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chloroquine resistance

Yangfeng Xiang, Jianqiang Zhao, Ming Zhao, Kejing Wang
Allicin has been reported to inhibit cancer cell proliferation, induce cell apoptosis and enhance the accumulation of reactive oxygen species. However, it has remained elusive whether allicin improves multidrug resistance in thyroid cancer cells through modulating autophagy. The present study demonstrated that combined use of allicin and cisplatin or carboplatin resulted in an enhanced growth inhibitory effect on SW1736 and HTh-7 cells. Furthermore, treatment with allicin significantly increased SW1736 and HTh-7 cell autophagy...
April 2018: Experimental and Therapeutic Medicine
Ishag Adam, Yassin Ibrahim, Gasim I Gasim
BACKGROUND: Malaria is a major public health problem in endemic countries including Sudan, where about 75% of populations are at risk. Due to widespread of chloroquine-resistant strains of Plasmodium falciparum, artemisinin-based combination therapy (ACT) is currently treatment of choice for malaria in the vast majority of malaria-endemic countries. This systematic review and meta-analysis is performed to obtain an overall stronger evidence of the outcomes of ACT in the treatment of uncomplicated falciparum malaria from the existing literature in Sudan...
March 13, 2018: Malaria Journal
Hiroyuki Monma, Yuichi Iida, Tamami Moritani, Tamio Okimoto, Ryosuke Tanino, Yoshitsugu Tajima, Mamoru Harada
Autophagy contributes to the treatment-resistance of many types of cancers, and chloroquine (CQ) inhibits autophagy. The tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) kills cancer cells but is minimally cytotoxic to normal cells. However, because the therapeutic efficacy of TRAIL is limited, it is necessary to augment TRAIL-induced anti-tumor effects. In this study, we explored the anti-tumor effects of a combination of CQ and TRAIL on two human pancreatic cancer cell lines: TRAIL-sensitive MiaPaCa-2 cells and Panc-1 cells that are less sensitive to TRAIL...
2018: PloS One
Hui-Ping Chang, Chi-Cheng Lu, Jo-Hua Chiang, Fuu-Jen Tsai, Yu-Ning Juan, Je-Wei Tsao, Hong-Yi Chiu, Jai-Sing Yang
Pterostilbene is a natural polyphenolic compound that is primarily found in fruits, such as blueberries and has a similar structure to resveratrol. Pterostilbene exhibits antioxidant, anti-inflammatory and antitumor activity but the effects of pterostilbene on drug-resistant oral cancer cells and its underlying mechanisms of action have not yet been explored. Therefore, the present study was performed to clarify the anticancer effects of pterostilbene on cisplatin-resistant human oral cancer CAR cells. The results demonstrated that CAR cells exhibited marked shrinkage, cell membrane breakage and autophagic vacuole formation following treatment with pterostilbene...
March 2, 2018: International Journal of Oncology
Pooja Agarwal, A R Anvikar, C R Pillai, Kumkum Srivastava
Background & objectives: : The in vitro assays for susceptibility of Plasmodium falciparum to antimalarial drugs are important tools for monitoring drug resistance. During the present study, efforts were made to establish long-term continuous in vitro culture of Indian field isolates of P. falciparum and to determine their sensitivity to standard antimalarial drugs and antibiotics. Methods: Four (MZR-I, -II, -III and -IV) P. falciparum isolates were obtained from four patients who showed artemisinin-based combination therapy (ACT) from Mizoram, a north-eastern State of India, and characterized for their in vitro susceptibility to chloroquine diphosphate (CQ), quinine hydrochloride dehydrate, mefloquine, piperaquine, artemether, arteether, dihydro-artemisinin (DHA), lumefantrine and atovaquone and antibiotics, azithromycin and doxycycline...
November 2017: Indian Journal of Medical Research
Gautam Kumar, Omprakash Tanwar, Jitender Kumar, Mymoona Akhter, Supriya Sharma, C R Pillai, Md Mumtaz Alam, M S Zama
A series of pyrazole-pyrazoline substituted with benzenesulfonamide were synthesized and evaluated for their antimalarial activity in vitro and in vivo. The compounds were active against both chloroquine (CQ) sensitive (3D7) and CQ resistant (RKL-9) strains of Plasmodium falciparum. Seven compounds (7e, 7i, 7j, 7l, 7m, 7o and 7p) exhibiting EC50 less than 2 μM. A mechanistic study of compound 7o revealed that these compound act through the inhibition of β-hematin. The study indicated that these compounds can serve as lead compounds for further development of potent antimalarial drugs...
February 15, 2018: European Journal of Medicinal Chemistry
Jorge Vallecillo-Hernández, Maria Dolores Barrachina, Dolores Ortiz-Masiá, Sandra Coll, Juan Vicente Esplugues, Sara Calatayud, Carlos Hernández
NSAIDs inhibit tumorigenesis in gastrointestinal tissues and have been proposed as coadjuvant agents to chemotherapy. The ability of cancer epithelial cells to adapt to the tumour environment and to resist cytotoxic agents seems to depend on rescue mechanisms such as autophagy. In the present study we aimed to determine whether an NSAID with sensitizing properties such as indomethacin modulates autophagy in gastric cancer epithelial cells. We observed that indomethacin causes lysosomal dysfunction in AGS cells and promotes the accumulation of autophagy substrates without altering mTOR activity...
February 26, 2018: Scientific Reports
Rakesh Chopra, Kelly Chibale, Kamaljit Singh
Triazole tethered 7-chloroquinoline-pyrimidine-5-carboxylate hybrids were synthesized and evaluated for antiplasmodial activity against chloroquine sensitive (CQ S ) NF54 strain of Plasmodium falciparum. The most active hybrids of the series were further screened against the chloroquine resistant (CQ R ) Dd2 strain of the parasite and for in vitro cytotoxicity against mammalian Vero cell lines. Further, their physico-chemical properties, binding studies with hemin (monomeric &μ-oxo dimeric) and DNA [pUC-18, calf thymus (CT)] led us to plausible proposed binding mode of the most active member of the present series...
February 9, 2018: European Journal of Medicinal Chemistry
Catherine Fagundez, Diver Sellanes, Gloria Lourdes Serra
The results from the synthesis of peptides by Fmoc/SPPS on a 2-CTC resin and then lactamization in solution or solid phase for the preparation of cyclopeptides are presented. Both procedures allow the synthesis of the desired compounds in good to very good yield and with high cyclization efficiency for on-resin macrocyclization. In addition, the activities of the corresponding cyclopeptides against the chloroquine-resistant K1 strain of Plasmodium falciparum were evaluated. Cyclo-Cys(Trt)-Gly-Thr(tBu)-Gly-Cys(Trt)-Gly showed potent in vitro and selective activity against this parasite, EC50 = 28 nM...
February 15, 2018: ACS Combinatorial Science
Yudi T Pinilla, Stefanie C P Lopes, Vanderson S Sampaio, Francys S Andrade, Gisely C Melo, Alessandra S Orfanó, Nágila F C Secundino, Maria G V B Guerra, Marcus V G Lacerda, Kevin C Kobylinski, Karin S Escobedo-Vargas, Victor M López-Sifuentes, Craig A Stoops, G Christian Baldeviano, Joel Tarning, Gissella M Vasquez, Paulo F P Pimenta, Wuelton M Monteiro
BACKGROUND: The mosquito resistance to the insecticides threatens malaria control efforts, potentially becoming a major public health issue. Alternative methods like ivermectin (IVM) administration to humans has been suggested as a possible vector control to reduce Plasmodium transmission. Anopheles aquasalis and Anopheles darlingi are competent vectors for Plasmodium vivax, and they have been responsible for various malaria outbreaks in the coast of Brazil and the Amazon Region of South America...
February 14, 2018: PLoS Neglected Tropical Diseases
Shilpy Aggarwal, Deepika Paliwal, Dhirender Kaushik, Girish Kumar Gupta, Ajay Kumar
BACKGROUND: Malaria, one of the most vital infectious diseases caused by protozoan parasites of the Plasmodium genus. As P. falciparum, the cause of most of the severe cases of malaria, is increasingly resistant to available drugs such as amodioquine, chloroquine, artemisinin, and antifolates, there is an urgent need of identify new targets for chemotherapy Objective: This study screened novel pyrazole derivatives carrying iminium & benzothiazole group for antimalarial potential against P...
February 12, 2018: Combinatorial Chemistry & High Throughput Screening
Yadunanda Budigi, Eugenia Z Ong, Luke N Robinson, Li Ching Ong, Kirk J Rowley, Alexander Winnett, Hwee Cheng Tan, Sven Hobbie, Zachary Shriver, Gregory J Babcock, Sylvie Alonso, Eng Eong Ooi
Dengue virus (DENV) infection imposes enormous health and economic burden worldwide with no approved treatment. Several small molecules, including lovastatin, celgosivir, balapiravir and chloroquine have been tested for potential anti-dengue activity in clinical trials; none of these have demonstrated a protective effect. Recently, based on identification and characterization of cross-serotype neutralizing antibodies, there is increasing attention on the potential for dengue immunotherapy. Here, we tested the ability of VIS513, an engineered cross-neutralizing humanized antibody targeting the DENV E protein domain III, to overcome antibody-enhanced infection and high but brief viremia, which are commonly encountered in dengue patients, in various in vitro and in vivo models...
February 9, 2018: PLoS Neglected Tropical Diseases
Yan Cai, Jiajing Cai, Qiang Ma, Yuan Xu, Jiang Zou, Lei Xu, Dongsheng Wang, Xiaolan Guo
Esophageal carcinoma is a malignancy that severely threatens human health, with a high incidence rate and a low 5-year survival rate. Resistance to chemotherapy frequently emerges during its treatment, partly due to the induction of autophagy. Therefore, targeting autophagy may be a promising therapeutic approach for the treatment of esophageal carcinoma. In the present study, it was investigated how chloroquine (CQ) can influence the growth ability and biological behaviors of EC109 esophageal squamous carcinoma cells in vitro, as well as the potential molecular mechanisms behind its activity...
January 2018: Oncology Letters
Sarah M Tindall, Cindy Vallières, Dev H Lakhani, Farida Islahudin, Kang-Nee Ting, Simon V Avery
Antimalarial drug resistance hampers effective malaria treatment. Critical SNPs in a particular, putative amino acid transporter were recently linked to chloroquine (CQ) resistance in malaria parasites. Here, we show that this conserved protein (PF3D7_0629500 in Plasmodium falciparum; AAT1 in P. chabaudi) is a structural homologue of the yeast amino acid transporter Tat2p, which is known to mediate quinine uptake and toxicity. Heterologous expression of PF3D7_0629500 in yeast produced CQ hypersensitivity, coincident with increased CQ uptake...
February 6, 2018: Scientific Reports
Supriya Sharma, Ram Suresh Bharti, Nitin Bhardwaj, Anupkumar R Anvikar, Neena Valecha, Neelima Mishra
BACKGROUND: Antimalarial drug resistance is a potential threat for control and elimination of malaria. To ascertain the status of antimalarial drug resistance at the study sites, correlation between in vitro drug sensitivity pattern and drug resistance molecular markers in Plasmodium falciparum malaria was undertaken. MATERIALS AND METHODS: Polymorphisms in P. falciparum chloroquine resistance transporter (pfcrt) K76T and pfmdr1 N86Y were studied in relation to the in vitro susceptibility of P...
October 2017: Indian Journal of Medical Microbiology
Mahamane Haidara, Mohamed Haddad, Adama Denou, Guillaume Marti, Sandra Bourgeade-Delmas, Rokia Sanogo, Geneviève Bourdy, Agnès Aubouy
BACKGROUND: Plasmodium falciparum malaria is still one of the most deadly pathology worldwide. Efficient treatment is jeopardized by parasite resistance to artemisinin and its derivatives, and by poor access to treatment in endemic regions. Anti-malarial traditional remedies still offer new tracks for identifying promising antiplasmodial molecules, and a way to ensure that all people have access to care. The present study aims to validate the traditional use of Terminalia macroptera, a Malian plant used in traditional medicine...
February 5, 2018: Malaria Journal
Meghna Desai, Jenny Hill, Silke Fernandes, Patrick Walker, Christopher Pell, Julie Gutman, Kassoum Kayentao, Raquel Gonzalez, Jayne Webster, Brian Greenwood, Michel Cot, Feiko O Ter Kuile
Malaria remains one of the most preventable causes of adverse birth outcomes. Intermittent preventive treatment in pregnancy (IPTp) with sulfadoxine-pyrimethamine is used to prevent malaria, but resistance to this drug combination has decreased its efficacy and new alternatives are needed. In Africa, a meta-analysis showed three-course or monthly IPTp with sulfadoxine-pyrimethamine to be safe and more effective than the original two-course sulfadoxine-pyrimethamine strategy, prompting WHO to update its policy in 2012...
January 30, 2018: Lancet Infectious Diseases
O Maiques, C Barceló, A Panosa, J Pijuan, J L Orgaz, I Rodriguez-Hernandez, C Matas-Nadal, G Tell, R Vilella, A Fabra, Puig S, V Sanz-Moreno, X Matias-Guiu, C Canti, J Herreros, R M Marti, A Macià
Melanoma is a malignant tumor derived from melanocytes. Once disseminated, it is usually highly resistant to chemotherapy and is associated with poor prognosis. We have recently reported that T-type calcium channels (TTCCs) are overexpressed in melanoma cells and play an important role in melanoma progression. Importantly, TTCC pharmacological blockers reduce proliferation and deregulate autophagy leading to apoptosis. Here, we analyze the role of autophagy during migration/invasion of melanoma cells. TTCC Cav3...
January 31, 2018: Pigment Cell & Melanoma Research
Gabriel W Rangel, Martha A Clark, Usheer Kanjee, Caeul Lim, Kathryn Shaw-Saliba, Maria José Menezes, Anjali Mascarenhas, Laura Chery, Edwin Gomes, Pradipsinh K Rathod, Marcelo U Ferreira, Manoj T Duraisingh
Plasmodium vivax chloroquine resistance has been documented in nearly every region endemic for this malaria-causing parasite. Unfortunately, P. vivax resistance surveillance and drug discovery is challenging due to low parasitemias of patient isolates, and poor parasite survival through ex vivo maturation, that reduce the sensitivity and scalability of current P. vivax antimalarial assays. Using cryopreserved patient isolates from Brazil and fresh patient isolates from India, we established a robust enrichment method for P...
January 29, 2018: Antimicrobial Agents and Chemotherapy
Barry Jutten, Tom G Keulers, Hanneke J M Peeters, Marco B E Schaaf, Kim G M Savelkouls, Inge Compter, Ruud Clarijs, Olaf E M G Schijns, Linda Ackermans, Onno P M Teernstra, Marijke I Zonneveld, Resi M E Colaris, Ludwig Dubois, Marc A Vooijs, Johan Bussink, Julio Sotelo, Jan Theys, Guido Lammering, Kasper M A Rouschop
Expression of EGFRvIII is frequently observed in glioblastoma and is associated with increased cellular proliferation, enhanced tolerance to metabolic stresses, accelerated tumor growth, therapy resistance and poor prognosis. We observed that expression of EGFRvIII elevates the activation of macroautophagy/autophagy during starvation and hypoxia and explored the underlying mechanism and consequence. Autophagy was inhibited (genetically or pharmacologically) and its consequence for tolerance to metabolic stress and its therapeutic potential in (EGFRvIII+) glioblastoma was assessed in cellular systems, (patient derived) tumor xenopgrafts and glioblastoma patients...
January 29, 2018: Autophagy
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