Cytotoxic Activity of <i>Boesenbergia rotunda</i> Extracts against Nasopharyngeal Carcinoma Cells (HK1). Cardamonin, a <i>Boesenbergia rotunda</i> Constituent, Inhibits Growth and Migration of HK1 Cells by Inducing Caspase-Dependent Apoptosis and G2/M–Phase Arrest

Break, Mohammed Khaled Bin; Chiang, Michelle; Wiart, Christophe; Chin, Chiew Foan; Khoo, Alan Soo Beng; Khoo, Teng-Jin

doi:10.1080/01635581.2020.1751217

Cited by 19 publications

(17 citation statements)

References 17 publications

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“…This herb is widely used culinarily in China and Southeast Asia. Extracts of fingerroot rhizomes are well-known for its various pharmacological effects such as anti-allergic 30 , antibacterial 31 , 32 , antioxidant 33 , and anti-tumor activities 34 , 35 . Among the major active ingredients found in fingerroot, panduratin A, a prenylated cyclohexenyl chalcone, has been reported to possibly exhibit the antiviral activity against HIV-1 and dengue virus (DENV) 36 – 39 .…”

Section: Discussionmentioning

confidence: 99%

High-content screening of Thai medicinal plants reveals Boesenbergia rotunda extract and its component Panduratin A as anti-SARS-CoV-2 agents

Kanjanasirirat

Suksatu

Manopwisedjaroen

et al. 2020

Sci Rep

117

108

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Since December 2019, the emergence of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has caused severe pneumonia, a disease named COVID-19, that became pandemic and created an acute threat to public health. The effective therapeutics are in urgent need. Here, we developed a high-content screening for the antiviral candidates using fluorescence-based SARS-CoV-2 nucleoprotein detection in Vero E6 cells coupled with plaque reduction assay. Among 122 Thai natural products, we found that Boesenbergia rotunda extract and its phytochemical compound, panduratin A, exhibited the potent anti-SARS-CoV-2 activity. Treatment with B. rotunda extract and panduratin A after viral infection drastically suppressed SARS-CoV-2 infectivity in Vero E6 cells with IC50 of 3.62 μg/mL (CC50 = 28.06 µg/mL) and 0.81 μΜ (CC50 = 14.71 µM), respectively. Also, the treatment of panduratin A at the pre-entry phase inhibited SARS-CoV-2 infection with IC50 of 5.30 µM (CC50 = 43.47 µM). Our study demonstrated, for the first time, that panduratin A exerts the inhibitory effect against SARS-CoV-2 infection at both pre-entry and post-infection phases. Apart from Vero E6 cells, treatment with this compound was able to suppress viral infectivity in human airway epithelial cells. This result confirmed the potential of panduratin A as the anti-SARS-CoV-2 agent in the major target cells in human. Since B. rotunda is a culinary herb generally grown in China and Southeast Asia, its extract and the purified panduratin A may serve as the promising candidates for therapeutic purposes with economic advantage during COVID-19 situation.

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Section: Discussionmentioning

confidence: 99%

High-content screening of Thai medicinal plants reveals Boesenbergia rotunda extract and its component Panduratin A as anti-SARS-CoV-2 agents

Kanjanasirirat

Suksatu

Manopwisedjaroen

et al. 2020

Sci Rep

117

108

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“…31 antibacterial, 32,33 antioxidant, 34 and anti-tumor activities. 35,36 Among the major active ingredients found in ngerroot, panduratin A, a prenylated cyclohexenyl chalcone, has been reported to possibly exhibit the antiviral activity against HIV-1and dengue virus (DENV). [37][38][39][40] Several molecular and cellular mechanisms might be employed by panduratin A to exert its effect on anti-SARS-CoV-2 activity.…”

Section: Discussionmentioning

confidence: 99%

High-Content Screening of Thai Medicinal Plants Reveals Boesenbergia rotunda Extract and its Component Panduratin A as Anti-SARS-CoV-2 Agents

Kanjanasirirat

Suksatu

Manopwisedjaroen

et al. 2020

Preprint

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Since December 2019, the emergence of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has caused severe pneumonia, a disease named COVID-19, that became pandemic and created an acute threat to public health. The effective therapeutics are in urgent need. Here, we developed a high-content screening for the antiviral candidates using fluorescence-based SARS-CoV-2 nucleoprotein detection in Vero E6 cells coupled with plaque reduction assay. Among 122 Thai natural products, we found that Boesenbergia rotunda extract and its phytochemical compound, panduratin A, exhibited the potent anti-SARS-CoV-2 activity. Treatment with B. rotunda extract and panduratin A after viral infection drastically suppressed SARS-CoV-2 infectivity in Vero E6 cells with IC50 of 3.62 μg/mL (CC50 = 28.06 µg/mL) and 0.81 μΜ (CC50=14.71 µM), respectively. Also, the treatment of panduratin A at the pre-entry phase inhibited SARS-CoV-2 infection with IC50 of 5.30 µM (CC50=43.47 µM). Our study demonstrated, for the first time, that panduratin A exerts the inhibitory effect against SARS-CoV-2 infection at both pre-entry and post-infection phases. Since B. rotunda is a culinary herb generally grown in China and Southeast Asia, its extract and the purified panduratin A may serve as the promising candidates for therapeutic purposes with economic advantage during COVID-19 situation.

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“…Polyphenols are a family of natural products that are widely abundant in plants and display anticarcinogenic properties, resulting in a large number of studies being dedicated to developing polyphenols into effective anticancer agents. Cardamonin is a polyphenolic natural product that belongs to a larger family of compounds known as chalcones and was found to exhibit pronounced cytotoxic activity against a variety of cancer cell lines such as A549, M14, U266, MDA-MB-231, HK1, and MCF-7 [6,7]. Moreover, there were many studies that attempted to investigate cardamonin's mechanism of action where it was found to exert its cytotoxic activity via targeting a variety of signalling pathways such as JNK/FOXO3a, Wnt/β-catenin, and mTOR cascades [8][9][10].…”

Section: Introductionmentioning

confidence: 99%

Novel Semi-Synthetic Cu (II)–Cardamonin Complex Exerts Potent Anticancer Activity against Triple-Negative Breast and Pancreatic Cancer Cells via Inhibition of the Akt Signaling Pathway

et al. 2021

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Cardamonin is a polyphenolic natural product that has been shown to possess cytotoxic activity against a variety of cancer cell lines. We previously reported the semi-synthesis of a novel Cu (II)–cardamonin complex (19) that demonstrated potent antitumour activity. In this study, we further investigated the bioactivity of 19 against MDA-MB-468 and PANC-1 cancer cells in an attempt to discover an effective treatment for triple-negative breast cancer (TNBC) and pancreatic cancer, respectively. Results revealed that 19 abolished the formation of MDA-MB-468 and PANC-1 colonies, exerted growth-inhibitory activity, and inhibited cancer cell migration. Further mechanistic studies showed that 19 induced DNA damage resulting in gap 2 (G2)/mitosis (M) phase arrest and microtubule network disruption. Moreover, 19 generated reactive oxygen species (ROS) that may contribute to induction of apoptosis, corroborated by activation of caspase-3/7, PARP cleavage, and downregulation of Mcl-1. Complex 19 also decreased the expression levels of p-Akt and p-4EBP1, which indicates that the compound exerts its activity, at least in part, via inhibition of Akt signalling. Furthermore, 19 decreased the expression of c-Myc in PANC-1 cells only, which suggests that it may exert its bioactivity via multiple mechanisms of action. These results demonstrate the potential of 19 as a therapeutic agent for TNBC and pancreatic cancer.

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Cytotoxic Activity of Boesenbergia rotunda Extracts against Nasopharyngeal Carcinoma Cells (HK1). Cardamonin, a Boesenbergia rotunda Constituent, Inhibits Growth and Migration of HK1 Cells by Inducing Caspase-Dependent Apoptosis and G2/M–Phase Arrest

Cited by 19 publications

References 17 publications

High-content screening of Thai medicinal plants reveals Boesenbergia rotunda extract and its component Panduratin A as anti-SARS-CoV-2 agents

High-content screening of Thai medicinal plants reveals Boesenbergia rotunda extract and its component Panduratin A as anti-SARS-CoV-2 agents

High-Content Screening of Thai Medicinal Plants Reveals Boesenbergia rotunda Extract and its Component Panduratin A as Anti-SARS-CoV-2 Agents

Novel Semi-Synthetic Cu (II)–Cardamonin Complex Exerts Potent Anticancer Activity against Triple-Negative Breast and Pancreatic Cancer Cells via Inhibition of the Akt Signaling Pathway

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