Two New α-Glucosidase Inhibitors from Haplophyllum tuberculatum: Inhibition Kinetics and Mechanistic Insights Through in Vitro and in Silico Approaches.

Diabetes is a multifactorial global health disorder marked by unusually high plasma glucose levels, which can lead to serious consequences including diabetic neuropathy, kidney damage, retinopathy, and cardiovascular disease. One effective therapy approach for reducing hyperglycemia associated with type 2 diabetes is to target α-glucosidase, enzymes that catalyze starch breakdown in the intestine. In the current study, two new (1, 2) and nine known (3-11) compounds were isolated from the rutaceous plant Haplophyllum tuberculatum and characterized by extensive nuclear magnetic resonance spectroscopic techniques and high-resolution electrospray ionization mass spectrometry.

The vascular effects of peppermint ( L) on aorta in a mouse model: an and computational study.

The present study examined the vascular effects of peppermint or mint () using an abdominal aortic rings model. Concentration-response curves for mint oil were generated after precontracting isolated mouse aorta with phenylephrine. The effect of different receptor antagonists and ion channel or enzyme inhibitors on the vasorelaxant potential of mint oil were studied.

Chrysophanol attenuates cognitive impairment, neuroinflammation, and oxidative stress by TLR4/NFκB-Nrf2/HO-1 and BDNF/VEGF signaling in stress-intensified PTZ induced epilepsy in mice.

Background: Stress is among the most common comorbid conditions with epilepsy and a strong factor in the pathophysiology of seizures. An imbalance in neuronal circuits causes recurrent unprovoked seizures in epilepsy. Dysregulation of BDNF/VEGF expression, oxidative stress, increased levels of neuroinflammatory cytokines, and increased expression of apoptotic genes contribute to the underlying cause of the seizure.

Novel Anti-Tumor Effect of Natural Products from Aloe vera Resin and their In-Vitro/In-Silico Targeting Mechanism of Carbonic Anhydrase-II and IX.

Human carbonic anhydrase (hCA) plays a vital role in the development and progression of tumors in hypoxic conditions. Herein we report the hCA-II and hCA-IX activities of natural products isolated from Aloe vera (L.) Burm.

Triterpenoids from Frankincense and Boswellia: A focus on their pharmacology and C-NMR assignments.

Here we report for the first time the entire C-NMR spectral assignments of 119 (out of 127) triterpenoids from the oleo-gum resins of the medicinally important genus Boswellia, which includes the culturally highly valuable Frankincense species. The complete C-NMR resonances of these triterpenoids isolated between 1998 and 2024 and their biological activities are presented. C-NMR spectroscopy is a highly powerful tool for the characterization of these bioactive natural products.

Novel efficacy of pregnane and flavonoid glycosides from in in vivo nociceptive and inflammatory paradigms and their target prediction by cheminformatics approach.

Inflammation is associated with multiple life-threatening conditions. is an edible plant and traditionally used for managing various diseases. Three novel molecules, namely desmiflavaside-C (), nizwaside (), and desmiflanoside () were isolated from , and their structures were confirmed by mass spectrometry and through reported literature.

The Interplay of Carveol and All-Trans Retinoic Acid (ATRA) in Experimental Parkinson's Disease: Role of Inflammasome-Mediated Pyroptosis and Nrf2.

Parkinson's disease (PD) is a debilitating and the second most common neurodegenerative disorder with a high prevalence. PD has a multifaceted etiology characterized by an altered redox state and an excessive inflammatory response. Extensive research has consistently demonstrated the role of the nuclear factor E2-related factor (Nrf2) and inflammasomes, notably NLRP3 in neurodegenerative diseases.

Disrupting protease and deubiquitinase activities of SARS-CoV-2 papain-like protease by natural and synthetic products discovered through multiple computational and biochemical approaches.

The single-stranded RNA genome of SARS-CoV-2 encodes several structural and non-structural proteins, among which the papain-like protease (PLpro) is crucial for viral replication and immune evasion and has emerged as a promising therapeutic target. The current study aims to discover new inhibitors of PLpro that can simultaneously disrupt its protease and deubiquitinase activities. Using multiple computational approaches, six compounds (CP1-CP6) were selected from our in-house compounds database, with higher docking scores (-7.

Exploring the Anticancer Potential of Astragalin in Triple Negative Breast Cancer Cells by Attenuating Glycolytic Pathway through AMPK/mTOR.

Background: Aerobic glycolysis is crucial for cancer cells to survive, grow, and progress. In the current study, the anti-cancer effects of astragalin (ASG) on breast cancer cells and in the glycolytic pathway through AMPK/mTOR have been evaluated.

Objective: The objective of this study was to examine the impact of ASG, a natural flavonoid, on glycolysis via targeting AMPK/mTOR signalling in MDA-MB-231 breast cancer cells.

Identification of small molecular inhibitors of SIRT3 by computational and biochemical approaches a potential target of breast cancer.

Sirtuin 3 (SIRT3) belongs to the Sirtuin protein family, which consists of NAD-dependent lysine deacylase, involved in the regulation of various cellular activities. Dysregulation of SIRT3 activity has been linked to several types of cancer, including breast cancer. Because of its ability to stimulate adaptive metabolic pathways, it can aid in the survival and proliferation of breast cancer cells.

Unraveling the multi-faceted role of Rosmarinus officinalis L. (rosemary) and diosmetin in managing gut motility.

Ethnopharmacological Relevance: Rosmarinus officinalis L. (Rosemary) is a popular herb with reported effectiveness against diarrhea, anxiety and constipation, albeit with limited pharmacological evidence.

Aim Of The Study: The current study was aimed at evaluating the therapeutic potential, possible pharmacological mechanisms of action and active constituents of hydro-ethanolic extract of rosemary (Rs.

Designing and Synthesis of Novel Fexofenadine-Derived Hydrazone-Schiff Bases as Potential Urease Inhibitors: In-Vitro, Molecular Docking and DFT Investigations.

Thirteen novel hydrazone-Schiff bases (3-15) of fexofenadine were succesfully synthesized, structurally deduced and finally assessed their capability to inhibit urease enzyme (in vitro). In the series, six compounds 12 (IC=10.19±0.

Novel Natural Inhibitors for Glioblastoma by Targeting Epidermal Growth Factor Receptor and Phosphoinositide 3-kinase.

Background/aim: Glioblastoma is an extensively malignant neoplasm of the brain that predominantly impacts the human population. To address the challenge of glioblastoma, herein, we have searched for new drug-like candidates by extensive computational and biochemical investigations.

Methods: Approximately 950 compounds were virtually screened against the two most promising targets of glioblastoma, i.

Discovery of Novel Natural Inhibitors Against SARS-CoV-2 Main Protease: A Rational Approach to Antiviral Therapeutics.

Background/aim: The global pandemic caused by the novel SARS-CoV-2 virus underscores the urgent need for therapeutic interventions. Targeting the virus's main protease (Mpro), crucial for viral replication, is a promising strategy.

Objective: The current study aims to discover novel inhibitors of Mpro.

Calcium Channel Inhibitory Effect of Marjoram ( L.): Its Medicinal Use in Diarrhea and Gut Hyperactivity.

Background: The leaves of () are traditionally renowned for treating diarrhea and gut spasms. This study was therefore planned to evaluate its methanolic extract.

Methods: Gas chromatography-mass spectrometry (GC-MS) was used to identify the phytochemicals, and Swiss albino mice were used for an antidiarrheal assay.

Pharmacological Basis for the Antidiarrheal and Antispasmodic Effects of Cuminaldehyde in Experimental Animals: , and Studies.

Background: Medicinal herbs are frequently used for the management of gastrointestinal disorders because they contain various compounds that can potentially amplify the intended therapeutic effects. Cuminaldehyde is a plant-based constituent found in oils derived from botanicals such as cumin, eucalyptus, myrrh, and cassia and is responsible for its health benefits. Despite the utilization of cuminaldehyde for several medicinal properties, there is currently insufficient scientific evidence to support its effectiveness in treating diarrhea.

Attenuation of Streptozotocin-Induced Diabetic Neuropathic Allodynia by Flavone Derivative Through Modulation of GABA-ergic Mechanisms and Endogenous Biomarkers.

Diabetic neuropathic pain is one of the most devasting disorders of peripheral nervous system. The loss of GABAergic inhibition is associated with the development of painful diabetic neuropathy. The current study evaluated the potential of 3-Hydroxy-2-methoxy-6-methyl flavone (3-OH-2'MeO6MF), to ameliorate peripheral neuropathic pain using an STZ-induced hyperglycemia rat model.

Targeting papain-like protease by natural products as novel therapeutic potential SARS-CoV-2.

The highly infectious respiratory illness 'COVID-19' was caused by SARS-CoV-2 and is responsible for millions of deaths. SARS-single-stranded viral RNA genome encodes several structural and nonstructural proteins, including papain-like protease (PLpro), which is essential for viral replication and immune evasion and serve as a potential therapeutic target. Multiple computational techniques were used to search the natural compounds that may block the protease and deubiquitinase activities of PLpro.

Polyhydroquinoline derivatives for diabetic management: synthesis, and approaches.

Medication used to treat Type 2 diabetes by decreasing the absorption of carbohydrates in the intestine consists of α-glucosidase inhibitors. Polyhydroquinoline derivatives have attracted interest as excellent antidiabetic agents. Polyhydroquinoline derivatives () were synthesized and tested for α-glucosidase inhibitory activity.

Quercetin Alleviated Inflammasome-Mediated Pyroptosis and Modulated the mTOR/P70S6/P6/eIF4E/4EBP1 Pathway in Ischemic Stroke.

Stroke ranks as the world's second most prevalent cause of mortality, and it represents a major public health concern with profound economic and social implications. In the present study, we elucidated the neuroprotective role of quercetin on NLRP3-associated pyroptosis, Nrf2-coupled anti-inflammatory, and mTOR-dependent downstream pathways. Male Sprague Dawley rats were subjected to 72 h of transient middle cerebral artery ischemia, followed by the administration of 10 mg/kg of quercetin.

Enhanced cardioprotective activity of ferulic acid-loaded solid lipid nanoparticle in an animal model of myocardial injury.

Myocardial infarction results in an increased inflammatory and oxidative stress response in the heart, and reducing inflammation and oxidative stress after MI may offer protective effects to the heart. In the present study, we examined the cardioprotective effects of ferulic acid (FA) and ferulic acid nanostructured solid lipid nanoparticles (FA-SLNs) in an isoproterenol (ISO) induced MI model. Male Sprague Dawley rats were divided into five experimental groups to compare the effects of FA and FA-SLNs.

In-vivo anti-diabetic and anti-hyperlipidemic effects of natural metabolites from resin of Commiphora mukul and their in-silico to in-vitro target fishing.

Diabetes mellitus is a rapidly spreading global metabolic disorder that has serious social, health, and economic consequences. Herein, we have evaluated in vivo antidiabetic and antihyperlipidemic effects of myrrhanone-B and myrrhanol-B (isolated from Commiphora mukul Hook). We observed that treatment with myrrhanone-B and myrrhanol-B at a dose of 5 and 10 mg/kg body weight for 21 days significantly improved body weight loss, water consumption, and the concentration of blood glucose level (BGL) in alloxan (120 mg/kg) induced diabetic mice, which indicates that the compounds possess strong anti-diabetic activities.