JOURNAL OF RESEARCH IN MEDICAL SCIENCES (JRMS)
Year:2003 | Volume:7 | Issue:Supplement 2|Papers Count:23

Introduction. The genus Echinophora represented in the flora of Iran by four species including an endemic, E. platyloba known locally as khosharyzeh is traditionaly used in dairy as flaveuring agent.Methods. The hydrodistilled aerial parts oil of Echinophora platyloba DC. was analyzed by GC and GC/MS.Results. Eleven components have been identified, of which the major constituents were found to be trans- ß- ocimene (67.9%), 2-furanone (6.2%), myrcene (6.0'%), linalool (3.1%),and cis- ß-ocimene (2.3%).Discussion. The composition of E. platyloba oil was found to be rich in monoterpenes with predominance of hydrocarbone.

Introduction. Silybum marianum has been recognized as an antihepatotoxic plant. The active constituents of S. marianum include a group of flavonolignans known collectively as silymarin. Silymarin production by cell culture of S. marianum has been considered as a high lighted research. The succesful exploitation of S. marianum cultures requires an understanding of the physical and biochemical factors affecting flavonolignan production.Methods. Callus cultures of S. marianum were established by transferring seedling, grown on solidified MS medium supplemented with 1 ppm 2,4-Dichloro phenoxy acetic acid and 0.1 ppm kinetin. Callus cultures were subjected to various temperatures, light treatments, and culture medium pHs. Cultures were harvested after 28 days, then deried, and extracted with methanol. Qualitative and quantitative analysis of flavonolignans using TLC and spectrophotometric methods were carried out on the cells.Results. Higher levels of flavonolignan accumulation under dark rather than light and light-dark conditions were produced. The same results were observed at 20°C compared to 25°C or 30°C. Also, the culture medium pH 7 was superior to pH 5.6 or pH 9 for flavonolignan production.Discussion. The results demonstrate the influnce of temperature, medium pH, and light treatment on flavonolignan formation in S. marianum callus cultures.

Introduction. Following oral administration of nitrofurantoin (NTF), a nitrofuran antibiotic, blood concentrations are low due to rapid elimination of drug from the body. A sensitive analytical method is, therefore, required to quantify NTF blood levels for pharmacokinetic and bioequivalence studies. The aim of this study was, therefore, to develop a sensitive fluorometric assay for plasma NTF quantification using o-aminothiophenol to form a fluorescenet substance.Methods and Materials. Generally, sodium nitrate, o-aminothiophenol, and hydrochloric acid were added to 2 mL of sample containing NTF. The test tubes were then vortexed, heated in water bath and irradiated under a UV lamp. the fluorescence intensity (Fl) was subsequently measured at excitation of 375 and emission of 422 nm. To optimize the assay, the impact of solvents, type and concentration of acids, concentrations of o-aminothiophenol and sodium mitrate, the volume of organic solvents used to dissolve drug or reagents, reaction temperature, and surfactants were examined on the Fl. In order to further increase the assay sensitivity, the drug was extracted from plasma with ethylacetate and then subjected to the oputimized procedure.Results. Fl was enhanced when water was used as NTF solvent. Fl was increased with a concentration dependent manner once hydrochloric acid was used as medium acidifier. O-aminothiophenol resulted in greater Fl with a concentration dependent fashion. Considerabl Fl was also observed once volume of organic solvent reduced or the reaction temperature increased. The standard curve, covering a 50-2000 ng/mL concentration range, in plasma was linear (r2=0.999) and relative errors were within ± 14% and the CV% ranged from 2-16. Conclusions. The fluorescence method presented requires 2 mL of plasma, which can be conveniently taken from human subjects. The assay is relatively fast, sensitive, reliable, specific and applicable. The assay is especially useful for pharmacokonetic and bioequivalance studies of NTF in human beings.

Introduction. Dehydropeiandrosterone sulfate (DHEAS) is the most abundantly produced adrenal hormone, yet its biologic function has not been defined. A possible relation between DHEAS and coronary artery disease (CAD) has been suggested in some studies. On the other hand, insulin affects DHEA concentration and itself has a role in atherosclerosis. This study was designed to investigate DHEAS level and insulin resistance and their relation with serum lipids in patients with CAD.Methods. Forty men with chest pain (between 45-65 yr) who were supposed for doing angiography, participated in this study. Patients with obesity or a history of diabetes, hypertension or smoking in recent 6 months were excluded from the study. Serum samples were obtained from each patient in the morning after a 12-hour fast. They were sent for immediate FBS and lipid determination and frozen at 20°C for subsequent hormone analysis. FBS to insulin ratio was considered as an index for insulin resistance.Results. After angiography, 22 patients were assigned in CAD group, 10 in control and 8 were excluded from the study because of inaccessible angiographical response. There was no significant difference in DHEAS, insulin, FBS, lipid levels and FBS/insulin ratio between CAD patients and control group.A statistically significant positive relation between both insulin and DHEAS and LDL and total cholesterol was observed in this study. A strong advantage of our study is both - "clinical" and "angiographically" confirmation of CAD in case group.Discussion. Our findings does not support a protective role of DHEA in development of atherosclerosis. Its role as a missing link between insulin resistance and atherosclerosis has been questioned and its answer merits further investigation.These results also suggest continued skepticism about DHEA role in the etiology or prevention of coronary disease.

Introduction. S. hydrangea DC. ex Benth has been used as antireumatoid, analgesic, antihepatotoxic, carminative and antispasm in iranian traditional medicine. Also, its'anti-inflommatory, antihepatotoxic and antioxidant effects has been reported. In this study we sought to see whether S. hydrangra has any effect on immune system. Methods. S. hydrangea was collected from Dehaghan, identified and dried. Hydroalcoholic and polyphenolic extracts (by maceration) were prepared. Rosemarinic acid, a potent anti-inflommatory agent, was identified by thin layer chromatography and quantitated by spectrophotometer at 505 nm. To study the effects of S. hydrangea on acquired immunity, groups of Balb/c mice (n = 8) were used. SRBC was injected (sc, 1x108 cells/ml, 0.02 ml) and 5 days later hydroalocohofic extract (10-2000 mg/kg) and polyphenolic extract (4- 1000 mg/kg), betamethasone (4 mg/kg) or normal saline were given up. After one hour SRBC was injected to paw (sc, 1x108cells/ml, 0.02ml) and paw swelling was measured at specified intervals up to 72 hours. To investigate the effects of S. hydrangea on intrinsic immunity the same procedure was used but, animals only received one injection of SRBC to paw after administration of tested compounds. Results. The percent of concentrated total and polyphenolic extracts of S. hydrangea based on dried plant was 48.0 and 27.5 (W/W), respectively. The amount of hydroxy cynamic acid derivatives was 3.8%. Administration of SRBC induced paw swelling with maximum response at 6-8 hour in both models. Betamethasone (4 mg/kg) inhibited paw swelling in both models. Hydroalcoholic extract of S. hydrangea increased paw swelling in intrinsic immuiuty model, but its polyphenolic extract had no significant effect. Hydroalcoholic extract and Polyphenofic extract did not exhibit any effect on acquired immunity. Discussion. Our findings indicated different effects of hydroalcoholic and polyphenolic extracts of S. hydrangea on intrinsic and aquired immunity. To find out the cause of these differences, it is recomended to study the effects of different fraction of hydroxy cynamic acid and rosmarinic acid on cellular and humoral immunity.

Introduction. Amirkabiria odoratissima, a plant of umbelliferae family grows in Isfahan and chaharmahal-Bakhtiary provinces. Traditionally, it has been used as analgesic and antiinflammatory but it has not been studied pharmacologically sofar. Therefore, this study was aimed to find pharmacological evidences to support this claim.Methods. Total extract, polyphenolic extract and volatile oil were prepared according to standard methods. Analgesia was assessed using acetic cicid-induced writhing, formalin test and light tail flick, Carrageenan test was used for evaluation of antiinflammatory effect.Results. In light tail flick, total and polyphenolic extracts (500mg/100g) had not analgesic effect while essence (0.25ml/100g) at 15 to 60 minutes showed analgesic effect. All three fractions could significantly (P<0.01) decrease the number of writhes in acetic acid test. In formalin test all fractions alleviate both phases of formalin pain. Results of carrageenan test showed that these fractions have antiinflammatory effect.Discussion. The examined fractions showed analgesic and antiinflammatory effects. The plant may lack analgesic compounds with opioid-like effect since none of the fractions had good analgesia in light tail flick test. Considering the results of writhing, formalin and carrageenan test, it seems that this plant may be more effective in controlling inflammatory pain.

Introduction. The prevalence of serious mycotic infections in humans and animals has dramatically increased in the past decades. Because of the emerging resistance to polyene antibiotics and Amphotericin B, imidazole and triazole derivatives have been recently developed. In this study the antifungal properties of 1-Alkylimidazoles have been determined.Methods. Three dermatophytes (E.fluccosum, T.mentagrophytes, M.gypseum), two yeasts (T.beigelli, C.albicans), one bacteria (N.asteroids) and three agar media (S, SC, SCC) were selected for this study. Six alkylimidazoles with 8-14 carbons in their alkyl chains (octylimidazole, nonylimidazole, decylimidazole, undecylimidazole, dodecylimidazole, tetradecylimidazole) were used for demonstrating the antifungal effects of this type of compounds. The above derivatives were used in concentrations of 0.05%, 0.1% and 0.15% (V/V).Results. The results demonstrated, minimum inhibitory concentrations (MIC) 0.05% for dodecylimidazole, 0.1% for decyl and undecylimidazole, 0.1%-0.15% for nonyl and tetradecyfimidazofe and 0.15% for octylimidazole.Discussion. Out of the above alkylimidazole derivatives, dodecylimidazole had the lowest MIC while octylimidazole had the highest MlC. Therefore it can be concluded that in the alkylimidazole series the antifungal activity increases with the increase in the number of carbons in the alkyl chain (up to 12 carbons).

Introdution. The significant rise in the incidence of mycoses is due to the increased number of immunosuppressed patients, such as those with AlDS, neoplasms and transplant recepients. The usual antifungal drugs have some limitations with respect to efficacy and toxicity. Therefore, there is a need for new medications which have a better efficacy and less toxicity. Many antifungal azoles such as Isoconazole and Bifonazole have recently been developed. This study is an investigation on the synthesis of 1-Alkylimidazole derivatives.Methods. lmidazole ring was alkylated using the phase transfer technique. A quaternary ammonium salt (tetraethyl ammonium iodide) was used as phase transfer catalyst. The reaction was done between n-bromoalkanes (C4 - C14 and imidazole, in an alkaline pH and in the presence of benzene for 72 h at reflax temperature. The crude products were purified by vaccum distillation. The final compounds were identified by spectrophotometric methods.Results. 10 analogues of alkylimidazoles with the side chains: butyl, pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl and tetradecyl were synthesized. Purification of these compounds by vaccum distillation required a very low pressure (2-3mmHg). Spectrophotometric methods proved the structure of desired products.Discussion. Phase transfer technique is a quite useful route for synthesizing alkylimidazofes. In the alkylimidazole series, the boiling point increases as the alkyl chain becomes longer. Therefore for the purification of analogues with high molecular weights we need very low pressures which may result in reducing the randeman.

Introduction. Nepeta ispahanica Boiss. (Lamiaceae), is an endemic herbaceous plant, growing wild in Iran. Some of Nepeta species are used as medicinal plants in Iranian folk medicine. Because of biological activity of essential oils and in the course of studying on Nepta species, the essential oil of N. ispahanica is analyzed.Methods. Aerial parts of the wild plants of N. ispahanica were collected from Kolah-Ghazi in the south of Isfahan. The essential oil was obtained by hydrodistillation. The oil was analyzed by GC/MS method. Results. The aerial parts of N. ispahanica contained 0.4% (v/w) pale yellow essential oil. The major components were: 1,8-cineole (45.8%), ß-pinene (8.9%), 4aα,7α,7aα - nepetalactone (6.2%), α-terpineol (4.3%) and trans-ß-ocimene (3.3%).

Introduciton. Trigonella foenum-graecum L., is a native plant grows in Iran. The seeds of this plant contains the saponin diosgenin among other steroidal compounds. Diosgenin is trasferable to progesterone by chemical means.Methods. The total steroids of the dried seeds of the plant were extracted by ethanol 96%.Column chromatography followed by crytallization were applicable to obtain pure diosgenin. Diosgenin was transformed to the intermediate substance Δ16 pregnenolone acetate. Chemical and instrumental methods were used to identify and confirm the structure of diosgenin and pregnenolone acetate.Results and Discussion. The seeds were obtained from the market and pure diosgenin was extracted to the extental 0.1%. The primarily reported method for disclosure of diosgenin ring F by acetic anhydride at 200 °C and under pressure is avoidable by using Lewis acids as catalyst. Oxidation by CrO3 followed by refluxing with acetic anhydride will afford the intermediate substance Δ16prenenolone acetate Δ16. IR. NMR and Mass spectra whfirmed the structure ub Δ16pregnenaJoneacetate.11.

Introdution. Nepeta persica Boiss (Lamiaceae family) is one of the native medicinal plants of Iran that grows extensively in different parts of the country. Volatile oils are the most important constituents of the plant.Methods. The low content of volatile oils in this plant has served as an incentive for the development of cell cultures of N. persica capable cultivation and synthesis of secondary metabolites. In the present work, N. persica seeds were surface-sterilised with ethanol, hydrogen peroxide and chloramin-T and callus cultures were obtained from them. Calli were grown in Murashige and Skoog basal medium supplemented with some nutrients and growth regulators. After harvesting and drying of calli, preliminary phytochemical tests and GC and GC-MS analyses of callus extracts were carried out and compared with the results of similar experiments on the volatile oil of intact plant.Results and Discussion. The analyses showed the presence of tannins and flavonoids and absence of volatile oils in calli. Moreover some monoterpenoid compounds could be detected in intact plant volatile oil. Nepetalactone is the main component of this oil.

Introduction. Echinophora platyloba is one of the unique plant in Iran which is traditionally used for flavoring of cheese and yogurt. So far there is no report on its pharmacological action. In this study, we have investigated the anti-spasmodic effect of hydro-alcoholic extract and essential oil of E. Platyloba on contraction of isolated ileum.Methods. For this purpose male wistar rats were killed with ablow on the head and aportion of ileum was removed and placed in oxygenated Tyrode's solution. Isotonic contraction induced by spasmogens (KCI and acetylcholine) were recorded on a physiograph chart recorder paper. Effect of series concentrations of essential oil were studied on tonic contraction induced by 80mM KCI in order to determine the range of concentrations of hydroalcoholic extract and essential oil which may have an inhibitory effect on ileum. Then two or three concentrations were selected and their effects were studied on acetylcholine concentration-response curve. Effect of hydro-alcoholic extract and essential oil were compared with control tissues treated with an equivalent volume of vehicle. In addition, effect of remaining solution after extraction of essential oil alone and with essential oil for comparison, were also studied.Results. Essential oil of E. platylobal in nl/ml bath concentration concentration-dependently inhibited ileum contraction (IC50= 75 ± 10.4 nl/ml) and attenuated the maximum response of acetylcholine concentration-response curve. The hydro-alcholic extract also concentration-dependently inhibited ileum contraction (IC50= 250 ± 12.1µg/ml). Effect of hydro-alcoholic extract on acetylcholine response qualitatively were similar to that of essential oil. The remaining solution following extraction of essential oil as when essential oil only has slight inhibitory effect and its combiation with the essential oil had a similar inhibitory effect as when essential oil were used alone.Discussion. Essential oil and hydro-alcoholic extract of E.platyloba relaxant effect on ileum contraction due to KCl and acetylcholine shows that they have anti-spasmodic activity on ileum smooth muscle. Since anti-spasmodic drugs are used for irritable bowl syndrome, the essential oil and hydro-alcoholic extract of E. platyloba can potentially be useful for control of abdominal cramps. However, as their anti-spasmodic effect appears in a special concentrations range and in high concentuations, they can completely inhibit intestinal contraction, determination of standard dosage for anti-spasmodic effect is necessary.

Introduction. Antipsychotic drugs are known to produce analgesic effects, but the mechanisms are not well established. In addition, some calmodulin inhibitors are reported to produce antinociceptive effects. Among antipsychotic drugs, trifluoperazine is one of the most potent calmodulin inhibitors. We examined which of the known properties of this drug, including anti-dopaminergic, anti-cholinergic, anti-adrenergic, anti-histaminic, and calmodulin inhibition are involved in its anlgesic effect.Methods. The effects of varios agents on formalin test were evaluated 15 minutes after drug administration. All tested agents were injected through an intrathecal catheter. Since antinociceptive measures with formalin test are based on motor function, we also used rotarod test to quantify motor side effects of the drugs. Results and Discussion. Intrathecal trifluoperazine showed antinociceptive effects in a biphasic fashion i.e., analgesia at relatively low doses (1, 10 µg/rat) and hyperalgesia at the higher dose (100 µg/rat). No analgesic effects were observed after intrathecal injection of sulpiride, atropine, phentolamine and brompheniramine. Meanwhile, intrathecal calmidazolium induced a dose dependent analgesia (10, 50, 250 µg/rat). Low doses of histamine (1 µg/rat), physostigmine (1 µg/rat), bromocriptine (1 µg/rat) and norepinephrine (1 µg/rat) did not affect trifluoperazine-induced analgesia. Calcium attenuated antinociceptive effect of trifluoperazine and inhibited analgesic effect of calmidazolium. Finally, naloxone decreased trifluoperazine-induced antinociception but did not have any effect on calmidazolium-induced analgesia. We concluded that calmodulin inhibition may be involved in the analgesia produced by trifluoperazine. With increasing doses of trifluoperazine, algesic effect seems to overcome the analgesic effect. It is also suggested that the opioidergic system does not connect with "calmodulin inhibition"-induced analgesia even though this system has partial role in trifluoperazine-induced analgesia.

Introdution. Amoxicillin alone is used for a wide range of clinical indications. It is also available commercially as Augmentinø, an oral antibacterial combination containing ß-Lactamase inhibitor potassium clavulanate, the potassium salt of clavulanic acid. This combination is recently formulated and available commercially as Co-amoxyclav in Iran. The relative bioavailability of orally administered Co-amoxyclav and Augmentinø were compared following a single 625 mg dose (amoxicillin 500 mg as amoxicillin trihydrate, and clavulanic acid 125 mg as potassium clavulanates).Bioavailability parameters -including area under the serum concentration time curve (AUC) as a measure of the extent of drug absorption, and the highest concentration (Cmax )and the time to reach to a highest concentration (tmax)as a measure of the rate of absorption, were calculated from circulating drug levels and compared between the two products for each subject.Methods. twelve healthy adult male supjects were enrolled under fasted conditions using a two way cross over study. Samples of venous blood (10 ml) were obtained pre dose and at 0.33,0.66, 1, 1.5, 2, 3, 4, 5 and 7h post dose. Serum concentration of both amoxicillin and clavulanate were measured by a reverse phase high performance liquid chromatography previously reported. Amoxycillin was determined by monitoring at 227 nm, and the limits of detection in human serum were 0.5 mg/ml. Calibration curves were linear through 0.05-10 mg/ml for both amoxicillin and clavulanic acid (correlation coefficients> 0.99).For both active drugs, inter and intra day coefficients of variation were less than 10% at both low and high concentrations.Results and Discussion. Amoxicillin and clavulanic acid have mean half lives of 1.11 (0.2) and 0.8 (0.2) hours, respectively. Results from this study show that 90% confidence intervals were 1.05-1.12 and 1.14-1.16 for AUC0-t 1.06-1.15 and 1.02-1.16 for AUC0-¥ 0.97-1.03 and 0.99-1.19 for Cmax and 0.89-1.19 and 0.8D-1.07 for tmax for amoxicillin and clavulanic acid respectively. These results clearly demonstrating bioequivalence of the two products.

Introduction. Sodium alginate is a natural hydrogel polymer that is used to modulate drug release as adelivery system. The objective of this study was to investigate the effect of processing and structural variables of calcium alginate gel beads, on the swelling characteristics, loading efficiency, and drug release behaviour of this polymer.Methods. The studied variables consisted of polymer and cross-linking agent (CaCI2) concentrations, type of gelling cations, solubility and percentage of loaded drug, curring time of the polymer, pH and particle size of the alginate beads. The beads were then coated with Eudragit S-100 and drug release profiles were chracterized.Results and Discussion. Increasing the sodium alginate and CaCI2 concentration, prolonged the release time of caffeine (the model drug). Release kinetic of low-water-soluble drugs (i.e., theobromine) followed a zero-order kinetic while release of highly-water-soluble drugs was better fitted with a first order kinetic. Among the different cations which caused gelation. Ca2+ showed a better swelling profile. The effect of drug water solubility on the loading efficiency of beads, showed the order of caffeine <theophylline < theobromine. Increasing the curring time of the gels changeg the release kinetic of caffeine from first-order to Higuchi model. Drug loading method in the beads had no effect on the loading efficiency, while it was effective on the release profile of caffeine. Increasing the caffeine concentration in the beads, prolonged the release time of the drug. DSC studies confirmed an ionic interaction between calcium alginate and caffeine in high concentrations which slowed the drug release.

Introduction. Pectin is a purified carbohydrate product obtained mainly from the dilute acid extract of the inner part of the rind of citrus fruits or from apple drosses. It is a natural hydrophilic colloid consisting chiefly of partially methoxylated polygalacturonic acids.Considering the importance of usage of pectin in the food industries and also high availability of citrus rind and drosses of other fruits in our country, it was decided to extract pectin from citrus rind and drosses of apple and carrot and determine its percentage. Methods. To convert the insoluble protopectin of fruits to soluble form, the rinds and drosses of fruits were heated, using dilute sulfuric or hydrochloric acid. The obtained soluble pectin was then precipitated by either ethanol or isopropanol. The amount and percentage of pectin powders of different fruits were measured.Results and Discussion. According to the obtained results, the yield of extracted pectin from citrus rinds was more than other soures. Among citrus species, pectin extracted from those fruits that have thick inner layer in their rinds (e.g. grape fruit) showed to have high percent of pectin. It was, therefore, recommended to obtain high amounts of pectin from grape fruit rinds, The results of this study also showed that grape fruit albedo as well as its rinds contain 14.08-14.54 and 11.94-12.72 percent pectin respectively, as calculated on the basis of dry weight. These yields were the highest quantities among the yields of other citrus rinds and drosses of apple and carrot fruits.