Search results for "Artemisinin"
showing 9 items of 59 documents
Synthesis and study of cytotoxic activity of 1,2,4-trioxane- and egonol-derived hybrid molecules against Plasmodium falciparum and multidrug-resistan…
2014
Abstract Malaria and cancer cause the death of millions of people every year. To combat these two diseases, it is important that new pharmaceutically active compounds have the ability to overcome multidrug resistance in cancer and Plasmodium falciparum strains. In search of effective anti-cancer and anti-malaria hybrids that possess improved properties compared to their parent compounds, a series of novel 1,2,4-trioxane-based hybrids incorporating egonol and/or ferrocene fragments were synthesized and tested in vitro against P. falciparum strains, CCRF–CEM cells and the multidrug-resistant P-glycoprotein-over-expressing CEM/ADR5000 cells. The most active compounds against P. falciparum stra…
Cytotoxic activity of secondary metabolites derived from Artemisia annua L. towards cancer cells in comparison to its designated active constituent a…
2010
Artemisia annua L. (sweet wormwood, qinhao) has traditionally been used in Chinese medicine. The isolation of artemisinin from Artemisia annua and its worldwide accepted application in malaria therapy is one of the showcase success stories of phytomedicine during the past decades. Artemisinin-type compounds are also active towards other protozoal or viral diseases as well as cancer cells in vitro and in vivo. Nowadays, Artemisia annua tea is used as a self-reliant treatment in developing countries. The unsupervised use of Artemisia annua tea has been criticized to foster the development of artemisinin resistance in malaria and cancer due to insufficient artemisinin amounts in the plant as c…
Novel Developments on Artemisinin and Its Derivatives for Cancer Therapy
2009
The lack of effective long-term anticancer therapy highlights the necessity to identify new potent anticancer compounds. Many biocompounds of naturally occurring medicinal plants have pharmacological activities and, thus, represent a source of molecules that may have anti-proliferative effects on a variety of cancers. During the past 10 years, we have systematically analyzed medicinal plants used in traditional Chinese medicine and focused our interest on Artemisia annua (sweet wormwood herb). The active principle of sweet wormwood herb is Artemisinin, a sesquiterpene, which exerts not only anti-malarial activity but also profound cytotoxicity against tumour cells. The anti-tumour mechanism…
<strong>Artemisinin: Tentative Mechanism of Action and Resistance</strong>
2016
The sesquiterpene lactones constitute a large class of secondary plant metabolites, which carry a‑methylene‑g‑lactone groups as common structural element and display a number of bioactivities. Every year, 1–2 million people living in the tropics and subtropics die of malaria. Lactone artemisinin is the most effective treatment vs. malaria, the most infectious disease in the world today. Artemisinins are derived from extracts of sweet wormwood (Artemisia annua) and are well established for the treatment of malaria, e.g., highly drug-resistant strains. They resulted in one of the most significant advances in the treatment of malaria since the discovery and first use of quinine over 300 years …
Synthesis and biological evaluation of antimalarial and antileukemic activity of new C-10 modified artemisinin derivatives
2021
Abstract Several non-acetal artemisinin derivatives were synthesized and their antimalarial activity against chloroquine-resistant parasites as well as their antileukemic activity were investigated. The azide 10 was proved to have slightly better activity than the current antimalarial drugs such as artesunate and chloroquine. In addition, the azide 10 and the aldehyde 7 were found to be effective in decreasing cell proliferation in leukemia cells.
Activation of Mitochondria-Driven Pathways by Artemisinin and Its Derivatives
2014
Mitochondria have recently emerged as promising agents for cancer therapy. Of particular interest and potential clinical relevance are agents that target these organelles, promoting cell death. There are literally thousands of compounds that act on mitochondria and destabilise them. Of these, naturally occurring compounds are particularly interesting, since they are often more ‘biocompatible’; besides, natural compounds can be lead drugs for the design of novel and more efficient anti-cancer agents. In this paper, we focus on the natural product artemisin and its semisynthetic derivatives, and document the molecular mechanism of their activity and their potential use as clinically relevant …
Artemisinin–Second Career as Anticancer Drug?
2015
Artemisinin represents a showcase example not only for the activity of medicinal herbs deriving from traditional chinese medicine, but for phytotherapy in general. Its isolation from Sweet Wormwood (qinhao, Artemisia annua L.) represents the starting point for an unprecedent success story in the treatment of malaria worldwide. Beyond the therapeutic value against Plasmodium parasites, it turned out in recent years that the bioactivity of artemisinin is not restricted to malaria. We and others found that this sesquiterpenoid also exerts profound anticancer activity in vitro and in vivo. Artemisinin-type drugs exert multi-factorial cellular and molecular actions in cancer cells. Ferrous iron …
A conceptually new treatment approach for relapsed glioblastoma: Coordinated undermining of survival paths with nine repurposed drugs (CUSP9) by the …
2013
Kast, Richard E. et al.
Cytotoxicity of natural products and derivatives toward MCF-7 cell monolayers and cancer stem-like mammospheres
2015
Abstract Although cancer stem-like cells (CSCs) are rare, they can enter a non-proliferative or dormant state and resist therapy. Furthermore, quiescent CSCs are responsible for metastases that can appear after curative surgical treatment of a primary tumor. Because of drug resistance of CSCs, the development of novel therapies is urgently required that specifically target CSCs. Purpose The aim of the present study was to investigate the potential of a panel of natural products and derivatives to inhibit CSC-enriched mammospheres of MCF-7 breast cancer cells. Methods CD44high/CD24low cells were identified by flow cytometry and maintained as mammospheres. As a control, we used two clinically…