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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/29200830/notoginsenoside-r1-attenuates-high-glucose-induced-endothelial-damage-in-rat-retinal-capillary-endothelial-cells-by-modulating-the-intracellular-redox-state
#1
Chunlan Fan, Yuan Qiao, Minke Tang
The aim of this study was to examine whether Notoginsenoside R1 (NR1) attenuates high glucose-induced cell damage in rat retinal capillary endothelial cells (RCECs) and to explore the mechanisms involved. The exposure of rat RCECs to high concentration of glucose (30 mM) for 72 h led to significant cytotoxicity, including decreased cell viability, reduced mitochondrial DNA copy number, increased lactate dehydrogenase release and elevated apoptosis. NR1, when present in the culture medium, markedly attenuated the high glucose-induced cytotoxicity in rat RCECs...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29200829/andrographolide-enhanced-5-fluorouracil-induced-antitumor-effect-in-colorectal-cancer-via-inhibition-of-c-met-pathway
#2
Meng Su, Baoli Qin, Fang Liu, Yuze Chen, Rui Zhang
Colorectal cancer (CRC) is the third most common malignant neoplasm worldwide. 5-Fluorouracil (5-Fu) is the most important chemotherapeutic drug used for the treatment of CRC. However, resistance to 5-Fu therapies is a growing concern in CRC clinical practice recently. Andrographolide (Andro) is a main bioactive constituent of the herb Andrographis paniculata, which has various biological effects including anti-inflammation and antitumor activities. In the present study, we investigated the effects of combined Andro with 5-Fu against CRC HCT-116 cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29200828/fentanyl-induced-respiratory-depression-is-attenuated-in-pregnant-patients
#3
Xiaofei Cao, Shijiang Liu, Jie Sun, Min Yu, Yin Fang, Zhengnian Ding
Background: Respiratory depression is a complication of intravenous fentanyl administration. The effect of pregnancy on respiratory depression following opioid administration is unclear. This study investigated the effect of pregnancy on fentanyl-induced respiratory depression. Patients and methods: Female patients were divided into three groups (n=20 per group): control group (non-pregnant and scheduled for laparoscopic surgery), early pregnancy group (pregnant for 45-60 days and scheduled for abortion), and postpartum group (5-7 days postpartum scheduled for complete curettage of uterine cavity)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29200827/severe-hypertriglyceridemia-and-colchicine-intoxication-following-suicide-attempt
#4
Shaul Lev, David Snyder, Carmil Azran, Victor Zolotarsky, Arik Dahan
Colchicine overdose is uncommon but potentially life threatening. Due to its serious adverse systemic effects, overdose must be recognized and treated. We report a case of an 18-year-old female who ingested 18 mg (~0.4 mg/kg) of colchicine in a suicide attempt. The patient's clinical manifestations included abdominal cramps, vomiting, pancytopenia, hypocholesterolemia, and rhabdomyolysis. Two unique manifestations of toxicity in this patient were profound and persistent, severe hypertriglyceridemia and electrolyte imbalance, mainly hypophosphatemia, with no other evident cause except the colchicine intoxication...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29200826/anticancer-effect-of-dentatin-and-dentatin-hydroxypropyl-%C3%AE-cyclodextrin-complex-on-human-colon-cancer-ht-29-cell-line
#5
Ashwaq Shakir Al-Abboodi, Abdullah Rasedee, Ahmad Bustamam Abdul, Yun Hin Taufiq-Yap, Wafaa Abd Alwahed Alkaby, Mostafa Saddam Ghaji, Peter M Waziri, Mothanna Sadiq Al-Qubaisi
Introduction: Dentatin (DEN) (5-methoxy-2, 2-dimethyl-10-(1, 1-dimethyl-2propenyl) dipyran-2-one), a natural compound present in the roots of Clausena excavata Burm f, possesses pro-apoptotic and antiproliferative effects in various cancer cells. Because of its hydrophobicity, it is believed that its complexation with hydroxy-β-cyclodextrin (HPβCD) will make it a potent inhibitor of cancer cell growth. In the current work, the molecular mechanisms of apoptosis induced by DEN and DEN-HPβCD complex were demonstrated in human colon HT-29 cancer cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29200825/efficacy-and-safety-of-quadruple-therapy-including-tirofiban-in-the-treatment-of-chinese-nste-acs-patients-failing-to-receive-timely-percutaneous-coronary-intervention
#6
Lan Li, Zhenrong Ge, Dengke Zhang, Jun Kuang, Xiang Ma, Shubin Jiang
Background: Although it has been shown to be superior to simple antithrombotic drug therapy, most patients are unable to receive timely percutaneous coronary intervention (PCI) and are treated with conventional triple antithrombotic therapy (aspirin, clopidogrel, low-molecular-weight heparin). Here, we evaluate the efficacy and safety of adding low-dose tirofiban to this regimen. Methods: A total of 1,783 patient records (unable to receive PCI) indicating non-ST-segment elevation acute coronary syndrome (NSTE-ACS) were included...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29200824/pharmacodynamic-testing-and-new-validated-hplc-method-to-assess-the-interchangeability-between-multi-source-orlistat-capsules
#7
Abdel Naser Zaid, Nihal Zohud, Bushra E'layan, Tasneem Aburadi, Nidal Jaradat, Iyad Ali, Fatima Hussein, Mashhour Ghanem, Aiman Qaddomi, Yara Abu Zaaror
Background: Orlistat is an irreversible inhibitor of the lipase enzyme that prevents trigylcerides from being digested, thereby inhibiting triglyceride hydrolysis and absorption. The resultant reduced calorie uptake enables a positive effect on weight control. Systemic absorption of the drug is, therefore, not necessary for its mode of action. An alternative in vitro study (pharmacodynamic) has been introduced for this drug, as in vivo bioavailability studies are irrelevant with regard to the achievement of the product's intended purposes...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29184392/paeoniflorin-attenuates-incipient-diabetic-nephropathy-in-streptozotocin-induced-mice-by-the-suppression-of-the-toll-like-receptor-2-signaling-pathway
#8
Yun-Xia Shao, Xing-Xin Xu, Kun Wang, Xiang-Ming Qi, Yong-Gui Wu
Toll-like receptors (TLRs) may be involved in diabetic nephropathy (DN). Paeoniflorin (PF) is an effective Chinese traditional medicine with anti-inflammatory and immunoregulatory effects that may inhibit the TLR2 signaling pathway. In this study, we investigated the effects of PF on the kidneys of mice with streptozotocin-induced type 1 diabetes mellitus using TLR2 knockout mice (TLR2-/-) and wild-type littermates (C57BL/6J-WT). After 12 weeks of intraperitoneal injection of PF at doses of 25, 50, and 100 mg/kg once a day, diabetic mice had significantly reduced albuminuria and attenuated renal histopathology...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29184391/novel-production-method-of-innovative-antiangiogenic-and-antitumor-small-peptides-in-escherichia-coli
#9
Sarra Setrerrahmane, Jian Yu, Jingchao Hao, Heng Zheng, Hanmei Xu
Background: Developing innovative drugs with potent efficacy, specificity, and high safety remains an ongoing task in antitumor therapy development. In the last few years, peptide drugs have become attractive agents in cancer therapy. HM-3, mainly with antiangiogenic effect, and AP25, with an additional antiproliferative effect, are two peptides designed in our laboratory targeting αvβ3 and α5β1 integrins, respectively. The low molecular weight of the two peptides renders their recombinant expression very difficult, and the complicated structure of AP25 makes its chemical synthesis restricted, which presents a big challenge for its development...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29184390/erratum-quantum-mechanics-implementation-in-drug-design-workflows-does-it-really-help-corrigendum
#10
(no author information available yet)
[This corrects the article on p. 2551 in vol. 11.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29184389/baracle%C3%A2-vs-baraclude%C3%A2-for-48-weeks-in-patients-with-treatment-na%C3%A3-ve-chronic-hepatitis-b-a-comparison-of-efficacy-and-safety
#11
Do Young Kim, Ju Hyun Kim, Won Young Tak, Jong Eun Yeon, Joon Hyeok Lee, Jung Hwan Yoon, Youn Jae Lee, Byung Seok Lee, Byung Hoon Han, Han Chu Lee
Background and objective: Entecavir (ETV) is a standard of care for chronic hepatitis B (CHB). In a bioequivalence study, ETV from Dong-A ST (Baracle®) was found to have a pharmacokinetic profile equivalent to ETV from Bristol-Myers Squibb (BMS) (Baraclude®). The present study was conducted to evaluate the antiviral activity and safety of ETV from Dong-A ST in comparison to ETV from BMS in patients with CHB. Methods: In this multicenter, double-blind, active-controlled, stratified-randomized, parallel group, comparative trial, 118 treatment-naïve patients with CHB were randomly assigned to receive either 0...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29180852/in-silico-based-identification-of-human-%C3%AE-enolase-inhibitors-to-block-cancer-cell-growth-metabolically
#12
Jrhau Lung, Kuan-Liang Chen, Chien-Hui Hung, Chih-Cheng Chen, Ming-Szu Hung, Yu-Ching Lin, Ching-Yuan Wu, Kuan-Der Lee, Neng-Yao Shih, Ying Huang Tsai
Unlimited growth of cancer cells requires an extensive nutrient supply. To meet this demand, cancer cells drastically upregulate glucose uptake and metabolism compared to normal cells. This difference has made the blocking of glycolysis a fascinating strategy to treat this malignant disease. α-enolase is not only one of the most upregulated glycolytic enzymes in cancer cells, but also associates with many cellular processes or conditions important to cancer cell survival, such as cell migration, invasion, and hypoxia...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29180851/differences-of-statin-activity-in-2d-and-3d-pancreatic-cancer-cell-cultures
#13
Miglė Paškevičiūtė, Vilma Petrikaitė
Purpose: To evaluate the anticancer activity of lovastatin (LOVA), mevastatin (MEVA), pitavastatin (PITA), and simvastatin (SIMVA) in 2D and 3D models of three human pancreatic cancer cell lines (BxPC-3, MIA PaCa-2, and PANC-1). Methods: The effect of statins on cell viability was estimated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test. The activity of statins in 3D pancreatic cancer cell cultures was examined by measuring the size change of spheroids...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29180850/role-of-nebulized-glycopyrrolate-in-the-treatment-of-chronic-obstructive-pulmonary-disease
#14
REVIEW
Pierachille Santus, Dejan Radovanovic, Andrea Cristiano, Vincenzo Valenti, Maurizio Rizzi
In the upcoming years, the proportion of elderly patients with chronic obstructive pulmonary disease (COPD) will increase, according to the progressively aging population and the increased efficacy of the pharmacological treatments, especially considering the management of chronic comorbidities. The issue to prescribe an appropriate inhalation therapy to COPD patients with significant handling or coordination difficulties represents a common clinical experience; in the latter case, the choice of an inadequate inhalation device may jeopardize the adherence to the treatment and eventually lead to its ineffectiveness...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29180849/adjuvant-immunotherapy-of-dendritic-cells-and-cytokine-induced-killer-cells-is-safe-and-enhances-chemotherapy-efficacy-for-multiple-myeloma-in-china-a-meta-analysis-of-clinical-trials
#15
Yan Wang, Benji Lv, Ke Li, Anqi Zhang, Hong Liu
Objective: The aim of this study was to systematically evaluate the efficacy and safety of the combination of dendritic cells and cytokine-induced killer cells (DC-CIK) adjuvant immunotherapy and chemotherapy in the treatment of multiple myeloma (MM). Methods: Clinical trials were gathered by searching Web of Science, PubMed, Embase, Cochrane Library, Wanfang, and CNKI database. Outcome measurements including therapeutic efficacy, prognosis, immune function, and adverse events were extracted and evaluated...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29180848/safety-and-efficacy-of-the-addition-of-pertuzumab-to-t-dm1-%C3%A2-taxane-in-patients-with-her2-positive-locally-advanced-or-metastatic-breast-cancer-a-pooled-analysis
#16
REVIEW
Jing Zhang, Jinying Li, Chenjing Zhu, Yanlin Song, Fan Xia, Xuelei Ma
Background: The aim of this review was to systematically evaluate the safety and efficacy of the addition of pertuzumab to trastuzumab emtansine (T-DM1) ± taxane in patients with human epidermal growth factor receptor 2 (HER2)-positive, locally advanced breast cancer (LABC) or metastatic breast cancer (MBC). Materials and methods: Several databases were searched for relevant clinical trials. The study characteristics, details of adverse events (AEs) and details of treatment efficacy were extracted for analysis...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29158666/tenofovir-alafenamide-in-the-treatment-of-chronic-hepatitis-b-design-development-and-place-in-therapy
#17
REVIEW
Eiichi Ogawa, Norihiro Furusyo, Mindie H Nguyen
Tenofovir alafenamide (TAF), a novel prodrug of tenofovir (TFV), has been approved for the treatment of chronic hepatitis B virus (HBV) infection. TAF has been shown to be a potent inhibitor of HBV replication at a low dose, with high intracellular concentration and more than 90% lower systemic TFV concentration than tenofovir disoproxil fumarate (TDF). In two randomized, double-blind, multinational, Phase 3, non-inferiority trials for hepatitis B e antigen (HBeAg)-positive and -negative patients (primary analysis: 48 weeks), TAF 25 mg orally once-daily was not inferior to TDF 300 mg in achieving an HBV DNA level <29 IU/mL at week 48...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29158665/pharmacokinetics-and-tolerability-of-mb12066-a-beta-lapachone-derivative-targeting-nad-p-h-quinone-oxidoreductase-1-two-independent-double-blind-placebo-controlled-combined-single-and-multiple-ascending-dose-first-in-human-clinical-trials
#18
Seokuee Kim, SeungHwan Lee, Joo-Youn Cho, Seo Hyun Yoon, In-Jin Jang, Kyung-Sang Yu
MB12066 is a molecule derived from β-lapachone that shown effects on obesity in previous studies. The present studies were conducted to evaluate the tolerability and pharmacokinetics (PK) of MB12066 after the oral administration of single and multiple doses to healthy volunteers. The study comprised 2 independent, randomized, double-blind, placebo-controlled, combined single and multiple ascending dose first-in-human clinical trials to evaluate the safety, tolerability and PK of MB12066 in healthy Korean volunteers...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29158664/impact-of-baseline-blood-pressure-on-the-magnitude-of-blood-pressure-lowering-by-nifedipine-gastrointestinal-therapeutic-system-refreshing-the-wilder-s-principle
#19
Haijuan Hu, Jidong Zhang, Yan Wang, Zejun Tian, Demin Liu, Guangming Zhang, Guoqiang Gu, Hongmei Zheng, Ruiqin Xie, Wei Cui
Background: The objective of the study was to investigate the relationship between baseline blood pressure (BP) and the magnitude of BP reduction in patients with essential hypertension treated with nifedipine gastrointestinal therapeutic system (NGTS). Methods and patients: One hundred and thirty-eight patients with essential hypertension were enrolled in this prospective, single-arm, open-label study. NGTS was administered for 24 weeks to achieve target BP of 140/90 mmHg...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29158663/a-comparative-pharmacokinetic-and-tolerability-analysis-of-the-novel-orotic-acid-salt-form-of-tenofovir-disoproxil-and-the-fumaric-acid-salt-form-in-healthy-subjects
#20
Yu Kyong Kim, Mun Ju Choi, Tae Young Oh, Kyung-Sang Yu, SeungHwan Lee
A novel orotic acid salt form of tenofovir disoproxil (DA-2802) was developed and is expected to replace the fumaric acid salt form. The pharmacokinetic (PK) characteristics and tolerability profiles of DA-2802 were compared to those of tenofovir disoproxil fumarate (TDF, Viread(®)) in healthy subjects. A randomized, open-label, single-dose study was conducted in 36 healthy subjects using a two-treatment, two-period, and two-sequence crossover design. Subjects received a single oral dose of 319 mg DA-2802 or 300 mg TDF, during each period, with a 7-day washout...
2017: Drug Design, Development and Therapy
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