Study of pharmaceutical excipient PEG400 alteration of pharmacokinetics and tissue distribution of main flavonoids metabolites of baicalin

2020 ◽  
Vol 16 ◽  
Author(s):  
Ya-nan Zhu ◽  
Shuo Zhang ◽  
Min Zhang ◽  
Xiao-xia Meng ◽  
Peng-jiao Wang ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Tissue Distribution ◽  
High Performance ◽  
Polyethylene Glycol 400 ◽  
Pharmaceutical Excipient ◽  
Protein Expressions ◽  
T Values

: Polyethylene glycol 400 (PEG400), as a good traditional Chinese medicine solvent, diluent and solubilizer, is widely used as a main pharmaceutical excipient in traditional Chinese medicine compound preparations containing active ingredient baicalin. PEG400 could increase the solubility and release of baicalin in vivo, but it was unknown if PEG400 affected the absorption and distribution of baicalin or not. At present, the effects of PEG400 after oral administration of baicalin on the pharmacokinetic characteristics and tissue distribution behaviors of baicalin itself and its main flavonoid metabolites baicalein-6-O-β-glucopyranoside (B6G) and baicalein were investigated by a rapid, efficient and sensitive ultra-high performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) method. Moreover, we respectively studied the effects of PEG400 on the activities and protein expressions of two subtypes UDP-glucuronyltransferase 1 A8/A9 (UGT1A8 and UGT1A9) of UDP-glucuronosyltransferases (UGTs) in vitro and vivo experiments to determine the partial mechanisms by which PEG400 altered the pharmacokinetics and tissue distribution behaviors of the three flavonoid metabolites. The results showed that PEG400 significantly increased the Cmax and AUC0-t values (P<0.05 or P<0.01) of baicalin and B6G while baicalein could not be quantified due to its extremely low concentration (lower the LLOQ) in plasma. Baicalin, B6G and baicalein were mainly distributed in the stomach, small intestine, kidney and liver. PEG400 changed the distribution of three flavonoid metabolites in various tissues and also increased the activities and expressions of UGT1A8 and UGT1A9. In conclusion, PEG400 significantly altered the pharmacokinetic characteristics and tissue distribution behaviors of three flavonoid metabolites. This may partly result from PEG400 upregulation of the activities and expressions of the drug biphasic metabolic enzymes UGT1A8 and UGT1A9, which provided a material basis.

scholarly journals Antimalarial Effect of the Total Glycosides of the Medicinal Plant, Ranunculus japonicus

Pathogens ◽  
2021 ◽  
Vol 10 (5) ◽  
pp. 532
Author(s):  
Hae-Soo Yun ◽  
Sylvatrie-Danne Dinzouna-Boutamba ◽  
Sanghyun Lee ◽  
Zin Moon ◽  
Dongmi Kwak ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Hematological Parameters ◽  
Significant Inhibition ◽  
Ic50 Values ◽  
The Republic

In traditional Chinese medicine, Ranunculus japonicus has been used to treat various diseases, including malaria, and the young stem of R. japonicus is consumed as a food in the Republic of Korea. However, experimental evidence of the antimalarial effect of R. japonicus has not been evaluated. Therefore, the antimalarial activity of the extract of the young stem of R. japonicus was evaluated in vitro using both chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) strains; in vivo activity was evaluated in Plasmodium berghei-infected mice via oral administration followed by a four-day suppressive test focused on biochemical and hematological parameters. Exposure to extracts of R. japonicus resulted in significant inhibition of both chloroquine-sensitive (3D7) and resistant (Dd2) strains of P. falciparum, with IC50 values of 6.29 ± 2.78 and 5.36 ± 4.93 μg/mL, respectively. Administration of R. japonicus also resulted in potent antimalarial activity against P. berghei in infected mice with no associated toxicity; treatment also resulted in improved hepatic, renal, and hematologic parameters. These results demonstrate the antimalarial effects of R. japonicus both in vitro and in vivo with no apparent toxicity.

Phytochemistry and Pharmacology of the Genus Pedicularis Used in Traditional Chinese Medicine

2014 ◽  
Vol 42 (05) ◽  
pp. 1071-1098 ◽  
Author(s):  
Mao-Xing Li ◽  
Xi-Rui He ◽  
Rui Tao ◽  
Xinyuan Cao
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Chemical Constituents ◽  
Iridoid Glycosides ◽  
In Vivo Studies ◽  
Chemical Components ◽  
Wide Range ◽  
Phenylpropanoid Glycosides

In the present review, the literature data on the chemical constituents and biological investigations of the genus Pedicularis are summarized. Some species of Pedicularis have been widely applied in traditional Chinese medicine. A wide range of chemical components including iridoid glycosides, phenylpropanoid glycosides (PhGs), lignans glycosides, flavonoids, alkaloids and other compounds have been isolated and identified from the genus Pedicularis. In vitro and in vivo studies indicated some monomer compounds and extracts from the genus Pedicularis have been found to possess antitumor, hepatoprotective, anti-oxidative, antihaemolysis, antibacterial activity, fatigue relief of skeletal muscle, nootropic effect and other activities.

scholarly journals Evaluation of the anti-cancer activity of the triterpenoidal saponin fraction isolated from the traditional Chinese medicine Conyza blinii H. Lév.

RSC Advances ◽  
2017 ◽  
Vol 7 (6) ◽  
pp. 3408-3412 ◽  
Author(s):  
Long Ma ◽  
Haiyan Liu ◽  
Lingpei Meng ◽  
Ping Qin ◽  
Botao Zhang ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Anti Cancer ◽  
Saponin Fraction ◽  
Cancer Activity

Triterpenoidal saponins fraction isolated from a traditional Chinese medicine Conyza blinii H. Lév. demonstrates anti-cancer activity both in vitro and in vivo.

scholarly journals The Anti-Neuroinflammatory Effect of Fuzi and Ganjiang Extraction on LPS-Induced BV2 Microglia and Its Intervention Function on Depression-Like Behavior of Cancer-Related Fatigue Model Mice

2021 ◽  
Vol 12 ◽  
Author(s):  
Songwei Yang ◽  
Yantao Yang ◽  
Cong Chen ◽  
Huiqin Wang ◽  
Qidi Ai ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Inflammatory Mediators ◽  
Critical Role ◽  
Chinese Herb ◽  
Experimental Studies ◽  
Research Results ◽  
Cancer Related Fatigue

The Chinese herb couple Fuzi and Ganjiang (FG) has been a classic combination of traditional Chinese medicine that is commonly used clinically in China for nearly 2000 years. Traditional Chinese medicine suggests that FG can treat various ailments, including heart failure, fatigue, gastrointestinal upset, and depression. Neuroinflammation is one of the main pathogenesis of many neurodegenerative diseases in which microglia cells play a critical role in the occurrence and development of neuroinflammation. FG has been clinically proven to have an efficient therapeutic effect on depression and other neurological disorders, but its mechanism remains unknown. Cancer-related fatigue (CRF) is a serious threat to the quality of life of cancer patients and is characterized by both physical and psychological fatigue. Recent studies have found that neuroinflammation is a key inducement leading to the occurrence and development of CRF. Traditional Chinese medicine theory believes that extreme fatigue and depressive symptoms of CRF are related to Yang deficiency, and the application of Yang tonic drugs such as Fuzi and Ganjiang can relieve CRF symptoms, but the underlying mechanisms remain unknown. In order to define whether FG can inhibit CRF depression-like behavior by suppressing neuroinflammation, we conducted a series of experimental studies in vitro and in vivo. According to the UPLC-Q-TOF/MSE results, we speculated that there were 49 compounds in the FG extraction, among which 30 compounds were derived from Fuzi and 19 compounds were derived from Ganjiang. Our research data showed that FG can effectively reduce the production of pro-inflammatory mediators IL-6, TNF-α, ROS, NO, and PGE2 and suppress the expression of iNOS and COX2, which were related to the inhibition of NF-κB/activation of Nrf2/HO-1 signaling pathways. In addition, our research results revealed that FG can improve the depression-like behavior performance of CRF model mice in the tail suspension test, open field test, elevated plus maze test, and forced swimming test, which were associated with the inhibition of the expression of inflammatory mediators iNOS and COX2 in the prefrontal cortex and hippocampus of CRF model mice. Those research results suggested that FG has a satisfactory effect on depression-like behavior of CRF, which was related to the inhibition of neuroinflammation.

Flavonoid constituents of Amomum tsao-ko Crevost et Lemarie and its antioxidant, antidiabetic effects in diabetic rats–in vitro and in vivo studies

2021 ◽  
Author(s):  
Xiaofeng Zhang ◽  
Yujun Tang ◽  
Xiaoxian Guan ◽  
Xin Lu ◽  
Jiao Li ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Diabetic Rats ◽  
In Vivo Studies ◽  
Antidiabetic Effects

Amomum tsao-ko Crevost et Lemarie (A. tsao-ko) is a well-known dietary spice and traditional Chinese medicine. This study aimed to identify the flavonoids in A. tsao-ko and evaluate its antioxidant...

Excavating Anticonvulsant Compounds from Prescriptions of Traditional Chinese Medicine in the Treatment of Epilepsy

2018 ◽  
Vol 46 (04) ◽  
pp. 707-737 ◽  
Author(s):  
Zefeng Zhao ◽  
Xirui He ◽  
Cuixia Ma ◽  
Shaoping Wu ◽  
Ye Cuan ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Therapeutic Strategy ◽  
In Vitro Models ◽  
New Drugs ◽  
Treatment Of Epilepsy ◽  
Effective Therapeutic Strategy ◽  
Promising Source

Traditional Chinese medicine (TCM) has a long history and been widely used in prevention and treatment of epilepsy in China. This paper is intended to review the advances in the active anticonvulsant compounds isolated from herbs in the prescription of TCM in the treatment of epilepsy. These compounds were introduced with the details including classification, CAS number specific structure and druggability data. Meanwhile, much of the research in these compounds in the last two decades has shown that they exhibited favorable pharmacological properties in treatment of epilepsy both in in vivo and in vitro models. In addition, in this present review, the evaluation of the effects of the anticonvulsant classical TCM prescriptions is discussed. According to these rewarding pharmacological effects and chemical substances, the prescription of TCM herbs could be an effective therapeutic strategy for epilepsy patients, and also could be a promising source for the development of new drugs.

scholarly journals Preparation, Characterization, and Dissolution RateIn VitroEvaluation of TotalPanaxNotoginsenoside Nanoparticles, Typical Multicomponent Extracts from Traditional Chinese Medicine, Using Supercritical Antisolvent Process

2015 ◽  
Vol 2015 ◽  
pp. 1-12 ◽  
Author(s):  
Ying Zhang ◽  
Xiuhua Zhao ◽  
Wengang Li ◽  
Yuangang Zu ◽  
Yong Li ◽  
...  
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
High Performance ◽  
Solution Concentration ◽  
Solution Flow Rate ◽  
Optimum Conditions ◽  
Solution Flow ◽  
Supercritical Antisolvent ◽  
Differential Scanning Calorimeters

TotalPanaxnotoginsenosides nanoparticles, typical multicomponent extracts from traditional Chinese medicine, were prepared with a supercritical antisolvent (SAS) process using ethanol as solvent and carbon dioxide as antisolvent. The optimum conditions were determined to be as follows: TPNS solution concentration of 2.5 mg/mL, TPNS solution flow rate of 6.6 mL/min, precipitation temperature of 40°C, and precipitation pressure of 20 MPa. Under the optimum conditions, TPNS nanoparticles with a MPS of 141.5 ± 18.2 nm and total saponins amounts (TSA) of 78.9% were obtained. The TPNS nanoparticles obtained were characterized by scanning electron microscopy (SEM), dynamic light scattering (DLS), Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimeters (DSC), and high performance liquid chromatography (HPLC). The results showed that the chemical and crystal structure of the obtained TPNS nanoparticles has not changed. Dissolutionin vitrostudies showed that the solubility and dissolution rate of notoginsenosides R1 and ginsenoside Rb1 in TPNS nanoparticles are higher than these in raw TPNS, with no obvious difference in Rg1. These results suggest that TPNS nanoparticles can be helpful to the improvement of its bioavailability for the treatment of cardiovascular diseases.

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