Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

Peter, Sijongesonke; Aderibigbe, Blessing Atim

doi:10.3390/molecules24193604

Cited by 117 publications

(56 citation statements)

References 75 publications

(141 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Natural products have been discovered as rich and powerful sources for anticancer and antimalarial therapies, including vinblastine from Catharanthus roseus [ 15 , 16 ], paclitaxel or taxol from Taxus brevifolia [ 17 , 18 ], curcurmin from Curcuma longa [ 19 ] and artemisinin from Artemisia annua [ 13 , 20 , 21 ]. Moreover, synthetic compounds were identified to be effective on both cancer cells and Plasmodium , such as gold- or iron-metallocenes [ 22 , 23 , 24 ]. One of these, ferroquine, an analog of chloroquine, showed high in vitro activity against P. falciparum [ 25 , 26 , 27 ] and antitumor activity [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

Cytotoxic and Anti-Plasmodial Activities of Stephania dielsiana Y.C. Wu Extracts and the Isolated Compounds

et al. 2020

View full text Add to dashboard Cite

Natural products remain a viable source of novel therapeutics, and as detection and extraction techniques improve, we can identify more molecules from a broader set of plant tissues. The aim of this study was an investigation of the cytotoxic and anti-plasmodial activities of the methanol extract from Stephania dielsiana Y.C. Wu leaves and its isolated compounds. Our study led to the isolation of seven alkaloids, among which oxostephanine (1) is the most active against several cancer cell lines including HeLa, MDA-MB231, MDA-MB-468, MCF-7, and non-cancer cell lines, such as 184B5 and MCF10A, with IC50 values ranging from 1.66 to 4.35 μM. Morever, oxostephanine (1) is on average two-fold more active against cancer cells than stephanine (3), having a similar chemical structure. Cells treated with oxostephanine (1) are arrested at G2/M cell cycle, followed by the formation of aneuploidy and apoptotic cell death. The G2/M arrest appears to be due, at least in part, to the inactivation of Aurora kinases, which is implicated in the onset and progression of many forms of human cancer. An in-silico molecular modeling study suggests that oxostephanine (1) binds to the ATP binding pocket of Aurora kinases to inactivate their activities. Unlike oxostephanine (1), thailandine (2) is highly effective against only the triple-negative MDA-MB-468 breast cancer cells. However, it showed excellent selectivity against the cancer cell line when compared to its effects on non-cancer cells. Furthermore, thailandine (2) showed excellent anti-plasmodial activity against both chloroquine-susceptible 3D7 and chloroquine-resistant W2 Plasmodium falciparum strains. The structure–activity relationship of isolated compound was also discussed in this study. The results of this study support the traditional use of Stephania dielsiana Y.C. Wu and the lead molecules identified can be further optimized for the development of highly effective and safe anti-cancer and anti-plasmodial drugs.

show abstract

Section: Introductionmentioning

confidence: 99%

Cytotoxic and Anti-Plasmodial Activities of Stephania dielsiana Y.C. Wu Extracts and the Isolated Compounds

et al. 2020

View full text Add to dashboard Cite

show abstract

“…Ferrocene derivatives have anti-proliferative activity against several cancer cell lines [125]. In addition, they are stable in aqueous solution and display advantageous redox properties with low toxicity [126,127].…”

Section: Fe Containing Moleculesmentioning

confidence: 99%

Iron Dysregulation in Human Cancer: Altered Metabolism, Biomarkers for Diagnosis, Prognosis, Monitoring and Rationale for Therapy

Lelièvre

Sancey

Coll

et al. 2020

Preprint

View full text Add to dashboard Cite

Iron (Fe) is a trace element that plays essential roles in various biological processes such as DNA synthesis and repair, as well as cellular energy production, or oxygen transport, and it is currently widely recognized that iron homeostasis is dysregulated in many cancers. Indeed, several iron homeostasis proteins may be responsible for malignant tumor initiation, proliferation, and for metastatic spread of tumors. A large number of studies demonstrated the potential clinical value of turning these deregulated proteins as prognostic and/or predictive biomarkers of malignancy and /or response to anticancer treatments. Additionally, the iron addiction of cancer cells and the importance of iron in ferroptosis cell death signaling pathways prompted the development of therapeutic strategies against advanced stage or resistant cancers. In this review, we selected relevant and promising studies in the field of iron metabolism in cancer research and clinical oncology. Besides, we discuss some co-existing discrepant findings. We will also present and discuss the latest lines of research related to targeting iron, or its regulatory pathways, as potential promising anti-cancer strategies for human therapy. Iron chelators, such as deferoxamine or iron-oxide based nanoparticles, which are already tested in clinical trials, alone or in combination with chemotherapy will also be reported.

show abstract

“…Among the various types of cancers, breast, lung, and colorectal cancer are the common types of cancers [ 3 ]. In 2018, it was estimated that there were 18.1 million cases of cancer with 9 million deaths worldwide [ 4 ]. The strategies that have been employed for the treatment of cancer include chemotherapy (anticancer drugs), surgery, immunotherapy, hormonal therapy, radiotherapy.…”

Section: Introductionmentioning

confidence: 99%

Nanoparticles Formulations of Artemisinin and Derivatives as Potential Therapeutics for the Treatment of Cancer, Leishmaniasis and Malaria

Alven

Aderibigbe

2020

Pharmaceutics

Self Cite

View full text Add to dashboard Cite

Cancer, malaria, and leishmaniasis remain the deadly diseases around the world although several strategies of treatment have been developed. However, most of the drugs used to treat the aforementioned diseases suffer from several pharmacological limitations such as poor pharmacokinetics, toxicity, drug resistance, poor bioavailability and water solubility. Artemisinin and its derivatives are antimalarial drugs. However, they also exhibit anticancer and antileishmanial activity. They have been evaluated as potential anticancer and antileishmanial drugs but their use is also limited by their poor water solubility and poor bioavailability. To overcome the aforementioned limitations associated with artemisinin and its derivatives used for the treatment of these diseases, they have been incorporated into nanoparticles. Several researchers incorporated this class of drugs into nanoparticles resulting in enhanced therapeutic outcomes. Their potential efficacy for the treatment of parasitic infections such as malaria and leishmaniasis and chronic diseases such as cancer has been reported. This review article will be focused on the nanoparticles formulations of artemisinin and derivatives for the treatment of cancer, malaria, and leishmaniasis and the biological outcomes (in vitro and in vivo).

show abstract

Ferrocene-Based Compounds with Antimalaria/Anticancer Activity

Cited by 117 publications

References 75 publications

Cytotoxic and Anti-Plasmodial Activities of Stephania dielsiana Y.C. Wu Extracts and the Isolated Compounds

Cytotoxic and Anti-Plasmodial Activities of Stephania dielsiana Y.C. Wu Extracts and the Isolated Compounds

Iron Dysregulation in Human Cancer: Altered Metabolism, Biomarkers for Diagnosis, Prognosis, Monitoring and Rationale for Therapy

Nanoparticles Formulations of Artemisinin and Derivatives as Potential Therapeutics for the Treatment of Cancer, Leishmaniasis and Malaria

Contact Info

Product

Resources

About