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Satyrium nepalense: A RARE MEDICINAL ORCHID OF WESTERN HIMALAYA (INDIA); PHYTOCHEMICAL SCREENING, ANTIMICROBIAL EVALUATION AND CONSERVATION STUDIES
Satyrium nepalense is an endangered medicinal herb found at the higher altitude of 2400-5000m. Local inhabitant used tubers of Satyrium nepalense as an energetic tonic and as an important medicine to cure different type of fever in traditional health care system of Uttarakhand (INDIA). Present study was carried out to evaluate the phytochemical, antibacterial screening against four (Streptococcus mutans, Pseudomonas aeruginosa, Staphylococcus aureus and Klebsiella pneumoniae) microorganisms in methanolic extracts and habitat studies for conservation of S. nepalense. Tubers of Satyrium nepalense were extracted separately with methanol by hot extraction process using soxhlet apparatus. The extracts were subjected to Lyophilization to get dry extract and preserved in aseptic condition. The different group reagents used for phytochemical screening as dragendorffs’s for alkaloid, molisch’s test for carbohydrates, shinoda test for flavonoids etc. Antibacterial study was carried out by disc diffusion method. The highest zone of inhibition was recorded as 15.0±0.00 mm against Klebsiella pneumonia and 15.0±0.82 mm against Staphylococcus aureus. Phytochemical screening shows the presence of alkaloids, carbohydrates/glycosides, flavonoids and unsaturated sterols/triterpenes in Satyrium nepalense. The result indicates that methanolic extract of Satyrium nepalense shows potent antibacterial activity against all four bacterial strains.Key words: Uttarakhand, Satyrium nepalense, medicinal orchid, antibacterial, phytochemical
PHYTOCHEMICAL SCREENING AND ANALYSIS POLYPHENOLIC ANTIOXIDANT ACTIVITY OF METHANOLIC EXTRACT OF WHITE DRAGON FRUIT (Hylocereus undatus)
White dragon fruit is a well known and widely used herbal medicine, especially in Asia, which contains several interesting bioactive constituents and possesses health promoting properties. The aim of this study was to analyze for the bioactive compounds, evaluate total phenolic contents and antioxidant capacities of methanolic extract of white dragon fruit. The antioxidant activity was determined by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity assay. Total phenolic content were determined by Folin-Ciocalteu method. Phytochemical screening of the white dragon fruit showed the presence of triterpenoid, alkaloid, flavonoid and saponin. The extract exhibited strong antioxidant activity with IC50 of 193 μg/mL, and total phenolic content of 246 μg/mL in 1 Kg dry extract.Key words: antioxidant activity, total phenolic, DPPH, white dragon frui
DEVELOPMENT THE VALIDATION OF INDONESIAN VERSION OF SF-36 QUESTIONNAIRE IN CANCER DISEASE
A Cancer patients need long term therapy in the treatment of their disease. One of the outcome of cancer treatment in patients of quality of life. Because of the limited instrument for measuring cancer patients’ quality of life in Indonesian version, thus this study is aimed to develop the validation of Indonesian version of Short Form-36 questionnaire in cancer patients. The observational study was carried out in this study. Data were collected from cancer patients in the Oncology Department of Sardjito Hospital, Yogyakarta, Indonesia, who were treated with cisplatin at the dosage of ≥ 50mg/m2 as monotherapy or in combinations. The validation process involved known-group validity, discriminant validity, convergent validity and factor analysis. About 203 subjects who were diagnosed with cancer were recruited in this study. Theknown-group validity test showed that there were no significant differences of SF-36 domains among different diagnosa. All of the questions met the criteria of convergent validity except for the questions number 26, 28, 30 and 32. Furthermore, the questions number 2 and 28 did not meet the criteria of discriminant validity. This study presents that many questions are needed to be reconstructed, due to the result of factor analysis which showed that those questions are loaded significantly with other domain’s questions. The development of Indonesian version of SF-36 scales in cancer disease is still less unstatisfactory. According to the result of this study, future study with new construction of questions in this version is still necessary.Key words: validation, SF-36, Indonesia, cancer
SYNTHESIS AND ANALGESIC ACTIVITY OF 6-(MNITROPHENYL)-4-SUSTITUTED BENZYLIDENE-4,5-DIHYDROPYRIDAZIN-3(2H)-ONE DERIVATIVES
Many research groups have been interested in 3(2H)-pyridazinones for the development of potential analgesic and antiinflammatory agents. Stimulated by these findings, three 6-(mNitrophenyl)-4-sustituted benzylidene-4,5-dihydropyridazin-3(2H)-ones (IVa-IVc) have been synthesized and evaluated for analgesic activity against hot plate method. Compounds IVa-IVc were prepared from 6-m-nitrophenyl-4,5-pyridazin-3(2H)-one by condensation with respective aldehydes. All compounds (IVa-IVc) having nitro phenyl and benzylidene groups at position 6 and 4 of the pyridazinone ring receptively. All compounds (IVa-IVc) showed significant analgesic activity when compare to control group and were found less potent than reference drug aspirin.Key words:Pyridazinones, analgesic, benzylidene, nitrophenyl
PREDICTORS OF THE USE OF GASTROPROTECTIVE AGENTS IN PATIENTS USING NSAID IN YOGYAKARTA INDONESIA
Non Steroid Anti-Inflammatory (NSAID) is one type of AntiInflammatory drug that is used to treat pain in patients of osteoarthritis (OA) and rheumatoid arthritis (RA). The use of NSAIDs can cause gastrointestinal side effects. To prevent the side effects, NSAIDs are prescribed in combination with gastroprotective agent (GPA). The aim of the study is to determine the factors considered in the GPA prescription by the doctors in patients who have risk factors for gastric disorder due to NSAIDs use. This study was performed using a cross-sectional observational design. The data were collected retrospectively during a period of January to December 2010. The subjects were OA and RA patients considering the inclusion and exclusion criteria. The data included patient characteristics (gender, age, occupation, payment method, the primary diagnosis), prescription of NSAID, prescription of GPA, history of gastrointestinal disease, NSAID prescription with corticosteroids, prescription with antiplatelet. The data were processed descriptively and quantitatively, and analyzed statistically using chi-square and log. regression with 95% Confidence Interval. The results showed that there were correlation between some predictor factors with prescription of gastroprotective agent. These factors were women patient, patient age of ≥ 65 years, oxicam prescribing, diclofenac sodium prescribing, prescribing >1 type of NSAIDs, prescription of NSAID concomitant with corticosteroids, prescription of NSAID concomitant with antiplatelet, patients with history of gastrointestinal, prescribing NSAIDs with duration of ≥ 3 months. Patient with a history of gastrointestinal disease was the most predictor influential factor, with OR (odds ratio) of 3.6 (95% CI: 2.79 - 4.66). Predictor factor of patients with a history of dyspepsia possessed the highest OR {OR=4,29 (CI 95%: 3.23–5.7)}. It means that patients with a history of dyspepsia prescribed NSAIDs would have greater risk of 4.29 times to get GPA prescription than patients without a history of dyspepsia. Prescribing NSAIDs > 1 DDD (defined daily dose) had p value of 0.777, which means there was no relationship between GPA prescription with NSAIDs > 1 DDD prescription.Key words: Gastroprotective Agent, Non-steroid anti-inflammatory, Osteoarthritis, Rheumatoid Arthriti
ANTHELMINTIC ACTIVITY OF Cuminum cyminum, FOENICULUM VULGARE AND Eugenia caryophyllusAGAINST Pheritima posthuma
Ethanol extract of fruit of Cuminum cyminum (EECC), aqueous extract of fruit of Cuminum cyminum (AECC), Ethanol extract of fruit of Foeniculum vulgare (EEFV), aqueous extract of fruit of Foeniculum vulgare (AEFV) and Ethanol extract of flowering bud of Eugenia caryophyllus( EEEC), aqueous extract of flowering bud of Eugenia caryophyllus( AEEC) were taken up for in vitro studies on the Anthelmintic activity against Pheritima posthuma. Different concentrations (25, 50, 100, 200mg/mL) were used for the activity is compared with the reference standard Albendazole at concentration 20mg/mL and normal saline( 0.9% NaCl) was used in control treatment. The results were expressed in terms of time in minutes to report the time of paralysis and time of death of the earth worms. The results obtained from study indicate towards anthelmintic activity, supporting folk used of all three plants compared with reference standard. The result established that EEEC and AEEC is more potent as compared with EECC, AECC and EEFV, AEFV.Key words: Anthelmintic activity, Cuminum cyminum, Eugenia caryophyllus, Foeniculum vulgare, Pheritima posthuma.
ANTIOXIDANT ACTIVITY OF ETHYL ACETATE EXTRACT OF RED Psidium guajavaL. LEAVES GROWN IN MANOKO, LEMBANG - INDONESIA
Psidium guajava L. (Myrtaceae) is a well known plant in Malaysia and Indonesia. Its leaves extract was found to possess antidiarrhea, antimicrobial, hepatoprotective and antioxidant activities. Objective of this research is to isolate an antioxidant subtance from Red Psidium guajava L. leaves. The crude leaves was extracted using Soxhlet apparatus by gradual polarity of three different solvents, n-hexane, ethyl acetate and methanol. Antioxidant activity of each extract was tested by using DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging method. Total phenol, total flavonoid and total tannin content of the extracts were also measured. Ethyl acetate extract was fractionated using vacuum liquid chromato-graphy for fractionation. Purification was performed using TLC preparative. Isolate then characterized using specific spray reagent, UV-Vis spectrophotometry and infrared spectrophotometry. Crude drug of Psidiumguajava contained flavonoid, tannin, quinone, saponin and steroid/ triterpenoid. Antioxidant activity of ethyl acetate extract is 65.63% with total phenol 4.25%, total flavonoid 0.53% and total tannin 1.16%. Antioxidant compound N was isolated from ethyl acetate extract.Antioxidant compound N was supposed to be aglycone flavone that has OH at C -4’, C-5 and C-7.Key words: Psidium guajava L. , antioxidant activity, ethyl acetate extrac
QSAR MODELING OF 2-[CH(OH)X]-5,8-(OY)2 -1,4-NAPHTHOQUININES AGAINST L1210 CELLS USING MULTIPLE LINEAR REGRESSION
Quinones are present in many drugs such as anthracyclines, daunorubicin, doxorubicin, mitomycin, mitoxantrones and saintopin, which are used clinically in the therapy of solid cancers. The cytotoxic effects of these quinone are mainly due to the inhibition of DNA topoisomerase-II. It is the necessity to develop the 1,4-Naphthoquinone analogues with Cytotoxic effect. Here 2-[CH(OH)X]-5,8-(OY)2-1,4-Naphthoquinines analogues have been used to correlate the cytotoxic activity with the Eccentric Connectivity index (ECI), Fragment Complexity (FC) and McGowan Volumes (MG) for studying the Quantitative Structure Activity Relationship (QSAR). Correlation may be an adequate predictive model which can help to provide guidance in designing and subsequently yielding greatly specific compounds that may have reduced side effects and improved pharmacological activities. We have used Multiple Linear Regression (MLR), one of the best methods for developing the QSAR model. Results from this QSAR study have suggested that ECI, FC and MG are the important descriptors for cytotoxic activities of 1,4-Naphthoquinones against L1210 cells. For the validation of the developed QSAR model, statistical analysis such as data point-descriptor ratio, fraction of variance, cross validation test, standard deviation, quality factor, Fischer’s test; and internal validation such as Y-randomization test have been performed and all the tests validated this QSAR model.Key words: 1,4-Naphthoquinones, QSAR, Eccentric connectivity index, Fragment complexity, McGowan Volume, Multiple Linear Regression
PASSIVE AND IONTOPHORETIC PERMEATION OF CAPTOPRIL GEL: AN IN VITRO AND IN VIVO STUDY
The Objective of this work was to formulate and evaluate captopril gel to assess its suitability for transdermal delivery by passive and iontophoresis. A polymer gel was prepared using hydroxypropyl methyl cellulose and in vitro skin permeability was assessed in full thickness skin of rabbits and pigs. For in vivo studies New Zealand rabbits were used. In vitro passive permeation was carried out in Franz diffusion cell but for iontophoresis, diffusion cell was modified according to Glikfield design. Iontophoresis was performed at a current density of 0.5 mA/cm2via silver /silver chloride electrodes with passive controls but for in vivo study current density wasreduced to 0.1 mA/cm2. Blood samples were analyzed for drug content by HPLC. Results of the in vitro study indicated that iontophoresis considerably increased the permeation rate of captopril compared to passive controls in both the skin types (P<0.01). The plasma concentration of captopril was significantly higher (P<0.001) than that obtained in the passive controls. Results showed that the target permeation rates for captopril could be achieved with the aid of iontophoresis by increasing the area in an appreciable range.Key words: Captopril, iontophoresis, transdermal, Rabbit, Pigskin, in vitro, in vivo
IN VIVO EVALUATION OF MISOPROSTOL FLOATING MICROSPHERES
Prostaglandin (PG) has been reported to be an important protective and acid suppressive factor in the gastric mucosa. The objective of the study was to develop and evaluate a stomach specific drug delivery system for controlled release of Misoprostal a PE analogue for gastric ulcer induced NSAIDs. Floating microspheres were prepared by emulsification-solvent evaporation method using ethyl cellulose as a polymer, carbopol as mucoadhesive polymer. Ulcers were induced by the oral administration of absolute ethanol (5 mL/kg) to 24 h fasted Wistar male rats (n=8), weighing 200 g. Sodium bicarbonate solution, misoprostal solution and drug loaded microspheres were tested. Formulations were administered orally 1h before the administration of ethanol. Prior to the oral administration, rats were anesthetized with ethylic ether. After 2 h of ethanol administration, animals were sacrificed; the stomachs were removed, opened along he greater curvature and examined for lesion measurements. Ulcer indexes (UI) were calculated. The in vivo evaluation showed that ulcer index values were 0.61 ± 0.14 for the sodium bicarbonate solution, 0.58 ±0.18 for the misoprostal and 0.11 ± 0.06 for the misoprostal-loaded microspheres. The KruskalWallis test detected statistical differences (p =0.002) between the ulcer indexes. The multiple analyses (Student-Newman-Keuls) showed that the misoprostal loaded microspheres presented a gastric ulcer index statistically lower than that of the sodium bicarbonate solution (p = 0.001) and the misoprostal solution (p = 0.021). The percentages of ulceration inhibition were 31 and 75% after the administration of misoprostal solution and microspheres, respectively. In conclusion, the in vivo evaluation showed that the microspheres presented ulcer index lower than the solutions, showing that misoprostal-loaded microspheres were efficient in protecting the stomach against ulcer formation.Key words: Misoprostal, microspheres, ulcer index,