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https://www.readbyqxmd.com/read/28810188/novel-tacrine-derivatives-exhibiting-improved-acetylcholinesterase-inhibition-design-synthesis-and-biological-evaluation
#1
Eeda Koti Reddy, Chandran Remya, Kumar Mantosh, Ayyiliath M Sajith, R V Omkumar, C Sadasivan, Shaik Anwar
A novel series of twenty four tacrine derivatives were designed and synthesised. Among these, thirteen were taken for the acetylcholinesterase (AChE) inhibition studies. Three compounds such as 4c, 6c and 6f were found to possess significant AChE inhibitory properties with IC50 values 12.97 ± 0.47 nM, 5.17 ± 0.24 nM and 7.14 ± 0.78 nM respectively. In silico docking studies revealed that these compounds can bind strongly in the active site of the enzyme and prevent enzyme-substrate interactions...
August 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28809737/acute-liver-failure-due-to-etodolac-a-selective-cycloxygenase-2-cox-2-inhibitor-non-steroidal-anti-inflammatory-drug-established-by-rucam-based-causality-assessment
#2
Sunil Taneja, Pramod Kumar, Sahaj Rathi, Ajay Duseja, Virendra Singh, Radha Krishan Dhiman, Yogesh Kumar Chawla
Drug induced liver injury is a common cause of acute liver failure (ALF). While most of these cases are due to dose dependent hepatotoxicity with acetaminophen, idiosyncratic drug-induced liver injury (DILI) is responsible for about 15% cases of ALF. Antibiotics are the most common cause of idiosyncratic DILI as well as DILI induced ALF. Etodolac is a selective cycloxygenase- 2 (COX -2) inhibitor non-steroidal anti-inflammatory drug used as an analgesic and anti-inflammatory in musculoskeletal diseases. Severe liver impairment is extremely rare...
August 8, 2017: Annals of Hepatology
https://www.readbyqxmd.com/read/28806057/rational-design-and-multi-biological-profiling-of-novel-donepezil-trolox-hybrids-against-alzheimer-s-disease-with-cholinergic-antioxidant-neuroprotective-and-cognition-enhancing-properties
#3
Pei Cai, Si-Qiang Fang, Xue-Lian Yang, Jia-Jia Wu, Qiao-Hong Liu, Hao Hong, Xiao-Bing Wang, Lingyi Kong
A novel series of donepezil-trolox hybrids were designed, synthesized and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41...
August 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28803824/the-clinical-spectrum-of-hepatic-manifestations-in-chronic-lymphocytic-leukemia
#4
REVIEW
Natalia Kreiniz, Ofrat Beyar Katz, Aaron Polliack, Tamar Tadmor
Chronic lymphocytic leukemia (CLL) is the most common leukemia in the Western world, characterized by the presence of long-lived circulating leukemic cells in the peripheral blood that may infiltrate all organs, particularly those of the reticulo-endothelial system. Liver enlargement and elevation of liver enzymes related to specific involvement by the underlying disease are well-recognized features in these patients. In CLL, the differential diagnosis of liver disorders is broad and includes liver infiltration by leukemic cells, immunologic manifestations associated with CLL, primary and secondary hepatic malignancies, drug-induced hepatotoxicity, infections, and Richter transformation...
July 23, 2017: Clinical Lymphoma, Myeloma & Leukemia
https://www.readbyqxmd.com/read/28803044/new-racemic-annulated-pyrazolo-1-2-b-phthalazines-as-tacrine-like-ache-inhibitors-with-potential-use-in-alzheimer-s-disease
#5
Leili Jalili-Baleh, Hamid Nadri, Alireza Moradi, Syed Nasir Abbas Bukhari, Mojtaba Shakibaie, Mandana Jafari, Mostafa Golshani, Farshad Homayouni Moghadam, Loghman Firoozpour, Ali Asadipour, Saeed Emami, Mehdi Khoobi, Alireza Foroumadi
A novel series of tacrine-like compounds 7a-u possessing a fused pyrazolo[1,2-b]phthalazine structure were designed and synthesized as potent and selective inhibitors of AChE. The in-vitro biological assessments demonstrated that several compounds had high anti-AChE activity at nano-molar level. The more promising compound 7l with IC50 of 49 nM was 7-fold more potent than tacrine and unlike tacrine, it was highly selective against AChE over BuChE. The cell-based assays against hepatocytes (HepG2) and neuronal cell line (PC12) revealed that 7l had significantly lower hepatotoxicity compared to tacrine, with additional neuroprotective activity against H2O2-induced damage in PC12 cells...
July 31, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28800917/thyrotoxic-rubber-antioxidants-2-mercaptobenzimidazole-and-its-methyl-derivatives-cause-both-inhibition-and-induction-of-drug-metabolizing-activity-in-rat-liver-microsomes-after-repeated-oral-administration
#6
Atsuko Miyajima, Kazue Sakemi-Hoshikawa, Makoto Usami, Katsuyoshi Mitsunaga, Tomohiko Irie, Yasuo Ohno, Momoko Sunouchi
We examined the effects of thyrotoxic rubber antioxidants, 2-mercaptobenzimidazole (MBI, 0.3 mmol/kg/day) and its methyl derivatives, methyl-MBIs [4-methyl-MBI (4-MeMBI, 0.6 mmol/kg/day), 5-methyl-MBI (5-MeMBI, 0.6 mmol/kg/day), and 4(or 5)-methyl-MBI (4(5)-MeMBI, 0.6 or 1.2 mmol/kg/day)], on the drug-metabolizing activity in male rat liver microsomes by 8-day repeated oral administration. The weight of liver and thyroid were increased by all the test chemicals; MBI was most potent, and there was no additive or synergistic effect between 4-MeMBI and 5-MeMBI...
August 8, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28799976/effect-of-gene-gene-and-gene-environment-interactions-associated-with-antituberculosis-drug-induced-hepatotoxicity
#7
Julián G Chamorro, Jorge P Castagnino, Omar Aidar, Rosa M Musella, Ana Frías, Mabel Visca, Mabel Nogueras, Lucas Costa, Alessandro Perez, Fabio Caradonna, Gabriela F de Larrañaga
OBJECTIVES: This study evaluated the association between environmental factors and genetic variations in enzymes that metabolize antituberculosis (anti-TB) drugs [arylamine N-acetyltransferase 2, cytochrome P450 2E1 (CYP2E1), glutathione S-transferase theta 1 (GSTT1), and glutathione S-transferase mu 1] with antituberculosis drug-induced hepatotoxicity (ATDH). We also investigated the potential gene-gene and gene-environment interactions as well as their association with ATDH development in a population of hospitalized TB patients from Buenos Aires...
August 9, 2017: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/28797532/assessment-of-in-vitro-antifungal-efficacy-and-in-vivo-toxicity-of-amphotericin-b-loaded-plga-and-plga-peg-blend-nanoparticles
#8
T C Moraes Moreira Carraro, C Altmeyer, N Maissar Khalil, R Mara Mainardes
Amphotericin B (AmB) is widely applied in treatment of systemic fungal infections. However, the emergence of severe adverse effects, such as nephrotoxicity, hepatotoxicity and hemolytic anemia, can limit its clinical use. Poly(lactide-co-glycolide) (PLGA) or poly(lactide-co-glycolide)-poly(ethylene glycol) (PLGA-PEG) blend nanoparticles containing AmB were developed with the aim to decrease AmB toxicity and propose the oral route for AmB delivery. Nanoparticles were characterized by particle size, polydispersity index, Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffraction analyses...
August 7, 2017: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/28793897/aqueous-extract-of-phragmitis-rhizoma-ameliorates-myelotoxicity-of-docetaxel-in-vitro-and-in-vivo
#9
Jinhee Kim, You Jin Lee, Young Ah Kim, Eun-Sang Cho, Eunna Huh, Ok-Sun Bang, No Soo Kim
BACKGROUND: A variety of anticancer chemotherapeutics induce adverse side effects including myelotoxicity. Dried roots of Phragmites communis Trinius, Phragmitis rhizoma, have been clinically used in traditional folk medicine to relieve various symptoms like fever. In this study, we evaluated the protective effect of the aqueous extract of Phragmitis rhizoma (EPR) against docetaxel-induced myelotoxicity in vitro and in vivo. METHODS: The in vitro myelo-protective effect of EPR was evaluated using the colony forming unit (CFU) assay with hematopoietic progenitor cells...
August 9, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28782199/check-your-microbiota-when-taking-the-drug
#10
EDITORIAL
Katrin Hochrath, Bernd Schnabl
In this edition of Hepatology, Yip's article entitled "The Liver-Gut Microbiota Axis Modulates Hepatotoxicity of Tacrine in the Rat" [1] elegantly uncovers the impact of the intestinal microbiota in the inter-individual variation of tacrine-induced hepatotoxicity. This article is protected by copyright. All rights reserved.
August 6, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/28781827/deferasirox-associated-with-liver-failure-and-death-in-a-sickle-cell-anemia-patient-homozygous-for-the-1774delg-polymorphism-in-the-abcc2-gene
#11
Caroline C B Braga, Bruno Deltreggia Benites, Dulcineia M de Albuquerque, Marisa C Alvarez, Tiago Seva-Pereira, Bruno K L Duarte, Fernando F Costa, Simone C O Gilli, Sara T O Saad
This manuscript describes the case of a patient with sickle cell anemia who died of fulminant hepatitis after therapy with the iron chelator Deferasirox. The patient was homozygous for the -1774delG polymorphism in the Abcc2 gene, which raises the concern about the use of hepatotoxic drugs in this specific context.
August 2017: Clinical Case Reports
https://www.readbyqxmd.com/read/28774898/fda-approval-summary-trabectedin-for-unresectable-or-metastatic-liposarcoma-or-leiomyosarcoma-following-an-anthracycline-containing-regimen
#12
Amy Barone, Dow-Chung Chi, Marc R Theoret, Huanyu Chen, Kun He, Dubravka Kufrin, Whitney S Helms, Sriram Subramaniam, Hong Zhao, Anuja Patel, Kirsten B Goldberg, Patricia Keegan, Richard Pazdur
On October 23, 2015, the U.S. Food and Drug Administration approved trabectedin, a new molecular entity for the treatment of patients with unresectable or metastatic liposarcoma or leiomyosarcoma who received a prior anthracycline-containing regimen. Approval was based on results of a single, randomized, active-controlled, 518-patient, multicenter study comparing the safety and efficacy of trabectedin 1.5 mg/m(2) as a 24-hour continuous intravenous (i.v.) infusion once every 3 weeks to dacarbazine 1000 mg/m(2) i...
August 3, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28774309/fungal-endophytes-associated-with-viola-odorata-linn-as-bioresource-for-pancreatic-lipase-inhibitors
#13
M Katoch, A Paul, G Singh, S N C Sridhar
BACKGROUND: As per the recent statistical reports of World Health Organisation (WHO), 13% of total global population is obese. Orlistat remains to be the only drug approved for the long term treatment of obesity. Recent findings highlighted severe adverse effects of orlistat that included hepatotoxicity, gall stones, kidney stones and acute pancreatitis. Therefore, search for new drug is required. The investigations based on endophytic natural products would prove pivotal in the global fight against this health issue...
August 3, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28772086/highlights-of-drug-and-herb-induced-liver-injury-in-the-literature-from-2016-how-best-to-translate-new-information-into-clinical-practice
#14
Omar Shahbaz, Sandeep Mahajan, James H Lewis
INTRODUCTION: More than 1500 papers on drug-induced liver injury (DILI) and herb-induced liver injury (HILI) were published in 2016, many of which have the potential to impact clinical practice. AREAS COVERED: Clinical studies and case series that lent themselves to new concepts or directions in diagnosing, preventing, and treating DILI were selected for inclusion. Epidemiology of DILI in large prospective registries was highlighted, including the US DILIN network and Spanish DILI registry...
August 3, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28766672/seabuckthorn-berry-polysaccharide-protects-against-carbon-tetrachloride-induced-hepatotoxicity-in-mice-via-anti-oxidative-and-anti-inflammatory-activities
#15
Wei Zhang, Xiaohui Zhang, Kai Zou, Jiming Xie, Shimin Zhao, Jingran Liu, Huan Liu, Jinling Wang, Yuzhen Wang
The berries of Seabuckthorn (Hippophae rhamnoides L.) are traditional medicinal foods that have been used by Tibetans and Mongolians for thousands of years. The polysaccharides are the main components of Seabuckthorn berries, possessing immune stimulating, anti-cancer and anti-fatigue activities. The present study focused on evaluating the protective effects and mechanisms of Seabuckthorn berry polysaccharide (SP) against carbon tetrachloride (CCl4)-induced hepatotoxicity. Mice were orally administrated with 50, 100 and 200 mg kg(-1) of SP once daily for 14 consecutive days prior to CCl4 challenge...
August 2, 2017: Food & Function
https://www.readbyqxmd.com/read/28763317/rocuronium-is-more-hepatotoxic-than-succinylcholine-in-vitro
#16
Martin Sauer, Ines Piel, Cristof Haubner, Georg Richter, Miriam Mann, Gabriele Nöldge-Schomburg, Thomas Mencke
BACKGROUND: The development of liver failure is a major problem in critically ill patients. The hepatotoxicity of many drugs, as one important reason for liver failure, is poorly screened for in human models. Rocuronium and succinylcholine are neuromuscular blocking agents used for tracheal intubation and for rapid-sequence induction. OBJECTIVE: We used an in-vitro test with a permanent cell line and compared rocuronium and succinylcholine for hepatotoxicity. DESIGN: In-vitro study...
September 2017: European Journal of Anaesthesiology
https://www.readbyqxmd.com/read/28762043/customised-in-vitro-model-to-detect-human-metabolism-dependent-idiosyncratic-drug-induced-liver-injury
#17
Laia Tolosa, Nuria Jiménez, Gabriela Pérez, José V Castell, M José Gómez-Lechón, M Teresa Donato
Drug-induced liver injury (DILI) has a considerable impact on human health and is a major challenge in drug safety assessments. DILI is a frequent cause of liver injury and a leading reason for post-approval drug regulatory actions. Considerable variations in the expression levels of both cytochrome P450 (CYP) and conjugating enzymes have been described in humans, which could be responsible for increased susceptibility to DILI in some individuals. We herein explored the feasibility of the combined use of HepG2 cells co-transduced with multiple adenoviruses that encode drug-metabolising enzymes, and a high-content screening assay to evaluate metabolism-dependent drug toxicity and to identify metabolic phenotypes with increased susceptibility to DILI...
July 31, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28758587/atypical-form-of-adult-onset-still-s-disease-with-distal-interphalangeal-joints-involvement
#18
Safaa Belghali, Nejla El Amri, Khadija Baccouche, Sadok Laataoui, Monia Bouzaoueche, Hela Zeglaoui, Elyes Bouajina
Distal interphalangeal (DIP) joints involvement in the adult-onset Still's disease (ASD) has been described in some publications but is rarely severe. We report severe DIP joints damages in a young patient with ASD. A 22 years old patient presented to our department complaining of inflammatory joints pain associated with prolonged fever and cutaneous rash. Physical examination identified polyarthritis and hepatosplenomegaly but no lymphadenopathies. After an extensive screening for neoplastic, infectious or hematologic diseases, the patient was finally diagnosed with ASD...
July 28, 2017: Current Rheumatology Reviews
https://www.readbyqxmd.com/read/28758238/design-synthesis-and-docking-study-of-pyrimidine-triazine-hybrids-for-gaba-estimation-in-animal-epilepsy-models
#19
Meeta Sahu, Nadeem Siddiqui, Mohd Javed Naim, Ozair Alam, Mohammad Shahar Yar, Vidushi Sharma, Sharad Wakode
A series of new pyrimidine-triazine hybrids (4a-t) was designed and synthesized, from which potent anticonvulsant agents were identified. Most of the compounds exhibited promising anticonvulsant activity against the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests, along with minimal motor impairment with higher safety compared to the standard drugs, phenytoin and carbamazepine. In the series, 5-(4-(4-fluorophenyl)-6-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4o) and 5-(6-(4-hydroxy-3-methoxyphenyl)-4-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4s) emerged as most potent anticonvulsant agents with median doses of 22...
July 31, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28750235/investigation-of-the-effect-of-plasma-albumin-levels-on-regorafenib-induced-hepatotoxicity-using-a-validated-liquid-chromatography-tandem-mass-spectrometry-method
#20
Yi Yun Pang, Yeong Lan Tan, Han Kiat Ho
Regorafenib is an oral multikinase inhibitor indicated for metastatic colorectal cancer and gastrointestinal stromal tumour. Due to its extensive plasma protein binding and low calculated hepatic extraction ratio, the hepatotoxicity observed with usage of the drug may be related to its plasma exposure. To investigate the highly dynamic free:bound drug concentration for regorafenib in the plasma, a bioanalytical liquid chromatography-tandem mass spectrometric assay was developed and validated in human plasma...
July 17, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
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