Astaxanthin-S-Allyl Cysteine Ester Protects Pancreatic β-Cell From Glucolipotoxicity by Suppressing Oxidative Stress, Endoplasmic Reticulum Stress and mTOR Pathway Dysregulation.

Glucolipotoxicity (GLT) has emerged as established mechanism in the progression of diabetes. Identifying compounds that mitigate GLT-induced deleterious effect on β-cells are considered important strategy to overcome diabetes. Hence, in the present study, astaxanthin-s-allyl cysteine (AST-SAC) diester was studied against GLT in β-cells.

Mammalian maltase-glucoamylase and sucrase-isomaltase inhibitory effects of Artocarpus heterophyllus: An in vitro and in silico approach.

Alpha-glucosidase (maltase, sucrase, isomaltase and glucoamylase) activities which are involved in carbohydrate metabolism are present in human intestinal maltase-glucoamylase (MGAM) and sucrase-isomaltase (SI). Hence, these proteins are important targets to identify drugs against postprandial hyperglycemia thereby for diabetes. To find natural-based drugs against MGAM and SI, Artocarpus heterophyllus leaf was explored for MGAM and SI inhibition in in vitro and in silico.

Exploring the interaction of phytochemicals from Hibiscus rosa-sinensis flowers with glucosidase and acetylcholinesterase: An integrated in vitro and in silico approach.

Targeting multiple factors such as oxidative stress, alpha glucosidase and acetylcholinesterase (AChE) are considered advantageous for the treatment of diabetes and diabetes associated-cognitive dysfunction. In the present study, Hibiscus rosa-sinensis flowers anthocyanin-rich extract (HRA) was prepared. Phytochemical analysis of HRA using LC-ESI/MS/MS revealed the presence of various phenolic acids, flavonoids and anthocyanins.

Synthesis and Characterization of Plumbagin S-Allyl Cysteine Ester: Determination of Anticancer Activity In Silico and In Vitro.

In recent years, derivatives of natural compounds are synthesized to increase the bioavailability, pharmacology, and pharmacokinetics properties. The naphthoquinone, plumbagin (PLU), is well known for its anticancer activity. However, the clinical use of PLU is hindered due to its toxicity.

Protection of pancreatic beta cells against high glucose-induced toxicity by astaxanthin-s-allyl cysteine diester: alteration of oxidative stress and apoptotic-related protein expression.

High glucose (HG)-induced oxidative stress is associated with apoptosis in pancreatic β-cells. The protective effect of astaxanthin-s-allyl cysteine diester (AST-SAC) against HG-induced oxidative stress in pancreatic β-cells (βTC-tet cell line) in was studied. βTC-tet cell line was exposed to HG in the presence and absence of AST-SAC.

Aquaporin 9 regulates Leydig cell steroidogenesis in diabetes.

Diabetes mellitus induced hyperglycemia increases oxidative stress, which contributes to impairment of male reproductive function. Aquaporins (AQPs) belong to a transmembrane protein superfamily containing 13 isoforms (AQP0-12), differentially expressed in various organs, and play a pivotal role in male reproductive function. In the current study, we investigated the relationship between AQPs and testicular steroidogenesis under hyperglycemia and .

and investigation of anticancer effect of newly synthesized nonivamide-s-allyl cysteine ester.

Nonivamide (NOV), less pungent analogue of capsaicin present in various species is known for various biological properties. S-allyl cysteine (SAC) abundantly present in aged garlic extract is gaining importance for anticancer property. NOV was esterified with SAC to increase the biological activity.

Astaxanthin-s-allyl cysteine diester against high glucose-induced neuronal toxicity in vitro and diabetes-associated cognitive decline in vivo: Effect on p53, oxidative stress and mitochondrial function.

Neuroprotective effect of astaxanthin-s-allyl cysteine diester (AST-SAC) against high glucose (HG)-induced oxidative stress in in vitro and cognitive decline under diabetes conditions in in vivo has been explored. Pretreatment of AST-SAC (5, 10 and 15 μM) dose-dependently preserved the neuronal cells (SH-SY5Y) viability against HG toxicity through i) decreasing oxidative stress (decreasing reactive oxygen species generation and increasing endogenous antioxidants level); ii) protecting mitochondrial function [oxidative phosphorylation (OXPHOS) complexes activity and mitochondrial membrane potential (MMP)]; and iii) decreasing p53 level thereby subsequently decreasing the level of apoptotic marker proteins. Male Spraque-Dawley rats were orally administered AST-SAC (1 mg/kg/day) for 45 days in streptozotocin-induced diabetes mellitus (DM) rats.

In silico, theoretical biointerface analysis and in vitro kinetic analysis of amine compounds interaction with acetylcholinesterase and butyrylcholinesterase.

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are considered important target for drug design against Alzheimer's disease. In the present study in silico analysis; theoretical analysis of biointerface between ligand and interacting amino acid residues of proteins; and in vitro analysis of enzyme inhibition kinetics were carried out to delineate the inhibitory property of amine compounds against AChE/BChE. High throughput virtual screening of amine compounds identified three compounds (2-aminoquinoline, 2-aminobenzimidazole and 2-amino-1-methylbenzimidazole) that best interacted with AChE/BChE.

The possible role of sirtuins in male reproduction.

Global influence of male infertility is increasing in recent decades. Proper understanding of genetics, anatomy, physiology and the intricate interrelation of male reproductive system are much needed for explaining the etiology of male infertility; and a detailed study on the epigenetics, indeed, will reveal the molecular mechanism behind its etiology. Sirtuins, the molecular sensors, are NAD dependent histone deacetylases and ADP- ribosyl transferases, participate in the chief events of epigenetics.

Could aquaporin modulators be employed as prospective drugs for COVID-19 related pulmonary comorbidity?

COVID-19 initially an epidemic caused by SARS-CoV-2 has turned out to be a life- threatening global pandemic with increased morbidity and mortality. The presence of cytokine storm has been linked with the pathogenesis of severe lung injury as evinced in COVID-19. Aquaporins (AQPs) are molecular water channels, facilitating water transport across the cell membrane in response to osmotic gradients.

Inhibition of glutathione and s-allyl glutathione on pancreatic lipase: Analysis through in vitro kinetics, fluorescence spectroscopy and in silico docking.

Inhibition of pancreatic lipase (PL) is considered one of the important therapeutic interventions against obesity. In the present study, the inhibition of porcine (mammalian) PL (PPL) by two tripeptides glutathione (GSH) and s-allyl glutathione (SAG) was studied. In vitro kinetic analysis was done to determine the inhibition of GSH and SAG against PPL.

Role of Aquaporins in Inflammation-a Scientific Curation.

Inflammation is a universal response mechanism existing as inter-communicator of biological systems. Uncontrolled or dysregulated inflammation addresses chronic low-grade effects eventually resulting in multimorbidity. Active solute transport across the membrane establishes varying osmotic gradients.

Role of Aquaporins in Spermatogenesis and Testicular Steroidogenesis.

The transport of water and several other small molecules across cell membranes is vital in many of the processes underlying reproduction. Fluid transport in cells and tissues inclusive of male reproductive organs are regulated by disparate isoforms of aquaporins (AQPs) in living organisms. Alteration in the expression, function and/or regulation of AQPs leads to some forms of male subfertility and infertility.

Purification of fucoxanthin from Sargassum wightii Greville and understanding the inhibition of angiotensin 1-converting enzyme: An in vitro and in silico studies.

The isolation and purification of active components from the brown algae Sargassum.wightii is highly limited. In the present study, fucoxanthin was purified from S.

Leaching of AuNPs from the surface of GO: Sensitive turn on fluorescence detection of toxic preservative.

Development of a novel colorimetric and turn-on fluorescent sensor for potassium metabisulphite (KMS) using graphene oxide stabilized gold nanoparticles (GO-AuNPs) was described. The red color GO-AuNPs was changed to violet while adding 250 × 10 M KMS whereas the absorbance band at 523 nm was decreased. The observed changes were ascribed to the leaching of AuNPs from GO.

In vitro and in silico analysis of novel astaxanthin-s-allyl cysteine as an inhibitor of butyrylcholinesterase and various globular forms of acetylcholinesterases.

In Alzheimer's disease (AD) and diabetes-associated cognitive decline, the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activity is increased. AChE exists as different globular molecular forms: tetramer (G4), dimer (G2) and monomer (G1). In adult brain, G4 form is abundant however in AD, the ratio of lower molecular forms (G1) to G4 form increased.

Green synthesized selenium nanoparticles using Spermacoce hispida as carrier of s-allyl glutathione: to accomplish hepatoprotective and nephroprotective activity against acetaminophen toxicity.

s-allyl glutathione (SAG) an analogue of glutathione is explored for its antioxidative and liver protection property in recent years. Selenium nanoparticles (Sh-SeNPs) were synthesized using medicinal plant Spermacoce hispida and conjugated with SAG (SAG-Sh-SeNPs). SAG-Sh-SeNPs and Sh-SeNPs were characterized using by Fourier transform infrared spectroscopy, Transmission electron microscopy, Energy dispersive X-ray analysis, X-ray diffraction analysis and zeta potential analysis.

Design, 3D QSAR modeling and docking of TGF-β type I inhibitors to target cancer.

Transforming growth factor-β (TGF-β) family members plays a vital role in regulating hormonal function, bone formation, tissue remodeling, and erythropoiesis, cell growth and apoptosis. TGF-β super-family members mediate signal transduction via serine/threonine kinase receptors located on the cell membrane. Variation in expression of the TGF-β type I and II receptors in the cancer cells compromise its tumor suppressor activities which direct to oncogenic functions.

S-allyl cysteine as potent anti-gout drug: Insight into the xanthine oxidase inhibition and anti-inflammatory activity.

S-allyl cysteine (SAC) is known for its various beneficial effects such as neuroprotection and immunomodulation. The beneficial effect of SAC against gout has not been explored. The present study aims to describe the two roles of SAC: (1) inhibitory effect against xanthine oxidase (XO) enzyme activity; and (2) anti-inflammatory property against MSU crystal-induced gouty inflammation in rat.

Biological interaction of newly synthesized astaxanthin-s-allyl cysteine biconjugate with Saccharomyces cerevisiae and mammalian α-glucosidase: In vitro kinetics and in silico docking analysis.

In humans, alpha-glucosidase activity is present in sucrase-isomaltase (SI) and maltase-glucoamylase (MGAM). α-glucosidase is involved in the hydrolyses of disaccharide into monosaccharides and results in hyperglycemia. Subsequently chronic hyperglycemia induces oxidative stress and ultimately leads to the secondary complications of diabetes.

S-allyl-glutathione, a synthetic analogue of glutathione protected liver against carbon tetrachloride toxicity: Focus towards anti-oxidative efficiency.

A simple analogue of well known natural antioxidant glutathione (GSH) called S-allyl-glutathione (SAG) was evaluated against carbon tetrachloride (CCl)-induced oxidative stress liver injury in rat. Pretreatment of SAG attenuated the CCl-toxicity induced elevation of liver injury markers such as enzymes (AST, ALT, GGT, ALP and LDH) and bilirubin in the blood circulation. Such protective effect of SAG resulted in preservation of liver function observed as normal level of total protein and albumin in plasma as well as inhibition of dyslipidemia in liver.

Asiatic acid prevents the quinolinic acid-induced oxidative stress and cognitive impairment.

Increased accumulation of endogenous neurotoxin quinolinic acid has been found in various neurodegenerative diseases. Oxidative stress caused by quinolinic acid is considered as imperative factor for its toxicity. Asiatic acid, a natural triterpene is widely studied for its various medicinal values.

Rapid biosynthesis of Bauhinia variegata flower extract-mediated silver nanoparticles: an effective antioxidant scavenger and α-amylase inhibitor.

Silver nanoparticles (AgNPs) were biosynthesized using Bauhinia variegata flower extract (BVFE). The BVF-AgNPs was found to be spherical shaped with the size of 5-15 nm. The phytoconstituents analysis and FTIR spectrum indicated that bioactive compounds like, phenols, flavonoids, benzophenones, nitro compounds, aromatics and aliphatic amines from BVFE might absorb on the surface of BVF-AgNPs.

Plant extract as environmental-friendly green catalyst for the reduction of hexavalent chromium in tannery effluent.

The aqueous extract of various plants like Coriandrum sativum (AECS), Alternanthera tenella colla (AEAT), Spermacoce hispida (AESH) and Mollugo verticillata (AEMV) was studied for its hexavalent chromium (Cr) reduction property. Even though antioxidant activity was present, AEAT, AESH and AEMV did not reduce Cr. AECS showed rapid and dose-dependent Cr reduction.