Influence of verapamil on the pharmacokinetics of rotundic acid in rats and its potential mechanism

Hong, Shang; Wang, Ze; Ma, Hong; Sun, Yinghui; Ci, Xiaoyan; Gu, Yuan; Liu, Changxiao; Si, Duanyun

doi:10.1080/13880209.2021.1871634

Cited by 8 publications

(7 citation statements)

References 35 publications

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“…Another study indicates that the poor bioavailability of RA could be attributed to CYP3A‐induced metabolism and the involvement of the efflux transporter P‐gp. The study also found that co‐administration of RA with verapamil could enhance the absorption of RA by suppressing the effect of P‐gp in a Caco‐2 cell model, as well as slow down the metabolism of RA in the liver of rats by suppressing the activity of CYP3A [74] . A different study reported that the main metabolic pathways for RA include demethylation, desaturation, hydroxylation, reduction, sulfation, and glucuronidation [75] .…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 86%

“…The study also found that co-administration of RA with verapamil could enhance the absorption of RA by suppressing the effect of P-gp in a Caco-2 cell model, as well as slow down the metabolism of RA in the liver of rats by suppressing the activity of CYP3A. [74] A different study reported that the main metabolic pathways for RA include demethylation, desaturation, hydroxylation, reduction, sulfation, and glucuronidation. [75] The study also found that RA is eliminated rapidly, with a half-life (t1/2) of nearly 2 hours.…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 87%

“…A different study reported that the main metabolic pathways for RA include demethylation, desaturation, hydroxylation, reduction, sulfation, and glucuronidation [75] . The study also found that RA is eliminated rapidly, with a half‐life (t1/2) of nearly 2 hours [74] …”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 98%

“…[75] The study also found that RA is eliminated rapidly, with a half-life (t1/2) of nearly 2 hours. [74] Table 1. Biological sources of rotundic acid.…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 99%

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Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

Bhuia,

Chowdhury,

Sonia

et al. 2024

Chemistry & Biodiversity

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Rotundic acid (RA) is a naturally occurring pentacyclic triterpene with a multitude of pharmacological activities. The primary emphasis of this study is on summarizing the anticancer properties with the underlying mechanisms of RA and its derivatives, as well as the pharmacokinetic features. Data was collected (up to date as of November 10, 2023) from various reliable and authentic literatures by searching in different academic search engines, including PubMed, Springer Link, Scopus, Wiley Online, Web of Science, ScienceDirect, and Google Scholar. The findings imply that RA and its synthetic derivatives possess promising anti‐cancer properties against breast, colorectal, liver, and cervical cancers in various preclinical pharmacological test systems. The results also indicate that RA and its derivatives demonstrated anticancer effects via a number of cellular mechanisms, including apoptotic cell death, inhibition of oxidative stress, anti‐inflammatory effect, cytotoxicity, cell cycle arrest, anti‐proliferative effect, anti‐angiogenic effect, and inhibition of cancer cell migration and invasion. It has been proposed that RA and its derived compounds have the capability to serve as a hopeful chemotherapeutic agent, so further extensive clinical research is necessary.

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Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 86%

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 87%

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 98%

“…[75] The study also found that RA is eliminated rapidly, with a half-life (t1/2) of nearly 2 hours. [74] Table 1. Biological sources of rotundic acid.…”

Section: Biopharmaceutical Profile Of Rotundic Acidmentioning

confidence: 99%

See 2 more Smart Citations

Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

Bhuia,

Chowdhury,

Sonia

et al. 2024

Chemistry & Biodiversity

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“…Moreover, because of its important role in drug metabolism, changes in liver function under pathological states, such as NAFLD, are bound to affect certain enzymes and transporters which are related to the internal metabolism and transportation of drugs. It was reported that RA is a substrate of P-glycoprotein and can be substantially metabolized by Cytochrome P450 (CYP) 3A4 [ 20 ], which explains its relatively low oral bioavailability in rats (16–19%) [ 21 ]. Moreover, our previous study into the pharmacological effect of RA on NAFLD showed that RA had no effect on the oleic acid-induced rat primary hepatocyte in vitro model, but effectively ameliorated non-alcoholic steatohepatitis after oral administration in rats [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

UPLC-QTOF-MS Based Comparison of Rotundic Acid Metabolic Profiles in Normal and NAFLD Rats

Liu

Zou

et al. 2022

Metabolites

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Rotundic acid, the principal bioactive constituent of the herbal remedy “Jiubiying”, has been considered as a candidate compound for treating non-alcoholic fatty liver disease (NAFLD). However, the in vivo and in vitro metabolism of rotundic acid has remained unclear. With the aim of elucidating its metabolic profile, a reliable approach that used ultra-high performance liquid chromatography combined with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS) was applied for screening and identifying rotundic acid in vivo (plasma, feces, urine, and liver tissue of normal and NAFLD model rats) and in vitro (rat liver microsomes) metabolites. Herein, 26 metabolites of rotundic acid were identified, including 22 metabolites in normal rats, 20 metabolites in NAFLD model rats, and eight metabolites in rat liver microsomes. Among them, 17 metabolites were identified for the first time. These data illustrate that the pathological status of NAFLD affects the metabolism of rotundic acid. Furthermore, the major pathways of metabolism included phase Ⅰ (demethylation, desaturation, etc.) and phase Ⅱ (sulfation and glucuronidation) reactions, as well as a combined multiple-step metabolism. This work provides important information on the metabolism of rotundic acid and lays the foundation for its future clinical application.

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Transepithelial transport characteristics of Hydroxysafflor yellow A across cellular monolayers and the effects of the influx and efflux transporters

Tang,

Ye,

Chen

et al. 2023

Food Bioscience

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Influence of verapamil on the pharmacokinetics of rotundic acid in rats and its potential mechanism

Cited by 8 publications

References 35 publications

Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

Efficacy of Rotundic Acid and Its Derivatives as Promising Natural Anticancer Triterpenoids: A Literature‐Based Study

UPLC-QTOF-MS Based Comparison of Rotundic Acid Metabolic Profiles in Normal and NAFLD Rats

Transepithelial transport characteristics of Hydroxysafflor yellow A across cellular monolayers and the effects of the influx and efflux transporters

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