Delving into the Latest Updates on Arbutin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Arbutoside, Ursin, Uvasol

Target

TYR

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

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 UGT72 gene family encodes proteins that glycosylate phenylpropanoids, and thus contribute to the synthesis of various phenolic substances. However, their functional role and evolutionary history in Pyrus spp. remains poorly understood. Here we explored the evolution, amplification, coding region structural variation, and functional divergence of the UGT72 gene family and its subfamilies. Further, we identified functional genes involved in arbutin synthesis and functionally validated the key genes. 15 UGT72 genes were identified in the complete genome sequence and classified into two subfamilies of Pyrus betulifolia. Significant expansion of the UGT72 gene family occurred after genome duplication in P. betulifolia. 53.33 % of all UGT72 family genes were found to have undergone expansion via WGD/segmental duplication. A noteworthy discovery was that the amplification of functional genes such as PbUGT72B1714 during polyploidization, combined with the loss of vital motifs and variations at important sites within these genes, significantly impacted the diversification of arbutin metabolism. These findings offer novel insights into how gene gains and losses caused by WGDs have contributed to metabolic diversification and evolutionary adaptation in Pyrus, as well as a groundwork for more detailed investigations into the mechanisms of arbutin metabolism.

01 Jan 2025·Journal of Food Science

A comprehensive profiling of phenolic compounds and antioxidant activities of 24 varieties of red raspberry cultivated in Northeast China

Article

Author: Wang, Jinling ; Zhang, Haonan ; Zhang, Hegu ; Zhao, Xin ; Yu, Yiping

AbstractRed raspberries, valued for their nutrients and bioactive compounds, have broad uses in processing and healthy products. However, limited comprehensive research focused on the comparison of phenolic compounds of red raspberry, especially species cultivated in Northeast China, has been reported. This study aimed to conduct a thorough investigation of 24 red raspberry varieties in Northeast China for the first time, evaluating their phenolic compounds and antioxidant capacities. The results showed that ‘DNS1’ had the highest total phenolic content (TPC), ‘Willamette’ had the highest total flavonoid content (TFC), and ‘Boyne’ had the highest total anthocyanin content (TAC). Phenolic compounds in red raspberries were predominantly found in esterified form, while glycosylated phenolics should not be overlooked. Chlorogenic acid, cryptochlorogenic acid, ellagic acid, and arbutin were the main phenolic compounds, and the distribution of their contents varied between varieties. The antioxidant activity in the red raspberry had a close association with the content of phenolic compounds. Principal component analysis (PCA) showed that phenolic compounds and antioxidant activities were higher in samples from ‘DNS1’, ‘Boyne’, ‘Beijing10’, ‘DNS5’, and ‘Willamette’ varieties. These varieties should be given priority in breeding programs that aim to boost the utility and bioactive profile of red raspberries.Practical ApplicationRed raspberry is becoming a desirable commercially grown fruit species and is viewed as a new functional food. In this context, this research offers strong support for confirming the quality of 24 varieties of red raspberry and plays a critical role in the food industry. It also indicates the potential sources of superior varieties of red raspberry, which are advantageous for growers and consumers in search of high‐quality red raspberry varieties.

01 Jan 2025·Journal of Cosmetic Dermatology

The Efficacy of Topical Cosmetic Containing Alpha‐Arbutin 5% and Kojic Acid 2% Compared With Triple Combination Cream for the Treatment of Melasma: A Split‐Face, Evaluator‐Blinded Randomized Pilot Study

Article

Author: Sripha, Apinya ; Chongmelaxme, Bunchai ; Tantanasrigul, Pimpa

ABSTRACTBackgroundWhile the gold standard treatment for melasma is triple combination cream (TCC), arbutin and kojic acid demonstrate their benefits and may be used as an alternative.AimsTo investigate the efficacy of cream containing alpha‐arbutin 5% and kojic acid 2% (AAK) compared with TCC for melasma treatment.Patients/MethodsA split‐faced, randomized study was conducted among 30 participants with melasma, and all were randomized to receive AAK or TCC on each side of their face for 12‐week along with 4‐week follow‐up period. The melanin index (MI), modified Melasma Area Severity Index (mMASI), and physician global assessment (PGA) scores were used to measure the effectiveness of interventions. Recurrence of melasma after treatment discontinuation was evaluated by MI and mMASI. Patient satisfactions and adverse effects were also evaluated. In the analysis, the mean difference (MD) was used for MI and mMASI, while Wilcoxon signed‐rank test was for the PGA scores, adverse effects, and patient satisfaction.ResultsThe MD of MI and mMASI scores were not different between groups (mMASI [p = 0.344] and MI [p = 0.268]). The PGA scores only showed improvement on the TCC‐treated side (p = 0.032). Compared to the AKK group, the subjects with TCC showed higher severity of recurrence (MI [p = 0.004] and mMASI [p = 0.045]). No difference in patient satisfaction score between the groups, but erythema and stinging were higher in the TCC group.ConclusionsThe AAK cream appeared to be effective for melasma treatment, highlighting a lower recurrent rate and fewer adverse events than standard therapy.Trial Registration: thaiclinicaltrials.org: TCTR20230124004

100 Deals associated with Arbutin

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