A review: Pharmacology and pharmacokinetics of Schisandrin A

Fu, Ke; Zhou, Honglin; Wang, Cheng; Gong, Lihong; Ma, Cheng; Zhang, Yafang; Li, Yunxia

doi:10.1002/ptr.7456

Cited by 25 publications

(17 citation statements)

References 140 publications

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“…In addition, SA displayed a mixed‐type (noncompetitive and competitive) inhibitory activity against CYP3A in RLMs. 27 Correspondingly, our in vitro data revealed that both SA and SB caused pharmacokinetic changes of poziotinib, and SB showed a stronger inhibitory activity on poziotinib with IC 50 values of 2.55 μM for M1 and 6.97 μM for M2, which exhibited the same results in animal studies. Furthermore, we supported that SA mainly inhibited poziotinib metabolism by inhibiting the enzymatic activity of CYP2D6, whereas SB mainly by inhibiting CYP3A4 in RLMs.…”

Section: Discussionsupporting

confidence: 72%

Inhibitory effect of Schisandrin on the pharmacokinetics of poziotinib in vivo and in vitro by UPLC‐MS/MS

et al. 2023

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Background As a pan‐HER tyrosine kinase inhibitor with a promising application prospect, poziotinib is likely to be coadministered with Schisandrins in clinical treatment due to its anticancer activities. Methods Eighteen Sprague–Dawley rats were randomly divided into three groups: Schisandrin A group and Schisandrin B group (20 mg/kg daily for 1 week), and control group (vehicle). On day 8, poziotinib (2 mg/kg) was administered by oral gavage 30 min later. An in vitro study was developed to identify the possible mechanisms of Schisandrins on poziotinib metabolism. All analytes were detected by UPLC/MS–MS, and molecular docking was performed by AutoDock Tools. Results When rats were preadministered with Schisandrin A, AUC (0−∞) and Cmax of poziotinib were obviously increased by 0.79‐ and 1.17‐fold, whereas the Vz/F and CLz/F values were dramatically decreased. The results in Schisandrin B group presented similarly. Both Schisandrin A and Schisandrin B were mixed inhibitors of poziotinib in RLMs, and Schisandrin B showed stronger inhibitory activity with IC 50 values of 2.55 μM for M1 and 6.97 μM for M2. Molecular docking analysis demonstrated that Schisandrin A and Schisandrin B exhibited a strong binding ability towards CYP2D6 as compared to CYP3A4. Conclusion All results provided the direct evidence of the pharmacokinetic drug–drug interactions (DDIs) between Schisandrin and poziotinib. Thus, particular attention should be paid when poziotinib is taken together with Schisandrins in clinical practice.

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Section: Discussionsupporting

confidence: 72%

Inhibitory effect of Schisandrin on the pharmacokinetics of poziotinib in vivo and in vitro by UPLC‐MS/MS

et al. 2023

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“…Various studies indicate that both S. chinensis berry preparations and their bioactive individual compounds, especially lignans and polysaccharides, appear to have cardioprotective potential; however, many of these works are limited to in vitro models. Nevertheless, the available literature indicates both to have anti-inflammatory, antioxidant, and anti-obesity potential [ 11 , 52 ]. For example, more details about the pharmacology and pharmacokinetics of bioactive compounds, including schisandrin A isolated from S. chinensis berries are described by Fu et al [ 11 ] and Yang et al [ 52 ].…”

Section: Discussionmentioning

confidence: 99%

“…Nevertheless, the available literature indicates both to have anti-inflammatory, antioxidant, and anti-obesity potential [ 11 , 52 ]. For example, more details about the pharmacology and pharmacokinetics of bioactive compounds, including schisandrin A isolated from S. chinensis berries are described by Fu et al [ 11 ] and Yang et al [ 52 ]. In addition, various lignans from S. chinensis berries have been found to demonstrate cardioprotective potential and these are summarized in Figure 2 , together with their mechanisms.…”

Section: Discussionmentioning

confidence: 99%

“…Various in vitro and in vivo studies have found them to demonstrate various antioxidative, anti-inflammatory, anticancer, and antiviral properties, among others. For example, S. chinensis has an inhibitory effect on cytochrome P450, family 3, subfamily A (CYP3A), and P-glycoprotein (P-gp), which can mediate metabolism or efflux of substrates, and may interact with many drugs [ 5 , 6 , 7 , 8 , 9 , 10 , 11 , 12 ]. In addition, Nasser et al [ 9 ] described various biological properties of schisandrin B.…”

Section: Introductionmentioning

confidence: 99%

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Cardioprotective Potential of Berries of Schisandra chinensis Turcz. (Baill.), Their Components and Food Products

Olas

2023

Nutrients

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Schisandra chinensis (S. chinensis) berries, originally a component of traditional herbal medicine in China, Korea, and other east Asian countries, are also valuable agents in modern phototherapy. S. chinensis berry preparations, including extracts and their chemical components, demonstrate anti-cancer, hepatoprotective, anti-inflammatory, and antioxidant properties, among others. These valuable properties, and their therapeutic potential, are conditioned by the unique chemical composition of S. chinensis berries, particularly their lignan content. About 40 of these compounds, mainly dibenzocyclooctane type, were isolated from S. chinensis. The most important bioactive lignans are schisandrin (also denoted as schizandrin or schisandrol A), schisandrin B, schisantherin A, schisantherin B, schisanhenol, deoxyschisandrin, and gomisin A. The present work reviews newly-available literature concerning the cardioprotective potential of S. chinensis berries and their individual components. It places special emphasis on the cardioprotective properties of the selected lignans related to their antioxidant and anti-inflammatory characteristis.

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“…Traditional Chinese medicine (TCM) has unique advantages in the clinical treatment of liver injury due to its characteristics of multitarget and multiapproach ( Fu et al, 2021 ). The pharmacokinetic study of TCM is helpful to elucidate the in vivo process characteristics of the active ingredients of TCM and clarify the pharmacodynamic material basis of them ( Fu et al, 2022 ). The liver is the crucial detoxifying organ, responsible for the body’s metabolism of foreign substances, including drugs.…”

Section: Introductionmentioning

confidence: 99%

Comparative Pharmacokinetics of Three Bioactive Diterpenoids of Rabdosia serra Extract in Normal and Con A-Induced Liver Injury Rats Using UPLC-MS/MS

et al. 2022

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Rabdosia serra (Maxim.) Hara (R. serra), one of the source plants of “Xihuangcao”, has been widely used as a Chinese folk herb with the concomitant function of both medicine and foodstuff for the prevention and treatment of liver disease. Diterpenoids were considered as the major bioactive components in R. serra, responsible for their effect on hepatoprotection in previous phytochemical and pharmacological studies, while few comparative pharmacokinetic studies have been conducted under the physiological and pathological conditions. To reveal the difference in the pharmacokinetics process of R. serra extract (RSE) in normal and Con A-induced liver injury rats, a rapid ultra-high-pressure liquid chromatography–tandem mass spectrometry method (total running time: 5 min) was established to simultaneously determine three bioactive diterpenoids (enmein, epinodosin, and isodocarpin) in rat plasma. The results showed significant differences in the pharmacokinetic properties of three analytes between the physiological and pathological states. Compared with normal rats, the AUC of the three analytes was remarkably higher in liver injury rats, while the Tmax, T1/2, and MRT were shortened. It indicated that RSE has higher exposure and quicker elimination in liver injury rats than that in normal rats. Our results suggested that the pharmacokinetics of hepatoprotective medications was affected by liver injury, which prospected to provide essential information for guiding the healthcare and clinical application of R. serra in pathological states.

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A review: Pharmacology and pharmacokinetics of Schisandrin A

Cited by 25 publications

References 140 publications

Inhibitory effect of Schisandrin on the pharmacokinetics of poziotinib in vivo and in vitro by UPLC‐MS/MS

Inhibitory effect of Schisandrin on the pharmacokinetics of poziotinib in vivo and in vitro by UPLC‐MS/MS

Cardioprotective Potential of Berries of Schisandra chinensis Turcz. (Baill.), Their Components and Food Products

Comparative Pharmacokinetics of Three Bioactive Diterpenoids of Rabdosia serra Extract in Normal and Con A-Induced Liver Injury Rats Using UPLC-MS/MS

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