Andrographolide and its potent derivative exhibit anticancer effects against imatinib-resistant chronic myeloid leukemia cells by downregulating the Bcr-Abl oncoprotein

Liao, Hsin Chia; Chou, Yi Ju; Lin, Ching Cheng; Liu, Sheng Hung; Oswita, Giovanni Audrey; Huang, Yi; Wang, Ying Lien; Syu, Jia Ling; Sun, Chung‐Ming; Leu, Chuen Miin; Chao, Lin; Fu, Shu Ling

doi:10.1016/j.bcp.2019.02.028

Cited by 27 publications

(14 citation statements)

References 33 publications

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“…Accumulating evidences from clinical studies indicate that Andrographis paniculata extract and andrographolide reduce symptoms in patients with HIV, upper respiratory infection, ulcerative colitis or rheumatoid arthritis with considerable safety [ 10 , [27] , [28] , [29] , [30] ]. Furthermore, experimental data from preclinical studies demonstrated the diverse pharmacological mechanisms of A. paniculata and andrographolide, including those in anti-inflammation, antiviral activity, hepatoprotection, anti-pulmonary fibrosis, and cardiopretection [ 10 , 12 , [31] , [32] , [33] ] Particularly, their safety profile in clinical uses are well accepted and andrographolide up to 30 μM did not cause cytotoxicity on human peripheral blood mononuclear cells (PBMC) [ 10 , 34 ].…”

Section: Discussionmentioning

confidence: 99%

Andrographolide and its fluorescent derivative inhibit the main proteases of 2019-nCoV and SARS-CoV through covalent linkage

Shi

Huang²,

Chen³

et al. 2020

Biochemical and Biophysical Research Communications

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102

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The coronavirus disease 2019 (COVID-19) pandemic caused by 2019 novel coronavirus (2019-nCoV) has been a crisis of global health, whereas the effective vaccines against 2019-nCoV are still under development. Alternatively, utilization of old drugs or available medicine that can suppress the viral activity or replication may provide an urgent solution to suppress the rapid spread of 2019-nCoV. Andrographolide is a highly abundant natural product of the medicinal plant, Andrographis paniculata , which has been clinically used for inflammatory diseases and anti-viral therapy. We herein demonstrate that both andrographolide and its fluorescent derivative, the nitrobenzoxadiazole-conjugated andrographolide (Andro- NBD), suppressed the main protease (M pro ) activities of 2019-nCoV and severe acute respiratory syndrome coronavirus (SARS-CoV). Moreover, Andro-NBD was shown to covalently link its fluorescence to these proteases. Further mass spectrometry (MS) analysis suggests that andrographolide formed a covalent bond with the active site Cys 145 of either 2019-nCoV M pro or SARS-CoV M pro . Consistently, molecular modeling analysis supported the docking of andrographolide within the catalytic pockets of both viral M pro s. Considering that andrographolide is used in clinical practice with acceptable safety and its diverse pharmacological activities that could be beneficial for attenuating COVID-19 symptoms, extensive investigation of andrographolide on the suppression of 2019-nCoV as well as its application in COVID-19 therapy is suggested.

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Section: Discussionmentioning

confidence: 99%

Andrographolide and its fluorescent derivative inhibit the main proteases of 2019-nCoV and SARS-CoV through covalent linkage

Shi

Huang²,

Chen³

et al. 2020

Biochemical and Biophysical Research Communications

Self Cite

102

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“…The 2D and 3D structures of non-bond interactions of triptolide, stevioside, sphaeropsidin A, and caesalacetal with the target protein NS1 are shown in Figure 6. Andrographolide is a lactone diterpene, isolated from Andrographis paniculata, and possesses many biological effects, including antioxidant [39], anti-inflammatory [40], neuroprotective [41], hepatoprotective [42], anti-viral [43][44][45], anti-thrombotic [46], anticancer [47], and others. This diterpene lactone at 100 and 200 µM concentration showed an anti-DENV effect via GRP78 interaction pathway and at 5, 10, 15, and 25 ppm, a concentration larvicidal effect by inducing cytopathic effects in the midgut epithelium (LC 50 : 12 ppm) [23].…”

Section: Methyldodovi Sate Amentioning

confidence: 99%

Diterpenes/Diterpenoids and Their Derivatives as Potential Bioactive Leads against Dengue Virus: A Computational and Network Pharmacology Study

et al. 2021

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Dengue fever is a dangerous infectious endemic disease that affects over 100 nations worldwide, from Africa to the Western Pacific, and is caused by the dengue virus, which is transmitted to humans by an insect bite of Aedes aegypti. Millions of citizens have died as a result of dengue fever and dengue hemorrhagic fever across the globe. Envelope (E), serine protease (NS3), RNA-directed RNA polymerase (NS5), and non-structural protein 1 (NS1) are mostly required for cell proliferation and survival. Some of the diterpenoids and their derivatives produced by nature possess anti-dengue viral properties. The goal of the computational study was to scrutinize the effectiveness of diterpenoids and their derivatives against dengue viral proteins through in silico study. Methods: molecular docking was performed to analyze the binding affinity of compounds against four viral proteins: the envelope (E) protein, the NS1 protein, the NS3 protein, and the NS5 protein. Results: among the selected drug candidates, triptolide, stevioside, alepterolic acid, sphaeropsidin A, methyl dodovisate A, andrographolide, caesalacetal, and pyrimethamine have demonstrated moderate to good binding affinities (−8.0 to −9.4 kcal/mol) toward the selected proteins: E protein, NS3, NS5, and NS1 whereas pyrimethamine exerts −7.5, −6.3, −7.8, and −6.6 kcal/mol with viral proteins, respectively. Interestingly, the binding affinities of these lead compounds were better than those of an FDA-approved anti-viral medication (pyrimethamine), which is underused in dengue fever. Conclusion: we can conclude that diterpenoids can be considered as a possible anti-dengue medication option. However, in vivo investigation is recommended to back up the conclusions of this study.

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“…Diterpene andrographolide pharmacological actions include immune‐stimulating, antiviral, anticancer, hepatoprotective, antioxidant, antibacterial, and neuroprotective activities (Ajaya Kumar et al, 2004 ; Banerjee et al, 2017 ; Gupta et al, 2017 ; Liao et al, 2019 ; Luo et al, 2020 ; Nagalekshmi et al, 2011 ; Xu et al, 2019 ). Andrographolide is isolated from medicinal herbaceous plant Andrographis paniculata (Ajaya Kumar et al, 2004 ).…”

Section: Immunostimulation By Natural Productsmentioning

confidence: 99%

Combination of natural antivirals and potent immune invigorators: A natural remedy to combat COVID‐19

Shah

Rasul

Yousaf

et al. 2021

Phytotherapy Research

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The flare‐up in severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) that emerged in December 2019 in Wuhan, China, and spread expeditiously worldwide has become a health challenge globally. The rapid transmission, absence of anti‐SARS‐CoV‐2 drugs, and inexistence of vaccine are further exacerbating the situation. Several drugs, including chloroquine, remdesivir, and favipiravir, are presently undergoing clinical investigation to further scrutinize their effectiveness and validity in the management of COVID‐19. Natural products (NPs) in general, and plants constituents specifically, are unique sources for various effective and novel drugs. Immunostimulants, including vitamins, iron, zinc, chrysin, caffeic acid, and gallic acid, act as potent weapons against COVID‐19 by reinvigorating the defensive mechanisms of the immune system. Immunity boosters prevent COVID‐19 by stimulating the proliferation of T‐cells, B‐cells, and neutrophils, neutralizing the free radicals, inhibiting the immunosuppressive agents, and promoting cytokine production. Presently, antiviral therapy includes several lead compounds, such as baicalin, glycyrrhizin, theaflavin, and herbacetin, all of which seem to act against SARS‐CoV‐2 via particular targets, such as blocking virus entry, attachment to host cell receptor, inhibiting viral replication, and assembly and release.

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Andrographolide and its potent derivative exhibit anticancer effects against imatinib-resistant chronic myeloid leukemia cells by downregulating the Bcr-Abl oncoprotein

Cited by 27 publications

References 33 publications

Andrographolide and its fluorescent derivative inhibit the main proteases of 2019-nCoV and SARS-CoV through covalent linkage

Andrographolide and its fluorescent derivative inhibit the main proteases of 2019-nCoV and SARS-CoV through covalent linkage

Diterpenes/Diterpenoids and Their Derivatives as Potential Bioactive Leads against Dengue Virus: A Computational and Network Pharmacology Study

Combination of natural antivirals and potent immune invigorators: A natural remedy to combat COVID‐19

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