Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Li, Gangmin; Chen, Jun-Ren; Zhang, Huiqiong; Cao, Xiaoyu; Sun, Chen; Peng, Fu; Yin, Yongguang; Lin, Ziwei; Yu, Long-Chuan; Chen, Yan; Yun-li, Tang; Xie, Xing; Peng, Cheng

doi:10.1155/2021/4582412

Cited by 23 publications

(26 citation statements)

References 84 publications

(85 reference statements)

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“…Physcion has a moderate intestinal permeability with P eff values of (3.32 ± 1.50) × 10 –3 (2.30 ± 1.57) × 10 –3 (2.40 ± 0.58) × 10 –3 , and (7.45 ± 3.30) × 10 –3 cm/min in the duodenum, jejunum, ileum, and colon, respectively ( Wang P. et al, 2011 ). Rhein is mostly administered orally due to its low solubility, although achieving a stable and effective blood concentration is difficult ( Li et al, 2021 ). The components detected in the plasma gradually increased as the dose increased.…”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetics, Tissue Distribution, and Excretion Characteristics of a Radix Polygoni Multiflori Extract in Rats

Cheng

Yuan

et al. 2022

Front. Pharmacol.

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Although progress has been achieved in the pharmacological activity and toxicity of Radix Polygoni Multiflori (RPM), the chemical basis of its toxicity is still unclear. Here, we performed a multicompound pharmacokinetic analysis and investigated the tissue distribution and excretion characteristics of RPM components after oral administration in rats. The findings demonstrated that the active ingredients of the RPM extract were quickly absorbed after oral administration, with high exposure levels of emodin, 2,3,5,4′-teterahydroxystilbene-2-O-β-D-glucoside (TSG), citreorosein, torachrysone-8-O-glucoside (TG), emodin-8-O-β-D-glucoside (EG), and physcion-8-O-β-D-glucoside (PG). The tissue distributions of emodin, TSG, TG, EG, and PG were high in the liver and kidney. These components were the key contributors to the effectiveness and toxicity of RPM on the liver and kidney. Most of the active ingredients were mainly excreted through feces and bile, while a few were converted into other products in the body and excreted through urine and feces.

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Section: Resultsmentioning

confidence: 99%

Pharmacokinetics, Tissue Distribution, and Excretion Characteristics of a Radix Polygoni Multiflori Extract in Rats

Cheng

Yuan

et al. 2022

Front. Pharmacol.

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“…There is little doubt that rhein can reversibly bind to FTO and inhibit m 6 A demethylation in vitro [817]; however, rhein is not a selective inhibitor of m 6 A "erasers" that include the ALKB family proteins [818]. Furthermore, rhein is a natural product with an impressive array of pharmacological activities [819], including antiviral mechanisms. Rhein can significantly inhibit IAV adsorption and replication via antioxidant-dependent pathways in vitro [820].…”

Section: Is M 6 a A Positive Or Negative Regulator Of Sars-cov-2 Repl...mentioning

confidence: 99%

Melatonin: Regulation of Viral Phase Separation and Epitranscriptomics in Post-Acute Sequelae of COVID-19

Loh¹,

Reíter

2022

IJMS

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The relentless, protracted evolution of the SARS-CoV-2 virus imposes tremendous pressure on herd immunity and demands versatile adaptations by the human host genome to counter transcriptomic and epitranscriptomic alterations associated with a wide range of short- and long-term manifestations during acute infection and post-acute recovery, respectively. To promote viral replication during active infection and viral persistence, the SARS-CoV-2 envelope protein regulates host cell microenvironment including pH and ion concentrations to maintain a high oxidative environment that supports template switching, causing extensive mitochondrial damage and activation of pro-inflammatory cytokine signaling cascades. Oxidative stress and mitochondrial distress induce dynamic changes to both the host and viral RNA m6A methylome, and can trigger the derepression of long interspersed nuclear element 1 (LINE1), resulting in global hypomethylation, epigenetic changes, and genomic instability. The timely application of melatonin during early infection enhances host innate antiviral immune responses by preventing the formation of “viral factories” by nucleocapsid liquid-liquid phase separation that effectively blockades viral genome transcription and packaging, the disassembly of stress granules, and the sequestration of DEAD-box RNA helicases, including DDX3X, vital to immune signaling. Melatonin prevents membrane depolarization and protects cristae morphology to suppress glycolysis via antioxidant-dependent and -independent mechanisms. By restraining the derepression of LINE1 via multifaceted strategies, and maintaining the balance in m6A RNA modifications, melatonin could be the quintessential ancient molecule that significantly influences the outcome of the constant struggle between virus and host to gain transcriptomic and epitranscriptomic dominance over the host genome during acute infection and PASC.

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“…have extensive protective effects on various targets of renal fibrosis, there are also certain limitations. For example, some natural ingredients have poor solubility, low bioavailability, poor intestinal absorption, strong dose dependence when intervening in some targets, hepatotoxicity and nephrotoxicity ( Dong et al, 2016 ; Xie et al, 2019 ; Dong et al, 2020 ; Li et al, 2021 ). Most of the above conclusions are based on animal experiments, and there is a lack of their use in clinical practice.…”

Section: Discussion and Outlookmentioning

confidence: 99%

“…Modern pharmacological studies have found that rhein has anti-inflammatory, antitumor and antifibrotic effects and has certain protective effects in the liver and kidneys. The molecular schematic diagram of rhein is shown in Figure 4 ( Sun H. et al, 2016 ; Li et al, 2021 ). Chrysophanol is derived from Polygonaceae plants.…”

Section: Modern Pharmacological Studies Of Natural Components In ...mentioning

confidence: 99%

The progress and prospect of natural components in rhubarb (Rheum ribes L.) in the treatment of renal fibrosis

Wang

Yu²,

Li³

et al. 2022

Front. Pharmacol.

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Background: Renal fibrosis is a key pathological change that occurs in the progression of almost all chronic kidney diseases . CKD has the characteristics of high morbidity and mortality. Its prevalence is increasing each year on a global scale, which seriously affects people’s health and quality of life. Natural products have been used for new drug development and disease treatment for many years. The abundant natural products in R. ribes L. can intervene in the process of renal fibrosis in different ways and have considerable therapeutic prospects.Purpose: The etiology and pathology of renal fibrosis were analyzed, and the different ways in which the natural components of R. ribes L. can intervene and provide curative effects on the process of renal fibrosis were summarized. Methods: Electronic databases, such as PubMed, Life Science, MEDLINE, and Web of Science, were searched using the keywords ‘R. ribes L.’, ‘kidney fibrosis’, ‘emodin’ and ‘rhein’, and the various ways in which the natural ingredients protect against renal fibrosis were collected and sorted out.Results: We analyzed several factors that play a leading role in the pathogenesis of renal fibrosis, such as the mechanism of the TGF-β/Smad and Wnt/β-catenin signaling pathways. Additionally, we reviewed the progress of the treatment of renal fibrosis with natural components in R. ribes L. and the intervention mechanism of the crucial therapeutic targets.Conclusion: The natural components of R. ribes L. have a wide range of intervention effects on renal fibrosis targets, which provides new ideas for the development of new anti-kidney fibrosis drugs.

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Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Cited by 23 publications

References 84 publications

Pharmacokinetics, Tissue Distribution, and Excretion Characteristics of a Radix Polygoni Multiflori Extract in Rats

Pharmacokinetics, Tissue Distribution, and Excretion Characteristics of a Radix Polygoni Multiflori Extract in Rats

Melatonin: Regulation of Viral Phase Separation and Epitranscriptomics in Post-Acute Sequelae of COVID-19

The progress and prospect of natural components in rhubarb (Rheum ribes L.) in the treatment of renal fibrosis

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