DARU, Journal of Pharmaceutical Sciences
Volume:14 Issue: 3, Autumn 2006

Abstract: Citrullus colocynthis (L.) Schrad. (Cucurbitaceae) is an Iranian medicinal plant that has traditionally been used as an abortifacient and to treat constipation, oedema, bacterial infections, cancer and diabetes. As part of our on-going studies on Iranian medicinal plants, thorough phytochemical investigation was carried out on this plant. The reversed-phase preparative HPLC was employed to isolate compounds from the butanol fraction of the hydro-methanolic (70%) extract of the fruits of the locally grown C. colocynthis. Structures of the isolated compounds [1-5] were elucidated by spectroscopic means. The antioxidant property of the flavonoids 1-3 was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Three flavone glucosides, isosaponarin [1], isovitexin [2] and isoorientin 3’-O-methyl ether [3] and two cucurbitacin glucosides, 2-O-β-D-glucopyranosylcucurbitacin I [4) and 2-O-β-D-glucopyranosylcucurbitacin L [5] were isolated and identified. Flavonoids 1-3 showed significant antioxidant properties. Since reactive oxygen species are important contributors to tissue injury, inflammation, cancer and many other ailments, the antioxidant properties of 1-3 probably contribute, at least to some extent, to the pharmacological and traditional medicinal uses of the C. colosynthis

Abstract: Ethyl acetate and n- butanol fractions obtained from the column chromatography of methanolic extract of aerial parts of P. olivieri gave chrysoeriol-7-O-β-D-glucoside (I) and verbascoside (II), respectively. In addition, two flavonoid glycosides as compound (I) and chrysoeriol-7-β-D- (3''-E-p-coumaroyl) glucoside (III) and one iridoid glycoside, namely, lamiide (IV) were isolated from the ethyl acetate, ether and n- butanol fractions of a methanolic extract of aerial parts of Phlomis persica, respectively. Isolation and structural elucidation of compounds were accomplished by PTLC, CC, HPLC and spectroscopic methods (UV, FTIR, EIMS, 1H-NMR, 13C-NMR, DEPT, 1H- 1H COSY, HMQC and HMBC).

Abstract: Toxic pyrrolizidine alkaloids are present in some species of Echium (Boraginaceae). In this study petals of Echium amoenum Fisch. & Mey. (Gol-e-Gavzaban) as a popular herbal medicine in Iran, were investigated for pyrrolizidine alkaloids (PAs). The alkaloids were separated and purified by preparative TLC and characterized by IR, one and two dimensional 1H and 13C-NMR and Mass spectroscopy. Four toxic alkaloids namely: echimidine I, echimidine isomer II, 7-angeloyl retronecine III and 7-tigloyl retronecine IV were identified.

Abstract: The chemical compositions of the essential oils of Ocimum basilicum L. cv. purple and Ocimum basilicum L. cv. green cultivated in Iran were investigated by GC-MS. Twenty constituents (98.5% of the total oil) were identified in the volatile oil of O. basilicum L. cv. Purple. The main constituents found in the oil were methyl chavicol (52.4%), linalool (20.1%), epi--cadinol (5.9%) and trans--bergamotene (5.2%). In the volatile oil of O. basilicum L. cv. green, twelve components were characterized representing 99.4% of the total oil. Methyl chavicol (40.5%), geranial (27.6%), neral (18.5%) and caryophyllene oxide (5.4%) were the major components. Methyl chavicol is the dominant constituent in each of the two oils. Although the oil of green basil was characterized by a highccontent (46.1%) of citral (neral and geranial), citral was not detected in the oil of purple basil oil.

Abstract: Effects of Anethum graveolens L. (dill) extracts on female reproductive system were studied in fifty four wistar female rats with regular estrous cycle in 6 groups. The experimental groups were fed 0.045 g/kg and 0.45 g/kg of aqueous extract and 0.5 g/kg and 5 g/kg of ethanol extract for 10 days. The sham group was fed with solvent and controls received no treatment. The estrus cycle changes were determined by daily vaginal smear changes. At the beginning and at the end of experiment blood samples were withdrawn to determine the blood estradiole and progesterone concentration. The ovaries were removed and granulosa lutein cells were studied under transmission electron microscopy. Treatment with high dose of the extract resulted in a significant increase in duration of the estrous cycle and diestrus phase and the progesterone concentration. Smooth endoplasmic reticulum (SER), rough endoplasmic reticulum (RER) and mitochondria were increased in granulosa lutein cells in high dose groups. While more studies are required to clarify the properties of this herb, results of this investigation show that dill can be used as an either regulatory agent of menstrual cycle of women with irregular cycle or as an antifertility agent.

Abstract: This study was designed to find possible relationship between QTc prolongation and erythrocyte or plasma lithium concentrations. Fifty-six patients with bipolar disorder entered this case- control study. Subjects were between 17 to 63 years of age and were receiving lithium alone, or lithium plus haloperidol or lithium plus thioridazine. The exclusion criteria were past history of cardiovascular, hepatic, renal or metabolic disorders or using other medications known to cause rhythm disturbances. The case group included males with QTc 450ms and females with QTc470ms while the control group included males and females with QTc<450 and QTc< 470ms, respectively. Serum sodium and potassium levels, erythrocyte and plasma lithium concentrations as well as lithium ratio were determined for all subjects and compared between the case and control groups by independent sample t-test. The mean of these levels were not different between the case and control groups. Additionally, no correlations were found between QTc and erythrocyte or plasma lithium concentration, lithium ratio, serum sodium or potassium levels. Analyzing the data for patients treated with lithium alone showed no significant correlations between QTc prolongation and erythrocyte or plasma lithium concentration, lithium ratio or serum potassium level. However, a significant correlation was found between serum sodium concentration and QTc prolongation. It should be noted that QTc prolongation occurred six times more in patients who were taking thioridazine and lithium concomitantly. This study noted no influence of sex or co-administration of haloperidol with lithium on QTc prolongation. It is concluded that plasma or erythrocyte lithium levels may not be able to predict QTc prolongation and its consequences.

Abstract: This report describes the frequency of Enteroccoci phenotypic and genotypic susceptibility patterns of VRE (Vancomycin Resistant Enterococci) from three hospitals in Tehran, Iran. One hundred and twenty enterococcal urine cultures were isolate from patients with urinary tract infection (UTI). After identification of enterococcal species by biochemical tests, glycopeptide susceptibility of each isolate was assessed by disk agar diffusion method according to NCCLS guideline. Glycopeptide minimum inhibitory concentration (MIC) for each VRE isolate was determined by the agar dilution method and the vanA gene was detected by PCR. Seven percent (8/120) of the isolates were VRE, including E. faecalis 38% (3/8), E. faecium 25% (2/8), E. mundtii 25% (2/8), and E. raffinosus 12% (1/8). All 8 isolates resistant to vancomycin showed vancomycin MIC of >512µg/ml, and teicoplanin MIC’s ranging from 8->64µg/ml, and they all possessed the vanA gene. Six (75%) of VRE were isolated from a referral tertiary care hospital, i.e. Ahari Children Medical Center (ACMC). Almost 90% of Enterococci were E. faecalis (57%) and E. faecium (30%). The remaining 13% were identified as E. mundtii (6%), E. avium (3%), E. durans (1%), E. hirea (2%), and E. raffinosus (1%). The diverse VRE species combined with high rate of VRE isolation in Iran, as well as isolation of E. raffinosus and E. mundtii in the Middle East (ME) region for the first time, suggests a rapid spread of resistance among Enterococci along with an emerging shift in VRE distribution in Iran.

Abstract: Carotenoids are widely used in nutraceutical, additives and cosmetics as colorants and antioxidants. Dunaliella is the main natural source which accumulates massive amount of carotenoids. This study examines the effect of different concentrations of NaCl (0.3M to 2M) and light intensities of 50 and 150 μmol/m²s on total carotenoids accumulated by Dunaliella tertiolecta (DCCBC26), from Urmia lake (North West of Iran) compared to those obtained from Dunaliella salina CCAP 19/18 and also the wild type Dunaliella salina WT strains. In all microalgaes production of carotenoids were triggered by increase in light intensities. Changes of intensity from 50 μmol/m²s to 150 μmol/m²s led to 2.4, 2.1 and 1.4 folds of carotenoids production by D. salina CCAP, D. salina WT and D. tertiolecta respectively. In both salina strains carotenoids production improved with higher salinity picking at salt concentration of 2M, while D. tertiolecta showed optimum carotenoids production at 0.7M.

Abstract: In this study the reactivity of methandrostenolone or [(17b)-17-hydroxy-17-methylandrosta-1, 4-diene-3-one], as a dienophil in a Diels-Alder type cycloaddition reaction was investigated. The purpose of this approach was to investigate whether the 1-dehydro position of methandrostenolone 1 undergoes a cycloaddition reaction with dienes, such as 1, 3 butadiene or cyclopentadiene, and to investigate the biological behavior of the reaction adducts, i.e, compound 3 {(17b)-17-hydroxy-17-methyl androsta [1a, 2a] cyclohex 3’, 4-diene-3-one} and compound 4 {(17b)-17-hydroxy-17-methyl androsta [1a, 2a] cyclohex (2’,5’ methylene) 3’, 4-diene-3-one}, relative to compound 1. The results indicated that thedDiels-Alder reactionddid notpproceed under the usual circumstances of high pressure and temperature, but could proceed in the presence of a Lewis acid (AlCl3). The structures of compounds 3 and 4 were confirmed by spectroscopic methods. The androgenic behavior of compounds 3 and 4 in comparison to compound 1 in the apomorphine test indicated that both compounds were almost devoid of androgenic activity, but prevented apomorphine mediated penile erection in male rats in a similar manner as cyproterone acetate.

Abstract: Dry powder inhaler (DPI) formulations usually contain micronized drug particles and lactose as a carrier. Fine lactose could be used as a ternary component to improve drug delivery from DPIs. The aim of this study was to investigate the deposition profile of a model drug, cefotaxime sodium (CS), using coarse and fine carriers after aerosolization at 60 l/min via a spinhaler® into a twin stage liquid impinger (TSI). Two micronization methods. jet milling and spray drying were used to micronize the active drug and carrier. The particle size of CS and lactose were characterized by laser diffraction, and the morphology of formulations was examined by scanning electron microscopy. X-ray diffraction of jet milled lactose showed crystalline nature, but spray dried lactose exhibited an amorphous state. The results showed the existence of fine lactose in formulations significantly (p<0.05) influenced the deposition profiles of aerosolized jet milled CS. However, no significant (p>0.05) difference was observed between the effect of jet milled and spray dried lactose. On the other hand selection of micronization technique to reduce particle size of CS, was very effective on deposition profile. The highest influence of fine lactose was obtained by formulation containing jet milled CS in ratio of drug/carrier 1/1 and 10% of fine lactose as third component.