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Artemisinin toxicity

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https://www.readbyqxmd.com/read/28032463/developmental-toxicity-studies-of-lumefantrine-and-artemether-in-rats-and-rabbits
#1
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
#2
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...
December 2016: EBioMedicine
https://www.readbyqxmd.com/read/27930305/artemisia-annua-mutant-impaired-in-artemisinin-synthesis-demonstrates-importance-of-nonenzymatic-conversion-in-terpenoid-metabolism
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
https://www.readbyqxmd.com/read/27478545/therapeutic-effects-of-dihydroartemisinin-and-transferrin-against-glioblastoma
#12
Suk Hee Kim, Seong Hee Kang, Bo Sun Kang
BACKGROUND/OBJECTIVES: Artemisinin, a natural product isolated from Gaeddongssuk (artemisia annua L.) and its main active derivative, dihydroartemisinin (DHA), have long been used as antimalarial drugs. Recent studies reported that artemisinin is efficacious for curing diseases, including cancers, and for improving the immune system. Many researchers have shown the therapeutic effects of artemisinin on tumors such as breast cancer, liver cancer and kidney cancer, but there is still insufficient data regarding glioblastoma (GBM)...
August 2016: Nutrition Research and Practice
https://www.readbyqxmd.com/read/27321410/antimalarial-actions-of-lawsonia-inermis-tithonia-diversifolia-and-chromolaena-odorata-in-combination
#13
Funmilayo I D Afolayan, Olayemi M Adegbolagun, Beatrice Irungu, Lucy Kangethe, Jennifer Orwa, Chiaka I Anumudu
ETHNOPHARMACOLOGICAL RELEVANCE: Chromolaena odorata, Tithonia diversifolia and Lawsonia inermis are medicinal plants used in treating malaria in traditional medicine system. Previous studies however showed that their dichloromethane, methanol (1:1) extracts were more active against Plasmodium parasite than the aqueous extracts. AIM OF THE STUDY: To determine the in vitro and in vivo antiplasmodial activity of dichloromethane, methanol (1:1) extracts of Chromolaena odorata, Tithonia diversifolia and Lawsonia inermis in combination and evaluate their safety using acute limit toxicity test...
September 15, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27278417/teratogenicity-of-artemether-clindamycin-nanostructured-lipid-carriers-in-rats
#14
Soniya A Jain, Madhavi Awale, Sulabha Pathak, Geeta Vanage, Vandana B Patravale, Shobhona Sharma
Currently, artemisinin-based combination therapy is considered the best option in the treatment of malaria. However, toxicity of artemisinins limits their use in pregnancy. In the absence of sufficient toxicity data, the World Health Organization recommends that artemisinins are not to be used in the first trimester of pregnancy and can be used only in second and third trimesters, when other treatments are not available. We have recently observed that drugs loaded in nanolipid carriers are selectively taken up in Plasmodium-infected erythrocytes with a concomitant reduction in the dose required to cure animals...
July 2016: International Journal of Toxicology
https://www.readbyqxmd.com/read/27240160/controllable-synthesis-of-dual-mofs-nanostructures-for-ph-responsive-artemisinin-delivery-magnetic-resonance-and-optical-dual-model-imaging-guided-chemo-photothermal-combinational-cancer-therapy
#15
Dongdong Wang, Jiajia Zhou, Ruhui Chen, Ruohong Shi, Gaozheng Zhao, Guoliang Xia, Ren Li, Zhenbang Liu, Jie Tian, Huijuan Wang, Zhen Guo, Haibao Wang, Qianwang Chen
Theranostic nanoagents which integrate diagnostic and therapeutic moieties into a single platform have attracted broad attention in cancer therapy, however the development of more effective and less toxic diagnostic and therapeutic interventions is still of great urgency. Herein, novel core-shell PB@MIL-100(Fe) dual metal-organic-frameworks (d-MOFs) nanoparticles are fabricated and their combined theranostic effects in vitro and in vivo are investigated. The d-MOFs nanoparticles can serve as a T1-T2 dual-modal magnetic resonance imaging (MRI) contrast and fluorescence optical imaging (FOI) agent due to the existence of inner PB MOFs and outer MIL-100(Fe) MOFs...
September 2016: Biomaterials
https://www.readbyqxmd.com/read/27230403/pyrrolidine-acridine-hybrid-in-artemisinin-based-combination-a-pharmacodynamic-study
#16
Swaroop Kumar Pandey, Subhasish Biswas, Sarika Gunjan, Bhavana Singh Chauhan, Sunil Kumar Singh, Kumkum Srivastava, Sarika Singh, Sanjay Batra, Renu Tripathi
Aiming to develop new artemisinin-based combination therapy (ACT) for malaria, antimalarial effect of a new series of pyrrolidine-acridine hybrid in combination with artemisinin derivatives was investigated. Synthesis, antimalarial and cytotoxic evaluation of a series of hybrid of 2-(3-(substitutedbenzyl)pyrrolidin-1-yl)alkanamines and acridine were performed and mode of action of the lead compound was investigated. In vivo pharmacodynamic properties (parasite clearance time, parasite reduction ratio, dose and regimen determination) against multidrug resistant (MDR) rodent malaria parasite and toxicological parameters (median lethal dose, liver function test, kidney function test) were also investigated...
September 2016: Parasitology
https://www.readbyqxmd.com/read/27210430/straightforward-conversion-of-decoquinate-into-inexpensive-tractable-new-derivatives-with-significant-antimalarial-activities
#17
Richard M Beteck, Dina Coertzen, Frans J Smit, Lyn-Marie Birkholtz, Richard K Haynes, David D N'Da
As part of a programme aimed at identifying rational new triple drug combinations for treatment of malaria, tuberculosis and toxoplasmosis, we have selected quinolones as one component, given that selected examples exhibit exceptionally good activities against the causative pathogens of the foregoing diseases. The quinolone decoquinate (DQ), an old and inexpensive coccidiostat, displays anti-malarial activity in vitro against Plasmodium falciparum (Pf). However, because of its exceedingly poor solubility in water or organic solvents, development of DQ as a drug is problematical...
July 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27150250/cysteamine-broadly-improves-the-anti-plasmodial-activity-of-artemisinins-against-murine-blood-stage-and-cerebral-malaria
#18
Neda Moradin, Sabrina Torre, Susan Gauthier, Mifong Tam, Jalal Hawari, Kirsten Vandercruyssen, Bart De Spiegeleer, Anny Fortin, Mary M Stevenson, Philippe Gros
BACKGROUND: The potential emergence and spread of resistance to artemisinins in the Plasmodium falciparum malaria parasite constitutes a major global health threat. Hence, improving the efficacy of artemisinins and of artemisinin-based combination therapy (ACT) represents a major short-term goal in the global fight against malaria. Mice defective in the enzyme pantetheinase (Vnn3) show increased susceptibility to blood-stage malaria (increased parasitaemia, reduced survival), and supplementation of Vnn3 mutants with the reaction product of pantetheinase, cysteamine, corrects in part the malaria-susceptibility phenotype of the mutants...
2016: Malaria Journal
https://www.readbyqxmd.com/read/27128799/therapeutic-efficacy-of-artemether-lumefantrine-coartem%C3%A2-in-treating-uncomplicated-p-falciparum-malaria-in-metehara-eastern-ethiopia-regulatory-clinical-study
#19
Desalegn Nega, Ashenafi Assefa, Hussein Mohamed, Hiwot Solomon, Adugna Woyessa, Yibeltal Assefa, Amha Kebede, Moges Kassa
BACKGROUND: As per the WHO recommendation, the development of resistance by P. falciparum to most artemisinin combination therapies (ACTs) triggered the need for routine monitoring of the efficacy of the drugs every two years in all malaria endemic countries. Hence, this study was carried out to assess the therapeutic efficacy of Artemether-Lumefantrine (Coartem®) in treating the uncomplicated falciparum malaria, after 9 years of its introduction in the Metehara, Eastern Ethiopia. METHOD: This is part of the therapeutic efficacy studies by the Federal Ministry of Health Ethiopia, which were conducted in regionally representative sentinel sites in the country from October 2014 to January 2015...
2016: PloS One
https://www.readbyqxmd.com/read/27079849/rational-design-of-proteasome-inhibitors-as-antimalarial-drugs
#20
Camille Le Chapelain, Michael Groll
One life, two strategies: Crucial structural differences between the human and the Plasmodium falciparum proteasomes were recently identified. A combination of cryo-EM and functional characterization enabled the design of a selective antimalarial proteasome inhibitor that shows low toxicity in the host. When used with artemisinin, this ligand offers a new approach for the efficient treatment of malaria at all stages of the parasite lifecycle.
May 23, 2016: Angewandte Chemie
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