Open Access Original Research Article

Synthesis and Ca2+-desensitizing Activity of 2-methyl-7-aryl(α-furyl)-[1,3]thiazolo[4,5-d]pyridazin-4(5H)-ones

Anatoly Soloviev, Sergey Demchenko, Ludmyla Bobkova, Valentyn Panchenko, Sergey Zelenskyi, Anatoly Demchenko

Journal of Pharmaceutical Research International, Page 1-11
DOI: 10.9734/JPRI/2018/37338

Aims: Search of new chemical compounds for pressure decrease in accordance with new mode of action.

Study Design: Novel 2-methyl-7-aryl(α-furyl)-[1,3]thiazolo[4,5-d]pyridazin-4(5H)-ones were synthesized in 67-84% yields via reaction of 2-methyl-5-benzoyl(furoyl)-thiazol-4-carboxylates with hydrazines.

Place and Duration of Study: Synthesis of new compounds has been performed at National T. Shevchenko University “Chernihiv Collegium” and Institute of Pharmacology and Toxicology, National Academy of Medical Sciences. Physiological studies have been conducted at Institute of Pharmacology and Toxicology, National Academy of Medical Sciences of Ukraine.

Methodology: Design of chemical structures which relax vascular smooth muscle cells without significant decreasing in intracellular calcium concentration, [Ca2+]i.

Results: These new compounds have been successfully tested for the aim to search so-called calcium desensitizers, i.e. compounds which possess the ability to decrease Ca2+-sensitivity of myofilaments and therefore, vascular smooth muscle cells (VSMc) contractility and, hence, vascular tone.

Conclusion: 2-Methyl-7-aryl(α-furyl)-[1,3]thiazolo[4,5-d]pyridazin-4(5H)-ones may be used in future as safety and good therapeutic approach under arterial hypertension and local vasospasm development.

Open Access Original Research Article

Self-Medication with Analgesics: Knowledge and Attitudes of Senior Medical Students and Interns at King Abdulaziz University, Jeddah, Saudi Arabia

Nahla Khamis Ibrahim, Banan Mohamed Alamoudi

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/JPRI/2018/39245

Aim: The study was conducted to assess the knowledge and attitudes of clinical years’ medical students and interns towards self-medications with analgesics, King Abdulaziz University (KAU), Jeddah, Saudi Arabia.

Methodology: A cross-sectional study design was conducted among senior medical students (4th- 6th year) and interns at the medical college of KAU. A multistage stratified random sampling technique was used. A confidential, validated, self-administered questionnaire was used. It inquired about personal and socio-demographic information. It contained 10 questions asked about their knowledge concerning self-medication with analgesics. The knowledge score was calculated, ranged from 0-10. It was categorized into: satisfactory score (≥7), fair score (5 - <7) and poor score (< 5). Their attitudes towards analgesic self-medication were determined through rating 10 attitudes’ statements on a 3-points Likert scale. Descriptive and inferential statists were done.

Results: Only 48% of the participants obtained a satisfactory knowledge score about self-medication with analgesics. Males had a significantly lower level of knowledge compared to females (X2=11.41, P <0.001). After controlling confounding factors in logistic regression, the first predictor of having a satisfactory knowledge score about self-medication with analgesics was being in a higher educational grade (aOR; 2.35, 95% CI: 1.54 - 3.58), followed by female gender. Regarding attitude, 70.8% of respondents agreed that self-medication with analgesics can cause side effects.

Conclusion: Some lack of knowledge about self-medication with analgesics was found among our participants. However, the participants had sound attitudes towards some its issues. Knowledge of medical students and interns about self-medications needs improvement through more educational and training programs.

Open Access Original Research Article

Investigation of Phenolic Content, Antioxidant Capacities, Anthelmintic and Cytotoxic Activities of Thymus zygioides Griseb.

Arzu Kaska, Mehmet Çiçek, Nahide Deniz, Ramazan Mammadov

Journal of Pharmaceutical Research International, Page 1-13
DOI: 10.9734/JPRI/2018/39688

Aims: This study was designed to evaluate the total phenolic, flavonoid content and antioxidant properties of various extracts (ethanol, methanol, acetone, water) of Thymus zygioides and the ethanol extract was also investigated for phenolic components, anthelmintic and cytotoxic activities.

Materials and Methods: The antioxidant capacities of the extracts were examined for radical scavenging activities (DPPH, ABTS), antioxidant activities (β-carotene/linoleic acid test system, phosphomolybdenum method), power reducing and metal chelating activities. The phenolic content of the ethanol extract was determined using HPLC. The brine shrimp lethality test was used to screen for possible cytotoxic activity. Anthelmintic activity was evaluated using the aquarium worm, Tubifex tubifex.

Results: Among the four different extracts of T. zygioides evaluated, the methanol extract showed the highest amount of free radical scavenging (DPPH, 20.82µg/mL and ABTS, 11.44µg/mL) and antioxidant activities (phosphomolybdenum, 45.63µg/mg). In the metal chelating activity, acetone extract was statistically different from the other extracts (54.26%, P<0.05). The water extract exhibited the highest antioxidant capacity (β-carotene/linoleic acid test system, 82.20%) and the ethanol extract showed the highest amount of ferric reducing power activity (0.141 mg/mL). The HPLC analysis of the ethanolic extract showed the presence of some phenolics, such as caffeic acid, quercetin, and epicatechin. In addition, the ethanol extract exhibited cytotoxic activity with LC50, 436.25 µg/mL. Dose-dependent activity was observed in the anthelmintic properties of the ethanol extract and all doses of the ethanol extract showed better anthelmintic activity than the standard.

Conclusion: The results will help us to understand the importance and usage of this medicinal species in the food industry, traditional medicine, and pharmaceutical applications.

Open Access Review Article

Role of Toxins of Uropathogenic Escherichia coli in Development of Urinary Tract Infection

Saber Soltani, Amir Darb Emamie, Mahsa Dastranj, Abbas Farahani, Abolfazl Davoodabadi, Parviz Mohajeri

Journal of Pharmaceutical Research International, Page 1-11
DOI: 10.9734/JPRI/2018/39188

Three clinical syndromes including diarrhea/enteritis, urinary tract infection and septicemia/meningitis can be found as a result of infection with each of the E. coli pathotypes. Uropathogenic Escherichia coli toxins are one of the most important factors in the spread of these infections, including urinary tract infections, which we will review in this study.
The first CDT toxin (Cyclomodulins) was reported in E. coli strains in 1987; CDT toxins show a new function and act on DNA. This unique CDTs has unlocked novel questions in the field of Toxicology. The E. coli strains involved in UTIs often produce exotoxins such as hemolysin, cytotoxic factor type 1 (CNF1), and colonization factors. Enteroaggregative E. coli (EAEC) toxins include heat-resistant enterotoxigenic toxin (EAST1) plasmid, a potent agent for diarrhea, encoded by a plasmid (Pet), which has cytotoxic activity against cultured intestinal cells and red blood cells,toxin Pic and ShET1 Toxins that have intestinal toxicity. EHEC toxins include Shiga Toxin (Stx) and Verotoxin (VT) and Enterohemolysin. Also, EAST1 was reported for the first time in EAEC strains, and this toxin is also present in EHEC strains. ETEC enterotoxins belong to one of the two heat-sensitive enterotoxins (LTs) and heat-resistant enterotoxins (STs). EPEC toxins include EspC enterotoxin. VAT toxin is a known cytotoxin that expresses through UPEC over a systemic infection. CysK also contributes to the expression of UPEC toxins and the cause of toxicity and cellular inhibition caused by UPEC infections.

Open Access Review Article

Effects of Medicinal Plants on Urinary Incontinence: A Systematic Review

Mahnaz Yavangi, Saeid Heidari-Soureshjani

Journal of Pharmaceutical Research International, Page 1-7
DOI: 10.9734/JPRI/2018/39691

Urinary incontinence is one of the disorders that may develop for various reasons, affect different aspects of life, and declining quality of life.

Relevant key terms were used to retrieve the articles published between 2000 and 2018 and indexed in the Institute for Scientific Information and PubMed. Then, the articles about the medicinal plants and the plant-based products whose effects were investigated on urinary incontinence (UI) were selected and analyzed by two members of the research team.

Different plants such as Cannabis sativa, St. John's wort, Ephedra sinica, Salvia sclarea, Ramulus Cinnamomi, and Alpinia oxyphylla exert anti-UI effects through various mechanisms. The phytoestrogen derivatives of the plants mainly in menopausal women, isoflavonoid compounds, Gosha-jinki-gan, and Weng-li-tong, exert anti-UI effects. It should be considered that plants and their derivatives can be used as dietary supplements, independently, and mainly with chemical drugs.

Plants and plant-based combinations can induce anti-UI effects through phytosterogenic properties in women, decreasing stress and affecting the neuromuscular system as well as decreasing the activities of the detrusor muscle and regulating the activity of the urethral sphincters.