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Pharm Biol [journal]
- Modulation of cyclophosphamide-induced early lung injury by allicin. [Journal Article]
- Pharm Biol 2013 Jun; 51(6):806-11.
Context:Cyclophosphamide (CP) causes lung injury in rats through its ability to generate free radicals with subsequent epithelial and endothelial cell damage.
Objective:This study was conducted to assess whether allicin can ameliorate CP-induced early lung injury in rats. Materials and methods: Male Sprague Dawely rats were divided into four groups. Group I was the control group. Group II received allicin (50 mg/kg/d, p.o.) for 14 consecutive days. Group III was injected once with CP (150 mg/kg, i.p.). Group IV received allicin for seven consecutive days, before and after CP injection (150 mg/kg, i.p.). The parameters of study were serum biomarkers, lung tissue antioxidant profile and histopathological changes in lung tissue.
Results:A single intraperitoneal injection of CP markedly altered the levels of several biomarkers in lung homogenates. Significant increases in lung content of lipid hydroperoxides were seen that paralleled the decreased levels of total reduced glutathione. Superoxide dismutase activity (SOD) was significantly increased. CP increased the level of serum biomarkers; total protein, lactate dehydrogenase (LDH) and tumor necrosis factor-alpha (TNF-α). Pretreatment of rats daily with oral allicin seven days prior to and seven days after CP inject significantly inhibited the development of lung injury, prevented the alterations in lung and serum biomarkers associated with inflammatory reactions, with less lipid peroxidation (LP) and restoration of antioxidants. Moreover, allicin attenuated the secretion of proinflammatory cytokine, TNF-α expression in rat serum. In addition, allicin effectively blunted CP-induced histopathological changes in lung tissue. Discussion and conclusion: Our results suggest that allicin is efficient in blunting CP-induced pulmonary damage.
- Therapeutic potential of octyl gallate isolated from fruits of Terminalia bellerica in streptozotocin-induced diabetic rats. [Journal Article]
- Pharm Biol 2013 Jun; 51(6):798-805.
Context:Medicinal plants are a potential source of antidiabetic drugs. Terminalia bellerica Roxb. (Combretaceae) is used in Indian traditional systems of medicine to treat diabetes mellitus.
Objective:The aim of this study was to isolate and identify antihyperglycemic principle(s) from the fruits of T. bellerica and assess the bioactivity in streptozotocin (STZ)-induced diabetic rats. Materials and methods: Bioassay-guided fractionation was followed to isolate the active compound(s), structure was elucidated using (1)H and (13)C NMR, IR and mass spectrometry and administered intragastrically to diabetic Wistar rats at different doses (5, 10 and 20 mg/kg, body weight) for 28 d. Plasma glucose, insulin, C-peptide and other biochemical parameters were studied.
Results:Octyl gallate (OG) isolated first time from the fruit rind of T. bellerica significantly (p < 0.05) reduced plasma glucose to near normal values (108.47 ± 6.9 mg/dl) after 14 d at the dose of 20 mg/kg. In addition, OG significantly increased plasma insulin, C-peptide, total protein, albumin, tissue glycogen, body weight and markedly decreased serum total cholesterol, triglyceride, LDL-cholesterol, urea, uric acid and creatinine in diabetic rats. Also OG restored the altered regulatory enzymes of carbohydrate metabolism. Discussion and conclusion: OG might have augmented the secretion of insulin by the modulation of cAMP and intracellular calcium levels in the β cells of the pancreas. Our findings indicate that OG isolated first time from the fruit rind of T. bellerica has potential antidiabetic effect as it augments insulin secretion and normalizes the altered biochemical parameters in experimental diabetic rat models.
- Antinociceptive activity and chemical composition of Wei-Chang-An-Wan extracts. [Journal Article]
- Pharm Biol 2013 Jun; 51(6):790-7.
Context:Currently, famous traditional Chinese medicine formulas have undergone re-evaluation and development in China. Wei-Chang-An-Wan (WCAW) as one of them has been used for treating various gastrointestinal diseases for several decades. The secondary development of WCAW is in progress so as to interpret the effective material basis or find new pharmacological activity.
Objective:To evaluate the antinociceptive effect of methanol extract of WCAW (ME) as well as four fractions (P.E., EtOAc, n-BuOH, H2O) and obtain information on the correlation between the contents of the fractions and antinociceptive effect. Materials and methods: ME was divided into four parts extracted by petroleum ether, ethyl acetate and n-butanol. Antinociceptive activity was evaluated by three models of acetic acid-induced writhing, formalin and hot-plate test in mice after repetitive administration of ME at 200, 400 or 800 mg/kg, P.E. 132 mg/kg, EtOAc 106 mg/kg, n-BuOH 176 mg/kg and H2O 176 mg/kg for six days. The chemical compounds were analyzed by HPLC-ESI-MS.
Results:ME at 800 mg/kg inhibited acid-induced writhing by 84.69%, and reduced the licking time of second phase in formalin test by 53.23%. The inhibition rates in acid-induced writhing of P.E., EtOAc, n-BuOH and H2O were 27.79, 33.85, 38.97 and 37.69%, respectively, and in formalin test about 50%. They had no effect on the hot-plate test. HPLC-ESI-MS analysis showed that 68 chemical compounds were detected and 41 compounds were identified from ME. Discussion and conclusion: The results obtained herein indicate that WCAW possesses the antinociceptive activity that provides a new aspect in clinical application.
- Anti-arthritic activity of ethanol extract of Fagopyrum cymosum with adjuvant-induced arthritis in rats. [Journal Article]
- Pharm Biol 2013 Jun; 51(6):783-9.
Context:Fagopyrum cymosum (Trey.) Meisn (Polygonaceae) (EFC) has long been used as a folk medicine to treat various ailments of the lung, dysentery and rheumatism in China.
Objective:The present study evaluated the anti-arthritic effect of 95% ethanol extract of EFC (extract of Fagopyrum cymosum). Materials and methods: The anti-arthritic activity was investigated by adjuvant arthritic (AA) rat model induced by Freund's complete adjuvant (FCA). The AA rats were randomly separated into different groups and then treated with EFC (40, 80 and 160 mg/kg) from day 7 to day 28 after immunization. Arthritis was evaluated by hind paw swelling, polyarthritis index, body weight and index of immune organs. In addition, the severity of arthritis in the knee joints was evaluated by histopathological and hemorheological examination. The levels of interleukin 1 (IL-1) and tumor necrosis factor alpha (TNF-α) in the serum were assessed by ELISA.
Results:The high dose level of EFC (160 mg/kg) significantly suppressed the swelling of hind paw of AA rats (p < 0.01) and inhibited their body weight loss (p < 0.01). Based on histopathological examination, all EFC groups showed great amelioration compared with the model group. EFC (80 and 160 mg/kg) also decreased the plasma viscosity in different shear rates (p < 0.01). Moreover, EFC significantly reduced the production of IL-1 and TNF-α in the serum of AA (p < 0.01). Discussion and conclusion: This study provides a scientific basis for the claims that F. cymosum is effective in preventing and suppressing the development and progression of experimental arthritis, with reductions in inflammatory response.
- Antimicrobial activities of some mushrooms in Turkey. [Journal Article]
- Pharm Biol 2013 Jun; 51(6):707-11.
Context:Terfezia boudieri Chatin (Pezizaceae), Agaricus brunnescens Peck (Agaricaceae) and Lactarius vellereus (Fr.) Fr. (Russulaceae) are well-known species in Turkey, and are used both for food and traditional medicine.
Objective:The powdered fruit bodies of T. boudieri, A. brunnescens and L. vellereus were used to evaluate the antimicrobial activities. Materials and methods: Chloroform, acetone and methanol extracts of T. boudieri, A. brunnescens and L. vellereus were tested for their antimicrobial activities against four Gram-positive bacteria, five Gram-negative bacteria and yeast using a micro-dilution method.
Results:The strongest minimum inhibitory concentration (MIC) value observed against the test microorganisms was with the chloroform extract of T. boudieri (MIC 2.4 µg/mL) against Streptococcus pyogenes. Maximum antimicrobial effects were observed with the acetone extracts of T. boudieri and L. vellereus (MIC 4.8 µg/mL) against Bacillus subtilis. The strongest antifungal activity was observed with the acetone extracts of T. boudieri (MIC 2.4 µg/mL) and A. brunnescens (MIC 19.5 µg/mL) against Candida albicans. The strongest MIC values for all fungal extracts were observed between 78 and 2.4 µg/mL. Discussion and conclusion: Present results demonstrated that these three mushroom species have excellent antimicrobial and antifungal activities, and thus have great potential as a source for natural health products.
- Antinociceptive effects of matrine on neuropathic pain induced by chronic constriction injury. [JOURNAL ARTICLE]
- Pharm Biol 2013 Apr 29.
Context:Sophora alopecuroides L. (Leguminosae) is a commonly used Chinese herbal drug that possesses antipyretic, anti-inflammatory and analgesic effects. Among various alkaloids isolated from S. alopecuroides, matrine has been identified as the major bioactive component contributing to a variety of pharmacological effects, and studies have also shown that matrine has an analgesic effect.
Objective:To investigate the antinociceptive effects of matrine on neuropathic pain induced by chronic constriction injury (CCI) in mice. Materials and methods: The von Frey, plantar, cold-plate, locomotor activity and rota-rod test were performed to assess the degree of mechanical, radiant, thermal, spontaneous locomotor activity and motor coordination changes respectively, at different time intervals, i.e., one day before surgery and 7, 8, 10, 12 and 14 days post surgery. Matrine was administered from the 8th day after the surgery for seven days.
Results:Our present study shows that matrine at the dose of 30 mg/kg i.p. increased the paw withdrawal threshold (0.88 ± 0.16), paw withdrawal latency (7.01 ± 0.11) and the counts of paw withdrawal (19.7 ± 1.15) from the day 8 for the nerve injured paw compared to the CCI group (0.18 ± 0.04, 4.62 ± 0.18, 44.3 ± 2.99, respectively). Matrine, in a dose-dependent effect, was also found to produce a protective role in both plantar and cold-plate tests. The analysis of the effect supports the hypothesis that matrine is useful in neuropathic pain therapy. Discussion and conclusion: The results of this study suggest that matrine could be useful in the treatment of different kinds of neuropathic pains as an adjuvant to conventional medicines.
- Correlation between polyphenol content and anti-inflammatory activity of Verbascum phlomoides (mullein). [JOURNAL ARTICLE]
- Pharm Biol 2013 Apr 29.
Context:Verbascum phlomoides L. (Scrophulariaceae) (mullein) used in the European folk medicine due to its anti-inflammatory and soothing action on the respiratory tract is thoroughly documented in handbooks and scientific literature. Nevertheless, information regarding the influence of the polyphenol content on pharmacological activity is scarce.
Objective:This study explored the antioxidant and anti-inflammatory potential of V. phlomoides polyphenol-rich extract. Materials and methods: Dried mullein flowers (200 g) were subjected to water extraction (60 °C, 2 h, herb/solvent ratio = 1/10 m/v) and further to n-butanol partition. Total phenolics were spectrophotometrically determined and specific compounds were evaluated by HPLC. The antioxidant activity was assessed by the 2,2-di(4-tert-octylphenyl)-1-picrylhydrazyl (DPPH) assay. The anti-inflammatory potential of the extract (50-200 μg/mL) was evaluated in vitro by ELISA measurement of ICAM-1 expression in TNF-α-stimulated endothelial cells and in vivo by the rat paw edema assay.
Results:The mullein extract contained 4.18% total polyphenols expressed as gallic acid. The main components identified by HPLC were: rosmarinic acid (14.93 mg/g), caffeic acid (39.96 mg/g), ferulic acid (29.61 mg/g) and quercetin (17.29 mg/g). Acteoside was not detected; aucubin was detected in traces (0.028 mg/g). Depending on concentration, the extract exerted scavenging activity on DPPH radical (EC50 7.09 mg/mL), significantly inhibited TNF-α-induced ICAM-1 expression by 55-58.8% on human umbilical vein endothelial cells at 100 and 200 μg/mL, but failed to reduce egg-white-induced rat paw edema. Discussion and conclusion: Mullein polyphenols play an important role in exerting the antioxidant effect but have a weak influence on anti-inflammatory activity that is correlated, probably, to a higher content of iridoids and phenylethanoids.
- Protective effects of saffron (Crocus sativus) against lethal ventricular arrhythmias induced by heart reperfusion in rat: A potential anti-arrhythmic agent. [JOURNAL ARTICLE]
- Pharm Biol 2013 Apr 29.
Context:Saffron (Crocus sativus L.) has been used as a cuisine spice in eastern and western societies for thousands of years. In traditional medicine, saffron is recommended for the treatment of various kinds of disorders including heart palpitations.
Objective:We investigated the hypothesis of the protective effect of saffron on lethal cardiac arrhythmias induced by heart ischemia-reperfusion in rat. Materials and methods: Animals were divided into a control (CTL) group that received tap water, Saf50, Saf100 and Saf200 groups that were orally treated with aqueous extracts of saffron, at dosages of 50, 100 and 200 mg/kg/day, respectively, and amiodarone (Amio) group that orally received 30 mg/kg/day for seven days. On day 8, heart ischemia-reperfusion was induced by ligation and releasing of the left anterior descending coronary artery.
Results:During reperfusion, the numbers and durations of ventricular fibrillation (VF) decreased in all groups compared to the CTL group (p < 0.05). Ventricular tachycardia (VT)/VF numbers (3.2 ± 1.2), durations (4.9 ± 2.6) and also arrhythmia severity (1.9 ± 0.35) were decreased significantly in the Saf100 group versus CTL group values (18.4 ± 11.6, 52 ± 31 and 3.3 ± 0.3, respectively). The PR and QTcn intervals of ECG were significantly longer in the Saf200 group (p < 0.001 versus CTL). The other doses of saffron only significantly prolonged the QTcn interval.
Conclusion:The results suggest that pretreatment with saffron, especially at the dosage of 100 mg/kg/day, attenuates the susceptibility and incidence of fatal ventricular arrhythmia during the reperfusion period in the rat. This protective effect is apparently mediated through reduction of electrical conductivity and prolonging the action potential duration.
- Protective effect of rutin against acute gastric mucosal lesions induced by ischemia-reperfusion. [JOURNAL ARTICLE]
- Pharm Biol 2013 Apr 29.
Context:Rutin, a flavonoid commonly present in onions, apples and tea, has been suggested to have a variety of pharmacological activities, including immunomodulator, anti-inflammatory and antioxidant activities.
Objectives:The present study was to examine the protective effects of rutin on gastric mucosal damage induced by gastric ischemia-reperfusion (I/R) in rats. Materials and methods: Rutin (50, 100, 200 mg/kg) was administered intragastrically for five consecutive days before ischemia. Sixty minutes after the last administration of rutin, under anesthesia, the celiac artery was clamped for 30 min, and then the clamp was removed for 60 min reperfusion. After reperfusion, the stomach was removed for biochemical and histological examinations.
Results:As compared with the I/R group (116.7 ± 21.5), administration of rutin at doses of 50, 100 and 200 mg/kg significantly prevented the increase of gastric mucosal injury index induced by gastric I/R (73.4 ± 14.8, 65.9 ± 9.6 and 26.9 ± 5.7, respectively). ED50 value was 138.7 mg/kg. Moreover, rutin at doses of 50, 100 and 200 mg/kg showed an inhibition on the increased myeloperoxidase (24.6, 41.3 and 53.1% reduction) activity and malondialdehyde levels (27.4, 40.3 and 50.7% reduction) in gastric mucosa. Also, the elevation of inducible NO synthase (iNOS) activity as well as the decrease of constitutive NO synthase (cNOS) in the gastric mucosa were significantly prevented by rutin pretreatment.
Conclusion:These results suggested that rutin has a protective effect against gastric mucosal injury induced by gastric I/R and that the gastroprotection was related to the NOS/NO pathway and its antioxidant activity.
- Protective effect of Cnestis ferruginea and its active constituent on scopolamine-induced memory impairment in mice: A behavioral and biochemical study. [JOURNAL ARTICLE]
- Pharm Biol 2013 Apr 29.