ArticleTumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine2015
RPF151, a novel capsaicin-like analogue: in vitro studies and in vivo preclinical antitumor evaluation in a breast cancer model.
Article in Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 28 citations in OpenAlex.
- Do Amino-Oxetanes Resemble Amides? A Matched Molecular Pairs Property and Structural Comparison.Journal of medicinal chemistry · 2026Article
- Natural and Synthetic Capsaicin Analogues: A Comprehensive Review of Biological Effects and Synthetic Pathways.Current medicinal chemistry · 2025Review
- Capsaicin Exerts Antitumor Activity in Mesothelioma Cells.Nutrients · 2024Article
- Anticancer Activity of Region B Capsaicin Analogs.Journal of medicinal chemistry · 2023Review
- Peppers: A "Hot" Natural Source for Antitumor Compounds.Molecules (Basel, Switzerland) · 2021Review
- Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.Journal of medicinal chemistry · 2020Review
- The "Yin and Yang" of Natural Compounds in Anticancer Therapy of Triple-Negative Breast Cancers.Cancers · 2018Review
- Multi-Spectroscopic and Theoretical Analysis on the Interaction between Human Serum Albumin and a Capsaicin Derivative-RPF101.Biomolecules · 2018Article
- Anticancer Activity of Natural and Synthetic Capsaicin Analogs.The Journal of pharmacology and experimental therapeutics · 2018Review
- Harnessing the Therapeutic Potential of Capsaicin and Its Analogues in Pain and Other Diseases.Molecules (Basel, Switzerland) · 2016Review
- Expression and functionality of TRPV1 in breast cancer cells.Breast cancer (Dove Medical Press) · 2016Article
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Authors and funding
13 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Capsaicin, the primary pungent component of the chili pepper, has antitumor activity. Herein, we describe the activity of RPF151, an alkyl sulfonamide analogue of capsaicin, against MDA-MB-231 breast cancer cells. RPF151 was synthetized, and molecular modeling was used to compare capsaicin and RPF151. Cytotoxicity of RPF151 on MDA-MB-231 was also evaluated by the 3-[4,5-dimethylthiazol-2-yl]-2,5diphenyltetrazolium bromide (MTT) assay. Cell cycle analysis, by flow cytometry, and Western blot analysis of cycle-related proteins were used to evaluate the antiproliferative mechanisms. Apoptosis was evaluated by phosphatidyl-serine externalization, cleavage of Ac-YVAD-AMC, and Bcl-2 expression. The production of reactive oxygen species was evaluated by flow cytometry. RPF151 in vivo antitumor effects were investigated in murine MDA-MB-231 model. This study shows that RPF151 downregulated p21 and cyclins A, D1, and D3, leading to S-phase arrest and apoptosis. Although RPF151 has induced the activation of TRPV-1 and TRAIL-R1/DR4 and TRAIL-2/DR5 on the surface of MDA-MB-231 cells, its in vivo antitumor activity was TRPV-1-independent, thus suggesting that RPF151 should not have the same pungency-based limitation of capsaicin. In silico analysis corroborated the biological findings, showing that RPF151 has physicochemical improvements over capsaicin. Overall, the activity of RPF151 against MDA-MB-231 and its lower pungency suggest that it may have a relevant role in cancer therapy.
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Registered trials
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.