In vitro adjuvant antitumor activity of various classes of semi-synthetic poststerone derivatives
Open accessAbstract
Various classes of semi-synthetic analogs of poststerone, the product of oxidative cleavage of the C20-C22 bond in the side chain of the phytoecdysteroid 20-hydroxyecdysone, were synthesized. The analogs were obtained by reductive transformations using L-Selectride and H 2-Pd/C, by molecular abeo-rearrangements using the DAST reagent or ultrasonic treatment in the NaI-Zn-DMF system, and by acid-catalyzed reactions of poststerone derivatives with various aldehydes (o-FC 6 H 4 CHO, m-CF 3 C 6 H 4 CHO, CO 2 Me(CH 2)8 CHO). The products were tested on a mouse lymphoma cell line pair, L5178 and its ABCB1-transfected multi-drug resistant counterpart, L5178 MDR, for their in vitro activity alone and in combination with doxorubicin, and for the ability to inhibit the ABCB1 transporter. Among the tested compounds, new 2,3-dioxolane derivatives of the pregnane ecdysteroid were found to have a pronounced chemosensitizing activity towards doxorubicin and could be considered as promising candidates for further structure optimization for the development of effective chemosensitizing agents.
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20E may possess antineoplastic activity.
“Recent studies have shown that 20E may also possess antineoplastic activity.”
From 20-Hydroxyecdysone Confers Antioxidant and Antineoplastic Properties in Human Non-Small Cell Lung Cancer Cells (2023) · cites this paper as [19]
20E and its derivatives sensitize breast cancer cells to genotoxic stress, induce autophagy, and attenuate multiple drug resistance.
“We and others have shown that 20E and its derivates sensibilize breast cancer cells to genotoxic stress, induce autophagy, and attenuate multiple drug resistance [12,13,14,15,16,17,18,19].”
From 20-Hydroxyecdysone Confers Antioxidant and Antineoplastic Properties in Human Non-Small Cell Lung Cancer Cells (2023) · cites this paper as [19]
20E and its derivatives modulate the resistance of cancer cells to genotoxic drugs and mitigate multidrug resistance.
“Furthermore, it has been shown previously that 20E and its derivates modulate the resistance of cancer cells to genotoxic drugs and mitigate multidrug resistance [12,13,14,15,16,17,18,19].”
From 20-Hydroxyecdysone Confers Antioxidant and Antineoplastic Properties in Human Non-Small Cell Lung Cancer Cells (2023) · cites this paper as [19]
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- Authors
- Savchenko, R. G., Nové, M., Spengler, G., Hunyadi, A., & Parfenova, L. V.
- Affiliations
- University of Szeged (HU)
- Institute of Catalysis and Petrochemistry (RU)
- Corresponding author
- Hunyadi, Attila
- Parfenova, Lyudmila V.
- Venue
- Bioorganic Chemistry
- Publisher
- Elsevier BV
- Published
- 2021-01
- Volume
- 106
- Pages
- 104485
- ISSN
- 0045-2068 (ISSN-L)
- OpenAlex
- W3102002327
- Cited by
- 8
- References
- 39
- Citations by year
- 2026: 2 · 2023: 1 · 2022: 3 · 2021: 2
- FWCI
- 0.49
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Bioorganic Chemistry (publishedVersion)
- PubMed (publishedVersion)
- SZTE Publicatio Repozitórium (University of Szeged) (acceptedVersion, other-oa)
- Funders
- National Research, Development and Innovation Office (K119770)
- Ministry of Education and Science of the Russian Federation (2019-05-595-000-058)
- Russian Foundation for Basic Research (20-03-00649, AAAA-A19-119022290012-3)
- Russian Academy of Sciences
- Nemzeti Kutatási Fejlesztési és Innovációs Hivatal
- Emberi Eroforrások Minisztériuma (20391-3/2018/FEKUSTRAT)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Phytochemical Studies and Bioactivities
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Steroid Chemistry and Biochemistry
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Natural product bioactivities and synthesis
- Keywords
- phytoecdysteroids, 20-hydroxyecdysone, chemosensitizers, multidrug resistance, doxorubicin, reductive transformation
- MeSH terms
- Antineoplastic Agents, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Ecdysterone, Humans, Structure-Activity Relationship, Tumor Cells, Cultured, Molecular Structure, Cell Proliferation
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