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Artemisinin

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https://www.readbyqxmd.com/read/28341405/synthesis-of-novel-c-9-carbon-substituted-derivatives-of-artemisinin
#1
Daniel Meyer, Toni Smeilus, Dimanthi Pliatsika, Farnoush Mousavizadeh, Athanassios Giannis
Several artemisinin derivatives carrying several groups (alkyl, hydroxyalkyl, allyl or azide) at position 9 have been synthesized starting from artemisinin via enolate formation and subsequent reaction with appropriate electrophiles.
March 14, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28340622/anti-plasmodial-activity-of-norcaesalpin-d-and-extracts-of-four-medicinal-plants-used-traditionally-for-treatment-of-malaria
#2
Ramadhani Selemani Omari Nondo, Mainen Julius Moshi, Paul Erasto, Pax Jessey Masimba, Francis Machumi, Abdul Waziri Kidukuli, Matthias Heydenreich, Denis Zofou
BACKGROUND: Malaria is an old life-threatening parasitic disease that is still affecting many people, mainly children living in sub-Saharan Africa. Availability of effective antimalarial drugs played a significant role in the treatment and control of malaria. However, recent information on the emergence of P. falciparum parasites resistant to one of the artemisinin-based combination therapies suggests the need for discovery of new drug molecules. Therefore, this study aimed to evaluate the antiplasmodial activity of extracts, fractions and isolated compound from medicinal plants traditionally used in the treatment of malaria in Tanzania...
March 24, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28336173/effects-of-artesunate-on-some-biochemical-parameters-in-pregnant-albino-wistar-rats-challenged-with-lethal-strain-plasmodium-berghei-nk65-appreciating-the-activities-of-artemisinin-drugs-on-key-pregnancy-hormone-balance
#3
Chinaka O Nwaehujor, Onyeka V Asuzu, Daniel D Nwibo, Obichukwu C Nwobi, Ihechiluru I Ezeigbo
In humans, malaria in pregnancy can cause serious maternal and foetal morbidity and in extreme untreated cases, foetal mortality occurs. The therapeutic approach to curbing this malaise is the administration of an effective and/or combinations of anti-malaria medicaments. Acute or chronic administration of some of these drugs, however, gives rise to some adverse medical conditions including reproductive dysfunction, especially in pregnancy. Studies aimed at the hormonal interplays following administration of these drugs in pregnancy have been limited due to too few appropriate animal models...
March 20, 2017: Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft Für Toxikologische Pathologie
https://www.readbyqxmd.com/read/28330254/enhanced-production-of-an-anti-malarial-compound-artesunate-by-hairy-root-cultures-and-phytochemical-analysis-of-artemisia-pallens-wall
#4
Zarna Pala, Vishnu Shukla, Anshu Alok, Subhash Kudale, Neetin Desai
Artemisinin and its derivatives are still one of the most effective drugs for the treatment of malaria. Artemisia pallens commonly known as Dhavanam, is an aromatic herb belonging to the family Asteraceae. Increasing the artemisinin content of A. pallens by genetic engineering would improve the availability of this much needed drug. In the present study, Agrobacterium rhizogenes (strain NCIM 5140) mediated genetic transformation of Artemisia pallens were carried out for hairy root induction. The effect of different media (Half MS, MS, MS along with BAP 0...
December 2016: 3 Biotech
https://www.readbyqxmd.com/read/28320794/innovative-public-private-partnership-to-target-subsidised-antimalarials-a-study-protocol-for-a-cluster-randomised-controlled-trial-to-evaluate-a-community-intervention-in-western-kenya
#5
Jeremiah Laktabai, Adriane Lesser, Alyssa Platt, Elisa Maffioli, Manoj Mohanan, Diana Menya, Wendy Prudhomme O'Meara, Elizabeth L Turner
INTRODUCTION: There are concerns of inappropriate use of subsidised antimalarials due to the large number of fevers treated in the informal sector with minimal access to diagnostic testing. Targeting antimalarial subsidies to confirmed malaria cases can lead to appropriate, effective therapy. There is evidence that community health volunteers (CHVs) can be trained to safely and correctly use rapid diagnostic tests (RDTs). This study seeks to evaluate the public health impact of targeted antimalarial subsidies delivered through a partnership between CHVs and the private retail sector...
March 20, 2017: BMJ Open
https://www.readbyqxmd.com/read/28319807/targeting-nf-kappa-b-signaling-by-artesunate-restores-sensitivity-of-castrate-resistant-prostate-cancer-cells-to-antiandrogens
#6
Jessica J Nunes, Swaroop K Pandey, Anjali Yadav, Sakshi Goel, Bushra Ateeq
Androgen deprivation therapy (ADT) is the most preferred treatment for men with metastatic prostate cancer (PCa). However, the disease eventually progresses and develops resistance to ADT in majority of the patients, leading to the emergence of metastatic castration-resistant prostate cancer (mCRPC). Here, we assessed artesunate (AS), an artemisinin derivative, for its anticancer properties and ability to alleviate resistance to androgen receptor (AR) antagonists. We have shown AS in combination with bicalutamide (Bic) attenuates the oncogenic properties of the castrate-resistant (PC3, 22RV1) and androgen-responsive (LNCaP) PCa cells...
March 16, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28319782/synthesis-and-antiplasmodial-activity-of-novel-indoleamide-derivatives-bearing-sulfonamide-and-triazole-pharmacophores
#7
N Devender, Sarika Gunjan, Renu Tripathi, Rama Pati Tripathi
Due to the recent reports of growing parasite resistance to artemisinins and other antimalarial drugs, development of new antimalarial chemotypes is an urgent priority. Here in, we report a novel series of adamantyl/cycloheptyl indoleamide derivatives bearing sulfonamide and triazole pharmacophores adopting different chemical modifications and evaluated them for antiplasmodial activity in vitro. Among all the indoleamides, compounds 22, 24, 26 and 30 with sulfonamide pharmacophore showed promising activity with IC50 of 1...
March 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28319724/interactions-between-tafenoquine-and-artemisinin-combination-therapy-partner-drug-in-asexual-and-sexual-stage-plasmodium-falciparum
#8
Karen Kemirembe, Mynthia Cabrera, Liwang Cui
The 8-aminoquinoline tafenoquine (TFQ), a primaquine derivative, is currently in late-stage clinical development for the radical cure of P. vivax. Here drug interactions between TFQ and chloroquine and six artemisinin-combination therapy (ACT) partner drugs in P. falciparum asexual stages and gametocytes were investigated. TFQ was mostly synergistic with the ACT-partner drugs in asexual parasites regardless of genetic backgrounds. However, at fixed ratios of 1:3, 1:1 and 3:1, TFQ only interacted synergistically with naphthoquine, pyronaridine and piperaquine in gametocytes...
March 11, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28318947/docking-synthesis-and-antimalarial-activity-of-novel-4-anilinoquinoline-derivatives
#9
Shilpa Vijayaraghavan, Supriya Mahajan
A series of 4-anilinoquinoline triazine derivatives were designed, synthesized and screened for in vivo antimalarial activity against a chloroquine-sensitive strain of Plasmodium berghei. The compounds were further subjected to in vitro antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum and β-haematin inhibition studies. All the compounds exhibited in vivo antimalarial activity better than that shown by the standard drug, chloroquine. Twelve out of fifteen compounds showed better inhibition than that of chloroquine against chloroquine-resistant W2 strain of Plasmodium falciparum...
March 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28315999/artesunate-protects-lps-induced-acute-lung-injury-by-inhibiting-tlr4-expression-and-inducing-nrf2-activation
#10
Deli Zhao, Jinling Zhang, Guangquan Xu, Qiushi Wang
Artesunate, a derivative of artemisinin, has been reported to have anti-inflammatory property. However, few studies showed the protective effects of artesunate on lung injury. In this study, we aimed to investigate the effects of artesunate on LPS-induced lung injury in mice. The mice were treated with artesunate 1 h before or after LPS treatment. The effects of artesunate on lung MPO activity and malondialdehyde (MDA) content were detected. The lung wet/dry radio and the numbers of inflammatory cells in BALF were also measured...
March 18, 2017: Inflammation
https://www.readbyqxmd.com/read/28302108/confirmation-of-plasmodium-falciparum-in-vitro-resistance-to-monodesethylamodiaquine-and-chloroquine-in-dakar-senegal-in-2015
#11
Silman Diawara, Marylin Madamet, Mame Bou Kounta, Gora Lo, Khalifa Ababacar Wade, Aminata Nakoulima, Raymond Bercion, Rémy Amalvict, Mamadou Wague Gueye, Bécaye Fall, Bakary Diatta, Bruno Pradines
BACKGROUND: In response to increasing resistance to anti-malarial drugs, Senegal adopted artemisinin-based combination therapy (ACT) as the first-line treatment for uncomplicated malaria in 2006. However, resistance of Plasmodium falciparum parasites to artemisinin derivatives, characterized by delayed parasite clearance after treatment with ACT or artesunate monotherapy, has recently emerged and rapidly spread in Southeast Asia. After 10 years of stability with rates ranging from 5.6 to 11...
March 16, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28299804/simultaneous-determination-of-piperaquine-and-its-n-oxidated-metabolite-in-rat-plasma-using-lc-ms-ms
#12
Huixiang Liu, Meitong Zang, Aijuan Yang, Jianbo Ji, Jie Xing
A sensitive and efficient liquid chromatography tandem mass spectrometry method was firstly developed and validated for the simultaneous determination of piperaquine (PQ) and its N-oxidated metabolite (PQ-M) in plasma. A simple protein precipitation procedure was used for sample preparation. Adequate chromatographic retention was achieved on a C18 column under gradient elution with acetonitrile and 2 mM aqueous ammonium acetate containing 0.15% formic acid and 0.05% trifluoroacetic acid. A triple-quadrupole mass spectrometer equipped with an electrospray source was set up in the positive ion mode and multiple reaction monitoring mode...
March 16, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28296396/seeking-the-elusive-long-acting-ozonide-discovery-of-artefenomel-oz439
#13
Ho Shin Kim, Jared T Hammill, R Kiplin Guy
The majority of frontline therapies for the treatment of malaria are combination drugs containing artemisinin (or its semisynthetic analogs), known as artemisinin combination therapies (ACTs). While generally efficacious, ACTs and the first generation fully synthetic ozonide, arterolane (OZ277, 1), suffer from rapid clearance requiring 3-day dosing regimens. Extensive structure-activity studies led to the discovery of a second-generation ozonide, artefenomel (OZ439, 2), which has overcome this limitation, maintaining the rapid onset of action and potent activity of the artemisinin derivatives while exhibiting greatly improved pharmacokinetics, low projected cost of goods, prophylactic activity, and the potential for a single dose cure...
March 15, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28295751/the-role-of-plant-derived-products-in-pancreatitis-experimental-and-clinical-evidence
#14
REVIEW
Pratibha Anchi, Amit Khurana, Swarna Bale, Chandraiah Godugu
Pancreatitis is a gastrointestinal disease with a worldwide sharp surge during the past decade. Pancreatitis includes acute and chronic subtypes, which are graded based on the amount of pancreatic inflammation. Phytoconstituents represent a promising class of therapeutic agents with wide acceptability not only based on folk practices but sound presence of pharmacological and molecular evidences. Growing research evidence indicates that different molecular mechanisms are involved in their protective effect. Many phytoremedies have been tried for the treatment of pancreatic injuries and have shown success in preclinical animal models of pancreatitis...
March 15, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28294491/an-efficient-chemoenzymatic-synthesis-of-dihydroartemisinic-aldehyde
#15
Melodi Demiray, Xiaoping Tang, Thomas Wirth, Juan A Faraldos, Rudolf K Allemann
Artemisinin from the plant Artemisia annua is the most potent pharmaceutical for the treatment of malaria. In the plant, the sesquiterpene cyclase amorphadiene synthase, a cytochrome-dependent CYP450, and an aldehyde reductase convert farnesyl diphosphate (FDP) into dihydroartemisinic aldehyde (DHAAl), which is a key intermediate in the biosynthesis of artemisinin and a semisynthetic precursor for its chemical synthesis. Here, we report a chemoenzymatic process that is able to deliver DHAAl using only the sesquiterpene synthase from a carefully designed hydroxylated FDP derivative...
March 13, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28294340/neuroprotective-effects-of-artemisinin-against-isoflurane-induced-cognitive-impairments-and-neuronal-cell-death-involve-jnk-erk1-2-signalling-and-improved-hippocampal-histone-acetylation-in-neonatal-rats
#16
Guang Xu, Yun-Li Huang, Ping-le Li, Hai-Ming Guo, Xue-Ping Han
OBJECTIVE: This study was performed to assess the effect of artemisinin against isoflurane-induced neuronal apoptosis and cognitive impairment in neonatal rats. METHODS: Artemisinin (50, 100 or 200 mg/kg b.wt/day; oral gavage) was administered to separate groups of neonatal rats starting from postnatal day 3 (P3) to postnatal day 21 (P21). On postnatal day 7 (P7), animals were exposed to inhalation anaesthetic isoflurane (0.75%) for 6 h. KEY FINDINGS: Neuronal apoptosis following anaesthetic exposure was significantly reduced by artemisinin...
March 12, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28294321/artesunate-inhibits-rankl-induced-osteoclastogenesis-and-bone-resorption-in-vitro-and-prevents-lps-induced-bone-loss-in-vivo
#17
Cheng-Ming Wei, Qian Liu, Fang-Ming Song, Xi-Xi Lin, Yi-Ji Su, Jiake Xu, Lin Huang, Shao-Hui Zong, Jin-Min Zhao
Osteoclasts are multinuclear giant cells responsible for bone resorption in lytic bone diseases such as osteoporosis, arthritis, periodontitis, and bone tumors. Due to the severe side-effects caused by the currently available drugs, a continuous search for novel bone-protective therapies is essential. Artesunate (Art), the water-soluble derivative of artemisinin has been investigated owing to its anti-malarial properties. However, its effects in osteoclastogenesis have not yet been reported. In this study, Art was shown to inhibit the nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis, the mRNA expression of osteoclastic-specific genes, and resorption pit formation in a dose-dependent manner in primary bone marrow-derived macrophages cells (BMMs)...
March 15, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28289248/antimalarial-drug-resistance-a-threat-to-malaria-elimination
#18
Didier Menard, Arjen Dondorp
Increasing antimalarial drug resistance once again threatens effective antimalarial drug treatment, malaria control, and elimination. Artemisinin combination therapies (ACTs) are first-line treatment for uncomplicated falciparum malaria in all endemic countries, yet partial resistance to artemisinins has emerged in the Greater Mekong Subregion. Concomitant emergence of partner drug resistance is now causing high ACT treatment failure rates in several areas. Genetic markers for artemisinin resistance and several of the partner drugs have been established, greatly facilitating surveillance...
March 13, 2017: Cold Spring Harbor Perspectives in Medicine
https://www.readbyqxmd.com/read/28289193/host-immunity-to-plasmodium-falciparum-and-the-assessment-of-emerging-artemisinin-resistance-in-a-multinational-cohort
#19
Ricardo Ataide, Elizabeth A Ashley, Rosanna Powell, Jo-Anne Chan, Michael J Malloy, Katherine O'Flaherty, Eizo Takashima, Christine Langer, Takafumi Tsuboi, Arjen M Dondorp, Nicholas P Day, Mehul Dhorda, Rick M Fairhurst, Pharath Lim, Chanaki Amaratunga, Sasithon Pukrittayakamee, Tran Tinh Hien, Ye Htut, Mayfong Mayxay, M Abul Faiz, James G Beeson, Francois Nosten, Julie A Simpson, Nicholas J White, Freya J I Fowkes
Artemisinin-resistant falciparum malaria, defined by a slow-clearance phenotype and the presence of kelch13 mutants, has emerged in the Greater Mekong Subregion. Naturally acquired immunity to malaria clears parasites independent of antimalarial drugs. We hypothesized that between- and within-population variations in host immunity influence parasite clearance after artemisinin treatment and the interpretation of emerging artemisinin resistance. Antibodies specific to 12 Plasmodium falciparum sporozoite and blood-stage antigens were determined in 959 patients (from 11 sites in Southeast Asia) participating in a multinational cohort study assessing parasite clearance half-life (PCt1/2) after artesunate treatment and kelch13 mutations...
March 13, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28289029/antimalarial-hybrid-molecules-a-close-reality-or-a-distant-dream
#20
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
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