Publications by authors named "Sreedhar Madishetti"
COVID-19 pandemic caused by the SARS-CoV-2 virus has led to a worldwide crisis. In view of emerging variants time to time, there is a pressing need of effective COVID-19 therapeutics. Setomimycin, a rare tetrahydroanthracene antibiotic, remained unexplored for its therapeutic uses.
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- A library of new spiroisoxazoline analogues of arteannuin B was created and tested for anti-inflammatory effects in macrophage cells.
- Three selected analogues (8i, 8m, and 8n) showed stronger suppression of pro-inflammatory cytokines IL-6 and TNF-α compared to arteannuin B itself.
- The analogues demonstrated effective inhibition of nitric oxide production without affecting cell viability, indicating their potential for developing new treatments for inflammatory diseases.
Article Synopsis
- Inflammation is a complex process that needs a balance between signals that start and stop it, and an imbalance can cause tissue damage, particularly in an aging population increasingly affected by inflammatory diseases.* -
- Oreganum Vulgare, a plant used in traditional medicine for various health issues, was studied for its potential anti-inflammatory effects through specific in vitro tests.* -
- The study found that extracts from Oreganum Vulgare effectively reduced inflammatory cytokines without harming cell viability, supporting its traditional medicinal use.*
Role of environmental pollutants in Alzheimer's disease: a review.
Environ Sci Pollut Res Int
December 2020
Article Synopsis
- - Neurodegenerative disorders like Alzheimer's disease (AD) are influenced by a mix of lifestyle, environmental, and genetic factors, but the exact causes of AD remain unclear.
- - Recent research suggests that environmental factors, such as heavy metals, air pollutants, and industrial chemicals, may increase the risk and progression of AD by affecting key mechanisms in the brain.
- - The review compiles data linking these environmental exposures to the buildup of harmful substances like amyloid-β peptides and tau phosphorylation, which contribute to neuron death and AD pathology.
In the present study, a novel series of 3-pyrimidinylazaindoles were designed and synthesized using a bioinformatics strategy as cyclin-dependent kinases CDK2 and CDK9 inhibitors, which play critical roles in the cell cycle control and regulation of cell transcription. The present approach gives new dimensions to the existing SAR and opens a new opportunity for the lead optimizations from comparatively inexpensive starting materials. The study led to the identification of the alternative lead candidate 4ab with a nanomolar potency against CDK2 and CDK9 and potent antiproliferative activities against a panel of tested tumor cell lines along with a better safety ratio of ∼33 in comparison to reported leads.
View Article and Find Full Text PDFBackground And Purpose: The μ-opioid receptor has been characterized as the main mediator of opioid signalling in neuronal cells. Opioid-induced pain suppression was originally proposed to be mediated by μ-opioid receptor-induced inhibitory effects on cAMP, which is known to mediate inflammatory hypernociception. Recent investigations revealed PI3Kγ and Akt (PKB) as additional elements of μ-opioid receptor signalling.
View Article and Find Full Text PDFWe describe a rapid screening methodology for performing pharmacokinetic (PK) studies in mice called Fast PK. In this Fast PK method, two mice were used per compound and four blood samples were collected from each mouse. The sampling times were staggered (sparse sampling) between the two mice, thus yielding complete PK profile in singlicate across eight time points.
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