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https://www.readbyqxmd.com/read/29454189/pyrimidine-chloroquinoline-hybrids-synthesis-and-antiplasmodial-activity
#1
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
https://www.readbyqxmd.com/read/29453806/cq-sensitizes-human-pancreatic-cancer-cells-to-gemcitabine-through-the-lysosomal-apoptotic-pathway-via-reactive-oxygen-species
#2
Zhiping Fu, Cheng Xi, Jie Kuang, Haoran Feng, Lingxie Chen, Juyong Liang, Xiaonan Shen, Stanley Yuen, Peng Chenghong, Shen Baiyong, Jin Zhijian, Weihua Qiu
As an established anti-cancer drug, gemcitabine (GEM) is an effective systemic treatment for advanced pancreatic cancer (PC). However, little is known about the potential effectors that may modify tumour cell sensitivity towards GEM. Autophagy, as a physiological cellular mechanism, is involved in both cell survival and cell death. In this study, we found that exposure to GEM induced a significant increase in autophagy in a dose-dependent manner in PANC-1 and BxPC-3 cells. Inhibition of autophagy by chloroquine (CQ) and ATG7 siRNA increased GEM-induced cytotoxicity, and CQ was more effective than ATG7 siRNA...
February 17, 2018: Molecular Oncology
https://www.readbyqxmd.com/read/29453292/clonal-selection-drives-protective-memory-b-cell-responses-in-controlled-human-malaria-infection
#3
Rajagopal Murugan, Lisa Buchauer, Gianna Triller, Cornelia Kreschel, Giulia Costa, Gemma Pidelaserra Martí, Katharina Imkeller, Christian E Busse, Sumana Chakravarty, B Kim Lee Sim, Stephen L Hoffman, Elena A Levashina, Peter G Kremsner, Benjamin Mordmüller, Thomas Höfer, Hedda Wardemann
Affinity maturation, the clonal selection and expansion of antigen-activated B cells expressing somatically mutated antibody variants that develop during T cell-dependent germinal center reactions, is considered pivotal for efficient development of protective B cell memory responses to infection and vaccination. Repeated antigen exposure promotes affinity maturation but each time also recruits antigen-reactive naïve B cells into the response. Here, we determined the relative impact of affinity maturation versus antigen-mediated clonal selection of naïve B cells to mount potent B cell memory responses in humans after repeated exposure to a complex pathogen, the malaria parasite Plasmodium falciparum (Pf)...
February 16, 2018: Science Immunology
https://www.readbyqxmd.com/read/29452162/pseudorabies-virus-induces-autophagy-to-enhance-viral-replication-in-mouse-neuro-2a-cells-in-vitro
#4
Changmeng Xu, Mi Wang, Zhongbao Song, Zhijian Wang, Qianyu Liu, Ping Jiang, Juan Bai, Yufeng Li, Xianwei Wang
Autophagy of cytoplasmic components plays an essential role in the pathogenic infection process. Furthermore, research suggests that autophagy is an extremely important component of the innate immune response. Our study aimed to reveal the effect of virus-induced autophagy on pseudorabies virus (PRV) replication. Our results confirmed that light chain 3 (LC3)-I was converted into LC3-II after PRV infection; this transition is considered an important indicator of autophagy. Transmission electron microscopy (TEM) revealed that PRV infection could notably increase the number of autophagosomes in mouse neuro-2a (N2a) cells...
February 13, 2018: Virus Research
https://www.readbyqxmd.com/read/29452093/autophagy-inhibition-enhances-anticancer-efficacy-of-artepillin-c-a-cinnamic-acid-derivative-in-brazilian-green-propolis
#5
Satoshi Endo, Manami Hoshi, Toshiyuki Matsunaga, Takahiro Inoue, Kenji Ichihara, Akira Ikari
Propolis, a resinous substance produced by honeybees, possesses various biological actions including anticancer activity towards tumor cells. Recently, the ethanol extract of Brazilian green propolis has been shown to induce autophagy, which is known to be induced in treatment of cancer cells with anticancer drugs, leading to cancer cell survival and decreased sensitivity to anticancer agents. In this study, we aimed to identify autophagy-inducing components of the propolis and elucidated the reciprocal relationship between anticancer cytotoxicity and protective autophagy in prostate cancer CWR22Rv1 cells...
February 13, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29449537/predictive-and-preventive-significance-of-ampk-activation-on-hepatocarcinogenesis-in-patients-with-liver-cirrhosis
#6
Xiaoli Yang, Yan Liu, Menghui Li, Hao Wu, Yunbing Wang, Yu You, Peizhi Li, Xiong Ding, Chang'an Liu, Jianping Gong
Metformin has been demonstrated to prevent hepatocellular carcinoma (HCC). Metformin acts mainly by phosphorylation of AMPK. However, the phosphorylation status of AMPK and its role in the prediction and prevention of HCC in cirrhotic patients remains unclear. The phosphorylation status of AMPK (Thr172) was determined by immunostaining in tissue microarrays of 426 cirrhotic liver tissues. Low expression of p-AMPK was observed in 94 (22.1%) cases. The median follow-up time was 87 months. HCC occurrence probability at 1/3/5/10 years after Hassab procedure was 3...
February 15, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29449536/impaired-autophagic-flux-is-associated-with-the-severity-of-trauma-and-the-role-of-a-2a-r-in-brain-cells-after-traumatic-brain-injury
#7
Xu-Jia Zeng, Ping Li, Ya-Lei Ning, Yan Zhao, Yan Peng, Nan Yang, Zi-Ai Zhao, Jiang-Fan Chen, Yuan-Guo Zhou
Recent studies have shown that after traumatic brain injury (TBI), the number of autophagosomes is markedly increased in brain cells surrounding the wound; however, whether autophagy is enhanced or suppressed by TBI remains controversial. In our study, we used a controlled cortical impact system to establish models of mild, moderate and severe TBI. In the mild TBI model, the levels of autophagy-related protein 6 (Beclin1) and autophagy-related protein 12 (ATG12)-autophagy-related protein 5 (ATG5) conjugates were increased, indicating the enhanced initiation of autophagy...
February 14, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29447354/creb3-regulatory-factor-mtor-autophagy-regulates-goat-endometrial-function-during-early-pregnancy
#8
Diqi Yang, Tingting Jiang, Jianguo Liu, Beibei Zhang, Pengfei Lin, Huatao Chen, Dong Zhou, Keqiong Tang, Aihua Wang, Yaping Jin
In domestic ruminants, a receptive endometrium is crucial for successful pregnancy. Although many essential molecular modulators and pathways have been identified during early pregnancy, the precise mechanisms regulating goat endometrial function remains largely unknown. Here, we describe a novel regulator during early pregnancy, whereby hormones increased CREB3 Regulatory Factor (CREBRF) expression and act as a potential activator of autophagy in endometrial epithelial cells (EECs) via the mTOR pathway. Our results showed that knockdown of CREBRF via shCREBRF hampered EECs proliferation by S-phase cell cycle arrest and significantly inhibited endometrial function...
February 13, 2018: Biology of Reproduction
https://www.readbyqxmd.com/read/29446619/synthesis-of-cyclic-peptides-as-potential-anti-malarials
#9
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
https://www.readbyqxmd.com/read/29445224/lup-20-29-en-3%C3%AE-28-di-yl-nitrooxy-acetate-affects-mcf-7-proliferation-through-the-crosstalk-between-apoptosis-and-autophagy-in-mitochondria
#10
Xiaoning Yan, Lei Yang, Gaili Feng, Zhuli Yu, Minjie Xiao, Weibin Cai, Yanmei Xing, Shasha Bai, Junqia Guo, Zhiyu Wang, Tao Wang, Rong Zhang
Betulin (BT), a pentacyclic lupine-type triterpenoid natural product, possesses antitumor activity in various types of cancers. However, its clinical development was discouraged due to its low biological activities and poor solubility. We prepared lup-20(29)-en-3β,28-di-yl-nitrooxy acetate (NBT), a derivative of BT, that was chemically modified at position 3 of ring A and C-28 by introducing a NO-releasing moiety. This study mainly explored the mechanism of NBT in treating breast cancer through the crosstalk between apoptosis and autophagy in mitochondria...
February 14, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29444080/promising-approach-to-reducing-malaria-transmission-by-ivermectin-sporontocidal-effect-against-plasmodium-vivax-in-the-south-american-vectors-anopheles-aquasalis-and-anopheles-darlingi
#11
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
https://www.readbyqxmd.com/read/29436997/pyrazole-schiff-base-hybrid-as-an-anti-malarial-agent-synthesis-in-vitro-screening-and-molecular-docking-study
#12
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
https://www.readbyqxmd.com/read/29435951/correction-of-huntington-s-disease-phenotype-by-genistein-induced-autophagy-in-the-cellular-model
#13
Karolina Pierzynowska, Lidia Gaffke, Aleksandra Hać, Jagoda Mantej, Natalia Niedziałek, Joanna Brokowska, Grzegorz Węgrzyn
Huntington's disease (HD) is a monogenic disorder, caused by mutations in the HTT gene which result in expansion of CAG triplets. The product of the mutated gene is misfolded huntingtin protein that forms aggregates leading to impairment of neuronal function, neurodegeneration, motor abnormalities and cognitive deficits. No effective cure is currently available for HD. Here we studied effects of genistein (trihydroxyisoflavone) on a HD cellular model consisting of HEK-293 cells transfected with a plasmid bearing mutated HTT gene...
February 12, 2018: Neuromolecular Medicine
https://www.readbyqxmd.com/read/29435010/chloroquine-potentiates-the-anticancer-effect-of-sunitinib-on-renal-cell-carcinoma-by-inhibiting-autophagy-and-inducing-apoptosis
#14
Man-Li Li, You-Zhi Xu, Wen-Jie Lu, Yong-Huai Li, Shi-Sheng Tan, Hong-Jun Lin, Tian-Ming Wu, Yan Li, Si-Ying Wang, Ying-Lan Zhao
Sunitinib based adjuvant chemotherapy combined with chloroquine (CQ) for the treatment of renal cell carcinoma (RCC) is in clinical trials; however, its anti-RCC effect and the mechanism remain unclear. In the present study, the anti-RCC effect of sunitinib with CQ and the underlying mechanism was investigated. An MTT assay demonstrated that CQ enhanced the proliferation inhibitory effect of sunitinib against the OS-RC-2 RCC cell line. CQ inhibited sunitinib-induced autophagy in OS-RC-2, which was evidenced by the inhibition of autophagic vacuoles, acidic vesicular organelle formation, light chain 3 (LC3)-II recruitment to the autophagosomes and the conversion of LC3-I to LC3-II, as induced by sunitinib...
March 2018: Oncology Letters
https://www.readbyqxmd.com/read/29434902/chloroquine-exerts-antitumor-effects-on-nb4-acute-promyelocytic-leukemia-cells-and-functions-synergistically-with-arsenic-trioxide
#15
Shousheng Liu, Xiuyu Cai, Liangping Xia, Chang Jiang, Ping Chen, Xiaopai Wang, Bei Zhang, Hong Yun Zhao
Chloroquine (CQ) has been confirmed to exhibit antitumor effects on different types of cancer cell, but whether it exerts the same effect on acute promyelocytic leukemia (APL) cells remains to be confirmed. In the present study, the effects of various concentrations of CQ on the growth, apoptosis and cell cycle distribution of NB4 cells, as well as the potential mechanisms underlying these effects, were examined. The combined effect of CQ and arsenic trioxide (ATO) on the growth of NB4 cells was also determined...
February 2018: Oncology Letters
https://www.readbyqxmd.com/read/29433507/sudden-spleen-rupture-in-a-plasmodium-vivax-infected-patient-undergoing-malaria-treatment
#16
Aleix Elizalde-Torrent, Fernando Val, Ingrid Cardoso C Azevedo, Wuelton M Monteiro, Luiz C L Ferreira, Carmen Fernández-Becerra, Hernando A Del Portillo, Marcus V G Lacerda
BACKGROUND: Splenomegaly is one of the most common features of malaria. However, spontaneous splenic rupture, although unusual, represents a severe complication often leading to death. It is mostly seen in acute infection and primary attack, and it is most commonly associated with Plasmodium vivax. Here, a case of spontaneous splenic rupture diagnosed with a portable ultrasound apparatus shortly after starting treatment and with recurrent parasitaemia after splenectomy, is reported. CASE DESCRIPTION: In November 2015, a 45-year-old Brazilian man presented to the hospital in Manaus with fever, headache and myalgia...
February 13, 2018: Malaria Journal
https://www.readbyqxmd.com/read/29425203/neutralization-of-antibody-enhanced-dengue-infection-by-vis513-a-pan-serotype-reactive-monoclonal-antibody-targeting-domain-iii-of-the-dengue-e-protein
#17
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
https://www.readbyqxmd.com/read/29422973/chloroquine-affects-autophagy-to-achieve-an-anticancer-effect-in-ec109-esophageal-carcinoma-cells-in-vitro
#18
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
https://www.readbyqxmd.com/read/29416002/ezh2-inhibits-autophagic-cell-death-of-aortic-vascular-smooth-muscle-cells-to-affect-aortic-dissection
#19
Rui Li, Xin Yi, Xiang Wei, Bo Huo, Xian Guo, Cai Cheng, Ze-Min Fang, Jing Wang, Xin Feng, Ping Zheng, Yun-Shu Su, Jackson Ferdinand Masau, Xue-Hai Zhu, Ding-Sheng Jiang
Enhancer of zeste homolog 2 (EZH2), a methyltransferase that di- and tri-methylates lysine-27 of histone H3, largely functions as a transcriptional repressor, and plays a critical role in various kinds of cancers. Here we report a novel function of EZH2 in regulating autophagic cell death (ACD) of vascular smooth muscle cells (VSMCs) that affect aortic dissection (AD). Inhibition of EZH2 activity by UNC1999 or knockdown EZH2 resulted in VSMC loss, while overexpression of EZH2 facilitated VSMC growth, and these effects of EZH2 on VSMCs were independent of proliferation and apoptosis...
February 7, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29410767/hyperpigmentation-of-hard-palate-induced-by-chloroquine-therapy
#20
Bruno-Augusto-Benevenuto de Andrade, Nelson-Alejandro Padron-Alvarado, Edgar-Manuel Muñoz-Campos, Thayná-Melo-de Lima Morais, Ricardo Martinez-Pedraza
The antimalarials are one of the most commonly prescribed drugs for conditions such as lupus erythematosus and rheumatoid arthritis, and the side effects, though infrequent, are well known. The antimalarial agent chloroquine diphosphate usually causes pigmentary changes in the oral mucosa characterized by a bluish-grey to black discolorations mainly in the hard palate. Considering only the hard palate hyperpigmentation caused by chloroquine, to the best of our knowledge, only 13 cases have been reported in the English language literature...
December 2017: Journal of Clinical and Experimental Dentistry
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