Pharmacokinetics and tissue distribution study of tanshinone IIA after oral administration of Bushen Huoxue Qubi granules to rats with blood stasis syndrome

Wang, Yuanqing; Yan, Jian-Ye; Li, Shunxiang; Cai, Xiong; Wang, Wei; Luo, Kun; Huang, Dan; Gao, Jiesheng

doi:10.4103/0973-1296.137369

Cited by 8 publications

(3 citation statements)

References 14 publications

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“…Tanshinone IIA is the main constituent in Bushen Huoxue Qubi (BHQ) granules, a TCM preparation that is used clinically for the treatment of blood stasis syndrome. A pharmacokinetics and tissue distribution study involving rats with acute blood stasis treated with orally administered BHQ has reported significantly higher values for the area under the concentration-time curve (AUC), maximum plasma concentration (C max ), biological half-life (t 1/2 ), lower total body clearance (CL) and apparent volume of distribution (Vd) of tanshinone IIA in plasma and higher AUC 0-t of tanshinone IIA in the analyzed tissues of the BHQ-treated rats, compared with normal rats [ 45 ]. In addition, high density lipoprotein (HDL)-loaded tanshinone IIA markedly improved pharmacokinetic behaviors of tanshinone IIA in vivo [ 46 ].…”

Section: Discussionmentioning

confidence: 99%

Tanshinone IIA inhibits angiogenesis in human endothelial progenitor cells in vitro and in vivo

et al. 2017

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Accumulating evidence reports that bone marrow-derived endothelial progenitor cells (EPCs) regulate angiogenesis, postnatal neovascularization and tumor metastasis. It has been suggested that understanding the molecular targets and pharmacological functions of natural products is important for novel drug discovery. Tanshinone IIA is a major diterpene quinone compound isolated from Danshen (Salvia miltiorrhiza) and is widely used in traditional Chinese medicine (TCM). Evidence indicates that tanshinone IIA modulates angiogenic functions in human umbilical vein endothelial cells. However, the anti-angiogenic activity of tanshinone IIA in human EPCs has not been addressed. Here, we report that tanshinone IIA dramatically suppresses vascular endothelial growth factor (VEGF)-promoted migration and tube formation of human EPCs, without cytotoxic effects. We also show that tanshinone IIA markedly inhibits VEGF-induced angiogenesis in the chick embryo chorioallantoic membrane (CAM) model. Importantly, tanshinone IIA significantly attenuated microvessel formation and the expression of EPC-specific markers in the in vivo Matrigel plug assay in mice. Further, we found that tanshinone IIA inhibits EPC angiogenesis through the PLC, Akt and JNK signaling pathways. Our report is the first to reveal that tanshinone IIA reduces EPC angiogenesis both in vitro and in vivo. Tanshinone IIA is a promising natural product worthy of further development for the treatment of cancer and other angiogenesis-related pathologies.

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Section: Discussionmentioning

confidence: 99%

Tanshinone IIA inhibits angiogenesis in human endothelial progenitor cells in vitro and in vivo

et al. 2017

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“…The day before taking blood, rats except the blank group were hypodermically injected with adrenaline hydrochloride (0.8 mL/kg) twice at an interval of 4 h. Two hours after the first injection of adrenaline hydrochloride, the rats were kept in ice-cold water (0–2°C) to swim for 5 min. [ 7 ]…”

Section: Methodsmentioning

confidence: 99%

Therapeutic effects of Cyathula officinalis Kuan and its active fraction on acute blood stasis rat model and identification constituents by HPLC-QTOF/MS/MS

Cao

Zhao

et al. 2017

Phcog Mag

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Background:Cyathula officinalis Kuan is widely used in the clinics for the treatment of blood stasis in China.Objective:To evaluate the improving blood rheology and anti-inflammatory properties of C. officinalis Kuan extract (CO) and its active fraction (ACO) on acute blood stasis model Wistar rats and characterize the correlative constituents.Materials and Methods:CO at 0.26, 0.53, and 1.04 g/kg and ACO at 0.38, 0.75, and 1.5 g/kg were administered to acute blood stasis model Wistar rats for 3 days. Whole blood viscosity, plasma viscosity, and the levels of interleukin-6 (IL-6), nitric oxide (NO), tumor necrosis factor alpha (TNF-α), and cyclooxygenase-2 (COX-2) in the plasma were measured. HPLC-QTOF/MS/MS method was used to identify the major constituents of ACO; the properties of two representative components (cyasterone and chikusetsusaponin IV) from ACO on thrombin-induced human umbilical vein endothelial cells damage model were also assessed by the levels of thromboxane A2 (TXA2), endothelin (ET), malondialdehyde (MDA), COX-2, endothelial nitric oxide synthase (eNOS), and superoxide dismutase (SOD).Results:CO and ACO significantly reduced whole blood viscosity, plasma viscosity, and levels of IL-6, NO, TNF-α, and COX-2 in vivo. Forty compounds were identified from ACO, mainly as phytoecdysteroids and saponins. Cyasterone and chikusetsusaponin IV could significantly inhibit levels of TXA2, ET, MDA, and COX-2 and promote the activities of eNOS and SOD in vitro.Conclusion:CO and ACO possessed significant improving blood rheology and anti-inflammatory effects on acute blood stasis model rats and the representative components Cyasterone and chikusetsusaponin IV showed significant anti-inflammatory, antioxidant, and anticoagulant effects in vitro.SUMMARY Cyathula officinalis Kuan is widely used in the clinic for the treatment of blood stasis in ChinaThe C. officinalis Kuan extract and the active fraction of C. officinalis Kuan (ACO) possessed significant improving blood rheology and anti-inflammatory effects on acute blood stasis model ratsForty compounds were identified from ACO, mainly as phytoecdysteroids and saponins Abbreviations used: TCM: Traditional Chinese Medicine, CO: Cyathula officinalis Kuan extract, ACO: Active fraction of Cyathula officinalis Kuan, ROS: Reactive oxygen species, IL-6: Interleukin-6, TNF-α: Tumor necrosis factor alpha, NO: Nitric oxide, COX-2: Cyclooxygenase-2, TXA2: Thromboxane A2, ET: Endothelin, MDA: Malondialdehyde, eNOS: Endothelial nitric oxide synthase, SOD: Superoxide dismutase, ESI: Electronic spray ionization, ELISA: Enzyme-linked immunosorbent assay, HUVECs: Human umbilical vein endothelial cells, DMEM: Dulbecco's modified Eagle medium, MMP: Matrix metalloproteinase.

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“…Among them, ligustilide acting as one of the main bioactive compounds in the FSS formula accounted for 2.351 mg/g in content, and it was reported to exert anti-inflammatory and neuroprotective activities ( Wu et al, 2020 ; Mao et al, 2022 ; Wu et al, 2022 ). The essential oil originating from Radix Angelica Sinensis showed analgesic effects and blood circulation improvements by adjusting glycine and arachidonic acid levels ( Wang et al, 2016 ; Li et al, 2017 ; Hua et al, 2019 ). In addition, the volatile oil derived from Chuanxiong Rhizoma also exhibited anti-migraine effects by relieving pain behaviors ( Guo-Jing et al, 2020 ; Yuan et al, 2021 ).…”

Section: Introductionmentioning

confidence: 99%

Potential analgesic effect of Foshousan oil-loaded chitosan-alginate nanoparticles on the treatment of migraine

Chen,

Cheng,

Zeng

et al. 2023

Front. Pharmacol.

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Background: Migraine is a common neurovascular disorder with typical throbbing and unilateral headaches, causing a considerable healthcare burden on the global economy. This research aims to prepare chitosan-alginate (CS-AL) nanoparticles (NPs) containing Foshousan oil (FSSO) and investigate its potential therapeutic effects on the treatment of migraine.Methods: FSSO-loaded CS-AL NPs were prepared by using the single emulsion solvent evaporation method. Lipopolysaccharide (LPS)-stimulated BV-2 cells and nitroglycerin (NTG)-induced migraine mice were further used to explore anti-migraine activities and potential mechanisms of this botanical drug.Results: FSSO-loaded CS-AL NPs (212.1 ± 5.2 nm, 45.1 ± 6.2 mV) had a well-defined spherical shape with prolonged drug release and good storage within 4 weeks. FSSO and FSSO-loaded CS-AL NPs (5, 10, and 15 μg/mL) showed anti-inflammatory activities in LPS-treated BV-2 cells via reducing the levels of pro-inflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6), and nitric oxide (NO), but elevating interleukin-10 (IL-10) expressions. Moreover, FSSO-loaded CS-AL NPs (52 and 104 mg/kg) raised pain thresholds against the hot stimulus and decreased acetic acid-induced writhing frequency and foot-licking duration in NTG-induced migraine mice. Compared with the model group, calcitonin gene-related peptide (CGRP) and NO levels were downregulated, but 5-hydroxytryptamine (5-HT) and endothelin (ET) levels were upregulated along with rebalanced ET/NO ratio, and vasomotor dysfunction was alleviated by promoting cerebral blood flow (CBF) in the FSSO-loaded CS-AL NPs (104 mg/kg) group.Conclusion: FSSO-loaded CS-AL NPs could attenuate migraine via inhibiting neuroinflammation in LPS-stimulated BV-2 cells and regulating vasoactive substances in NTG-induced migraine mice. These findings suggest that the FSS formula may be exploited as new phytotherapy for treating migraine.

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Pharmacokinetics and tissue distribution study of tanshinone IIA after oral administration of Bushen Huoxue Qubi granules to rats with blood stasis syndrome

Cited by 8 publications

References 14 publications

Tanshinone IIA inhibits angiogenesis in human endothelial progenitor cells in vitro and in vivo

Tanshinone IIA inhibits angiogenesis in human endothelial progenitor cells in vitro and in vivo

Therapeutic effects of Cyathula officinalis Kuan and its active fraction on acute blood stasis rat model and identification constituents by HPLC-QTOF/MS/MS

Potential analgesic effect of Foshousan oil-loaded chitosan-alginate nanoparticles on the treatment of migraine

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