2,618 results match your criteria: "CSIR--Central Drug Research Institute[Affiliation]"
Phytomedicine
October 2024
In vivo Testing facility, Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, Uttar Pradesh 226015, India; AcSIR, Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Background: Malaria, characterised by inflammation and multi-organ complications, needs novel chemotherapeutics due to the rise of drug-resistant malaria parasites, which is a serious health issue. Naringin (NGN), a flavanone glycoside (naringenin 7-O-neohesperidose), has a broad spectrum of pharmacological activities but its effect against malaria, alone and in combination, was not deeply investigated.
Purpose: To assess the pharmacological efficacy of NGN alone and in combination with chloroquine (CQ) against a Plasmodium strain resistant to CQ and to elucidate its potential mode of action.
RSC Med Chem
August 2024
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute BS 10/1, Sector 10, Jankipuram Extension, Sitapur Road Lucknow 226031 India
This study investigates the potential of click chemistry for the development of novel anti-tuberculosis agents. A targeted library of 1,4-dihydropyridine-1,2,3-triazole conjugates was synthesized and evaluated for their activity against HRa using the resazurin microtiter assay (REMA). Among the synthesized derivatives, compounds J10, J11, J14, J22 and J23 demonstrated significant antimycobacterial activity.
View Article and Find Full Text PDFNanomedicine (Lond)
October 2024
Division of Pharmaceutics & Pharmacokinetics, CSIR-Central Drug Research Institute, Lucknow, 226031, UP, India.
This study evaluates the potential of combining paclitaxel (PTX) and bortezomib (BTZ) for breast cancer therapy. The nanoformulation was optimized via Box-Behnken Design (BBD), with method validation adhering to US-FDA guidelines. Multiple reaction monitoring transitions for PTX, BTZ and internal standard were m/z 855.
View Article and Find Full Text PDFFEBS J
October 2024
Division of Cancer Biology, CSIR-Central Drug Research Institute, Lucknow, India.
CCAAT/enhancer-binding protein α (C/EBPα), a key myeloid transcription factor, drives myeloid differentiation from blast cells by regulating the expression of granulocyte colony stimulating factor receptor and C/EBPε as required for promoting granulocyte differentiation. Here, we show that serine/threonine-protein kinase NLK, also known as Nemo-like kinase, physically associates with C/EBPα and phosphorylates it at multiple sites, including Ser21, Thr226, Thr230 and S234, leading to its ubiquitin-mediated degradation. Individual phospho-point mutants of C/EBPα could be phosphorylated by NLK, but a mutant with all phosphorylatable residues replaced by alanine resisted phosphorylation and degradation by NLK, as did the single point mutants.
View Article and Find Full Text PDFArch Pharm (Weinheim)
November 2024
Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Balanagar, Hyderabad, Telangana, India.
The escalating severity of the menace posed by bacterial resistance has rendered the existing antibiotics less effective, thus necessitating the discovery of new antibacterial agents. The current study reports the exploration of substituted N-pyridinylaminonaphthols produced by a straightforward, one-pot multicomponent reaction process as antibacterial agents. The synthesized derivatives were assessed in vitro for their antibacterial properties against a panel of bacterial pathogens.
View Article and Find Full Text PDFOrg Lett
August 2024
Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, U.P., India.
5,10-Dihydroindeno[1,2-]indole has served as an important starting precursor for BARAC-fluor reagent in medicinal chemistry. Herein, an unprecedented -TsOH assisted intramolecular C2-arylation of NH-indoles via C(sp)-CN/C(sp)-H coupling, offering a series of 5,10-dihydroindeno[1,2-]indoles with moderate to good yields, has been showcased under redox-neutral conditions. Furthermore, successful scalability and synthetic applications highlight the practical nature of the method.
View Article and Find Full Text PDFLife Sci
September 2024
Division of Toxicology and Experimental Medicine, CSIR-Central Drug Research Institute (CSIR-CDRI), Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Cell
August 2024
Department of Biological Sciences and Bioengineering, Indian Institute of Technology Kanpur, Kanpur 208016, India. Electronic address:
The Duffy antigen receptor is a seven-transmembrane (7TM) protein expressed primarily at the surface of red blood cells and displays strikingly promiscuous binding to multiple inflammatory and homeostatic chemokines. It serves as the basis of the Duffy blood group system in humans and also acts as the primary attachment site for malarial parasite Plasmodium vivax and pore-forming toxins secreted by Staphylococcus aureus. Here, we comprehensively profile transducer coupling of this receptor, discover potential non-canonical signaling pathways, and determine the cryoelectron microscopy (cryo-EM) structure in complex with the chemokine CCL7.
View Article and Find Full Text PDFExpert Opin Ther Pat
September 2024
Division of Biochemistry and Structural Biology, CSIR-Central Drug Research Institute, Lucknow, India.
Introduction: The sodium-glucose co-transporter 2 (SGLT2) inhibitors are FDA-approved class of drugs for diabetes management. They improve glycemic control by inducing glucosuria. Notwithstanding with potent anti-hyperglycemic activity, SGLT2 inhibitors are emerging as drugs with multifaceted therapeutic potential, evidenced for cardioprotective, renoprotective, antihypertensive, and neuroprotective activities.
View Article and Find Full Text PDFLeukemia
September 2024
Division of Cancer Biology, CSIR-Central Drug Research Institute, Lucknow, Uttar Pradesh, 226031, India.
Arch Pharm Res
September 2024
Division of Endocrinology and Centre for Research in Anabolic Skeletal Targets in Health and Illness (ASTHI), CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, 226031, India.
Biomedicines
July 2024
Division of Endocrinology, CSIR-Central Drug Research Institute, Council of Scientific and Industrial Research, Lucknow 226031, India.
Nitroimidazoles comprise a class of broad-spectrum anti-microbial drugs with efficacy against parasites, mycobacteria, and anaerobic Gram-positive and Gram-negative bacteria. Among these drugs, metronidazole (MTZ) is commonly used with other antibiotics to prevent infection in open fractures. However, the effect of MTZ on bone remains understudied.
View Article and Find Full Text PDFJ Org Chem
August 2024
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
The construction of biologically interesting -heterocycles under metal-free conditions is a constant goal in industry and academia. Herein, we have developed an hexafluoroisopropanol (HFIP)-mediated intramolecular cyclization of allenamides, providing tetrahydro-β-carboline derivatives embedded with a C1-vinyl functionality. The metal-free protocol provided tetrahydro-β-carboline derivatives atom-efficiently under room temperature with a broad substrate scope in good to excellent yields.
View Article and Find Full Text PDFReprod Biol Endocrinol
July 2024
Division of Endocrinology, CSIR-Central Drug Research Institute, Lucknow, India.
Background: Spermatogenesis is a temperature-sensitive process, and elevation in temperature hampers this process quickly and significantly. We studied the molecular effects of testicular heating on piRNAs and gene expression in rat testicular germ cells.
Methods: We generated a cryptorchid rat model by displacing the testis from the scrotal sac (34 °C) to the abdominal area (37 °C) and sacrificed animals after 1 day, 3 days, and 5 days.
Cancer Cell Int
July 2024
Department of Biochemical Engineering and Biotechnology, Indian Institute of Technology Delhi, New Delhi, 110016, India.
Background: Glioblastoma (GBM) is the most aggressive among the tumors of the central nervous system (CNS), and has a dismal prognosis. Altered metabolism, especially the increased rate of aerobic glycolysis promotes rapid proliferation of GBM cells. Here, we investigated the role of aldehyde dehydrogenase 5 family member A1 (ALDH5A1), a mitochondrial enzyme in the aspect of GBM metabolism.
View Article and Find Full Text PDFACS Infect Dis
August 2024
Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, Lucknow 226031, India.
sporozoites invade hepatocytes, transform into liver stages, and replicate into thousands of merozoites that infect erythrocytes and cause malaria. Proteins secreted from micronemes play an essential role in hepatocyte invasion, and unneeded micronemes are subsequently discarded for replication. The liver-stage parasites are potent immunogens that prevent malarial infection.
View Article and Find Full Text PDFACS Omega
July 2024
Molecular Microbiology and Immunology Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Organoid technology, revolutionizing biomedical research, offers a transformative approach to studying human developmental biology, disease pathology, and drug discovery. Originating from the pioneering work of Henry Van Peters Wilson in 1907 and evolving through subsequent breakthroughs, organoids are three-dimensional structures derived from stem cells or tissue explants that mimic the architecture and function of organs . With the ability to model various organs such as intestine, liver, brain, kidney, and more, organoids provide unprecedented insights into organ development, disease mechanisms, and drug responses.
View Article and Find Full Text PDFJ Cell Physiol
September 2024
Division of Cancer Biology, CSIR-Central Drug Research Institute, Lucknow, Uttar Pradesh, India.
J Chromatogr B Analyt Technol Biomed Life Sci
August 2024
CSIR-National Botanical Research Institute, Rana Pratap Marg, Lucknow-226 001, UP, India.
C. madagascariensis, an unexplored species of Burseraceae is used by local population for the management of inflammation and throat pain. The disease alleviation by this plant could be due to the presence of rich repository of active compounds with various pharmacological importances.
View Article and Find Full Text PDFPLoS One
July 2024
Ethnopharmacology Laboratory, Department of Botany, Visva-Bharati, Santiniketan, India.
In eastern India, the tubers of Pueraria tuberosa (Willd.) DC. are used by the ethnic communities for its wide range of medicinal and nutritional value, especially to rejuvenate livestock health and to treat helminthiasis.
View Article and Find Full Text PDFMol Cell Neurosci
September 2024
Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow 226031, U.P., India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Hypertension-induced brain renin-angiotensin system (RAS) activation and neuroinflammation are hallmark neuropathological features of neurodegenerative diseases. Previous studies from our lab have shown that inhibition of ACE/Ang II/AT1R axis (by AT1R blockers or ACE inhibitors) reduced neuroinflammation and accompanied neurodegeneration via up-regulating adult hippocampal neurogenesis. Apart from this conventional axis, another axis of RAS also exists i.
View Article and Find Full Text PDFJ Med Chem
July 2024
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
In the quest for the discovery of antidiabetic compounds, a series of 27 1,4-dihydropyridine-indole derivatives were synthesized using a diversity approach. These compounds were systematically evaluated for their antidiabetic activity, starting with an in vitro assessment for GLUT4 translocation stimulation in L6-GLUT4 myotubes, followed by in vivo antihyperglycemic activity evaluation in a streptozotocin (STZ)-induced diabetic rat model. Among the synthesized compounds, , , , , , , and demonstrated significant potential to stimulate GLUT4 translocation in skeletal muscle cells.
View Article and Find Full Text PDFBioanalysis
June 2024
Division of Pharmaceutics & Pharmacokinetics, CSIR-Central Drug Research Institute, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P, India.
A HPLC method was developed and validated for the novel combination of rutin (RN) and donepezil (DNP). RN and DNP were simultaneously eluted through a C18 column (Ø 150 × 4.6 mm) with a 60:40 v/v ratio of 0.
View Article and Find Full Text PDFAutophagy Rep
December 2024
Department of Endocrinology, Sanjay Gandhi Postgraduate Institute of Medical Sciences, Lucknow 226014, India.
Breast cancer is a heterogeneous disease, with a subpopulation of tumor cells known as breast cancer stem cells (BCSCs) with self-renewal and differentiation abilities that play a critical role in tumor initiation, progression, and therapy resistance. The tumor microenvironment (TME) is a complex area where diverse cancer cells reside creating a highly interactive environment with secreted factors, and the extracellular matrix. Autophagy, a cellular self-digestion process, influences dynamic cellular processes in the tumor TME integrating diverse signals that regulate tumor development and heterogeneity.
View Article and Find Full Text PDFLife Sci
September 2024
Endocrinology Division, Council of Scientific and Industrial; Research (CSIR)-Central Drug Research Institute (CDRI), Sector-10, Jankipuram Extension, Sitapur Road, Lucknow 226031, U.P., India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, India. Electronic address:
Aims: MCP-1 has been shown to be elevated in endometriosis. ILK functions in several cellular events and interacts with MCP-1-signaling. In the current study, we evaluated the role of MCP-1-ILK signaling in human endometriotic cell's (Hs832(C).
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