dihydroxyacetone (Nigrantil)

✓ Approved

Vinas · 小分子 · 小分子

什么是 dihydroxyacetone？

dihydroxyacetone 是一种小分子，由Vinas研发。该药已获批，用于治疗相关适应症。

药物档案

商品名	Nigrantil
公司	Vinas
药物类别	小分子
状态	Approved

来源： ClinicalTrials.gov, Vinas

治疗适应症

dihydroxyacetone 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域	疾病/病症	分期
Skin and subcutaneous tissue disorders	Vitiligo	✓ Approved

相关研究文献

PubMedCells2026-06-11

Flexible Cooperation Between Peroxisomes and the Endoplasmic Reticulum During Lipid Synthesis of Dictyostelium.

da Silva Telinhos Dina Sofia DS, Maniak Markus M

Ether lipids in varying amounts are membrane constituents and storage material in the protist and animal kingdoms, but are largely absent from fungi and plants. Their biosynthesis pathway starts in the peroxisome and involves a set of well-conserved enzymes. Only one step, the reduction of alkyl-dihydroxyacetone-phosphate to alkyl-glycerol-3-phosphate, is mediated by so-called short-chain dehydrogenases/reductases, which are members of huge protein families. Here, using GFP fusions, we identify a peroxisomal enzyme in Dictyostelium, as well as a highly related protein residing in the endoplasmic reticulum. Single-gene knockouts indicate that these enzymes largely compensate for one another, suggesting a flexible redistribution of lipid metabolites between these organelles. The double knockout, however, is severely affected in ether lipid composition and displays a clear growth retardation. The defects can also be reverted by expression of the cognate yeast enzyme, demonstrating conservation of this metabolic step across kingdoms of life.

PMID 42274617

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PubMedJournal of nanobiotechnology2026-05-27

Dihydroxyacetone nanoparticles ameliorate osteoarthritis via P21-mediated regulation of chondrocyte repair.

Fang Chao C, Ji Zhou Z, Pan Yankai Y, Li Zhi Z et al.

Osteoarthritis (OA) is a disease characterized by progressive cartilage degeneration. P21, as a cell cycle regulator, participates in maintaining cartilage homeostasis. This study aimed to evaluate the therapeutic potential of dihydroxyacetone (DHA) and its hyaluronic acid methacrylate (HAMA)-DHA nanoparticles in improving OA through the P21-mediated PI3K/AKT signaling pathway. Findings from the analyzed human cohorts and animal models revealed significantly reduced P21 expression in OA cartilage, which negatively correlated with disease severity within the examined stages. P21 overexpression enhanced chondrocyte anabolism, alleviated oxidative stress, and suppressed catabolic responses, whereas P21 deficiency exacerbated cartilage degeneration. The combined analysis of RNA sequencing and metabolomics indicated that DHA is a key metabolic node regulating P21. DHA treatment restored P21 levels, alleviated oxidative stress via the P21-mediated PI3K/AKT signaling pathway, promoted expression of anabolic markers (SOX9, COL2, and ACAN), and suppressed catabolic markers (MMP13, ADAMTS-4, and COL10). Compared to free DHA, DHA@HAMA nanoparticles significantly enhanced stability, cellular compatibility, and chondroprotective effects while enabling sustained release. This approach was observed to further promote P21-mediated PI3K/AKT signaling, which corresponded with mitigated cartilage erosion, subchondral bone loss, and OA severity. This study establishes that DHA exerts critical protective effects in OA via the P21-mediated PI3K/AKT signaling pathway. DHA@HAMA nanoparticles alleviate OA progression by more effectively enhancing P21 expression and function, offering a promising new therapeutic strategy for OA treatment.

PMID 42192449

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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.

PMID 42157352

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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.

PMID 42136260

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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.

PMID 42133630

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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.

PMID 42035276

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dihydroxyacetone (Nigrantil)

什么是 dihydroxyacetone？

药物档案

治疗适应症

相关研究文献

Flexible Cooperation Between Peroxisomes and the Endoplasmic Reticulum During Lipid Synthesis of Dictyostelium.

Dihydroxyacetone nanoparticles ameliorate osteoarthritis via P21-mediated regulation of chondrocyte repair.

Metabolomic signatures of colonic infection by Brachyspira hyodysenteriae.

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

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

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

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