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dihydroxyacetone (Nigrantil)

✓ Approved

Vinas · Small Molecule · Small Molecule

What is dihydroxyacetone?

dihydroxyacetone is a small molecule developed by Vinas. It is approved for therapeutic indications.

Drug Profile

Brand NamesNigrantil
CompanyVinas
Drug ClassSmall Molecule
StatusApproved

Therapeutic Indications

dihydroxyacetone is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Skin and subcutaneous tissue disordersVitiligo✓ Approved

Related Research Articles

PubMedVeterinary research2026-05-20

Metabolomic signatures of colonic infection by Brachyspira hyodysenteriae.

Pérez-Pérez Lucía L, Galisteo Cristina C, Castillo-Peinado Laura de Los Santos LLS, Tomé-Rodríguez Sonia S et al.

Despite swine dysentery's relevance in the pork industry, there are still gaps in our understanding of its pathogenesis and the impact of the infection in the gut. This study aimed to characterize the in vivo colonic metabolome of pigs experimentally infected with Brachyspira hyodysenteriae at the onset of fecal shedding (Early_inf group, n = 6) and during acute clinical disease characterized by mucohemorrhagic diarrhea (Acute_inf group, n = 8) compared with non-infected controls (n = 16). The metabolic profile of the colonic contents changed progressively with disease severity, showing an intermediate pattern in the Early_inf group between the control and the Acute_inf groups (p < 0.05). In acute disease, the metabolome was defined by increased concentrations of amino acids, carnitine derivatives, arachidic acid, 1,2-butanediol, and lactic acid, along with decreased levels of anti-inflammatory compounds. In the Early_inf group, increases were observed in amino acids, organic acids, amines, myo-inositol, quinoline, and 1,2-butanediol, whereas linolenic acid and oxalic acid decreased. Integrated analysis of the colonic metabolome and metagenome revealed a strong correlation between metabolic and microbial profiles, particularly in the Acute_inf group, where differential metabolites were associated with B. hyodysenteriae, Campylobacter hyointestinalis, and Velocimicrobium ethanolgignens. Metabolites showed high predictive potential for the disease stage, with lactic acid and arachidic acid being key markers of acute infection and dihydroxyacetone and leucine distinguishing early infection. Overall, this study reveals significant alterations in the colonic metabolome and its association with the microbiota during swine dysentery, providing new insights into the pathophysiology of the disease and contributing to the development of improved prevention and treatment strategies.

PubMedACS nano2026-05-15

Ligand-Driven Aldehyde Condensation via Zeolitic Imidazolate Framework-Based Pro-Nanozymes with Formolase-like Activity.

Shi Wei W, Wang Qian Q, Sun Minmin M, Yu Yixin Y et al.

The sustainable conversion of formaldehyde (FA) into high-value carbohydrate compounds via C-C condensation by formolase (FLS) is critically significant yet challenging, primarily due to its instability under high FA concentrations and its high cost. Here, we demonstrate that zeolitic imidazolate frameworks (ZIF-67 series) function as FLS-like pro-nanozymes, whose activity is initiated by water-mediated hydrolysis. This process releases metal-imidazole coordination clusters capable of catalyzing the condensation of FA and glycolaldehyde (GA) mainly into glyceraldehyde (GCA) and dihydroxyacetone (DHA) under neutral aqueous conditions. The products comprise 59% C3 carbohydrates and 41% C4 carbohydrates, with tolerance to a temperature up to 90 °C and FA concentrations up to 250 mM. Mechanism analyses demonstrate that the nucleophilicity (basicity) of N atoms in the imidazole-based ligands is critical for activating GA's α-H to form enolate anions, thereby initiating the C-C condensation with FA. The product yield and variety can be modulated by introducing different substituents into imidazole ligands and coordinating with metal ions (e.g., Zn, Co, or Ni), respectively. This work not only develops an effective strategy for rationally designing FLS-like pro-nanozymes with ZIF materials but also establishes an efficient platform for the green synthesis of multicarbon carbohydrates upon carbon recycling.

PubMedPloS one2026-05-14

Enhanced production of l-fuculose by Escherichia coli engineered via genome-scale metabolic modeling.

Yeon Gun-Hwi GH, Kang Du-Kyeong DK, Koo Hyun-Jin HJ, Go Daewon D et al.

l-Fuculose is a rare deoxyketohexose sugar and is a structural isomer of l-fucose, which exhibits skin-lightening, moisturizing, and anti-aging effects. Due to their structural similarity, l-fuculose is also expected to provide potential health benefits. However, l-fuculose exists only in trace amounts in nature, making extraction from natural sources virtually impossible; to date, it has been synthesized mainly by enzymatic conversion. This approach, however, suffers from major limitations: both the substrate (l-fucose) and the enzyme involved (l-fucose isomerase) are costly; the enzymatic reaction cannot achieve complete conversion due to the chemical equilibrium; and the methods for purification of l-fuculose from the reaction mixture containing both l-fucose and l-fuculose are inefficient and uneconomical. Microbial cell factories have been explored as an alternative route for l-fuculose biosynthesis, but their production titers remain extremely low, limiting their industrial applicability. In this study, a microbial cell factory was engineered in Escherichia coli by redirecting the pathway of l-fucose metabolism toward l-fuculose production. Overexpression of fucA enabled the aldol condensation of lactaldehyde and dihydroxyacetone phosphate to produce l-fuculose-1-phosphate, which was subsequently dephosphorylated to l-fuculose by a sugar phosphatase. To prevent diversion of substrates and products into competing pathways, the fucI, fucK, tpiA, fucO, and aldA genes were deleted. The final engineered strain produced 50.25 ± 4.30 mg/L of l-fuculose, a 32.4-fold increase compared to that achieved previously by microbial biosynthesis. This study establishes a foundation for the industrial production of l-fuculose, which has potential application as a valuable ingredient in cosmetics, functional foods, and pharmaceuticals.

PubMedChemMedChem2026-04-26

A Novel Triose Phosphate Isomerase Inhibitor With Dual Trypanosomicidal Activity was Identified Using Artificial Intelligence-Based Virtual Screening.

Aguilera Elena E, Ramos Rachel R, Davtyan Aram A, Cabrera Nallely N et al.

Chagas disease and leishmaniasis are neglected protozoan diseases recognized by the World Health Organization as major public health problems. These diseases affect millions of people worldwide, yet effective treatments remain unavailable. Triosephosphate isomerase (TIM), a glycolytic enzyme that exhibits high catalytic efficiency for the isomerization of glyceraldehyde-3-phosphate and dihydroxyacetone-phosphate exclusively in its dimeric form, was subjected to virtual screening. Using a deep neural network for structure-based drug design that predicts binding affinity between small molecules and proteins of known structure, 12.5 million commercially available compounds were screened. From this, 82 compounds were selected for in vitro evaluation. Six compounds inhibited TIM from Trypanosoma cruzi, three of which exhibited anti-T. cruzi activity. Eight compounds demonstrated activity against the parasites T. cruzi and Leishmania infantum. Two compounds showed similar potency against both parasites: 3-(1-acetyl-5-(4-bromophenyl)-4,5-dihydro-1H-pyrazol-3-yl)-4-hydroxy-6-methyl-2H-pyran-2-one (IC50 = 16 ± 3 μM) and 3-[(4-bromophenyl)sulfanyl]-1-(3-nitrophenyl)propan-1-one (IC50 = 12 ± 1 μM). These compounds exhibit favorable selectivity and toxicological profiles, as well as in vivo activity, indicating their potential for future drug development.

PubMedEMBO reports2026-04-15

Glycerol enhances mitochondrial metabolism and inflammatory response in pro-inflammatory macrophages.

Tanaka Manami M, Hishiki Takako T, Matsuura Tomomi T, Yasui Masato M et al.

Although glycerol is a ubiquitous metabolite in mammalian systems, its cellular metabolic pathways and functions have not been fully elucidated. Here, we find that elevated extracellular glycerol modulates intracellular metabolism and pro-inflammatory responses of macrophages. In pro-inflammatory macrophages stimulated with lipopolysaccharide, glycerol is taken up through glycerol channels including Aquaporin 3 (AQP3) and metabolized to glycerol-3-phosphate (G3P), which is then converted to dihydroxyacetone phosphate by glycerol-3-phosphate dehydrogenase 2 (GPD2). This glycerol-driven pathway enhances mitochondrial ATP production, potentially by supplying electrons to the electron transport chain (ETC) via GPD2, and by upregulating the transcription of genes encoding ETC complexes. In addition, glycerol supplementation elevates intracellular acetyl-CoA levels, promotes histone acetylation at the promoters of pro-inflammatory cytokine genes, and consequently increases cytokine gene expression, suggesting enhanced pro-inflammatory response. In vivo experiments, macrophage-specific AQP3 conditional knockout mice exhibit reduced weight gain and adipose tissue inflammation in a high-fat diet-induced obesity model. Our findings provide novel insights into the metabolic regulation and macrophage inflammation by extracellular glycerol.

PubMedAdvances in experimental medicine and biology2026-04-01

The Historiography of Galactose and Its Recognition by Galectins.

Hirabayashi Jun J, Iwaki Jun J, Sato Sachiko S

A possible scenario for the origin of elementary hexoses (fructose, glucose, mannose, and galactose) has been presented (Hirabayashi 1996). The scenario suggests that the formose reaction, starting with formaldehyde (CH2O) forms the foundation of carbohydrate chemistry. The process includes key reactions, such as aldol condensation between two trioses, glyceraldehyde and dihydroxyacetone, which produces ketohexoses, including fructose. Once the fructose is produced, it undergoes the Lobry de Bruyn-Alberda van Ekenstein transformation to produce the corresponding aldohexoses, glucose and mannose, which emerged during chemical evolution. While it remains an open question how these elementary hexoses were accumulated on a prebiotic Earth, glucose is considered the most stable monosaccharide and is thus regarded as the primary substrate for "bricolage" in the subsequent biological evolution. Among these products is galactose, which results from the invention of a 4-keto-intermediate of UDP-Glc, facilitated by NADH (coenzyme). This mechanism enables both reduction and epimerization at the C3, C4, and C5 positions. From a biological recognition perspective, galactose is unique due to its axial configuration of the C4-OH group (referred to as 4-epi-Glc), which sharply distinguishes it from other major monosaccharides, such as glucose and mannose (2-epi-Glc). Moreover, as a "late-comer" saccharide in contrast to glucose and mannose, galactose is frequently positioned at the outermost regions of glycoconjugates. These characteristics likely offered multicellular organisms advantages in navigating complex cellular communities. The structural heterogeneity originating from the positioning of galactose in glycans might be further amplified by the diversification of galactose modifications, including sialylation and fucosylation-both of which are biosynthesized from mannose in modern biosystems. Glycosyltransferases for these late-comer saccharides (galactose, sialic acid, and fucose) are located downstream in the biosynthetic pathway, specifically in the Golgi apparatus. The hetero-geneity of galactose-containing epitopes likely co-evolved with the carbohydrate-recognition proteins that decode them. Among these, galectins are distinctive because, unlike most lectins, they are stored in the cytoplasm, typically isolating them from their target ligand under normal conditions. Furthermore, their sugar-binding specificity is largely restricted to β-galactosides, typically N-acetyllactosamine. However, galectins also exhibit a remarkable ability to decode the galactose-driven glycan heterogeneity for various biological functions. In this review, we explore the origin of galactose, the specificity and biological functions of these "avant-garde" lectins, and introduce galectin-driving liquid-liquid phase separation and its roles.

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