ArticleCellular and molecular life sciences : CMLS2015
Sphaeropsidin A shows promising activity against drug-resistant cancer cells by targeting regulatory volume increase.
Article in Cellular and molecular life sciences : CMLS, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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18 citing papers in PubMed, 43 citations in OpenAlex.
- Sphaeropsidin A C15-C16 Cross-Metathesis Analogues with Potent Anticancer Activity.ChemMedChem · 2024Article
- ent-8(14),15-Pimaradiene-2β,19-diol, a diterpene from Aleuritopteris albofusca, inhibits growth and induces protective autophagy in hepatocellular carcinoma cells.Naunyn-Schmiedeberg's archives of pharmacology · 2024Article
- New hemisynthetic derivatives of sphaeropsidin phytotoxins triggering severe endoplasmic reticulum swelling in cancer cells.Scientific reports · 2024Article
- Article
- Sphaeropsidin A: A Pimarane Diterpene with Interesting Biological Activities and Promising Practical Applications.Chembiochem : a European journal of chemical biology · 2021Review
- Diterpenes/Diterpenoids and Their Derivatives as Potential Bioactive Leads against Dengue Virus: A Computational and Network Pharmacology Study.Molecules (Basel, Switzerland) · 2021Article
- Polygodial and Ophiobolin A Analogues for Covalent Crosslinking of Anticancer Targets.International journal of molecular sciences · 2021Article
- Deciphering the chemical instability of sphaeropsidin A under physiological conditions - degradation studies and structural elucidation of the major metabolite.Organic & biomolecular chemistry · 2020Article
- Article
- Fungal Metabolite Antagonists of Plant Pests and Human Pathogens: Structure-Activity Relationship Studies.Molecules (Basel, Switzerland) · 2018Review
- Synthetic analogues of the montanine-type alkaloids with activity against apoptosis-resistant cancer cells.Bioorganic & medicinal chemistry letters · 2018Article
- Marine Mollusk-Derived Agents with Antiproliferative Activity as Promising Anticancer Agents to Overcome Chemotherapy Resistance.Medicinal research reviews · 2017Review
- Ophiobolin A, a sesterpenoid fungal phytotoxin, displays different mechanisms of cell death in mammalian cells depending upon the cancer cell origin.International journal of oncology · 2017Article
- A patient with multisystem dysfunction carries a truncation mutation in humanCold Spring Harbor molecular case studies · 2016Article
- Peripheral motor neuropathy is associated with defective kinase regulation of the KCC3 cotransporter.Science signaling · 2016Article
- Isatin derivatives with activity against apoptosis-resistant cancer cells.Bioorganic & medicinal chemistry letters · 2016Article
- In Vitro Growth Inhibitory Activities of Natural Products from Irciniid Sponges against Cancer Cells: A Comparative Study.BioMed research international · 2016Article
- Wittig derivatization of sesquiterpenoid polygodial leads to cytostatic agents with activity against drug resistant cancer cells and capable of pyrrolylation of primary amines.European journal of medicinal chemistry · 2015Article
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14 authors at 7 institutions in 4 countries.
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Abstract
Despite the recent advances in the treatment of tumors with intrinsic chemotherapy resistance, such as melanoma and renal cancers, their prognosis remains poor and new chemical agents with promising activity against these cancers are urgently needed. Sphaeropsidin A, a fungal metabolite whose anticancer potential had previously received little attention, was isolated from Diplodia cupressi and found to display specific anticancer activity in vitro against melanoma and kidney cancer subpanels in the National Cancer Institute (NCI) 60-cell line screen. The NCI data revealed a mean LC50 of ca. 10 µM and a cellular sensitivity profile that did not match that of any other agent in the 765,000 compound database. Subsequent mechanistic studies in melanoma and other multidrug-resistant in vitro cancer models showed that sphaeropsidin A can overcome apoptosis as well as multidrug resistance by inducing a marked and rapid cellular shrinkage related to the loss of intracellular Cl(-) and the decreased HCO3 (-) concentration in the culture supernatant. These changes in ion homeostasis and the absence of effects on the plasma membrane potential were attributed to the sphaeropsidin A-induced impairment of regulatory volume increase (RVI). Preliminary results also indicate that depending on the type of cancer, the sphaeropsidin A effects on RVI could be related to Na-K-2Cl electroneutral cotransporter or Cl(-)/HCO3 (-) anion exchanger(s) targeting. This study underscores the modulation of ion-transporter activity as a promising therapeutic strategy to combat drug-resistant cancers and identifies the fungal metabolite, sphaeropsidin A, as a lead to develop anticancer agents targeting RVI in cancer cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.