Anti-leukaemia effects of leonurine in vitro and in vivo

Zhuang, Qiang; Ruan, Lina; Jin, Ting; Zheng, Xiangkuo; Jin, Zhi

doi:10.4149/gpb_2021018

Cited by 8 publications

(6 citation statements)

References 36 publications

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“…Yuan et al reported that leonurine hydrochloride inhibited the NF-κB and PI3K/Akt signaling pathways, preventing estrogen-efficiencyassociated osteoporosis [18]. Moreover, leonurine inhibits the activation of PI3K/Akt pathway by reducing the phosphorylation levels of PI3K and Akt [8]. To study the signaling mechanisms affected by leonurine in regulation of human breast cancer cells, the effect of leonurine on PI3K/AKT/mTOR pathway was evaluated.…”

Section: Discussionmentioning

confidence: 99%

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Leonurine inhibits breast cancer cell growth and angiogenesis via PI3K/AKT/mTOR pathway

Tian¹,

Peng²,

Wang³

2023

Trop. J. Pharm Res

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Purpose: To elucidate the effect of leonurine on the proliferation, invasion, migration, and angiogenetic potential of breast cancer cells. Methods: Human breast cancer cell line (MDA-MB-231) and normal breast cell line, (SK-BR-3) were cultured. Both cell lines were treated with 200, 400, or 800 μM leonurine and cultured for 0 (control), 24, 48, or 72 h. Cell counting kit-8 (CCK8) and colony formation assays were performed to measure cell viability and proliferation. Invasion and migration were evaluated using in vitro invasion and wound healing assays, respectively, while angiogenesis was evaluated by the formation of branching point structures. Furthermore, phosphorylation of PI3K, AKT, and mTOR were assessed by Western blot. Cell viability, invasion, migration, and angiogenesis were further investigated in media including 740Y-P, 800 μM leonurine, and 800 μM leonurine plus 740Y-P. Results: Leonurine inhibited the proliferation of breast cancer cells and weakened breast cancer cell invasion, migration, and angiogenetic potential in a dose-dependent manner (p < 0.05). Furthermore, leonurine repressed PI3K/AKT/mTOR pathway by reducing the phosphorylation of PI3K, AKT, and mTOR. Leonurine also inhibited breast cancer progression (p < 0.05). Conclusion: Leonurine inhibits breast cancer progression by inhibiting PI3K/AKT/mTOR pathway, and is thus, a potential agent for the management of breast cancer.

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Section: Discussionmentioning

confidence: 99%

“…Moreover, leonurine suppresses colony formation and proliferation and enhances apoptosis of chronic myeloid leukemia cells [7]. Leonurine also inhibits the activity of PI3K/Akt pathway by reducing PI3K and Akt phosphorylation [8]. However, the effects of leonurine on breast cancer and its related mechanisms are still unclear.…”

Section: Introductionmentioning

confidence: 99%

Leonurine inhibits breast cancer cell growth and angiogenesis via PI3K/AKT/mTOR pathway

Tian¹,

Peng²,

Wang³

2023

Trop. J. Pharm Res

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“…Firstly, we established an in vivo model using the U-937 cell line. We used this cell line because it is more aggressive, has a histiocytic subtype, and exhibits diffuse proliferation; moreover, it is routinely used for the evaluation of antitumor and cytotoxic activity in natural products [ 25 , 26 , 27 , 28 ]. At day 29, we found substantial differences in the weight gains of the left and right inguinal and axillary lymph nodes, compared to our healthy control ( Figure 6 ).…”

Section: Discussionmentioning

confidence: 99%

Understanding the Antilymphoma Activity of Annona macroprophyllata Donn and Its Acyclic Terpenoids: In Vivo, In Vitro, and In Silico Studies

et al. 2022

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Annona macroprophyllata Donn (A. macroprophyllata) is used in traditional Mexican medicine for the treatment of cancer, diabetes, inflammation, and pain. In this work, we evaluated the antitumor activity of three acyclic terpenoids obtained from A. macroprophyllata to assess their potential as antilymphoma agents. We identified the terpenoids farnesyl acetate (FA), phytol (PT) and geranylgeraniol (Gg) using gas chromatography–mass spectroscopy (GC-MS) and spectroscopic (1H, and 13C NMR) methods applied to petroleum ether extract of leaves from A. macroprophyllata (PEAm). We investigated antitumor potential in Balb/c mice inoculated with U-937 cells by assessing brine shrimp lethality (BSL), and cytotoxic activity in these cells. In addition, to assess the potential toxicity of PEAm, FA, PT and Gg in humans, we tested their acute oral toxicity in mice. Our results showed that the three terpenoids exhibited considerable antilymphoma and cytotoxic activity. In terms of lethality, we determined a median lethal dose (LD50) for thirteen isolated products of PEAm. Gg, PT and AF all exhibited a higher lethality with values of 1.41 ± 0.42, 3.03 ± 0.33 and 5.82 ± 0.58 µg mL−1, respectively. To assess cytotoxic activity against U-937 cells, we calculated the mean cytotoxic concentration (CC50) and found that FA and PT were closer in respect to the control drug methotrexate (MTX, 0.243 ± 0.007 µM). In terms of antilymphoma activity, we found that FA, PT and Gg considerably inhibited lymph node growth, with median effective doses (ED50) of 5.89 ± 0.39, 6.71 ± 0.31 and 7.22 ± 0.51 mg kg−1 in females and 5.09 ± 0.66, 5.83 ± 0.50 and 6.98 ± 0.57mg kg −1 in males, respectively. Regarding acute oral toxicity, we classified all three terpenoids as category IV, indicating a high safety margin for human administration. Finally, in a molecular docking study of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, we found binding of terpenoids to some amino acids of the catalytic site, suggesting an effect upon activity with a resulting decrease in the synthesis of intermediates involved in the prenylation of proteins involved in cancer progression. Our findings suggest that the acyclic terpenoids FA, PT, and Gg may serve as scaffolds for the development of new treatments for non-Hodgkin’s lymphoma.

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“…Leo displays antitumor effects both in vivo and in vitro, with physiological effects as shown in Figure 1. It exerts its antitumor actions by inducing tumor cell apoptosis and inhibiting tumor cell proliferation, invasion, and migration Hu et al, 2019;Zhuang et al, 2021).…”

Section: Main Antitumor Mechanisms Of Leomentioning

confidence: 99%

New Mechanisms for Anti-Cancer Drugs

2024

Frontiers Research Topics

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Frontiers is more than just an open access publisher of scholarly articles: it is a pioneering approach to the world of academia, radically improving the way scholarly research is managed. The grand vision of Frontiers is a world where all people have an equal opportunity to seek, share and generate knowledge. Frontiers provides immediate and permanent online open access to all its publications, but this alone is not enough to realize our grand goals. Frontiers journal seriesThe Frontiers journal series is a multi-tier and interdisciplinary set of openaccess, online journals, promising a paradigm shift from the current review, selection and dissemination processes in academic publishing. All Frontiers journals are driven by researchers for researchers; therefore, they constitute a service to the scholarly community. At the same time, the Frontiers journal series operates on a revolutionary invention, the tiered publishing system, initially addressing specific communities of scholars, and gradually climbing up to broader public understanding, thus serving the interests of the lay society, too. Dedication to qualityEach Frontiers article is a landmark of the highest quality, thanks to genuinely collaborative interactions between authors and review editors, who include some of the world's best academicians. Research must be certified by peers before entering a stream of knowledge that may eventually reach the public -and shape society; therefore, Frontiers only applies the most rigorous and unbiased reviews. Frontiers revolutionizes research publishing by freely delivering the most outstanding research, evaluated with no bias from both the academic and social point of view. By applying the most advanced information technologies, Frontiers is catapulting scholarly publishing into a new generation. What are Frontiers Research Topics?Frontiers Research Topics are very popular trademarks of the Frontiers journals series: they are collections of at least ten articles, all centered on a particular subject. With their unique mix of varied contributions from Original Research to Review Articles, Frontiers Research Topics unify the most influential researchers, the latest key findings and historical advances in a hot research area.

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Anti-leukaemia effects of leonurine in vitro and in vivo

Cited by 8 publications

References 36 publications

Leonurine inhibits breast cancer cell growth and angiogenesis via PI3K/AKT/mTOR pathway

Leonurine inhibits breast cancer cell growth and angiogenesis via PI3K/AKT/mTOR pathway

Understanding the Antilymphoma Activity of Annona macroprophyllata Donn and Its Acyclic Terpenoids: In Vivo, In Vitro, and In Silico Studies

New Mechanisms for Anti-Cancer Drugs

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