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AKR1D1*36 C>T (rs1872930) allelic variant is associated with variability of the CYP2C9 genotype predicted pharmacokinetics of ibuprofen enantiomers – a pilot study in healthy volunteers

Abstract

The relative contribution of CYP2C9 allelic variants to the pharmacokinetics (PK) of ibuprofen (IBP) enantiomers has been studied extensively, but the potential clinical benefit of pharmacogenetically guided IBP treatment is not evident yet. The role of AKR1D1*36C>T (rs 1872930) allelic variant in interindividual variability of CYP450 mediated drug metabolism was recently elucidated. A total of 27 healthy male subjects, volunteers in IBP single-dose two-way cross-over bioequivalence studies were genotyped for CYP2C9*2, CYP2C9*3 and AKR1D1*36 polymorphisms. The correlation between CYP2C9 and AKR1D1 genetic profile and the PK parameters for S-(+) and R-(−)-IBP was evaluated. Remarkable changes in the PK values pointing to reduced CYP2C9 enzyme activity were detected only in the CYP2C9*2 allelic variant carriers. Statistically significant association between the AKR1D1*36 allele and the increased IBP metabolism (low AUC 0-t and 0–∞, high Cl tot and short t max values for both enantiomers) was observed in subjects carrying the CYP2C9 *1/*3 or CYP2C9*1/*1 genotype. The clinical value of concomitant CYP2C9 and AKR1D1 genotyping has to be further verified.

Open access
Anticholinesterase and antioxidant activities of foliar extract from a tropical species: Psidium guajava L. (Myrtaceae) grown in Algeria

Abstract

Guava (Psidium guajava L.) is a fruit tree largely used in folk medicine in tropical and subtropical areas. This exotic species was introduced in a botanical garden in the northeast of Algeria in the 1950’s. The aim of this study is to estimate, for the first time, the antioxidant and anticholinesterase activities of chloroform, ethyl acetate and n-butanol extracts of P. guajava growing in Algeria. Six antioxidant assays were tested, results showed very important efficiency in free radical scavenging, reducing power and β-carotene bleaching of tested extracts. Values of IC50 or A0.5 of some samples were lower than those of standards. With regard to anticholinesterase activity, the inhibitory of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) was investigated. The extracts exhibited interesting capacity to inhibit these enzymes with low values of IC50 and even less than that of galanthamine. These activities were correlated with total phenolic content which was more important compared to the one found in extracts from trees growing in tropical and subtropical region. This could be due to resistance and adaptation of P. guajava grown in Algeria. The data obtained suggest the use of bioactive compounds from P. guajava leaves as antioxidant and drugs for symptomatic treatment of Alzheimer disease.

Open access
Biochemical aspects of KB-28 compound on physically loaded study subjects

Abstract

In previous studies of actoprotective activity of 5-R-thio-tetrazolo[1,5]quinazoline derivatives in normal and complicated experimental conditions, sodium 2-(tetrazolo [1,5-c]quinazoline-5-ylthio)acetate (KB-28) was found to be the leader of the experiment. The objective of the current study was to characterize the effects of KB-28 compounds on carbohydrate and lipid exchange indices under the conditions of physical load as a possible mechanism of actoprotective effect. In the course of the experiment, the indices of carbohydrate and lipid exchange in the muscle, blood and liver of animal models were determined following a 15-day physical load course. In doing so, glucose, glycogen and total lipid concentrations were assessed. The KB-28 compound was administered daily at levels determined during the course of regular physical load normalized metabolic processes in rats. The results were then compared to a control which received intraperitoneally the equivolume 0.9% sodium chloride solution. The phenomenon of actoprotection consisted in enhancing concentrations of glycogen in skeletal muscles and liver. Compared to the control figures, this increase was 28.8% and 25.0%, accordingly. Moreover, the course of KB-28 caused a statistically significant reduction (by 32.1%) of the total serum lipid concentration in the animals under physical load. The effect may be a sign of the ability of this substance to utilize active lipolysis for improvement of the skeletal muscle performance. Having analyzed the results obtained, we can draw a conclusion that influencing the biochemical processes in the study models is one of the mechanisms of the KB-28 actoprotective effect.

Open access
Clinical testing of antiretroviral drugs as future prevention against vaginal and rectal transmission of HIV infection – a review of currently available results

Abstract

The original purpose of vaginally applied microbicides was to slow down the HIV epidemic among the population until an effective vaccination was developed. Nowadays, antiretrovirals applied in the form of gels or vaginal rings are considered most prominent in this field and are tested via vaginal or, rarely, rectal applications in numerous clinical studies (9 different antiretroviral drugs in 33 clinical studies, especially in Africa). Only tenofovir (1 % gel) and dapivirine (25 mg in vaginal ring) progressed into the phase III clinical testing. Their efficiency depended on the user´s strict adherence to the application regimen (for tenofovir 54 %, for dapivirine 61 % in participants over 25 years of age). Despite this, they are expected to be important and effective tools of preventive medicine in the near future. This review summarizes the results obtained during long-term clinical testing (2005–2018) of antiretroviral drugs against vaginal and rectal transmission of HIV infection.

Open access
Comparison of high-performance thin layer chromatography/UV-densitometry and UV-derivative spectrophotometry for the determination of trimetazidine in pharmaceutical formulations

Abstract

New methods for assaying trimetazidine dihydrochloride on the basis of thin layer chromatography and spectrophotometry are proposed and compared in the paper. In HPTLC/UV-densitometry, separation is achieved by using a mobile phase composed of ammonia-methanol (30:70, V/V) on silica gel HPTLC plates F254. Quantification using a non-linear calibration curve is accomplished by densito-metric detection at 230 nm. Derivative spectrophotometric determination of trimetazidine dihydrochloride is carried out from the fourth derivative of the absorbance at 233 nm in peak-zero mode. Statistical comparison led to the conclusion that there is no significant difference between the two studied methods and, moreover, that they demonstrate satisfactory accuracy and precision for routine applications.

Open access
Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength

Abstract

Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.

Open access
Cytoreductive surgery and HIPEC (hyperthermic intraperitoneal chemotherapy) in combined treatment of ovarian cancer: time for the beginning of personalized therapy?

Abstract

Background and objectives. During the two past decades, a new therapeutic approach to ovarian cancer (OC) has been developed. This combines cytoreductive surgery (CRS) and hyperthermic intraperitoneal chemotherapy (HIPEC). However, almost no data exist regarding the utility of biomarkers of morphological heterogeneity as prognostic factors in such patients.

Methods. A retrospective study of the effectiveness of CRS and HIPEC was carried out in 59 patients with ovarian cancer. Biomarkers of morphological heterogeneity of OC were studied as prognostic factors: OC pathogenic types (based on the identification of р53 mutated gene protein expression) and homologous recombination deficit (basing on the identification of BRCA 1 gene expression status).

Results. The survival of patients reliably differed with the division into two pathogenetic OC types established by immunohistochemistry: the median disease-free survival of type I OC patients was 14±1.7 months, type ІІ – 8±1.6 months (р = 0.007); the median overall survival of type I OC patients was 23.5±6.7 months, type ІІ – 12±1.9 months (р = 0.017). The median overall survival of patients with the somatic mutation of BRCA 1 gene and complete cytoreduction was 22±4.8 months, and without the somatic mutation of BRCA 1 gene – 12±3.3 months (р = 0.047).

Conclusions. These data demonstrate that identification of the pathogenetic type of OC and BRCA 1 status may be useful for the personalized therapy of ovarian cancer patients treated with CRS/HIPEC.

Open access
The effects of pomegranate peel extract on recurrent aphthous stomatitis

Abstract

As high as 20% of the population is thought to have recurrent aphthous stomatitis (RAS), hence, finding new therapeutic agents may be needed. Pomegranate (Punica granatum), has been extensively used in the folk medicine of many cultures, as it possesses antioxidant, anti-inflammatory and anti-bacterial properties. In this study, it is hypothesized that a topical form of pomegranate peel extract (PPE) may shorten the duration, accelerate the healing and reduce the pain of RAS patients. The presented randomized, double-blind study was conducted on 56 patients. Herein, 28 patients were advised to apply PPE gel, and the other 28 patients were given placebo gel, twice daily for one week. Efficacy evaluations were made at days 0 (before using the gel), 3, 5 and 7. The mean values of ulcer size, pain and healing duration of ulcers were compared in both groups. PPE gel was significantly effective in reducing the pain (p<0.001), ulcer size (p<0.001), and healing duration of ulcers (p<0.001) over a period of one week. PPE in the form of oral gel can be used in the management of aphthous ulcers.

Open access
Fenugreek seeds estrogenic activity in ovariectomized female rats

Abstract

The estrogenic activities of fenugreek seeds (Trigonella foenum-graecum L.), widely used in traditional pharmacopoeia, are reflected in the uterus of ovariectomized female rats, with a slight increase in dry and wet weight, a thickening of the stroma and the uterine epithelium and the development of the endometrial glands. In the vagina, the estrogenic action is shown through an increase in the epidermal cell number and a tendency to keratinization, leading to vaginal opening.

Furthermore, this estrogenic potential of fenugreek seeds is confirmed by the over-expression of progesterone receptors in the uterine tissues supporting possible interactions between phytoestrogens and estrogen receptors.

Therefore, Fenugreek seeds may be capable of promoting the development of reproductive tissues of immature ovariectomized rats, and its estrogenic activity may take its action by holding phystoestrogens that interact with estrogen binding sites and activate the same estradiol-mediated cell signaling pathways.

Thus, our results give added scientific support to the popular use of Fenugreek seeds as an alternative for several health problems such as fertility and menopause related disorders.

Open access