1.Effects of different processing methods on traits and chemical constituents of Forsythiae Fructus.
Rong-Rong XU ; Rui LI ; Chu-Han ZHANG ; Wei TIAN ; Xin-Guo WANG ; Li-Ying NIU ; Wei FENG
China Journal of Chinese Materia Medica 2025;50(2):465-471
This study aims to investigate the correlations of the appearance traits, total antioxidant capacity, and component content of Forsythiae Fructus processed by different methods, explore the effects of different processing methods on the abovementioned three aspects of Forsythiae Fructus, and screen out the internal and external indicators that have important effects on its quality. It determined the length, diameter, stem length, chroma value L~*, a~*, b~*, and other appearance indexes and antioxidant activity of Forsythiae Fructus processed by different methods. The content of forsythiaside A, rutin, forsythin, pinoresinol, and phillygenin was determined by ultra performance liquid chromatography(UPLC). Correlation analysis, principal component analysis(PCA), orthogonal partial least squares discriminant analysis(OPLS-DA), and independent sample t-test analysis were performed on the appearance indexes and the component content. The correlation analysis showed that there were differences in the appearance traits and the component content. L~* and E~* had highly significant negative correlations with pinoresinol and phillygenin(P<0.01) and significant positive correlations with forsythiaside A(P<0.05). There were a highly significant negative correlation between a~* and forsythiaside A(P<0.01) and highly significant positive correlations of a~* with pinoresinol and phillygenin(P<0.01). There were a highly significant positive correlation between b~* and forsythiaside A(P<0.01) and highly significant negative correlations of b~* with pinoresinol and phillygenin(P<0.01). The total antioxidant capacity had highly significant negative correlations with pinoresinol and phillygenin(P<0.01). The PCA results showed that there were differences among Forsythiae Fructus samples processed by different methods. OPLS-DA marked five important indicators, which were forsythiaside A, stem length, E~*, L~*, and b~*. The results of independent sample t-test showed that the content of forsythiaside A, pinoresinol, and phillygenin, the total antioxidant capacity, and the appearance traits such as L~*, a~*, b~*, and E~* were significantly different between the Forsythiae Fructus samples processed by steaming and boiling(P<0.05). According to content determination and a related biological activity analysis, steaming is a good choice from the perspective of improving the stability of chemical constituents and antioxidant activity of Forsythiae Fructus. From the point of view of improving the stability of chemical constituents and anti-inflammatory and anti-cancer activities of Forsythiae Fructus, it is recommended to use boiling as the processing method. Based on the above analysis methods, the main indexes for the appearance traits of Forsythiae Fructus processed by different methods are powder chroma value(L~*, a~*, b~*, E~*), stem length, and total antioxidant capacity, and those for chemical constituents are the content of forsythiaside A, pinoresinol, and phillygenin. This study provides reference for seeking scientific processing methods of Forsythiae Fructus.
Forsythia/chemistry*
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Drugs, Chinese Herbal/isolation & purification*
;
Fruit/chemistry*
;
Antioxidants/analysis*
;
Chromatography, High Pressure Liquid
;
Glycosides/analysis*
;
Principal Component Analysis
;
Furans
;
Lignans
2.Two new lignans from Ajania purpurea.
Yu-Shun CUI ; Min YAO ; Xin-Jun DI ; Zhi-Qiang LI ; Shan HAN ; Jun-Mao LI ; Yu-Lin FENG
China Journal of Chinese Materia Medica 2025;50(12):3322-3334
Macroporous resin adsorption column chromatography, silica gel column chromatography, ODS column chromatography, and semi-preparative high-performance liquid chromatography, combined with analytical methods such as NMR and MS, were employed to separate and identify compounds from the 70% ethanol extract of Ajania purpurea. A total of 30 compounds were isolated and identified, including 13 phenolic acids, 7 coumarins, 2 lignans, 1 flavonoid, 2 sesquiterpenes, 1 steroid, and 4 others. Among them, compounds 1 and 2 were newly discovered compounds, and compounds 4, 6, 8, 12, 14-23, 25, 28, and 30 were isolated from Ajania plants for the first time. Bioactivity screening showed that multiple compounds significantly inhibited the production of nitric oxide in lipopolysaccharide-stimulated RAW264.7 cells in a dose-dependent manner. Furthermore, compound 2 elevated the levels of glutathione in LPS-induced BEAS-2B cells, reduced the expression of pro-inflammatory cytokines such as tumor necrosis factor(TNF)-α, interleukin(IL)-6, and IL-1β, enhanced the mRNA of GPX4, HMOX1, NFE2L2, and enhanced protein levels of GPX4, HO-1, Nrf2, and SLC7A11, demonstrating potential anti-ferroptotic effect.
Mice
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Animals
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Lignans/isolation & purification*
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RAW 264.7 Cells
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Humans
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Nitric Oxide
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Tumor Necrosis Factor-alpha/immunology*
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Drugs, Chinese Herbal/isolation & purification*
;
NF-E2-Related Factor 2/metabolism*
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Macrophages/metabolism*
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Interleukin-6/immunology*
3.Diterpenoids and lignans from fossil Chinese medicinal succinum and their activity against renal fibrosis.
Yefei CHEN ; Yunfei WANG ; Yunyun LIU ; Yongming YAN ; Yongxian CHENG
Chinese Journal of Natural Medicines (English Ed.) 2025;23(7):888-896
Five previously undescribed diterpenoids, named succipenoids D‒H (1‒5), along with four undescribed lignans, named succignans A‒D (6‒9), were isolated from the dichloromethane extract of Chinese medicinal succinum. Compounds 1‒5 were characterized as nor-abietane diterpenoids, while compounds 6‒9 were identified as lignans polymerized from two groups of phenylpropanoid units. The structures of these novel compounds, including their absolute configurations, were determined through spectroscopic and computational methods. Biological assessments of renal fibrosis demonstrated that compounds 6 and 7 effectively reduce the expression of proteins associated with renal fibrosis, including α-smooth muscle actin (α-SMA), collagen I, and fibronectin in transforming growth factor-β1 (TGF-β1) induced normal rat kidney proximal tubular epithelial cells (NRK-52e).
Animals
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Rats
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Lignans/isolation & purification*
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Diterpenes/isolation & purification*
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Fibrosis/drug therapy*
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Drugs, Chinese Herbal/pharmacology*
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Molecular Structure
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Cell Line
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Kidney Diseases/pathology*
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Transforming Growth Factor beta1/genetics*
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Kidney/metabolism*
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Actins/genetics*
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Fibronectins/genetics*
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Collagen Type I/genetics*
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Epithelial Cells/metabolism*
4.Ten new lignans with anti-inflammatory activities from the leaves of Illicium dunnianum.
Ting LI ; Xiaoqing HE ; Dabo PAN ; Xiaochun ZENG ; Siying ZENG ; Zhenzhong WANG ; Xinsheng YAO ; Wei XIAO ; Haibo LI ; Yang YU
Chinese Journal of Natural Medicines (English Ed.) 2025;23(8):990-996
The anti-inflammatory phytochemical investigation of the leaves of Illicium dunnianum (I. dunnianum) resulted in the isolation of five pairs of new lignans (1-5), and 7 known analogs (6-12). The separation of enantiomer mixtures 1-5 to 1a/1b-5a/5b was achieved using a chiral column with acetonitrile-water mixtures as eluents. The planar structures of 1-2 were previously undescribed, and the chiral separation and absolute configurations of 3-5 were reported for the first time. Their structures were determined through comprehensive spectroscopic data analysis [nuclear magnetic resonance (NMR), high-resolution electrospray ionization mass (HR-ESI-MS), infrared (IR), and ultraviolet (UV)] and quantum chemistry calculations (ECD). The new isolates were evaluated by measuring their inhibitory effect on NO in lipopolysaccharide (LPS)-stimulated BV-2 cells. Compounds 1a, 3a, 3b, and 5a demonstrated partial inhibition of NO production in a concentration-dependent manner. Western blot and real-time polymerase chain reaction (PCR) assays revealed that 1a down-regulated the messenger ribonucleic acid (mRNA) levels of tumor necrosis factor α (TNF-α), interleukin-6 (IL-6), COX-2, and iNOS and the protein expressions of COX-2 and iNOS. This research provides guidance and evidence for the further development and utilization of I. dunnianum.
Lignans/isolation & purification*
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Plant Leaves/chemistry*
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Anti-Inflammatory Agents/isolation & purification*
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Mice
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Animals
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Molecular Structure
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Plant Extracts/pharmacology*
;
Illicium/chemistry*
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Cyclooxygenase 2/immunology*
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Interleukin-6/immunology*
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Nitric Oxide/metabolism*
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Cell Line
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Tumor Necrosis Factor-alpha/immunology*
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Nitric Oxide Synthase Type II/immunology*
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Lipopolysaccharides
5.Evaluation of neuroactive effects of ethanol extract of Schisandra chinensis, Schisandrin, and Schisandrin B and determination of underlying mechanisms by zebrafish behavioral profiling.
Jia-Wei WANG ; Feng-Yin LIANG ; Xiang-Shuo OUYANG ; Pei-Bo LI ; Zhong PEI ; Wei-Wei SU
Chinese Journal of Natural Medicines (English Ed.) 2018;16(12):916-925
Schisandra chinensis, a traditional Chinese medicine (TCM), has been used to treat sleep disorders. Zebrafish sleep/wake behavioral profiling provides a high-throughput platform to screen chemicals, but has never been used to study extracts and components from TCM. In the present study, the ethanol extract of Schisandra chinensis and its two main lignin components, schisandrin and schisandrin B, were studied in zebrafish. We found that the ethanol extract had bidirectional improvement in rest and activity in zebrafish. Schisandrin and schisandrin B were both sedative and active components. We predicted that schisandrin was related to serotonin pathway and the enthanol extract of Schisandra chinensis was related to seoronin and domapine pathways using a database of zebrafish behaviors. These predictions were confirmed in experiments using Caenorhabditis elegans. In conclusion, zebrafish behavior profiling could be used as a high-throughput platform to screen neuroactive effects and predict molecular pathways of extracts and components from TCM.
Animals
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Behavior, Animal
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drug effects
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Caenorhabditis elegans
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Central Nervous System Agents
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chemistry
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isolation & purification
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pharmacology
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Cyclooctanes
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analysis
;
isolation & purification
;
pharmacology
;
Drugs, Chinese Herbal
;
chemistry
;
pharmacology
;
Lignans
;
analysis
;
isolation & purification
;
pharmacology
;
Plant Extracts
;
chemistry
;
isolation & purification
;
pharmacology
;
Polycyclic Compounds
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analysis
;
isolation & purification
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pharmacology
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Schisandra
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chemistry
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Zebrafish
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physiology
6.Improved stability and oral bioavailability of Ganneng dropping pills following transforming lignans of herpetospermum caudigerum into nanosuspensions.
Juan-Juan LI ; Ling CHENG ; Gang SHEN ; Ling QIU ; Cheng-Ying SHEN ; Juan ZHENG ; Rong XU ; Hai-Long YUAN
Chinese Journal of Natural Medicines (English Ed.) 2018;16(1):70-80
The present study was designed to improve storage stability and oral bioavailability of Ganneng dropping pills (GNDP) by transforming lignans of Herpetospermum caudigerum (HL) composed of herpetrione (HPE) and herpetin (HPN) into nanosuspension (HL-NS), the main active ingredient of GNDP, HL-NS was prepared by high pressure homogenization and lyophilized to transform into solid nanoparticles (HL nanoparticles), and then the formulated HL nanoparticles were perfused into matrix to obtain NS-GNDP by melting method. For a period of 3 months, the content uniformity, storage stability and pharmacokinetics test in vivo of NS-GNDP were evaluated and compared with regular GNDP at room temperature. The results demonstrated that uniformity of dosage units of NS-GNDP was acceptable according to the criteria of Chinese Pharmacopoeia 2015J. Physical stability of NS-GNDP was investigated systemically using photon correlation spectroscopy (PCS), zeta potential measurement, and scanning electron microscopy (SEM). There was a slight increase in particles and PI of HL-NS re-dispersed from NS-GNDP after storage for 3 months, compared with new formulated NS-GNDP, which indicated a good redispersibility of the NS-GNDP containing HL-NS after storage. Besides, chemical stability of NS-GNDP was studied and the results revealed that HPE and HPN degradation was less when compared with that of GNDP, providing more than 99% of drug residue after storage for 3 months. In the dissolution test in vitro, NS-GNDP remarkably exhibited an increased dissolution velocity compared with GNDP and no distinct dissolution difference existed within 3 months. The pharmacokinetic study showed that HPE and HPN in NS-GNDP exhibited a significant increase in AUC, C and decrease in T when compared with regular GNDP. These results indicated that NS-GNDP possessed superiority with improved storage stability and increased dissolution rate and oral bioavailability.
Animals
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Benzofurans
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chemistry
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Biological Availability
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Cucurbitaceae
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chemistry
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Drug Carriers
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chemistry
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Drug Compounding
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Drug Stability
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Freeze Drying
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Furans
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chemistry
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Humans
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Lignans
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administration & dosage
;
chemistry
;
isolation & purification
;
pharmacokinetics
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Male
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Nanoparticles
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administration & dosage
;
chemistry
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Particle Size
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Plant Extracts
;
chemistry
;
isolation & purification
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Rats
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Rats, Sprague-Dawley
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Solubility
7.A new caffeate compound from Nardostachys chinensis.
Ying-peng CHEN ; Zhong-ping WANG ; Hong-hong ZHENG ; Yan-tong XU ; Yani ZHU ; Peng ZHANG ; Hong-hua WU
Acta Pharmaceutica Sinica 2016;51(1):100-104
A new caffeate compound, (E)-erythro-syringylglyceryl caffeate (1), was isolated from the roots and rhizomes of Nardostachys chinensis Batal., together with nine known phenolic compounds, including (+)-licarin A (2), naringenin 4', 7-dimethyl ether (3), pinoresinol-4-O-β-D-glucoside (4), caraphenol A (5), Z-miyabenol C (6), protocatechuic acid (7), caffeic acid (8), gallic acid (9) and vanillic acid (10). Their chemical structures were elucidated on the basis of spectroscopic data and physicochemical properties. Furthermore, this is the first report of compounds 2, 5 and 6 from Nardostachys genus.
Caffeic Acids
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chemistry
;
isolation & purification
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Flavanones
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chemistry
;
isolation & purification
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Furans
;
chemistry
;
isolation & purification
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Glucosides
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chemistry
;
isolation & purification
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Hydroxybenzoates
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chemistry
;
isolation & purification
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Lignans
;
chemistry
;
isolation & purification
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Nardostachys
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chemistry
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Plant Roots
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chemistry
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Rhizome
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chemistry
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Vanillic Acid
;
chemistry
;
isolation & purification
8.Lignans from stems of Cistanche deserticola cultured in Tarim desert.
Ze-dong NAN ; Ming-bo ZHAO ; Yong JIANG ; Peng-fei TU
China Journal of Chinese Materia Medica 2015;40(3):463-468
In order to clarify the chemical constituents of Cistanche deserticola cultured in Tarim desert, a systematically phytochemical investigation was carried out. The chemical constituents were isolated by column chromatography, such as silica gel, Sephadex LH- 20, MCI gel, ODS and semi-preparative HPLC, and their structures were determined on the basis of MS, NMR spectroscopic analysis and/or comparison with literature data. Eleven lignans were isolated from the 85% ethanol extract of the stems of C. deserticola cultured in Tarim desert. Their structures were identified as (+)-syringaresinol-4'-O-β-D-glucopyranoside (1), (+)-isoeucommin A (2), eucommin A (3), (+)-pinoresinol monomethylether β-D-glucoside (4), lariciresinol 4'-O-β-D-glucopyranoside (5), lariciresinol 4-O-β-D-glucopyranoside (6), conicaoside (7), dehydrodiconiferyl alcohol 4-O-β-D-glucopyranoside (8), dehydrodiconiferyl alcohol γ'-O-β-D-glucoside (9), citrusin A (10), and alaschanioside A (11). Compounds 1, 3-7, 10 and 11 were isolated from this genus for the first time, and compounds 2, 8 and 9 were obtained from this species for the first time.
Cistanche
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chemistry
;
growth & development
;
Lignans
;
chemistry
;
isolation & purification
;
Plant Stems
;
chemistry
9.Correlation research on contents of podophyllotoxin and total lignans in Sinopodophyllum hexandrum and ecological factors.
Min LI ; Guo-yue ZHONG ; Ao-lin WU ; Shou-wen ZHANG ; Wei JIANG ; Jian LIANG
China Journal of Chinese Materia Medica 2015;40(9):1831-1836
To explore the correlation between the ecological factors and the contents of podophyllotoxin and total lignans in root and rhizome of Sinopodophyllum hexandrum, podophyllotoxin in 87 samples (from 5 provinces) was determined by HPLC and total lignans by UV. A correlation and regression analysis was made by software SPSS 16.0 in combination with ecological factors (terrain, soil and climate). The content determination results showed a great difference between podophyllotoxin and total lignans, attaining 1.001%-6.230% and 5.350%-16.34%, respective. The correlation and regression analysis by SPSS showed a positive linear correlation between their contents, strong positive correlation between their contents, latitude and annual average rainfall within the sampling area, weak negative correlation with pH value and organic material in soil, weaker and stronger positive correlations with soil potassium, weak negative correlation with slope and annual average temperature and weaker positive correlation between the podophyllotoxin content and soil potassium.
Berberidaceae
;
chemistry
;
China
;
Chromatography, High Pressure Liquid
;
Climate
;
Drugs, Chinese Herbal
;
chemistry
;
isolation & purification
;
Ecosystem
;
Lignans
;
chemistry
;
isolation & purification
;
Podophyllotoxin
;
chemistry
;
isolation & purification
;
Soil
;
chemistry
;
Temperature
10.Honokiol ameliorates endothelial dysfunction through suppression of PTX3 expression, a key mediator of IKK/IkappaB/NF-kappaB, in atherosclerotic cell model.
Ling QIU ; Rong XU ; Siyang WANG ; Shuijun LI ; Hongguang SHENG ; Jiaxi WU ; Yi QU
Experimental & Molecular Medicine 2015;47(7):e171-
Pentraxin 3 (PTX3) was identified as a marker of the inflammatory response and overexpressed in various tissues and cells related to cardiovascular disease. Honokiol, an active component isolated from the Chinese medicinal herb Magnolia officinalis, was shown to have a variety of pharmacological activities. In the present study, we aimed to investigate the effects of honokiol on palmitic acid (PA)-induced dysfunction of human umbilical vein endothelial cells (HUVECs) and to elucidate potential regulatory mechanisms in this atherosclerotic cell model. Our results showed that PA significantly accelerated the expression of PTX3 in HUVECs through the IkappaB kinase (IKK)/IkappaB/nuclear factor-kappaB (NF-kappaB) pathway, reduced cell viability, induced cell apoptosis and triggered the inflammatory response. Knockdown of PTX3 supported cell growth and prevented apoptosis by blocking PA-inducted nitric oxide (NO) overproduction. Honokiol significantly suppressed the overexpression of PTX3 in PA-inducted HUVECs by inhibiting IkappaB phosphorylation and the expression of two NF-kappaB subunits (p50 and p65) in the IKK/IkappaB/NF-kappaB signaling pathway. Furthermore, honokiol reduced endothelial cell injury and apoptosis by regulating the expression of inducible NO synthase and endothelial NO synthase, as well as the generation of NO. Honokiol showed an anti-inflammatory effect in PA-inducted HUVECs by significantly inhibiting the generation of interleukin-6 (IL-6), IL-8 and monocyte chemoattractant protein-1. In summary, honokiol repaired endothelial dysfunction by suppressing PTX3 overexpression in an atherosclerotic cell model. PTX3 may be a potential therapeutic target for atherosclerosis.
Apoptosis/drug effects
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Atherosclerosis/chemically induced/*drug therapy/immunology/pathology
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Biphenyl Compounds/chemistry/isolation & purification/*pharmacology
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C-Reactive Protein/*genetics/immunology
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Down-Regulation/drug effects
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Drugs, Chinese Herbal/chemistry/isolation & purification/*pharmacology
;
Human Umbilical Vein Endothelial Cells
;
Humans
;
I-kappa B Kinase/*immunology
;
Lignans/chemistry/isolation & purification/*pharmacology
;
Magnolia/chemistry
;
Palmitic Acid
;
Protein-Serine-Threonine Kinases/*immunology
;
Serum Amyloid P-Component/*genetics/immunology
;
Signal Transduction/drug effects

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