Cytotoxicity of Lapachol and Derivatized Analogues from Kigelia africana (Lam.) Benth. on Cancer Cell Lines

Atolanı, Olubunmi; Olatunji, Gabriel Ademola; Adeyemi, Oluyomi Stephen

doi:10.1007/s13369-020-05113-1

Cited by 6 publications

(3 citation statements)

References 14 publications

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“…Other recent studies have shown that complexes of ruthenium with different phosphine ligands can induce cytotoxic activity against cancer cell lines ( 54 – 56 ). Lapachol and its derivatives showed antiproliferative effects in different histological types of cells, including ovary, colon, lung, breast, leukemia, esophageal, cervical, melanoma, and prostate ( 7 , 57 – 63 ). In this study, both lapachol-containing ruthenium(II) complexes displayed cytotoxic activity up to 100-fold higher than metal-free lapachol.…”

Section: Discussionmentioning

confidence: 99%

A Novel Ruthenium(II) Complex With Lapachol Induces G2/M Phase Arrest Through Aurora-B Kinase Down-Regulation and ROS-Mediated Apoptosis in Human Prostate Adenocarcinoma Cells

et al. 2021

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Lapachol is a well-studied natural product that has been receiving great interest due to its anticancer properties that target oxidative stress. In the present work, two novel lapachol-containing ruthenium(II) complexes [Ru(Lap)(dppm)(bipy)]PF6 (1) and [Ru(Lap)(dppm)(phen)]PF6 (2) [Lap = lapachol, dppm = 1,1′-bis(diphosphino)methane, bipy = 2,2′-bipyridine, phen = 1,10-phenantroline] were synthesized, fully characterized, and investigated for their cellular and molecular responses on cancer cell lines. We found that both complexes exhibited a potent cytotoxic effect in a panel of cancer cell lines in monolayer cultures, as well as in a 3D model of multicellular spheroids formed from DU-145 human prostate adenocarcinoma cells. Furthermore, the complex (2) suppressed the colony formation, induced G2/M-phase arrest, and downregulated Aurora-B. The mechanism studies suggest that complex (2) stimulate the overproduction of reactive oxygen species (ROS) and triggers caspase-dependent apoptosis as a result of changes in expression of several genes related to cell proliferation and caspase-3 and -9 activation. Interestingly, we found that N-acetyl-L-cysteine, a ROS scavenger, suppressed the generation of intracellular ROS induced by complex (2), and decreased its cytotoxicity, indicating that ROS-mediated DNA damage leads the DU-145 cells into apoptosis. Overall, we highlighted that coordination of lapachol to phosphinic ruthenium(II) compounds considerably improves the antiproliferative activities of resulting complexes granting attractive selectivity to human prostate adenocarcinoma cells. The DNA damage response to ROS seems to be involved in the induction of caspase-mediated cell death that plays an important role in the complexes' cytotoxicity. Upon further investigations, this novel class of lapachol-containing ruthenium(II) complexes might indicate promising chemotherapeutic agents for prostate cancer therapy.

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Section: Discussionmentioning

confidence: 99%

A Novel Ruthenium(II) Complex With Lapachol Induces G2/M Phase Arrest Through Aurora-B Kinase Down-Regulation and ROS-Mediated Apoptosis in Human Prostate Adenocarcinoma Cells

et al. 2021

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“…The antioxidant potential of the essential oils was determined by using DPPH (1,1-diphenyl1-2picrylhydrazyl) assay following standard procedure 14,16 . DPPH solution (0.1mM) was prepared in methanol and incubated at room temperature overnight in the dark before use.…”

Section: Dpph Assaymentioning

confidence: 99%

CHEMICAL COMPOSITION AND ANTIOXIDANT ACTIVITY OF THE ESSENTIAL OILS FROM WHITE AND GREEN LEAVES OF NIGERIA-GROWN Ficus microcarpa

Atolanı¹,

Adeosun²,

Oluyori³

et al. 2019

RJC

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The chemical composition and antioxidant potentials of the essential oils obtained from white and green leaves of Ficus microcarpa were investigated. The essential oils were derived using hydro-distillation method and Gas Chromatography -Mass Spectrometry analysis was used to detect the different constituents in the essential oils. The 1,1-diphenyl-2-picryl radical antioxidant assay was performed to investigate the free radical scavenging capacity of the essential oils. Twenty phytochemicals were common to both essential oils while some notable differences were observed between them. Phytol (40.90%) and copaene (15.85%) were the most abundant compounds in the white leaves while megastigmatrienone (14.98%), 1,3-cyclohexadiene (9.20%) and 1-hexanol (8.80%) were the most abundant in the green leaves. The essential oil from the white leaves with a higher concentration of phytol exhibited the greater antioxidant potential. The plant may, therefore, be employed as a viable phytochemical bio-resource in medical applications.

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“…Bioactive principles have been obtained from various parts of plants which include the leaves, stem, wood, root, flowers and seed [ 14 ]. The root of plant has been a source isolation of bioactive principles [ [15] , [16] , [17] , [18] ]. While nanoparticles have been used for various things like biosensor preparation [ 19 , 20 ], the nanoparticles produced from the plant exhibited anti-inflammatory and antinociceptive activities in the animal model [ 21 , 22 ].…”

Section: Introductionmentioning

confidence: 99%

Isolation, characterization and anti-inflammatory activity of compounds from the Vernonia amygdalina

Atolani,

Usman,

Adejumo

et al. 2024

Heliyon

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Cytotoxicity of Lapachol and Derivatized Analogues from Kigelia africana (Lam.) Benth. on Cancer Cell Lines

Cited by 6 publications

References 14 publications

A Novel Ruthenium(II) Complex With Lapachol Induces G2/M Phase Arrest Through Aurora-B Kinase Down-Regulation and ROS-Mediated Apoptosis in Human Prostate Adenocarcinoma Cells

A Novel Ruthenium(II) Complex With Lapachol Induces G2/M Phase Arrest Through Aurora-B Kinase Down-Regulation and ROS-Mediated Apoptosis in Human Prostate Adenocarcinoma Cells

CHEMICAL COMPOSITION AND ANTIOXIDANT ACTIVITY OF THE ESSENTIAL OILS FROM WHITE AND GREEN LEAVES OF NIGERIA-GROWN Ficus microcarpa

Isolation, characterization and anti-inflammatory activity of compounds from the Vernonia amygdalina

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