Malaria remains a global health challenge with significant mortality and morbidity annually, with resistant parasite strains complicating treatment efforts. There is an acute need for novel antimalarial drugs that can put a stop to the future public health crisis caused by the multi-drug resistance strains of the parasite However, the discovery of these new components is very challenging in the context of the generation of multi-drug resistance properties of malaria. The novel drugs also need to have several properties involving enhanced therapeutic prospects, successful treatment capabilities, and novel mechanisms of action that will forestall the resistance.
View Article and Find Full Text PDFBackground: Human African Trypanosomiasis (HAT), also known as sleeping sickness, and Chagas disease are neglected tropical diseases caused by Trypanosoma brucei and Trypanosoma cruzi, respectively. These diseases present significant challenges in treatment due to the toxicity, low efficacy, and drug-resistant strains associated with current therapies.
Introduction: Cysteine proteases play vital roles in the life cycles of these parasites, making them potential targets for therapeutic intervention.
Background: Genotoxins are chemical constituents that damage DNA or chromosomal architecture, leading to alterations in the genetic level. Streptozotocin, a monofunctional nitrosourea derivative, is often utilized to induce diabetes mellitus in laboratory animals because of its detrimental effects on pancreatic cells. The purpose of this work was to investigate possible protective efficacy against the genotoxic effects of Streptozotocin.
View Article and Find Full Text PDFComb Chem High Throughput Screen
April 2024
Synthetic drugs currently prescribed for the treatment of Human African Trypanosomiasis (HAT) are non-specific, toxic, demand extended therapeutic regimes and are of varying efficacy. Along with the challenging demographic and socio-economic hurdles, the everincreasing risk of drug resistance is another major problem to be addressed. Cysteine protease, Heat shock proteins (HSP-90), Trypanothione reductase (TR), Farnesyl diphosphate synthase, Glucose-6-phosphate dehydrogenase, UP-4-galactose epimerase, and Cytidine triphosphate synthetase are potential enzymatic targets for the development of novel inhibitors against HAT which are the main focus of this review.
View Article and Find Full Text PDFThe present study predicts the molecular targets and druglike properties of the phyto-compound piperine (PIP) by in silico studies including molecular docking simulation, druglikeness prediction and ADME analysis for prospective therapeutic benefits against diabetic complications. PIP was encapsulated in biodegradable polymer poly-lactide-co-glycolide (PLGA) to form nanopiperine (NPIP) and their physico-chemical properties were characterized by AFM and DLS. ∼ 30 nm sized NPIP showed 86.
View Article and Find Full Text PDFObjectives: The -derived diferuloylmethane compound CUR, loaded on Poly (lactide-co-glycolic) acid (PLGA) nanoparticles was utilized to combat DN-induced renal apoptosis by selectively targeting and modulating Bcl2.
Methods: Upon molecular docking and screening study CUR was selected as the core phytocompound for nanoparticle formulation. PLGA-nano-encapsulated-curcumin (NCUR) were synthesized following standard solvent displacement method.
A unique ant-mimicking behaviour has been observed in the rove beetle genus Naddia sp. (Coleoptera: Staphylinidae: Staphylininae: Staphylinini: Staphylinina) from the campus of the University of Kalyani, Kalyani, Nadia, West Bengal, India. The individual has been observed to undergo imperfect Batesian mimicry by mimicking ants of the genus Pseudoneoponera (Hymenoptera: Formicidae: Ponerinae: Ponerini).
View Article and Find Full Text PDFReceptor tyrosine kinase (RTK) regulates multiple pathways, including Mitogenactivated protein kinases (MAPKs), PI3/AKT, JAK/STAT pathway, etc. which has a significant role in the progression and metastasis of tumor. As RTK activation regulates numerous essential bodily processes, including cell proliferation and division, RTK dysregulation has been identified in many types of cancers.
View Article and Find Full Text PDFComb Chem High Throughput Screen
September 2024
Background: Dengue, a mosquito-borne viral disease spread by the dengue virus (DENV), has become one of the most alarming health issues in the global scenario in recent days. The risk of infection by DENV is mostly high in tropical and subtropical areas of the world. The mortality rate of patients affected with DENV is ever-increasing, mainly due to a lack of anti-dengue viral-specific synthetic drug components.
View Article and Find Full Text PDFThe present study tends to evaluate the possible potential of bio-active Morroniside (MOR), against alloxan (ALX)-induced genotoxicity and hyperglycaemia. prediction revealed the interaction of MOR with Poly (ADP-ribose) polymerase (PARP) protein which corroborated well with experimental L6 cell line and mice models. Data revealed the efficacy of MOR in the selective activation of PARP protein and modulating other stress proteins NF-κB, and TNF-α to initiate protective potential against ALX-induced genotoxicity and hyperglycaemia.
View Article and Find Full Text PDFBackground: Trypanosomiasis, caused by protozoan parasites of the genus, remains a significant health burden in several regions of the world. Cysteine proteases play a crucial role in the pathogenesis of parasites and have emerged as potential therapeutic targets for the development of novel antiparasitic drugs.
Introduction: This review article aims to provide a comprehensive overview of the role of cysteine proteases in trypanosomiasis and their potential as therapeutic targets.
Background: This review critically addresses the putative molecular targets of Diabetic Nephropathy (DN) and screens effective phytocompounds that can be therapeutically beneficial, and highlights their mechanistic modalities of action.
Introduction: DN has become one of the most prevalent complications of clinical hyperglycemia, with individual-specific variations in the disease spectrum that leads to fatal consequences. Diverse etiologies involving oxidative and nitrosative stress, activation of polyol pathway, inflammasome formation, Extracellular Matrix (ECM) modifications, fibrosis, and change in dynamics of podocyte functional and mesangial cell proliferation adds up to the clinical complexity of DN.
Background: Diabetes is a chronic metabolic disorder having a global prevalence of nearly doubled over the last 30 years and has become one of the major health concerns worldwide. The number of adults with diabetes increased to 537 million in 2021.
Introduction: The overarching goal of diabetic research and treatment has always been to restore insulin independence and an average blood glucose level.
The present study describes the preparation and characterization of poly-lactide-co-glycolide encapsulated nano-curcumin (NCUR) drug, and its potential efficacy against the pesticide, such as cypermethrin-induced DNA damage and genotoxicity. Cypermethrin, the chosen pesticide, contaminates the aquatic environment after being washed off from the agricultural field to nearby water bodies leading to biomagnification-related perturbation of the ecological balance and overall environmental health by elevating adverse effects on non-target organisms producing toxic metabolites through biotransformation. The physico-chemical properties of NCUR were evaluated by employing the AFM, DLS and UV-Vis techniques.
View Article and Find Full Text PDFThere is a need to explore natural compounds against COVID-19 due to their multitargeted actions against various targets of nCoV. They act on multiple sites rather than single targets against several diseases. Thus, there is a possibility that natural resources can be repurposed to combat COVID-19.
View Article and Find Full Text PDFNeurodegeneration is the progressive loss of structure or function of neurons, which may ultimately involve cell death. The most common neurodegenerative disorder in the brain happens with Alzheimer's disease (AD), the most common cause of dementia. It ultimately leads to neuronal death, thereby impairing the normal functionality of the central or peripheral nervous system.
View Article and Find Full Text PDFComb Chem High Throughput Screen
November 2022
The human has two lungs responsible for respiration and drug metabolism. Severe lung infection caused by bacteria, mycobacteria, viruses, fungi, and parasites may lead to lungs injury. Smoking and tobacco consumption may also produce lungs injury.
View Article and Find Full Text PDFBackground: With the advent of food additives centuries ago, the human race has found ways to improve and maintain the safety of utility, augment the taste, color, texture, nutritional value, and appearance of the food. Since the 19th century, when the science behind food spoilage was discerned, food additives in food preservation have been increasing worldwide and at a fast pace to get along with modern lifestyles. Although food additives are thought to be used to benefit the food market, some of them are found to be associated with several health issues at an alarming rate.
View Article and Find Full Text PDFThe three discrete [Zn] complexes [NaZn(cpdp)(μ-Bz)(CHOH)][ZnCl][ZnCl(HO)]3CHOH1.5HO (), [NaZn(cpdp)(μ--OBz)(CHOH)]2HO (), and [NaZn(cpdp)(μ--NOBz)(CHOH)]Cl2HO (), supported by the carboxylate-based multidentate ligand ,'-bis[2-carboxybenzomethyl]-,'-bis[2-pyridylmethyl]-1,3-diaminopropan-2-ol (Hcpdp), have been successfully synthesized and fully characterized (Bz = benzoate; -OBz = dianion of -hydroxybenzoic acid; -NOBz = -nitrobenzoate). The complexes have been characterized by elemental analysis, FTIR, UV-vis, NMR spectroscopy, PXRD, and thermal analysis, including single-crystal X-ray crystallography of and .
View Article and Find Full Text PDFComb Chem High Throughput Screen
November 2022
Background: Cyclooxygenase (COX) and Lipoxygenase (LOX) enzymes catalyze the production of pain mediators like Prostaglandins (PGs) and Leukotrienes (LTs), respectively from arachidonic acid.
Introduction: The COX and LOX enzyme modulators are responsible for the major PGs and LTs mediated complications like asthma, osteoarthritis, rheumatoid arthritis, cancer, Alzheimer's disease, neuropathy and Cardiovascular Syndromes (CVS). Many synthetic Nonsteroidal Anti- Inflammatory Drugs (NSAIDs) used in the treatment have serious side effects like nausea, vomiting, hyperacidity, gastrointestinal ulcers, CVS, etc.
Cyclin-Dependent Kinases (CDKs) are the chief regulators in cell proliferation; the kinase activities are largely regulated by their interactions with CDK Inhibitors (CKIs) and Cyclins. The association of different CDKs with CDKIs and Cyclins at the cell-cycle checkpoints of different stages of mitotic cell cycle function act more likely as the molecular switches that regulate different transcriptional events required for progression through the cell cycle. A fine balance in response to extracellular and intracellular signals is highly maintained in the orchestrated function of CDKs along with Cyclins and CDKIs for normal cell proliferation.
View Article and Find Full Text PDFThe molecular mechanisms of mitotic cell cycle progression involve very tightly restricted types of machinery which are highly regulated by a fine balance between the positive and negative accelerators (or regulators). These regulators include several checkpoints that have proteins acting as enzymes and their activating partners. These checkpoints incessantly monitor the external as well as internal environments such as growth signals, favorable conditions for growth, cell size, DNA integrity of the cell and hence function to maintain the highly ordered cell cycle progression by sustaining cell homeostasis and promoting error-free DNA replication and cell cycle division.
View Article and Find Full Text PDFComb Chem High Throughput Screen
December 2021
Objectives: The issue of food-additive-toxicity causing several health hazards needs to be therapeutically managed with an immediate effect. Alloxan, a food additive, is used for whitening and shining flour. It is capable of inducing genotoxicity, diabetes, and associated mitochondrial dysfunction.
View Article and Find Full Text PDFFood-additive toxicity has become a major health hazard issue globally. Alloxan (ALX), a food-additive, intaken daily through flour causes diabetes and genotoxicity by inducing chromosomal-aberration and DNA-damage. The use of phytochemicals as a protective measure of health hazards has become quite evident because of their least side effects.
View Article and Find Full Text PDF