CYTOTOXICITY AND ANTITUMOR ACTIVITY OF SESQUITERPENE LACTONES. STRUCTURE, ACTIVITY
Adekenov S. Maslova O. Iskakova Z. Doskaliyev A.
2023Technology Center
ScienceRise: Pharmaceutical Science
2023#46Issue 653 - 63 pp.
The article discusses the results of screening 19 samples of sesquiterpene γ-lactones argolide, groshemin, estafiatine, 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 tumour cell lines. The aim. The aim of this study is to study the cytotoxicity and antitumor activity of the sesquiterpene γ-lactones argolide, groshemin, estafiatine 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 sarcoma 45-resistant to 5-fluorouracil. The antitumor activity of the samples was studied in vivo experiments on white outbred rats with transplanted tumour strains and was assessed by inhibition of tumour 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 vitro samples of the sesquiterpene γ-lactones argolide, groshemin, and estafiatine 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-acetylgroshemin, 13-morpholingroshemin, 3-keto-4-methylene-cis-guaianolide, 3α-acetoxy-isosalusanin C, and 10α(14)-epoxy-1,5,7α,4,6β(H)-guai-11(13)-ene-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, sarcoma 45, resistant to 5-fluorouracil.
antitumor activity , cytotoxicity , inoculated tumour lines , sesquiterpene lactones , tumour cell culture
Text of the article Перейти на текст статьи
JSC International Research and Production Holding “Phytochemistry”, M. Gazalieva str., 4, Karaganda, 100009, Kazakhstan
JSC International Research and Production Holding “Phytochemistry”
10 лет помогаем публиковать статьи Международный издатель
Книга Публикация научной статьи Волощук 2026 Book Publication of a scientific article 2026