Icariin and its metabolites as potential protective phytochemicals against cardiovascular disease: From effects to molecular mechanisms

Zeng, Yufei; Xiong, Yilin; Yang, Tao; Wang, Yan; Zeng, Jinshan; Zhou, Shaoyu; Luo, Yunbai; Liu, Lisheng

doi:10.1016/j.biopha.2022.112642

Cited by 36 publications

(25 citation statements)

References 93 publications

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“…Cardiovascular disease (CVD) is the leading cause of morbidity and mortality around the world ( Zeng et al, 2022 ). Cardiac arrhythmias are the abnormalities of heartbeat.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Herb–Drug Interaction Between Danshen and Rivaroxaban in Rat and Human Liver Microsomes

Wang

Zhang

et al. 2022

Front. Pharmacol.

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The combination of Salvia miltiorrhiza (Danshen) and rivaroxaban is a promising treatment option in clinical practice in China, but the herb–drug interaction between Danshen and rivaroxaban remains unclear. Therefore, this study aims to reveal the interaction between Danshen and rivaroxaban. We not only investigated the inhibitory properties of Danshen tablet on rivaroxaban metabolism in rat and human liver microsomes but also evaluated the inhibitory effects of Danshen tablet and its eight active components (dihydrotanshinone I, tanshinone I, tanshinone IIA, cryptotanshinone, danshensu, salvianolic acid A, salvianolic acid B, and salvianolic acid C) on cytochrome P450 (CYP) enzymes. The results showed that Danshen tablet potently inhibited the metabolism of rivaroxaban in rat and human liver microsomes. In the CYP inhibition study, we found that dihydrotanshinone I, the active component of Danshen tablet, potently inhibited the activities of rat CYP3A and CYP2J, with IC50 values at 13.85 and 6.39 μM, respectively. In further inhibition kinetic study, we found that Danshen tablet is a mixed inhibitor in rivaroxaban metabolism in rat and human liver microsomes, with the Ki value at 0.72 and 0.25 mg/ml, respectively. In conclusion, there is a potential interaction between Danshen tablet and rivaroxaban. Danshen tablet inhibits the metabolism of rivaroxaban, which may be because its lipid-soluble components such as dihydrotanshinone I strongly inhibit the activities of CYP enzymes, especially CYP3A and CYP2J. Therefore, when Danshen tablet and rivaroxaban are used simultaneously in the clinic, it is necessary to strengthen the drug monitoring of rivaroxaban and adjust the dosage.

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“…Cardiovascular disease (CVD) is the leading cause of morbidity and mortality around the world ( Zeng et al, 2022 ). Cardiac arrhythmias are the abnormalities of heartbeat.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Herb–Drug Interaction Between Danshen and Rivaroxaban in Rat and Human Liver Microsomes

Wang

Zhang

et al. 2022

Front. Pharmacol.

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“…It is noteworthy that the potential inhibitors (TCM1-TCM6) screened from the TCM database were mostly phenolic phyto-chemicals ( polyphenols). Phytochemicals are known to exert therapeutic effects on cancers, 84-87 cardiovascular diseases, [88][89][90][91] hypertension, 92 and diabetes. [93][94][95][96] Especially, flavonoids consist of various subclasses and present great potential as therapeutics that can reduce the risk of chronic diseases.…”

Section: Food and Function Papermentioning

confidence: 99%

Pharmacophore-driven identification of human glutaminyl cyclase inhibitors from foods, plants and herbs unveils the bioactive property and potential of Azaleatin in the treatment of Alzheimer's disease

et al. 2022

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“…Icariin (ICA), the main active ingredient in Epimedium genus plants, has a wide range of pharmacological activities [174][175][176]. Studies have shown that ICA inhibits NF-κB activation after IS by upregulating the PPARs/Nrf2 pathway and downregulating the JAK2/STAT3 pathway, thereby enhancing mild hypothermia-induced neuroprotection [127].…”

Section: Flavonolsmentioning

confidence: 99%

Polyphenols for the Treatment of Ischemic Stroke: New Applications and Insights

et al. 2022

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Ischemic stroke (IS) is a leading cause of death and disability worldwide. Currently, the main therapeutic strategy involves the use of intravenous thrombolysis to restore cerebral blood flow to prevent the transition of the penumbra to the infarct core. However, due to various limitations and complications, including the narrow time window in which this approach is effective, less than 10% of patients benefit from such therapy. Thus, there is an urgent need for alternative therapeutic strategies, with neuroprotection against the ischemic cascade response after IS being one of the most promising options. In the past few decades, polyphenolic compounds have shown great potential in animal models of IS because of their high biocompatibility and ability to target multiple ischemic cascade signaling pathways, although low bioavailability is an issue that limits the applications of several polyphenols. Here, we review the pathophysiological changes following cerebral ischemia and summarize the research progress regarding the applications of polyphenolic compounds in the treatment of IS over the past 5 years. Furthermore, we discuss several potential strategies for improving the bioavailability of polyphenolic compounds as well as some essential issues that remain to be addressed for the translation of the related therapies to the clinic.

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Icariin and its metabolites as potential protective phytochemicals against cardiovascular disease: From effects to molecular mechanisms

Cited by 36 publications

References 93 publications

Evaluation of Herb–Drug Interaction Between Danshen and Rivaroxaban in Rat and Human Liver Microsomes

Evaluation of Herb–Drug Interaction Between Danshen and Rivaroxaban in Rat and Human Liver Microsomes

Pharmacophore-driven identification of human glutaminyl cyclase inhibitors from foods, plants and herbs unveils the bioactive property and potential of Azaleatin in the treatment of Alzheimer's disease

Polyphenols for the Treatment of Ischemic Stroke: New Applications and Insights

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