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Aloperine Inhibits Proliferation and Promotes Apoptosis in Colorectal Cancer Cells by Regulating the circNSUN2/miR-296-5p/STAT3 Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-25 Wei Han; Desong Kong; Qin Lu; Wei Zhang; Zhimin Fan
Background: Aloperine can regulate miR-296-5p/Signal Transducer and Activator of Transcription 3 (STAT3) pathway to inhibit the malignant development of colorectal cancer (CRC), but the regulatory mechanism is unclear. This study explored the upstream mechanism of Aloperine in reducing CRC damage from the perspective of the circRNA-miRNA-mRNA regulatory network. Methods: After treatment with gradient
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Breviscapine Pretreatment Inhibits Myocardial Inflammation and Apoptosis in Rats After Coronary Microembolization by Activating the PI3K/Akt/GSK-3β Signaling Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-25 Zhi-Qing Chen; You Zhou; Feng Chen; Jun-Wen Huang; Jing Zheng; Hao-Liang Li; Tao Li; Lang Li
Purpose: Coronary microembolization (CME) can cause myocardial inflammation, apoptosis and progressive cardiac dysfunction. On the other hand, breviscapine exerts a significant cardioprotective effect in many cardiac diseases although its role and the potential mechanisms in CME remain unclear. Therefore, the present study aimed to ascertain whether pretreatment with breviscapine could improve CME-induced
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Current Understanding on Perioperative Management in Lung Cancer: Implications for Anesthetic Considerations Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-25 Jian Wang; Lei Liu; Yuli Song; Jinghua Jiao; Yifan Zhong
Abstract: Narcotic drugs are often used to treat perioperative pain for patients with lung cancer. However, anesthetic management and narcotic substance use may have significant impacts on patients with lung cancer, including anti-cancer or promoting cancer effects. In this study, we summarize the effects of anesthetic management and its related substances on lung cancer. An evidence-based review of
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Effects of Sugammadex versus Neostigmine on Intraoperative Coagulation Profiles in Patients with Thyroidectomy Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-25 Dizhou Zhao; Jieyu Fang; Wei Xiong; Jun Lin; Wanmei Chen; Chujun Wu
Background: Sugammadex has been a revolutionary reversal of neuromuscular blockade. It is known to be highly efficient. However, a change in the coagulation profile is one of the most dangerous potential complications which is a concern for both surgeon and anesthetist. Bleeding may cause hypovolemic shock, hematoma, and so on. To investigate the effects of sugammadex on coagulation profiles in patients
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Predicting and Exploring the Mechanisms of Erzhi Pill in Prevention and Treatment of Osteoporosis Based on Network Pharmacology and Zebrafish Experiments Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-24 Zhiguo Zhong; Yuyun Li; Yan Chen; Wen Chen; Siyan Li; Xiaohua Lv; Shiying Luo
Background: Erzhi Pill (EZP), a traditional Chinese medicine (TCM) prescription, has been widely applied to improve bone metabolism and treat osteoporosis (OP) in China. However, its effective constituents and mechanisms remain unclear. Methods: By combining network pharmacology and zebrafish experiments, an integrative method was employed to address this problem. Firstly, the disease targets of OP
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Efficacy and Safety of Retinol Palmitate Ophthalmic Solution in the Treatment of Dry Eye: A Japanese Phase II Clinical Trial [Corrigendum] Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-24 Hiroshi Toshida; Toshinari Funaki; Koichi Ono; Nobuhito Tabuchi; Sota Watanabe; Tamotsu Seki; Hiroshi Otake; Takuji Kato; Nobuyuki Ebihara; Akira Murakami
Efficacy and Safety of Retinol Palmitate Ophthalmic Solution in the Treatment of Dry Eye: A Japanese Phase II Clinical Trial [Corrigendum]
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Danggui Buxue Decoction in the Treatment of Metastatic Colon Cancer: Network Pharmacology Analysis and Experimental Validation Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-24 Shi-Han Feng; Bin Zhao; Xue Zhan; Retsepile Motanyane; Shu-Mei Wang; Ao Li
Purpose: This study aimed to reveal Danggui Buxue Decoction (DBD) candidate targets and mechanisms in the treatment of metastatic colon cancer (MCC), using network pharmacology-based analyses and experimental validation. Methods: Traditional Chinese Medicine Systems Pharmacology (TCMSP) database query and text mining were used to screen active compounds in DBD, and the Swiss target prediction platform
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Glucocorticoid-Like Activity of Escin: A New Mechanism for an Old Drug Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-24 Luca Gallelli; Erika Cione; Tian Wang; Leiming Zhang
Abstract: Saponins are a group of compounds used in clinical practice in the management of several diseases. Escin is a natural mixture of triterpene saponins which mainly consist of several isoforms, in which the α- and β-escin are predominant. β-escin is the major active compound that exerts a therapeutic effect by relieving tissue edema, promoting venous drainage, and reducing inflammation. In this
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Convallatoxin Promotes M2 Macrophage Polarization to Attenuate Atherosclerosis Through PPARγ-Integrin αvβ5 Signaling Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-23 Yi Zhang; Xiujin Shi; Jialun Han; Wenxing Peng; Zhenwei Fang; Yang Zhou; Xiaoyu Xu; Jie Lin; Fucheng Xiao; Limin Zhao; Yang Lin
Introduction: As the primary immune cells, macrophages play a key role in atherosclerotic progression. M2 macrophage polarization has been reported to promote tissue repair and attenuate plaque formation upon the expression of anti-inflammatory factors. Convallatoxin (CNT) is a natural cardiac glycoside with anti-inflammatory pharmacological properties. However, whether CNT protects against atherosclerosis
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Dopamine-Mediated Vanillin Multicomponent Derivative Synthesis via Grindstone Method: Application of Antioxidant, Anti-Tyrosinase, and Cytotoxic Activities Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-23 Arunadevi Mani; Anis Ahamed; Daoud Ali; Saud Alarifi; Idhayadhulla Akbar
Purpose: This study aimed to determine the extent of contribution of dopamine to antioxidant and anti-tyrosinase activities, by dopamine addition to vanillin. This study achieved the synthesis of dopamine-associated vanillin Mannich base derivatives prepared via a one-step reaction involving a green chemistry approach, and investigation of antioxidant and anti-tyrosinase activities. Methods: Novel
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The Volatile Oil of Zanthoxylum bungeanum Pericarp Improved the Hypothalamic-Pituitary-Adrenal Axis and Gut Microbiota to Attenuate Chronic Unpredictable Stress-Induced Anxiety Behavior in Rats Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-22 Daneng Wei; Yafei Zhao; Mengmeng Zhang; Lei Zhu; Li Wang; Xing Yuan; Chunjie Wu
Background: Anxiety disorders (ADs) are the most prevalent mental disorders worldwide. Stress-induced activation of the hypothalamic-pituitary-adrenal (HPA) axis and dysbiosis of gut microbiota seem to contribute to the onset of ADs. This study was designed to investigate the ameliorative effect of volatile oil of Zanthoxylum bungeanum (VOZB) on chronic unpredictable stress (CUS) induced anxiety behavior
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Mechanism of Action of Xiaoyao San in Treatment of Ischemic Stroke is Related to Anti-Apoptosis and Activation of PI3K/Akt Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-22 Yue Xu; Weiyin Chen; Zeran Chen; Mengyuan Huang; Fang Yang; Yang Zhang
Objective: The traditional Chinese medicine (TCM) formulation Xiaoyao San (XYS) has a good clinical effect in treating ischemic stroke (IS). We explored the mechanism and material basis of XYS in IS treatment. Methods: Network pharmacology was used to construct a network of XYS components and IS targets. R software was used to analyze the biological process and pathway analysis of the targets of XYS
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The Effectiveness of Ruxolitinib for Acute/Chronic Graft-versus-Host Disease in Children: A Retrospective Study Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-22 Wenli Yang; Guanghua Zhu; Maoquan Qin; Zhigang Li; Bin Wang; Jun Yang; Tianyou Wang
Objective: This study aimed to evaluate the effectiveness of Ruxolitinib for acute/chronic graft-versus-host disease in children. Methods: This study was a retrospective trial. We analyzed the clinical characteristics of children who responded poorly to previous treatment for graft-versus-host disease (GVHD) and received ruxolitinib treatment after allogeneic hematopoietic stem cell transplantation
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Addition of Celebrex and Pregabalin to Ropivacaine for Posterior Spinal Surgery: A Randomized, Double-Blinded, Placebo-Controlled Trial Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-22 Ye Zhang; Bin He; Jinqiu Zhao; Muzi Zhang; Qinsong Ren; Wei Zhang; Shuai Xu; Zhengxue Quan; Yunsheng Ou
Background: Serious pain commonly occurs after posterior spinal surgery. This study aims to evaluate the effect of preemptive and multimodal analgesia using celebrex, pregabalin and ropivacaine on pain control after this surgery. Methods: Ninety-three patients undergoing posterior spinal surgery were enrolled in this prospective, randomized, double-blind, placebo-controlled clinical trial. All patients
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The Risks of miRNA Therapeutics: In a Drug Target Perspective Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-22 Song Zhang; Zhujun Cheng; Yanan Wang; Tianyu Han
Abstract: RNAi therapeutics have been growing. Patisiran and givosiran, two siRNA-based drugs, were approved by the Food and Drug Administration in 2018 and 2019, respectively. However, there is rare news on the advance of miRNA drugs (another therapeutic similar to siRNA drug). Here we report the existing obstacles of miRNA therapeutics by analyses for resources available in a drug target perspective
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The Effectiveness and Safety of Intravenous Dexmedetomidine of Different Concentrations Combined with Butorphanol for Post-Caesarean Section Analgesia: A Randomized Controlled Trial Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-18 Shijiang Liu; Peipei Peng; Youli Hu; Cunming Liu; Xiaofei Cao; Chun Yang; Mei Gao
Purpose: The present study aimed to determine the effectiveness of intravenous dexmedetomidine of different concentrations and to evaluate its maternal and neonatal safety when combined with butorphanol in parturients undergoing cesarean section. Patients and Methods: A total of 114 parturients between 24 and 43 years of age, with singleton pregnancy who underwent elective cesarean section under epidural
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Trans-Cinnamaldehyde Increases Random Pattern Flap Survival Through Activation of the Nitric Oxide Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-18 Xiaobin Luo; Bin Zhao; Baoxia Chen; Hongyu Chen; Tao Han; Najeeb Bassam Najeeb Bsoul; Hede Yan
Background: The application of random pattern skin flaps is limited in plastic surgery reconstruction due to necrosis. Trans-cinnamaldehyde has antibacterial, anticancer, and antioxidant properties. In this study, we aimed to investigate the effect of trans-cinnamaldehyde on skin flap survival and its possible mechanism regarding nitric oxide. Materials and Methods: One hundred forty male Sprague-Dawley
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Thiazole-Based Thiosemicarbazones: Synthesis, Cytotoxicity Evaluation and Molecular Docking Study Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-17 Sobhi M Gomha; Hyam A Abdelhady; Doaa ZH Hassain; Aboubakr H Abdelmonsef; Mohamed El-Naggar; Mahmoud M Elaasser; Huda K Mahmoud
Introduction: Hybrid drug design has developed as a prime method for the development of novel anticancer therapies that can theoretically solve much of the pharmacokinetic disadvantages of traditional anticancer drugs. Thus a number of studies have indicated that thiazole-thiophene hybrids and their bis derivatives have important anticancer activity. Mammalian Rab7b protein is a member of the Rab GTPase
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Pharmacokinetic and Pharmacodynamic Comparison of Two Formulations of a Fixed-Dose Combination of Gemigliptin/Rosuvastatin 50/20 mg: A Randomized, Open-Label, Single-Dose, Two-Way Crossover Study Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-17 Eunsol Yang; Hyounggyoon Yoo; In-Jin Jang; Kyung-Sang Yu; SeungHwan Lee
Purpose: A fixed-dose combination (FDC) of gemigliptin/rosuvastatin 50/20 mg as a monolayer tablet has been used to treat patients with both type 2 diabetes mellitus and dyslipidemia. To improve the stability of the FDC, a new FDC formulation as a bilayer tablet was developed. This study aimed to compare the pharmacokinetics (PKs) and pharmacodynamics (PDs) of the FDC of gemigliptin/rosuvastatin 50/20
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Progress in Clinical Research on Gonadotropin-Releasing Hormone Receptor Antagonists for the Treatment of Prostate Cancer Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-16 Yi-Fu Liu; Sheng-Qiang Fu; Yu-Chang Yan; Bin-Bin Gong; Wen-Jie Xie; Xiao-Rong Yang; Ting Sun; Ming Ma
Abstract: Gonadotropin-releasing hormone (GnRH) receptor agonists are still the most commonly used androgen deprivation treatment (ADT) drugs for prostate cancer in clinical practice. Currently, the GnRH receptor antagonists used for endocrine therapy for prostate cancer primarily include degarelix and relugolix (TAK-385). The former is administered by subcutaneous injection, while the latter is an
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Safety, Tolerability, and Pharmacokinetics of Ibuprofenamine Hydrochloride Spray (NSAIDs), a New Drug for Rheumatoid Arthritis and Osteoarthritis, in Healthy Chinese Subjects Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-16 Panpan Xie; Wei Xue; Wenyuan Qi; Yang Li; Lei Yang; Zhaojun Yang; Aixin Shi
Background: Ibuprofenamine hydrochloride spray is novel transdermal nonsteroidal anti-inflammatory drugs (NSAIDs), under clinical development for the treatment of Rheumatoid Arthritis and Osteoarthritis as a novel transdermal drug. Methods: A single and multiple ascending dose study investigated the safety, tolerability and pharmacokinetics of ibuprofenamine hydrochloride in healthy Chinese subjects
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Treatment of Severe Acute Bacterial Keratitis in Rabbits Using Continuous Topical Ocular Instillation with Norvancomycin Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-16 Wenxiang Lin; Libei Zhao; Qian Tan; Ding Lin
Purpose: Efficacy of norvancomycin (NVCM) through continuous topical ocular instillation drug delivery (CTOIDD) system for treating severe acute bacterial keratitis infection with Staphylococcus aureus was investigated. Methods: Rabbits with bacterial keratitis were treated using CTOIDD with NVCM (n=13), topical NVCM eye drops (n=11), and CTOIDD with saline (n=8). Clinical signs of keratitis in all
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Effect of Different Dosage Frequency of Polymyxin B on Rat Nephrotoxicity Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-16 Wenrui Sun; Binchuan Hu; Xiaoshan Zhang; Yuzhen Wang; Zheng Xiang; Guanyang Lin
Background: Polymyxin B, as the final treatment against multidrug-resistant Gram-negative bacilli, is widely used in clinical practice. However, little is known about the nephrotoxicity of polymyxin B. The purpose of this study was to elucidate the relationship between polymyxin B nephrotoxicity and daily administration frequency. Methods: Sprague–Dawley rats were randomly divided into three groups:
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Preparation, Characterization and in vitro/in vivo Evaluation of Lovastatin-Loaded PLGA Microspheres by Local Administration for Femoral Head Necrosis Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-16 Yang Sun; Di Long
Background: The present work is an effort to develop a novel locally injection LVTT-loaded PLGA microspheres (LVTT-PLGA-MS) on the treatment of rabbits with femoral head necrosis (FHN). Methods: LVTT-loaded PLGA microspheres (LVTT-PLGA MS) were prepared by an emulsion-solvent evaporation method. The physicochemical properties of LVTT-PLGA-MS were investigated to ensure that they have good qualities
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Nephroprotective Effect of Adropinin Against Streptozotocin-Induced Diabetic Nephropathy in Rats: Inflammatory Mechanism and YAP/TAZ Factor Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-16 Ling Guo; Bei Jiang; Dengren Li; Xiaoyan Xiao
Background: Diabetic Nephropathy remains a major cause of morbidity and mortality in patients suffering from renal dysfunction. This study accessed the nephroprotective role of Adropinin against streptozotocin (STZ) induced diabetic nephropathy in rats and scrutinizes the possible mechanism of action. Methods: STZ (45 mg/kg) dose was used for inducing diabetic nephropathy (DN) and rats were divided
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Effects of Quercetin on the Efficacy of Various Chemotherapeutic Drugs in Cervical Cancer Cells Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-15 Wenbin Xu; Shangdan Xie; Xin Chen; Shuya Pan; Hongfei Qian; Xueqiong Zhu
Purpose: This study aimed to investigate the effects of quercetin on the efficacy of various chemotherapeutic drugs in cervical cancer cells. Methods: All drug experiments were performed in HeLa and SiHa cells. The cell viability was detected by Cell Counting Kit-8 assay, and cell proliferation was estimated by bromodeoxyuridine assay. CompuSyn software was utilized to calculate the combination index
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Self-Nanoemulsifying Drug Delivery System of Genkwanin: A Novel Approach for Anti-Colitis-Associated Colorectal Cancer Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-12 Hua-Feng Yin; Chun-Ming Yin; Ting Ouyang; Shu-Ding Sun; Wei-Guo Chen; Xiao-Lin Yang; Xin He; Chun-Feng Zhang
Purpose: The aim of the present study was to develop an optimized Genkwanin (GKA)-loaded self-nanoemulsifying drug delivery system (SNEDDS) formulation to enhance the solubility, intestinal permeability, oral bioavailability and anti-colitis-associated colorectal cancer (CAC) activity of GKA. Methods: We designed a SNEDDS comprised oil phase, surfactants and co-surfactants for oral administration of
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Magnesium Isoglycyrrhizinate Alleviates Arsenic Trioxide-Induced Cardiotoxicity: Contribution of Nrf2 and TLR4/NF-κB Signaling Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-12 Bin Zheng; Yakun Yang; Jinghan Li; Jing Li; Saijie Zuo; Xi Chu; Shan Xu; Donglai Ma; Li Chu
Purpose: Magnesium isoglycyrrhizinate (MgIG), a single stereoisomer magnesium salt of glycyrrhizic acid, has beneficial effects on the cardiovascular system through anti-inflammatory, anti-oxidation, and anti-apoptotic actions. However, MgIG has not been shown to provide protection against cardiotoxicity induced by arsenic trioxide (ATO). This study aims to demonstrate the protection of MgIG against
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Budesonide/Formoterol Anti-Inflammatory Reliever and Maintenance or Fluticasone Propionate/Salmeterol Plus as-Needed, Short-Acting β2 Agonist: Real-World Effectiveness in patients Without Optimally Controlled asthma (REACT) Study [Corrigendum] Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-12 Shih-Lung Cheng; Ming-Lin Ho; Yun-Fa Lai; Hao-Chien Wang; Jeng-Yuan Hsu; Shih-Feng Liu; Ming-Shyang Huang; Cheng-Hung Lee; Ching-Hsiung Lin; Liang-Wen Hang; Yu-Chih Liu; Kuang-Yao Yang; Jia-Horng Wang
Budesonide/Formoterol Anti-Inflammatory Reliever and Maintenance or Fluticasone Propionate/Salmeterol Plus as-Needed, Short-Acting β2 Agonist: Real-World Effectiveness in patients Without Optimally Controlled asthma (REACT) Study [Corrigendum]
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Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry for Simultaneous Determination of Antipsychotic Drugs in Human Plasma and Its Application in Therapeutic Drug Monitoring Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-12 Yingjie Qi; Guangxuan Liu
Purpose: We developed and validated an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for simultaneous therapeutic drug monitoring (TDM) and clinical pharmacokinetic antipsychotic drugs: clozapine (CLP), chlorpromazine (CPZ), risperidone (RPD), paliperidone (PLD), quetiapine (QTP;), aripiprazole (APZ), dehydroaripiprazole (DAP), olanzapine (OZP), ziprasidone (ZRD)
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Synergistic Anticancer Strategy of Sonodynamic Therapy Combined with PI-103 Against Hepatocellular Carcinoma Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-11 Huajing Yang; Hui Jing; Xue Han; Haoyan Tan; Wen Cheng
Purpose: Sonodynamic therapy (SDT) is considered a promising therapeutic strategy for the effective elimination of cancer cells. However, developing novel sonosensitizers with potentially high SDT efficacy remains a considerable challenge. Herein, we utilized near-infrared dye IR820 nanobubbles (NBs) combined with a dual PI3K/mTOR inhibitor PI-103 for the SDT treatment of hepatocellular carcinoma (HCC)
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L-Cysteine Provides Neuroprotection of Hypoxia-Ischemia Injury in Neonatal Mice via a PI3K/Akt-Dependent Mechanism Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-11 Tingting Li; Jiangbing Li; Tong Li; Yijing Zhao; Hongfei Ke; Shuanglian Wang; Dexiang Liu; Zhen Wang
Background: Previous work within our laboratory has revealed that hydrogen sulfide (H2S) can serve as neuroprotectant against brain damage caused by hypoxia-ischemia (HI) exposure in neonatal mice. After HI insult, activation of the phosphatidylinositol-3-kinase (PI3K)/protein kinase B (Akt) signaling pathway has been shown to be implicated in neuro-restoration processes. The goal of the current study
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Loganin Attenuates Septic Acute Renal Injury with the Participation of AKT and Nrf2/HO-1 Signaling Pathways Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-11 Jin Zhang; Changsong Wang; Kai Kang; Haitao Liu; Xiaowei Liu; Xiaonan Jia; Kaijiang Yu
Purpose: Sepsis, a destructive inflammatory response syndrome, is the principal reason to induce death in the intensive care unit. Loganin has been proved to possess the property of anti-inflammation, antioxidant, neuroprotection, and sedation. The primary aim of this study was to evaluate whether Loganin could alleviate acute kidney injury (AKI) during sepsis and investigate the latent mechanisms
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EGCG Regulates Cell Apoptosis of Human Umbilical Vein Endothelial Cells Grown on 316L Stainless Steel for Stent Implantation Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-11 Jinpeng Wang; Yue Wang; Yuyi Zhao; Jinbin Zhao; Beilin Zhang; Kun Xu
Background: Nowadays, medical grade 316L stainless steel (316L SS) is being widely used for intravascular stents, and the drug-eluting stent (DES) system is able to significantly reduce the occurrences of in-stent restenosis. But the drugs and the polymer coating used in DES potentially induce the forming of late stent thrombosis. In order to reduce the occurrence of ISR after stent implantation, the
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Long Noncoding RNA SOX2-OT Aggravates Doxorubicin-Induced Apoptosis of Cardiomyocyte by Targeting miR-942-5p/DP5 Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-11 Haining Wang; Xiule Lin; Jilin Li; Guoning Zeng; Tan Xu
Background: Long non-coding RNAs (LncRNAs) play important roles in doxorubicin (DOX)-induced apoptosis of cardiomyocytes. However, the function of lncRNA SOX2-OT is unclear. This study was carried out to investigate the function of SOX2-OT in doxorubicin-induced cardiomyocyte apoptosis. Methods: qRT-PCR and immunoblotting were used to detect the expression levels of SOX2-OT, miR-942-5p and death protein-5
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Profile of Enfortumab Vedotin in the Treatment of Urothelial Carcinoma: The Evidence to Date Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-11 Mohamad Moussa; Athanasios Papatsoris; Mohamed Abou Chakra; Athanasios Dellis
Abstract: Nowadays the therapeutic landscape for advanced and metastatic urothelial carcinoma continues to evolve. The recent regulatory approval of enfortumab vedotin (EV) for the treatment of advanced urothelial cancer confirms the evolving role of antibody-drug conjugates. EV demonstrates a favorable profile in heavily pretreated patients with locally advanced or metastatic urothelial carcinoma
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Effect of Evodiamine on Rat Colonic Hypermotility Induced by Water Avoidance Stress and the Underlying Mechanism Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-10 HaiXia Ren; FangTing Yuan; Wei Tan; YiJuan Ding; Ping An; HeSheng Luo
Background and Aim: EVO is a natural alkaloid that reportedly has potential value in regulating gastrointestinal motility, but this conclusion remains controversial, and the molecular mechanism is unclear. In this study, we aimed to explore the effect of short-chain fatty acids on rat colonic hypermotility induced by water avoidance stress and the underlying mechanism. Methods: We constructed a hypermotile
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Zafirlukast in Combination with Pseudohypericin Attenuates Spinal Cord Injury and Motor Function in Experimental Mice [Corrigendum] Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-09 Xiao-Gang Chen; Fu Hua; Shou-Guo Wang; Yong-Yi Xu; Hai-Tao Yue; Jin Sun
Zafirlukast in Combination with Pseudohypericin Attenuates Spinal Cord Injury and Motor Function in Experimental Mice [Corrigendum]
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Development and Characterization of PLGA Nanoparticle-Laden Hydrogels for Sustained Ocular Delivery of Norfloxacin in the Treatment of Pseudomonas Keratitis: An Experimental Study Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-05 Rana M Gebreel; Noha A Edris; Hala M Elmofty; Mina I Tadros; Mohamed A El-Nabarawi; Doaa H Hassan
Aim: Norfloxacin (NFX) has low ocular bioavailability. The current work aimed to develop NFX-loaded nanoparticle (NP)-laden hydrogels to improve the ocular potential of NFX, minimize the need for frequent instillations and lower undesirable side effects. Methods: NFX-loaded NPs were developed via the double-emulsion/solvent evaporation technique, according to 21 .41 full factorial design, using two
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Design, Synthesis, Molecular Modelling, and Biological Evaluation of Oleanolic Acid-Arylidene Derivatives as Potential Anti-Inflammatory Agents Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-04 Reyaz Hassan Mir; Goutami Godavari; Nasir Ali Siddiqui; Bilal Ahmad; Ramzi A Mothana; Riaz Ullah; Omer M Almarfadi; Sanjay M Jachak; Mubashir Hussain Masoodi
Introduction: Oleanolic acid, a pentacyclic triterpenic acid, is widely distributed in medicinal plants and is the most commonly studied triterpene for various biological activities, including anti-allergic, anti-cancer, and anti-inflammatory. Methods: The present study was carried out to synthesize arylidene derivatives of oleanolic acid at the C-2 position by Claisen Schmidt condensation to develop
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Thiazolidine Derivatives Attenuate Carrageenan-Induced Inflammatory Pain in Mice Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-04 Zulkifal Malik; Muzaffar Abbas; Lina Tariq Al Kury; Fawad Ali Shah; Mahboob Alam; Arif-ullah Khan; Humaira Nadeem; Saad Alghamdi; Muhammad Umar Khayam Sahibzada; Shupeng Li
Background: Peripheral inflammation leads to the development of persistent thermal hyperalgesia and mechanical allodynia associated with increased expression of interleukin-1β (IL-1β) in the spinal cord. The aim of the present study was to investigate the effects of thiazolidine derivatives, 1b ([2-(2-hydroxyphenyl)-1,3-thiazolidin-4-yl](morpholin-4-yl)methanone) and 1d (2-hydroxy-4-{[2-(2-hydroxyphenyl)-1
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Irisin Protects Against Hind Limb Ischemia Reperfusion Injury Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-04 Ayşegül Küçük; Yücel Polat; Aydan Kılıçarslan; Nuran Süngü; Hakan Kartal; Ali Doğan Dursun; Mustafa Arslan
Aim: The aim of this study was to evaluate the effects of irisin in a murine model of hind limb ischemia reperfusion (I/R). Methods: The mice were divided into four groups (n = 6 in each group): control, irisin, ischemia reperfusion (I/R), and irisin-ischemia reperfusion (I–I/R). Irisin (0.5 μg.g− 1, intraperitoneally [i.p.]) was administered 30 min before the I/R procedure. After 2 h of ischemia and
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New Approach in Ocular Drug Delivery: In vitro and ex vivo Investigation of Cyclodextrin-Containing, Mucoadhesive Eye Drop Formulations Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-02-03 Tivadar Bíró; Alexandra Bocsik; Bisera Jurišić Dukovski; Ilona Gróf; Jasmina Lovrić; Ildikó Csóka; Mária A Deli; Zoltán Aigner
Background: Optimal transcorneal penetration is necessary for ocular therapy; meanwhile, it is limited by the complex structure and defensive mechanisms of the eye. Antimicrobial stability of topical ophthalmic formulations is especially important. According to previous studies, the mostly used preservative, benzalkonium-chloride is irritative and toxic on corneal epithelial cells; therefore, novel
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Therapeutic Effects of Modified Gengnianchun Formula on Stress-Induced Diminished Ovarian Reserve Based on Experimental Approaches and Network Pharmacology [Erratum] Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-27 Lingyun Gao; Yang Zhang; Huangfang Xu; Fangui Zhao; Wenjun Wang
Therapeutic Effects of Modified Gengnianchun Formula on Stress-Induced Diminished Ovarian Reserve Based on Experimental Approaches and Network Pharmacology [Erratum]
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A Retrospective Observational Study of Anlotinib in Patients with Platinum-Resistant or Platinum-Refractory Epithelial Ovarian Cancer Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-27 Qingli Cui; Yanhui Hu; Dongyang Ma; Huaimin Liu
Objective: Anlotinib, an oral small-molecular tyrosine kinase inhibitor (TKI) on tumor angiogenesis and growth, has a wide spectrum of inhibitory effects on targets such as vascular endothelial growth factor receptors 2/3 (VEGFR2/3), etc. The efficacy and safety of anlotinib in the treatment of platinum-resistant or platinum-refractory ovarian cancer were evaluated. Patients and Methods: Patients with
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Tezepelumab as an Emerging Therapeutic Option for the Treatment of Severe Asthma: Evidence to Date Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-27 Zachariah L Dorey-Stein; Kartik V Shenoy
Abstract: Asthma is a complex heterogeneous disease defined by chronic inflammation of the airways. Patients present with wheezing, chest tightness, cough and shortness of breath. Bronchial hyperresponsiveness and variable expiratory airflow limitation are hallmark features. About 3.6– 6.1% of patients, despite receiving high-dose inhaled corticosteroids (ICS) and a second controller medication, report
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CircNRIP1 Modulates the miR-515-5p/IL-25 Axis to Control 5-Fu and Cisplatin Resistance in Nasopharyngeal Carcinoma Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-27 Junwu Lin; Hong Qin; Yue Han; Xinghua Li; YuJuan Zhao; Guangsheng Zhai
Background: The development of drug resistance leads many NPC patients to experience disease relapse following the completion of chemotherapy. It is thus essential that the mechanistic basis for such chemoresistance be clarified in an effort to identify approaches to sensitizing NPC tumors to treatment with cisplatin and related agents. Methods: A qRT-PCR approach was used to measure the expression
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Administration of Dexmedetomidine Does Not Produce Long-Term Protective Effect on Testicular Damage Post Testicular Ischemia-Reperfusion Injury Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-27 Jing Xiao; Wenbo Wan; Ying Zhang; Jun Ma; Lin Yan; Yukun Luo; Jie Tang
Background: After surgical correction of testicular torsion, up to 68% of ipsilateral testes undergo atrophy due to ischemia-reperfusion injury (IRI). Recent studies have shown that dexmedetomidine (Dex) alleviates IRI in various vital organs. However, those studies evaluated its protective effect on short-term reperfusion. Purpose: We aimed to investigate whether Dex has a long-term protective effect
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Phenotyping Study of Cyclophosphamide 4-Hydroxylation in Malay Cancer Patients Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-26 Yesi Ihdina Fityatal Hasanah; Yahdiana Harahap; Denni Joko Purwanto
Background: Cyclophosphamide (CP) is an anticancer alkylating group (nitrogen mustard) and a prodrug that will be metabolized to form its active metabolite, 4-hydroxycyclophosphamide (4-OHCP). The various enzymes involved in its bioactivation can cause a wide range of CP expression and activity among patients and ultimately affect the metabolism, efficacy and toxicity of this drug. The effectiveness
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Gypenosides Inhibit Inflammatory Response and Apoptosis of Endothelial and Epithelial Cells in LPS-Induced ALI: A Study Based on Bioinformatic Analysis and in vivo/vitro Experiments Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-25 Qing Tu; Yabing Zhu; Yuan Yuan; Long Guo; Lu Liu; Liangfang Yao; Yun Zou; Jinbao Li; Feng Chen
Introduction: Severe inflammatory response leads to poor prognosis of acute lung injury (ALI), the role of gypenosides (GPs) on ALI is not fully clear. The study aimed at investigating the effects of GPs on ALI. Methods: We firstly established LPS-induced ALI mice model. Then, we tested whether GPs contributed to alleviate inflammatory response and lung injury of ALI in vivo. In order to identify specific
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Physcion Protects Rats Against Cerebral Ischemia-Reperfusion Injury via Inhibition of TLR4/NF-kB Signaling Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-25 Xiaobo Dong; Lei Wang; Guangrong Song; Xu Cai; Wenxin Wang; Jiaqi Chen; Gesheng Wang
Background: Ischemic stroke (IS) is characterized by the rapid loss of brain function due to ischemia. Physcion has been found to have a neuroprotective effect against cerebral ischemia-reperfusion (I/R) injury. However, the mechanism by which physcion regulates cerebral I/R injury remains largely unknown. Methods: An oxygen-glucose deprivation/reperfusion (OGD/R) model in SH-SY5Y cells and a rat cerebral
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Effects of Caffeic Acid and Its Derivatives on Bone: A Systematic Review Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-22 Sophia Ogechi Ekeuku; Kok-Lun Pang; Kok-Yong Chin
Purpose: Caffeic acid is a metabolite of hydroxycinnamate and phenylpropanoid, which are commonly synthesized by all plant species. It is present in various food sources that are known for their antioxidant properties. As an antioxidant, caffeic acid ameliorates reactive oxygen species, which have been reported to cause bone loss. Some studies have highlighted the effects of caffeic acid against bone
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Paeoniflorin Sensitizes Breast Cancer Cells to Tamoxifen by Downregulating microRNA-15b via the FOXO1/CCND1/β-Catenin Axis Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-22 Yanhong Wang; Qian Wang; Xibei Li; Gongwen Luo; Mou Shen; Jia Shi; Xueliang Wang; Lu Tang
Background: Paeoniflorin (Pae) possesses anti-tumor activity in various malignancies. However, it is unclear whether Pae plays a sensitizer role in breast cancer (BC) and the molecular mechanisms involved in this process. Our oligonucleotide microarray revealed that microRNA (miR)-15b is the most significantly downregulated miRNA in MCF-7/4-hydroxytamoxifen (4-OHT) cells treated with Pae. This paper
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Gracillin Isolated from Reineckia carnea Induces Apoptosis of A549 Cells via the Mitochondrial Pathway Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-20 Jianqiong Yang; Ling Cao; Yamei Li; Hai Liu; Minhong Zhang; Huamou Ma; Biao Wang; Xiaoliang Yuan; Qian Liu
Background: Reineckia carnea is commonly used to treat cough, pneumonia and other diseases in China. In our previous study, it was found that the ethanol extracts of Reineckia carnea have a strong inhibitory effect on the proliferation of human lung cancer A549 cells. Here, we isolated gracillin from ethanol extracts for the first time. Purpose: Clarify the antiproliferation effect of gracillin on
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Galangin Improved Non-Alcoholic Fatty Liver Disease in Mice by Promoting Autophagy [Corrigendum] Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-20 Xinxu Zhang; Yuanyuan Deng; Juan Xiang; Huixia Liu; Jiani Zhang; Jie Liao; Ke Chen; Bo Liu; Jun Liu; Ying Pu
Acknowledgments This work was supported by Youth Program of National Natural Science Foundation of China (21708050), Hunan Provincial Health Committee’s General Subsidy Project (20200100), General Program of National Natural Science Foundation of China (8187032317) and In-hospital Youth Fund of Xiangya Hospital of Central South University (2015Q03). Read the original article
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Clinical Significance of Continuable Treatment with Nintedanib Over 12 Months for Idiopathic Pulmonary Fibrosis in a Real-World Setting Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-18 Motoyasu Kato; Shinichi Sasaki; Misa Tateyama; Yuta Arai; Hiroaki Motomura; Issei Sumiyoshi; Yusuke Ochi; Junko Watanabe; Hiroaki Ihara; Shinsaku Togo; Kazuhisa Takahashi
Purpose: The INPULSIS-ON study suggested the safety and tolerability of long-term nintedanib treatment for idiopathic pulmonary fibrosis (IPF). However, there are no real-world studies on long-term nintedanib treatment. The main aim of the study was to investigate the efficacy and the tolerability of long-term treatment with nintedanib for IPF in clinical practice. Patients and Methods: This retrospective
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H2O2-Inactivated Salmonella typhimurium RE88 Strain as a New Cancer Vaccine Carrier: Evaluation in a Mouse Model of Cancer Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-15 Yingzi Fan; Tingting Bai; Yaomei Tian; Bailing Zhou; Yuanda Wang; Li Yang
Purpose: This study aimed to describe a novel cancer vaccine developed using H2O2-inactivated Salmonella typhimurium RE88 [with deletions of AroA (the first enzyme in the aromatic amino acid biosynthesis pathway) and DNA adenine methylase] as the carrier. Methods: The pVLT33 plasmid was used to engineer an RE88 strain induced to express ovalbumin (OVA) by isopropylthiogalactoside (RE88-pVLT33-OVA)
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Quaternary Lidocaine Derivatives: Past, Present, and Future Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-14 Qi Wang; Yujun Zhang; Jin Liu; Wensheng Zhang
Abstract: Local anesthetics have the advantage of complete analgesia with fewer side effects compared to systemic analgesics. However, their clinical use is limited due to their short duration of action. Thus, local anesthetics with fast onset, long duration of action, selective nociceptive block, and low local and systemic toxicity are highly desirable. In the past electrophysiological studies, quaternary
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Bioequivalence and Pharmacokinetic Profiles of Generic and Branded Obeticholic Acid in Healthy Chinese Subjects Under Fasting and Fed Conditions Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-14 Meng-Na Wang; Hai-Tao Yu; Ya-Qian Li; Yun Zeng; Shuang Yang; Guo-Ping Yang; Qi Pei; Jie Huang
Objectives: This study was conducted to evaluate the bioequivalence (BE) of a generic form of obeticholic acid (OCA) and OcalivaTM under fasting and fed conditions and to determine the effects of food on the pharmacokinetic (PK) profiles of OCA in healthy Chinese subjects. Methods: A randomized, single-dose, three-sequence, three-period, partial replicated crossover study was conducted with a 21-day
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Combination of Sodium Cantharidinate with Cisplatin Synergistically Hampers Growth of Cervical Cancer Drug Des. Dev. Ther. (IF 3.216) Pub Date : 2021-01-13 Xiangxun Chen; Mengxi Zhou; Wenjie Fan; Mingwei Yang; Lin Yang
Background: Sodium cantharidinate (SC) has been broadly applied in lung cancer treatment in China, while its specific function in cervical cancer (CC), a great contributor to death of female reproductive system cancers, remains unclear. Our research evaluated the anti-tumor effects of SC in CC and the mechanism involved. Methods: First, cisplatin (DDP)-resistant Caski-1 and ME180 cell lines were developed
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