Search bioRxiv⌕ Search

bioRxiv · 10.64898/2025.12.22.695928

A Data-Driven Approach for the Development of a Time-informed Adverse Outcome Pathway-network for Cardiotoxicity of Environmental Chemicals

Abstract

We present a novel Adverse Outcome Pathway (AOP) network for environmental chemical-induced cardiotoxicity using a bottom-up, data-driven AOP development approach. Mechanistic endpoints were systematically extracted from 339 in vitro and in vivo studies, yielding 1,759 Key Event (KE) entries and 4,938 Key Event Relationship (KER) entries, including information on experimental methods, essentiality evidence (intervention experiments demonstrating upstream-downstream dependence), and study metadata. After quality filtering (high risk of bias, confounding cytotoxicity in vitro, excessive toxicity or animal well-being concerns in vivo, and low-frequency observations), 112 unique KEs and 829 unique KERs supported by at least three independent observations were retained for network construction. Network analysis identified oxidative stress and mitochondrial dysfunction as dominant hub processes linking diverse upstream perturbations to downstream cardiomyocyte injury, inflammation, cardiac remodelling (fibrosis and hypertrophy), decreased cardiac contractility, and reduced left ventricular function. Incorporating exposure duration at the KER level enabled time-resolved pathway interpretation and demonstrated that KE timing is relationship-dependent, revealing temporal patterns not apparent when analysing KEs in isolation. This evidence-weighted, time-resolved AOP network can support endpoint prioritisation and exposure-window selection for non-animal method (NAM) test batteries and mechanistically informed cardiotoxicity assessment. SynopsisEnvironmental chemicals converge on shared stress and injury pathways that drive cardiac remodelling and ventricular dysfunction. A time-resolved AOP network helps prioritise endpoints and exposure windows for non-animal cardiotoxicity testing.

Explore related subjects

Keep this discovery

Explore connections, maps & timelines

BibTeXRIS

Schaffert, A., Murugadoss, S., Roos, T., Linzalone, N., Donzelli, G., Gehring, R., Mertens, B., Paparella, M.. 2025-12-24. A Data-Driven Approach for the Development of a Time-informed Adverse Outcome Pathway-network for Cardiotoxicity of Environmental Chemicals. https://doi.org/10.64898/2025.12.22.695928

Cite the original work for its findings. Save a collection to share your selection of sources.

KEEP EXPLORING

Related preprints

Lipid-ASO therapeutics exhibit differential tissue targeted delivery upon systemic or local CNS administration

Antisense oligonucleotides (ASOs) are a powerful therapeutic modality, but their full potential is hindered by pharmacokinetic properties that affect tissue and cellular delivery. Lipid conjugation is increasingly used to modulate ASO's biodistribution and promote extrahepatic activity, yet lipid dependent effects on in vivo functional delivery, particularly in the central nervous system (CNS), remain less explored. Here, we performed a side by side in vivo comparison of cholesterol, palmitic acid (C16:0), docosanoic acid (C22:0), and eicosapentaenoic acid (C20:5) conjugated to a fully phosphorothioated 3 10 3 LNA gapmer ASO targeting the Malat1 long non coding RNA. Lipid-ASO conjugates were administered systemically or locally in the brain of mice and evaluated for tissue level and cellular level distribution by imaging, qPCR and single-cell RNA sequencing, simultaneously annotating cell origin and global transcriptional changes within the cell. Following systemic administration in mice, lipid conjugation improved overall multi organ efficacy compared to unconjugated ASO, but with pronounced tissue specific differences. Single cell sequencing of liver and heart transcriptomes revealed lipid dependent cellular uptake patterns and transcriptional responses distinct from administration of unconjugated ASO. After intracerebroventricular administration, selected fatty acid conjugates enhanced silencing in deep brain regions such as the striatum, whereas cholesterol conjugation impaired functional delivery despite increased CNS retention. Light-sheet microscopy showed restricted parenchymal penetration of cholesterol ASOs compared with broader but heterogeneous distribution of palmitic acid conjugate. Together, these findings demonstrate that lipid identity critically determines ASO efficacy, productive cellular uptake, and regional CNS engagement, emphasizing the need for context specific lipid design in ASO therapeutic development.

pharmacology and toxicology↗

Novel Dissymmetric Ionizable Lipid-Assembled Lipid Nanoparticles for Delivery of Ferroptosis-Related siRNA in Diabetic Treatment

Small interfering RNA (siRNA) enables precise post-transcriptional gene silencing for refractory diseases, yet its clinical translation remains limited by the lack of safe and efficient delivery vectors. Inspired by the dissymmetric alkyl chain architecture of natural membrane phospholipids, we designed and synthesized 34 novel ionizable lipids with dissymmetric hydrophobic tails and formulated them into lipid nanoparticles (LNPs). Through systematic physicochemical and biological assessments, we established clear structure-activity relationships and identified two lead LNPs (O14-LNP, H18a-LNP) with superior endosomal escape capacity, enhanced in vivo gene silencing potency, and favorable biosafety relative to the clinical benchmark MC3-LNP. In both streptozotocin-induced and spontaneous db/db type 2 diabetes (T2D) mouse models, lead LNPs delivering ferroptosis-related siRNAs effectively ameliorated glucose and lipid metabolic disorders, restored islet function, and alleviated hepatic steatosis. This study not only lays a theoretical foundation for the rational design of novel ionizable lipids, but also validates the therapeutic potential of siRNA therapy targeting ferroptosis, providing a versatile delivery platform and targeted therapeutic strategy for the treatment of T2D.

pharmacology and toxicology↗

Red yeast rice-derived MKA ameliorates cardiac hypertrophy in hypertensive rats by inhibiting ERK1/2/c-Fos pathway

BackgroundCardiac hypertrophy is a key pathological process in hypertensive heart failure, yet current antihypertensive therapies do not directly target it. Red yeast rice (RYR), rich in monacolin K {beta}-hydroxy acid (MKA), is known for lipid-lowering effects, but its potential to ameliorate cardiac hypertrophy is unreported. PurposeTo investigate the effects of RYR-derived MKA on cardiac hypertrophy in spontaneously hypertensive rats (SHR) and elucidate its molecular mechanisms. MethodsSpontaneously hypertensive rats (SHR) were treated with 0.6% red yeast rice for 8 weeks to assess its effects on blood pressure, cardiac function (echocardiography), cardiac hypertrophy and fibrosis (histopathology), and multi-organ toxicity (histopathology). A multigenerational study was conducted to evaluate protective effects in offspring. Network pharmacology and transcriptomic analysis were integrated to predict molecular targets, which were subsequently validated by molecular docking and experiments. ResultsEight-week RYR treatment significantly reduced blood pressure, inhibited cardiac hypertrophy and fibrosis, and improved cardiac function without gender differences. No pulmonary, hepatic, or renal toxicity was observed. Offspring from treated parents exhibited further reduced hypertrophy upon continued treatment. Mechanistically, MKA bound ERK1/2 with high affinity, inhibiting its phosphorylation and downstream c-Fos expression, thereby downregulating hypertrophy markers. ConclusionRed yeast rice improves hypertensive cardiac hypertrophy via MKA-mediated inhibition of the ERK1/2/c-Fos pathway. Its multi-organ safety and transgenerational effects offer a novel dual-therapy strategy for hypertension and cardiac hypertrophy. Graphic abstract O_FIG O_LINKSMALLFIG WIDTH=139 HEIGHT=200 SRC="FIGDIR/small/710945v1_ufig1.gif" ALT="Figure 1"> View larger version (57K): org.highwire.dtl.DTLVardef@8225acorg.highwire.dtl.DTLVardef@775f43org.highwire.dtl.DTLVardef@10f5201org.highwire.dtl.DTLVardef@d0cd88_HPS_FORMAT_FIGEXP M_FIG C_FIG

pharmacology and toxicology↗