- 1. Cytotoxicity screening of several tomato extracts.
The cytotoxic effects of extracts of the tomato variety "Racimo" have been evaluated through the use of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay at several concentrations. Three extracts-ethanol-water, petroleum ether, and in vitro digested tomato-exhibited in vitro cytotoxicity against the proliferation of the cultured cancer cell line HT-29. The concentration that caused 50% inhibition of cancer cell growth occurred (GI(50)) of the different extracts for HT-29 cells was 62.5 μg/mL for the petroleum ether extract and 87.0 μg/mL for the digested tomato extract. For the ethanol-water extract, it was not possible to determine this parameter at the assayed extract concentrations. These results clearly indicate that after the digestion process, the less polar substances, such as carotenoids and sterols, are bioavailable as active species against cancer cells. The GI(50) levels for tomato extracts are similar to those values reported for medicinal plants. The results of the MTT assay on nonmutagenic CCD-18 cells showed a lack of negative effect on cell growth, which indicates that tomato extracts act selectively on HT-29 tumor cells. (1)H-Nuclear magnetic resonance spectra confirmed the presence of known compounds with accepted cytotoxic activity against tumor lines (lycopene and β-carotene). The high cytotoxicity for HT-29 cells showed by the petroleum ether extract might be due to the simultaneous presence in the extract of both carotenoids and glyceryl esters of fatty acids. The results of this work clearly indicate the importance of carotenoid consumption on colon tumor proliferation and prevention, and also the importance of the dietary fats in carotenoid bioavailability....(more)
Guil-Guerrero JL, et al. J Med Food 2011 Jan-Feb;14(1-2):40-5.
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- 2. Effects and Mechanism of Action of a Tribulus terrestris Extract on Penile Erection.
PURPOSE:
Tribulus terrestris has been used as an aphrodisiac. However, little is known about the effects and mechanism of action of T. terrestris on penile erection. Therefore, the effect of a T. terrestris extract and the mechanism of action of the extract on relaxation of the corpus cavernosum (CC) were investigated. The erectogenic effects of an oral preparation of the extract were also assessed.
MATERIALS AND METHODS:
The relaxation effects and mechanism of action of the T. terrestris extract on rabbit CC were investigated in an organ bath. The intracavernous pressure (ICP) was calculated after oral administration of the extract for 1 month to evaluate whether the relaxation response of the CC shown in the organ bath occurred in vivo. Additionally, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) were measured in the CC by immunoassay. Smooth muscle relaxation was expressed as the percentage decrease in precontraction induced by phenylephrine. The ICP was also assessed in rats after oral administration of the extract for 1 month, and changes in concentrations of cGMP and cAMP were monitored.
RESULTS:
Concentration-dependent relaxation effects of the extract on the CC were detected in the organ bath study. Relaxation of the CC by the T. terrestris extract was inhibited in both an endothelium-removed group and an L-arginen methyl ester pretreatment group. The ICP measured after oral administration of the T. terrestris extract for 1 month was higher than that measured in the control group, and a significant increase in cAMP was observed in the T. terrestris extract group.
CONCLUSIONS:
The T. terrestris extract induced concentration-dependent relaxation of the CC in an organ bath. The mechanism included a reaction involving the nitric oxide/nitric oxide synthase pathway and endothelium of the CC. Moreover, in an in vivo study, the T. terrestris extract showed a significant concentration-dependent increase in ICP. Accordingly, the T. terrestris extract may improve erectile function....(more)
Do J, et al. Korean J Urol 2013 Mar;54(3):183-8.
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- 3. Alternative treatment of ovarian cysts with Tribulus terrestris extract: a rat model.
Tribulus terrestris has long been used in traditional medicine to treat impotency and improve sexual functions in man. The aim of this study was to evaluate the efficiency of T. terrestris extract in the treatment of polycystic ovary (PCO) in Wistar rat. Estradiol valerate was injected to 15 mature Wistar rats to induce PCO. Rats were randomly divided into three groups (control, low-dose and high-dose groups) of five each and received 0, 5 and 10 mg of T. terrestris extract, respectively.Treatments began on days 50 and 61 after estradiol injection; at the same time, vaginal smear was prepared. The ovaries were removed on day 62, and histological sections were prepared accordingly. The number and diameter of corpora lutea, thickness of the theca interna layer and the number of all follicles were evaluated in both ovaries. In comparison with the control group, the number of corpora lutea and primary and secondary follicles significantly increased following T. terrestris treatment; however, the number of ovarian cysts significantly decreased. It can be concluded that T. terrestris have a luteinizing effect on ovarian cysts, which may relate to its gonadotropin-like activity; also, a high dose of the extract can efficiently remove ovarian cysts and resume ovarian activity....(more)
Dehghan A, et al. Reprod Domest Anim 2012 Feb;47(1):e12-5.
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- 4. Influence of Tribulus terrestris on testicular enzyme in fresh water ornamental fish Poecilia latipinna.
The influence of Tribulus terrestris on the activities of testicular enzyme in Poecilia latipinna was assessed in lieu of reproductive manipulation. Different concentrations of (100, 150, 200, 250, and 300 mg) Tribulus terrestris extract and of a control were tested for testicular activity of enzymes in Poecilia latipinna for 2 months. The testis and liver were homogenized separately in 0.1 mol/l potassium phosphate buffer (0.1 mol/l, pH 7.2). The crude homogenate was centrifuged, and supernatant obtained was used as an enzyme extract for determination of activities. The activities of testicular functional enzyme ALP, ACP, SDH, LDH, and G6PDH levels were changed to different extent in treated groups compared with that of the control. The total body weight and testis weight were increased with the Tribulus terrestris-treated fish (Poecilia latipinna). These results suggest that Tribulus terrestris induced the testicular enzyme activity that may aid in the male reproductive functions. It is discernible from the present study that Tribulus terrestris has the inducing effect on reproductive system of Poecilia latipinna....(more)
Kavitha P, et al. Fish Physiol Biochem 2011 Dec;37(4):801-7.
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- 5. Hepatoprotective activity of Tribulus terrestris extract against acetaminophen-induced toxicity in a freshwater fish (Oreochromis mossambicus).
The potential protective role of Tribulus terrestris in acetaminophen-induced hepatotoxicity in Oreochromis mossambicus was investigated. The effect of oral exposure of acetaminophen (500 mg/kg) in O. mossambicus at 24-h duration was evaluated. The plant extract (250 mg/kg) showed a remarkable hepatoprotective activity against acetaminophen-induced hepatotoxicity. It was judged from the tissue-damaging level and antioxidant levels in liver, gill, muscle and kidney tissues. Further acetaminophen impact induced a significant rise in the tissue-damaging level, and the antioxidant level was discernible from the enzyme activity modulations such as glutamate oxaloacetic transaminase, glutamate pyruvic transaminase, alkaline phosphatase, acid phosphatase, glucose-6-phosphate dehydrogenase, lactate dehydrogenase, superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, glutathione S-transferase, lipid peroxidase and reduced glutathione. The levels of all these enzymes have significantly (p < 0.05) increased in acetaminophen-treated fish tissues. The elevated levels of these enzymes were significantly controlled by the treatment of T. terrestris extract (250 kg/mg). Histopathological changes of liver, gill and muscle samples were compared with respective controls. The results of the present study specify the hepatoprotective and antioxidant properties of T. terrestris against acetaminophen-induced toxicity in freshwater fish, O. mossambicus....(more)
Kavitha P, et al. In Vitro Cell Dev Biol Anim 2011 Dec;47(10):698-706.
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- 6. Diminution of oxalate induced renal tubular epithelial cell injury and inhibition of calcium oxalate crystallization in vitro by aqueous extract of Tribulus terrestris.
PURPOSE:
Recurrence and persistent side effects of present day treatment for urolithiasis restrict their use, so an alternate solution, using phytotherapy is being sought. The present study attempted to evaluate the antilithiatic properties of Tribulus terrestris commonly called as "gokhru" which is often used in ayurveda to treat various urinary diseases including urolithiasis.
MATERIALS AND METHODS:
The activity of Tribulus terrestris was investigated on nucleation and the growth of the calcium oxalate (CaOx) crystals as well as on oxalate induced cell injury of NRK 52E renal epithelial cells.
RESULTS:
Tribulus terrestris extract exhibited a concentration dependent inhibition of nucleation and the growth of CaOx crystals. When NRK-52E cells were injured by exposure to oxalate for 72 h, Tribulus terrestris extract prevented the injury in a dose-dependent manner. On treatment with the different concentrations of the plant, the cell viability increased and lactate dehydrogenase release decreased in a concentration dependent manner.
CONCLUSION:
The current data suggests that Tribulus terrestris extract not only has a potential to inhibit nucleation and the growth of the CaOx crystals but also has a cytoprotective role. Our results indicate that it could be a potential candidate for phytotherapy against urolithiasis....(more)
Aggarwal A, et al. Int Braz J Urol 2010 Jul-Aug;36(4):480-8; discussion 488, 489.
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- 7. Influence of Tribulus terrestris extract on lipid profile and endothelial structure in developing atherosclerotic lesions in the aorta of rabbits on a high-cholesterol diet.
The aim of this study was to investigate the pleotropic effects of an extract of a traditional herb, Tribulus terrestris (TT), on the lipid profile and vascular endothelium of the abdominal aorta in New Zealand rabbits fed a cholesterol-rich diet. Eighteen rabbits were randomly divided into three groups (n=6 for each). One experimental group (EG-I) was given a cholesterol-rich diet, a second experimental group (EG-II) was treated with TT following a cholesterol-rich diet, and a control group (CG) was fed a standard diet. Blood samples were collected on day 0 and then at weeks 4 and 12 to determine total serum cholesterol (TC), high density lipid-cholesterol (HDL-C), low density lipid-cholesterol (LDL-C) and triglyceride (TG) levels. Tissues were collected from the abdominal aorta for immunohistochemistry and transmission and scanning electron microscopy. In EG-II, the serum lipid profile was significantly lower than that of EG-I at week 12 with a reduction of TC: 65%; LDL-C: 66%; HDL-C: 64%; TG: 55%. Ultrastructural analysis revealed that endothelial damage was more prominent in EG-I compared to EG-II. The ruptured endothelial linings and damaged cellular surfaces increased in EG-I compared to EG-II. Our data indicate that dietary intake of TT can significantly lower serum lipid profiles, decrease endothelial cellular surface damage and rupture and may partially repair the endothelial dysfunction resulting from hyperlipidemia....(more)
Tuncer MA, et al. Acta Histochem 2009;111(6):488-500.
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- 8. The influence of the Tribulus terrestris extract on the parameters of the functional preparedness and athletes' organism homeostasis.
The influence of the Tribulus terrestris extract on the parameters of the functional preparadness and athletes' organism homeostase was investigated. It was established the positive impact of dietary supplement "Tribulus" (Optimum Nutrition, U.S.A.) using per 1 capsule 3 times a day during 20 days on athletes' physical power in various energy producing zones: anaerobic alactic muscular power and anaerobic alactic glycolytic power statistically reliable increased. Tribulus terrestris extract, after 20 days of consuming it, did not have essential effect on erythrocytes, haemoglobin and thrombocytes indices. During the experimental period statistically importantly increased percentage of granulocytes and decreased percentage of leucocytes show negative impact of this food supplement on changes of leucocytes formula in athletes' blood. Creatinkinase concentration in athletes' blood statistically importantly has increased and creatinine amount has had a tendency to decline during 20 days period of consuming Tribulus terrestris extract. The declining tendency of urea, cholesterol and bilirubin concentrations has appeared. The concentration of blood testosterone increased statistically reliable during the first half (10 days) of the experiment; it did not grow during the next 10 days while consuming Tribulus still....(more)
Milasius K, et al. Fiziol Zh 2009;55(5):89-96.
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- 9. The analgesic effect of Tribulus terrestris extract and comparison of gastric ulcerogenicity of the extract with indomethacine in animal experiments.
Tribulus terrestris has been used in traditional medicine for relieving rheumatic pain and as an analgesic plant for a long time. In this investigation the analgesic effect of methanolic extract of this plant on male albino mice was evaluated by formalin and tail flick test. Extraction of the fruits of the plant was done by two different methods (suxheletion and percolation) with methanol 80%. The percolated extract was injected intraperitoneally in mice at 50, 100, 200, 400, and 800 mg/kg. The results showed that a dose of 100 mg/kg of percolated extract had the highest significant analgesic effect compared to the control group (P < 0.01) in formalin and tail flick test. There is no significant difference in the analgesic effect of suxheleted and percolated extract. The analgesic effect of the extract was lower than morphine, 2.5 mg/kg in both tests, and higher than ASA 300 mg/kg in chronic phase of pain in formalin test (P < 0.05). Pretreatment of animal with naloxone did not change the analgesia induced by the plant extract in both tests, therefore the involvement of opioid receptor in the analgesic effect of this plant was excluded. The results of ulcerogenic studies indicate that the gastric ulcerogenecity of plant extract is lower than the indomethacin in the rat's stomach. It can therefore be concluded that T. terrestris extract has a suitable analgesic effect and further studies are required to produce a more effective product of this plant to substitute for conventional analgesic drugs....(more)
Heidari MR, et al. Ann N Y Acad Sci 2007 Jan;1095:418-27.
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- 10. Antinociceptive and anti-inflammatory effects of orally administrated denatured naja naja atra venom on murine rheumatoid arthritis models.
To investigate the antinociceptive and anti-inflammatory activities of the denatured Naja Naja atra venom (NNAV) in rheumatoid arthritis-associated models, the denatured NNAV (heat treated; 30, 90, 270 μ g/kg), the native NNAV (untreated with heat; 90 μ g/kg), and Tripterygium wilfordii polyglycoside (TWP, 15 mg/kg) were administrated orally either prophylactically or therapeutically. We measured time of licking the affected paw in formaldehyde-induced inflammatory model, paw volume in egg-white-induced inflammation, and granuloma weight in formalin-soaked filter paper-induced granuloma. For adjuvant-induced arthritis (AIA) rats, paw edema, mechanical withdrawal threshold, serum levels of TNF- α and IL-10, and histopathological changes of the affected paw were assessed. We found that the denatured NNAV (90, 270 μ g/kg) significantly reduced time of licking paw, paw volume, and granuloma weight in above inflammatory models and also attenuated paw edema, mechanical hyperalgesia, and histopathology changes in AIA rats. Additionally, the increase in serum TNF- α and the decrease in serum IL-10 in AIA rats were reversed by the denatured NNAV. Although the native NNAV and TWP rendered the similar pharmacological actions on the above four models with less potency than that of the denatured NNAV, these findings demonstrate that oral administration of the denatured NNAV produces antinociceptive and anti-inflammatory activities on rheumatoid arthritis....(more)
Zhu KZ, et al. Evid Based Complement Alternat Med 2013;2013:616241.
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- 11. Herbal preparations for uterine fibroids.
BACKGROUND:
Uterine fibroids are the most common non-malignant growths in women of childbearing age. They are associated with heavy menstrual bleeding and subfertility. Herbal preparations are commonly used as alternatives to surgical procedures.
OBJECTIVES:
To evaluate the effectiveness and safety of Chinese herbal medicine for treatment of uterine fibroids.
SEARCH METHODS:
The authors with the guidance of the Trials Search Coordinator searched the following electronic databases: the Trials Registers of the Cochrane Menstrual Disorders and Subfertility Group and the Cochrane Complementary Medicine Field, the Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library 2012, Issue 4), MEDLINE, EMBASE, the Chinese Biomedical Database, the Traditional Chinese Medical Literature Analysis and Retrieval System (TCMLARS), AMED, and LILACS. The searches were up to 11 September 2012.
SELECTION CRITERIA:
Randomised controlled trials comparing herbal preparations with no intervention, placebo, medical treatment, or surgical procedures in women with uterine fibroids. We included trials of herbal preparations with or without conventional therapy.
DATA COLLECTION AND ANALYSIS:
Two review authors collected data independently. We assessed trial risk of bias according to our methodological criteria. We presented dichotomous data as risk ratios (RR) and continuous outcomes as mean differences (MD), both with 95% confidence intervals (CI).
MAIN RESULTS:
We included 21 randomised trials (involving 2222 women) and the majority of them had unclear or high risk of bias. There were several different herbal preparations used within the included trials. The average treatment duration was three to six months. The primary outcome of uterine fibroid related symptoms was not reported in any of the included trials. The majority of the trials reported fibroid volume and size of the uterus.Compared with mifepristone, Tripterygium wilfordii extract was associated with a greater reduction in the fibroid volume (MD -23.03 cm(3), 95% CI -28.39 to -17.67; 2 trials) and in uterine size (MD -51.25 cm(3), 95% CI -77.70 to -24.80; 2 trials). There was no evidence of a significant difference between Nona Roguy herbal product and gonadotropin-releasing hormone (GnRH) agonist on the average fibroid volume or the uterine size. The combination of Guizhi Fuling formula and mifepristone was associated with a greater reduction in the fibroid volume (-1.72 [-2.42, -1.02] 7 trials) and in uterine size (MD -31.63 [95% CI -54.58, -8.68] 3 trials)) compared with mifepristone alone. Only 13/21 trials reported on adverse events and no serious adverse effects from herbal preparations were reported.
AUTHORS' CONCLUSIONS:
Current evidence does not support or refute the use of herbal preparations for treatment of uterine fibroids due to insufficient studies with large sample sizes and of high quality. Further high quality trials evaluating clinically relevant outcomes are warranted....(more)
Liu JP, et al. Cochrane Database Syst Rev 2013 Apr 30;4:CD005292.
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- 12. Celastrol protects human neuroblastoma SH-SY5Y cells from rotenone-induced injury through induction of autophagy.
Celastrol, an active component found in the Chinese herb tripterygium wilfordii has been identified as a neuroprotective agent for neurodegenerative diseases including Parkinson's disease (PD) through unknown mechanism. Celastrol can induce autophagy, which plays a neuroprotective role in PD. We tested the protective effect of celastrol on rotenone-induced injury and investigated the underlying mechanism using human neuroblastoma SH-SY5Y cells. The SH-SY5Y cells were treated with celastrol before rotenone exposure. The cells survival, apoptosis, accumulation of α-synuclein, oxidative stress and mitochondrial function, and autophagy production were analyzed. We found celastrol (500nM) pre-treatment enhanced cell viability (by 28.99%, P<0.001), decreased cell apoptosis (by 54.38%, P<0.001), increased SOD and GSH (by 120.53% and 90.46%, P<0.01), reduced accumulation of α-synuclein (by 35.93%, P<0.001) and ROS generation (by 33.99%, P<0.001), preserved MMP (33.93±3.62%, vs. 15.10±0.71% of JC-1 monomer, P<0.001) and reduced the level of cytochrome C in cytosol (by 45.57%, P<0.001) in rotenone treated SH-SY5Y cells. Moreover, celastrol increased LC3-II/LC3 I ratio by 60.92% (P<0.001), indicating that celastrol activated autophagic pathways. Inhibiting autophagy by 3-methyladenine (3-MA) abolished the protective effects of celastrol. Our results suggested that celastrol protects SH-SY5Y cells from rotenone induced injuries and autophagic pathway is involved in celastrol neuroprotective effects.
Copyright © 2013. Published by Elsevier Ltd....(more)
Deng YN, et al. Neurochem Int 2013 Apr 23.
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- 13. [Differential expressions of miRNAs in kidney in puromycin aminonucleoside nephropathy model and intervened effects of Leizhi capsule].
OBJECTIVE:
To observe the differential expression characteristics of microRNAs (miRNAs) in renal tissues in puromycin aminonucleoside (PAN) nephritic model, and its relationship with key structural molecules of slid diaphragm (SD) nephrin and podocin and expression of skeleton protein synaptopodin; and to explore the in vivo mechanisms of Leizhi capsule (LZC) for ameliorating the expressions of nephrin, podocin and synaptopodin and reducing proteins by regulating the modal rat renal tissues miRNAs.
METHOD:
Fifty male Wistar rats were randomly divided into five groups: the control group (A), the model group (B), the LZC-treated group (C), the multi-glycoside of Tripterygium wilfordii (GTW)-treated group (D) and the valsartan-treated group (E). Apart from group A, all of rats in the remaining groups are injected with PAN (100 mg x kg(-1)) through jugular veins to establish the PAN nephropathy model. On the 2nd day after PAN nephropathy model was established, group C was orally administered with LZC (5 mL x kg(-1) x d(-1)) in group C, group DGTW (10 mL x kg(-1) x d(-1)), and E group valsartan (7.5 mL x kg(-1) x d(-1)), while groups A and B were intervened with physiological saline, for 10 days. Body weight and 24 h urinary protein ration (Upro) in all rats were measured at day 0, 3, and 9. All rats were sacrificed at day 11 after the establishment of the model, and their blood and renal tissues were collected to observe such blood biochemical indicators including albumin (Alb), serum creatinine (Scr), blood urea nitrogen (BUN) and glomerular ultrastructure (podocyte foot process form) and expressions of dicer enzyme, nephrin, podocin and synaptopodin in renal tissues. Meanwhile, the differential expressional characteristics of miRNAs in renal cortex were analyzed by biochip assay. Additionally, the differential expressional volumes of rno-miR-23a, rno-miR-300-3p, rno-miR-24 and rno-miR-30c were measured by real-time PCR.
RESULT:
Proteinuria, renal dysfunction, hypoproteinemia and podocyte foot process fusion were investigated in model rats induced by PAN. In renal tissues of PAN nephropathy model rats, dicer enzyme affected the expressions of nephrin, podocin and synaptopodin in podocytes, up-regulated the expressions of rno-miR-23a and rno-miR-300-3p, and down-regulated the expressions of rno-miR-24 and rno-miR-30c. The miRNAs with differential expressions included rno-miR-24, rno-miR-30c, rno-miR-23a and rno-miR-300-3p. LZC could improve the general state, proteinuria, serum BUN and podocyte foot process fusion of PAN nephropathy model rats, reduced the expressions of dicer enzyme, increased the expressions of nephrin, podocin and synaptopodin in podocytes, weakened the up-regulated rno-miR-23a and rno-miR-300-3p, and strengthened the down-regulated rno-miR-24 and rno-miR-30c in renal tissues.
CONCLUSION:
PAN in vivo impacts the expressions of miRNAs in renal tissues, intervenes the expressions of nephrin, podocin and synaptopodin in podocytes, damages podocyte structures and functions and generates proteinuria by means of differential expression of dicer enayme/miRNAs. LZC can reduce proteinuria in PAN nephropathy model rats. Its mechanism may intervene dicer enayme/miRNAs differential expression, regulate nephrin, podocin and synaptopodin in podocytes and improve podocyte structures and functions....(more)
Sun W, et al. Zhongguo Zhong Yao Za Zhi 2013 Jan;38(1):81-90. Chinese.
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- 14. Attenuating heat-induced cellular autophagy, apoptosis and damage in H9c2 cardiomyocytes by pre-inducing HSP70 with heat shock preconditioning.
Abstract Purpose: We sought to assess whether heat-induced autophagy, apoptosis and cell damage in H9c2 cells can be affected by pre-inducing HSP70 (heat shock protein 70). Materials and methods: Cell viability was determined using 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl tetrazolium bromide staining and a lactate dehydrogenase assay. Apoptosis was evidenced using both flow cytometry and counting caspase-3 positive cells, whereas autophagy was evidenced by the increased LC3-II expression and lysosomal activity. Results: The viability of H9c2 cells was temperature-dependently (40-44 °C) and time-dependently (90-180 min) significantly (p < 0.05) reduced by severe heat, which caused cell damage, apoptosis and autophagy. Heat-induced cell injury could be attenuated by pretreatment with 3-methylademine (an autophagy inhibitor) or Z-DEVD-FMK (a caspase-3 inhibitor). Neither apoptosis nor autophagy over the levels found in normothermic controls was induced in heat-shock preconditioned controls (no subsequent heat injury). The beneficial effects of mild heat preconditioning (preventing heat-induced cell damage, apoptosis and autophagy) were significantly attenuated by inhibiting HSP70 overexpression with triptolide (Tripterygium wilfordii) pretreatment. Conclusion: We conclude that pre-inducing HSP70 attenuates heat-stimulated cell autophagy, apoptosis and damage in the heart. However, this requires in vivo confirmation....(more)
Hsu SF, et al. Int J Hyperthermia 2013 May;29(3):239-47.
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- 15. Prevention of postoperative recurrence of Crohn's disease: Tripterygium wilfordii polyglycoside versus mesalazine.
OBJECTIVES:
To explore effectiveness and safety of polyglycosides of Tripterygium wilfordii (GTW) and mesalazine (5-aminosalicylic acid [5-ASA]) in preventing postoperative clinical and endoscopic recurrence of Crohn's disease.
METHODS:
In this prospective, single-centre, single-blind study, postoperative Crohn's disease patients in remission were randomized to receive 1 mg/kg GTW daily, orally, or 4 g 5-ASA daily, orally, for 52 weeks. Patients underwent physical examinations, ileocolonoscopies and biochemical analyses at baseline and weeks 13, 26 and 52, or when clinical recurrence was suspected. Outcome measures were proportion of patients showing clinical or endoscopic recurrence at week 52, and changes in Rutgeerts' and Crohn's Disease Activity Index (CDAI) scores.
RESULTS:
Twenty-one patients were assigned to receive GTW and 18 to 5-ASA; two patients on GTW and one on 5-ASA were withdrawn. Clinical and endoscopic recurrences were less common in the GTW group (n = 4) versus the 5-ASA group (n = 9). There were improvements in Rutgeerts' scores for those taking GTW. Mean between-group CDAI scores were similar. No serious adverse events were reported.
CONCLUSION:
These findings indicate that GTW appears to be an effective, well-tolerated prophylactic regimen, superior to oral 5-ASA, for preventing clinical and endoscopic recurrence in postsurgical Crohn's disease....(more)
Ren J, et al. J Int Med Res 2013 Feb;41(1):176-87.
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- 16. Triptolide-Conditioned Dendritic Cells Induce Allospecific T-Cell Regulation and Prolong Renal Graft Survival.
ABSTRACT Background: Previous studies show that triptolide (TPT), a diterpenoid isolated from the Chinese herb Tripterygium wilfordii Hook.f, inhibits dendritic cell (DCs) maturation. Whether TPT-conditioned DCs (TPT-DCs) may regulate allospecific immune responses remains unclear. In this study, we investigated the effects of TPT on allostimulatory function and phenotype of rat bone marrow-derived DCs (BMDCs). Methods: Brown Norway rats BMDCs were cultured with or without TPT and then stimulated with lipopolysaccharide (LPS). IL-10 in supernatants was quantitatively measured, and the cells were analyzed by flow cytometry and used as stimulators in mixed leukocyte reaction in which naive Lewis rat T lymphocytes were used as responders. The tolerogenic potential of TPT-BMDCs was evaluated in vivo in a rat model of MHC fully mismatched kidney transplantation. Results: After treatment with TPT, BMDCs remained immature with low expression of CD80 and CD86 in the presence of LPS. At low concentrations of TPT (1 and 2.5 nM), BMDCs produced higher levels of IL-10 than the untreated cells (431 and 205.4 pg/ml, respectively, vs. 122.9 pg/ml, p < .05). T cells cocultured with TPT-BMDCs were hyporesponsive in allogeneic mixed lymphocyte reaction. The CD25+foxp3+Treg cell populations increased from 19.9% to 29.7% in the coculture system. Without immunosuppressive therapy, infusion of TPT-BMDCs in recipients before transplantation prolonged rat kidney allograft survival (18.8 ± 1.30 days). Conclusions: Our findings demonstrate that TPT inhibits the maturation and allogenicity of BMDCs and promotes the expansion of CD25+foxp3+ regulatory T cells. It suggests that TPT-DCs are potentially useful for preventing kidney transplant rejection....(more)
Zhang G, et al. J Invest Surg 2013 Mar 20.
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- 17. Role of oxidative stress, endoplasmic reticulum stress and ERK activation in triptolide-induced apoptosis.
Since its isolation from Tripterygium wilfordii in 1972, triptolide has been shown to possess potent anticancer activity against a variety of cancers, and has entered phase I clinical trial. It is a diterpenoid triepoxide that acts through multiple molecular targets and signaling pathways. The mitogen-activated protein kinases are well known for their modulation of cell survival and proliferation. In particular, the ERK pathway has a dual role in cell proliferation and cell death. Thus far, data on the effect of triptolide on ERK signaling remain limited. In our current study, we have shown for the first time that ERK activation rather than inhibition occurred in a dose- and time-dependent manner following triptolide treatment in MDA-MB-231 breast cancer cells. ERK activation was crucial in mediating triptolide-induced caspase-dependent apoptosis. Tritpolide-induced ERK activation modulated the expression of the Bcl-2 protein family member Bax but was not involved in the downregulation of Bcl-xL expression. Signals acted upstream of ERK activation included generation of reactive oxygen species (ROS) and endoplasmic reticulum stress predominantly via the PERKeIF2α pathway, as the MEK inhibitor U0126 did not inhibit the phosphorylation of PERK and eIF2α or the generation of ROS....(more)
Tan BJ, et al. Int J Oncol 2013 May;42(5):1605-12.
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- 18. Therapeutic effect of Tripterygium wilfordii Hook F multiglycosides on gut barrier dysfunction in rats with acute necrotizing pancreatitis.
The aim of the current study was to investigate the therapeutic effect of Tripterygium wilfordii Hook F multiglycosides (TWG) on gut barrier dysfunction in rats with acute necrotizing pancreatitis (ANP). ANP was induced in rats using 3.5% sodium taurocholate. The rats were divided into 3 groups: the sham operation (SO), ANP and ANP+TWG groups. Biochemical and pathological change of pancreatic tissue and ileal mucosa, bacterial cultures and the survival rate were measured following surgery and treatment. TWG treatment significantly decreased amylase and lipase activities and plasma endotoxin and D-lactate levels. Edema and inflammation in the pancreas and ileal mucosa were alleviated. Positive bacterial cultures were significantly reduced. The survival rate of the rats in the ANP+TWG group was higher than that of the rats in the ANP group. TWG treatment showed beneficial effects by protecting the pancreas from bacterial infection caused by gut barrier dysfunction and improving the outcomes of the rats with ANP....(more)
Wang J, et al. Exp Ther Med 2013 Feb;5(2):461-466.
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- 19. The clinical course and long-term outcome of primary focal segmental glomerulosclerosis in Chinese adults.
Objective: To explore the long-term outcome and prognostic factors of primary focal segmental glomerulosclerosis (FSGS) in Chinese adults. Methods: A retrospective study was conducted in 104 adults with primary FSGS. Clinical records and renal biopsies were reviewed. The primary endpoint was end-stage renal disease (ESRD) and death. Results: The most frequent FSGS variant was not otherwise specified (45.2%), followed by tip lesion (20.2%). 57 patients presented nephrotic syndrome. Among the nephrotic patients with first episode, the total remission rate was 94.75% by prednisone treatment and 50% by Tripterygium wilfordii (TW) multiglycoside treatment. Steroid-resistant patients treated by TW multiglycoside achieved a total remission rate of 80%. Over a median follow-up of 72 months, 25 patients developed ESRD. The median renal survival was 116 months. The renal survival rates were 83.5% and 43.8% at 5 and 10 years after the biopsy, respectively. By multivariate Cox proportional analysis, the degree of proteinuria, acute kidney injury (AKI) with chronic kidney disease (CKD) Stage 3, chronic tubulointerstitial injury, and complete and partial remission were independent predictors of ESRD. Conclusion: TW is a new potential treatment for steroid-resistant nephrotic FSGS. The 5-year renal outcome in adults with primary FSGS in China is better in comparison to the west. Severe proteinuria, CKD with AKI, chronic tubulointerstitial injury, and no response were independent risk factors of prognosis....(more)
Tang X, et al. Clin Nephrol 2013 Feb 5.
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- 20. Triptolide-mediated cell death in neuroblastoma occurs by both apoptosis and autophagy pathways and results in inhibition of nuclear factor-kappa B activity.
BACKGROUND:
Neuroblastoma is an aggressive pediatric malignancy with significant chemotherapeutic resistance. We assessed triptolide as a potential therapy.
METHODS:
SH-SY5Y and IMR-32 neuroblastoma cell lines were treated with triptolide. Viability, intracellular calcium, caspase activation, protein, and mRNA levels were measured. Autophagy was evaluated with confocal microscopy. Nuclear factor-kappa B (NF-κB) activation was measured using a dual luciferase assay.
RESULTS:
Triptolide treatment resulted in death in both cell lines within 72 hours, with sustained increases in intracellular calcium. IMR-32 cells underwent cell death by apoptosis. Conversely, light chain 3II (LC3II) protein levels were elevated in SH-SY5Y cells, which is consistent with autophagy. Confocal microscopy confirmed increased LC3 puncta in SH-SY5Y cells compared with control cells. Heat shock pathway protein and mRNA levels decreased with treatment. NF-κB assays demonstrated inhibition of tumor necrosis factor (TNF)-α-induced activity with triptolide.
CONCLUSIONS:
Triptolide treatment induces cell death in neuroblastoma by different mechanisms with multiple pathways targeted. Triptolide may serve a potential chemotherapeutic role in advanced cases of neuroblastoma.
Copyright © 2013 Elsevier Inc. All rights reserved....(more)
Krosch TC, et al. Am J Surg 2013 Apr;205(4):387-96.
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- 21. Immunosuppression with a combination of triptolide and cyclosporin A in rat vascularized groin flap allotransplantation.
BACKGROUND:
Triptolide is an immunosuppressive fraction purified from a Chinese medicinal plant. In an effort to develop a new immunosuppressive strategy for vascularized composite allotransplantation, the authors investigated the effects of combined treatment with cyclosporin A and triptolide on the survival of rat groin flap allotransplants.
METHODS:
Groin flap transplantation was performed from Brown Norway rats to Fischer 344 recipients, which were then treated with triptolide, cyclosporin A, or both. Flap biopsy specimens were harvested, stained, and submitted to histopathologic evaluation. Levels of CCR5, CCR7, CCL19, CCL21, and Foxp3 in spleen were examined by real-time polymerase chain reaction, and the percentage of CD4+CD25+ regulatory T cells was detected by flow cytometry.
RESULTS:
The mean survival time for allografts in recipients receiving triptolide and cyclosporin A was 57 ± 7.7 days compared with 20.5 ± 2.3 days for cyclosporin A alone, 23.3 ± 3.6 days for triptolide alone, and 7.8 ± 0.8 days for no treatment. Histologic examination also showed that inflammatory cell infiltration was reduced in grafts with combination treatment. Down-regulation of CCR5, CCR7, and CCL19 in the combination treatment was accompanied by increased expression of Foxp3. Flow cytometric analysis also revealed that the percentage of CD4+CD25+ regulatory T cells in the combination treatment was higher than in the monotherapy groups.
CONCLUSIONS:
Combination therapy with triptolide and cyclosporin A substantially prolonged allograft survival, which means calcineurin inhibitor-related drug-toxicity may be alleviated and treatment cost reduced. This immunosuppressive effect is mediated by inhibition of dendritic cells maturation and the expansion of regulatory T cells....(more)
Liu F, et al. Plast Reconstr Surg 2013 Mar;131(3):343e-50e.
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- 22. Role of oxidative stress, endoplasmic reticulum stress and ERK activation in triptolide-induced apoptosis.
Since its isolation from Tripterygium wilfordii in 1972, triptolide has been shown to possess potent anticancer activity against a variety of cancers, and has entered phase I clinical trial. It is a diterpenoid triepoxide that acts through multiple molecular targets and signaling pathways. The mitogen-activated protein kinases are well known for their modulation of cell survival and proliferation. In particular, the ERK pathway has a dual role in cell proliferation and cell death. Thus far, data on the effect of triptolide on ERK signaling remain limited. In our current study, we have shown for the first time that ERK activation rather than inhibition occurred in a dose- and time-dependent manner following triptolide treatment in MDA-MB-231 breast cancer cells. ERK activation was crucial in mediating triptolide-induced caspase-dependent apoptosis. Tritpolide-induced ERK activation modulated the expression of the Bcl-2 protein family member Bax but was not involved in the downregulation of Bcl-xL expression. Signals acted upstream of ERK activation included generation of reactive oxygen species (ROS) and endoplasmic reticulum stress predominantly via the PERKeIF2α pathway, as the MEK inhibitor U0126 did not inhibit the phosphorylation of PERK and eIF2α or the generation of ROS....(more)
Tan BJ, et al. Int J Oncol 2013 May;42(5):1605-12.
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- 23. Minnelide reduces tumor burden in preclinical models of osteosarcoma.
Osteosarcoma is the most common bone cancer in children and adolescents with a 5-year survival rate of about 70%. In this study, we have evaluated the preclinical therapeutic efficacy of the novel synthetic drug, Minnelide, a prodrug of triptolide on osteosarcoma. Triptolide was effective in significantly inducing apoptosis in all osteosarcoma cell lines tested but had no significant effect on the human osteoblast cells. Notably, Minnelide treatment significantly reduced tumor burden and lung metastasis in the orthotopic and lung colonization models. Triptolide/Minnelide effectively downregulated the levels of pro-survival proteins such as heat shock proteins, cMYC, survivin and targets the NF-κB pathway....(more)
Banerjee S, et al. Cancer Lett 2013 Mar 14.
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- 24. Triptolide-Conditioned Dendritic Cells Induce Allospecific T-Cell Regulation and Prolong Renal Graft Survival.
ABSTRACT Background: Previous studies show that triptolide (TPT), a diterpenoid isolated from the Chinese herb Tripterygium wilfordii Hook.f, inhibits dendritic cell (DCs) maturation. Whether TPT-conditioned DCs (TPT-DCs) may regulate allospecific immune responses remains unclear. In this study, we investigated the effects of TPT on allostimulatory function and phenotype of rat bone marrow-derived DCs (BMDCs). Methods: Brown Norway rats BMDCs were cultured with or without TPT and then stimulated with lipopolysaccharide (LPS). IL-10 in supernatants was quantitatively measured, and the cells were analyzed by flow cytometry and used as stimulators in mixed leukocyte reaction in which naive Lewis rat T lymphocytes were used as responders. The tolerogenic potential of TPT-BMDCs was evaluated in vivo in a rat model of MHC fully mismatched kidney transplantation. Results: After treatment with TPT, BMDCs remained immature with low expression of CD80 and CD86 in the presence of LPS. At low concentrations of TPT (1 and 2.5 nM), BMDCs produced higher levels of IL-10 than the untreated cells (431 and 205.4 pg/ml, respectively, vs. 122.9 pg/ml, p < .05). T cells cocultured with TPT-BMDCs were hyporesponsive in allogeneic mixed lymphocyte reaction. The CD25+foxp3+Treg cell populations increased from 19.9% to 29.7% in the coculture system. Without immunosuppressive therapy, infusion of TPT-BMDCs in recipients before transplantation prolonged rat kidney allograft survival (18.8 ± 1.30 days). Conclusions: Our findings demonstrate that TPT inhibits the maturation and allogenicity of BMDCs and promotes the expansion of CD25+foxp3+ regulatory T cells. It suggests that TPT-DCs are potentially useful for preventing kidney transplant rejection....(more)
Zhang G, et al. J Invest Surg 2013 Mar 20.
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- 25. Anti-inflammatory effects of triptolide improve left ventricular function in a rat model of diabetic cardiomyopathy.
AIMS:
Given the importance of inflammation in the onset and progression of diabetic cardiomyopathy, we investigated the potential protective effects of triptolide, an anti-inflammatory agent, in streptozotocin-induced diabetic rat model and in H9c2 rat cardiac cells exposed to high glucose.
METHODS AND RESULTS:
Diabetic rats were treated with triptolide (100, 200, or 400 μg/kg/day respectively) for 6 weeks. At the end of this study, after cardiac function measurements were performed, rats were sacrificed and their hearts were harvested for further histologic and molecular biologic analysis. Enhanced activity and expression of nuclear factor-kappaB (NF-κB) p65 in diabetic hearts were associated with increased inflammatory response, as demonstrated by increased pro-inflammatory cytokines, cell adhesion molecules and invading inflammatory cells, as well as increased fibrosis, in line with impaired left ventricular function. Triptolide attenuated these morpho-functional alterations. Furthermore, triptolide (20 ng/ml) also attenuated high glucose-induced inflammation in H9c2 rat cardiac cells.
CONCLUSION:
Our data demonstrate that anti-inflammatory effects of triptolide involving the NF-κB signaling pathway can improve left ventricular function under diabetic conditions, suggesting triptolide treatment might be beneficial in diabetic cardiomyopathy....(more)
Wen HL, et al. Cardiovasc Diabetol 2013 Mar 25;12:50.
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- 26. Triptolide protects rat heart against pressure overload-induced cardiac fibrosis.
BACKGROUND:
Emerging evidence underlines the role of inflammation activation in the process of cardiac fibrosis. Triptolide has potent anti-inflammatory and anti-proliferative properties, and extensively used in the treatment of chronic inflammatory disorders. In the current study, we test the hypothesis that triptolide treatment facilitates to attenuate chronic pressure overload-induced cardiac fibrosis in a model of rat.
METHODS:
Adult male Sprague-Dawley rats were subjected to a suprarenal abdominal aorta constriction (AC) or sham (as control) to induce sustained pressure overload. Eight weeks later, rats were randomly assigned to receive triptolide (9μg/kg.d, i.p) or vehicle (0.1% dimethyl sulfoxide, 0.2ml/d, i.p) treatment for an additional 8weeks.
RESULTS:
AC caused significant pathological hypertrophy, cardiac fibrosis and reduced cardiac diastolic function. Triptolide treatment markedly inhibited AC-induced increases in myocardial collagen volume fraction, collagen type I/III deposition, left ventricular end-diastolic pressure, expressions of pro-fibrogenic factors (transforming growth factor-β and angiotensin II) and pro-inflammatory cytokines (IL-1β and IL-6), NF-κB activation and inflammatory cell infiltration in left ventricles compared with vehicle, without affecting cardiac hypertrophy. However, triptolide had no effects on systemic blood pressure and circulating angiotensin II level.
CONCLUSIONS:
Collectively, the findings suggested that triptolide treatment elicits favorable anti-fibrogenic effect in a blood pressure-independent manner, at least in part, through inhibiting myocardial pro-fibrogenic factor production and inflammatory activation in the pressure overloaded heart.
Copyright © 2013 Elsevier Ireland Ltd. All rights reserved....(more)
Zhang Z, et al. Int J Cardiol 2013 Mar 27.
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- 27. The genetic depletion or the triptolide inhibition of TFIIH in p53 deficient cells induce a JNK-dependent cell death in Drosophila.
TFIIH participates in transcription, nucleotide excision repair and the control of the cell cycle. In this work, we demonstrate that the Dmp52 subunit of TFIIH in Drosophila physically interacts with the fly p53 homologue, Dp53. The depletion of Dmp52 in the wing disc generates chromosome fragility, increases apoptosis and produces wings with a reduced number of cells; cellular proliferation, however, is not affected. Interestingly, instead of suppressing the apoptotic phenotype, the depletion of Dp53 in Dmp52-depleted wing disc cells increases apoptosis and the number of cells that suffer from chromosome fragility. The apoptosis induced by the depletion of Dmp52 alone is partially dependent on the JNK pathway. In contrast, the enhanced apoptosis caused by the simultaneous depletion of Dp53 and Dmp52 is absolutely JNK-dependent. In this study, we also show that the anti-proliferative drug triptolide, which inhibits the ATPase activity of the XPB subunit of TFIIH, phenocopies the JNK-dependent massive apoptotic phenotype of Dp53-depleted wing disc cells; this observation suggests that the mechanism by which triptolide induces apoptosis in p53-deficient cancer cells involves the activation of the JNK death pathway....(more)
Villicaña C, et al. J Cell Sci 2013 Apr 8.
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- 28. Triptolide Prevents Bone Destruction in the Collagen-Induced Arthritis Model of Rheumatoid Arthritis by Targeting RANKL/RANK/OPG Signal Pathway.
Focal bone destruction within inflamed joints is the most specific hallmark of rheumatoid arthritis (RA). Our previous study indicated that the therapeutic efficiency of triptolide in RA may be due partially to its chondroprotective and anti-inflammatory effects. However, its roles in bone destruction are still unclear. In this study, our data firstly showed the therapeutic effects of triptolide on severity of arthritis and arthritis progression in collagen-induced arthritis (CIA) mice. Then, by micro-CT quantification, triptolide treatment significantly increased bone mineral density, bone volume fraction, and trabecular thickness and decreased trabecular separation of inflamed joints. Interestingly, triptolide treatment could prevent the bone destruction by reducing the number of osteoclasts in inflamed joints, reducing the expression of receptor activator of NF- κ B (RANK) ligand (RANKL) and RANK, increasing the expression of osteoprotegerin (OPG), at both mRNA and protein levels, and decreasing the ratio of RANKL to OPG in sera and inflamed joints of CIA mice, which were further confirmed in the coculture system of human fibroblast-like synovial and peripheral blood mononuclear cells. These findings offer the convincing evidence for the first time that triptolide may attenuate RA partially by preventing the bone destruction and inhibit osteoclast formation by regulating RANKL/RANK/OPG signal pathway....(more)
Liu C, et al. Evid Based Complement Alternat Med 2013;2013:626038.
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- 29. Impairment of triptolide on liver mitochondria in isolated liver mitochondria and HL7702 cell line.
OBJECTIVE:
To observe the impairing effects of triptolide on liver mitochondria in isolated rat-liver mitochondria and human normal liver HL7702 cell line.
METHODS:
Rat-liver mitochondria were isolated from adult female Sprague-Dawley (SD) rats. Liver mitochondria were incubated with 0, 1.25, 2.5, 5 and 10 μmol/L triptolide for detecting mitochondrial swelling and with 0, 2.5, 5 and 10 μmol/L triptolide for mitochondrial permeability transition pore (MPTP) activity. Mitochondrial swelling was estimated by measuring the apparent absorbance change during 600 s in the mitochondrial suspensions at 520 nm with a mitochondrial swelling examining kit. The effect of triptolide on MPTP was determined with a fluorescence detection kit by detecting the fluorescence intensity at an excitation wavelength of 488 nm emitted at 527 nm. Human normal liver HL7702 cells were treated without or with 0.02, 0.1 and 0.5 μmol/L triptolide for 24 h for analyzing mitochondrial transmembrane potential (ΔΨm) and reactive oxygen species (ROS). ΔΨm was measured using the fluorescent probe 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethylbenzimidazolylcarbocyanine iodide (JC-1). ROS was measured using fluorescent probe 2',7'-dichlorofluorescin diacetate (DCFH-DA). The cells were harvested and dyed with JC-1 and DCFH-DA, and analyzed by flow cytometry, respectively.
RESULTS:
Incubation of isolated mitochondria with triptolide results in swollen mitochondria in a concentration-dependent manner. Moreover, triptolide significantly activated mitochondrial permeability transition at 5 and 10 μmol/L (P<0.05 and P<0.01). When HL7702 cells were exposed to a various concentration triptolide for 24 h, mitochondrial membrane depolarization and increase of ROS were caused by triptolide in a concentration-dependent manner. Triptolide significantly induced the mitochondrial membrane depolarization at 0.1 and 0.5 μmol/L (P<0.05 and P<0.01) and the increase of ROS at 0.1 and 0.5 μmol/L (P<0.05 and P<0.01).
CONCLUSION:
Triptolide could induce mitochondrial impairment, which may be one of the mechanisms by which hepatotoxicity occurs....(more)
Fu Q, et al. Chin J Integr Med 2013 Apr 10.
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- 30. [Diterpene constituents of Tripterygium willfordii (II)].
In order to study the constituents and pharmacology of Tripterygium plants (Tripterygium willfordii Hook.f), a variety of chromatography methods were used. Four compounds were isolated from Tripterygium plant and their structures were elucidated by UV, IR, MS, HR-MS, 1H NMR, 13C NMR and 2D-NMR techniques. The isolated compounds were named as triptonide (1), neo-triptetraolide (2), 2alpha-hydroxytriptonide (3), and 15-hydroxytriptonide (4), separately. Compounds 3, 4 belong to new diterpenoids, which can inhibit the growth of K562 cells (leukemia cells) and HL60 cells (acute myeloid leukemia cells)....(more)
Lin S, et al. Yao Xue Xue Bao 2011 Aug;46(8):942-5. Chinese.
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- 31. Immunochemical characterization of the functional constituents of Tripterygium wilfordii contributing to its anti-inflammatory property.
1. Tripterygium wilfordii (TW) contains bioactive compounds that possess immunosuppressive properties. These compounds are considered to be potential drugs in the treatment of acute graft rejections. However, their structure-activity relationships remain unknown. 2. The aim of the present study was to delineate the molecular moieties of triptolide that could account for its ability to inhibit inflammatory responses. In this context, purified TW active compounds (triptolide and triptonide) and synthetic triptolide derivatives were prepared to investigate the structure-activity relationships of triptolide. To this end, rat splenocytes were treated with increasing concentrations of the compounds and then allogenically stimulated using a mixed lymphocyte reaction to determine their antiproliferative activities. From the results, the IC50 value of each compound was calculated. 3. Modification of the beta-hydroxyl group at the C-14 position of the triptolide molecule significantly affected the immunosuppressive activity of T59, as demonstrated by a sevenfold increase of the IC50. Conversely, reduction of the gamma-butyrolactone group in T60 and T61 completely abrogated the antiproliferative effect. Alterations in the C-14 beta-hydroxyl and gamma-butyrolactone groups also resulted in reduced cytotoxicity. 4. The present findings demonstrate that the C-14 beta-hydroxyl and gamma-butyrolactone moieties of the triptolide molecule are crucial for its anti-inflammatory properties and cytotoxicity and are responsible for the compound's antiproliferative activity....(more)
Wong KF, et al. Clin Exp Pharmacol Physiol 2008 Jan;35(1):55-9.
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- 32. Determination of triptonide by cloud point extraction combined with MEKC.
A method has been developed for the determination of triptonide in the traditional Chinese herb Tripterygium wilfordii Hook F. by micellar electrokinetic capillary chromatography combined with cloud point extraction. The analyte was extracted at pH 3.0 by micelles of the nonionic surfactant polyoxyethylene 7,5-octylphenyl ether (Triton X-114). A 250-muL aliquot from the extracted surfactant-rich phase was diluted to 400 muL with ethanol to reduce its viscosity before separation by MEKC. Under optimum conditions, an enrichment factor of 25 is obtained and the determination limit of triptonide is found to be 3.15 x 10(-7) mol/L. The proposed method has been successfully applied to the determination of triptonide in T. wilfordii tablet and spiked urine matrix, demonstrating the feasibility and reliability of the proposed method....(more)
Wu YW, et al. J Sep Sci 2008 Mar;31(5):865-71.
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- 33. Flow rate gradient high-speed counter-current chromatography separation of five diterpenoids from Triperygium wilfordii and scale-up.
In this paper, high-speed counter-current chromatography (HSCCC) instruments with different gravitational forces were applied for the separation of bioactive compounds from Triperygium wilfordii Hook.f. The critical parameters including sample concentration, sample volume and flow rate were first optimized on an analytical Mini-DE HSCCC system, and then scaled up to a preparative TBE 300A HSCCC system. Although this scale-up process was performed using different CCC instruments with different centrifuges and gravitational forces, the same resolutions were obtained and the elution time could be predictable. Five diterpenoid compounds and one unknown compound were separated from Triperygium wilfordii Hook.f. by HSCCC with a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (HEMW) (3:2:3:2, v/v/v/v). This one-step flow gradient separation produced triptonide (25 mg), isoneotriptophenolide (77 mg), hypolide (83 mg), unknown compound (1 mg), triptophenolide (42 mg), triptonoterpene methyl ether VI (37 mg) from 320 mg crude extract with purities of 98.2%, 96.6%, 98.1%, 95.3%, 95.1%, and 96.5%, respectively. Their purities and structures were identified by high-performance liquid chromatography, mass spectrometry and NMR. This paper demonstrates that analytical CCC plays an important role in optimizing parameters and scale-up process when analytical CCC and preparative CCC are supplied by different manufacturers with different gravitational forces, and the scale-up process from analytical CCC to preparative CCC is still predictable....(more)
Peng A, et al. J Chromatogr A 2008 Jul 25;1200(2):129-35.
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- 34. Troxerutin counteracts domoic acid-induced memory deficits in mice by inhibiting CCAAT/enhancer binding protein β-mediated inflammatory response and oxidative stress.
The C/EBP β is a basic leucine zipper transcription factor that regulates a variety of biological processes, including metabolism, cell proliferation and differentiation, and immune response. Recent findings show that C/EBP β-induced inflammatory responses mediate kainic acid-triggered excitotoxic brain injury. In this article, we show that protein kinase C ζ enhances K-ras expression and subsequently activates the Raf/MEK/ERK1/2 pathway in the hippocampus of domoic acid (DA)-treated mice, which promotes C/EBP β expression and induces inflammatory responses. Elevated production of TNF-α impairs mitochondrial function and increases the levels of reactive oxygen species by IκB kinase β/NF-κB signaling. The aforementioned inflammation and oxidative stress lead to memory deficits in DA-treated mice. However, troxerutin inhibits cyclin-dependent kinase 1 expression, enhances type 1 protein phosphatase α dephosphorylation, and abolishes MEK/ERK1/2/C/EBP β activation, which subsequently reverses the memory impairment observed in the DA-treated mice. Thus, troxerutin is recommended as a potential candidate for the prevention and therapeutic treatment of cognitive deficits resulting from excitotoxic brain damage and other brain disorders....(more)
Lu J, et al. J Immunol 2013 Apr 1;190(7):3466-79.
Related Products: Troxerutin
- 35. Radioprotective effects of troxerutin against gamma irradiation in mice liver.
PURPOSE:
The purpose of this study was to conduct research in mice to determine the radioprotective effects of troxerutin. Thirty-day survival, oxidative status and histological changes in the liver were all evaluated.
MATERIALS AND METHODS:
Troxerutin was administered orally to mice for six days before irradiation with different doses (6, 7, 8 and 10 Gy) of γ-rays and the mice were observed for 30 days after radiation to calculate 30-day survival and median lethal dose of 30 days (LD50/30). Its radioprotective efficacy was compared with the positive drug amifostine which is currently the most effective radioprotector. The animals pretreated with troxerutin for 6 days were sacrificed on day 11 after radiation (6 Gy) in order to make 10% homogenate and histological sections of liver. Antioxidant enzymes were detected in strict accordance with kit requirements. Histological liver sections were examined by hematoxylin-eosin (HE) staining.
RESULTS:
Pretreatment with troxerutin resulted in a significantly higher 30-day survival rate for 70% of mice compared with 30% of irradiation group after exposure to a potentially lethal dose of 8 Gy; LD50/30 of drug treatment group was 9 Gy compared with 7.7 Gy for irradiation group. The results indicated that troxerutin increased the activity of various antioxidant enzymes, such as superoxide dismutase (SOD) in mice liver, which was reduced by radiation treatment. Maleic dialdehyde (MDA) levels were significantly reduced by troxerutin, which was increased after 6 Gy radiation. These results were further confirmed by histopathological examinations which indicated that pre-administration with the effective dose of troxerutin reduced the hepatic damage induced by radiation.
CONCLUSIONS:
Administration of troxerutin before irradiation, provided higher survival of experimental mice, improvement of biochemical parameters, and preserved major histological parameters of the liver. These results collectively indicate that troxerutin is an effective radioprotective agent....(more)
Ping X, et al. Int J Radiat Biol 2012 Aug;88(8):607-12.
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