bims-supasi Biomed News
on Sulfation pathways and signalling
Issue of 2025–03–02
seventeen papers selected by
Jonathan Wolf Mueller, University of Birmingham



  1. Curr Protoc. 2025 Feb;5(2): e70110
      Mucopolysaccharidoses (MPSs) are complex lysosomal diseases that result in the accumulation of glycosaminoglycans (GAGs) in urine, blood, and tissues. Lysosomal enzymes responsible for GAG degradation are defective in MPSs. GAGs including chondroitin sulfate (CS), dermatan sulfate (DS), heparan sulfate (HS), and keratan sulfate (KS) are biomarkers for MPSs. This article describes a stable isotope dilution-tandem mass spectrometric method for quantifying CS, DS, and HS in urine samples. The GAGs are methanolyzed to uronic/iduronic acid-N-acetylhexosamine or uronic/iduronic acid-N-glucosamine dimers and mixed with internal standards derived from deuteriomethanolysis of GAG standards. Specific dimers derived from HS, DS, and CS are separated by ultra-performance liquid chromatography (UPLC) and analyzed by electrospray ionization (ESI) tandem mass spectrometry (MS/MS) using selected reaction monitoring for each targeted GAG product and its corresponding internal standard. This UPLC-MS/MS GAG assay is useful for identifying patients with MPS types I, II, III, VI, and VII. © 2025 Wiley Periodicals LLC. Basic Protocol: Urinary GAG analysis by ESI-MS/MS Support Protocol 1: Prepare calibration samples Support Protocol 2: Preparation of stable-isotope-labeled internal standards Support Protocol 3: Preparation of quality controls for GAG analysis in urine Support Protocol 4: Optimization of methanolysis time Support Protocol 5: Measurement of methanolic HCl concentration Support Protocol 6: Preparation of working methanolic HCl solution (1.1 M) Support Protocol 7: Dilution of prepared urine sample.
    Keywords:  LC‐ESI‐MS/MS; dermatan sulfate; glycosaminoglycan; heparan sulfate; isotope dilution; mucopolysaccharidosis
    DOI:  https://doi.org/10.1002/cpz1.70110
  2. Food Chem. 2025 Feb 17. pii: S0308-8146(25)00700-9. [Epub ahead of print]476 143449
      Anthocyanins (ACNs) are widely used in the culinary, cosmetic, and biomedical industries owing to their potent bioactivities. However, the rapid degradation of ACNs in extreme environments is a major limiting factor for their physicochemical stability and bioactivity. This study reported a facile and environmental-friendly ACN embedding strategy using chondroitin sulfate (CS) and whey protein isolate (WPI) to prepare the CS/WPI@ACN complex. The encapsulation efficiency of CS/WPI@ACN reached up to 84.87 % when the CS-to-WPI mass ratio was 1:5, and the core-to-wall material ratio was 1:3. Molecular docking analysis revealed that the CS/WPI complex harbored a concave chamber, which was conducive for the embedding of small ACN molecules and promoting drug activity. The CS/WPI@ACN complex enabled sustained ACN release in the gastrointestinal tract in vitro. The CS/WPI@ACN complex was stable under ascorbic acid treatment conditions, high temperatures, and a wide range of pH levels. In vitro release data demonstrated that most encapsulated ACNs were released in the small intestine. Furthermore, the antioxidant activity of the CS/WPI@ACN complex was higher than that of free ACN. Therefore, this study proposed a strategy to protect unstable active substances, and laid a foundation for blueberry anthocyanins in the high-value utilization of functional drinks.
    Keywords:  Anthocyanin; Chondroitin sulfate; Encapsulation efficiency; Stability; Whey protein isolate
    DOI:  https://doi.org/10.1016/j.foodchem.2025.143449
  3. Int J Biol Macromol. 2025 Feb 22. pii: S0141-8130(25)01958-0. [Epub ahead of print] 141407
      Sulfated polysaccharides (SPS) are a unique secondary metabolite isolated from Laetiporus sulphureus. This study examined the detailed molecular mechanisms of action of F2, a medium molecular weight SPS of L. sulphureus, on breast cancer MDA-MB-231 cell proliferation and metastasis. Results showed that the sulfate and protein content of F2 were 2.1 % and 15.6 %, respectively. F2 had a molecular weight of 23.8 kDa and did not contain a triple helix conformation. The monosaccharide composition of F2 was mannose, galactose, glucose, and fucose. F2 inhibited MDA-MB-231 cell proliferation mainly by blocking the cell cycle at the G0/G1 phase, which was attributed to the down-regulation of CDK4 and cyclin D1 and the up-regulation of p21 protein expression. F2 suppressed epidermal growth factor receptor (EGFR)-mediated intracellular signaling events, such as phosphorylation of ERK1/2, Akt, and GSK-3β and activation of NF-κB and β-catenin, resulting in the cell cycle arrest. Moreover, F2 significantly reduced the EGFR phosphorylation and expression, and the level of mutant p53 protein. F2 also effectively inhibited breast cancer cell migration and invasion through down-regulating MMP-9 and MMP-2 protein expression. In conclusion, this study demonstrated that F2 exhibited anti-proliferative and anti-metastatic activities against MDA-MB-231 cells by inhibiting the activation of EGFR-mediated signaling pathways.
    Keywords:  EGFR; Laetiporus sulphureus; Sulfated polysaccharides; Triple-negative breast cancer cells
    DOI:  https://doi.org/10.1016/j.ijbiomac.2025.141407
  4. Int J Biol Macromol. 2025 Feb 25. pii: S0141-8130(25)02050-1. [Epub ahead of print] 141499
      Dysregulation of blood coagulation can result in thrombosis, highlighting the importance of anticoagulants that target both the extrinsic and intrinsic pathways of fibrin clot formation. This study explores the anticoagulant effects of TOSP-3, a sulfated polysaccharide characterized as [→3)-4-O-SO₃--α-Fucp-(1 → 3)-4-O-SO₃--β-Galp-(1→] from brown seaweed Turbinaria ornata, composed of sulfated α-(1 → 3)-fucopyranose (Fucp) and β-(1 → 3)-galactopyranose (Galp) units. In vitro analysis revealed that TOSP-3 (25 μg/mL) markedly extended activated partial thromboplastin time (100.49 s) and prothrombin time (77.57 s), highlighting its regulation on both intrinsic and extrinsic coagulation cascades. TOSP-3 induced a substantial reduction in coagulation factor Xa expression (89 %) in human umbilical vein endothelial cells. It further exhibited a five-fold stronger inhibition of thrombin-catalyzed fibrin polymerization and reduced platelet aggregation by approximately 87 % compared to the negative control (10 μM ADP). TOSP-3 attenuated thrombin-induced intracellular Ca2+ mobilization (~33 %), while concurrently diminishing total thrombin production (33 %), thereby highlighting its inhibitory effects on thrombin-mediated signaling pathways. The sulfate content, patterns, and linkage structure of TOSP-3 allow it to inhibit FXa expression and reduce thrombin-catalyzed fibrin polymerization through electrostatic interactions, thereby more effectively modulating the coagulation cascade compared to heparin. These findings highlight the potential of TOSP-3 as a natural anticoagulant for managing thrombotic disorders.
    Keywords:  Brown seaweed Turbinaria ornata; Sulfated polysaccharide; Thrombin-catalyzed fibrin polymerization
    DOI:  https://doi.org/10.1016/j.ijbiomac.2025.141499
  5. Biomolecules. 2025 Jan 25. pii: 178. [Epub ahead of print]15(2):
      Keratan sulfate (KS) is a negatively charged carbohydrate linked to proteins. Several KS-bearing structural glycosaminoglycans participate to maintain the homeostasis of a functional extracellular matrix. Dysfunction of its biochemical composition and structure might therefore lead to pathological situations. For this reason, imaging of KS in tissues is an important diagnostic tool. Here, we describe the identification of the KS paratope derived from the ancestral anti-KS IgG mAb MZ15, as well as the engineering, functional recombinant expression in E. coli, and purification of an anti-KS single-chain variable fragment (ScFv). The ScFv enabled in vitro imaging of KS in cryosections of rat cornea by immunofluorescence microscopy comparable to the ancestral IgG MZ15.
    Keywords:  MZ15; ScFv; antibody; glycosaminoglycans; imaging; immunohistochemistry; keratan sulfate; paratope; recombinant expression
    DOI:  https://doi.org/10.3390/biom15020178
  6. Int J Mol Sci. 2025 Feb 13. pii: 1567. [Epub ahead of print]26(4):
      Chronic kidney disease (CKD) is a significant public health concern. Osteoarthritis (OA), a common form of arthritis, has been shown to have a dramatically increased prevalence, particularly among individuals aged 40-50 and older, in the presence of CKD. Furthermore, CKD may exacerbate the progression and impact of OA. A survey study revealed that 53.9% of CKD patients undergoing long-term hemodialysis were diagnosed with OA. These findings underscore the potential association between CKD and OA. Uremic toxins, such as indoxyl sulfate, p-cresyl sulfate, transforming growth factor-β, and advanced glycation end-products, are regarded as potential risk factors in various CKD-related conditions, affecting bone and joint metabolism. However, whether these factors serve as a bridging mechanism between CKD and OA comorbidities, as well as their detailed roles in this context, remains unclear. Addressing the progression of OA in CKD patients and identifying effective treatment and prevention strategies is an urgent challenge that warrants immediate attention. This review focuses on describing and discussing the molecular pathological mechanisms underlying CKD-associated OA and the possible therapeutic strategies.
    Keywords:  calcium; chronic kidney disease; iron; osteoarthritis; uremic toxins
    DOI:  https://doi.org/10.3390/ijms26041567
  7. ACS Catal. 2024 May 03. 14(9): 6577-6588
      Heparin is a widely used drug to treat thrombotic disorders in hospitals. Heparosan synthase 2 from Pasteurella multocida (PmHS2) is a key enzyme used for the chemoenzymatic synthesis of heparin oligosaccharides. It has both activities: glucosaminyl transferase activity and glucuronyl transferase activity; however, the mechanism to carry out the glyco-oligomerization is unknown. Here, we report crystal structures of PmHS2 constructs with bound uridine diphosphate (UDP) and a cryo-EM structure of PmHS2 in complex with UDP and a heptasaccharide (NS 7-mer) substrate. Using a LC-MC analytical method, we discovered the enzyme displays both a two-step concerted oligomerization mode and a distributive oligomerization mode depending on the non-reducing end of the starting oligosaccharide primer. Removal of 7 amino acid residues from the C-terminus results in an enzymatically active monomer instead of dimer and loses the concerted oligomerization mode of activity. In addition, the monomer construct can transfer N-acetyl glucosamine at a substrate concentration that is ∼7-fold higher than wildtype enzyme. It was also determined that an F529A mutant can transfer an N-sulfo glucosamine (GlcNS) saccharide from a previously inactive UDP-GlcNS donor. Performing the glyco-transfer reaction at a high substrate concentration and the capability of using unnatural donors are desirable to simplify the chemoenzymatic synthesis to prepare heparin-based therapeutics.
    Keywords:  Cryo-EM; Heparan sulfate biosynthesis; chemoenzymatic synthesis; oligosaccharide; protein/substrate complex
    DOI:  https://doi.org/10.1021/acscatal.4c00677
  8. Molecules. 2025 Feb 08. pii: 782. [Epub ahead of print]30(4):
      Accurate quantification of indoxyl sulfate (IndS) and p-cresyl sulfate (pCS) is essential for understanding their role in chronic kidney disease (CKD) progression and for developing strategies to mitigate their harmful effects, including cardiovascular morbidity and renal fibrosis. Advances in liquid chromatography-high-resolution mass spectrometry (LC-HRMS) enable the integration of powerful diagnostic tools into clinical laboratories. Along with accurate quantification, precise mass measurements allow for untargeted compound identification.
    METHODS: An LC-HRMS was validated for quantifying IndS and pCS in human serum, following EMA guidelines. The method involved protein precipitation with methanol, micro-LC for chromatographic separation, and detection based on accurate mass, with simultaneous high-resolution full-scan acquisition. Clinical samples from patients with varying degrees of renal insufficiency and samples obtained before and after hemodiafiltration were analyzed.
    RESULTS: The method demonstrated acceptable linearity, precision, and accuracy. The measurement range for both analytes was from 100 to 40,000 ng/mL. Serum levels of IndS and pCS correlated with decreased renal function. After hemodiafiltration, there was a significant reduction of IndS (50%) and pCS (43%). Simultaneous untargeted analysis allowed to identify metabolites significantly underexpressed after hemodiafiltration.
    CONCLUSIONS: An accurate LC-HRMS method was validated for the quantification of IndS and pCS serum levels in patients with CKD, providing insights into toxin dynamics and enabling untargeted metabolic evaluation.
    Keywords:  chronic kidney disease; hemodiafiltration; high-resolution mass spectrometry; metabolomics; micro-liquid chromatography; uremic toxins
    DOI:  https://doi.org/10.3390/molecules30040782
  9. Diseases. 2025 Feb 01. pii: 42. [Epub ahead of print]13(2):
      Obesity, chronic pain, and aging are prevalent global challenges with profound implications for health and well-being. Central to these processes are adrenal hormones, particularly cortisol and dehydroepiandrosterone (DHEA), along with its sulfated form (DHEAS). Cortisol, essential for stress adaptation, can have adverse effects on pain perception and aging when dysregulated, while DHEA/S possess properties that may mitigate these effects. This review explores the roles of cortisol and DHEA/S in the contexts of obesity, acute and chronic pain, aging, and age-related diseases. We examine the hormonal balance, specifically the cortisol-to-DHEA ratio (CDR), as a key marker of stress system functionality and its impact on pain sensitivity, neurodegeneration, and physical decline. Elevated CDR and decreased DHEA/S levels are associated with worsened outcomes, including increased frailty, immune dysfunction, and the progression of age-related conditions such as osteoporosis and Alzheimer's disease. This review synthesizes the current literature to highlight the complex interplay between these hormones and their broader implications for health. It aims to provide insights into potential future therapies to improve pain management and promote healthy weight and aging. By investigating these mechanisms, this work contributes to a deeper understanding of the physiological intersections between pain, aging, and the endocrine system.
    Keywords:  DHEA; DHEAS; acute pain; aging; chronic pain; cortisol; cortisol-to-DHEA ratio; obesity
    DOI:  https://doi.org/10.3390/diseases13020042
  10. mBio. 2025 Feb 25. e0353424
      Despite providing the first example of archaeal N-glycosylation almost 50 years ago, detailed insight into the pathway used by Halobacterium salinarum to assemble and attach an N-linked tetrasaccharide decorating glycoproteins in this haloarchaea has only recently appeared. Still, numerous components of this pathway remain to be identified, including sulfotransferase(s), which modify the third and fourth tetrasaccharide sugars. In the present report, a series of bioinformatics, genetic, biochemical, and structural approaches served to reveal how membrane-associated VNG1056C and soluble VNG1057C respectively sulfate the iduronic acid at tetrasaccharide position three and the terminal glucuronic acid, seemingly independent of each other. Deletion of VNG1056C but not of VNG1057C reduced cell motility to a minor degree and did not cause archaellum filament bundling. Finally, transcription of VNG1056C or VNG1057C was augmented upon deletion of the other when cells were grown in low but not high salinity conditions possibly in an attempt to compensate for the loss of sugar sulfation resulting from the deletion. This augmented transcription, however, had no effect on the extent of tetrasaccharide sulfation. With demonstrated roles in Hbt. salinarum N-glycosylation, VNG1056C and VNG1057C were respectively re-annotated as Agl30 and Agl31, employing the nomenclature used to define archaeal N-glycosylation pathway components.
    IMPORTANCE: Like essentially all Archaea, the halophile Halobacterium salinarum performs N-glycosylation, namely, the covalent attachment of a glycan moiety to select asparagine residues in a target protein. Moreover, Hbt. salinarum represents one of the few current archaeal examples in which the pathway of N-glycosylation has been largely defined. Still, several components of this pathway remain to be defined, including the sulfotransferase(s) responsible for modifying the iduronic acid and glucuronic acid corresponding to the third and final sugars of the N-linked tetrasaccharide that decorates glycoproteins in this haloarchaeon. In the present report, a series of bioinformatics, genetic, biochemical, and structural approaches served to reveal how membrane-associated VNG1056C and soluble VNG1057C respectively sulfate the iduronic acid at tetrasaccharide position three and the terminal glucuronic acid, seemingly independent of each other. The need for two different enzymes reflects the sulfation of these sugars at distinct positions.
    Keywords:  Halobacterium salinarum; N-glycosylation; archaea; glycoprotein; sulfotransferase
    DOI:  https://doi.org/10.1128/mbio.03534-24
  11. J Steroid Biochem Mol Biol. 2025 Feb 21. pii: S0960-0760(25)00040-8. [Epub ahead of print] 106712
      Bile acids (BA) are C24 steroids synthesized from cholesterol in liver. Hardly any data exist on BA in the most accessible human biofluid urine. As bile acids bear great potential as future biomarkers in diagnosis and monitoring of metabolic diseases, we aimed at developing and implementing a new method for the quantification of urinary bile acids using targeted liquid chromatography-tandem mass spectrometry (LC-MS/MS). A second goal consisted in creating first reference values of urinary bile acids during childhood and to investigate their excretion patterns in obese children and adolescents. Our method required 2mL of urine and sample preparation consisting of protein precipitation and solid phase extraction. Stable isotopes of BA were included as internal standards (IS). Our method is capable of simultaneously determining 18 BA: the primary BA cholic acid (CA) and chenodeoxycholic acid (CDCA), and the secondary BA deoxycholic acid (DCA) and lithocholic acid (LCA) as well as glycine and taurine conjugates of these four BA. Furthermore, ursodeoxycholic acid (UDCA) and five BA in their sulfated forms (LCA-S, GLCA-S, TLCA-S, GCDCA-S, GDCA-S) were analyzed. After successful validation (intra-day precision 1.02% - 11.07%; inter-day precision 0.42% to 11.47%.; intra-day accuracy 85.75% - 108.90%; inter-day accuracy 86.76% - 110.99%; no significant matrix effect; recovery 90.49% - 113.99%)., the method was applied to samples of 80 healthy children as well as 237 obese children of various age groups. Sulfated BA showed the highest concentrations, with GCDCA-S (nmol/L, medians, controls vs. obese 588.4 vs. 360.2) being the most abundant among all BA, followed by GLCA-S (353.9 vs. 344.8) and GDCA-S (319,3 vs. 323.9). CA (135.1 vs. 174.6) and GCA (100.2 vs. 92.4) were the two dominant non-sulfated BA. In conclusion, we developed a LC-MS/MS method for the simultaneous determination of 18 urinary bile acids in children and adolescents. We created reference values and investigated obese children. Sulfated bile acids dominated in both study groups. Lower bile acid sulfation and amidation in obese children point to limitations in their hepatic metabolic capacity.
    DOI:  https://doi.org/10.1016/j.jsbmb.2025.106712
  12. J Pharm Sci. 2025 Feb 22. pii: S0022-3549(25)00141-8. [Epub ahead of print] 103705
      Hydrophilic steroid conjugates require active and facilitated transport mechanisms for their distribution into tissues and excretion from the body. The ATP-binding cassette (ABC) and solute carrier organic anion (SLCO) transporters involved in androgen sulfate (-S) disposition have been poorly characterized. In this study, we investigated the in vitro transport of testosterone-S, epitestosterone-S, dehydroepiandrosterone-S (DHEA-S), androsterone-S, and etiocholanolone-S by the multidrug resistance-associated proteins 2-4 (MRP2-4, ABCC2-4), breast cancer resistance protein (BCRP, ABCG2), and organic anion-transporting polypeptides (OATP) 1B1, 1B3, and 2B1 (SLCO1B1, SLCO1B3, and SLCO2B1) using human transporter-overexpressing HEK293 cells and membrane vesicles. We found testosterone-S, epitestosterone-S, and DHEA-S to be selectively transported by BCRP and/or MRP4, whereas all studied androgen sulfates were substrates of MRP3, OATP1B1, OATP1B3, and OATP2B1. MRP2 did not transport any of the studied compounds. Evaluation of transport kinetics revealed MRP4 to interact with its substrates at high to moderate affinity, whereas the observed affinities towards MRP3, BCRP, and OATPs were mostly moderate. These results help to build a better mechanistic understanding of the disposition of androgen sulfates in the human body. Additionally, this data may be used to assess the feasibility of androgen sulfates as additional biomarkers in doping detection.
    Keywords:  ATP-Binding Cassette (ABC) transporter(s); Breast Cancer Resistance Protein (BCRP); Conjugate(s); Hepatic transport; Hormone(s); Intestinal transport; Membrane transporter(s); Multidrug Resistance-associated protein(s); Organic Anion-Transporting Polypeptide(s) (OATP)
    DOI:  https://doi.org/10.1016/j.xphs.2025.103705
  13. Cells. 2025 Feb 11. pii: 256. [Epub ahead of print]14(4):
      The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection is intricately related to the reprogramming of host metabolism. However, existing studies have mainly focused on peripheral blood samples and barely identified specific metabolites that are critically involved in the pathology of coronavirus disease 2019 (COVID-19). In the current small-scale study, we performed metabolic profiling in plasma (n = 61) and paired bronchoalveolar lavage fluid (BALF) samples (n = 20) using parallel two-dimensional liquid chromatography-mass spectrometry (2DLC-MS). In addition, we studied how an identified metabolite regulates the immunopathogenesis of COVID-19. The results unveiled distinct metabolome changes between healthy donors, and moderate and severe patients in both plasma and BALF, indicating that locations and disease severity play critical roles in COVID-19 metabolic alteration. Notably, a vital metabolite, indoxyl sulfate, was found to be elevated in both the plasma and BALF of severe COVID-19 patients. Indoxyl sulfate selectively induced TNF-α production, reduced co-stimulatory signals, and enhanced apoptosis in human monocytes. Moreover, its levels negatively correlated with the strength of co-stimulatory signals and antigen presentation capability in monocytes of COVID-19 patients. Collectively, our findings suggest that the levels of indoxyl sulfate could potentially serve as a functional biomarker to monitor COVID-19 disease progression and guide more individualized treatment for COVID-19 patients.
    Keywords:  COVID-19; immune regulation; indoxyl sulfate; metabolism; monocytes
    DOI:  https://doi.org/10.3390/cells14040256
  14. Int J Mol Sci. 2025 Feb 15. pii: 1656. [Epub ahead of print]26(4):
      Studies in animals have shown that androgens promote early follicular development and granulosa cell proliferation by augmenting follicle-stimulating hormone (FSH) receptor expression in granulosa cells. Inconsistency exists regarding the association between basal serum androgen levels and follicular development in low responders undergoing in vitro fertilization (IVF), although the number of studies is limited. The aim of the current study was to assess the association between basal serum androgen concentrations and the number of follicles ≥ 11 mm on the day of triggering final oocyte maturation in low responders undergoing IVF. This prospective study was performed from June 2020 to September 2024 in 96 low responders, categorized according to the Bologna criteria. Total testosterone, dehydroepiandrosterone sulfate (DHEAS), 17-OH progesterone (17-OH-P), Δ4-androstenedione (Δ4-A), and sex hormone-binding globulin (SHBG) were measured on the day of initiation of ovarian stimulation. No association was found between basal serum testosterone (coef.: -0.002, p = 0.98), DHEAS (coef.: -0.096, p = 0.35), 17-OH-P (coef.: +0.086, p = 0.40), Δ4-A (coef.: -0.028, p = 0.79), and SHBG (coef.: +0.160, p = 0.12) concentrations and the number of follicles ≥ 11 mm on the day of triggering final oocyte maturation. The results of the current study challenge the usefulness of basal serum androgen measurements prior to ovarian stimulation in low responders as predictors of ovarian response.
    Keywords:  DHEAS; androgens; follicles; low responders; testosterone
    DOI:  https://doi.org/10.3390/ijms26041656
  15. Discov Oncol. 2025 Feb 24. 16(1): 231
      Heparin, traditionally known for its anticoagulant properties, has recently been identified as a potential agent in cancer therapy. Its derivatives, including low-molecular-weight heparin (LMWH) and unfractionated heparin (UFH), are being investigated for their multifaceted roles in oncology. This review focuses on the expanding exploration of heparin's anticancer effects and its possible integration into cancer treatment protocols. The primary aim is to consolidate and analyze current research on the anticancer properties of heparin and its derivatives. It seeks to illuminate the mechanisms by which these compounds influence cancer progression, including their impact on angiogenesis, tumor cell proliferation, immune response modulation, and the inhibition of cancer cell migration and invasion. Additionally, the review aims to evaluate the potential of heparin and its derivatives in complementing existing chemotherapy treatments. An extensive literature review was conducted, encompassing in vitro, in vivo, and clinical studies. Sources included a range of scientific databases, employing keywords related to heparin and oncology. The selected studies were critically reviewed to extract relevant data on the efficacy, mechanisms, and potential clinical applications of heparin in cancer therapy. The results reveals that heparin and its derivatives exhibit significant anticancer activity across various research settings; key findings include the inhibition of angiogenesis, reduction in tumor cell proliferation, stimulation of immune responses, and the limitation of cancer cell migration and invasion. The compounds also show promise as adjuncts to conventional chemotherapy, potentially enhancing the efficacy of existing cancer treatments. This review highlights the burgeoning role of heparin and its derivatives in the realm of cancer therapy, marking a shift from their traditional use as anticoagulants. While promising, the research underscores the need for further comprehensive studies to fully understand the mechanisms of action, optimal dosing, potential side effects, and patient selection criteria. The potential integration of heparin into cancer treatment regimens opens new therapeutic possibilities warranting continued investigation in this rapidly evolving field.
    Keywords:  Anticoagulation; Cancer therapy; Heparin; Heparin derivatives; Low molecular weight heparin; Oncology; Thrombosis; Unfractionated heparin
    DOI:  https://doi.org/10.1007/s12672-025-01985-7
  16. Biomedicines. 2025 Feb 11. pii: 432. [Epub ahead of print]13(2):
      Background/Objectives: Beneficial effects of neurosteroid dehydroepiandrosterone sulphate (DHEAS) on cognition, emotions and behavior have been previously reported, suggesting its potential in the prevention and treatment of various neuropsychiatric and neurodegenerative disorders, including Alzheimer's disease (AD). This study aimed to investigate the potential neuroprotective actions of DHEAS against Aβ toxicity in both cellular and animal models of AD. Methods: After optimizing the AD model in vitro, we investigated the DHEAS effects on the viability and death of primary mouse neurons exposed to toxic Aβ42 oligomers for 24 h. In order to extend our research to an in vivo study, we further tested the acute effects of intraperitoneal DHEAS administration on the Aβ plaque density in different brain regions of 3xTg-AD mice, an animal model of AD. Results: In cell culture, DHEAS hampered the decrease in the neuronal viability caused by toxic Aβ oligomers, primarily by influencing mitochondrial function and apoptosis. DHEAS also counteracted the increase in the mRNA expression of selected genes (PI3K, Akt, Bcl2, Bax), induced in neuronal culture by treatment with Aβ42 oligomers. Obtained data suggested the involvement of mitochondria, caspases 3 and 7, as well as the PI3K/Akt and Bcl2 signaling network in the antiapoptotic properties of DHEAS in neurons. Forty-eight hours after DHEAS treatment, a significantly lower number of Aβ plaques was observed in the motor cortex but not in other brain areas of 3xTg-AD mice. Conclusions: Results indicated potential neuroprotective effects of DHEAS against Aβ toxicity and accumulation, suggesting that DHEAS supplementation should be further studied as a novel option for AD prevention and/or treatment.
    Keywords:  3xTg-AD mice; Alzheimer’s disease; Aβ oligomers; dehydroepiandrosterone sulphate; neuroprotection; primary neurons
    DOI:  https://doi.org/10.3390/biomedicines13020432
  17. ACS Omega. 2025 Feb 18. 10(6): 6079-6091
      Sulfated flavonoids, a class of polyphenols integral to plant secondary metabolism and chemical defense, exhibit notable pharmacological potential. Seagrasses, marine angiosperms with critical ecological and socioeconomic roles, often accumulate these compounds in high concentrations. However, their complex chemical profiles-including closely related sulfated flavonoids-are challenging to characterize due to potential degradation during extraction. This study provides the first comprehensive analysis of sulfated flavonoids in Phyllospadix scouleri alongside a comparative analysis of P. torreyi. The Phyllospadix genus, known for forming productive intertidal meadows on rocky Pacific coastlines of North America, serves as a valuable model for understanding flavonoid diversity and adaptation in marine environments. From P. scouleri foliar tissues, we isolated and identified 1 phenolic acid and 15 sulfated flavonoids (HPLC-DAD, NMR, LC-MS), including previously undescribed 6-hydroxyflavonoid disulfates and monosulfates, and flavonoids not earlier reported for the genus. Lower amounts of sulfated glycosides were also tentatively identified in both species for the first time. The flavonoid profiles showed clear species-specific patterns: P. scouleri primarily produced 6-hydroxyflavonoids (70%), while P. torreyi favored 5- and 6-methoxyflavonoids (60 and 70%). Samples collected from nearby locations in May 2024 from both species showed similar flavonoid concentrations (∼20 mg/g DW) and comparable ratios between total flavonoids and rosmarinic acid (∼6:1). P. torreyi exhibited more disulfated flavonoids (84.3%) than monosulfated types (11.9%), whereas P. scouleri had 25.2% disulfated and 66.5% monosulfated flavonoids. Given the proven link between phenolic compounds and the physiological acclimation of surfgrasses to emersion during intertidal periods, as well as to marine heatwaves, this study provides a robust baseline for further research into the basic chemical ecology of these compounds and their responses to climate change.
    DOI:  https://doi.org/10.1021/acsomega.4c10402