the cheaper, safer, and potent medicines to challenge the dreadful human disease.

In vitro chemosensitivity testing of mammospheres cultured from circulating epithelial tumor cells (CETCs) of breast cancer patients: Comparision to chemosensitivity of total CETCs.

2014 ◽  
Vol 32 (26_suppl) ◽  
pp. 50-50
Author(s):  
Monika Pizon ◽  
Dorothea Zimon ◽  
Ulrich A. Pachmann ◽  
Katharina Pachmann
Keyword(s):  
Suspension Culture ◽  
Tumor Cells ◽  
Anticancer Drugs ◽  
White Blood Cells ◽  
Biologically Active ◽  
Epithelial Tumor ◽  
Chemosensitivity Testing ◽  
In Vitro Chemosensitivity ◽  
Epithelial Tumor Cells

50 Background: In vitro chemosensitivity testing of circulating epithelial tumor cells (CETCs) provides real-time information about the sensitivity of the tumor cells present in the patient. Nevertheless, a fraction of CETCs can survive after conventional chemotherapy and grow into distant metastasis. This may be a subpopulation of CETCs with proliferation activity which has the ability to form floating spheres in suspension culture. Spheroids exhibit stem cell-like properties and may be responsible for chemotherapeutic resistance. Therefore, the aim of our study was to determine the efficacy of chemotherapeutics on spheroids cultured from CETCs. Methods: The enumeration of CETCs from patients with solid tumors in clinical stage I to IV was performed using the maintrac method. Subsequently, CETCs in the context of the surrounding white blood cells were cultured in a suspension culture allowing for spheroid formation. To evaluate the cytotoxic effect of drugs on CETCs and spheroids we exposed them to anticancer drugs in short time culture in different concentrations and for different periods of time. Results: In contrast to CETCs, spheroids were significantly more chemotherapy resistant. Active drugs led to disintegration of tumor spheres. Interestingly, some cells in the spheres were able to survive. Epirubicin and especially salinomycin, a polyether ionophore antibiotic isolated from Streptomyces albus, showed high efficacy in a high proportion of cells. Furthermore, our data suggested that curcumin, a natural biologically active compound that is extracted from the plant Curcuma longais a promising agent for cancer treatment. Docetaxel, cyclophosphamide, and 5-fluoruracil showed lower cytotoxic effects onto the cells in the spheres. Conclusions: Our results show, for the first time, that stem cells circulating in peripheral blood, capable of forming spheroids are way more resistant to anticancer drugs than the remnant circulating tumor cells. We, furthermore, demonstrate that salinomycin and curcumin efficiently destroy spheroids cultured from CETCs, strengthening their role as promising anticancer therapeutics.

Towards targeting anticancer drugs: ruthenium(ii)–arene complexes with biologically active naphthoquinone-derived ligand systems

2016 ◽  
Vol 45 (33) ◽  
pp. 13091-13103 ◽  
Author(s):  
Mario Kubanik ◽  
Wolfgang Kandioller ◽  
Kunwoo Kim ◽  
Robert F. Anderson ◽  
Erik Klapproth ◽  
...  
Keyword(s):  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Biologically Active ◽  
Arene Complexes

2-Hydroxy-[1,4]-naphthoquinone-derived ligands and their RuII(η6-p-cymene)Cl complexes were prepared with the aim to obtain multimodal anticancer agents.

scholarly journals The Protein-Binding Behavior of Platinum Anticancer Drugs in Blood Revealed by Mass Spectrometry

2021 ◽  
Vol 14 (2) ◽  
pp. 104
Author(s):  
Jingchen Wang ◽  
Jianmei Tao ◽  
Shuailong Jia ◽  
Meiqin Wang ◽  
Hongliang Jiang ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Protein Binding ◽  
Anticancer Drugs ◽  
Biologically Active ◽  
Platinum Drugs ◽  
Ionization Mass ◽  
Esi Ms ◽  
Binding Behavior ◽  
Platinum Anticancer Drugs ◽  
Drugs In Blood

Cisplatin and its analogues are widely used as chemotherapeutic agents in clinical practice. After being intravenously administrated, a substantial amount of platinum will bind with proteins in the blood. This binding is vital for the transport, distribution, and metabolism of drugs; however, toxicity can also occur from the irreversible binding between biologically active proteins and platinum drugs. Therefore, it is very important to study the protein-binding behavior of platinum drugs in blood. This review summarizes mass spectrometry-based strategies to identify and quantitate the proteins binding with platinum anticancer drugs in blood, such as offline high-performance liquid chromatography/inductively coupled plasma mass spectrometry (HPLC–ICP-MS) combined with electrospray ionization mass spectrometry (ESI-MS/MS) and multidimensional LC–ESI-MS/MS. The identification of in vivo targets in blood cannot be accomplished without first studying the protein-binding behavior of platinum drugs in vitro; therefore, relevant studies are also summarized. This knowledge will further our understanding of the pharmacokinetics and toxicity of platinum anticancer drugs, and it will be beneficial for the rational design of metal-based anticancer drugs.

Delivery of Constitutively Active Mutant MKK6(E) With TAT-OSBP Induces Apoptosis in Human Ovarian Carcinoma HO8910 Cells

2015 ◽  
Vol 25 (9) ◽  
pp. 1548-1556
Author(s):  
Hua Liao ◽  
Jia-li Kang ◽  
Wen-yan Jiang ◽  
Cui Deng ◽  
Jin Yuan ◽  
...  
Keyword(s):  
Ovarian Cancer ◽  
Ovarian Carcinoma ◽  
Anticancer Drugs ◽  
Cancer Cell ◽  
Biologically Active ◽  
Cell Permeability ◽  
Significant Difference ◽  
Tumor Selectivity ◽  
Human Ovarian Carcinoma ◽  
Constitutively Active

AbstractBiologically active peptides and proteins are novel agents that show promise in the development of anticancer drugs. Their relatively low cell permeability and poor tumor selectivity, however, impede their widespread applicability. In this study, we evaluated the tumor selectivity, cellular internalization, and biological activity of a cell-permeable ovarian cancer cell–specific therapeutic protein consisting of TAT-OSBP and constitutively active MKK6(E), an upstream kinase of the p38 signaling pathway that mediates cellular apoptosis. OSBP, a 7-amino-acid peptide with high affinity for human ovarian cancer HO8910 cells, was conjugated to the cell-penetrating peptide (TAT) to form a tumor-selective peptide (TAT-OSBP), which was further conjugated with EGFP or MKK6(E). Flow cytometry and fluorescent microscopy were performed to evaluate the tumor-targeted penetration of TAT-OSBP-EGFP. The inhibitory effects of TAT-OSBP-MKK6(E) were determined by cell proliferation and apoptosis assays. The internalization efficiency of TAT-OSBP-EGFP was significantly higher than that of TAT-EGFP. TAT-OSBP-EGFP selectively penetrated HO8910 cells. TAT-OSBP-MKK6(E) fusion protein inhibited cancer cell growth to varying degrees, with the highest level of inhibition in HO8910 cells. Moreover, TAT-OSBP-MKK6(E) significantly induced apoptosis of HO8910 cells. However, there was no significant difference in apoptosis in the normal ovarian epithelial cells treated with either TAT-OSBP-MKK6(E) or TAT-MKK6(E). Our results demonstrate that TAT-OSBP-MKK6(E) is a novel artificially designed molecule, which induces apoptosis and selectively targets human ovarian carcinoma HO8910 cells. Our study provides novel insights that may aid in the development of a new generation of anticancer drugs.

Characterization of photosystem II with the atomic-force microscope

1992 ◽  
Vol 50 (2) ◽  
pp. 1146-1147
Author(s):  
Kathleen M. Marr ◽  
Mary K. Lyon
Keyword(s):  
Photosystem Ii ◽  
Atomic Force Microscope ◽  
Three Dimensional ◽  
Biologically Active ◽  
Atomic Force ◽  
Freeze Etching ◽  
Image Averaging ◽  
Oxygen Evolving ◽  
Averaging Techniques

Photosystem II (PSII) is different from all other reaction centers in that it splits water to evolve oxygen and hydrogen ions. This unique ability to evolve oxygen is partly due to three oxygen evolving polypeptides (OEPs) associated with the PSII complex. Freeze etching on grana derived insideout membranes revealed that the OEPs contribute to the observed tetrameric nature of the PSIl particle; when the OEPs are removed, a distinct dimer emerges. Thus, the surface of the PSII complex changes dramatically upon removal of these polypeptides. The atomic force microscope (AFM) is ideal for examining surface topography. The instrument provides a topographical view of individual PSII complexes, giving relatively high resolution three-dimensional information without image averaging techniques. In addition, the use of a fluid cell allows a biologically active sample to be maintained under fully hydrated and physiologically buffered conditions. The OEPs associated with PSII may be sequentially removed, thereby changing the surface of the complex by one polypeptide at a time.

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