IRANIAN JOURNAL OF PHARMACOLOGY AND THERAPEUTICS (IJPT)
Year:2011 | Volume:10 | Issue:1|Papers Count:9

Phytochemical investigations of Piper sarmentosum Roxb., yielded four compounds; three amides, identified as 3- (3’, 4’, 5’-trimethoxyphenylpropanoyl) pyrrolidine, 3- (4’-methoxyphenylpropanoyl) pyrrole, N-(3-phenylpropanoyl) pyrrole and a sterol namely b-sitosterol.3- (4’-Methoxyphenylpropanoyl) pyrrole was found for the first time in this Piper species. All chemical constituents were tested for their antibacterial activity using disk diffusion method and cytotoxicity screening using sul-forhodamine B (SRB) assay. All of the compounds were found only active towards gram-positive bacteria except 3- (4’-methoxyphenylpropanoyl) pyrrole with no activity against both gram-positive and gram-negative bacteria. Meanwhile, the cytotoxicity screening using SRB assay indicated that none of these compounds was active as an anticancer agent.

Aqueous extract and volatile oil were obtained from Miliusa tomentosa by using soxhlet extractor and hy-dro distillation with a Clevenger-type apparatus respectively. The extract and volatile oil both were screened for Antimicrobial activity against different bacteria (Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Klebsiella pncumoniae, Pseudomonas aeruginosa, Bacillus pumilis) and fungi (Candida albicans, Aspergillus niger, Fusarium monoliforme, Trichoderma viridae, Phanerochaete chrysosporium and Pcilomyces species) by cup plate diffusion method. Minimal Inhibitory Concentration (MIC) values of aqueous extract and volatile oil obtained were determined using modified cup plate method. The aqueous extract exhibited weak activity against all the bacteria and one fungi (Candida albicans), while volatile oil showed strong activity against most bacteria including Escherichia coli, Bacillus subtilis, Pseudommonas aeruginosa, Klebsiella pneumoni. Also, a moderate activity was seen against Staphylococcus aureus and Bacillus pumilis. It also showed strong activity against fungi like Candida albicans and Fusarium monoli-forme, whereas moderate activity was observed on Aspergillus niger, Trichoderma viridae and the weak activity against the remaining fungi. It can be concluded that Miliusa tomentosa leaf volatile oil finds its use as broad-spectrum antimicrobial agent after extensive investigation, and this may provide a basis for the isolation of constituents of biological interest from Miliusa tomentosa for its potent activity.

Spasticity or increase in muscle tone is one of the problems following stroke. Due to this increase in muscle tone, patients are confronted to problems in motor control and difficulties in activities of daily living and complications such as shortness and contracture. The aim of this study is to compare the effects of using splint or botulinum toxin injection on spasticity, range of motion and upper extremity function in a 3-month period. The method of this research study was a two comparison design, done in rehabilitation clinics in Tehran. At first, 50 patients with chronic stroke were selected and based on the inclusion criteria, a total of 28 stroke patients after completing the consent forms were entered to intervention groups of splint or botulinum toxin injection and they were followed up about 3 months. At last, 18 patients completed the study. Goniometery was the method to measure range of motion, and Modified Ashworth scale was used to examine the spasticity and the upper extremity function was scored based on Fugl-Meyer assessment. All outcome measures improved in each group, but the differences between two groups were not significant (p value >0.05). In this study, the effects of botulinum toxin injection and Volar-Dorsal Wrist/Hand Immobilization splint were not significantly different between the interventions in a 3-month follow-up.

The pharmacokinetics of cefpirome after a single intravenous injection of 10 mg.kg-1 was studied in febrile cross-bred calves.E. coli endotoxin was administered intravenously to induce fever in calves. Blood samples were collected at different time intervals and cefpirome levels were estimated by using microbiological assay technique. Based on the plasma drug levels, the pharmacokinetic parameters were determined. Maximum concentration of cefpirome was attained at 1 min and the drug was detected above MIC in plasma up to 12 h after its administration. The values of t1/2a, Vdarea and AUC were 0.06±0.003 h, 0.75±0.02 L.kg-1 and 36.6±0.82 mg.ml-1.h. The high values of t1/2b (1.90±0.03 h) and ClB (0.27±0.006 L.kg-1.h-1) reflected rapid elimination and body clearance of the drug in febrile calves. The study suggested that cefpirome was rapidly distributed and rapidly eliminated in febrile crossbred calves.

The present study was conducted to evaluate the protective effect of methanolic leaf extract of Caesalpinia bonduc (L.) on gentamicin-induced hepatotoxicity and nephrotoxicity in rats. A control group (saline, group I, n=6) was compared with rats administrated 80 mg/kg gentamicin, once daily for 7 days (groups II, III and IV). The effect of methanolic leaf extract of Caesalpinia bonduc (group III and IV) at a dose level of 250 mg/kg and 500 mg/kg was compared in gentamicin-induced hepatotoxicity and nephrotoxicity. The activities of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), triglyceride (TG), bilirubin, and total protein the values of urea, sodium, potassium and chloride were significantly increased in rats exposed to gentamicin. Moreover, administration of gentamicin resulted in damage to liver and kidney structures. Administration of methanolic extract of C. bonduc before gentamicin exposure prevented severe alterations of biochemical parameters and disruptions of liver and kidney structures. In conclusion, this study obviously demonstrated that pretreatment with methanolic extract of C. bonduc significantly attenuated the physiological and histopathological alterations induced by gentamicin. Also, the present study identifies new areas of research for development of better therapeutic agents for liver, kidney, and other organs dysfunctions and diseases.

Neutralization effects of Acorus calamus and Withania somnifera root extracts were tested against Echis carinatus venom. Both plant extracts were effectively neutralized the various pharmacological activities induced by Echis carinatus venom. About 0.14 mg of Acorus calamus and 0.16 mg of Withania somnifera root extracts were able to completely neutralize the lethal activity of 2LD50 of Echis carinatus venom. Various pharmacological activities like haemorrhagic, coagulant, edema and phospholipase activities were effectively neutralized by both plant extracts. The above observations confirmed that both plant extracts possess potent snake venom neutralizing compounds, which inhibit the activity of Echis carinatus venoms.

The novel bicyclo thieno 1, 2, 3-triazines (BTT) namely BTT-1, BTT-2, BTT-3 and BTT-4 were evaluated for analgesic, anti-inflammatory and anti-arthritic activity. Analgesic and anti-inflammatory activity was evaluated using hot plate test, formalin-induced paw licking test and formalin-induced paw edema test respectively. Complete fruend’s adjuvant (CFA) -induced arthritis model was used for anti-arthritic activity. All test drugs showed significant analgesic activity by increasing the reaction latency time in hot plate test and decreasing the number of lickings in formalin test. BTT-3 was found to be effective in both early and late phase, while all other test drugs were found to be effective only in late phase of nociception. In anti-inflammatory studies, the BTT-3 (25 and 50 mg/kg, i.p.) had significantly reduced the formalin-induced paw edema. In CFA-induced arthritis models, the BTT-3 has showed activity from the 4th day of the treatment, while all the other test drugs have showed significant inhibition of CFA-induced paw edema from the 7th day of the treatment by decreasing the elevated levels of WBC, % Hb, ESR, along with decreasing the serum levels of C-reactive protein (CRP) and rheumatoid factor (RF). In conclusion, all test drugs were found to possess very good analgesic, anti-inflammatory and anti-arthritic activity and BTT-3 was found to be more potent compared to other compounds.

The effects of Tahitian noni juice (TNJ), vitamin C and vitamin E on male reproductive functions in cyclophosphamide-treated wistar rats were compared. Thirty five male wistar rats with mean body weight of 180±24.3 g were randomly divided into five groups. Group one were treated with cyclophosphamide (50 mg/kg, i.p.) while, group two were treated with TNJ (10 ml/kg, i.p.) and cyclophosphamide. Group three were treated with TNJ (10 ml/kg, i.p.) alone. Group four and five were treated with cyclophosphamide and either of vitamin C (100 mg/kg) or E (1 mg/kg) respectively. All drugs were administered for four weeks. In this study, mean weight gain, sperm motility (SM), live-dead ratio (LDR), epididymal sperm counts (ESC), percentage sperm abnormality, as well as, testicular histological changes were determined. Data were expressed as mean ± standard deviation. The ESC, SM and LDR were compared with analysis of variance (ANOVA). Median score for the histologic changes was analyzed using Wilcoxon sign rank test. The mean weight gain was higher in Groups 2 and 3 compared with other groups (p<0.05). Similarly, the SM was higher in rats treated with TNJ compared with other groups (p<0.001). The LDR, ESC, and testicular histologic scores did not differ between the five groups of rats. However, the percentage sperm abnormality was lower in groups 2 and 3 (p<0.05). In conclusion, TNJ improved weight gain and protected against adverse effect of cyclophosphamide on sperm motility and abnormalities.

Drug-drug interaction (DDI) is one of the most important problems in the treatment of patients suffering from different chronic intractable diseases. The war-injured veterans are one of the groups that are prone to chronic refractory diseases. This investigation was conducted on war-injured veterans treated in a multi-disciplinary clinic in Tehran. Using Poisson model, a total of 150 patients was collected from the patients treated in a multidisciplinary clinic during three months. The prescriptions were processed using the Drug Interactions Checker. Drug interactions in these patients were categorized to three levels, i.e. mild, moderate, and severe. Drug interactions were identified in 148 patients with different intensity. Based on FDA classification, the mild, moderate, and severe DDI were observed in 56 (37.3%), 139 (92.7%), and 74 (49.3%) patients, respectively. The total number of drug interactions was 1239 in these patients. The most common type of DDI was observed in the patients who received anti-depression drugs. This study shows that war-injured veterans are a group of patients with high risk of drug interaction. The results indicate the necessity and importance of devising some guidelines to prevent or at least decrease the drug interactions in war-injured veterans with chronic refractory diseases.