Pharmacokinetics, hepatic disposition, and heart tissue distribution of 14 compounds in rat after oral administration of Qi‐Li‐Qiang‐Xin capsule via ultra‐high‐performance liquid chromatography coupled with triple quadrupole tandem mass spectrometry

Tang, Xiyang; Dai, Zi-qin; Zeng, Jiaxing; Li, Zi‐Ting; Fan, Cai‐lian; Yao, Zhihong; Yao, Xin‐Sheng; Dai, Yi

doi:10.1002/jssc.202101008

Cited by 9 publications

(6 citation statements)

References 37 publications

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“…astragaloside IV, ginsenoside Rb1, periplocymarin, benzoylmesaconine, benzoylhypaconine, and alisol A. 11 A second report that relied on the identification of compounds with bioactivity on isolated cardiomyocytes yielded astragaloside, tanshinone IIA, ginsenoside Re, songorin, calycosin-7-O-β-D-glucopyranoside, hesperidin and alisol A. 12 Similar listings of constituents (including other ginsenosides) have been published by others.…”

Section: Identification Of Active Ingredients Of Qiliqiangxinmentioning

confidence: 90%

“…orientale (Oriental waterplantian), (7) the rhizome of Polygonatum odoratum (Mill.) Druce (solomonseal), (8) the flower of Carthamus tinctorius (L.) (safflower), (9) the root bark of Periploca sepium Bunge (Chinese silkvine), (10) the pericarp of Citrus reticulata Blanco (dried tangerine peel), and (11) the branch of Cinnamomum cassia Perl (cassia twig). These ingredients are combined in capsules that are available for prescription.…”

Section: Formulation and Active Ingredients Of Qiliqiangxinmentioning

confidence: 99%

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Qiliqiangxin: A multifaceted holistic treatment for heart failure or a pharmacological probe for the identification of cardioprotective mechanisms?

Packer

2023

European J of Heart Fail

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The active ingredients in many traditional Chinese medicines are isoprene oligomers with a diterpenoid or triterpenoid structure, which exert cardiovascular effects by signaling through nutrient surplus and nutrient deprivation pathways. Qiliqiangxin (QLQX) is a commercial formulation of 11 different plant ingredients, whose active compounds include astragaloside IV, tanshione IIA, ginsenosides (Rb1, Rg1 and Re) and periplocymarin. In the QUEST Trial, QLQX reduced the combined risk of cardiovascular death or heart failure hospitalization (hazard ratio 0.78 [95% CI 0.68‐0.90]), based on 859 events in 3119 patients over a median of 18.2 months; the benefits were seen in patients taking foundational drugs except for SGLT2 inhibitors. Numerous experimental studies of QLQX in diverse cardiac injuries have yielded highly consistent findings. In marked abrupt cardiac injury, QLQX mitigated cardiac injury by upregulating nutrient surplus signaling through the PI3K/Akt/mTOR/HIF‐1α/NRF2 pathway; the benefits of QLQX were abrogated by suppression of PI3K, Akt, mTOR, HIF‐1α or NRF2. In contrast, in prolonged measured cardiac stress (as in chronic heart failure), QLQX ameliorated oxidative stress, maladaptive hypertrophy, cardiomyocyte apoptosis, and proinflammatory and profibrotic pathways, while enhancing mitochondrial health and promoting glucose and fatty acid oxidation and ATP production. These effects are achieved by an action of QLQX to upregulate nutrient deprivation signaling through SIRT1/AMPK/PGC‐1α and enhanced autophagic flux. In particular, QLQX appears to enhance the interaction of PGC‐1α with PPARα, possibly by direct binding to RXRα; silencing of SIRT1, PGC‐1α and RXRα abrogated the favorable effects of QLQX in the heart. Since PGC‐1α/RXRα is also a downstream effector of Akt/mTOR signaling, the actions of QLQX on PGC‐1α/RXRα may explain its favorable effects in both acute and chronic stress. Intriguingly, the individual ingredients in QLQX — astragaloside IV, ginsenosides, and tanshione IIA — share QLQX's effects on PGC‐1α/RXRα/PPARα signaling. QXQL also contains periplocymarin, a cardiac glycoside that inhibits Na+‐K+‐ATPase. Taken collectively, these observations support a conceptual framework for understanding the mechanism of action for QLQX in heart failure. The high likelihood of overlap in the mechanism of action of QLQX and SGLT2 inhibitors requires additional experimental studies and clinical trials.This article is protected by copyright. All rights reserved.

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Section: Identification Of Active Ingredients Of Qiliqiangxinmentioning

confidence: 90%

Section: Formulation and Active Ingredients Of Qiliqiangxinmentioning

confidence: 99%

Qiliqiangxin: A multifaceted holistic treatment for heart failure or a pharmacological probe for the identification of cardioprotective mechanisms?

Packer

2023

European J of Heart Fail

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“…In recent years, the pharmacokinetics of sinapic acid ( 2 ) from SS in rat plasma has been investigated by a validated UPLC-MS/MS method ( Li et al, 2020 ). The dynamic distribution of sinapine thiocyanate ( 3 ) has been monitored using a validated UPLC-MS/MS method ( Tang et al, 2022 ). The quantitative method validation was established according to the United States Food and Drug Administration (FDA) guidelines ( US Food and Drug Administration, 2018 ).…”

Section: Methodsmentioning

confidence: 99%

Sinapis Semen: A review on phytochemistry, pharmacology, toxicity, analytical methods and pharmacokinetics

2023

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Sinapis Semen (SS), the dried mature seed of Sinapis alba L. and Brassica juncea (L.) Czern. et Coss., is one of the traditional Chinese medicinal materials with a wide range of pharmacological effects being used for asthma, cough and many other ailments. SS is also widely used in food agriculture, medicine and other industries in North America and South Asia. More recently, the research on SS has gradually intensified and increased. However, there is no systematic review of SS. In this review, through literature exploration and analysis, the research advance on phytochemistry, pharmacology, toxicity, analytical methods and pharmacokinetics of SS was aggregated initially. Total 144 compounds have been isolated and identified from SS. Among them, glucosinolates and their hydrolysates and volatile oils are the main active ingredients and important chemical classification markers. SS has a wide range of pharmacological effects, especially in cough suppressing, asthma calming, anti-inflammatory, neuroprotective, cardiovascular protective, inhibiting androgenic effects, anti-tumor, and skin permeation promoting effects. Sinapine and sinapic acid are the main active ingredients of SS for its medicinal effects. However, SS has a strong skin irritation, presumably related to the time of application, the method of processing, and original medicinal plants. This review will provide useful data for the follow-up research and safe and reasonable clinical application of SS.

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“…Therefore, the pharmacokinetic study is an effective method for predicting effective substances and explaining their effective mechanisms. It plays a crucial role in evaluating clinical efficacy, guiding the rational use of traditional Chinese medicines, and promoting their development [3,4]. It has been reported that pathological conditions may affect biomembrane permeability, transporters, and metabolic enzyme activities in vivo, thus causing changes in absorption, distribution, metabolism, and excretion processes [5,6].…”

Section: Introductionmentioning

confidence: 99%

Comparative pharmacokinetic studies of Ephedra herba in common cold and nephrotic syndrome rat models

Cao

Zhou

Liu

et al. 2023

J of Separation Science

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Ephedra herba is a conventional Chinese medicine to treat cold, fever, asthma, edema, and lung diseases in the clinic. At present, most pharmacokinetic studies focus on the pharmacokinetic process of alkaloids in normal animals. However, the non-alkaloid components are also active. In addition, the pharmacokinetic studies under pathological state make more sense for clarifying the material basis of efficacy. In this study, a sensitive and rapid ultra-high-performance-tandem mass spectrometry method was developed and applied to determine nine bioactive components (ephedrine, pseudoephedrine, methylephedrine, (+)-catechin, epicatechin, vitexin, vicenin-2, cinnamic acid, and ferulic acid) in normal, common cold and nephrotic syndrome rats after the oral administration of Ephedra herba. Compared to the normal group, except for ferulic acid, the exposure levels of the other eight components were significantly increased and the plasma clearance clearly declined in common cold rats. Similarly, the exposure levels of seven components other than cinnamic acid and ferulic acid were also significantly augmented and the plasma clearance decreased significantly in nephrotic syndrome rats. In brief, the pathological conditions of the common cold and nephrotic syndrome could lead to alterations in the pharmacokinetics profiles of the nine components, which provide a reference for further exploration of the pharmacodynamics basis of Ephedra herba.

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Pharmacokinetics, hepatic disposition, and heart tissue distribution of 14 compounds in rat after oral administration of Qi‐Li‐Qiang‐Xin capsule via ultra‐high‐performance liquid chromatography coupled with triple quadrupole tandem mass spectrometry

Cited by 9 publications

References 37 publications

Qiliqiangxin: A multifaceted holistic treatment for heart failure or a pharmacological probe for the identification of cardioprotective mechanisms?

Qiliqiangxin: A multifaceted holistic treatment for heart failure or a pharmacological probe for the identification of cardioprotective mechanisms?

Sinapis Semen: A review on phytochemistry, pharmacology, toxicity, analytical methods and pharmacokinetics

Comparative pharmacokinetic studies of Ephedra herba in common cold and nephrotic syndrome rat models

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