MOSP - Macao Scientific Publishers

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Pharmacological justification for the ethnomedical use of Datura Stramonium stem-bark extract in treatment of diseases caused by some pathogenic bacteria

M. H. Shagal*, U.U. Modibbo, and A. B. Liman

Abstract: Phytochermical screening and antimicrobial activity of the aqueous and ethanolic extract of the stem-bark of Datura stramonium was carried out. The extraction with the two solvents (water and ethanol) was carried out at room temperature. The phytochemical investigations include saponins, tannins, steroids, alkaloids, flavonoids, phenols and glycosides. The antimicrobial activity was investigation on Staphylococcus aureus, Salmonella typhi, Shigella spp, Eschericia coli, Klebsiella pneumonia and Neisseria gonorrhea. The results revealed the presence of saponins, steroids, alkaloids, and glycosides in both the extracts. Flavonoid was present only in the ethanol extract. The antimicrobial activity revealed that ethanolic extract showed more antibacterial activity than the aqueous extract. It showed some activities against all the tested bacteria except Neisseria gonorrhea. The aqueous extract only showed activity against Staphylococcus aureus. Keywords: Datura stramonium, alkaloids, Microbes, antimicrobial activity, ethanolphytochemical screening.[...] Read More.

Keywords: Datura stramonium, alkaloids, Microbes, antimicrobial activity, ethanolphytochemical screening.

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Evaluation of response to loading doses of clopidogrel therapy in patients undergoing percutaneous coronary intervention (PCI)

Kheria Saade, *Manal El-Hamamsy, Mona Hamdy, Ahmed Magdy Mohamed

Abstract: Clopidogrel resistance plays a key role in ischemic recurrence after Percutaneous coronary intervention (PCI). The cytochrome P450 (CYP)–dependent conversion of Clopidogrel to its active metabolite may contribute to the variability in antiplatelet effect of Clopidogrel. To evaluate the response to 600 mg Clopidogrel loading dose versus 300 mg loading dose in patients undergo PCI. A total of 51 patients categorized to two groups: Group I consisted of 11 males (64.7%) and 6 females (35.3%) received 300 mg loading does, while Group II consisted of 28 males (82.4%) and 6 females (17.6%) received 600 mg Clopidogrel loading does. Detection of Clopidogrel response was assessed by measuring of the platelet aggregation percentage and CYP2C19 *2 assay in both groups. Clopidogrel resistance was defined by an arbitrary cut off value of ˂10% with respect definition as compared to control value. The percentage of Clopidogrel response among the studied patients was 29.2% for 300 mg Clopidogrel and 70.8% for 6oo mg Clopidogrel loading dose. In non or poor response to Clopidogrel group 10 patients (37%), were resistance to 300mg dose and 17 patients (63%) were resistance to 600mg Clopidogrel dose. Clopidogrel resistance groups were more likely have CYP2C19 genotype (CYP2C19*1.CYP2C19*2) (GA). There were highly significant association between good response group, non and poor response groups as regarding to genotype CYP2C19*1, CYP2C19*1 (GG) carriers and CYP2C19*1, CYP2C19*2 (GA) carriers. Platelet aggregation after 600mg Clopidogrel in both CYP2C19*1, CYP2C19*1 (GG) carriers and CYP2C19*1, CYP2C19*2(GA) carriers is statistically non significant with basal aggregation, before PCI and after PCI, while significant with day after PCI and highly significant with inhibition percentage before PCI. Platelet aggregation after 300mg Clopidogrel in both CYP2C19*1, CYP2C19*1 (GG) carriers and CYP2C19*1, CYP2C19*2(GA) carries is a statistically non significant with basal aggregation, before PCI, day after PCI, and after PCI, while significant with inhibition percentage before PCI. There was no variable individual response to the anti platelet effect of the standard dose (300mg) and higher loading dose (600mg) Clopidogrel therapy, but a variable individual response to Clopidogrel between patients carries CYP2C19*1.CYP2C19*2 (GA) genotype and carries CYP2C19*1.CYP2C19*1 (GG) genotype. Keywords: Clopidogrel, loading dose, cardiology, clinical pharmacy[...] Read More.

Keywords: Clopidogrel, loading dose, cardiology, clinical pharmacy

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Identification and spectrophometric determination of hydroquinone levels in some cosmetic creams

P. O. Odumosu* and T. O. Ekwe

Abstract: Hydroquinone, a dihydroxylated benzene derivative is used therapeutically as a topical agent for the treatment of certain skin conditions. Ten (10) cosmetic creams containing hydroquinone were randomly sampled based on consumer demand from the open market in Jos, Plateau State. The labels on the packages noticeably did not indicate the levels of hydroquinone present. The creams were subjected to colour and chromatographic test for identification, as well as assay by UV spectrophotometry. All ten (10) creams sampled, gave positive results to the test for hydroquinone. The level of hydroquinone was below 2% for seven of the creams, between 2 - 5% for two and above 5% for one. (The upper limit for cosmetic creams is 2 and 5% for therapeutic use). This study shows that despite the potential health hazards of hydroquinone, cosmetic products containing this agent are available for sale in the open market with inadequate warning on the labels.[...] Read More.

Keywords: Spectrophotometric analysis, hydroquinone, cosmetics.

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Anti-helicobacter pylori and protective effects of aqueous Fumaria vaillantii L extract in pylorus -ligated, indomethacin- and toxic-induced ulcers in rats

Rifat-uz-Zaman* and Attiq-ur-Rehman

Abstract: This paper evaluated anti-ulcer, anti-secretory and anti-helicobacter pylori effects of folkloric medicinal plant, Fumaria vaillantii L, in rats. Different toxic agents; ethanol (80%), NaOH (0.2 mol/L), NaCl (25%) and indomethacin (30 mg/kg, body weight) were used to produce acute gastric ulceration in rats. Anti-secretory studies were undertaken by using pylorus-ligation, Shay rat technique. F. vaillantii L aqueous extract (Aq-FV) was used in three doses (100, 200 and 300 mg/kg bodyweight). Aq-FV was further tested for anti-H. pylori activity. Extract significantly attenuated gastric mucosal damage induced by toxic agents and indomethacin in rats. Aq-FV restored partially mucus secretion in indomethacin model. In pylorus-ligated rats, Aq-FV significantly reduced the basal gastric acid secretion, acidity and ulceration. Aq-FV possesses significant and more potent anti- ulcer and cytoprotective activities against experimentally-induced gastric ulcers in comparison to Omeprazole. Extract showed significant but less potent anti-H. pylori activity in comparison to Clarithromycin. Evaluation agreed with the folkloric use of F. vaillantii L as anti-ulcer and anti-secretory tool.[...] Read More.

Keywords: Fumaria vaillantii L, cytoprotection, gastric ulcer, gastric secretion, gastric wall mucus, anti-helicobacter pylori.

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Gastroprotective effect of Phyllanthus niruri leaf extract against ethanol-induced gastric mucosal injury in rats

Mahmood Ameen Abdulla*, Khaled Abdul-Aziz Ahmed, Fouad Hussain AL-Bayaty and Yaghma Masood

Abstract: The main objective of this study is to evaluate the gastroprotective activity of the Phyllanthus niruri leaf extract against ethanol-induced gastric mucosal injury in rats. Six groups of Wistar rats were pre-treated, respectively, with distilled water; omeprazole 20 mg/kg; and 250, 500, 750 and 1000 mg/kg P. niruri leaf extract 30 min before oral administration of absolute ethanol to generate gastric mucosal injury. After one hour later, the rats were sacrificed and the ulcer areas of the gastric walls were determined. Gross evaluation has revealed that the negative control rats exhibited severe mucosal injury, whereas, pre-treatment with P. niruri leaf extract resulted in significantly less gastric mucosal injury and flattening of the mucosal folds. Histological studies of the gastric wall revealed that negative control rats suffered very severe damage of gastric mucosa, along with edema and leucocytes infiltration of the submucosal layer compared to rats pre-treated with P. niruri leaf extract where there was marked gastric protection along with reduction or inhibition of edema and leucocytes infiltration of the submucosa. The present finding suggests that P. niruri leaf extract promotes ulcer protection as ascertained by the comparative decreases in ulcer areas, inhibition or reduction of edema and leukocyte infiltration of the submucosa.[...] Read More.

Keywords: Phyllanthus niruri, rat, gastroprotection, ulcer.

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Synthesis and antimicrobial screening of peptidyl derivatives of bromocoumarins/methylimidazoles

Rajiv Dahiya*, Rita Mourya and Subhash Chand Agrawal

Abstract: In this investigation, it was of interest to synthesize novel series of peptide analogs of 3-bromocoumarins and 2-methylimidazoles. Substituted coumarinyl-oxyacetic acids 1, 2 were synthesized by alkylation of corresponding hydroxycoumarins with chloroacetic acid. The imidazolyl derivatives 13, 14 were prepared by interaction of 2-methylimidazole with substituted/unsubstituted anthranilic acids. Coupling of compounds 1, 2, 13 and 14 with different amino acid methyl ester hydrochlorides, dipeptide, tripeptide and tetrapeptide methyl esters afforded novel coumarino/imidazolopeptide derivatives 3-10 and 15-22. Selected peptide ester derivatives were further hydrolyzed by using lithium hydroxide to afford corresponding acid derivatives 11, 12 and 23, 24. The antibacterial and antifungal effects of synthesized peptide derivatives were studied against eight pathogenic microbes. Among the tested compounds, 19, 22 and its hydrolyzed analog 24 exhibited good antimicrobial activity against Pseudomonas aeruginosa, Klebsiella pneumoniae, Trichophyton mentagrophytes and Microsporum audouinii, and compounds 8, 10 and 12 displayed good antifungal activity against Candida albicans with minimum inhibitory concentration of 6.25 g/ml.[...] Read More.

Keywords: Bromocoumarin, methylimidazole, anthranilic acid, peptide coupling, antibacterial activity, antifungal activity.

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Safety research on community pharmacies in Kocaeli

Ozlem Nazan Erdogan* and Safiye Kaya

Abstract: The aim of this research was to understand the precautionary measures of pharmacies in terms of safety issues of service. There are 322 community pharmacies in Kocaeli. Cluster sampling was used to select the community pharmacies included into the study. Four of eight regions were selected to this end. Throughout December 2005, face-to-face questionnaires were administered in 156 of 247 community pharmacists in four regions. Two thirds of community pharmacists (33.3%) have described the service area as unsafe. Eighty-eight (88) pharmacists who had inadequate safety measures in their pharmacy indicated 122 reasons. Cost accounted for 64% of these reasons, lack of necessary regulations for 31%, lack of managerial direction for 21%. Pharmacists who had not experienced any threat to security of life and property (n = 47, 40.2%) used a higher ratio of new technology methods (safety measures alarm systems to inform the police and private security firms, sensors on windows and doors, digital video recording systems). Traditional safety measures taken by pharmacists were cameras, window-guards, guns and other objects used as weapons (such as metal bars) and never being alone on night duty. 64% of pharmacists explained their safety measures against earthquake as fixing shelves to the wall. It is understood that in 56% of community pharmacies, there was no provision made for drugs which need to be kept cold during power outages. Thus, In-services needs have to be made and provided for pharmacist regarding safety issues.[...] Read More.

Keywords: Safety, management, security system, community pharmacy, drug.

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Phenolic content and antioxidant activity of crude and fractionated extracts of Pereskia bleo (Kunth) DC. (Cactaceae)

K. S. Sim, A. M. Sri Nurestri * and A. W. Norhanom

Abstract: The total phenolic content of the extracts of Pereskia bleo were assessed by the Folin-Ciocalteau’s method while the antioxidant activities were determined by three different assays, namely scavenging activity on 1,1- diphenyl-2 -picrylhydrazyl (DPPH) radicals, reducing power assay and ß-carotene method. In the present study, the ethyl acetate extract exhibited the highest total phenolic content (40.12 mg of GAEs/g of extract) and showed the strongest antioxidant activity in the ß -carotene bleaching assay significantly. Whilst, the hexane extract showed significantly the highest antioxidant activity when determined by scavenging effect on DPPH radicals (EC50 210 µg/ml) and the reducing power assay.[...] Read More.

Keywords: Pereskia bleo, Cactaceae, antioxidant activity, phenolic content.

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Efficacy and safety of long-acting risperidone on early onset schizophrenia in adolescent patients

Liming Ruan, Shaohua Hu, Manli Huang, Jianpo Hu and Wei Cai*

Abstract: The present study is aimed at evaluating the efficacy and safety of long-acting risperidone on early onset schizophrenia in adolescent patients. A total of 31 adolescent patients (13 - 18 years) with schizophrenia met the DSM-IV-TR criteria for schizophrenia and their symptoms were stable when orally taking risperidone or olanzapine. They were admitted into a 24 week, open-label study on the long-acting risperidone. Risperidone was administered every 2 weeks at a dose of 25, 37.5 and up to a maximum dose of 50 mg. The Positive and Negative Syndrome Scale (PANSS), the Clinical Global Impressions (CGI) and the Extrapyramidal symptom rating scale (ESRS) were used to assess the improvement in the symptoms. Improvements in the symptoms of schizophrenia occurred in patients treated with long-acting risperidone at week 6 and continued throughout the study with significant reduction in total PANSS score at week 24 ( -4.2 ± 0.2, P < 0.01). At the same time, 51.6% of patients were rated as clinical improvement at the end of study. Among these 31 cases, the most frequently reported adverse events were depression (12.9%), anxiety (9.7%), headache (9.7%) and insomnia (6.4%). ESRS scores were reduced during the treatment with long-acting risperidone. The mean decrease in serum prolactin and body weight was 13.1 ng/ml and 4.5 kg, respectively. Intramuscular administration of long-acting risperidone was safe and well tolerated in adolescent patients. Long-acting risperidone also could improve the symptoms of schizophrenia in adolescent patients.[...] Read More.

Keywords: Long-acting risperidone, early onset schizophrenia, oral risperidone, olanzapine, adolescents.

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Effects of corn peptides on exercise tolerance, free radical metabolism in liver and serum glutamic-pyruvic transaminase activity of mice

Fusheng Miao*, Wenqian Yu, Yaoguang Wang, Meijuan Wang, Xiangyan Liu and Fenglin Li

Abstract: In order to carry out research on the effects of corn peptides on exercise tolerance, free radical metabolism in liver and serum Glutamic-pyruvic transaminase (GPT) activity of mice, sixty Kun-Ming male mice were randomly divided into two experimental groups, that is , Group (20 mice) and Group (40 mice). Group was a quiet group in which the mice were not trained; Group was a trained group in which the mice were trained. Either group was divided into control group and administered group. The control groups were administered with 1.5 ml distilled water by gavage every morning. The administered groups were administered with 1.50% corn peptides solution at the same dose for 28 days. The trained groups were trained to swim for 4 weeks and then were forced to swim without a load until being exhausted. The time of swimming to exhaustion and the Superoxide dismutase (SOD), Malondialdehyde (MDA) of liver and serum GPT were measured. The results indicated that corn peptides could significantly increase the body exercise tolerance, have a potent function of anti-lipid peroxidation injury and could reduce the body damage caused by endogenous free radicals produced in the movement. In addition, corn peptides had obvious protective effects on the body's liver cell membrane.[...] Read More.

Keywords: Corn peptide, exercise tolerance, free radicals, glutamic-pyruvic transaminase.

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