ABSTRACT
Tenuifolin， a main component in Polygalae Radix， is frequently used as an important indicator for quality control of Polygalae Radix and its processed products. Dementia is a serious and persistent cognitive disorder， and the number of dementia patients is increasing worldwide， which brings great economic burden and mental pressure to families and society. At present， cholinesterase inhibitor and other drugs can only alleviate the symptoms of dementia， and there are some toxic and side effects. It has been found that tenuifolin can significantly improve cognitive disorder， learning and memory and is expected to be a potential drug for treating dementia. Tenuifolin exerts protective effects on amyloid-β （Aβ） deposition， acetylcholine reduction， neuroinflammation， cellular oxidative damage and nerve cell apoptosis caused by neurodegenerative diseases via multiple mechanisms， and can be applied to various types of dementia. In addition， it can be quickly absorbed into the blood， mainly distributed in liver and kidney， and can enter into the brain through the blood-brain barrier. However， because of its large molecular mass and poor fat solubility， tenuifolin can be rapidly eliminated， generating some problems such as low oral absoBrbability and permeability of blood-brain barrier. Therefore， the information of chemistry， pharmacology， pharmacokinetics and toxicology of tenuifolin was summarized in this paper to provide reference and ideas for further research and application.
ABSTRACT
OBJECTIVE：To investig ate the effects of tenuifolin （TEN）on brain mitochondrial autophagy in Aizheimer ’s disease（AD）model mice. METHODS ：Totally 50 male APP/PS1 double transgenic mice were randomly divided into model group，TEN medium-dose+ 3-MA group [TEN 40 mg/（kg·d）+autophagy inhibitor 3-MA 30 mg/（kg·d）] and TEN low-dose ， medium-dose and high-dose groups [ 20，40，80 mg/（kg·d）]，with 10 mice in each group. In addition ，10 wild-type homologous mice were included in normal control group. Administration groups were intragastrically given corresponding drug solution ；normal control group and model group were intragastrically given 0.3％ sodium carboxymethyl cellulose solution ，once a day ，0.01 mL/g， for consecutive 3 months. After last administration ，positive expression [measured by integrated optical density （IOD）] of microtubule associated protein 1 light chain 3（LC3）in neuron was detected ；mRNA expressions of LC3，ubiquitin-binding protein p62，Cathepsin D ，Rab7，phosphatase and tensin homolog deleted on chromosome ten gene-induced putative kinase 1（PINK1） and E 3 ligase（Parkin）as well as protein expressions of LC 3，p62，PINK1 and Parkin were detected in brain mitochondria. RESULTS：Compared with normal control group ，IOD value of LC 3 in neuron as well as mRNA and protein expressions of LC 3， p62，PINK1 and Parkin in brain mitochondria were all increased significantly in model group （P＜0.05 or P＜0.01），while mRNA expressions of Cathepsin D and Rab 7 were decreased significantly （P＜0.05 or P＜0.01）. Compared wit h model group ，IOD values of LC 3（except for TEN low-dose and medium-dose groups ） in neuron ，mRNA expressions of LC 3，Cathepsin D ，Rab7， PINK1（except for TEN low-dose group ）and Parkin （except for TEN low-dose group ） in brain mitochondria as well as protein expressions of LC 3 （except for TEN medium-dose group），PINK1（except fo r TEN high-dose group decreased significantly）and Parkin （except for TEN low-dose group decreased significantly ）were increased significantly in TEN low-dose ， medium-dose and high-dose groups （P＜0.05 or P＜0.01）；mRNA（except for TEN low-dose group ）and protein expressions of p62 were decreased significantly （P＜0.05 or P＜0.01）. Compared with TEN medium-dose group ，the changes of above indexes were inhibited significantly in TEN medium-dose + 3-MA group （P＜0.05 or P＜0.01）. CONCLUSIONS ：TEN can induce mitophagy in brain tissue of AD model mice by activating PINK 1/Parkin signaling pathway and improve lysosome function.
ABSTRACT
Objective: The contents of five main components in Polygala tenuifolia from different habitats were determined, which provided certain data support and theoretical basis for the quality evaluation system of P. tenuifolia. Methods: The contents of polygalaxanthone III, 3,6’-disinapoyl sucrose, polygalacic acid, senegenin and tenuifolin of roots from different wild samples were determined by HPLC. Then SPSS 20.0 and SIMCA 11.5 were used for difference analysis, correlation analysis, hierarchical cluster analysis (HCA), and principal component analysis (PCA). Results: The content of the five main components in wild P. tenuifolia samples from different habitats was significantly different. The 20 samples were placed into two clusters (I, II) by HCA and PCA. Cluster I comprised three samples with higher content of 3,6’-disinapoyl sucrose, polygalaxanthone III, senegenin and tenuifolin from Weinan, Xianyang in Shannxi Province, and Xinjiang in Shanxi Province, whereas cluster II contained the other 17 samples. Conclusion: The results showed that the main components of P. enuifolia from Weinan, Xianyang in Shannxi Province and Xinjiang in Shanxi Province were significantly higher than other origins, and which provided a reference for the quality control, selection of excellent germplasm and cultivation bases of P. tenuifolia.
ABSTRACT
To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.
Subject(s)
Anisoles , Biological Availability , Diterpenes, Kaurane , Drug Delivery Systems , Emulsions , Particle Size , Solubility , Surface-Active AgentsABSTRACT
Objective To investigate the effects of different drying methods on composition and content of five active constituents in root bark and root of Polgala tenuifoliaroot. Methods The contents of polygalaxanthone III, 3,6’-disinapoyl sucrose, polygalacic acid, senegenin, and tenuifolin in root bark and root from different drying samples were determined by HPLC. Then the data analysis was performed by ANOVA and TOPSIS methods. Results There is a difference in the order of drying methods for bark and root of P. tenuifoliaroot. For P. tenuifoliaroot root bark, the order of different drying methods was microwave drying > 60 ℃ hot-air drying > 50 ℃ hot-air drying > 70 ℃ hot-air drying > freeze-drying > 40 ℃ hot-air drying > shade drying > sun drying; For P. tenuifolia root, the different drying methods were sorted by microwave drying > 60 ℃ hot-air drying > shade drying > sun drying > 50 ℃ hot-air drying > 40 ℃ hot-air drying > 70 ℃ hot-air drying > freeze-drying. Conclusion Combined with the production practice, this study suggests that microwave drying and hot-air drying at 60 ℃ are suitable drying methods for P. tenuifoliaroot bark and root, providing a basis for the determination of drying methods for the origin processing of P. tenuifolia.
ABSTRACT
Objective To establish the main component analysis method of commodity grade Polygala tenuifolia, and to explore the correlation between the grade character of P. tenuifolia and the main chemistry. Methods P. tenuifolia of four markets were determined by high performance liquid chromatography (HPLC) to analyze the different level of medicine and explore the correlation between commodity grade and composition for P. tenuifolia. Results The main components determination of P. tenuifolia in different market grades were not completely consistent with the grade of commodity. Conclusion There are certain limitations of the commodity grading standards for P. tenuifolia in the medicinal materials market. It is necessary to establish a new grade quality standard for accurately evaluating the quality of P. tenuifolia. This study also provides some reference for the comprehensive quantitative evaluation of P. tenuifolia.
ABSTRACT
OBJECTIVE: To carry out a comparison between the cortexes and the roots of Polygala tenuifolia, and to supply references for developing scientific processing method of P. tenuifolia. METHODS: A comprehensive comparison was made by comparing the chemical constitution and pharmacological activities of the cortexes and the roots of P. tenuifolia, i.e., multi-components determination and fingerprint analysis were used to analyze their chemical constituents, and the traditional pharmacological actions of P. tenuifolia, such as cough-relieving, sputum-removing and sedative effects were used to evaluate their efficacy. RESULTS: The chemical constitution of the cortexes, roots and heartwoods of P. tenuifolia was similar, but the contents of the various effective components in the cortexes were more than those in the roots and heartwoods. The pharmacological result revealed that there was no obvious difference between the cortexes and the roots of P. tenuifolia for their activities of cough-relieving, sputum-removing and sedative actions. The roots of P. tenuifolia showed a better tendency than the cortexes for cough-relieving and sputum-removing activities. CONCLUSION: In order to avoid the waste of crude drugs, and to save the cost during heartwood-discarding, the heartwoods of P. tenuifolia are suggested to be kept.
ABSTRACT
98 %).Conclusions Saponins are the major active ingredients in Radix Polygalae.Tenuifolin as an alkaline hydrolysis product of total saponins can be used as a chemical reference substance for the quality control of Radix Polygalae.