Delving into the Latest Updates on D-Pinitol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cerebrate, Pinitol

+ [2]

Target

APP x γ-secretase

Action

inhibitors

Mechanism

APP inhibitors(Beta amyloid A4 protein inhibitors), γ-secretase inhibitors(Gamma-secretase inhibitors)

Therapeutic Areas

Urogenital Diseases

Active Indication

Renal fibrosis

Inactive Indication

Alzheimer Disease

Originator Organization

Icahn School of Medicine at Mount Sinai

Active Organization

The Catholic University of Korea

Inactive Organization

Humanetics Corp.

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC7H14O6

InChIKeyDSCFFEYYQKSRSV-KLJZZCKASA-N

CAS Registry10284-63-6

ETHNOPHARMACOLOGICAL RELEVANCEGymnopodium floribundum Rolfe, known locally as "Dzidzilche" or "Ts'its'ilche," is a native species from Mexico and Central America. In Mayan communities, this plant is used to relieve inflammation and diverse respiratory diseases such as colds, catarrh, bronchitis, and asthma. Usually, a decoction of leaves or flowers is prepared and administered orally.AIMThis research explores the anti-inflammatory effects of the methanol extract of Gymnopodium floribundum Rolfe leaves (MGF) using in vitro and in vivo animal models of inflammation.METHODSMGF was characterized by GC-MS, and cytotoxicity was assessed using hemolysis and MTT assays. The antiphlogistic effect in vitro was measuring the release of cytokines, hydrogen peroxide, and nitric oxide in macrophages stimulated with LPS. Additionally, anti- and pro-inflammatory cytokines, prostaglandins, and leukotrienes in serum were quantified in carrageenan-induced mouse paw edema. Finally, 1-fluoro-2,4-dinitrobenzene (DNFB)-induced delayed-type hypersensitivity and TPA-induced ear edema models were analyzed.RESULTSCompounds found in MGF, such as D-pinitol and protocatechuic (3,4-dihydroxybenzoic) acid, are reported to exert anti-inflammatory effects. MGF showed no hemolytic or cytotoxic effects. Nevertheless, it displayed in vitro anti-inflammatory activity by decreasing the release of IL-6, IL-1β, TNF-α, hydrogen peroxide, and nitric oxide levels; on the other hand, it increased IL-10 production. Furthermore, the MGF significantly reduced inflammation in mouse models and reduced the release of leukotrienes, prostaglandins, and pro-inflammatory cytokines.CONCLUSIONGymnopodium floribundum Rolfe exhibits anti-inflammatory activity by suppressing pro-inflammatory mediators, altering cell migration mechanisms, and raising IL-10 production.

17 Mar 2025·ACS Applied Bio Materials

Fabricating Silver Nanoparticles with Antidiabetic d-Pinitol to Restrict Amyloid Formation of Insulin

Article

Author: Kar, Karunakar ; Mishra, Nishant ; Prajapati, Kailash Prasad ; Mittal, Shikha ; Mahato, Om Prakash ; Ansari, Masihuzzaman ; Anand, Bibin Gnanadhason

In this study, we synthesized silver nanoparticles functionalized with antidiabetic d-pinitol molecules and investigated their anti-amyloid effect on Insulin aggregation. Our results show that these functionalized nanoparticles effectively inhibit both spontaneous and seed-induced amyloid aggregation of Insulin in a dose-dependent manner. The d-pinitol-functionalized silver nanoparticles interact directly with the aggregation-prone regions of Insulin's partially unfolded structures, as demonstrated by quenching and computational experiments. Analysis of docking and simulation data suggests that antiamyloid activity of d-pinitol functionalized AgNPs is due to a strong Insulin-nanoparticle interaction, facilitated via hydrogen bonds. These interactions disrupt the Insulin monomer-dimer equilibrium and prevent the formation of toxic amyloid structures. The results could lead to the development of d-pinitol-based Insulin-stabilizing nanoformulations with potential antidiabetic properties.

01 Mar 2025·Brazilian Journal of Microbiology

Pioneering study of Egyptian Neem and Jojoba extracts with molecular docking combat hospital multidrug resistant bacteria

Article

Author: Salama, Hanaa Mohamed ; Khairy, Toka ; Amin, Dina Hatem ; Elkholy, Iman Mohamed Amin ; Sayed, Hayam Abd Elnabi ; Elnakib, Mostafa ; Gebreel, Hassan Mahmoud

Hospital surfaces are often contaminated with multidrug-resistant pathogenic bacteria that cause healthcare-associated infections and lead to increased mortality and morbidity. There is a need for new alternative antibacterial agents to overcome antibiotic resistance. Azadirachta indica and Simmondsia chinensis have been found to possess antibacterial activity and medicinal value. The antibacterial activity of these plant extracts against clinical isolates was investigated using the agar disc diffusion method. These clinical isolates included E. coli, Pseudomonas aeruginosa, Acinetobacter spp., Klebsiella pneumoniae, Stenotrophomonas maltophilia, and methicillin-resistant Staphylococcus aureus (MRSA), which were identified by the vitek-2 system, and resistance genes of selected bacterial strains were identified by using the bioFire FilmArray test. The most potent extract of these plants was the ethanolic extract, where the inhibition percentage of ethanolic Jojoba and Neem extracts was 90.9% and 74.5%, respectively against all the tested pathogens. On the other hand, the methanolic extracts of Neem and Jojoba have different degrees of antibacterial activity against the tested pathogens. The phytochemical components of the most potent extracts (ethanolic extracts) were investigated by gas chromatography‒mass spectrometry (GC\MS), which revealed that the ethanolic extracts were enriched in phenolics, flavonoids, and sugars. FTIR analyses of the plant extracts confirmed the presence of alcoholic, carboxylic, and aldehydic moieties. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) activity of the ethanolic extracts of Neem and Jojoba increased in a dose-dependent manner, with average IC50 values of 98.17 ± 0.85, 4.95 ± 0.06, and 4.17 ± 0.04 mg/mL, respectively, for the ethanolic Neem extract, the ethanolic Jojoba extract, and ascorbic acid (standard). Furthermore, increased cytotoxicity was demonstrated in the HFB4 cell line in a dose-dependent manner. The average IC50s of the ethanolic Neem extract and the ethanolic Jojoba extract were 18.18 ± 0.15 and 76.16 ± 1.49 mg/mL, respectively. Moreover, the results for the antibiofilm activity of the ethanolic Neem extract showed that 99.5% of the biofilms formed at 25 mg/ml. In addition, 50 mg/ml of the ethanolic extract of Jojoba had a suppressive effect of 98.2%. The significant components Nonanoic acid (21.9405%) and Palmitic Acid (16.0869%) from Neem and pinitol from Jojoba (82.85%) were selected throughout the molecular docking investigation, by which the chosen constituents inhibited the crystal structure of penicillin-binding protein 4 (PBP4) from Staphylococcus aureus (PDB ID: 1TVF) and the crystal structure of the OXA-48 beta-lactamase (PDB ID: 7AUX) from K. pneumoniae. Overall, our study reveals the effectiveness of antimicrobial plant extracts as therapeutic solutions for antibiotic resistance in Egypt and worldwide with some modifications to decrease their cytotoxicity.

100 Deals associated with D-Pinitol

Login to view more data