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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: 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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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.
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Objective To explore the roles of [Ca 2+ ]i in the apoptosis of Jurkat cells induced by Tripterygium Hypoglaucum (Levl) Hutch alkaloids. Methods After Jurkat cells were stained with Indo 1 AM and PI, changes of [Ca 2+ ]i were assessed by flow cytometry at the single cell level. Results THH alkaloids could induce no changes of [Ca 2+ ] inside cytoplasm. Conclusion THH alkaloids induce the apoptosis of Jurkat cells via other pathways rather than via the [Ca 2+ ] pathway.
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Objective To explore the acute toxicity and LD 50 of Tripterygium Hypoglaucum (Levl) Hutch(THH) solution to provide information for safe clinical application. Methods After oral administration of THH solution in mice, the mortality and the physiological and pathological changes were observed. Results The LD 50 (95% confidence limit) of THH in male and female mice was 79 g/kg(69～89 g/kg) and 100 g/kg (90～112 g/kg), respectively. No marked pathological change of the organs was found. Conclusion According to the standard of grading of acute toxicity, THH solution belongs to the moderate class. Therefore, it is safe in clinical practice and has a wide application.
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Objective To study the effects of Tripterygium Hypoglaucum Hutch(THH) and its extract(THW-4) on neointimal formation of rabbit carotid arteries after balloon angioplasty.Methods After injury of the common carotid arteries was set up by balloon angioplasty,the rabbits were divided into 3 groups and were given different treatment protocol including gastrogarage of THH(n=9),associated gastrogavage of THH with local administration of THW-4 into the injured arteries(n=9) and 0.25% DMSO saline local administration as the control(n=9).Neointimal fomation was evaluated on days after the procedure by proliferating all nuclear antigen(PCNA) and Evans Blue staining,and quantitative histomorphometric analysis was performed on 28 days.Results The PCNA-positive index in the neointima at day 14 after the procedure was reduced in the THH gastrogavage group and the THH/THW-4 group compared with the control(17.68%?5.27%,6.60%?2.52% vs 40.37%?7.12%,P