ArticleACS chemical biology2015
Colloidal aggregation and the in vitro activity of traditional Chinese medicines.
Article in ACS chemical biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed.
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- Nonspecific membrane bilayer perturbations by ivermectin underlie SARS-CoV-2bioRxiv : the preprint server for biology · 2023Article
- Reference compounds for characterizing cellular injury in high-content cellular morphology assays.Nature communications · 2023Article
- Prenylated flavonoids with significant anti-hepatoma activity from Daphne giraldii and effects on Fibroblast Growth Factor Receptor 1 (FGFR1).European journal of medicinal chemistry · 2023Article
- Computational Approaches to Enzyme Inhibition by Marine Natural Products in the Search for New Drugs.Marine drugs · 2023Review
- Rhubarb polysaccharide and berberine co-assembled nanoparticles ameliorate ulcerative colitis by regulating the intestinal flora.Frontiers in pharmacology · 2023Article
- Enhancing the Biopharmacological Characteristics of Asperosaponin VI: Unveiling Dynamic Self-Assembly Phase Transitions in the Gastrointestinal Environment.International journal of nanomedicine · 2023Article
- Structuring and De-Structuring of Nanovectors from Algal Lipids: Simulated Digestion, Preliminary Antioxidant Capacity and In Vitro Tests.Pharmaceutics · 2022Article
- Cannabidiol and Cannabigerol Inhibit Cholangiocarcinoma Growth In Vitro via Divergent Cell Death Pathways.Biomolecules · 2022Article
- Supramolecular assemblies based on natural small molecules: Union would be effective.Materials today. Bio · 2022Review
- Regarding the Mechanisms of Promiscuous Cannabinoid Pharmacology: An Elephant Has Entered the Room.Cannabis and cannabinoid research · 2021Article
- Preparing (Metalla)carboranes for Nanomedicine.ChemMedChem · 2021Review
- A Crowding Barrier to Protein Inhibition in Colloidal Aggregates.Journal of medicinal chemistry · 2021Article
- Biological functions of supramolecular assemblies of small molecules in cellular environment.RSC chemical biology · 2021Article
- Flavonoids from Pterogyne nitens as Zika virus NS2B-NS3 protease inhibitors.Bioorganic chemistry · 2021Article
- Synergistic Mechanisms of Constituents in Herbal Extracts during Intestinal Absorption: Focus on Natural Occurring Nanoparticles.Pharmaceutics · 2020Review
- Improving natural product research translation: From source to clinical trial.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020Article
- Resonant waveguide grating based assays for colloidal aggregate detection and promiscuity characterization in natural products.RSC advances · 2019Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
Traditional Chinese Medicines (TCMs) have been the sole source of therapeutics in China for two millennia. In recent drug discovery efforts, purified components of TCM formulations have shown activity in many in vitro assays, raising concerns of promiscuity. Here, we investigated 14 bioactive small molecules isolated from TCMs for colloidal aggregation. At concentrations commonly used in cell-based or biochemical assay conditions, eight of these compounds formed particles detectable by dynamic light scattering and showed detergent-reversible inhibition against β-lactamase and malate dehydrogenase, two counter-screening enzymes. When three of these compounds were tested against their literature-reported molecular targets, they showed similar reversal of their inhibitory activity in the presence of detergent. For three of the most potent aggregators, contributions to promiscuity via oxidative cycling were investigated; addition of 1 mM DTT had no effect on their activity, which is inconsistent with an oxidative mechanism. TCMs are often active at micromolar concentrations; this study suggests that care must be taken to control for artifactual activity when seeking their primary targets. Implications for the formulation of these molecules are considered.
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