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https://www.readbyqxmd.com/read/28804611/antimalarial-evaluation-of-selected-medicinal-plant-extracts-used-in-iranian-traditional-medicine
#1
Mohammad Hossein Feiz Haddad, Hamidreza Mahbodfar, Zahra Zamani, Ali Ramazani
OBJECTIVES: In an attempt to discover new natural active extracts against malaria parasites, the present study evaluated the antiplasmodial properties of selected plants based on Iranian traditional medicine. MATERIALS AND METHODS: Ten plant species found in Iran were selected and collected based on the available literature about the Iranian traditional medicine. The methanolic extracts of these plants were investigated for in vitro antimalarial properties against chloroquine-sensitive (3D7) and multi-drug resistant (K1) strains of Plasmodium falciparum...
April 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28797031/regulation-of-hypoxia-induced-autophagy-in-glioblastoma-involves-atg9a
#2
Siti Aminah Abdul Rahim, Anne Dirkse, Anais Oudin, Anne Schuster, Jill Bohler, Vanessa Barthelemy, Arnaud Muller, Laurent Vallar, Bassam Janji, Anna Golebiewska, Simone P Niclou
BACKGROUND: Hypoxia is negatively associated with glioblastoma (GBM) patient survival and contributes to tumour resistance. Anti-angiogenic therapy in GBM further increases hypoxia and activates survival pathways. The aim of this study was to determine the role of hypoxia-induced autophagy in GBM. METHODS: Pharmacological inhibition of autophagy was applied in combination with bevacizumab in GBM patient-derived xenografts (PDXs). Sensitivity towards inhibitors was further tested in vitro under normoxia and hypoxia, followed by transcriptomic analysis...
August 10, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28774427/synthesis-of-antimalarial-amide-analogues-based-on-the-plant-serrulatane-diterpenoid-3-7-8-trihydroxyserrulat-14-en-19-oic-acid
#3
Rohitesh Kumar, Sandra Duffy, Vicky M Avery, Rohan A Davis
A plant-derived natural product scaffold, 3,7,8-trihydroxyserrulat-14-en-19-oic acid (1) was isolated in high yield from the aerial parts of the endemic Australian desert plant Eremophila microtheca. This scaffold (1) was subsequently used in the generation of a series of new amide analogues via a one-pot mixed anhydride amidation using pivaloyl chloride. The structures of all analogues were characterized using MS, NMR, and UV data. The major serrulatane natural products (1-3), isolated from the plant extract, and all amide analogues (6-15) together with several pivaloylated derivatives of 3,7,8-trihydroxyserrulat-14-en-19-oic acid (16-18) were evaluated for their antimalarial activity against 3D7 (chloroquine sensitive) and Dd2 (chloroquine resistant) Plasmodium falciparum strains, and preliminary cytotoxicity data were also acquired using the human embryonic kidney cell line HEK293...
July 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28772211/autophagy-as-a-potential-therapeutic-target-during-epithelial-to-mesenchymal-transition-in-renal-cell-carcinoma-an-in-vitro-study
#4
Mamta Singla, Shalmoli Bhattacharyya
Cancer progression toward invasive and metastatic disease is aided by reactivation of epithelial-mesenchymal transition (EMT), involving transdifferentiation of epithelial cells into mesenchymal phenotype. This leads to increased migratory and stem cell-like features in the cells. These EMT cells are more resistant to chemotherapy and it is hypothesized that the phenomenon of autophagy induces resistance, providing a survival strategy for cells. In the present study, we induced EMT-like phenotype in renal carcinoma cells and identified corresponding higher autophagy flux in these cells...
July 31, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28768767/iron-is-a-substrate-of-the-plasmodium-falciparum-chloroquine-resistance-transporter-pfcrt-in-xenopus-oocytes
#5
Naziha Bakouh, Sebastiano Bellanca, Britta Nyboer, Sonia Moliner Cubel, Zoubida Karim, Cecilia P Sanchez, Wilfred D Stein, Gabrielle Planelles, Michael Lanzer
The chloroquine resistance transporter of the human malaria parasite Plasmodium falciparum, PfCRT, is an important determinant of resistance to several quinoline and quinoline-like antimalarial drugs. PfCRT also plays an essential role in the physiology of the parasite during development inside erythrocytes. However, the function of this transporter besides its role in drug resistance is still unclear. Using electrophysiological and flux experiments conducted on PfCRTexpressing Xenopus laevis oocytes, we show here that both wild type PfCRT and a PfCRT variant associated with chloroquine resistance transport both ferrous and ferric iron, albeit with different kinetics...
August 2, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28763644/norepinephrine-alkaloids-as-antiplasmodial-agents-synthesis-of-syncarpamide-and-insight-into-the-structure-activity-relationships-of-its-analogues-as-antiplasmodial-agents
#6
Eswar K Aratikatla, Tushar R Valkute, Sunil K Puri, Kumkum Srivastava, Asish K Bhattacharya
Syncarpamide 1, a norepinephrine alkaloid isolated from the leaves of Zanthoxylum syncarpum (Rutaceae) exhibited promising antiplasmodial activities against Plasmodium falciparum with reported IC50 values of 2.04 μM (D6 clone), 3.06 μM (W2 clone) and observed by us 3.90 μM (3D7 clone) and 2.56 μM (K1 clone). In continuation of our work on naturally occurring antimalarial compounds, synthesis of syncarpamide 1 and its enantiomer, (R)-2 using Sharpless asymmetric dihydroxylation as a key step has been accomplished...
July 25, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28759800/mesenchymal-stem-cells-derived-from-multiple-myeloma-patients-protect-against-chemotherapy-through-autophagy-dependent-activation-of-nf-%C3%AE%C2%BAb-signaling
#7
HongLiang Yang, YingChun Zheng, YiZhuo Zhang, Zeng Cao, Yingzhe Jiang
Chemotherapy resistance has been considered as a major problem for multiple myeloma (MM) treatment and bone marrow microenvironment plays a crucial role in the MM progression and chemoresistance. Recent studies reported that bone marrow mesenchymal stem cells derived from MM patients (MM-MSCs) revealed various characteristics compared with these from healthy subjects (NM-MSCs). However, the functions and mechanisms by which MM-MSCs mediate the chemotherapy resistance of MM remain unclear. In this study, we show that MM-MSCs decreased melphalan or doxorubicin-induced cell cycle arrest and apoptosis in two MM cell lines (U266 and RPMI-8226)...
July 25, 2017: Leukemia Research
https://www.readbyqxmd.com/read/28759591/genome-wide-diversity-and-differentiation-in-new-world-populations-of-the-human-malaria-parasite-plasmodium-vivax
#8
Thais C de Oliveira, Priscila T Rodrigues, Maria José Menezes, Raquel M Gonçalves-Lopes, Melissa S Bastos, Nathália F Lima, Susana Barbosa, Alexandra L Gerber, Guilherme Loss de Morais, Luisa Berná, Jody Phelan, Carlos Robello, Ana Tereza R de Vasconcelos, João Marcelo P Alves, Marcelo U Ferreira
BACKGROUND: The Americas were the last continent colonized by humans carrying malaria parasites. Plasmodium falciparum from the New World shows very little genetic diversity and greater linkage disequilibrium, compared with its African counterparts, and is clearly subdivided into local, highly divergent populations. However, limited available data have revealed extensive genetic diversity in American populations of another major human malaria parasite, P. vivax. METHODS: We used an improved sample preparation strategy and next-generation sequencing to characterize 9 high-quality P...
July 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28757774/prevalence-risk-factors-and-antimalarial-resistance-patterns-of-falciparum-plasmodiasis-among-pregnant-women-in-kaduna-metropolis-nigeria
#9
Maryam Muhammad Aliyu, Idris Abdullahi Nasir, Yahaya Abdullahi Umar, Anthony Philip Vanstawa, Jessy Thomas Medugu, Anthony Uchenna Emeribe, Dele Ohinoyi Amadu
OBJECTIVE: Pregnant women infected with malaria represent a significant obstetric problem, especially in the face of antimalarial resistance. This cross-sectional study investigated the prevalence of malaria parasitemia, associated risk factors as well as the antimalarial resistance pattern of Plasmodium isolates from pregnant women attending four selected secondary health facilities in Kaduna State, Nigeria. MATERIALS AND METHODS: Blood samples were collected from 353 pregnant women attending selected hospitals...
April 2017: Ci Ji Yi Xue za Zhi, Tzu-chi Medical Journal
https://www.readbyqxmd.com/read/28756265/4-aminoquinoline-chalcone-n-acetylpyrazoline-conjugates-synthesis-and-antiplasmodial-evaluation
#10
Sumit Kumar, Anu Saini, Jiri Gut, Philip J Rosenthal, Raghu Raj, Vipan Kumar
1H-1,2,3-triazole linked 4-aminoquinoline-chalcone/-N-acetylpyrazoline conjugates were synthesized and evaluated against cultured chloroquine (CQ) resistant strain. Antiplasmodial activities of the synthesized conjugates revealed dependence of activity on the length of the alkyl chain as well as on the presence of methoxy substituents on ring A/ring B of the chalcone. The most potent and non-cytotoxic conjugate showed comparable antiplasmodial activity with that of CQ, with an IC50 value of 53.7 nM.
July 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28753653/induction-of-sphk1-activity-in-obese-adipose-tissue-macrophages-promotes-survival
#11
Tanit L Gabriel, Mina Mirzaian, Berend Hooibrink, Roelof Ottenhoff, Cindy van Roomen, Johannes M F G Aerts, Marco van Eijk
During obesity, adipose tissue macrophages (ATM) are increased in concert with local inflammation and insulin resistance. Since the levels of sphingolipid (SLs) in adipose tissue (AT) are altered during obesity we investigated the potential impact of SLs on ATMs. For this, we first analyzed expression of SL metabolizing genes in ATMs isolated from obese mice. A marked induction of sphingosine kinase 1 (Sphk1) expression was observed in obese ATM when compared to lean ATM. This induction was observed in both MGL-ve (M1) and MGL1+ve (M2) macrophages from obese WAT...
2017: PloS One
https://www.readbyqxmd.com/read/28753578/autophagy-suppression-potentiates-the-anti-glioblastoma-effect-of-asparaginase-in-vitro-and-in-vivo
#12
Qicheng Chen, Li Ye, Jiajun Fan, Xuyao Zhang, Huan Wang, Siyang Liao, Ping Song, Ziyu Wang, Shaofei Wang, Yubin Li, Jingyun Luan, Yichen Wang, Wei Chen, Wenjing Zai, Ping Yang, Zhonglian Cao, Dianwen Ju
Asparaginase has been reported to be effective in the treatment of various leukemia and several malignant solid cancers. However, the anti-tumor effect of asparaginase is always restricted due to complicated mechanisms. Herein, we investigated the mechanisms of how glioblastoma resisted asparaginase treatment and reported a novel approach to enhance the anti-glioblastoma effect of asparaginase. We found that asparaginase could induce growth inhibition and caspase-dependent apoptosis in U87MG/U251MG glioblastoma cells...
July 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/28749761/molecular-characterization-of-a-cluster-of-imported-malaria-cases-in-puerto-rico
#13
Stella M Chenet, Luciana Silva-Flannery, Naomi W Lucchi, Ljolje Dragan, Emilio Dirlikov, Kimberly Mace, Brenda Rivera-García, Paul M Arguin, Venkatachalam Udhayakumar
The Caribbean island of Hispaniola is targeted for malaria elimination. Currently, this is the only island with ongoing transmission of malaria in the Caribbean. In 2015, six patients from Puerto Rico and one from Massachusetts, who traveled to Punta Cana, Dominican Republic, were confirmed to be infected with Plasmodium falciparum. Additional molecular analysis was performed at the Centers for Disease Control and Prevention to characterize the drug-resistant alleles and Plasmodium population genetic markers...
July 24, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28748174/antiplasmodial-activity-and-cytotoxicity-of-ethanol-extract-of-zea-mays-root
#14
Jude Efiom Okokon, Bassey Sunday Antia, Bala Adamu Azare, Patience Jude Okokon
OBJECTIVE: Zea mays root decoction that has been traditionally used for the treatment of malaria by various tribes in Nigeria, was evaluated for antimalarial potential against malaria parasites using in vivo and in vitro models. MATERIALS AND METHODS: The root extract of Zea mays was investigated for antimalarial activity against Plasmodium berghei in mice using rodent malaria models; suppressive, prophylactic and curative tests and in vitro antiplasmodial activity against chloroquine-sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using SYBR green assay method...
May 2017: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/28747223/return-of-chloroquine-sensitivity-to-africa-surveillance-of-african-plasmodium-falciparum-chloroquine-resistance-through-malaria-imported-to-china
#15
Feng Lu, Meihua Zhang, Richard L Culleton, Sui Xu, Jianxia Tang, Huayun Zhou, Guoding Zhu, Yaping Gu, Chao Zhang, Yaobao Liu, Weiming Wang, Yuanyuan Cao, Julin Li, Xinlong He, Jun Cao, Qi Gao
BACKGROUND: Chloroquine (CQ) was the cornerstone of anti-malarial treatment in Africa for almost 50 years, but has been widely withdrawn due to the emergence and spread of resistance. Recent reports have suggested that CQ-susceptibility may return following the cessation of CQ usage. Here, we monitor CQ sensitivity and determine the prevalence of genetic polymorphisms in the CQ resistance transporter gene (pfcrt) of Plasmodium falciparum isolates recently imported from Africa to China...
July 26, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28746333/transmission-dynamics-of-co-endemic-plasmodium-vivax-and-p-falciparum-in-ethiopia-and-prevalence-of-antimalarial-resistant-genotypes
#16
Eugenia Lo, Elizabeth Hemming-Schroeder, Delenasaw Yewhalaw, Jennifer Nguyen, Estifanos Kebede, Endalew Zemene, Sisay Getachew, Kora Tushune, Daibin Zhong, Guofa Zhou, Beyene Petros, Guiyun Yan
Ethiopia is one of the few African countries where Plasmodium vivax is co-endemic with P. falciparum. Malaria transmission is seasonal and transmission intensity varies mainly by landscape and climate. Although the recent emergence of drug resistant parasites presents a major issue to malaria control in Ethiopia, little is known about the transmission pathways of parasite species and prevalence of resistant markers. This study used microsatellites to determine population diversity and gene flow patterns of P...
July 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28738840/progress-towards-malaria-elimination-in-zimbabwe-with-special-reference-to-the-period-2003-2015
#17
Shadreck Sande, Moses Zimba, Joseph Mberikunashe, Andrew Tangwena, Anderson Chimusoro
BACKGROUND: An intensive effort to control malaria in Zimbabwe has produced dramatic reductions in the burden of the disease over the past 13 years. The successes have prompted the Zimbabwe's National Malaria Control Programme to commit to elimination of malaria. It is critical to analyse the changes in the morbidity trends based on surveillance data, and scrutinize reorientation to strategies for elimination. METHODS: This is a retrospective study of available Ministry of Health surveillance data and programme reports, mostly from 2003 to 2015...
July 24, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28733082/effects-of-novel-triple-stage-antimalarial-ionic-liquids-on-lipid-membrane-models
#18
Ricardo Ferraz, Marina Pinheiro, Ana Gomes, Cátia Teixeira, Cristina Prudêncio, Salette Reis, Paula Gomes
Primaquine-based ionic liquids, obtained by acid-base reaction between parent primaquine and cinnamic acids, were recently found as triple-stage antimalarial hits. These ionic compounds displayed significant activity against both liver- and blood-stage Plasmodium parasites, as well as against stage V P. falciparum parasites. Remarkably, blood-stage activity of the ionic liquids against both chloroquine-sensitive (3D7) and resistant (Dd2) P. falciparum strains was clearly superior to those of the respective covalent (amide) analogues and of parent primaquine...
July 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28729403/autophagy-inhibition-improves-sunitinib-efficacy-in-pancreatic-neuroendocrine-tumors-via-a-lysosome-dependent-mechanism
#19
Tabea Wiedmer, Annika Blank, Sophia Pantasis, Lea Normand, Ruben Bill, Philippe Krebs, Mario P Tschan, Ilaria Marinoni, Aurel Perren
Increasing the efficacy of approved systemic treatments in metastasized pancreatic neuroendocrine tumors (PanNETs) is an unmet medical need. The anti-angiogenic tyrosine kinase inhibitor sunitinib is approved for PanNET treatment. Additionally, sunitinib is a lysosomotropic drug and such drugs can induce lysosomal membrane permeabilization as well as autophagy. We investigated sunitinib-induced autophagy as a possible mechanism of PanNET therapy resistance. Sunitinib accumulated in lysosomes and induced autophagy in PanNET cell lines...
July 20, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28726781/autophagy-inhibition-reduces-chemoresistance-and-tumorigenic-potential-of-human-ovarian-cancer-stem-cells
#20
Anna Pagotto, Giorgia Pilotto, Elena Laura Mazzoldi, Maria Ornella Nicoletto, Simona Frezzini, Anna Pastò, Alberto Amadori
Epithelial ovarian cancer (EOC) is one of the most malignant gynecological tumors with a high mortality rate owing to tumor relapse after anticancer therapies. It is widely accepted that a rare tumor cell population, known as cancer stem cells (CSC), is responsible for tumor progression and relapse; intriguingly, these cells are able to survive nutrient starvation (such as in vitro culture in the absence of glucose) and chemotherapy treatment. Recent data also indicated that chemotherapy resistance is associated with autophagy activation...
July 20, 2017: Cell Death & Disease
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