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Artemisinin toxicity

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https://www.readbyqxmd.com/read/28289029/antimalarial-hybrid-molecules-a-close-reality-or-a-distant-dream
#1
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 towards finding alternate chemotherapeutic agents that are capable of combating multi-drug resistant parasite strains. In the above light, scientists have come up with the concept of hybridisation of two or more active pharmacophores into a single chemical entity, resulting in 'antimalarial hybrids.' The approach has been applied widely for lead generation against deadly diseases such as cancer and AIDS, with proven potential to be used as novel drugs, but is comparatively new in the sphere of antimalarial drug discovery...
March 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28287416/novel-pharmacological-activity-of-artesunate-and-artemisinin-their-potential-as-anti-tubercular-agents
#2
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
#3
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...
March 5, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28257497/investigating-antimalarial-drug-interactions-of-emetine-dihydrochloride-hydrate-using-calcusyn-based-interactivity-calculations
#4
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
#5
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
#6
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
#7
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...
February 16, 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
#8
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
#9
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
#10
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
https://www.readbyqxmd.com/read/27939426/preclinical-efficacy-and-safety-assessment-of-artemisinin-chemotherapeutic-agent-conjugates-for-ovarian-cancer
#11
Xiaoguang Li, Yu Zhou, Yanling Liu, Xu Zhang, Tao Chen, Kerong Chen, Qian Ba, Jingquan Li, Hong Liu, Hui Wang
Artemisinin (ARS) and its derivatives, which are clinically used antimalarial agents, have shown antitumor activities. Their therapeutic potencies, however, are limited by their low solubility and poor bioavailability. Here, through a pharmacophore hybridization strategy, we synthesized ARS-drug conjugates, in which the marketed chemotherapeutic agents chlorambucil, melphalan, flutamide, aminoglutethimide, and doxifluridine, were separately bonded to Dihydroartemisinin (DHA) through various linkages. Of these, the artemisinin-melphalan conjugate, ARS4, exhibited most toxicity to human ovarian cancer cells but had low cytotoxicity to normal cells...
December 2016: EBioMedicine
https://www.readbyqxmd.com/read/27930305/artemisia-annua-mutant-impaired-in-artemisinin-synthesis-demonstrates-importance-of-nonenzymatic-conversion-in-terpenoid-metabolism
#12
Tomasz Czechowski, Tony R Larson, Theresa M Catania, David Harvey, Geoffrey D Brown, Ian A Graham
Artemisinin, a sesquiterpene lactone produced by Artemisia annua glandular secretory trichomes, is the active ingredient in the most effective treatment for malaria currently available. We identified a mutation that disrupts the amorpha-4,11-diene C-12 oxidase (CYP71AV1) enzyme, responsible for a series of oxidation reactions in the artemisinin biosynthetic pathway. Detailed metabolic studies of cyp71av1-1 revealed that the consequence of blocking the artemisinin biosynthetic pathway is the redirection of sesquiterpene metabolism to a sesquiterpene epoxide, which we designate arteannuin X...
December 27, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27903279/in-vitro-and-in-vivo-anti-malarial-activity-of-novel-harmine-analog-heat-shock-protein-90-inhibitors-a-possible-partner-for-artemisinin
#13
Abebe Genetu Bayih, Asongna Folefoc, Abu Naser Mohon, Scott Eagon, Marc Anderson, Dylan R Pillai
BACKGROUND: The emergence of artemisinin-resistant Plasmodium falciparum strains poses a serious challenge to the control of malaria. This necessitates the development of new anti-malarial drugs. Previous studies have shown that the natural beta-carboline alkaloid harmine is a promising anti-malarial agent targeting the P. falciparum heat-shock protein 90 (PfHsp90). The aim of this study was to test the anti-malarial activity of harmine analogues. METHODS: Forty-two harmine analogues were synthesized and the binding of these analogues to P...
December 1, 2016: Malaria Journal
https://www.readbyqxmd.com/read/27900057/in-vitro-and-in-vivo-inhibition-of-tumor-cell-viability-by-combined-dihydroartemisinin-and-doxorubicin-treatment-and-the-underlying-mechanism
#14
Xiang Tai, Xiao-Bei Cai, Zhang Zhang, Rui Wei
The natural extract artemisinin and its derivatives have good anticancer activity. The present study aimed to investigate the in vitro inhibitory effects of combined dihydroartemisinin (DHA) and doxorubicin (DOX) treatment on a variety of tumor cell lines (HeLa, OVCAR-3, MCF-7, PC-3 and A549), as well as the underlying mechanisms. In addition, the in vivo effects of DHA and DOX were evaluated using a mouse HeLa tumor model. The HeLa, OVCAR-3, MCF-7, PC-3 and A549 cells were treated with a combination of DHA and DOX, and the effect on cell viability was detected by Cell Counting kit-8...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27739410/artemisinin-and-its-derivatives-as-a-repurposing-anticancer-agent-what-else-do-we-need-to-do
#15
REVIEW
Zhe Li, Qin Li, Jun Wu, Manyuan Wang, Junxian Yu
Preclinical investigation and clinical experience have provided evidence on the potential anticancer effect of artemisinin and its derivatives (ARTs) in the recent two decades. The major mechanisms of action of ARTs may be due to toxic-free radicals generated by an endoperoxide moiety, cell cycle arrest, induction of apoptosis, and inhibition of tumor angiogenesis. It is very promising that ARTs are expected to be a new class of antitumor drugs of wide spectrum due to their detailed information regarding efficacy and safety...
October 7, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27713827/evaluation-of-a-novel-pxr-knockout-in-heparg-%C3%A2-cells
#16
Beth Williamson, Mathias Lorbeer, Michael D Mitchell, Timothy G Brayman, Robert J Riley
The nuclear pregnane X receptor (PXR) regulates the expression of genes involved in the metabolism, hepatobiliary disposition, and toxicity of drugs and endogenous compounds. PXR is a promiscuous nuclear hormone receptor (NHR) with significant ligand and DNA-binding crosstalk with the constitutive androstane receptor (CAR); hence, defining the precise role of PXR in gene regulation is challenging. Here, utilising a novel PXR-knockout (KO) HepaRG cell line, real-time PCR analysis was conducted to determine PXR involvement for a range of inducers...
October 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/27652098/anti-inflammatory-and-acetylcholinesterase-activity-of-extract-fractions-and-five-compounds-isolated-from-the-leaves-and-twigs-of-artemisia-annua-growing-in-cameroon
#17
Rosine D K Chougouo, Yves M M Nguekeu, Jean P Dzoyem, Maurice D Awouafack, Jonas Kouamouo, Pierre Tane, Lyndy J McGaw, Jacobus N Eloff
BACKGROUND: Natural products, including those derived from higher plants have, over the years, contributed greatly to the development of modern therapeutic drugs. Due to the medicinal importance in traditional practice and the diversified biology and chemistry of the constituents from Artemisia spp., the genus has been receiving growing attention. The aim of this study was to investigate the ability of the ethanol extract, four fractions (F1-F4) and five compounds namely artemisinin (1), scopoletin (2), chrysosplenetin (3), eupatin (4) and 3-O-β-d-glucopyranoside of sitosterol (5) isolated from A...
2016: SpringerPlus
https://www.readbyqxmd.com/read/27599723/comparative-pharmacokinetics-and-pharmacodynamics-of-intravenous-artelinate-versus-artesunate-in-uncomplicated-plasmodium-coatneyi-infected-rhesus-monkey-model
#18
Paktiya Teja-Isavadharm, Duangsuda Siriyanonda, Maneerat Rasameesoraj, Amporn Limsalakpeth, Nitima Chanarat, Natthasorn Komcharoen, Peter J Weina, David L Saunders, Montip Gettayacamin, R Scott Miller
BACKGROUND: The US Army designed artelinate/lysine salt (AL) to overcome the instability of sodium artesunate in aqueous solution (AS). To select the most efficacious artemisinin treatment, direct comparison was performed in an uncomplicated non-human primate malaria model. METHODS: Splenectomized rhesus monkeys were inoculated with Plasmodium coatneyi and on day six, single equimolar loading dose of IV AL (11.8 mg kg(-1)) or IV AS (8 mg kg(-1)) were administered followed by 1/2 the first dose once daily for 2 more days...
2016: Malaria Journal
https://www.readbyqxmd.com/read/27596113/nanostructured-lipid-carriers-of-artemether-lumefantrine-combination-for-intravenous-therapy-of-cerebral-malaria
#19
Priyanka Prabhu, Shital Suryavanshi, Sulabha Pathak, Aditya Patra, Shobhona Sharma, Vandana Patravale
Patients with cerebral malaria (CM) are unable to take oral medication due to impaired consciousness and vomiting thus necessitating parenteral therapy. Quinine, artemether, and artesunate which are currently used for parenteral malaria therapy have their own drawbacks. The World Health Organization (WHO) has now banned monotherapy and recommends artemisinin-based combination therapy for malaria treatment. However, presently there is no intravenous formulation available for combination therapy of malaria. Artemether-Lumefantrine (ARM-LFN) is a WHO approved combination for oral malaria therapy...
November 20, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27506918/clinical-and-non-clinical-safety-of-artemisinin-derivatives-in-pregnancy
#20
Caroline Gomes, Ana Cláudia Boareto, Paulo Roberto Dalsenter
Malaria in pregnancy is a clinically wasting infectious disease, where drug therapy has to be promptly initiated. Currently, the treatment of this infection depends on the use of artemisinin derivatives. The World Health Organization does not recommend the use of these drugs in the first trimester of pregnancy due to non-clinical findings that have shown embryolethality and teratogenic effects. Nevertheless, until now, this toxicity has not been proved in humans. Artemisinin derivatives mechanisms of embryotoxicity are related to depletion of circulating embryonic primitive erythroblasts...
October 2016: Reproductive Toxicology
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