keyword
MENU ▼
Read by QxMD icon Read
search

antimalarial activity

keyword
https://www.readbyqxmd.com/read/28543724/predicting-binding-modes-of-reversible-peptide-based-inhibitors-of-falcipain-2-consistent-with-structure-activity-relationships
#1
Jorge Enrique Hernández González, Lilian Hernández Alvarez, Pedro Geraldo Pascutti, Pedro Alberto Valiente
Falcipain-2 (FP-2) is a major hemoglobinase of Plasmodium falciparum, considered an important drug target for the development of antimalarials. A previous study reported a novel series of twenty reversible peptide-based inhibitors of FP-2. However, the lack of tridimensional structures of the complexes hinders further optimization strategies to enhance the inhibitory activity of the compounds. Here we report the prediction of the binding modes of the aforementioned inhibitors to FP-2. A computational approach combining previous knowledge on the determinants of binding to the enzyme, docking and post-docking refinement steps, is employed...
May 24, 2017: Proteins
https://www.readbyqxmd.com/read/28539720/comparison-of-ultrasound-assisted-extraction-and-dynamic-maceration-over-content-of-tagitinin-c-obtained-from-tithonia-diversifolia-hemsl-a-gray-leaves-using-factorial-design
#2
Aline M R Silva, Nayara L O Ferreira, Anselmo E Oliveira, Leonardo L Borges, Edemilson C Conceição
BACKGROUND: Tithonia diversifolia belongs to the Asteraceae family. The leaves of T. diversifolia have been studied lately because of the presence of tagitinin C. OBJECTIVE: Looking for an easy and inexpensive method to extract tagitinin C from T. diversifolia leaves, this work aims to conduct a screening to evaluate the influence of different experimental factors using the dynamic maceration and ultrasound-assisted extraction methods with 2(3) factorial design based on response surface methodology in enhancing this chemical marker extraction...
April 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28539634/the-plasmodium-pi-4-k-inhibitor-kdu691-selectively-inhibits-dihydroartemisinin-pretreated-plasmodium-falciparum-ring-stage-parasites
#3
L Dembele, X Ang, M Chavchich, G M C Bonamy, J J Selva, M Yi-Xiu Lim, C Bodenreider, B K S Yeung, F Nosten, B M Russell, M D Edstein, J Straimer, D A Fidock, T T Diagana, P Bifani
Malaria control and elimination are threatened by the emergence and spread of resistance to artemisinin-based combination therapies (ACTs). Experimental evidence suggests that when an artemisinin (ART)-sensitive (K13 wild-type) Plasmodium falciparum strain is exposed to ART derivatives such as dihydroartemisinin (DHA), a small population of the early ring-stage parasites can survive drug treatment by entering cell cycle arrest or dormancy. After drug removal, these parasites can resume growth. Dormancy has been hypothesized to be an adaptive physiological mechanism that has been linked to recrudescence of parasites after monotherapy with ART and, possibly contributes to ART resistance...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28537265/a-tetraoxane-based-antimalarial-drug-candidate-that-overcomes-pfk13-c580y-dependent-artemisinin-resistance
#4
Paul M O'Neill, Richard K Amewu, Susan A Charman, Sunil Sabbani, Nina F Gnädig, Judith Straimer, David A Fidock, Emma R Shore, Natalie L Roberts, Michael H-L Wong, W David Hong, Chandrakala Pidathala, Chris Riley, Ben Murphy, Ghaith Aljayyoussi, Francisco Javier Gamo, Laura Sanz, Janneth Rodrigues, Carolina Gonzalez Cortes, Esperanza Herreros, Iñigo Angulo-Barturén, María Belén Jiménez-Díaz, Santiago Ferrer Bazaga, María Santos Martínez-Martínez, Brice Campo, Raman Sharma, Eileen Ryan, David M Shackleford, Simon Campbell, Dennis A Smith, Grennady Wirjanata, Rintis Noviyanti, Ric N Price, Jutta Marfurt, Michael J Palmer, Ian M Copple, Amy E Mercer, Andrea Ruecker, Michael J Delves, Robert E Sinden, Peter Siegl, Jill Davies, Rosemary Rochford, Clemens H M Kocken, Anne-Marie Zeeman, Gemma L Nixon, Giancarlo A Biagini, Stephen A Ward
K13 gene mutations are a primary marker of artemisinin resistance in Plasmodium falciparum malaria that threatens the long-term clinical utility of artemisinin-based combination therapies, the cornerstone of modern day malaria treatment. Here we describe a multinational drug discovery programme that has delivered a synthetic tetraoxane-based molecule, E209, which meets key requirements of the Medicines for Malaria Venture drug candidate profiles. E209 has potent nanomolar inhibitory activity against multiple strains of P...
May 24, 2017: Nature Communications
https://www.readbyqxmd.com/read/28535698/effect-of-urolithins-on-oxidative-stress-of-colorectal-adenocarcinomacells-caco-2
#5
Milica Kojadinovic, Aleksandra Arsic, Gordana Petovic-Oggiano, Marija Gavrovic-Jankulovic, Marija Glibetic, Milica Popovic
Urolithins (UROs) are metabolites derived from ellagic acid (EA) and ellagitannins (ETs) by gut microbiota after consumption of different ETs. The health effects attributed to UROs are numerous and diverse, ranging from antimalarial properties to anticancer activities and regulation of gene expression. The aim of this work was at assessing the effect of URO-A; -B; -C; -D on the oxidative status of colon epithelium using as a model colorectal adenocarcinoma cell line (Caco-2). No significant cytotoxic effects of UROs was noted, with the applied treatments...
May 23, 2017: International Journal of Food Sciences and Nutrition
https://www.readbyqxmd.com/read/28531310/nascent-rna-sequencing-reveals-mechanisms-of-gene-regulation-in-the-human-malaria-parasite-plasmodium-falciparum
#6
Xueqing Maggie Lu, Gayani Batugedara, Michael Lee, Jacques Prudhomme, Evelien M Bunnik, Karine G Le Roch
Gene expression in Plasmodium falciparum is tightly regulated to ensure successful propagation of the parasite throughout its complex life cycle. The earliest transcriptomics studies in P. falciparum suggested a cascade of transcriptional activity over the course of the 48-hour intraerythrocytic developmental cycle (IDC); however, the just-in-time transcriptional model has recently been challenged by findings that show the importance of post-transcriptional regulation. To further explore the role of transcriptional regulation, we performed the first genome-wide nascent RNA profiling in P...
May 22, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28526807/dihydroartemisinin-induces-autophagy-dependent-death-in-human-tongue-squamous-cell-carcinoma-cells-through-dna-double-strand-break-mediated-oxidative-stress
#7
Xinli Shi, Li Wang, Xiaoming Li, Jing Bai, Jianchun Li, Shenghao Li, Zeming Wang, Mingrui Zhou
Dihydroartemisinin is an effective antimalarial agent with multiple biological activities. In the present investigation, we elucidated its therapeutic potential and working mechanism on human tongue squamous cell carcinoma (TSCC). It was demonstrated that dihydroartemisinin could significantly inhibit cell growth in a dose- and time-dependent manner by the Cell Counting Kit-8 and colony formation assay in vitro. Meanwhile, autophagy was promoted in the Cal-27 cells treated by dihydroartemisinin, evidenced by increased LC3B-II level, increased autophagosome formation, and increased Beclin-1 level compared to dihydroartemisinin-untreated cells...
April 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28526743/systematic-identification-of-functional-residues-of-artemisia-annua-amorpha-4-11-diene-synthase
#8
Xin Fang, Jian-Xu Li, Jin-Quan Huang, You-Li Xiao, Peng Zhang, Xiao-Ya Chen
Terpene synthases (TPSs) are responsible for the extremely diversified and complex structure of terpenoids. Amorpha-4,11-diene synthase (ADS) has a high (90%) fidelity in generating the sesquiterpene precursor for biosynthesis of artemisinin, an antimalarial drug, however, little is known about how active site residues of ADS involved in the carbocation rearrangement and cyclization reactions. Here, we identify seven residues that are key to most of the catalytic steps in ADS. By structural modeling and amino acid sequence alignments of ADS with two functionally relevant sesquiterpene synthases from Artemisia annua, we performed site-directed mutagenesis and found that a single substitution, T296V, impaired the ring closure activity almost completely, and tetra-substitutions (L374Y/L404V/L405I/G439S) led to an enzyme generating 80% monocyclic bisabolyl-type sesquiterpenes, whereas a double mutant (T399L/T447G) showed compromised activity in regioselective deprotonation to yield 34...
May 19, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28513586/hundreds-of-dual-stage-antimalarial-molecules-discovered-by-a-functional-gametocyte-screen
#9
Celia Miguel-Blanco, Irene Molina, Ana I Bardera, Beatriz Díaz, Laura de Las Heras, Sonia Lozano, Carolina González, Janneth Rodrigues, Michael J Delves, Andrea Ruecker, Gonzalo Colmenarejo, Sara Viera, María S Martínez-Martínez, Esther Fernández, Jake Baum, Robert E Sinden, Esperanza Herreros
Plasmodium falciparum stage V gametocytes are responsible for parasite transmission, and drugs targeting this stage are needed to support malaria elimination. We here screen the Tres Cantos Antimalarial Set (TCAMS) using the previously developed P. falciparum female gametocyte activation assay (Pf FGAA), which assesses stage V female gametocyte viability and functionality using Pfs25 expression. We identify over 400 compounds with activities <2 μM, chemically classified into 57 clusters and 33 singletons...
May 17, 2017: Nature Communications
https://www.readbyqxmd.com/read/28513196/synthesis-and-in-vivo-antimalarial-activity-of-novel-naphthoquine-derivatives-with-linear-cyclic-structured-pendants
#10
Ling Tang, Zhuchun Bei, Yabin Song, Likun Xu, Hong Wang, Dongna Zhang, Yuanyuan Dou, Kai Lv, Hongquan Wang
AIM: Naphthoquine (NQ) was discovered by our institute as an antimalarial candidate in 1980s, and currently employed as an artemisinin-based combination therapy partner drug. Resistance to NQ was found in mouse model in laboratory, and might emerge in future as widely used. METHODOLOGY: We herein report the design and synthesis of NQ derivatives by replacing t-butyl moiety with linear/cyclic structured pendants. All the target compounds 6a-l and intermediates 5a-h were tested for their in vivo antimalarial activity against Plasmodium berghei K173 strain in mice...
May 17, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28512990/luminescence-circular-dichroism-and-in-silico-studies-of-binding-interaction-of-synthesized-naphthylchalcone-derivatives-with-bovine-serum-albumin
#11
Sharda Pasricha, Deepti Sharma, Himanshu Ojha, Pragya Gahlot, Mallika Pathak, Mitra Basu, Raman Chawla, Sugandha Singhal, Anju Singh, Rajeev Goel, Shrikant Kukreti, Shefali Shukla
Chalcones possess various biological properties, for example, antimicrobial, anti-inflammatory, analgesic, antimalarial, anticancer, antiprotozoal and antitubercular activity. In this study, naphthylchalcone derivatives were synthesized and characterized using (1) H NMR (13) C NMR, Fourier transform infrared and mass techniques. Yields for all derivatives were found to be >90%. Protein-drug interactions influence the absorption, distribution, metabolism and excretion (ADME) properties of a drug. Therefore, to establish whether the synthesized naphthylchalcone derivatives can be used as drugs, their binding interaction toward a serum protein (bovine serum albumin) was investigated using fluorescence, circular dichroism and molecular docking techniques under physiological conditions...
May 16, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28512601/anti-nociceptive-and-anti-inflammatory-potentials-of-vernoniaamygdalina-leaf-extract-via-reductions-of-leucocyte-migration-and-lipid-peroxidation
#12
Samuel Adetunji Onasanwo, Oyetola Tolulope Oyebanjo, Abayomi Mayowa Ajayi, Mujeedat Adebukola Olubori
BACKGROUND: Vernonia amygdalina is well known as a medicinal plant in folk medicine as antidiabetic, anthelmintic, antimalarial, laxative/purgative, and expectorant among others. AIM: This study was conducted to investigate the antinociceptive and anti-inflammatory effects of V. amygdalina. MATERIALS AND METHODS: Methanol extract of V. amygdalina leaf (MEVA) was evaluated for antinociceptive effect and possible mechanisms of action in the presence of naloxone (1 mg/kg), atropine (2 mg/kg), and prazosin (1 mg/kg) using acetic acid writhing test in mice...
April 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28511056/elimination-of-schistosoma-mansoni-in-infected-mice-by-slow-release-of-artemisone
#13
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/28507328/pro-inflammatory-ca-activated-k-channels-are-inhibited-by-hydroxychloroquine
#14
María Eugenia Schroeder, Sofía Russo, Carlos Costa, Juliana Hori, Inés Tiscornia, Mariela Bollati-Fogolín, Darío S Zamboni, Gonzalo Ferreira, Ernesto Cairoli, Marcelo Hill
Antimalarials have demonstrated beneficial effects in Systemic Lupus Erithematosus and Rheumatoid Arthritis. However, the mechanisms and the molecular players targeted by these drugs remain obscure. Although hydroxychloroquine (HCQ) is a known ion channel inhibitor, this property has not been linked to its anti-inflammatory effects. We aimed to study whether HCQ inhibits pro-inflammatory ion channels. Electrophysiology experiments demonstrated that HCQ inhibited Ca(++)-activated K(+) conductance in THP-1 macrophages in a dose-dependent manner...
May 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28505410/new-prodigiosin-derivatives-obtained-by-mutasynthesis-in-pseudomonas-putida
#15
Andreas Sebastian Klein, Andreas Domröse, Patrick Bongen, Hannah U C Brass, Thomas Classen, Anita Loeschcke, Thomas Drepper, Luca Laraia, Sonja Sievers, Karl-Erich Jaeger, Jörg Pietruszka
The deeply red-colored natural compound prodigiosin is a representative of the prodiginine alkaloid family, which possesses bioactivities as antimicrobial, antitumor and antimalarial agents. Various bacteria including the opportunistic human pathogen Serratia marcescens and different members of the Streptomycetaceae and Pseudoalteromonadaceae produce prodiginines. In addition, these microbes generally accumulate many structurally related alkaloids making efficient prodiginine synthesis and purification difficult and expensive...
May 15, 2017: ACS Synthetic Biology
https://www.readbyqxmd.com/read/28502855/caesalpinia-bonduc-serine-proteinase-inhibitor-cbti-2-exploring-the-conformational-features-and-antimalarial-activity
#16
Arindam Bhattacharyya, C R Babu
Seeds of tropical legumes posses a repertoire of proteinase inhibitors (PI) and the current study highlights some structural/functional features of a strong serine PI from the seeds of Caesalpinia bonduc (CbTI-2). Following purification, N-terminal sequence of CbTI-2 revealed over 40% similarity with a few serine PIs of Caesalpinioideae subfamily. Upon exposure to metal ions and ionic/non ionic surfactants, CbTI-2 showed immense variation in the levels of antitryptic activity. Exposure of CbTI-2 to 1,4-Dithiothreitol, Guanidinium HCl, H2O2 and Dimethyl sulfoxide led to a steady loss of inhibitory activity...
May 11, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28502016/correlation-between-in-vitro-and-in-vivo-antimalarial-activity-of-compounds-using-cq-sensitive-and-cq-resistant-strains-of-plasmodium-falciparum-and-cq-resistant-strain-of-p-yoelii
#17
Kumkum Srivastava, Pooja Agarwal, Awakash Soni, S K Puri
Present efforts have been made to establish a correlation between in vitro and in vivo antimalarial activity using MIC, IC50 and IC90 values against CQ-sensitive (3D7) and CQ-resistant (K1) strains of Plasmodium falciparum and in vivo activity against Plasmodium yoelii. The method of discriminant function analysis (DFA) was applied to analyze the data. It was observed that in vitro IC90 values against both 3D7 and K1 strains (p < 0.001) have strong correlation with in vivo curative activity. The respective IC50 and IC90 values of compounds, which cured mice (i...
May 13, 2017: Parasitology Research
https://www.readbyqxmd.com/read/28499255/identification-of-an-aspidospermine-derivative-from-borage-extract-as-an-anti-amyloid-compound-a-possible-link-between-protein-aggregation-and-antimalarial-drugs
#18
Hamid R Kalhor, Hossein Ashrafian
A number of human diseases, including Alzheimer's and Parkinson's have been linked to amyloid formation. To search for an anti-amyloidogenic product, alkaloid enriched extract from borage leaves was examined for anti-amyloidogenic activity using Hen Egg White Lysozyme (HEWL) as a model protein. After isolation of the plant extract using rHPLC, only one fraction indicated a significant bioactivity. TEM analysis confirmed a remarkable reduction of amyloid fibrils in the presence of the bioactive fraction. To identify the effective substance in the fraction, mass spectrometry, FTIR, and NMR were performed...
May 9, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28498611/design-synthesis-and-biological-evaluation-of-peptidomimetic-n-substituted-cbz-4-hyp-hpa-amides-as-novel-inhibitors-of-plasmodium-falciparum
#19
Valeriy A Bacherikov, Amar G Chittiboyina, Mitchell A Avery
A new series of peptidomimetic N-substituted Cbz-4-Hyp-Hpa-amides was designed, synthesized and evaluated for inhibition of the Plasmodium falciparum. Substituents on the N atom of the amide group were selected. They are the following alkyl-, allyl-, aryl-, 2-hydroxyethyl-, 2-cyanoethyl-, cyanomethyl-, 2-hydroxyethyl-, 2,2-diethoxyethyl-, or 2-ethoxy-2-oxoethylamino groups, and about forty new compounds were synthesized and evaluated for anti-plasmodial activity in vitro. Antimalarial activity was investigated as for the final peptide mimetics, and their immediate predecessors, carrying TBDMS or TBDPS protecting groups on 4-hydroxyproline residue and eighteen derivatives exhibited toxicity against P...
May 12, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28496487/chemical-composition-and-biological-activities-of-methanolic-extract-of-scrophularia-oxysepala-boiss
#20
Ardalan Pasdaran, Abbas Delazar, Seyed Abdulmajid Ayatollahi, Arsalan Pasdaran
Isolated five known iridoids glycosides (Scrophuloside A, Harpagoside B, 5-hydroxyloganin, 8-O-acetylharpagide and 6-O-methyl,1-glucopyranosyl catalpol), one phenyl ethanoid glycoside (Verbascoside) and a phenyl ethanol amine (2-(4-Chlorobenzyl amino) ethanol) compound from the methanolic extract of aerial parts of Scrophularia oxysepala using by high performance liquid chromatographyare based on isocratic and liner gradients by C18 column. The structure elucidations of the isolated compounds were performed by spectroscopic methods including1H-NMR, 13C-NMR, 2 D NMR technique such as HMBC( in deuterated methanol as solvent), GC-MS and UV, also methanolic extract and fractions( fractionated on solid phase extraction on C18 cartridge(Spack-C18)) of this plant was tested for free radical scavenging properties toward the 1, 1-diphenyl-1-picrylhydrazyl (DPPH), general toxicity (Brine shrimp toxicity assay) , insecticidal ( Contact toxicity insecticidal assay) and antimalarial activities (hemebiocrystallization inhibition assay)...
2017: Iranian Journal of Pharmaceutical Research: IJPR
keyword
keyword
43150
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"