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  • Author: T. Zlatanova x
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In Vivo Evaluation of Anti-inflammatory Activity of 2-[3-Acetyl- 5-(4-chloro-phenyl)-2-methyl-pyrrol-1-yl]-4-methylsulfanylbutyric Acid

Abstract

Background: Persisting inflammatory stimuli cause chronic inflammation recognized as the major factor contributing to the development of a number of diseases. One group of drugs used in the treatment of chronic inflammation is the group of non-steroidal anti-inflammatory drugs and, more specifically, the selective COX-2 inhibitors (coxibs). However, most of the coxibs were withdrawn from the market in view of their safety profile. In the present study, 2-[3-Acetyl-5-(4-chlorophenyl)- 2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e), an Npyrrolylcarboxylic acid derivative structurally related to celecoxib, is evaluated for anti-inflammatory activity after single and multiple (14 days) administration using an animal inflammation model.

Aim: To evaluate the anti-inflammatory properties of 2-[3-Acetyl-5-(4-chlorophenyl)-2-methyl-pyrrol-1-yl]-4-methylsulfanyl-butyric acid (compound 3e) after single and multiple (14 days) administration using an animal inflammation model.

Materials and methods: Forty Wistar rats were allocated into 5 groups (n=8) treated with saline (controls), diclofenac (25 mg/kg b.w.), compound 3e (10, 20 and 40 mg/kg b.w.) intraperitoneally. The volume of the right hind paw of the animals of all groups is measured prior to treatment and two, three and four hours after administration of carrageenan using a plethysmometer (Ugo Basile, Italy). The percentage of paw edema is calculated using the Trinus formula.

Results: In a single administration, compound 3e in doses of 10 and 20 mg/kg b.w. did not inhibit paw edema, while a dose of 40 mg/kg b.w. significantly inhibited carrageenan-induced paw edema at 2 hours in comparison with the control group. After continuous administration, compound 3e in doses of 10, 20 and 40 mg/kg b.w. significantly reduced paw edema at 2, 3, and 4 hours compared to animals treated with saline.

Conclusions: Compound 3e shows anti-inflammatory properties similar to those of diclofenac after continuous administration.

Open access
The Role of Control in the Effective Hospital Management

Abstract

The objective of the present study was to investigate the opinion of the managers working in the health system concerning their attitude towards the operations of control within the system and the impact of these operations on the activity of the health-care institutions.

Materials and Methods: From October 2016 till January 2017 using an anonymous questionnaire we studied the opinion of 407 medical doctors, medical and healthcare specialists working in various types of healthcare institutions for hospital care in Sofia and the countryside. Results: Only 1/5 of the respondents shared the opinion that the adequate control resulted in quality improvement of the provided medical caregiving, one in four (25,8%) believed that the control could raise the responsibilities of the officials with managerial titles; one in three (34,2%) shared the opinion it improved the responsibilities of the executives.

Conclusion: The new operational terms and conditions implemented in the health insurance system do not result in improving the work quality in the hospital, which allows the conclusion that by changing only the healthcare funding the desired positive changes could not be attained. The organization, management and provision of medical care should be generally revised.

Open access
Experimental Study of the Analgesic Effect of the Antidepressant Escitalopram

Abstract

Background: Antidepressants have been found to possess antinociceptive and analgesic properties and are prescribed in the treatment of chronic pain.

Aim: To evaluate the antinociceptive properties of escitalopram after a single administration.

Materials and methods: Forty Wistar rats were used in the study. They were divided into 5 groups (n=8) treated with saline solution (control group), metamizole (150 mg/kg b.w.), escitalopram (5, 10 and 20 mg/kg b.w.) intraperitoneally. The nociceptive tests we used employed thermal (hot plate and plantar test), mechanical (analgesimeter) and chemical (formalin test) stimuli. Criteria for analgesic effect were increased latency in hot plate, plantar test, analgesimeter and decreased paw licking time in formalin test.

Results: The reference analgesic metamizole showed significant analgesic effect in all tests excluding the first phase with formalin. Escitalopram in doses of 5 and 20 mg/kg b.w. increased paw withdrawal latency in analgesimeter at 2 hours compared to control. Escitalopram in a dose of 5 mg/kg b.w. increased the duration of the stay on the hot plate at 1 hour, while doses of 10 and 20 mg/kg b.w. significantly increased this indicator at 1 and 3 hours in comparison to the saline treated group. In the plantar test, escitalopram in all used doses significantly increased the nociceptive response latency compared to control. A dose of 5 mg/kg b.w. decreased hind paw licking time during phase 1 of the formalin test, whereas doses of 10 and 20 mg/kg b.w. decreased phase 2 licking time compared to the control group.

Conclusion: The antidepressant escitalopram has analgesic properties but they are not dose- or time-dependent.

Open access
Antidepressant Effect and Recognition Memory Improvement of Two Novel Plant Extract Combinations - Antistress I and Anti-stress II on Rats Subjected to a Model of Mild Chronic Stress

Abstract

Background: Chronic stress is one of the main factors which lead to depression – a psychiatric disorder affecting millions of people and predicted to be the second ranked cause of premature death in 2020. Depression is often associated with cognitive disturbances and memory deficit. Plant based therapy could be effective in the treatment of mild to moderate depression due to its low level of adverse reaction, its good tolerability and compliance.

Materials and methods: 72 male Wistar rats, divided in 9 groups were given orally for 8 weeks two combinations of dry plant extracts – Antistress I and Antistress II and five individual dry extracts obtained from Serratula coronata, Hypericum perforatum, Valeriana officinalis, Crataegus monogyna and Melissa officinalis. The animals were exposed to a chronic unpredictable mild stress for 8 weeks. The depression-like symptoms were evaluated with Forced swim test while the assessment of the memory deficit was performed with Novel object recognition test.

Results: Antistress II demonstrates antidepressant effect while Antistress I doesn’t improve the depressive-like symptoms. The individual extracts of Hypericum perforatum and Valeriana officinalis also possess antidepressant properties. Antistress II improves the cognition as well as the individual extracts of Hypericum perforatum, Valeriana officinalis and especially Serratula coronata. Dry extract from Serratula tend to have the best effect regarding the recognition memory. The effect of Antistress I on memory deficit is negligible.

Conclusions: Antistress II possesses antidepressant effect and improves the recognition memory while Antistress I doesn’t demonstrate any of the above-described effects.

Open access