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Journal: Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences

167

Background and the purpose of the study: Rizatriptan is used effectively for the treatment of migraine headache. In this study, a simple, rapid and low cost spectrophotometric method based on the ion-pair complexation is proposed for the determination of rizatriptan in raw material and dosage forms. METHODS: The ion-pair complexation using bromocresol green as reagent was performed in a buffer solution and the absorbance was measured by a spectrophotometer. The ion-pair formation conditions were optimized and the accuracy and precision of the method were calculated.Results and major conclusion: Best results were achieved by using 6 ml of the bromocresol green reagent in the presence of phosphate buffer (pH 3.0). The stoichiometry of the resulted complex was 1:1. The within-day and between-day precision values were lower than 2.9 and 1.8 percent for the calibration range of 0.5–50 and 10–100 mug/ml, respectively. The proposed method was successfully used for the determination of rizatriptan in dosage forms without any interference.

Concepts: Spectroscopy, Chemical equilibrium, PH, Phosphate buffered saline, Accuracy and precision, Buffer solution, Equilibrium chemistry, Spectrophotometry

167

BACKGROUND: A specific and sensitive UPLC-qTOF-MS/MS method has been developed for the simultaneous determination of curcuminoids. These Curcuminoids comprises of curcumin, a principal curcuminoid and other two namely, demethoxycurcumin, and bisdemethoxycurcumin obtained from rhizomes of Curcuma longa an ancient Indian curry spice turmeric, family (Zingiberaceae), METHODS: These analytes were separated on a reverse phase C18 column by using a mobile phase of acetonitrile: 5% acetonitrile in water with 0.07% acetic acid (75:25 v/v), flow rate of 100 muL/min was maintained. The qTOF-MS was operated under multiple reaction monitoring (MRM) mode using electro-spray ionization (ESI) technique with positive ion polarity. The major product ions in the positive mode for curcuminoids were at m/z 369.1066, 339.1023 and 309.0214 respectively. The recovery of the analytes from mouse plasma was optimized using solid phase extraction technique. RESULTS: The total run time was 5 min and the peaks of the compounds, bisdemethoxycurcumin, demethoxycurcumin and curcumin occurred at 2.06, 2.23 and 2.40 min respectively. The calibration curves of bisdemethoxycurcumin, demethoxycurcumin and curcumin were linear over the concentration range of 2–1000 ng/mL (r2, 0.9951), 2–1000 ng/mL (r2, 0.9970) and 2-1000 ng/mL (r2, 0.9906) respectively.Intra-assay and inter-assay accuracy in terms of% bias for curcumin was in between -7.95to +6.21, and -7.03 to + 6.34; for demethoxycurcumin was -6.72 to +6.34, and -7.86 to +6.74 and for bisdesmetoxycurcumin was -8.23 to +6.37 and -8.47 to +7.81. The lower limit of quantitation for curcumin, demethoxycurcumin and bisdemethoxycurcumin was 2.0 ng/mL. Analytes were stable under various conditions (in autosampler, during freeze-thaw, at room temperature, and under deep-freeze conditions). This validated method was used during pharmacokinetic studies of curcumin in the mouse plasma. CONCLUSIONS: A specific, accurate and precise UPLC-qTOF-MS/MS method for the determination of curcumin, demethoxycurcumin and bisdemethoxycurcumin both individually and simultaneously was optimized.

Concepts: Analytical chemistry, Ion, Mouse, Curcuma, Turmeric, Curcumin, Zingiberaceae, Curry

166

BACKGROUND: Several studies have been focused on design and synthesis of multi-target anti Alzheimer compounds. Utilizing of the dual Acetylcholinesterase/Butyrylcholinesterase inhibitors has gained more interest to treat the Alzheimer’s disease. As a part of a research program to find a novel drug for treating Alzheimer disease, we have previously reported 6-alkoxybenzofuranone derivatives as potent acetylcholinesterase inhibitors. In continuation of our work, we would like to report the synthesis of 5,6-dimethoxy benzofuranone derivatives bearing a benzyl pyridinium moiety as dual Acetylcholinesterase/Butyrylcholinesterase inhibitors. METHODS: The synthesis of target compounds was carried out using a conventional method. Bayer-Villiger oxidation of 3,4-dimethoxybenzaldehyde furnished 3,4-dimethoxyphenol. The reaction of 3,4-dimethoxyphenol with chloroacetonitrile followed by treatment with HCl solution and then ring closure yielded the 5,6-dimethoxy benzofuranone. Condensation of the later compound with pyridine-4-carboxaldehyde and subsequent reaction with different benzyl halides afforded target compounds. The biological activity was measured using standard Ellman’s method. Docking studies were performed to get better insight into interaction of compounds with receptor. RESULTS: The in vitro anti acetylcholinesterase/butyrylcholinesterase activity of compounds revealed that, all of the target compounds have good inhibitory activity against both Acetylcholinesterase/Butyrylcholinesterase enzymes in which compound 5b (IC50 = 52 +/- 6.38nM) was the most active compound against acetylcholinesterase. The same binding mode and interactions were observed for the reference drug donepezil and compound 5b in docking study. CONCLUSIONS: In this study, we presented a new series of benzofuranone-based derivatives having pyridinium moiety as potent dual acting Acetylcholinesterase/Butyrylcholinesterase inhibitors.

Concepts: Alzheimer's disease, Parkinson's disease, Acetylcholine, Acetylcholinesterase inhibitor, Memantine, Donepezil, Mild cognitive impairment

161

Traditional drug discovery approaches are mainly relied on the observed phenotypic changes following administration of a plant extract, drug candidate or natural product. Recently, target-based approaches are becoming more popular. The present study aimed to identify the cellular targets of crocin, the bioactive dietary carotenoid present in saffron, using an affinity-based method.

Concepts: Drug discovery, Medicinal chemistry, Natural product, Crocin, Crocetin

147

In recent times, the use of health technologies in the diagnosis and treatment of diseases experienced considerable and accelerated growth. The goal of the present study was to describe the designated pilot MCDM (Multiple Criteria Decision Making) model for priority setting of health technology assessment in Iran.

Concepts: Time, Decision theory, Decision making software, Philosophy of science, Technology, Neolithic, Technology assessment, Multi-criteria decision analysis

28

Tribulus terrestris as a herbal remedy has shown beneficial aphrodisiac effects in a number of animal and human experiments. This study was designed as a randomized double-blind placebo-controlled trial to assess the safety and efficacy of Tribulus terrestris in women with hypoactive sexual desire disorder during their fertile years. Sixty seven women with hypoactive sexual desire disorder were randomly assigned to Tribulus terrestris extract (7.5 mg/day) or placebo for 4 weeks. Desire, arousal, lubrication, orgasm, satisfaction, and pain were measured at baseline and after 4 weeks after the end of the treatment by using the Female Sexual Function Index (FSFI). Two groups were compared by repeated measurement ANOVA test.

Concepts: Sexual intercourse, Test method, Sexual arousal, Sexual dysfunction, Hypoactive sexual desire disorder, Aphrodisiac, Libido, Tribulus terrestris

9

The present study was designed to investigate the efficacy of a new formulation of alone, purified cannabidiol (CBD) (>98 %), the main non-psychotropic cannabinoid of Cannabis sativa, as a topical treatment in an experimental model of autoimmune encephalomyelitis (EAE), the most commonly used model for multiple sclerosis (MS). Particularly, we evaluated whether administration of a topical 1 % CBD-cream, given at the time of symptomatic disease onset, could affect the EAE progression and if this treatment could also recover paralysis of hind limbs, qualifying topical-CBD for the symptomatic treatment of MS.

Concepts: Time, Multiple sclerosis, Cannabis, Cannabinoid, Cannabidiol, Medical cannabis, Cannabis sativa

8

Zolpidem is a popular drug indicated for the short-term treatment of insomnia. Side effects are not uncommon with zolpidem. Herein we describe an Iranian 27-year-old man with no known mood disorder or neuropsychological disease who attempted suicide upon taking zolpidem. There are two interesting facts about this case: Firstly, the patient had not history of suicide attempt or thinking. Secondly, this case had experienced suicide ideation after taking 20 mg of zolpidem, suggesting a possible correlation between zolpidem psychological effects and dangerous psychological behaviors.

Concepts: Psychology, Mental disorder, Bipolar disorder, Suicide, Parasuicide

2

Cardanol was previously reported to be an antiproliferative compound purified from Thai Apis mellifera propolis. By morphology, it could induce the cell death to many cancer cell lines but not the control (non-transformed human foreskin fibroblast cell line, Hs27). Here, it was aimed to evaluate the molecular effects of cardanol on breast cancer derived cell line (BT-474).

Concepts: Cancer, Breast cancer, Metastasis, Cell division, Apoptosis, Chemotherapy, Cell cycle, P53

2

Cordyceps militaris has been used as a traditional medicine in Asian countries for a long time. Different types of Cordyceps extract were reported to have various pharmacological activities including an anti-cancer effect. We investigated the inhibitory effect of Cordyceps militaris ethanol extract on a human colorectal cancer-derived cell line, RKO.

Concepts: Cell, Cancer, Chromosome, Cell biology