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antimalarial activity

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https://www.readbyqxmd.com/read/28728898/kbe009-an-antimalarial-bestatin-like-inhibitor-of-the-plasmodium-falciparum-m1-aminopeptidase-discovered-in-an-ugi-multicomponent-reaction-derived-peptidomimetic-library
#1
Jorge González-Bacerio, Sarah El Chamy Maluf, Yanira Méndez, Isel Pascual, Isabelle Florent, Pollyana M S Melo, Alexandre Budu, Juliana C Ferreira, Ernesto Moreno, Adriana K Carmona, Daniel G Rivera, Maday Alonso Del Rivero, Marcos L Gazarini
Malaria is a global human parasitic disease mainly caused by the protozoon Plasmodium falciparum. Increased parasite resistance to current drugs determines the relevance of finding new treatments against new targets. A novel target is the M1 alanyl-aminopeptidase from P. falciparum (PfA-M1), which is essential for parasite development in human erythrocytes and is inhibited by the pseudo-peptide bestatin. In this work, we used a combinatorial multicomponent approach to produce a library of peptidomimetics and screened it for the inhibition of recombinant PfA-M1 (rPfA-M1) and the in vitro growth of P...
July 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28726419/hitoyol-a-and-b-two-norsesquiterpenoids-from-the-basidiomycete-coprinopsis-cinerea
#2
Junnosuke Otaka, Daisuke Hashizume, Yui Masumoto, Atsuya Muranaka, Masanobu Uchiyama, Hiroyuki Koshino, Yushi Futamura, Hiroyuki Osada
Hitoyol A (1), an unprecedented norsesquiterpenoid with an exo-tricyclo[5.2.1.0(2,6)]decane skeleton, was isolated from the culture broth of Basidiomycete Coprinopsis cinerea along with a novel skeletal hitoyol B (2) containing 4-cyclopentene-1,3-dione. Their structures and absolute configurations were analyzed by single-crystal X-ray diffraction and electronic circular dichroism spectroscopic methods. Compound 1 is possibly biosynthesized through decarboxylation-induced cyclization of lagopodin B, a known cuparene-type sesquiterpenoid...
July 20, 2017: Organic Letters
https://www.readbyqxmd.com/read/28720134/in-vitro-antioxidant-and-antimalarial-activities-of-leaves-pods-and-bark-extracts-of-acacia-nilotica-l-del
#3
Muhammad Bilal Sadiq, Pattamon Tharaphan, Kesinee Chotivanich, Joel Tarning, Anil Kumar Anal
BACKGROUND: The emergence of drug resistant malaria is threatening our ability to treat and control malaria in the Southeast Asian region. There is an urgent need to develop novel and chemically diverse antimalarial drugs. This study aimed at evaluating the antimalarial and antioxidant potentials of Acacia nilotica plant extracts. METHODS: The antioxidant activities of leaves, pods and bark extracts were determined by standard antioxidant assays; reducing power capacity, % lipid peroxidation inhibition and ferric reducing antioxidant power assay...
July 18, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28719180/heterologous-expression-purification-and-functional-analysis-of-plasmodium-falciparum-phosphatidylinositol-3-kinase
#4
Matthew Hassett, Anna Sternberg, Bryce Riegel, Craig J Thomas, Paul David Roepe
The Plasmodium falciparum malarial parasite genome appears to encode one and only one phosphatidylinositol 3'-kinase (PI3K) and sequence analysis suggests that the enzyme is a "class III" or "Vps34" type PI3K. The PfVps34 has generated excitement as a possible druggable target and potentially a key target of artemisinin-based antimalarials. In this study, we optimize the PfVps34 gene for heterologous expression in yeast, purify the protein to homogeneity, use a recently validated quantitative assay for phosphatidylinositol 3'-phosphate (PI3P) production from phosphatidylinositol (PI) (Hassett et al...
July 18, 2017: Biochemistry
https://www.readbyqxmd.com/read/28714383/novel-mannich-bases-as-potential-anticonvulsants-syntheses-characterization-and-biological-evaluation
#5
Amit Kumar Keshari, Aseem Tewari, Shweta Singh Verma, Shailendra K Saraf
BACKGROUND: Mannich bases are known to be an important pharmacophore or bioactive leads in the synthesis of various potential agents that have a variety of therapeutic activities like anticancer, antipsychotic, anticonvulsant, antimalarial, anti-inflammatory, antibacterial and so forth. Thus, in the present research, conjugation of moieties like 1,5-benzoxazepines and 1,5-benzothiazepines with secondary amines like piperazine, methyl piperazine and morpholine was carried out in a Mannich base with an anticipation of good anticonvulsant activity...
July 17, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28712788/antimalarial-agent-artesunate-protects-concanavalin-a-induced-autoimmune-hepatitis-in-mice-by-inhibiting-inflammatory-responses
#6
Xin Zhao, MingJiang Liu, JinGui Li, ShaoJie Yin, YangYang Wu, AnYuan Wang
The anti-malarial drug artesunate (ARS) has been shown to possess anti-inflammatory activity. Its effect on autoimmune hepatitis remains unclear. Concanavalin A (Con A)-induced hepatitis was used in this study to reveal the potential action of ARS and the related mechanism. Mice were pretreated with ARS followed by Con A challenge. Con A caused obvious hepatic injury with higher levels of liver enzymes, elevated pro-inflammatory cytokines and activation of nuclear factor-κB (NF-κB) and mitogen activated protein kinase (MAPK) signaling pathways...
July 13, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28709400/broad-range-potential-of-asphodelus-microcarpus-leaves-extract-for-drug-development
#7
Amalia Di Petrillo, Antonella Fais, Francesca Pintus, Celestino Santos-Buelga, Ana M González-Paramás, Vincenzo Piras, Germano Orrù, Antonello Mameli, Enzo Tramontano, Aldo Frau
BACKGROUND: Many plants have been used in traditional medicine for their antibacterial, antifungal, antiprotozoal, antiviral, antidiarrhoeal, analgesic, antimalarial, antioxidant, anti-inflammatory and anticancer activities. In order to find novel antimicrobial and antiviral agents, the aim of the present study was the evaluation of the antibacterial and antibiofilm susceptibility of Asphodelus microcarpus leaves extract. Moreover, the antiviral activity and the phytochemical composition of the active extract were also determined...
July 14, 2017: BMC Microbiology
https://www.readbyqxmd.com/read/28708672/artemisinin-disrupts-androgen-responsiveness-of-human-prostate-cancer-cells-by-stimulating-the-26s-proteasome-mediated-degradation-of-the-androgen-receptor-protein
#8
Andrea M Steely, Jamin A Willoughby, Shyam N Sundar, Vasiliki I Aivaliotis, Gary L Firestone
Androgen receptor (AR) expression and activity is highly linked to the development and progression of prostate cancer and is a target of therapeutic strategies for this disease. We investigated whether the antimalarial drug artemisinin, which is a sesquiterpene lactone isolated from the sweet wormwood plant Artemisia annua, could alter AR expression and responsiveness in cultured human prostate cancer cell lines. Artemisinin treatment induced the 26S proteasome-mediated degradation of the receptor protein, without altering AR transcript levels, in androgen-responsive LNCaP prostate cancer cells or PC-3 prostate cancer cells expressing exogenous wild-type AR...
July 13, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28696697/development-of-a-potent-inhibitor-of-the-plasmodium-proteasome-with-reduced-mammalian-toxicity
#9
Gregory M LaMonte, Jehad Almaliti, Betsaida Bibo-Verdugo, Lena Keller, Bing Yu Zou, Jennifer Yang, Yevgeniya Antonova-Koch, Pamela Orjuela-Sanchez, Colleen A Boyle, Edgar Vigil, Lawrence Wang, Gregory M Goldgof, Lena Gerwick, Anthony J O'Donoghue, Elizabeth A Winzeler, William H Gerwick, Sabine Ottilie
Naturally derived chemical compounds are the foundation of much of our pharmacopeia, especially in anti-proliferative and anti-infective drug classes. Here, we report that a naturally-derived molecule called carmaphycin B, is a potent inhibitor against both the asexual and sexual blood stages of malaria infection. Using a combination of in silico molecular docking and in vitro directed evolution in a well-characterized drug-sensitive yeast model, we determined that these compounds target the β5 subunit of the proteasome...
July 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28694749/variability-of-antioxidant-and-biological-activities-of-rhus-tripartitum-related-to-phenolic-compounds
#10
Hanène Ben Miled, Mariem Saada, Ines Jallali, Zaineb Ben Barka, Mounira Tlili, Hichem Alimi, Mohsen Sakly, Khémais Ben Rhouma, Manef Abderrabba, Hafedh Abdelmelek, Olfa Tebourbi, Riadh Ksouri
Rhus species are known in traditional medicine for their therapeutic virtue and their extracts showed numerous important properties including antimalarial, antimicrobial, antiviral, and hypoglycemic and anticonvulsant activities. Rhus tripartitum (Ucria) is a medicinal plant widely used in Tunisia folk medicine against chronic diarrhea and gastric ulcer. This study was designed to examine in vitro and ex vivo antioxidant, anti-inflammatory and anticancer activities of four extracts of Rhus tripartitum root cortex with increasing solvent polarity (hexane, dichloromethane, methanol and water)...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28692297/enantioselective-synthesis-and-in-vivo-evaluation-of-regioisomeric-analogues-of-the-antimalarial-arterolane
#11
Brian R Blank, Jiri Gut, Philip J Rosenthal, Adam R Renslo
We describe the first systematic study of antimalarial 1,2,4-trioxolanes bearing a substitution pattern regioisomeric to that of arterolane. Conformational analysis suggested that trans-3″-substituted trioxolanes would exhibit Fe(II) reactivity and antiparasitic activity similar to that achieved with canonical cis-4″ substitution. The chiral 3″ analogues were prepared as single stereoisomers and evaluated alongside their 4″ congeners against cultured malaria parasites and in a murine malaria model. As predicted, the trans-3″ analogues exhibited in vitro antiplasmodial activity remarkably similar to that of their cis-4″ comparators...
July 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28689867/ex-vivo-activity-of-proveblue-a-methylene-blue-against-field-isolates-of-plasmodium-falciparum-in-dakar-senegal-from-2013-2015
#12
Bécaye Fall, Marylin Madamet, Silman Diawara, Sébastien Briolant, Khalifa Ababacar Wade, Gora Lo, Aminata Nakoulima, Mansour Fall, Raymond Bercion, Mame Bou Kounta, Rémi Amalvict, Nicolas Benoit, Mamadou Wague Gueye, Bakary Diatta, Boubacar Wade, Bruno Pradines
Resistance to most antimalarial drugs has spread from Southeast Asia to Africa. Accordingly, new therapies to use with artemisinin-based combination therapy (triple ACT) are urgently needed. Proveblue, a methylene blue preparation, was found to exhibit antimalarial activity against Plasmodium falciparum strains in vitro. Proveblue has synergistic effects when used in combination with dihydroartemisinin, and has been shown to significantly reduce or prevent cerebral malaria in mice. The objectives of the current study were to evaluate the in vitro baseline susceptibility of clinical field isolates to Proveblue, compare its activity with that of other standard antimalarial drugs and define the patterns of cross-susceptibility between Proveblue and conventional antimalarial drugs...
July 6, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28689414/the-effects-of-quinoline-and-non-quinoline-inhibitors-on-the-kinetics-of-lipid-mediated-%C3%AE-hematin-crystallization
#13
Sharne-Mare Fitzroy, Johandie Gildenhuys, Tania Olivier, Ndivhuwo Olga Tshililo, David Kuter, Katherine Allison de Villiers
The throughput of a biomimetic lipid-mediated assay used to investigate the effects of inhibitors on the kinetics of β-hematin formation has been optimized through the use of 24-well microplates. The rate constant for β-hematin formation mediated by monopalmitoyl-rac-glycerol was reduced from 0.17 ± 0.04 min-1 previously measured in Falcon tubes to 0.019 ± 0.002 min-1 in the optimized assay. While this necessitated longer incubation times, transferring aliquots from multiple 24-well plates to a single 96-well plate for final absorbance measurements actually improved the overall turnaround time per inhibitor...
July 10, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28676003/synthesis-structural-characterization-and-antinociceptive-activities-of-new-arylated-quinolines-via-suzuki-miyaura-cross-coupling-reaction
#14
Malik Aman Ullah, Muhammad Adeel, Muhammad N Tahir, Abdur Rauf, Muhammad Akram, Taibi Ben Hadda, Yahia N Mabkhot, Naveed Muhammad, Fehmida Naseer, Mohammad S Mubarak
Backgorund: The quinoline ring system is one of the most commonly encountered heterocycles in medicinal chemistry, due to the pharmaceutical and medicinal uses of derivatives containing this ring. These quinoline-based compounds have remarkable biological activity, as they are employed as antimalarial, antibacterial, antifungal, and antitumor agents. The quinoline nucleus can be synthesized by various traditional methods such as the Skraup reaction, Friedlaender synthesis, Combes quinoline synthesis, Larock quinoline synthesis, among others...
July 4, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28674030/s-nitrosoglutathione-reductase-gsnor-deficiency-confers-improved-survival-and-neurological-outcome-in-experimental-cerebral-malaria
#15
Robyn E Elphinstone, Rickvinder Besla, Eric A Shikatani, Ziyue Lu, Alfred Hausladen, Matthew Davies, Clinton S Robbins, Mansoor Husain, Jonathan S Stamler, Kevin C Kain
Artesunate remains the mainstay of treatment for cerebral malaria, but is less effective in later stages of disease when the host inflammatory response and blood brain barrier integrity dictate clinical outcomes. Nitric oxide (NO) is an important regulator of inflammation and microvascular integrity, and impaired NO bioactivity is associated with fatal outcomes in malaria. Endogenous NO bioactivity in mammals is largely mediated by S-nitrosothiols (SNOs). Based on these observations, we hypothesized that animals deficient in the SNO-metabolizing enzyme, S-nitrosoglutathione (GSNO) reductase (GSNOR), which exhibit enhanced S-nitrosylation, would have improved outcomes in a preclinical model of cerebral malaria...
July 3, 2017: Infection and Immunity
https://www.readbyqxmd.com/read/28669839/optimal-antimalarial-dose-regimens-for-chloroquine-in-pregnancy-based-on-population-pharmacokinetic-modelling
#16
Sam Salman, Francesca Baiwog, Madhu Page-Sharp, Kay Kose, Harin A Karunajeewa, Ivo Mueller, Stephen J Rogerson, Peter M Siba, Kenneth F Ilett, Timothy M E Davis
Despite extensive use and accumulated evidence of safety, there have been few pharmacokinetic studies from which appropriate chloroquine (CQ) dose regimens could be developed specifically for pregnant women. Such optimized CQ-based regimens, used as treatment for acute malaria or as intermittent preventive treatment in pregnancy (IPTp), may have a valuable role if parasite CQ sensitivity returns following reduced drug pressure. In this study, population pharmacokinetic-pharmacodynamic modelling was used to simultaneously analyze plasma concentration-time data for CQ and its active metabolite desethylchloroquine (DCQ) in 44 non-pregnant and 45 pregnant Papua New Guinean women treated with CQ and sulfadoxine-pyrimethamine (SP) or azithromycin (AZI)...
June 29, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28668681/targeting-the-active-sites-of-malarial-proteases-for-antimalarial-drug-discovery-approaches-progress-and-challenges
#17
REVIEW
Kuldeep K Roy
Malaria is an infectious disease causing huge mortality and morbidity worldwide. Although antimalarial drugs are effective in several parts of the world, there is a serious threat to malaria control that malaria parasites are continuously developing widespread resistance against currently available antimalarial drugs, including artemisinin. Such widespread antimalarial drug resistance certifies the need of improving the efficacy of existing or new drugs, and developing alternative treatments through the identification of novel drug targets and development of candidate drugs...
June 28, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28662593/isolation-and-structure-elucidation-of-halymeniaol-a-new-antimalarial-sterol-derivative-from-the-red-alga-halymenia-floresii
#18
Srinu Meesala, Pratima Gurung, Krishanpal Karmodiya, Parameswaran Subrayan, Milind G Watve
A new mono-hydroxy acetylated sterol derivative: 12β-hydroxy-3β, 15α, 16β-triacetoxy-cholest-5-en-7-one (halymeniaol) (1), and cholesterol (2) were isolated from the marine red alga Halymenia floresii. The structure of the compound 1 (halymeniaol) was established from its spectral data, derived from HRMS/MS and 2D NMR. Compound 1 exhibited growth inhibitory activity against chloroquine-resistant Plasmodium falciparum 3D7 strain with an IC50 of 3.0 μM.
June 29, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28659034/a-review-on-annona-squamosa-l-phytochemicals-and-biological-activities
#19
Chengyao Ma, Yayun Chen, Jianwei Chen, Xiang Li, Yong Chen
Annona squamosa L. (Annonaceae) is a fruit tree with a long history of traditional uses. A. squamosa is an evergreen plant mainly located in tropical and subtropical regions. Srikayas, the fruits of A. squamosa, are extensively used to prepare candies, ice creams and beverages. A wide range of ethno-medicinal uses has been related to different portions of A. squamosa, such as tonic, apophlegmatisant, cool medicine, abortient and heart sedative. Numerous research projects on A. squamosa have found that it has anticancer, anti-oxidant, antidiabetic, antihypertensive, hepatoprotective, antiparasitic, antimalarial, insecticidal, microbicidel and molluscicidal activities...
June 28, 2017: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/28655583/evaluation-of-the-inhibitory-effect-of-n-acetyl-l-cysteine-on-babesia-and-theileria-parasites
#20
Mohamed Abdo Rizk, Shimaa Abd El-Salam El-Sayed, Mahmoud AbouLaila, Naoaki Yokoyama, Ikuo Igarashi
N-acetyl-L-cysteine is known to have antibacterial, antiviral, antimalarial, and antioxidant activities. Therefore, the in vitro inhibitory effect of this hit was evaluated in the present study on the growth of Babesia and Theileria parasites. The in vitro growth of Babesia bovis, Babesia bigemina, Babesia divergens, Theileria equi, and Babesia caballi that were tested was significantly inhibited (P < 0.05) by micromolar concentrations of N-acetyl-L-cysteine. The inhibitory effect of N-acetyl-L-cysteine was synergistically potentiated when used in combination with diminazene aceturate on B...
June 24, 2017: Experimental Parasitology
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