Research in Pharmaceutical Sciences
Volume:6 Issue: 1, Apr 2011

In everyday life, our body generates free radicals and other reactive oxygen species which are derived either from the endogenous metabolic processes (within the body) or from external sources. Many clinical and pharmacological studies suggest that natural antioxidants can prevent oxidative damage. Among the natural antioxidant products, Pycnogenol® (French Pinus pinaster bark extract) has been received considerable attention because of its strong free radical-scavenging activity against reactive oxygen and nitrogen species. P. pinaster bark extract (PBE) contains polyphenolic compounds (these compounds consist of catechin, taxifolin, procyanidins of various chain lengths formed by catechin and epicatechin units, and phenolic acids) capable of producing diverse potentially protective effects against chronic and degenerative diseases. This herbal medication has been reported to have cardiovascular benefits, such as vasorelaxant activity, angiotensin-converting enzyme inhibiting activity, and the ability to enhance the microcirculation by increasing capillary permeability. Moreover, effects on the immune system and modulation of nitrogen monoxide metabolism have been reported. This article provides a brief overview of clinical studies describing the beneficial and health-promoting effects of PBE.

Rosmarinus officinalis L. (Family Lamiaceae) popularly named rosemary, is a common household plant grown around the world, including Iran. Rosemary aerial parts are used as flavoring agent in foods, beverages, and cosmetic preparations and have various traditional uses in ethnomedicine including: analgesic, anti-inflammatory, anti-rheumatic, spasmolytic, carminative and choleretic applications. This study was carried out to investigate the effects of rosemary leaves hydroalcoholic extract (RHE) and essential oil (REO) in a well-defined model of experimental colitis induced by trinitrobenzene sulfonic acid (TNBS) in rats. Different doses of RHE (100, 200 and 400 mg/kg) and REO (100, 200 and 400 ml/kg) were administered orally and intraperitoneally (100, 400 mg/kg and 100, 400 ml/kg) to male Wistar rats (n=6), 6 h after colitis induction and continued for 5 days by intracolonic instillation of 0.25 ml TNBS (80 mg/kg)/ethanol 50% v/v. Wet colon weight/length ratio was measured and tissue damage scores as well as indices of colitis were evaluated both macroscopically and histopathologically. RHE and REO at all test doses used were effective to reduce colon tissue lesions and colitis indices while greater doses were significantly effective to diminish histopathologic parameters irrespective to the route of administration. Administration of oral prednisolone, Asacol® (mesalazine microgranules) and parenteral hydrocortisone acetate were effective to reduce colon tissue injures as well. These data suggest that RHE and REO are both effective to possess anti-colitic activity, and reinforce the use of this plant as a remedy for inflammatory bowel diseases in traditional medicine.

Quantitative relationships between molecular structure and azolo-adamantanes derivatives were discovered by different chemometric tools including factor analysis based multiple linear regressions (FA-MLR), principle component regression analysis (PCRA), and genetic algorithm-partial least squares GA-PLS. The FA-MLR describes the effect of geometrical and quantum indices on enzyme inhibition activity of the studied molecules. The quality of PCRA equation was found to be better than those derived from FA-MLR. GA-PLS analysis indicated that the topological (IC4 and MPC06), constitutional (nf) and geometrical (G (N..S)) parameters were the most significant ones on influenza A virus activity. Comparison of the different statistical methods employed revealed that GA-PLS represented superior results and it could explain and predict 85% and 77% of variances in the pIC50 data, respectively.

The cytotoxic chloroform fraction of Euphorbia aellenii Rech. F. (Euphorbiaceae) afforded two new phorbol diterpenoids: 4-deoxy-4α-phorbol-12-(2,3-dimethyl) butyrate-13-isobutyrate and 17-hydroxy-4-deoxy-4α-phorbol-12-(2,3-dimethyl) butyrate-13-isobutyrate. Their structures were elucidated by NMR and other spectroscopic methods. The immunomodulating potentials of the isolated compounds were tested using standard proliferation and chemiluminescence assays. Compound 2 showed moderate inhibitory activity against both T-cell proliferation and reactive oxygen species (ROS) production in whole blood with IC50 of 14.0 ± 0.57 and 44.1 ± 3.8 μg/ml, respectively, while compound 1 was relatively inactive with IC50 >50 μg/mL for T-cell proliferation, and >100 μg/mL for ROS.

Extract prepared from aerial part of Pycnocycla spinosa is a relaxant of rat ileum contractions. The objective of this research was to study the spasmolytic activity of P. spinosa root extract for comparison with the aerial part extract. Hydroalcoholic extracts were prepared by percolation method. A portion of rat ileum was removed and suspended under 1 g tension in Tyrode’s solution at 37 °C and gassed with O2. Isotonic contractions induced by electrical field stimulation (EFS), and KCl were recorded before and after addition of the extracts. Experiments were performed alongside time-matched vehicle controls. Both responses are blocked by lidocaine (74 µM), indicating that contractile responses are mediated by neuronal mechanism and partially was blocked by atropine. The root extract of P. spinosa (10-320 mg/ml) inhibited both initial rapid (IC50 = 71 ± 11.9 mg/ml) and secondary slow contraction (IC50 = 56 ± 7.8 mg/ml) evoked by EFS (n=6) as well as the KCl response (IC50 = 59 ± 11.7 mg/ml). The aerial part extract had a similar inhibitory effect on both KCl (IC50 = 47 ± 6.3 mg/ml) and EFS responses. This study confirms the inhibitory effects of root extract of P. spinosa on rat ileum contraction. However, the root extract was not more effective than the aerial part extract. Therefore, the aerial parts extract of P. spinosa could be used as a suitable substitute for the root extract.

Due to the widespread applications of xylitol dehydrogenase, an enzyme used for the production of xylitol, the present study was designed for the cloning of xylitol dehydrogenase gene from Glcunobacter oxydans DSM 2003. After extraction of genomic DNA from this bacterium, xylitol dehydrogenase gene was replicated using polymerase chain reaction (PCR). The amplified product was entered into pTZ57R cloning vector by T/A cloning method and transformation was performed by heat shocking of the E. coli XL1-blue competent cells. Following plasmid preparation, the cloned gene was digested out and ligated into the expression vector pET-22b(+). Electrophoresis of PCR product showed a 789 bp band. Recombinant plasmid (rpTZ57R) was then constructed. This plasmid was double digested with XhoI and EcoRI resulting in 800 bp and 2900 bp bands. The obtained insert was ligated into pET-22b(+) vector and its orientation was confirmed with XhoI and BamHI restriction enzymes. In conclusion, in the present study the recombinant expression vector containing xylitol dehydrogenase gene has been constructed and can be used for the production of this enzyme in high quantities.

This study was designed to assess the effect of five common anticonvulsant drugs on naloxone-precipitated withdrawal syndrome in morphine-dependent mice. Male mice (25-35 g) were made dependent by increasing doses of morphine (30-90 mg/kg). At least three doses of phenytoin, carbamazepine, sodium valproate, lamotrigine and topiramate were injected i.p. to morphine-dependent mice 45 min prior to induction of withdrawal syndrome by naloxone (5 mg/kg, i.p.). Control animals received vehicle. Number of jumpings was counted and ptosis, tremor, piloerection and diarrhea were checked in a 30 min period started just after naloxone injection. Results showed that lamotrigine, phenytoin and sodium valproate were ineffective in suppression of withdrawal syndrome while carbamazepine produced a dose-dependent reduction of jumpings. Topiramate at the maxium applied dose (100 mg/kg) significantly reduced number of naloxone-elicited jumpings. It seems that carbamazepine by inhibition of N-Methyl-D-Aspartate (NMDA) receptors and topiramate by inhibiting kainite-activated (AMPA) receptor antagonists suppress morphine withdrawal syndrome but further studies are needed to have a definite conclusion.

Chlorogenic acid, a pharmacologically important compound, is a phenolic compound that occurs in certain commonly used medicinal herbs. We looked for the presence of this compound in the callus cultures of Varthemia persica DC (var. persica). We have evaluated the conditions for establishment of callus cultures of V. persica and the in vitro production of chlorogenic acid. Callus was initiated by culturing seedling of V. persica on MS basal medium supplemented with different concentrations of kinetin, naphthalene acetic acid and 2,4-diphenoxy acetic acid. Also, the influence of light, and phytohormones on the production of chlorogenic acid was examined. Kinetin stimulated the production of chlorogenic acid. Replacement of 2,4-diphenoxy acetic acid with naphthalene acetic acid did not alter the chlorogenic acid production. The ability to induce the accumulation of chlorogenic acid in the V. persica callus cultures offers an opportunity to produce a phenolic compound with therapeutic value.