Pharmacokinetics of chelerythrine and its metabolite after oral and intramuscular administrations in pigs

Zhao, Na-Jiao; Wang, Lili; Liu, Zhao‐Ying; Wang, Qin; Liu, Lei; Sun, Zhi-Liang; Yong, Wu

doi:10.1080/00498254.2021.1882714

Cited by 4 publications

(2 citation statements)

References 28 publications

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“…The time to reach peak plasma concentration in a single oral administration was also rapid and was obtained in less than 2 hours. Half-life (T ½) of chelerythrine was calculated to be 2.03 hours and it is metabolized rapidly after a single oral administration [ 90 ].…”

Section: Pharmacokinetic and Toxicological Properties Of Chelerythrinementioning

confidence: 99%

Therapeutic potential of chelerythrine as a multi-purpose adjuvant for the treatment of COVID-19

et al. 2021

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Multifunctional nature of phytochemicals and their chemical diversity has attracted attention to develop leads originated from nature to fight COVID-19. Pharmacological activities of chelerythrine and its congeners have been studied and reported in the literature. This compound simultaneously has two key therapeutic effects for the treatment of COVID-19, antiviral and anti-inflammatory activities. Chelerythrine can prevent hyper-inflammatory immune response through regulating critical signaling pathways involved in SARS-CoV-2 infection, such as alteration in Nrf2, NF-κB, and p38 MAPK activities. In addition, chelerythrine has a strong protein kinase C-α/-β inhibitory activity suitable for cerebral vasospasm prevention and eryptosis reduction, as well as beneficial effects in suppressing pulmonary inflammation and fibrosis. In terms of antiviral activity, chelerythrine can fight with SARS-CoV-2 through various mechanisms, such as direct-acting mechanism, viral RNA-intercalation, and regulation of host-based antiviral targets. Although chelerythrine is toxic in vitro, the in vivo toxicity is significantly reduced due to its structural conversion to alkanolamine. Its multifunctional action makes chelerythrine a prominent compound for the treatment of COVID-19. Considering precautions related to the toxicity at higher doses, it is expected that this compound is useful in combination with proper antivirals to reduce the severity of COVID-19 symptoms.

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Section: Pharmacokinetic and Toxicological Properties Of Chelerythrinementioning

confidence: 99%

Therapeutic potential of chelerythrine as a multi-purpose adjuvant for the treatment of COVID-19

et al. 2021

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“…After oral and IM administrations in pigs, CHE rapidly reached C max of 5.04 ± 1.00 ng/ml at 1.83 ± 0.26 h and C max of 69.79 ± 15.41 ng/ml at 0.42 ± 0.13 h, respectively. The half-life ( T 1/2 ) was 2.03 ± 0.26 h for CHE ( Zhao et al, 2021 ). The results of these studies revealed that CHE is metabolized rapidly.…”

Section: Toxicity Study and Clinical Application Of Chelerythrinementioning

confidence: 99%

Rediscovery of Traditional Plant Medicine: An Underestimated Anticancer Drug of Chelerythrine

Chen

et al. 2022

Front. Pharmacol.

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In many studies, the extensive and significant anticancer activity of chelerythrine (CHE) was identified, which is the primary natural active compound in four traditional botanical drugs and can be applied as a promising treatment in various solid tumors. So this review aimed to summarize the anticancer capacities and the antitumor mechanism of CHE. The literature searches revolving around CHE have been carried out on PubMed, Web of Science, ScienceDirect, and MEDLINE databases. Increasing evidence indicates that CHE, as a benzophenanthridine alkaloid, exhibits its excellent anticancer activity as CHE can intervene in tumor progression and inhibit tumor growth in multiple ways, such as induction of cancer cell apoptosis, cell cycle arrest, prevention of tumor invasion and metastasis, autophagy-mediated cell death, bind selectively to telomeric G-quadruplex and strongly inhibit the telomerase activity through G-quadruplex stabilization, reactive oxygen species (ROS), mitogen-activated protein kinase (MAPK), and PKC. The role of CHE against diverse types of cancers has been investigated in many studies and has been identified as the main antitumor drug candidate in drug discovery programs. The current complex data suggest the potential value in clinical application and the future direction of CHE as a therapeutic drug in cancer. Furthermore, the limitations and the present problems are also highlighted in this review. Despite the unclearly delineated molecular targets of CHE, extensive research in this area provided continuously fresh data exploitable in the clinic while addressing the present requirement for further studies such as toxicological studies, combination medication, and the development of novel chemical methods or biomaterials to extend the effects of CHE or the development of its derivatives and analogs, contributing to the effective transformation of this underestimated anticancer drug into clinical practice. We believe that this review can provide support for the clinical application of a new anticancer drug in the future.

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Sex differences in the pharmacokinetics and tissue residues of Macleaya cordata extracts in rats

et al. 2022

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Pharmacokinetics of chelerythrine and its metabolite after oral and intramuscular administrations in pigs

Cited by 4 publications

References 28 publications

Therapeutic potential of chelerythrine as a multi-purpose adjuvant for the treatment of COVID-19

Therapeutic potential of chelerythrine as a multi-purpose adjuvant for the treatment of COVID-19

Rediscovery of Traditional Plant Medicine: An Underestimated Anticancer Drug of Chelerythrine

Sex differences in the pharmacokinetics and tissue residues of Macleaya cordata extracts in rats

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