Isolation and identification of two new compounds from Semen Persicae / 药学学报

Five compounds were isolated from the ethyl acetate fraction of Semen Persicae by using various chromatographic methods, including ODS, Sephadex LH-20, HPLC and semipreparative HPLC. Their structures were identified by 1D-NMR, 2D-NMR, HR-ESI-MS, UV, IR, circular dichroism (CD) and ECD calculation techniques: (2R,3R)-5,7,4′-trihydroxy-3′-methoxy-3-formylflavan-3-ol-5-O-β-D-glucopyranoside (1), (7R,8S)-dihydrodehydrodiconiferyl 6″-benzoyl alcohol-9-O-β-D-glucopyranoside (2), (7R,8S)-dihydrodehydrodiconiferyl alcohol-9-β-O-D-glucopyranosid (3), 2-methoxy-4-(2-propenyl)-phenyl-O-β-D-glucopyranoside (4), 2-[4-(3-hydroxypropyl)-2-methoxyphenoxy]-propane-1,3-diol (5). Compound 1 and 2 are new compounds, and compounds 3-5 were obtained from Prunus davidiana (Carr.) Franch. for the first time.

Mechanism of active components of "Notoginseng Radix et Rhizoma-Drynariae Rhizoma" in treatment of osteoporosis based on network pharmacology and in vitro cell experiment / 中国中药杂志

The present study aimed to explore the main active components and potential mechanisms of Panax notoginseng saponins(PNS) and osteopractic total flavone(OTF) in the treatment of osteoporosis(OP) through network pharmacology, molecular docking and in vitro cell experiments, which was expected to provide a theoretical basis for clinical applications. The blood-entering components of PNS and OTF were obtained from literature search and online database, and their potential targets were obtained from Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP) and SwissTargetPrediction. The OP targets were obtained by means of searching Online Mendelian Inheritance in Man(OMIM) and GeneCards. The common targets of the drug and disease were screened by Venn. Cytoscape was used to construct a "drug-component-target-disease" network, and the core components were screened according to the node degree. The protein-protein interaction(PPI) network of the common targets was constructed by STRING and Cytoscape, and the core targets were screened according to the node degree. GO and KEGG enrichment analysis of potential therapeutic targets were carried out by R language. Molecular docking was used to determine the binding activity of some active components to key targets by AutoDock Vina. Finally, HIF-1 signaling pathway was selected for in vitro experimental verification according to the results of KEGG pathway analysis. Network pharmacology showed that there were 45 active components such as leachianone A, kurarinone, 20(R)-protopanaxatriol, 20(S)-protopanaxatriol, and kaempferol, and 103 therapeutic targets such as IL6, AKT1, TNF, VEGFA and MAPK3 involved. PI3K-AKT, HIF-1, TNF and other signaling pathways were enriched. Molecular docking revealed that the core components had good binding ability to the core targets. In vitro experiments found that PNS-OTF could up-regulate the mRNA expression levels of HIF-1α, VEGFA and Runx2, indicating that the mechanism of PNS-OTF in treating OP may be related to the activation of HIF-1 signaling pathway, and thus PNS-OTF played a role in promoting angiogenesis and osteogenic differentiation. In conclusion, this study predicted the core targets and pathways of PNS-OTF in treating OP based on network pharmacology and carried out in vitro experimental verification, which reflected the characteristics of multi-component, multi-target and multi-pathway synergy of PNS-OTF, and provided new ideas for the future clinical treatment of OP.

Analysis on Components Absorbed into Blood of Citri Reticulatae Pericarpium in Rats Based on Sequential Metabolism and UPLC-HRMS / 中国实验方剂学杂志

ObjectiveTo study the metabolism of chemical components from Citri Reticulatae Pericarpium（CRP）in different parts of rats by sequential metabolism and ultra performance liquid chromatography-high resolution mass spectrometry（UPLC-HRMS）. MethodSD male rats were employed as experimental subjects， and blood samples of intestinal metabolism and hepatic metabolism were prepared after administration of CRP ethanol extract by in situ intestinal perfusion， and comprehensive metabolic samples were collected after intragastric administration. UPLC-HRMS was used to analyze the samples with acetonitrile（A）-0.1% formic acid aqueous solution（B）as the mobile phase for gradient elution（0-10 min， 10%-30%A； 10-30 min， 30%-95%A； 30-31 min， 95%-10%A； 31-35 min， 10%A）at a flow rate of 0.35 mL·min-1， using a heated electrospray ionization with positive and negative ion mode scanning in the range of m/z 100-1 500. Under these conditions， the differences in the profiles of CRP ethanol extract， blank plasma and drug-containing plasma under different treatment groups were compared， and the chemical components of each sample were analyzed and identified based on the retention time， accurate relative molecular mass， primary and secondary ion fragments， and the information of reference substances. ResultA total of 44 chemical components were identified in the CRP ethanol extract， including flavone-O-glycosides， flavone-C-glycosides and polymethoxyflavonoids， etc. The results of sequential metabolism showed that 22 chemical components in CRP were detected in the intestinal metabolic sample， 18 chemical components were detected in the hepatic metabolic sample， and 9 identical chemical components（narirutin， hesperidin， meranzin， 5，7，8，3ʹ，4ʹ，5ʹ-hexamethoxy-flavone， isosinensetin， sinensetin， 3，5，6，7，8，3ʹ，4ʹ-heptamethoxyflavone， nobiletin and tangeretin）could be detected in all three metabolic samples， with a total of 22 compounds entering the blood in prototype form. ConclusionThe identified 21 components with well-defined structures entering the blood as prototypes may be potential active components of CRP， and differences in the components at different metabolic parts can provide an experimental basis for elucidating the in vivo biotransformation process of the metabolic components of CRP.

Geranylated or prenylated flavonoids from Cajanus volubilis / 中国天然药物

Five new flavonoid derivatives, cajavolubones A-E (1-5), along with six known analogues (6-11) were isolated from Cajanus volubilis, and their structures were elucidated by spectroscopic analysis and quantum chemical calculations. Cajavolubones A and B (1 and 2) were identified as two geranylated chalcones. Cajavolubone C (3) was a prenylated flavone, while cajavolubones D and E (4 and 5) were two prenylated isoflavanones. Compounds 3, 8, 9 and 11 displayed cytotoxicity against HCT-116 cancer cell line.

Comparison of growth and quality of wild and cultivated Artemisia stolonifera / 中国中药杂志

This paper aims to compare the difference of growth and quality between wild and cultivated Artemisia stolonifera, thereby providing references for further development and utilization of A. stolonifera. The wild and cultivated A. stolonifera from different altitudes were collected, and the agronomic characters, moxa yield, volatile components, flavonoids, and phenolic acids were determined. The results showed that the cultivated species were taller and stronger, with more leaves and branches, than the wild species. The moxa yield and combustion quality of wild products were higher than those of cultivated products. The content of main volatile components in cultivated products was higher than that in wild products. The content of flavonoids and phenolic acids in wild products was higher than that in cultivated products. At high altitude, the ignition performance, combustion persistence, comprehensive combustion performance, and heat release during combustion of the wild and cultivated A. stolonifera. were optimal. At middle altitude, the content of main characteristic volatile components and flavone phenolic acids in the leaves of the cultivated and wild A. stolonifera were the highest. At low altitude, the combustion quality and the content of the above components of the cultivated A. stolonifera decrease significantly. Considering the combustion quality and the content of the internal components of the leaf lint, the middle and high altitude areas are suitable for the artificial cultivation of A. stolonifera.

Effects of total flavone of oldenlandia diffusa on the proliferation and apoptosis of hepatocellular carcinoma stem cell / 西安交通大学学报(医学版)

【Objective】 To investigate the effects of total flavone of oldenlandia diffusa (FOD) on the proliferation and apoptosis of hepatocellular carcinoma (HCC) stem cells sorted from Huh7. 【Methods】 Human HCC cell lines Huh7 was cultured in vitro; CD133 positive (CD133+) stem cells in Huh7 cell line were sorted by flow cytometry, and stem cell markers such as Nanog, Oct4 and Sox2 were tested by Western blotting. CD133+-Huh7 was stimulated by different concentrations (0 μg/mL, 50 μg/mL, 100 μg/mL and 400 μg/mL) of FOD for different time (24 h, 48 h, 72 h and 96 h). CCK8 and plate cell cloning assay were used to detect the effect of FOD on CD133+-Huh7 proliferation while Annexin V-PE/7-AAD was used to detect the effect of FOD on CD133+-Huh7 apoptosis. Western blotting was used to detect the protein expressions of protein 53 (P53), factor associated suicide-Fas-associating protein with a novel death domain (Fas-FADD), B-cell lymphoma-2 (Bcl-2), Cleaved-Caspase3, and Bcl-2 associated X protein (Bax). 【Results】 More than 95% of stem cells were purified for further experiments. Cell proliferation of CD133+-Huh7 was significantly inhibited by FOD, with the significant suppression at the concentration of 100 μg/mL for 72 h compared with negative control group (P<0.05). The apoptosis rate was significantly upregulated than that in the negative control group (P<0.05). The protein expression of Bcl2 decreased while Bax and Cleaved-Caspae3 increased via FAS/FADDD and P53 axis. 【Conclusion】 FOD can significantly inhibit the proliferation and promote the apoptosis of CD133+-Huh7.

Effect of total flavone of oldenlandia diffusa on the proliferation, apoptosis and stemness of breast cancer MDA-MB-231 cell lines / 西安交通大学学报(医学版)

【Objective】 To investigate the effect of total flavone of oldenlandia diffusa(FOD) on the stemness, proliferation and apoptosis of breast cancer(BC) stem cells sorted from MDA-MB-231. 【Methods】 Human BC cell lines MDA-MB-231 was cultured in vitro; MDA-MB-231 was stimulated by different concentrations(0 μg/mL, 100 μg/mL, 200 μg/mL and 400 μg/mL) of FOD for different time (24 h, 48 h and 72 h). CCK8 and plate cell cloning assay were used to detect the effect of FOD on MDA-MB-231 proliferation; CD44+/CD24-MDA-MB-231 cell line were tested by flow cytometry and stem cell markers such as Nanog, Oct4 and Sox2 were tested by Western blotting; Annexin V-PE/7-AAD was used to detect the effect of FOD on MDA-MB-231 apoptosis and Bcl2, cleaved-caspase3 and Bax were tested by Western blotting. 【Results】 Cell proliferation of MDA-MB-231 was significantly inhibited by FOD, with the significant suppression at concentrations of 400 μg/mL for 72 h compared with negative control group(P<0.05). The apoptosis rate was significantly upregulated than the negative control group (P<0.05). The protein expression of Bcl2 decreased while Bax and cleaved-caspae3 increased, and stemness markers such as Nanog, Sox2 and Oct4 decreased in FOD-treated cells. Moverover, Akt-GSK3β-β-catenin axis was inhibited in FOD-treated cells. 【Conclusion】 FOD could significantly inhibit the stemness and proliferation and promote the apoptosis of MDA-MB-231.

Effects of increasing efficacy and decreasing toxicity of ginkgo flavone aglycone on doxorubicin in the treatment of liver cancer / 中国药房

OBJECTIVE To study the effects of increasing efficacy and decreasing toxicity of ginkgo flavone aglycone （GA） on doxorubicin （DOX）in the treatment of liver cancer. METHODS A tumor bearing model was established by inoculating liver cancer cell H 22 into the right axillary skin of ICR mice. The successfully modeled mice were randomly divided into model control group，DOX group （2.5 mg/kg，once every other day ，via tail vein ），GA group （30 mg/kg，once a day ，gavage）and GA+DOX group（the usage was the same as single drug groups ），with 6 mice in each group. The administration cycle was 15 days. The general growth of mice in each group were observed ，body weight and tumor weight were measured ，and the inhibition rate of tumor was calculated. Jin’s formula was used to evaluate the effect of combined medication （Q）. The serum level of alpha-fetal protein（AFP），the pathological changes of tumor tissue ，cell apoptosis and the expression of platelet-endothelial cell adhesion molecule-1（CD31）were detected in each group. The cardiac index，serum levels of B-type natriuretic peptide （BNP）and N-terminal pro-brain natriuretic peptide （NT-pro BNP ），pathological changes of heart and myocardial fibrosis degree were also detected. RESULTS The percentage of body weight change （except for GA group ） and tumor weights of DOX group，GA group and GA + DOX group were all decreased significantly，compared with model control group （P＜0.05 or P＜0.01），while tumor weight of GA+DOX gro up was significantly lower than DOX group （P＜0.01）. Inhibitory rates of tumor in 3 administration groups were 54.29％，42.50％ and 89.29％ respectively，and Q of two-drug combination was 1.21. The tumor tissues of mice in each administration group were necrotic to varying degrees ；the serum level of AFP and the expression of CD31 in tumor tissue were decreased significantly ，compared with model control group （P＜0.05 or P＜0.01）；the percentage of necrosis area of tumor tissue and the positive rate of apoptosis （except for single drug groups ）were significantly increased （P＜0.05 or P＜0.01），while positive rate of apoptosis in GA+DOX group was significantly higher than DOX group （P＜0.05）. Cardiac index of mice in DOX group was significantly lower than model control group （P＜0.01）；serum levels of BNP and NT-pro BNP in DOX group and GA+ DOX group were significantly higher than model control group （P＜0.05 or P＜0.01）；pathological changes of heart and the degree of myocardial fibrosis in GA+DOX group were lower than DOX group. CONCLUSIONS GA combined with DOX show synergistic antitumor effect. GA can strengthen the apoptosis promoting effect of DOX ，and can help to reduce the cardiotoxicity of DOX.

A new flavone glycoside from Eriocaulon buergerianum / 药学学报

Ten compounds were isolated from the water extract of Eriocaulon buergerianum by HP20, ODS, Sephadex LH-20 and MCI Gel CHP-20 column chromatographic methods. Their structures were identified by spectroscopic and chemical approaches as 6-methoxyquercetin-3-O-(2′′′-vanilloyl)-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (1), syringaresinol-4′-O-β-D-glucopyranoside (2), rutin (3), 1-O-feruloylglycerol (4), 1,2-benzenediol (5), vomifoliol (6), β-D-(6-O-trans-feruloyl) fructofuranosyl-α-D-O-glucopyranosied (7), dihydroferulic acid (8), guanosine (9) and quercetin-3-O-β-gentiobioside (10). The compound 1 is a new compound, the compounds 2 and 4-10 were obtained from Eriocaulon genus for the first time, and the compound 3 was isolated from this plant for the first time. Molecular docking study showed that 1 is a potential inhibitor of TNF-α. The compound 1 was evaluated for their anti-inflammatory activities in vitro, and 1 showed significant inhibitory activity against TNF-α production in lipopolysaccharide (LPS)-induced RAW264.7 macrophage cells at the concentrations of 1, 10 and 100 μmol·L-1.

Study on the separation and identification of flavone C-glycosides from the leaves of Dendrobium officinale and their inhibitory activities to α-gulcosidase / 中国药房

OBJECTIVE To separ ate and identify the flavone C-glycosides from the leaves of Dendrobium officinale ，and to evaluate their in vitro inhibitory activities to α-glucosidase. METHODS The flavone C-glycosides from the leaves of D. officinale were separated and purified by macroporous adsorption resin and preparative high -performance liquid chromatography . The structure of obtained compound was elucidated and identified by spectroscopic methods ，such as ultraviolet spectrum ，nuclear magnetic resonance，high-resolution electrospray ionization mass spectrometry ，etc. The in vitro inhibitory activities of flavone C-glycosides and positive control （acarbose）to α-glucosidase were investigated . RESULTS Five apigenin -6，8-di-C-glycosides were isolated and purified from the leaves of D. officinale，and identified as apigenin -6-C-α-L-rhamnosyl-8-C-β-D-quinovoside（1）， schaftoside（2），isoschaftoside（3），isoviolanthin（4）and violanthin （5）. Half inhibitory concentration of compound 1-5 and acarbose inhibiting α-glucosidase were （1.79±1.27），（2.05±0.72），（1.93±0.67），（1.09±0.46），（1.36±0.58），（18.69±1.24）μmol/L， respectively. CONCLUSIONS Five apigenin -6，8-di-C-glycosides with α-glucosidase inhibitory activity are isolated from the leaves of D. officinale，of which compound 1 is a new compound and compound 2 is isolated from this plant for the first time .

Analysis of Chemical Constituents in Microctis Folium by UPLC-Q-TOF-MS/MS / 中国实验方剂学杂志

Objective:To analyze the chemical constituents in Microctis Folium by ultra performance liquid chromatography-quadrupole-time-of-flight high resolution mass spectrometry （UPLC-Q-TOF-MS/MS）. Method:Waters CORTECS UPLC C₁₈ column （2.1 mm×150 mm， 1.6 μm） was used for chromatographic separation with the mobile phase of methanol （A） -0.1% formic acid solution （B） for gradient elution （0-4 min， 14%-30%A； 4-16 min， 30%-58%A； 16-25 min， 58%-78%A； 25-25.1 min， 78%-98%A； 25.1-29 min， 98%A）， the flow rate was 0.25 mL· min^-1， the injection volume was 1 μL. The electrospray ionization （ESI） was adopted for determining the chromatographic effluent under positive and negative ion modes， the main chromatographic peaks were assigned and distinguished by Q-TOF， and the scanning range was <italic>m</italic>/<italic>z</italic> 100-1 500. Result:A total of 31 chemical constituents in Microctis Folium were identified by confirmation of reference substances， literature comparison and high resolution mass spectrometry data analysis. The chemical constituent cluster was composed of 28 flavonoids （9 flavone C-glycosides， 10 flavonols and their glycosides， 8 proanthocyanidins， 1 xanthone） and 3 organic acids （caffeic acid， <italic>p</italic>-coumaric acid， ferulic acid）. Conclusion:UPLC-Q-TOF-MS/MS technique provides a simple， rapid and accurate method for the identification of chemical constituents in Microctis Folium. Flavone C-glycosides， flavonol oxyglycosides and proanthocyanidins are the main chemical constituents. The 7 proanthocyanidins are reported for the first time in this herb. In conclusion， the chemical profile of Microctis Folium is characterized and the findings are meaningful for the in-depth quality assessment and material basis clarification of Microctis Folium.

Efficacy of Getong Tongluo Capsule () for Convalescent-Phase of Ischemic Stroke and Primary Hypertension: A Multicenter, Randomized, Double-Blind, Controlled Trial / 中国结合医学杂志

OBJECTIVE@#To evaluate whether the efficacy of Getong Tongluo Capsule (, GTC, consisted of total flavone of Radix Puerariae) on improving patients' quality of life and lowering blood pressure are superior to the extract of Ginkgo biloba (EGB) for patients with convalescent-phase ischemic stroke and primary hypertension.@*METHODS@#This randomized, positive-drug- and placebo-controlled, double-blind trial was conducted from September 2015 to October 2017. Totally 477 eligible patients from 18 hospitals in China were randomly assigned in a 2:1:1 ratio to the following interventions, twice a day for 12 weeks: (1) GTC 250 mg plus EGB-matching placebo 40 mg (237 cases, GTC group), (2) EGB 40 mg plus GTC-matching placebo 250 mg (120 cases, EGB group) or (3) GTC-matching placebo 250 mg plus EGB-matching placebo 40 mg (120 cases, placebo group). Moreover, all patients were orally administered aspirin enteric-coated tablets 100 mg, once a day for 12 weeks. The primary outcome was the Barthel Index (BI). The secondary outcomes included the control rate of blood pressure and National Institutes of Health Stroke Scale (NIHSS) scores. The incidence and severity of adverse events (AEs) were calculated and assessed.@*RESULTS@#The BI relative independence rates, the clinical recovery rates of NIHSS, and the total effective rates of NIHSS in the GTC and EGB groups were significantly higher than the placebo group at 12 weeks after treatment (P0.05). The control rate of blood pressure in the GTC group was significantly higher than the EGB and placebo groups at 12, 18 and 24 weeks after treatment (P0.05).@*CONCLUSION@#GTC exhibited significant efficacy in improving patients' quality of life as well as neurological function and controlling hypertension. (Registration No. ChiCTR1800016667).

Influence and mechanism of Xindakang on cardiac functions of isolated frog heart / 中国药理学与毒理学杂志

OBJECTIVE To evaluate the effects of flavonoids from Xindakang (Hippophae Fructus flavone) on myo?cardial systolic and diastolic functions of isolated frog hearts and explore the possible mechanism, and provide experi?mental basis for improving the effect and efficacy of Xindakang on cardiac function. METHODS The isolated frog heart perfusion specimens were prepared by Yagi's method, and the effects of different concentrations of Xindakang on myo?cardial contractility (0.0125, 0.025, 0.05, 0.1 and 0.2 g·L-1), heart rate and cardiac output of isolated frog heart were stud?ied. Acetylcholine, atropine and epinephrine were administered successively to analyze the effects of Xindakang on car?diac systolic function of isolated frogs under the action of different drugs, and compared with propranolol. The effect of extracellular calcium ion concentration on the action of Xindakang was studied by using low calcium concentration, high cal?cium concentration and normal Ren's solution. To study the effect and possible mechanism of Xindakang on cardiac systolic function of frog. RESULTS The concentration of Xindakang in the range of 0.0125-0.1 g·L-1 could weaken the contractility of isolated frog heart and increase the concentration of Xindakang. The inhibitory effect of Xindakang on con?tractility of isolated frog heart was enhanced, and showed obvious dose-effect relationship. Cardiac output was signifi?cantly decreased by Xindakang (P<0.01), slow heart rate (P<0.05); M receptor blocker atropine could not antagonize the contractile effect of Xindakang, and Xindakang could not completely antagonize the contractile effect of adrenalin. Xindakang could inhibit the isolated frog heart in low calcium concentration, high calcium concentration and normal Ren's solution, and increased with the increase of extracellular calcium concentration (P<0.01). CONCLUSION Xinda?kang has inhibitory effect on isolated frog heart, which may be achieved by blocking the calcium channel on myocardial cell membrane and reducing the calcium concentration in myocardial cells.

Promoting effect of osteopractic total flavone combined with nano-bone materials on proliferationand differentiation of MC3T3-E1 cells / 中国组织工程研究

BACKGROUND: Preliminary study has found that osteopractic total flavone can promote osteogenic differentiation of MC3T3-E1 cells on the surface of nano-bone material, but the underlying mechanism needs to be studied in depth. OBJECTIVE: To investigate the actin mechanism of osteopractic total flavone combined with nano-bone material on MC3T3-E1 cells. METHODS: MC3T3-E1 cells were co-cultured with nano-bone material, and 100 mg/L and 250 mg/L osteopractic total flavone were treated as drug intervention, including 10 μg/L transforming growth factor-β as positive control. The samples were divided into eight groups: (1) Normal group; (2) DKK1 group: Wnt pathway inhibitor DKK1 (0.1 mg/L) blocks Wnt/β-catenin signaling pathway; (3) DKK1+transforming growth factor-β group; (4) DKK1+100 mg/L osteopractic total flavone group; (5) DKK1+250 mg/L osteopractic total flavone group; (6) DKK1+ nano-hydroxyapatite/collagen+transforming growth factor-β group; (7) DKK1+nano-hydroxyapatite/collagen+100 mg/L osteopractic total flavone group; (8) DKK1+nano-hydroxyapatite/collagen+250 mg/L osteopractic total flavone group. Cells in each group were harvested after 24 and 48 hours of intervention. Immunofluorescence labeling was used to observe the binding of Wnt and LRP in osteoblasts in the Wnt/β-catenin pathway. The expression of β-catenin, LRP 5, GSK-3β, Cyclin D1, and RUNX2 was detected by real-time polymerase chain reaction and western blot assay. RESULTS AND CONCLUSION: (1) Confocal laser scanning microscope showed that obvious brown and yellow staining was shown in the DKK1+transforming growth factor-β group, DKK1+250 mg/L osteopractic total flavone group, DKK1+nano-hydroxyapatite/ collagen+transforming growth factor-β group, and DKK1+nano-hydroxyapatite/collagen+250 mg/L osteopractic total flavone group, indicating that Wnt and LRP combined better than other groups. (2) Real-time polymerase chain reaction and western blot assay results showed that osteopractic total flavone could promote the expression of β-catenin, LRP5 and RUNX2, and downregulated GSK3β expression. These findings confirm that osteopractic total flavone can promote the differentiation and proliferation of osteoblasts by activating the Wnt/β-catenin signaling pathway. Gene activation induced by osteopractic total flavone was dose-dependent.

Effects of pueraria total flavone on inflammatory cytokine and stat3 expression in brain tissue of exhaustive exercise rats / 中国组织工程研究

BACKGROUND: The physiological and pathological mechanisms underlying the inflammatory response of rat brain tissue caused by exhaustive exercise are very complicated. Studies have shown that Pueraria total flavonoids have anti-oxidative, neuroprotective, and cardio-cerebrovascular protective effects against brain injury. OBJECTIVE: To investigate the effect of Pueraria total flavone on inflammatory cytokines and signal transducer and activator of transcription-3 (STAT3) expression in rat brain tissue after exhaustive exercise. METHODS: Fifty healthy male Sprague-Dawley rats were randomly divided into a quiet control group, an exercise control group, low, middle, high dose Pueraria total flavone groups. Each training group conducted a 6-week sports training. At the end of 6-week exercise, the rats were confirmed to be exhausted. The rats were intragastrically administered 50, 100 and 200 mg/kg Pueraria total flavone in low, middle and high dose groups, respectively. Administration in each Pueraria total flavone group began at 30 minutes before exercise, once a day, and ended until the completion of the experiment. The activities of tumor necrosis factor-α, interleukin-8, interleukin-1β and interleukin-10 in serum and brain tissue of rats were determined by ELISA. The expression of STAT3 in rat brain tissue was detected by RT-PCR and western blot. The study protocol was approved by the Animal Ethics Committee of Guangxi Normal University (approval No. GXMU201703049). RESULTS AND CONCLUSION: The levels of tumor necrosis factor-α, interleukin-8, interleukin-1β and interleukin-10 in serum and brain tissue of exercise control rats were higher than those in the quiet control group (P < 0.01). The levels of tumor necrosis factor-α and interleukin-10 in serum and brain tissue of rats with middle and high dose of Pueraria total flavone were significantly lower than those in the exercise control group (P < 0.01). The levels of interleukin-8 and interleukin-1β in serum and brain tissue of rats with low, middle and high dose of Pueraria total flavone were significantly lower than those in the exercise control group (P < 0.01 or P < 0.05). The expression levels of STAT3 mRNA and protein in brain tissue of exercise control rats were significantly higher than those in the quiet control group (P < 0.01). The expression levels of STAT3 mRNA and protein in the brain tissue of rats with low, middle and high doses of Pueraria total flavone were significantly higher than those in the quiet control group (P < 0.01). To conclude, exhaustive exercise can cause inflammatory reaction and up-regulate STAT3 expression in rat brain tissue. The total flavonoids of Puerariae can regulate the expression of STAT3 in brain tissues and inhibit the inflammatory response of brain tissue, thus protecting damaged brain tissue.

A new diphenylpropanoid from Cassia floribunda / 中草药

Objective: To study the chemical composition of the stems and leaves of Cassiafloribunda. Methods: The chemical constituents from stems and leaves of C. floribunda were isolated by silica gel MCI, RP-18, TLC, and HPLC methods. Their structures were elucidated by spectroscopic methods and physicochemical properties. Results: Eighteen compounds were isolated from the 90% EtOH extract of C. floribunda and their structures were established ascassia cis-transdiphenylpropanoid(1), ethyl p-hydroxycinnamate (2), shonanin(3), dibutyl phthalate(4), 1,6,8-trihydroxyl-3-methyl-anthraquinone (5), 2,5-dimethyl-7-hydroxyl-chromogen, (6), 2-(2'-hydroxypropyl)-5-methyl-7-hydroxytryptophan(7), 4',7-dihydroxy-5-methoxy flavone(8), chrysoeriol(9), kaempferol(10), apigenin(11), 3-methoxy quercetin(12), 6-demethoxycapillarisin(13), 7,4'-dihydroxyflavone(14), luteolin(15), butin(16), liquiritigenin(17) anderiodictyol(18). Conclusion: Compound 1 is a new compound, and 2-18 are isolated from this plant for the first time.At the moment,2-4, 8, 9, 11, 13, 14, 16-18 are isolated from Cassia for the first time.

Chemical constituents of Schoenoplectus tabernaemontani / 中草药

Objective: To study the chemical constituents of the rhizomes of Schoenoplectus tabernaemontani. Methods: Compounds were isolated and purified by a combination of column chromatography including silica gel, polyamide and Sephadex LH-20. Their structures were elucidated by physiochemical properties and NMR analysis. Results: Twelve compounds were obtained from water extract of the rhizome of S. tabernaemontani and identified as 5,7,2',4'-tetrahydroxy-3, 5'-dimethoxyflavone (1), tricin (2), hesperetin (3), quercetin (4), luteolin (5), eriodictyol (6), apigenin (7), naringenin (8), chrysin (9), 5,7-dihydroxychromone (10), catechin (11) and tricin-7-O-β-D-glucoside (12), respectively. Conclusion: Compound 1 is a new flavone named schoenin. Compounds 2-5 and 7-12 are isolated from the Cyperaceae for the first time. Compound 6 is isolated from the genus Scirpus for the first time.

Antiproliferative and photoprotective activities of the extracts and compounds from Calea fruticosa

In this paper, we complement our previous study on the antiproliferative activity of Calea fruticosa (Asteraceae) by isolating the compounds apigenin-4',7-dimethyl ether (1), budlein A (2), quercetin (3), and cichoriin (4) from the plant's aerial parts. The antiproliferative activity of these compounds was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method against human tumor cell lines. Compound 3 displayed moderate antiproliferative activity in three cell lines (HCT-116, PC-3, and SF-295, with cell growth inhibition values of 72.97, 74.55, and 68.94%) and high antiproliferative activity (90.86%) in the HL-60 cell line. The in vitro sun protection factor (SPF) of the extracts and compound 4, with and without sunscreen, was determined by a spectrophotometric method. The ethanol extract exhibited the highest SPF (9.67) at a concentration of 0.100 mg/mL, while compound 4, isolated from this extract, showed a SPF of 13.79 at the same concentration. A relative increased efficacy of SPF was observed for the extracts and compound 4 when sunscreen was also used. Compound 4 has not been reported previously from any species within the genus Calea. Compounds 1-4 were obtained from this species for the first time.

Rapid Analysis and Identification of Chemical Constituents from Siwei Tumuxiang San by HPLC-Q-Exactive-MS/MS / 中国实验方剂学杂志

Objective::To rapidly characterize and identify the components of Siwei Tumuxiang San by using high performance liquid chromatography tandem quadrupole-electrostatic field orbitrap high resolution mass spectrometry (HPLC-Q-Exactive-MS/MS). Method::Agilent ZORBAX SB-Aq column (4.6 mm×150 mm, 5 μm) was adopted and 5 mmol·L-1 ammonium acetate+ 0.1% formic acid aqueous solution-acetonitrile were used as mobile phase. According to the separation and structure identification results of chemical components based on the methods of ChemSpider and ChemicalBook database retrieval, a local database of molecular formula, molecular weight, structural formula and MS/MS spectrum information of chemical components in Siwei Tumuxiang San was established. An HPLC-Q-Exactive-MS/MS analysis method was established. The complex compounds of Siwei Tumuxiang San were identified rapidly by using Xcalibar 3.0 software, comparison of reference materials and studies on MS/MS fragment pathways. Result::A total of 110 compounds were identified from the Siwei Tumuxiang San by HPLC-Q-Exactive-MS/MS technology, including 3 sesquiterpene compounds from Inulae Radix, 16 alkaloid compunds and 38 isoprene flavonoid compounds from Sophorae Radix flavescentis, 12 triterpenoid saponin compounds, 1 catechin compounds and 4 flavonoid glycoside compounds from Rubus sachalinensis. The fragment pathways of the main types of compounds were summarized. Among them, mass spectrometry information of 31 compounds was reported for the first time. Conclusion::This study can be used to identify the target compounds and non-target compounds in Siwei Tumuxiang San systematically, accurately and quickly, which will lay a foundation for the in vivo analysis and pharmacokinetic study of the formulation.

Pollen Typhae Total Flavone Inhibits Endoplasmic Reticulum Stress-Induced Apoptosis in Human Aortic-Vascular Smooth Muscle Cells through Down-Regulating PERK-eIF2α-ATF4-CHOP Pathway / 中国结合医学杂志

OBJECTIVE@#To test the hypothesis that the inhibition of endoplasmic reticulum (ER) stress-induced apoptosis in oxidized low-density lipoproteins (ox-LDL)-induced human aortic-vascular smooth muscle cells (HA-VSMCs) was associated with suppression of the protein kinase RNA-like ER kinase (PERK)-eukaryotic translation initiation factor 2α (eIF2α)-activating transcription factor 4 (ATF4)-CCAAT/enhancer binding protein homologous protein (CHOP) signaling pathway by Pollen Typhae total flavone (PTF).@*METHODS@#Primary HA-VSMCs were cultured and identified. The cultured HA-VSMCs were randomized into 5 groups, including a normal control group, an ox-LDL group (70 μg/mL high ox-LDL), an HPTF group (70 μg/mL high ox-LDL+500 μg/mL PTF), an MPTF group (70 μg/mL high ox-LDL+250 μg/mL PTF), and a LPTF group (70 μg/mL high ox-LDL+100 μg/mL PTF) in the first part; and a normal control group, an ox-LDL group (70 μg/mL high ox-LDL), an MPTF group (70 μg/mL high ox-LDL+250 μg/mL PTF), a shRNA group (transducted with PERK shRNA lentiviral particles), a scramble shRNA group (transducted with control shRNA lentiviral particles), an MPTF+ox-LDL+shRNA group (250 μg/mL PTF+70 μg/mL high ox-LDL+PERK shRNA lentiviral particles) and an ox-LDL+shRNA group (70 μg/mL high ox-LDL+PERK shRNA lentiviral particles) in the second part. The protein expression levels of ER-associated apoptosis proteins were detected by Western blot, and their mRNA expression levels were detected by quantitative real-time reverse transcription-polymerase chain reaction. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was applied to test cell viability, and the level of apoptosis was monitored by flow cytometry.@*RESULTS@#The MTT assay and flow cytometry showed that the ox-LDL group had a significant increase in apoptosis, which was attenuated in PTF treatment groups and shRNA groups. Moreover, the ox-LDL group had increased protein and mRNA levels of binding immunoglobulin protein and ER-associated apoptosis proteins, such as PERK, eIF2α, ATF4 and CHOP, which were attenuated in PTF treatment groups and shRNA groups.@*CONCLUSIONS@#The apoptosis induced by ox-LDL had a strong relation to ER stress. The protective effect of PTF on ER stressinduced apoptosis was associated with inhibition of the PERK-eIF2α-ATF4-CHOP pathway, which might be a potential therapeutic strategy for enhancing the stability of atherosclerotic plaques.