489,924 results match your criteria drug regulation

Leojaponin inhibits NLRP3 inflammasome activation through restoration of autophagy via upregulating RAPTOR phosphorylation.

J Ethnopharmacol 2021 Jun 9:114322. Epub 2021 Jun 9.

Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education; Yunnan Provincial Center for Research & Development of Natural Products; School of Chemical Science and Technology, Yunnan University, Kunming, 650091, China. Electronic address:

Ethnopharmacological Relevance: Duan Teng Yimu decoction is a Chinese herbal medicine compound with proven therapeutic effects on inflammasome-related diseases, such as rheumatoid arthritis. This decoction consists of three Chinese herbal medicines, including Leonurus japonicus (L. japonicus), which promotes the blood circulation and exhibits detumescence activity, traditionally curing gynecologic and inflammasome diseases. Read More

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p53 regulated senescence mechanism and role of its modulators in age-related disorders.

Biochem Pharmacol 2021 Jun 9:114651. Epub 2021 Jun 9.

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research- Raebareli, New Transit Campus, Bijnor-Sisendi Road, Sarojini Nagar, Near CRPF Base Camp, Lucknow Uttar Pradesh, 226301, India. Electronic address:

Multiple co-morbidities are associated with age, and there is a need for the broad-spectrum drug to prevent multiple regimens that may cause an adverse effect in the geriatric population. Cellular senescence is a primary mechanism for ageing in various tissues. p53, a tumor suppressor protein, plays a significant role in forming DNA damage foci and post different stress responses. Read More

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Emamectin benzoate induced enzymatic and transcriptional alternation in detoxification mechanism of predatory beetle Paederus fuscipes (Coleoptera: Staphylinidae) at the sublethal concentration.

Ecotoxicology 2021 Jun 11. Epub 2021 Jun 11.

Hubei Insect Resources Utilization and Sustainable Pest Management Key Laboratory, College of Plant Science and Technology, Huazhong Agricultural University, Wuhan, P.R. China.

In this study, the detoxification enzyme activity and the transcriptional profile changes in the second instar through RNA-sequencing technology due to emamectin benzoate (EB) were assessed. The cytochrome P450 monooxygenases (P450) enzyme activity was not altered by EB due to the change in concentration and exposure time in all treatments. The glutathione S-transferase (GST) enzyme was not considerably varying in all treatments, while exposure time significantly changed the enzyme activity. Read More

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The efficacy and safety of evinacumab for the treatment of hypercholesterolemia: a meta-analysis.

J Cardiovasc Pharmacol 2021 May 31. Epub 2021 May 31.

Department of Cardiology, the Second Affiliated Hospital, Xinjiang Medical University, Urumqi, Xinjiang, China. This author takes responsibility for all aspects of the reliability and freedom from bias of the data presented and their discussed interpretation. Department of Cardiology, the First Affiliated Hospital, Xinjiang Medical University, 830000 Urumqi, Xinjiang, China. This author takes responsibility for all aspects of the reliability and freedom from bias of the data presented and their discussed interpretation.

Abstract: Angiopoietin-like protein 3 (ANGPTL3) is essential in lipid metabolism regulation. However, the efficacy and safety of evinacumab (ANGPTL3 inhibition drug) for hypercholesterolemia treatment is unknown. In this study, a meta-analysis of randomized controlled trials (RCTs) was conducted to assess the efficacy and safety of evinacumab. Read More

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D-dopachrome tautomerase activates COX2/PGE pathway of astrocytes to mediate inflammation following spinal cord injury.

J Neuroinflammation 2021 Jun 11;18(1):130. Epub 2021 Jun 11.

Key Laboratory of Neuroregeneration of Jiangsu and Ministry of Education, Co-innovation Center of Neuroregeneration, Nantong University, Nantong, 226001, People's Republic of China.

Background: Astrocytes are the predominant glial cell type in the central nervous system (CNS) that can secrete various cytokines and chemokines mediating neuropathology in response to danger signals. D-dopachrome tautomerase (D-DT), a newly described cytokine and a close homolog of macrophage migration inhibitory factor (MIF) protein, has been revealed to share an overlapping function with MIF in some ways. However, its cellular distribution pattern and mediated astrocyte neuropathological function in the CNS remain unclear. Read More

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CCDC114, DNAI2 and TOP2A involves in the effects of tibolone treatment on postmenopausal endometrium.

BMC Womens Health 2021 Jun 11;21(1):240. Epub 2021 Jun 11.

Department of Obstetrics and Gynecology, People's Hospital of Jiaxiang County, No. 188 Yingfeng Road, Jiaxiang, Jining, 272400, Shandong, China.

Background: This study aimed to explore the molecular mechanisms of tibolone treatment in postmenopausal women.

Methods: The gene set enrichment profile, GSE12446, which includes 9 human endometrial samples from postmenopausal women treated with tibolone (tibolone group) and 9 control samples (control group), was downloaded from GEO database for analysis. Differentially expressed genes (DEGs) in tibolone vs. Read More

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The emerging role of circular RNAs in common solid malignant tumors in children.

Cancer Cell Int 2021 Jun 11;21(1):309. Epub 2021 Jun 11.

Surgical Center of Women and Children's Hospital, Qingdao University, No. 6, Tongfu Rd, Shibei District, Qingdao, 266011, Shandong, China.

Malignant tumors are one of the fatal diseases that threaten children's physical and mental health and affect their development. Research has shown that the occurrence and development of malignant tumors are associated with the abnormal expression and regulation of genes. Circular RNAs (circRNAs) are noncoding RNAs that have a closed circular structure, with a relatively stable expression, and do not undergo exonuclease-mediated degradation readily. Read More

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Regulation of TWIK-related K channel 1 in the anterior hippocampus of patients with temporal lobe epilepsy with comorbid depression.

Epilepsy Behav 2021 Jun 8;121(Pt A):108045. Epub 2021 Jun 8.

Department of Neurosurgery, Sanbo Brain Hospital, Capital Medical University, Beijing, China; Beijing Key Laboratory of Epilepsy, Beijing, China; Center of Epilepsy, Beijing Institute of Brain Disorders, Collaborative Innovation Center for Brain Disorders, Capital Medical University, Beijing, China. Electronic address:

Epilepsy with comorbid depression has recently attracted increasing attention. Temporal lobe epilepsy (TLE) may represent an increased risk of developing depression, especially if the seizures do not generalize. The two-pore domain potassium channel-TWIK-related K channel (TREK-1) plays important roles in both epilepsy and depression. Read More

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Genetic variant within CDK6 regulates immune response to palbociclib treatment.

Clin Immunol 2021 Jun 8:108777. Epub 2021 Jun 8.

Istituto di Ricerca Genetica e Biomedica (IRGB), Consiglio Nazionale delle Ricerche (CNR), 09042 Monserrato, Sardinia, Italy. Electronic address:

Everyone carries a set of genetic variants that contribute to regulation of the levels of blood cells, with unknown clinical impact. One of them, rs445 within the cell-cycle checkpoint gene CDK6, reduces the levels of myeloid cell types including granulocytes. We treated CD3+ T cells and whole blood with palbociclib in 41 individuals, who were stratified by genotype for analyses. Read More

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The role of circTmeff-1 in incubation of context-induced morphine craving.

Pharmacol Res 2021 Jun 8;170:105722. Epub 2021 Jun 8.

College of Forensic Medicine, Hebei Medical University, Hebei Key Laboratory of Forensic Medicine, Collaborative Innovation Center of Forensic Medical Molecular Identification, Research Unit of Digestive Tract Microecosystem Pharmacology and Toxicology, Chinese Academy of Medical Sciences, Hebei Province, Shijiazhuang 050017, PR China. Electronic address:

A progressive increase in drug craving following drug exposure is an important trigger of relapse. CircularRNAs (CircRNAs), key regulators of gene expression, play an important role in neurological diseases. However, the role of circRNAs in drug craving is unclear. Read More

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SIRT1/PGC-1α signaling activation by mangiferin attenuates cerebral hypoxia/reoxygenation injury in neuroblastoma cells.

Eur J Pharmacol 2021 Jun 8:174236. Epub 2021 Jun 8.

Xi'an Key Laboratory of Cardiovascular and Cerebrovascular Diseases, Xi'an No.3 Hospital, School of Life Sciences and Medicine, Northwest University, 10 Fengcheng Three Road, Xi'an, China; Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education. Faculty of Life Sciences, Northwest University, 229 Taibai North Road, Xi'an, China. Electronic address:

Ischemia reperfusion injury (IRI) is associated with poor prognoses in the setting of ischemic brain diseases. Silence information regulator 1 (SIRT1) is a member of the third class of nicotinamide adenine dinucleotide (NAD)-dependent sirtuins. Recently, the role of SIRT1/peroxisome proliferators-activated receptor-γ coactivator 1α (PGC-1α) pathway in organ (especially the brain) protection under various pathological conditions has been widely investigated. Read More

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Leishmanicidal potentials of extract and its fractions on in a murine model: parasite burden, gene expression, and histopathological profile.

J Med Microbiol 2021 Jun;70(6)

Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran.

Leishmaniasis is a neglected tropical and subtropical disease caused by over 20 protozoan species. Treatment of this complex disease with traditional synthetic drugs is a major challenge worldwide. Natural constituents are unique candidates for future therapeutic development. Read More

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Dynamical Basis of Allosteric Activation for the Protein Kinase G.

J Phys Chem B 2021 Jun 11. Epub 2021 Jun 11.

Department of Chemistry and Chemical Biology, McMaster University, Hamilton, Ontario L8S 4M1, Canada.

The cGMP-dependent protein kinase (PKG) is required for the progression of the 's life cycle and is therefore a promising malaria drug target. PKG includes four cGMP-binding domains (CBD-A to CBD-D). CBD-D plays a crucial role in PKG regulation as it is the primary determinant for the inhibition and cGMP-dependent activation of the catalytic domain. Read More

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Loss of MYSM1 inhibits the oncogenic activity of cMYC in B cell lymphoma.

J Cell Mol Med 2021 Jun 11. Epub 2021 Jun 11.

Department of Physiology, McGill University, Montreal, QC, Canada.

MYSM1 is a chromatin-binding protein, widely investigated for its functions in haematopoiesis in human and mouse; however, its role in haematologic malignancies remains unexplored. Here, we investigate the cross-talk between MYSM1 and oncogenic cMYC in the transcriptional regulation of genes encoding ribosomal proteins, and the implications of these mechanisms for cMYC-driven carcinogenesis. We demonstrate that in cMYC-driven B cell lymphoma in mouse models, MYSM1-loss represses ribosomal protein gene expression and protein synthesis. Read More

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Ozone nanobubble treatments improve survivability of Nile tilapia (Oreochromis niloticus) challenged with a pathogenic multi-drug-resistant Aeromonas hydrophila.

J Fish Dis 2021 Jun 10. Epub 2021 Jun 10.

Faculty of Science and Technology, Suan Sunandha Rajabhat University, Bangkok, Thailand.

A rapid increase in multi-drug-resistant (MDR) bacteria in aquaculture highlights the risk of production losses due to diseases and potential public health concerns. Previously, we reported that ozone nanobubbles (NB-O ) were effective at reducing concentrations of pathogenic bacteria in water and modulating fish immunity against pathogens; however, multiple treatments with direct NB-O exposures caused alterations to the gills of exposed fish. Here, we set up a modified recirculation system (MRS) assembled with an NB-O device (MRS-NB-O ) to investigate whether MRS-NB-O (a) were safe for tilapia (Oreochromis niloticus), (b) were effective at reducing bacterial load in rearing water and (c) improved survivability of Nile tilapia following an immersion challenge with a lethal dose of MDR Aeromonas hydrophila. Read More

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Cyclophosphamide bioactivation pharmacogenetics in breast cancer patients.

Cancer Chemother Pharmacol 2021 Jun 10. Epub 2021 Jun 10.

Auckland Regional Cancer and Blood Service, Auckland City Hospital, Grafton, Auckland, New Zealand.

Purpose: Genetic variation in the activation of the prodrug cyclophosphamide (CP) by cytochrome P450 (CYP) enzymes has been shown to influence outcomes. However, CYP are also subject to phenoconversion due to either the effects of comedications or cancer associated down-regulation of expression. The aim of this study was to assess the relationship between CP bioactivation with CYP2B6 and CYP2C19 genotype, as well as CYP2C19 phenotype, in breast cancer patients. Read More

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An effective NIR laser/tumor-microenvironment co-responsive cancer theranostic nanoplatform with multi-modal imaging and therapies.

Nanoscale 2021 Jun 11. Epub 2021 Jun 11.

College of Chemistry and Chemical Engineering, Anhui University, Hefei 230601, P. R. China.

Cancer is still a major threat to human health at present. Developing new types of integrated nanoplatforms for the accurate diagnosis and effective treatment of cancer is very significant. Herein, an intelligent dual-stage core-shell cancer theranostic nanoplatform ([email protected]@PbP) with NIR laser/tumor-microenvironment (TME) co-responsiveness and multi-modal imaging-therapy was successfully prepared, which was composed of the precisely structured oil-soluble Au1Ag24 nanoclusters (NCs) and Fe3+ ions easily assembled within the oil and aqueous phases of the polyethylene glycol (PEG) block grafted polyketal (PK) copolymer (PK-b-PEG, PbP) vesicles, respectively. Read More

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Role of LncRNAs in the Epithelial-Mesenchymal Transition in Hepatocellular Carcinoma.

Front Oncol 2021 25;11:690800. Epub 2021 May 25.

Department of Interventional Radiology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, China.

Hepatocellular carcinoma (HCC) is a type of primary liver cancer with a high incidence and mortality rate. HCC develops insidiously, and most newly diagnosed cases are in the middle and advanced stages. The epithelial-mesenchymal transition (EMT) is a vital mechanism underlying metastasis in patients with advanced HCC. Read More

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Role of HOXC10 in Cancer.

Front Oncol 2021 25;11:684021. Epub 2021 May 25.

Central Laboratory, Affiliated Jinhua Hospital, Zhejiang University School of Medicine, Jinhua, China.

The HOXC10 gene, a member of the HOX genes family, plays crucial roles in mammalian physiological processes, such as limb morphological development, limb regeneration, and lumbar motor neuron differentiation. HOXC10 is also associated with angiogenesis, fat metabolism, and sex regulation. Additional evidence suggests that HOXC10 dysregulation is closely associated with various tumors. Read More

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GLI1: A Therapeutic Target for Cancer.

Front Oncol 2021 25;11:673154. Epub 2021 May 25.

Oncology Department, Drug Discovery Division, Southern Research, Birmingham, AL, United States.

GLI1 is a transcriptional effector at the terminal end of the Hedgehog signaling (Hh) pathway and is tightly regulated during embryonic development and tissue patterning/differentiation. GLI1 has low-level expression in differentiated tissues, however, in certain cancers, aberrant activation of GLI1 has been linked to the promotion of numerous hallmarks of cancer, such as proliferation, survival, angiogenesis, metastasis, metabolic rewiring, and chemotherapeutic resistance. All of these are driven, in part, by GLI1's role in regulating cell cycle, DNA replication and DNA damage repair processes. Read More

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A near-infrared fluorescent probe with large Stokes shift for imaging Cys in tumor mice.

Anal Chim Acta 2021 Aug 21;1171:338655. Epub 2021 May 21.

Key Laboratory for Green Organic Synthesis and Application of Hunan Province, Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education, College of Chemistry, Xiangtan University, Xiangtan, 411105, PR China. Electronic address:

Cysteine (Cys), a kind of small molecule biological thiol, not only involves in the regulation of physiological processes, but also is considered a marker of tumor. However, it is challenging to develop suitable probe for detecting Cys in tumors. In this paper, a near-infrared (NIR) fluorescent probe named IX for Cys has been designed and synthesized. Read More

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A 3-styrylchromone converted from trimebutine 3D pharmacophore possesses dual suppressive effects on RAGE and TLR4 signaling pathways.

Biochem Biophys Res Commun 2021 Jun 7;566:1-8. Epub 2021 Jun 7.

Department of Genomic Medicinal Science, Research Institute for Science and Technology, Organization for Research Advancement, Tokyo University of Science, Noda, Chiba, 278-8510, Japan. Electronic address:

Receptor for advanced glycation end-products (RAGE) and Toll-like receptors (TLRs) are potential therapeutic targets in the treatment of acute and chronic inflammatory diseases. We previously reported that trimebutine, a spasmolytic drug, suppresses RAGE pro-inflammatory signaling pathway in macrophages. The aim of this study was to convert trimebutine to a new small molecule using in silico 3D pharmacophore similarity search, and dissect the mechanistic anti-inflammatory basis. Read More

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Evidences for the mechanism of Shenmai injection antagonizing doxorubicin-induced cardiotoxicity.

Phytomedicine 2021 May 21;88:153597. Epub 2021 May 21.

Hangzhou Medical college, Hangzhou, China. Electronic address:

Background: Doxorubicin (DOX) is a widely used antitumor drug. However, its clinical application is limited for its serious cardiotoxicity. The mechanism of DOX-induced cardiotoxicity is attributed to the increasing of cell stress in cardiomyocytes, then following autophagic and apoptotic responses. Read More

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Identification of neolignans with PCSK9 downregulatory and LDLR upregulatory activities from Penthorum chinense and the potential in cholesterol uptake by transcriptional regulation of LDLR via SREBP2.

J Ethnopharmacol 2021 Jun 7:114265. Epub 2021 Jun 7.

College of Pharmacy and Research Institute of Pharmaceutical Sciences,Seoul National University, 1, Gwanak-ro, Gwanak-gu,Seoul 08826,Republic of Korea. Electronic address:

Ethnopharmacological Relevance: Penthorum chinense has been used in East Asia for the treatment of cholecystitis, infectious hepatitis, jaundice and to treat liver problems. Recent evidences provided the potential for the clinical use of P. chinense in the treatment of metabolic disease. Read More

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Bcl-xL expression and regulation in the progression, recurrence, and cisplatin resistance of oral cancer.

Life Sci 2021 Jun 8;280:119705. Epub 2021 Jun 8.

Department of Life Sciences, School of Natural Sciences, Central University of Jharkhand, Ratu-Lohardaga Road, Brambe, Ranchi 835205, Jharkhand, India. Electronic address:

Background: Bcl-xL is an anti-apoptotic molecule, but its role in the progression and recurrent/ drug-resistant oral squamous cell carcinoma (OSCC) is poorly understood.

Materials And Methods: A total of one hundred twenty-five human OSCC tissue specimens including twenty-nine adjacent normals (AN), sixty-nine primary tumors (PT), twenty-seven recurrent chemoradiation resistance (RCRT) samples, and oral tongue SCC derived cisplatin-resistant (CisR SCC-4/-9) cells were used, for this study. Protein/mRNA expression levels of Bcl-xL and its regulation by ERK1/2, Stat-3, p53, NFκB, AP-1 (components: c-Jun, c-Fos, and Fra-2) molecules, and cell viability were measured by immunohistochemistry, Western blot, RT-PCR, and MTT analysis. Read More

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Sterol regulation of developmental and oncogenic Hedgehog signaling.

Biochem Pharmacol 2021 Jun 7:114647. Epub 2021 Jun 7.

Department of Cell Biology, Harvard Medical School, Boston, MA, USA. Electronic address:

The Hedgehog (Hh) family of lipid-modified signaling proteins directs embryonic tissue patterning and postembryonic tissue homeostasis, and dysregulated Hh signaling drives familial and sporadic cancers. Hh ligands bind to and inhibit the tumor suppressor Patched and allow the oncoprotein Smoothened (SMO) to accumulate in cilia, which in turn activates the GLI family of transcription factors. Recent work has demonstrated that endogenous cholesterol and oxidized cholesterol derivatives (oxysterols) bind and modulate SMO activity. Read More

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A meta-analysis of transcriptomic profiles of Huntington's disease patients.

PLoS One 2021 10;16(6):e0253037. Epub 2021 Jun 10.

Department of Gene Therapy, Ulm University, Ulm, Germany.

Description of robust transcriptomic alterations in Huntington's disease is essential to identify targets for biochemical studies and drug development. We analysed publicly available transcriptome data from the brain and blood of 220 HD patients and 241 healthy controls and identified 737 and 661 genes with robustly altered mRNA levels in the brain and blood of HD patients, respectively. In the brain, a subnetwork of 320 genes strongly correlated with HD and was enriched in transport-related genes. Read More

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NIR-Triggered Multi-Mode Antitumor Therapy Based on Bi Se /Au Heterostructure with Enhanced Efficacy.

Small 2021 Jun 10:e2100961. Epub 2021 Jun 10.

State Key Laboratory of Rare Earth Resource Utilization, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, P. R. China.

Of all the reaction oxygen species (ROS) therapeutic strategies, NIR light-induced photocatalytic therapy (PCT) based on semiconductor nanomaterials has attracted increasing attention. However, the photocatalysts suffer from rapid recombination of electron-hole pairs due to the narrow band gaps, which are greatly restricted in PCT application. Herein, Bi Se /Au heterostructured photocatalysts are fabricated to solve the problems by introducing Au nanoparticles (NPs) in situ on the surface of the hollow mesoporous structured Bi Se . Read More

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Hypoxia-inducible exosomes facilitate liver-tropic pre-metastatic niche in colorectal cancer.

Hepatology 2021 Jun 10. Epub 2021 Jun 10.

Key Laboratory of Environmental Medicine Engineering, Ministry of Education, School of Public Health, Southeast University, Nanjing, 210009, China.

Background & Aims: Liver metastasis is a frequent occurrences in patients with colorectal cancer (CRC), 15%-25% of CRC patients have liver metastases at the time of initial diagnosis (1). Specifically, some regional-stage patients with mild symptoms (stage Ⅰ or II) will also advance to liver metastases rapidly, even CRC lesion in situ is resected in time. Nevertheless, the precise mechanism of liver metastasis is still unclear. Read More

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Consumption of Ashtanga Ghrita (clarified cow butter added with herb extracts) improves cognitive dysfunction induced by scopolamine in rats via regulation of acetylcholinesterase activity and oxidative stress.

Drug Metab Pers Ther 2021 Jun 10. Epub 2021 Jun 10.

Department of Rasa Shastra & Bhaishajya Kalpana, Faculty of Ayurveda, Institute of Medical Sciences, Banaras Hindu University, Varanasi, Uttar Pradesh, India.

Objectives: Ashtanga Ghrita (AG), an Indian traditional formulation, has been used to promote neuropharmacological activities. AG is made up of clarified cow butter (ghee) and eight different herbs.

Methods: To test whether scopolamine (SCP)-induced dementia and brain oxidative stress can be counteracted by AG, rats were separated into five groups (n=6/group): group one control, group two SCP (1 mg/kg b. Read More

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