In Vitro and In Silico Studies on Leonotis nepetifolia (L.) R. Br. Root Extract against Cancer Cells

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  • Tytuł: In Vitro and In Silico Studies on Leonotis nepetifolia (L.) R. Br. Root Extract against Cancer Cells
  • Autor/Autorzy:
  • Nazwa czasopisma: CURRENT PHARMACEUTICAL BIOTECHNOLOGY
  • Rok: 2022
  • ISSN: 1389-2010
  • DOI: 10.2174/1389201023666220304095225
  • Adres www:: https://www.eurekaselect.com/article/121316
  • Strony od-do: 1-111
  • Język: angielski
  • Abstrakt: Background: Leonotis nepetifolia (L.) R. Br. (Lamiaceae) is a shrub traditionally used to alleviate inflammatory conditions. Objective: The present study aimed at investigating the biological activity of methanolic nontrans-formed and transformed Rhizobium rhizogenes root extracts from L. nepetifolia against human melanoma cells. Methods: Cytotoxicity and genotoxicity properties, the impact on topoisomerase I activity, and proapoptotic activity were evaluated by the MTT test, comet assay, topoisomerase I assay, and fluorescence-activated cell sorting analysis. Moreover, the expressions of p53 were examined by qPCR and Western blot analysis. Docking studies were conducted to assess the potential interac-tions of the identified phytochemicals with the p53 binding protein Mdm-2, and computational analyses exhibited their antioxidant potential. Results: Both extracts showed cytotoxic potential against human melanoma cells, but generally the activity was more potent for transformed roots than untransformed (IC50 760 μg/mL and 980 μg/mL, respectively). A similar effect was revealed during the evaluation of genotoxic and proapoptotic properties. Moreover, the expression of p53 was also found to be increased after ex-tract treatment. The most dominant identified compounds in both extracts were as follows: (+)-catechin, p-coumaric acid, m-coumaric acid, and (+)-rosmarinic acid. Docking studies and compu-tational analysis showed that (+)-rosmarinic acid possesses the highest binding affinity to the p53 binding protein, Mdm-2, and exhibits the best antioxidant property from the most commonly iden-tified phytochemicals. Conclusion: Our findings revealed the potential of L. nepetifolia transformed root extract as a source of bioactive compounds with cytotoxic, genotoxic, and proapoptotic activity against human melanoma cells as well as antioxidant properties.
  • Dyscyplina: nauki medyczne
  • 002 a In Vitro and In Silico Studies on Leonotis nepetifolia (L.) R. Br. Root Extract against Cancer Cells
  • 003 b 0000-0001-8757-6958
  • 003 a Anna Merecz-Sadowska (Autor)
  • 003 a EWA KUCHARSKA (Autor)
  • 003 a Hanna Zielińska-Bliźniewska (Autor)
  • 003 a Karolina Zajdel (Autor)
  • 003 a Katarzyna Malinowska (Autor)
  • 003 a Przemysław Sitarek (Autor)
  • 003 a Radosław Zajdel (Autor)
  • 003 a Tomasz Śliwiński (Autor)
  • 004 a Oryginalny artykuł naukowy
  • 006 a CURRENT PHARMACEUTICAL BIOTECHNOLOGY
  • 008 a 2022
  • 011 a 1389-2010
  • 013 a 10.2174/1389201023666220304095225
  • 014 a https://www.eurekaselect.com/article/121316
  • 015 a 1-111
  • 017 a angielski
  • 020 a Background: Leonotis nepetifolia (L.) R. Br. (Lamiaceae) is a shrub traditionally used to alleviate inflammatory conditions. Objective: The present study aimed at investigating the biological activity of methanolic nontrans-formed and transformed Rhizobium rhizogenes root extracts from L. nepetifolia against human melanoma cells. Methods: Cytotoxicity and genotoxicity properties, the impact on topoisomerase I activity, and proapoptotic activity were evaluated by the MTT test, comet assay, topoisomerase I assay, and fluorescence-activated cell sorting analysis. Moreover, the expressions of p53 were examined by qPCR and Western blot analysis. Docking studies were conducted to assess the potential interac-tions of the identified phytochemicals with the p53 binding protein Mdm-2, and computational analyses exhibited their antioxidant potential. Results: Both extracts showed cytotoxic potential against human melanoma cells, but generally the activity was more potent for transformed roots than untransformed (IC50 760 μg/mL and 980 μg/mL, respectively). A similar effect was revealed during the evaluation of genotoxic and proapoptotic properties. Moreover, the expression of p53 was also found to be increased after ex-tract treatment. The most dominant identified compounds in both extracts were as follows: (+)-catechin, p-coumaric acid, m-coumaric acid, and (+)-rosmarinic acid. Docking studies and compu-tational analysis showed that (+)-rosmarinic acid possesses the highest binding affinity to the p53 binding protein, Mdm-2, and exhibits the best antioxidant property from the most commonly iden-tified phytochemicals. Conclusion: Our findings revealed the potential of L. nepetifolia transformed root extract as a source of bioactive compounds with cytotoxic, genotoxic, and proapoptotic activity against human melanoma cells as well as antioxidant properties.
  • 966 a nauki medyczne
  • 985 a Wydział Pedagogiczny
  • 985 b Instytut Nauk o Wychowaniu
Repozytorium Akademii Ignatianum w Krakowie, które jest częścią Portalu Pracowniczego zostało zrealizowane w ramach projektu „Program wzmocnienia potencjału dydaktycznego Uczelni na rzecz rozwoju regionalnego” POWR.03.05.00-00-ZR10/18 współfinansowanego ze środków Unii Europejskiej w ramach Europejskiego Funduszu Społecznego.