Cytotoxicity and antitumor activity of sesquiterpene lactones. Structure, activity

Authors

DOI:

https://doi.org/10.15587/2519-4852.2023.295228

Keywords:

sesquiterpene lactones, tumour cell culture, cytotoxicity, inoculated tumour lines, antitumor activity

Abstract

The article discusses the results of 19 samples screening of sesquiterpene γ-lactones argolide, grosheimin, estafiatin, and their derivatives for cytotoxicity and antitumor activity. The research results indicate significant cytotoxicity and selectivity of the action of sesquiterpene γ-lactones and their derivatives against most tumor cell lines.

Aim. The purpose of this study is to study the cytotoxicity and antitumor activity of the sesquiterpene γ-lactones argolide, grosheimin, estafiatin and their chemically modified derivatives, as practically renewable materials.

Methods. The cytotoxicity of the compounds was determined using vero cells, THP-1, Pliss lymphosarcoma cell lines, Walker carcinosarcoma, sarcoma 45, sarcoma-180, alveolar liver cancer PC-1, P-388 leukemia, L-1210 leukemia, and resistant to 5-fluorouracil sarcoma 45.

The antitumor activity of the samples was studied in in vivo experiments on white outbred rats with transplanted tumor strains and was assessed by inhibition of tumor growth and the magnitude of the increase in average life expectancy.

Statistical processing of the results was carried out using the program “GraphPad Prism v. 6.0" (GraphPad Software Inc., USA).

Conclusion. When determining cytotoxicity in in vitro samples of the sesquiterpene γ-lactones argolide, grosheimin, and estafiatin showed selectivity of their action on cells of 8 tumor lines, on cells of human acute monocytic leukemia THP-1 and in relation to the larvae of sea crustaceans Artemia salina (Leach).

Samples of argolide, 8-acetylgrosheimin, 13-morpholinogrosheimin, 3-keto-4-methylene-cis-guaianolide, 3α-acetoxyisozaluzanin C, and 10α(14)-epoxy-1,5,7α,4,6β(H)-guai-11(13)-en-4(3),6(12)-diolide in experiments in vivo possessed high antitumor activity against transplantable tumor strains of Pliss lymphosarcoma, Walker carcinosarcoma, sarcoma 45, sarcoma 37, sarcoma 180, alveolar liver cancer PC-1, leukemia P-388 and L-1210, resistant to 5-fluorouracil sarcoma 45

Author Biographies

Olga Maslova, JSC International Research and Production Holding “Phytochemistry”

Master, Researcher

Pharmacology Laboratory

Zhanar Iskakova, JSC International Research and Production Holding “Phytochemistry”

PhD, Senior Researcher

Pharmacology Laboratory

Aidos Doskaliyev, JSC International Research and Production Holding “Phytochemistry”

PhD, Senior Researcher

Pharmacology Laboratory

Sergazy Adekenov, JSC International Research and Production Holding “Phytochemistry”

Doctor of Chemical Sciences, General Director

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Cytotoxicity and antitumor activity of sesquiterpene lactones. Structure, activity

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Published

2023-12-31

How to Cite

Maslova, O., Iskakova, Z., Doskaliyev, A., & Adekenov, S. (2023). Cytotoxicity and antitumor activity of sesquiterpene lactones. Structure, activity. ScienceRise: Pharmaceutical Science, (6(46), 53–63. https://doi.org/10.15587/2519-4852.2023.295228

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No. 6(46) (2023)

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Pharmaceutical Science

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Copyright (c) 2023 Olga Maslova, Zhanar Iskakova, Aidos Doskaliyev, Sergazy Adekenov

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