Delving into the Latest Updates on Arbutin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Arbutoside, Ursin, Uvasol

Target

TYR

Action

inhibitors

Mechanism

TYR inhibitors(Tyrosinase inhibitors)

Therapeutic Areas

Skin and Musculoskeletal DiseasesOther Diseases

Active Indication-

Inactive Indication

Melanosis

Originator Organization

Azidus Brasil

Active Organization-

Inactive Organization

Azidus Brasil

License Organization-

Drug Highest PhaseSuspendedPhase 2/3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC12H16O7

InChIKeyBJRNKVDFDLYUGJ-RMPHRYRLSA-N

CAS Registry497-76-7

The interaction between double-stranded calf thymus DNA (ctDNA) and the skin whitening agent arbutin (AR) examined by applying electrochemical and computational methods for the first time in literature. A single-use pencil graphite electrode via cyclic (CV) and differential pulse voltammetry (DPV) techniques were applied to determine the kinetic and thermodynamic parameters in the absence and presence of ctDNA. To examine the interaction process, oxidation peak currents and potentials of AR were observed prior to the addition of various ctDNA concentrations. The binding constants (K_AR-DNA) and Gibbs free energy (ΔG°) values for the AR-DNA complex were determined as 1.82 × 10⁴L/mol and -24.30 kJ/mol at 298 K, respectively. Temperature evaluation of the interaction was examined using thermodynamic parameters (ΔH°: -30.30 kJ/mol and ΔS°: -0.00197 kJ/mol) applying the Van't Hoff equation. The local interaction sites in the molecule structure were determined by applying Fukui functions and second-order perturbation theory in view of potential hydrogen binding centers. The optimized structure of AR was applied with a DNA structure revealing the binding position for AR-DNA complex. Experimental and computational examinations suggested that AR-DNA binds to ctDNA through a minor groove mode via conventional hydrogen bonds, hydrophobic interactions and van der Waals forces.

01 Jun 2025·Sugar Tech

An Assessment of Physico-Chemical Properties, Micronutrients, Polyphenolic Profile, and Antioxidant Activity of Non-Centrifugal Sugar

Author: Shah, Narendra G. ; Iyer, Yamini ; Pujari, Nisha ; Mahajani, Sanjay M. ; Gupta, Nidhi ; Dedhia, Nirali J. ; Arora, Amit

Jaggery, a non-centrifugal sugar (NCS), is regarded as a healthier option than refined sugar because of its non-sugar components.The study aimed to determine whether processing variation contributed significantly to changes in phys. characteristics, polyphenolic contents, antioxidant activity, and mineral and vitamin contents.Total of 30 (16 blocks and 14 powder) NCS samples produced in two states of India were evaluated for sugars, moisture, ash, water activity, color, total polyphenols and flavonoid contents, antioxidant activity, and mineral and vitamin contents.Profiling of polyphenolic compounds was conducted with liquid chromatog.-mass spectroscopy.In vitro radical scavenging and ferric reducing power were evaluated for antioxidant activities using whole NCS samples.Block and powder samples were found to differ in terms of the micronutrient profile, total polyphenolic content, water activity, and color index.A variation was also seen between the two selected regions of production in addition to variation within the same location.Several polyphenols, including maritimetin, prunitrin, and isoferulic acid, were found in few NCS samples.Variations among in vitro antioxidant activity could be correlated (r ≥ 0.5) to phenolics and flavonoids contents.Shelf-life assessment of representative NCS powder and blocks at two different storage conditions showed lower microbial stability of blocks compared to powders (p < 0.05).Therefore, NCS produced at the same unit during the same season cannot be considered as a standard composition of micronutrients and bioactives.This research provides more evidence demonstrating how the location, processing method, and sugarcane variety used can affect the nutritional profile of NCS and their potential health benefits.

01 May 2025·Chinese Chemical Letters

The synthesis and evaluation of novel BPA derivatives for enhanced blood-brain barrier penetration and boron neutron capture therapy

Author: Wang, Zhaoshuo ; Ding, Dandan ; Yan, Zhengzheng ; Tong, Jianfei ; Liang, Tianjiao ; Dai, Yunlu ; Liu, Huifang ; Zhang, Jinchao ; Li, Zhenhua ; Wang, Xueyi ; Mo, Shushan

Boron neutron capture therapy (BNCT) has emerged as a promising treatment for cancers, offering a unique approach to selectively target tumor cells while sparing healthy tissues.Despite its clin. utility, the widespread use of fructose-BPA (F-BPA) has been hampered by its limited ability to penetrate the blood-brain barrier (BBB) and potential risks for patients with certain complications such as diabetes, hyperuricemia, and gout, particularly with substantial dosages.Herein, a series of novel BPA derivatives were synthesized.After the primary screening, geniposide-BPA (G-BPA) and salidroside-BPA (S-BPA) exhibited high water solubility, low cytotoxicity and safe profiles for i.v. injection.Furthermore, both G-BPA and S-BPA had demonstrated superior efficacy in vitro against the 4T1 cell line compared with F-BPA.Notably, S-BPA displayed optimal BBB penetration capability, as evidenced by in vitro BBB models and glioblastoma models in vivo, surpassing all other BPA derivative candidates.Meanwhile, G-BPA also exhibited enhanced performance relative to the clin. drug F-BPA.In brief, G-BPA and S-BPA, as novel BPA derivatives, demonstrated notable safety profiles and remarkable boron delivery capabilities, thereby offering promising therapeutic options for BNCT in the clinic.

100 Deals associated with Arbutin

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