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OBJECTIVE@#To conduct qualitative and quantitative analyses of Tripterygium hypoglaucum in Yinning Tablets, a compound preparation of traditional Chinese herbal medicine.@*METHODS@#Thin-layer chromatography (TLC) was used for qualitative analysis of Tripterygium hypoglaucum in Yining Tablets and the analytical protocols were optimized. High-performance liquid chromatography (HPLC) was used to quantitatively analyze the content of triptolide (the main active ingredient of Tripterygium hypoglaucum) in Yinning Tablets.@*RESULTS@#The results of TLC analysis showed that the test sample of Yinning Tablets and the positive control samples both produced clear, well separated spots without obvious interference in the blank samples. Assessment of the influences of the thin-layer plates from different manufacturers, temperature and humidity on the test results demonstrated good durability of the test. HPLC analysis of triptolide showed a good linear relationship within the concentration range of 1-100 μg/mL (regression equation: A=22.219C-19.165, r=0.9999); the contents of triptolide in 3 batches of Yinning tablets were 0.34, 0.34, and 0.28 μg per tablet, all within the range of 0.28-0.34 μg per tablet. It was finally determined that each Yinning tablet should not contain more than 0.6 μg of triptolide.@*CONCLUSION@#TLC and HPLC are simple, accurate, durable and specific for qualitative and quantitative analyses of Tripterygium hypoglaucum in Yinning Tablets.
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China , Chromatography, High Pressure Liquid/methods , Plant Preparations , Tablets , Tripterygium/chemistryABSTRACT
OBJECTIVE：To study the toxic effect of the extract from Tripterygium hypoglaucum on pregnant animal and embryo-fetal development . METHODS ：Successfully mated New Zealand female rabbits were randomly divided into solvent control group，positive control group （cyclophosphamide，20 mg/kg）and T. hypoglaucum extract high-dose ，medium-dose and low- dose groups（15.0，7.50，3.75 g/kg，by the amount of crude drug ）according to their body weight ，with 18 rabbits in each group at least. The female rabbits in solvent control group and T. hypoglaucum extract groups were given water or the corresponding T. hypoglaucum extract solution from 6th to 18th day of pregnancy ，5 mL/kg，once a day. Positive control group was given cyclophosphamide subcutaneously into the neck from 10th to 13th day of pregnancy ，1 mL/kg，once a day. According to the related requirements of Technical Guidelines for the Study of Drug Reproductive Toxicity ，the general situation ，body weight ，body weight increase and food intake of female rabbits were observed and recorded during the experiment ，and euthanasia was carried out on 28th day of pregnancy ；the relative indexes of main organs ，fetal uterus ，placenta uterus ，placenta，ovary，implantation gland ， absorption fetus ，stillbirth，live fetus and corpus luteum were observed and recorded after anatomy ；the relative indexes of body weight，appearance，visceral and skeletal alterations of the fetus were detected . RESULTS ：Compared with solvent control group ， the body weight ，body weight increase ，food intake ，main organs ，pregnancy of pregnant rabbits ，as well as reproductive function，embryo formation ，fetal growth and development ，appearance，visceral and skeletal development indexes in T. hypoglaucum extract groups had no significant abnormal changes （P＞0.05）；above indexes in the positive control group had significant changes （P＜0.05），and significant maternal toxicity and embryotoxicity were found. CONCLUSIONS ：T. hypoglaucum extract 15.00-3.75 g/kg（by the amount of crude drug ）have no significant maternal toxicity ，embryotoxicity or fetal development toxicity to New Zealand rabbits.
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Objective: To study the chemical constitutes from the roots of Tripterygium hypoglaucum. Methods: The chemical constituents from 95% EtOH extract of the roots of T. hypoglaucum at room temperature were isolated and prepared by Silica gel column chromatography, Sephadex LH-20 column chromatography, and semi-pre HPLC after dichloromethane extraction, and their structures were elucidated by a variety of spectral and spectroscopic techniques. Results: Six compounds were isolated and identified as 2-(5’,7’-dimethoxy-2’,2’-dimethyl-2H-benzopyran-6’-)-3-formyl-5,6-dimethoxy-benzofuran (1), 3(R)-4’,5’-dihydroxy- 2’,5,7-trimethoxy-6-(3-methyl-but-2-enyl)-isoflavan (2), 3’-geranyl-5,7,2’,5’-tetrahydroxyisoflavone (3), β-sitosterolpalmitate (4), docosanoic acid 2’,3’-dihydroxypropyl ester (5), and β-sitosterol (6). Conclusion: Compound 1 is a new compound, named as hirtellanine C. Compounds 2-5 are isolated from the plants for the first time.
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Objective: To study the chemical constituents from the rhizome of Tripterygium hypoglaucum. Methods: The concrete exacted by 95% ethanol from the rhizome of T. hypoglaucum was isolated and purified by chromatography on silica gel column chromatography, gel column chromatography, MPLC, etc. The structures of the chemical constituents were elucidated by means of NMR, MS, etc. Results: Twelve compounds were isolated and identified as 3β-hydroxy-4-hydroxymethyl-abieta-8,11,13-trien-7-one (1), 3β-acetoxy oleanolic acid (2), physcion (3), canophyllal (4), chrysophenol (5), quinone 21 (6), tripterifordin (7), triptobenzene B (8), 3,4-dimethoxyphenol (9), integracin A (10), celastrol (11), and β-sitosterol (12). Conclusion: Compound 1 is a new diterpene named tripterone, compounds 8-10 are isolated from this plant for the first time.
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Objective:Computer network pharmacology technology was used to screen the main active ingredients of Tripterygium hypoglaucum radix-Leonurus japonicus herba for the treatment of rheumatoid arthritis(RA), predict the targets of the active ingredients, establish a pharmaceutical ingredient-active ingredient-target network, and further explore the potential mechanism of Tripterygium hypoglaucum radix-Leonurus japonicus herba for the treatment of RA. Method:RA disease targets were collected through DisGeNET, TTD, and Drugbank databases, the potential active components of Tripterygium hypoglaucum radix and Leonurus japonicus herba and their corresponding targets were obtained from the Chinese Medicine System Pharmacology Analysis Platform (TCMSP); common targets for drugs and diseases were screened by using the ImageGP platform; a common target interaction (PPI) network model was constructed by using the String database, a "drug-active ingredient-key target" network was constructed by using Cytoscape software, a protein interaction network was constructed by using the String database, gene function (GO) analysis and pathway enrichment analysis based on the Kyoto Gene and Genomic Encyclopedia (KEGG) were performed by using the ClueGO plug-in. Result:Through screening, 9 active pharmaceutical ingredients were obtained, involving a total of 235 targets, and 7 active ingredients were related to the disease targets. 24 common targets for Tripterygium hypoglaucum radix Leonurus japonicus herba-disease were obtained. The common targets were mainly enriched in 278 biological processes and 141 signaling pathways to play a role in the treatment of RA. Conclusion:The therapeutic effect of Tripterygium hypoglaucum radix Leonurus japonicus herba on RA reflects the characteristics of multi-component-multi-target-multi-channel of traditional Chinese medicine, and provides a scientific basis for explaining its mechanism and clinical application of RA.
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OBJECTIVE： To study the mechanism of couplet medicine of Tripterygium hypoglaucum-Spatholobus suberectus in the treatment of rheumatoid arthritis （RA）. METHODS： The RA targets were retrieved and obtained by therapeutic target database （TTD）， DrugBank and DisGeNET databases， and the protein protein interaction （PPI） network was constructed to screen its key targets. Using oral bioavailability（OB）≥30％， drug like（DL）≥0.18 and drug half-life （HL） ≥4 h as index， active components were obtained from couplet medicine of T. hypoglaucum-S. suberectus by using TCM systematic pharmacological analysis platform （TCMSP） and TCM integrated database （TCMID）， and the targets were predicted. The active component-target network of couplet medicine of T. hypoglaucum-S. suberectus was constructed. Systems Dock Web Site online platform and Genomics platform were used to screen the active component and common targets of RA of couplet medicine of T. hypoglaucum-S. suberectus； KEGG signaling pathways of common targets were analyzed by using Cluego plug-in unit of Cytoscape 3.2.1 software. RESULTS： Totally 1 956 RA targets were retrieved， involving 11 key targets [such as IL-6， TNF， VEGFA]. The couplet medicine contained 30 active components （including luteolin， erythroxanthin， β-sitosterol and triptolide） and 229 targets. There were 37 common targets for couplet medicine of T. hypoglaucum-S. suberectus and RA （including MMP2， TNF， VEGFA）. KEGG signaling way involved cell apoptosis， IL-17 signaling pathway， Th17 cell differentiation pathway and TNF signaling pathway. CONCLUSIONS： The couplet medicine of T. hypoglaucum-S. suberectus may play a role in the treatment of RA by acting on cell apoptosis， IL-17 signaling pathway and other signaling pathways through MMP2， TNF， and VEGFA target. The results of this study can provide a reference for further study on the mechanism of the effects of couplet medicine of T. hypoglaucum-S. suberectus on RA.
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Tripterygium hypoglaucum is an endangered species in arid areas of Xiannvshan Chongqing, China. The dynamic characteristics of seed rain and soil seed bank of T. hypoglaucum were studied in this paper．Results showed that T. hypoglaucum years of mature seeds distribution number up to October; the seed rain occurred from the last ten-day of September to in the first ten-day of November and the peak of scattered seed rain concentrated in the October．The numbers of soil seed bank at 2-5 cm soil layer,mainly concentrated in the 1.5-3.5 m range. T. hypoglaucum seeds to the wind as a force for transmission, the transmission ability is strong, but in the process of natural reproduction, full mature seed rate is low, the soil seed bank seeds seed short-lived factors these were unfavorable for the natural reproduction of T. hypoglaucum population.
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OBJECTIVE:To optimize the formulation of Compound tripterygium hypoglaucum gel. METHODS:Using the comprehensive score(total score was 15.0)composed by forming property,glossiness,uniformity,viscosity,pH,spreadable prop-erty and stability as indexes,using the usage amount of carbomer 940,propylene glycol,triethanolamine and extracts in formula as study factors,orthogonal test was designed to optimized the formulation of Compound tripterygium hypoglaucum gel,and the verification test was conducted. RESULTS:The optimal matrix formulation was as follow as carbomer 9401.0 g,azone 2.0 g,so-dium bisulfite 0.4 g,extracts 50 mL,propylene glycol 10 g,triethanolamine 1.0 g,adding water to 100 g. The average comprehen-sive score of the gel in verification test was 14.8 (RSD=1.35%,n=3). CONCLUSIONS:The optimized formulation of Com-pound tripterygium hypoglaucum gel shows good forming property,the quality meets the requirements.
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This paper is aimed to develop a method for the determination of five effective components in medicinal material of Tripterygium using ultra performance liquid chromalography coupled with electrospray ionization tandem mass spectrometry(UPLC-ESI-MS/MS), which then was used to study their contents in raw materials from different areas and different sources.The separation was performed on a Waters ACQUITY UPLC-CSH-C18S column(2.1 mm×100 mm,1.7 μm), usingacetonitrile-0.2% ammonium form ateaqueous solutionas mobile phase. The target components were detected in multiple-reaction monitoring(MRM) mode by mass spectrometry with electrospray ionization (ESI) source operated in positive ionization mode. The quantitative results showed that good linearity was achieved in their respective linear ranges and fine determination coefficient (r > 0.997 8),and the overall recoveries ranged from 96.72%-103.2% with the RSD ranging from 1.0%-2.4%.The method is sensitive and accurate, and suitable for the effective components quantification in medicinal material of Tripterygium; contents of five effective components from different sources vary significantly, so the quality and safety of medicinal material of Tripterygium needs to be improved. It is very important to control the quality with multi-index for clinic safety.
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Using six kinds of ionic liquids as extractants, ultrasonic-assisted extraction coupled with HPLC method was developed for the simultaneous determination of wilforgine, wiforizine, triptophenolide, wilforine and triptoquinone A in Tripterygium hypoglaucum. The separation was performed on an Inertsil ODS-4 column with the mobile phase of acetonitrile-0.1% phosphoric acid in gradient elution at a flow rate of 0.75 mL•min⁻¹. Detection wavelength was 220 nm and the column temperature was 30℃. Under the optimal extractions, the results showed that triptophenolide and triptoquinone A had the highest extraction yield by using 0.6 mol•L⁻¹ [BMIm]PF6 methanol solution as extraction solvent with the solid-liquid ratio of 1∶10. The calibration curves of triptophenolide and triptoquinone A showed a good linearity in the range of 0.000 65-0.026, 0.066 55-2.662 μg (r=0.999 9)respectively. The average recovery was 102.4% and 97.90% with RSD of 2.5% and 1.5%, respectively. Wilforgine, wiforizine and wilforine had the highest extraction yield when using 0.6 mol• L⁻¹ [BMIm]PF6absolute ethanol solution as extraction solvent with the solid-liquid ratio of 1∶10. The content of wilforgine, wiforizine and wilforine from 0.023 9-0.956, 0.002 7-0.108, 0.006 4-0.256 μg showed a good linearity (r=0.999 9), and the average recovery was 100.6%,99.50% and 98.70% with RSD of 2.1%,1.9% and 2.7%, respectively. The results indicated that this method is convenient, reliable and green, and can be used as a reliableanalytical method for the quality control of T.hypoglaucum.
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Objective: To establish a method suitable to the quality evaluation of the roots in Tripterygium wilfordii based on hepatotoxic potency. Methods: The inhibitory rates of T. wilfordii and its regional substitute-T. hypoglaucum, with normal human hepatocytes (L02 cell line) as carrier, were established by optimizing a series of factors, such as test samples prepared with conditions. Results: Taking p-acetaminophenol as positive control (toxic potency was 400 U/g), The 50% ethanol extract of T. wilfordii was dried under ultrasonic vacuum to obtaine the dry paste. The test solution with crude drug of 3 mg/mL was prepared by medium. The dilution ratio was 1:0.65. The hepatotoxic potencies of 18 batches of T. wilfordii and 5 batches of T. hypoglaucum were 17.78-4131.4 and 209.42-7422.2 U/g, respectively, detected by the reaction parallel line method, and the differences were over 200 and 30 times. There was the significant hepatotoxic potency of T. wilfordii and T. hypoglaucum from the various origins. In addition, the fresh collected samples had the larger hepatotoxic potency than that in the dried samples collected in the market. Conclusion: The preliminarily established hepatotoxic potency bioassay is useful to evaluate the quality of T. wilfordii which directs the correlation with the drug's hepatotoxic adverse effect in clinic. The method can provide the reference for the clinical safety use of T. wilfordii based on the quality control and be as the quantitative method used to screen the toxic components from T. wilfordii.
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Tripterygium hypoglaucum (THH) is a folk medicine with important medicinal property, used in the treatment of cataciasis, arthritis, and cancer. The principal chemical constituents of THH are diterpene, triterpene, and sesquiterpene alkaloids, and there are also flavonoid, steroid, tannin, and glucide in it. Diterpene and alkaloids are the major active ingredients. THH has various pharmacological effects such as anti-inflammation, antitumor, immunosuppressive activity, antiviral effect, and so on. It is usually used to treat rheumatiod arthritis, psoriasis, and chronic urticarial. In this paper, we summarize the chemical composition, pharmacological activity, and clinical application of THH, for reference to study and utilize it.
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Objective To observe the effect of different regions of tripterygium hypoglaucum (Lévl.) hutch on macrophage inflammatory factor, and to providetheoretical basis and experimental basis for the clinical application of tripterygium hypoglaucum (Lévl.) hutch. Methods 5 batches of tripterygium hypoglaucum (Lévl.) hutch were collected, then the samples turned into alcohol extract by extraction and isolation. The IC50 values of alcohol extracts were measured by MTT in BMDM cell. B MDM cell were induced by the 5 batches of samples with IC50, then IL-6, IL-10, iNOS were detected by Elisa. The efficacy of different regions of tripterygium hypoglaucum (Lévl.) hutch on macrophage inflammatory factor was evaluated by comparison with sulfasalazine. Results The content of IL-6 (4.22 ± 0.38 pg/ml, 4.55 ± 0.44 pg/ml vs.7.92 ± 0.84 pg/ml) and iNOS (0.07 ± 0.04 ng/ml, 0.28 ± 0.10 ng/ml vs. 0.86 ± 0.13 ng/ml) in HuNan and ZheJiang groups were significantly lower than sulfasalazine (P<0.05), and the content of IL-10 (19.34 ± 6.06 pg/ml, 24.34 ± 3.03 pg/ml vs. 9.06 ± 0.40 pg/ml) in Guizhou and Fujian groups were higher than sulfasalazine (P<0.05). Conclusion The anti-inflammatory effect of HuNan and ZheJiang's tripterygium hypoglaucum (Lévl.) hutch treat rheumatoid arthritis is better than sulfasalazine, so theyaregenuine regional drug in the treatment of rheumatoid arthritis. Additional research will analyze associations between tripterygium hypoglaucum (Lévl.) hutch and rheumatoid arthritis.
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[ ABSTRACT] AIM:To investigate the effect of tripterygium hypoglaucum Hutch ( THH) on collagen-induced ar-thritis ( CIA) in rats and its possible mechanism.METHODS:SD rats were randomly divided into normal group and CIA group.The rat model of type II CIA was successfully established and the model rats were randomly divided into 4 different groups:model group, dexamethasone group, THH (200 mg/kg) group, and THH (400 mg/kg) group.The contents of IL-12, IL-23 and IL-37 in the serum and foot paws of the CIA rats were detected by ELISA.The histopathological changes of the skin of the food paws were observed by HE staining.The protein expression of MMP-13 was determined by Western blot.The MMP-13 activity in the foot paws was detected by fluorescence labeling method.RESULTS:Compared with CIA group, THH at dose of 400 mg/kg significantly reduced the weight loss in typeⅡCIA rats ( P<0.01 ) .THH at dose of 400 mg/kg obviously decreased the contents of IL-12 by 28.31%, IL-23 by 41.57%in the serum and IL-12 by 30.78%, IL-23 by 39.46%in the foot paws, while IL-37 was significantly increased by 79.43% in the serum and 75.78% in the foot paws ( P<0.01) .The pathological changes of the subcutaneous tissues were improved by treating with THH (400 mg/kg).The protein expression of MMP-13 was significantly decreased by 31.82%(P<0.01), and the MMP-13 activity was also reduced.THH at dose of 200 mg/kg had no obvious improvement on the above indexes.CONCLUSION:THH has significant inhibitory effect on rat CIA by reducing the content of proinflammatory cytokines IL-12 and IL-23, increasing the content of anti-inflammatory factor IL-37, inhibiting inflammatory cell infiltration and vascular proliferation, and attenuating the protein expression of MMP-13 and MMP-13 activity in rats.
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This article was aimed to study the latest research progress of Tripterygium hypoglaucum, in order to pro-vide references for further research on T. hypoglaucum. CNKI Chinese Journal Full-text Database was used as data source. Bibliometric analysis was conducted on T. hypoglaucum research articles issued from 1915~2013. Bibliometric method was used in the analysis on the change trend among years, research institutes, publication dates, research per-sonnels and research topics of the articles with the built-in analysis tools and network analysis tools. The results indi-cated that T. hypoglaucum research was still in the development stage. And there is still plenty of room for growth in aspects including resources, material basis, manufacturing pharmacy and so on.
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Objective To find antitumor cOnstituents from Tripterygium hypoglaucum.Methods The chloroform extract of T.hypoglaucum was separated by silica gel column chromatography and preparative HPLC.The structures of compounds isolated were identified by spectral analysis and chemical evidence.Results Seven compounds were isolated and identified as rhein ethyl ester(1),chrysophenol(2),physcion(3),emodin(4),wilfordine(5),wilforgine(6),and wilforine(7).The cytotoxic activities of the compounds against cancer cell lines were assayed.Conclusion Compound 1 is a new natural compound with strong activities against human cancer cell lines (A2780 and OVCAR-3).Compounds 2-4 are isolated from this genus plants for the first time.The possible structure-activity relationship among compounds 1-4 shows that the methoxy group or oxyethyl moiety might be responsible for the cytotoxity.
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Herpes simplex virus type 1 (HSV-1) is a commonly occurring human pathogen worldwide. There is an urgent need to discover and develop new alternative agents for the management of HSV-1 infection. Tripterygium hypoglaucum (level) Hutch (Celastraceae) is a traditional Chinese medicine plant with many pharmacological activities such as anti-inflammation, anti-tumor and antifertility. The usual medicinal part is the roots which contain about a 1% yield of alkaloids. A crude total alkaloids extract was prepared from the roots of T. hypoglaucum amd its antiviral activity against HSV-1 in Vero cells was evaluated by cytopathic effect (CPE) assay, plaque reduction assay and by RT-PCR analysis. The alkaloids extract presented low cytotoxicity (CC_(50) = 46.6 μg/mL) and potent CPE inhibition activity, the 50% inhibitory concentration (IC_(50)) was 6.5 μg/mL, noticeably lower than that of Acyclovir (15.4 μg /mL). Plaque formation was significantly reduced by the alkaloids extract at concentrations of 6.25 μg/mL to 12.5 μg/mL, the plaque reduction ratio reached 55% to 75% which was 35% higher than that of Acyclovir at the same concentration. RT-PCR analysis showed that, the transcription of two important delayed early genes UL30 and UL39, and a late gene US6 of HSV-1 genome all were suppressed by the alkaloids extract, the expression inhibiting efficacy compared to the control was 74.6% (UL30), 70.9% (UL39) and 62.6% (US6) respectively at the working concentration of 12.5μg/mL. The above results suggest a potent anti-HSV-1 activity of the alkaloids extract in vitro.
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To study the efficacy and the mechanism of Colquhoumia root (Tripterygium hypoglaucum (Le,vL)Hutch) in the treatment of mesangial proliferation glomerulonephritis (MsPGN), SD rats were injected with anti-thymocyte serum (ATS) to make MsPGN model (anti-Thy1 model). The rats were then divided into 3 groups: normal control group, anti-Thy1 model group and treatment group. Histopathological (HE, PAS), immunohistochemical, RT-PCR technique and computer imaging analysis system were used to evaluate mesangial matrix production, the expression of TGF-β1 protein and mRNA in the tissues of kidney.Our result showed that proteinuria and the ratio of extracellular matrix/glomerular capillaries area (ECM/CA) were increased significantly in model group. The expression of both TGF-β1 protein and mRNA in glomeruli was much higher in model group than in control group (P<0.01). After the treatment with Colquhoumia root, proteinuria, ECM/CA and the expression of both TGF-β1 protein and mRNA in glomeruli were significantly decreased in treatment group as compared with those in model group. It is concluded that Colquhoumia root is effective in reducing proteinuria and mesangial matrix proliferation in MsPGN and it may achieve these effects by inhibiting the expressions of TGF-β1 protein and mRNA of mesangial cells.
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Objective To study the effects of the cytotoxicity, cell cycle and time dependent apoptosis of Jurkat T lymphoma cells induced by Tripterygium Hypoglaucum (Levl) Hutch (THH) alkaloids so ad to explore the mechanisms of the apoptosis induced by the THH alkaloids. Methods Cell vitality and cell proliferation were measured by Typan blue staining. Cell cycle and the time dependent apoptosis were determined by DNA staining, TUNEL labeling and flow cytometry. Results THH alkaloids could effectively inhibit cell proliferation of Jurkat cells and induce the G 1 arrest and could induce apoptosis in G 2/S phase first and then G 1 phase. Conclusion THH alkaloids can inhibit DNA synthesis, cell proliferation and can also induce apoptosis of Jurkat T lymphoma cells in all phases.
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Objective To investigate the effects of Tripterygium Hypoglaucum (Levl) Hutch alkaloids on the nuclear DNA strand breaks and DNA fragmantation in Jurkat T lymphoma cells to understand the mechanisms of the apoptosis. Methods After Jurkat cells were induced by the alkaloids, DNA stand breaks were labeled by TUNEL assay and DNA fragmentation was analyzed by DNA content analysis. Flow cytometry was performed to determine these phenomena. Results THH alkaloids could effectively induce DNA stand breaks and DNA fragmentation. Conclusion There are great changes in nuclear DNA in the apoptosis of Jurkat T lymphoma cells induced by THH alkaloids.