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Artemisinin toxicity

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https://www.readbyqxmd.com/read/28511056/elimination-of-schistosoma-mansoni-in-infected-mice-by-slow-release-of-artemisone
#1
Daniel Gold, Mohammed Alian, Avraham Domb, Yara Karawani, Maysa Jbarien, Jacques Chollet, Richard K Haynes, Ho Ning Wong, Viola Buchholz, Andreas Greiner, Jacob Golenser
The current treatment of schistosomiasis is based on the anti-helminthic drug praziquantel (PZQ). PZQ affects only the adult stages of schistosomes. In addition, resistance to PZQ is emerging. We suggest a drug, which could serve as a potential alternative or complement to PZQ, and as a means of treating infections at earlier, pre-granuloma stage. Derivatives of the peroxidic antimalarial drug artemisinin have been indicated as alternatives, because both plasmodia and schistosomes are blood-feeding parasites...
May 4, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28466458/rip1-dependent-reactive-oxygen-species-production-executes-artesunate-induced-cell-death-in-renal-carcinoma-caki-cells
#2
Anil Kumar Chauhan, Kyoung-Jin Min, Taeg Kyu Kwon
Artesunate is a well-known anti-malarial drug originated from artemisinin as a Chinese herb and has been reported to have anti-cancer potential in many cancer cells. In the present study, we examined the efficacy of artesunate against the renal carcinoma Caki cells and explored its mechanism of cytotoxicity. A steep decline in cell viability within 18 h was recorded upon artesunate exposure, but pretreatment of z-VAD-FMK had no effect on the loss of the cell viability by artesunate. On the other hand, necrostatin-1 pretreatment and knockdown of RIP-1 significantly reduced the cytotoxicity of artesunate against Caki cell...
May 2, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28454894/the-antimalarial-drug-artemisinin-induces-an-additional-sod1-supressible-anti-mitochondrial-action-in-yeast
#3
Chen Sun, Bing Zhou
The molecular action of artemisinins (ARTs) is not well understood. To determine the molecular and cellular basis that might underlie their differential effects observed in anti-malarial and anti-cancer studies, we utilized the yeast Saccharomyces cerevisiae to examine their toxicity profiles and properties. Previously we reported that while both low levels (2-8μM) of artemisinin (ART) and dihydroartemisinin (DHA) partly depolarize the mitochondrial membranes, inhibiting yeast growth on non-fermentable media, only DHA at moderate levels (such as 40μM) potently represses yeast growth on fermentable media via a heme-mediated pathway...
April 25, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28447781/artemisinin-protectes-retinal-neuronal-cells-against-oxidative-stress-and-restores-rat-retinal-physiological-function-from-light-exposed-damage
#4
Fengxia Yan, Hai-Tao Wang, Yang Gao, Jiang-Ping Xu, Wenhua Zheng
Oxidative stress plays a key role in the pathogenesis of age-related macular degeneration (AMD), a leading cause of severe visual loss and blindness in the aging population which lacks any effective treatments currently. In this study, artemisinin, a well-known anti-malarial drug was found to suppress hydrogen peroxide (H2O2)-induced cell death in retinal neuronal RGC-5 cells. Artemisinin, in the therapeutically relevant dosage, concentration-dependently attenuated the accumulation of intracellular reactive oxygen species (ROS), increased mitochondrial mitochondrial membrane potential and decreased cell apoptosis in RGC-5 cells induced by H2O2...
April 27, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28391183/artemisinin-protects-pc12-cells-against-%C3%AE-amyloid-induced-apoptosis-through-activation-of-the-erk1-2-signaling-pathway
#5
Zhiwen Zeng, Jinying Xu, Wenhua Zheng
Accumulating evidence displays that an abnormal deposition of amyloid beta-peptide (Aβ) is the primary cause of the pathogenesis of Alzheimer's disease (AD). And therefore the elimination of Aβ is regarded as an important strategy for AD treatment. The discovery of drug candidates using culture neuronal cells against Aβ peptide toxicity is believed to be an effective approach to develop drug for the treatment of AD patients. We have previously showed that artemisinin, a FDA-approved anti-malaria drug, has neuroprotective effects recently...
April 4, 2017: Redox Biology
https://www.readbyqxmd.com/read/28368011/a-mitochondria-targeting-artemisinin-derivative-with-sharply-increased-antitumor-but-depressed-anti-yeast-and-anti-malaria-activities
#6
Chen Sun, Yu Cao, Pan Zhu, Bing Zhou
The potent anti-malarial drug artemisinins are additionally anti-tumorigenic and inhibitory to yeast growth. The action mechanism of artemisinins, however, is not well understood. Heme and mitochondrial membrane are both suggested to be involved in the action of artemisinins. Because heme is also synthesized in the mitochondrion, mitochondria appear to be a critical organelle for artemisinins' activities. In this study, we synthesized a mitochondria-targeting artemisinin derivative by conjugating triphenylphosphonium (TPP) to artelinic acid (ARTa)...
April 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28366726/cancer-combination-therapies-with-artemisinin-type-drugs
#7
REVIEW
Thomas Efferth
Artemisia annua L. is a Chinese medicinal plant, which is used throughout Asia and Africa as tea or press juice to treat malaria. The bioactivity of its chemical constituent, artemisinin is, however, much broader. We and others found that artemisinin and its derivatives also exert profound activity against tumor cells in vitro and in vivo. Should artemisinin-type drugs be applied routinely in clinical oncology in the future, then it should probably be as part of combination therapy regimens rather than as monotherapy...
March 31, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28361857/artemisinin-modulating-effect-on-human-breast-cancer-cell-lines-with-different-sensitivity-to-cytostatics
#8
V F Chekhun, N Yu Lukianova, T V Borikun, T V Zadvorny, A Mokhir
AIM: To explore effects of Artemisinin on a series of breast cancer cells with different sensitivity to typical cytotoxic drugs (doxorubicin - Dox; cisplatin - DDP) and to investigate possible artemisinin-induced modification of the mechanisms of drug resistance. MATERIALS AND METHODS: The study was performed on wild-type breast cancer MCF-7 cell line (MCF-7/S) and its two sublines MCF-7/Dox and MCF-7/DDP resistant to Dox and DDP, respectively. The cells were treated with artemisinin and iron-containing magnetic fluid...
March 2017: Experimental Oncology
https://www.readbyqxmd.com/read/28359890/artemisinin-loaded-chitosan-magnetic-nanoparticles-for-theefficient-targeting-to-the-breast-cancer
#9
Subramanian Natesan, Chandrasekar Ponnusamy, Abimanyu Sugumaran, Senthilkumar Chelladurai, Sharavanan Shanmugam Palaniappan, Rajaguru Palanichamy
Artemisinin, a natural anti-malarial agent, also possesses anti-proliferative and anti-angiogenic activity in cancer cells with very low toxicity to normal healthy cells. Drug loaded magnetic nanoparticlesby using external magnetic field could selectively accumulate the drug at the target site and thereby reduce the doses required to achieve therapeutic concentration which may otherwise produce serious side effects on healthy cells. In the present study the artemisinin magnetic nanoparticles were successfully formulated using chitosan by ionic-gelation method...
March 27, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28356736/nanoliposomal-artemisinin-for-the-treatment-of-murine-visceral-leishmaniasis
#10
Muzamil Y Want, Mohammad Islammudin, Garima Chouhan, Hani A Ozbak, Hassan A Hemeg, Asoke P Chattopadhyay, Farhat Afrin
Visceral leishmaniasis (VL) is a fatal, vector-borne disease caused by the intracellular protozoa of the genus Leishmania. Most of the therapeutics for VL are toxic, expensive, or ineffective. Sesquiterpenes are a new class of drugs with proven antimicrobial and antiviral activities. Artemisinin is a sesquiterpene lactone with potent antileishmanial activity, but with limited access to infected cells, being a highly lipophilic molecule. Association of artemisinin with liposome is a desirable strategy to circumvent the problem of poor accessibility, thereby improving its efficacy, as demonstrated in a murine model of experimental VL...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28289029/are-antimalarial-hybrid-molecules-a-close-reality-or-a-distant-dream
#11
REVIEW
Drishti Agarwal, Rinkoo D Gupta, Satish K Awasthi
Emergence of drug-resistant Plasmodium falciparum strains has led to a situation of haste in the scientific and pharmaceutical communities. Hence, all their efforts are redirected toward finding alternative chemotherapeutic agents that are capable of combating multidrug-resistant parasite strains. In light of this situation, scientists have come up with the concept of hybridization of two or more active pharmacophores into a single chemical entity, resulting in "antimalarial hybrids." The approach has been applied widely for generation of lead compounds against deadly diseases such as cancer and AIDS, with a proven potential for use as novel drugs, but is comparatively new in the sphere of antimalarial drug discovery...
May 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28287416/novel-pharmacological-activity-of-artesunate-and-artemisinin-their-potential-as-anti-tubercular-agents
#12
Won Hyung Choi
Tuberculosis is a major infectious disease that globally causes the highest human mortality. From this aspect, this study was carried out to evaluate novel pharmacological activities/effects of artesunate and artemisinin causing anti-tubercular activity/effects against Mycobacterium tuberculosis (Mtb). The anti-Mtb activities/effects of artesunate and artemisinin were evaluated using different anti-Mtb indicator assays, such as the resazurin microtiter assay, the Mycobacteria Growth Indicator Tube (MGIT) 960 system assay, and the Ogawa slant medium assay, as well as in vivo tests...
March 10, 2017: Journal of Clinical Medicine
https://www.readbyqxmd.com/read/28273638/antimalarial-activity-and-safety-assessment-of-flueggea-virosa-leaves-and-its-major-constituent-with-special-emphasis-on-their-mode-of-action
#13
Shiv Vardan Singh, Ashan Manhas, Yogesh Kumar, Sonali Mishra, Karuna Shanker, Feroz Khan, Kumkum Srivastava, Anirban Pal
A clinical emergency stands due to the appearance of drug resistant Plasmodium strains necessitate novel and effective antimalarial chemotypes, where plants seem as the prime option, especially after the discovery of quinine and artemisinin. The present study was aimed towards bioprospecting leaves of Flueggea virosa for its antimalarial efficacy and active principles. Crude hydro-ethanolic extract along with solvent derived fractions were tested in vitro against Plasmodium falciparum CQ sensitive (3D7) and resistant (K1) strains, where all the fractions exhibited potential activity (IC50 values <10μg/mL) against both the strains...
May 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28257497/investigating-antimalarial-drug-interactions-of-emetine-dihydrochloride-hydrate-using-calcusyn-based-interactivity-calculations
#14
Holly Matthews, Jon Deakin, May Rajab, Maryam Idris-Usman, Niroshini J Nirmalan
The widespread introduction of artemisinin-based combination therapy has contributed to recent reductions in malaria mortality. Combination therapies have a range of advantages, including synergism, toxicity reduction, and delaying the onset of resistance acquisition. Unfortunately, antimalarial combination therapy is limited by the depleting repertoire of effective drugs with distinct target pathways. To fast-track antimalarial drug discovery, we have previously employed drug-repositioning to identify the anti-amoebic drug, emetine dihydrochloride hydrate, as a potential candidate for repositioned use against malaria...
2017: PloS One
https://www.readbyqxmd.com/read/28249591/controlled-release-of-artemisone-for-the-treatment-of-experimental-cerebral-malaria
#15
Jacob Golenser, Viola Buchholz, Amir Bagheri, Abed Nasereddin, Ron Dzikowski, Jintao Guo, Nicholas H Hunt, Sara Eyal, Natalia Vakruk, Andreas Greiner
BACKGROUND: Cerebral malaria (CM) is a leading cause of malarial mortality resulting from infection by Plasmodium falciparum. Treatment commonly involves adjunctive care and injections or transfusion of artemisinins. All artemisinins that are in current use are metabolized to dihydroxyartemisinin (DHA), to which there is already some parasite resistance. We used artemisone, a derivative that does not convert to DHA, has improved pharmacokinetics and anti-plasmodial activity and is also anti-inflammatory (an advantage given the immunopathological nature of CM)...
March 1, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28230749/design-of-drug-delivery-systems-containing-artemisinin-and-its-derivatives
#16
REVIEW
Blessing Atim Aderibigbe
Artemisinin and its derivatives have been reported to be experimentally effective for the treatment of highly aggressive cancers without developing drug resistance, they are useful for the treatment of malaria, other protozoal infections and they exhibit antiviral activity. However, they are limited pharmacologically by their poor bioavailability, short half-life in vivo, poor water solubility and long term usage results in toxicity. They are also expensive for the treatment of malaria when compared to other antimalarials...
February 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28207169/design-synthesis-and-biological-evaluation-of-novel-1-2-4-trioxanes-as-potential-antimalarial-agents
#17
Amit K Gupta, Kanika Varshney, Vivek Kumar, Kumkum Srivastava, Aditya B Pant, Sunil K Puri, Anil K Saxena
A series of substituted 1,2,4-trioxanes were synthesized and evaluated for their antimalarial potential, in silico ADME properties and cytotoxicity on neuronal cell lines. Among the 15 synthesized substituted 1,2,4-trioxanes, two compounds (compound 15, IC50  = 25.71 nM; compound 21, IC50  = 19.6 nM) exhibited promising in vitro antimalarial potential comparable to those of the existing drugs chloroquine and artemisinin. Both of these compounds were found to be nontoxic up to 20 µM concentration in neuronal PC-12 cells...
April 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28128956/accepting-the-invitation-to-open-innovation-in-malaria-drug-discovery-synthesis-biological-evaluation-and-investigation-on-the-structure-activity-relationships-of-benzo-b-thiophene-2-carboxamides-as-antimalarial-agents
#18
Marco Pieroni, Elisa Azzali, Nicoletta Basilico, Silvia Parapini, Michal Zolkiewski, Claudia Beato, Giannamaria Annunziato, Agostino Bruno, Federica Vacondio, Gabriele Costantino
Malaria eradication is a global health priority, but current therapies are not always suitable for providing a radical cure. Artemisinin has paved the way for the current malaria treatment, the so-called Artemisinin-based Combination Therapy (ACT). However, with the detection of resistance to ACT, innovative compounds active against multiple parasite species and at multiple life stages are needed. GlaxoSmithKline has recently disclosed the results of a phenotypic screening of an internal library, publishing a collection of 400 antimalarial chemotypes, termed the "Malaria Box"...
February 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28122572/artemether-lumefantrine-and-liver-enzyme-abnormalities-in-non-severe-plasmodium-falciparum-malaria-in-returned-travellers-a-retrospective-comparative-study-with-quinine-doxycycline-in-a-portuguese-centre
#19
André Silva-Pinto, Rogério Ruas, Francisco Almeida, Raquel Duro, André Silva, Cândida Abreu, António Sarmento
BACKGROUND: Artemisinin-based therapy is the current standard treatment for non-severe malaria due to Plasmodium falciparum. The potential for asymptomatic liver toxicity of this therapy and its implication in clinical practice is currently unknown. The aim of this study is to assess the hepatic function in patients treated with a standard three-day artemisinin-based regimen and to compare it with the quinine-doxycycline regimen. METHODS: Retrospective and comparative study of returned adult travellers admitted with non-severe P...
January 25, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28032463/developmental-toxicity-studies-of-lumefantrine-and-artemether-in-rats-and-rabbits
#20
Robert L Clark, Maureen Youreneff, Anthony M DeLise
The combination of artemether plus lumefantrine is a type of artemisinin-based combination therapy (ACT) recommended by the World Health Organization for uncomplicated falciparum malaria except in the first trimester of pregnancy. The first trimester restriction was based on the marked embryotoxicity in animals (including embryo death and cardiac and skeletal malformations) of artemisinins such as artesunate, dihydroartemisinin, and artemether. Before recommending ACTs for use in the first trimester, the World Health Organization has requested that all information relevant to the assessment of risk of ACTs to the embryo be made available to the public...
December 2016: Birth Defects Research. Part B, Developmental and Reproductive Toxicology
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