In this study, methanolic crude extracts of Stephania japonica (Thunb.) Miers. (MESJ) whole plants were examined for possible antidepressant and sedative-hypnotic activities. Herein, the forced swimming test and tail suspension test were conducted to explore the antidepressant activity. In addition, the open field test and hole-board test were performed to evaluate the sedative-hypnotic activities. In the acute toxicity test, the MESJ ensured safety up to a dose of 2000 mg/kg, p.o. The experimental doses were 100 and 200 mg/kg p.o. In both the forced swimming test and tail suspension test, the extract significantly (p<0.01 and p<0.05) inhibited immobility time in a dose dependent manner compared to the control. These results (13.56-26.46% inhibition) indicate the mild antidepressant activity of MESJ compared to nortriptyline (60.4-64.6% inhibition). The open field test and hole-board test demonstrated the dose dependent significant (p<0.001, p<0.01 and p<0.05) and moderate sedative-hypnotic activities of the extract compared to diazepam. However, these activities were found to gradually decrease after 60 min in the open field test and must be considered as short-term activities, compared to diazepam. It can be claimed that the methanolic crude extract of Stephania japonica possesses mild antidepressant and moderate but short-term sedative-hypnotic activities.
Utilizing the batch Diazotization coupling reaction and the cloud point extraction kinetic spectrophotometric method, trace and Ultra trace amounts from reducing Nitrazepam and Clonazepam were evaluated by way of using 2,5-dimethoxyaniline as a new Chromogenic reagent to give colored products (red) in acidic medium which have a maximum absorption at 500 and 502 nm, respectively. In the work, the analytical data of batch and cloud point for Nitrazepam and Clonazepam depended on initial rate and fixation time. This involved concentrations of (0,3-9), (0.05-1.2), (0.5-10) and (0.025-1) µg mL−1, as well as molar absorptivity of (3.8×104), (3.1×105) (3.39×104) and (3.47×105) L mol−1 cm−1. According to our results, Sandall’s sensitivity were (0.0074), (0.0009), (0.0092) and (0.0009) µg cm−2, while detection limits were (0.055) and (0.069) µg mL−1, (8.4) and (8.5) ng mL−1. In addition, the measurements enrichment factors were (33.33) and (50), while preconcentration factors were (8) and (9.9), respectively. The reaction of Nitrazepam and Clonazepam with 2,5-dimethoxyaniline were a pseudo first order according to kinetic studies. The proposed methods are not affected by existence of excipients so the methods can be applied successfully for determination of Nitrazepam and Clonazepam in pharmaceutical preparations.
Liver damage is a common problem all over the world. To optimize the drug provision in the limited financing of the Health Care System, it is necessary to develop new drugs with hepatoprotective properties that are highly effective and of low cost. That is why we developed the original drug Lavaflam. Lavaflam is a combination of the following substances: dry concentrate of Helichrysum arenarium and Lavender oil. The purpose of the research was to assess the biochemical evidence of the hepatoprotective properties of the drug Lavaflam on the experimental model of subchronic hepatitis in rats. Construction of an experimental model of subchronic hepatitis in rats, comparison of hepatoprotective properties of Lavaflam and Carsil preparations on the basis of biochemical research. The subject of the study was to determine the hepatoprotective properties of Lavaflam tablets. Experimental subchronic hepatitis induced in rats by way of intragastrical introduction of tetrachlormethane. The study drug Lavaflam in this experimental model of subchronic tetrachlormethane hepatitis in rats showed a positive effect on oxidant processes by increasing the compensatory mechanisms of antioxidant systems; inhibiting free radical pathology; having positive effect on the processes of biliary excretion, cholestasis, reduction of infiltrative, destructive and inflammatory process in the liver; decreasing the cytolytic process; restoring the structure of the membrane components of hepatocytes; stabilizing and enhancing functional activity of the liver; restoring its protein-synthetic function; and increasing the ability of the drug Lavaflam to restore metabolic and liver damage.
As a result of the performed biochemical study of the hepatoprotective action of Lavaflam, it has been found that in the developed drug Lavaflam, the level of hepatoprotective action corresponds with the reference drug Carsil.
Aseptic meningitis is one of the most common inflammatory disorders of the meninges of the central nervous system (CNS). The aim of our study was to investigate the cytokine profiles in the CSF and in the serum of children with aseptic meningitis to determine their role in CNS inflammation. Sixty-eight (68) children were kept under observation. Cytokine profile of CSF and blood (based on the results of determining of IL-1β, IL-4, IL-10, TNF-α levels) and procalcitonin in children were revealed, meningitis severity were estimated by AMSS score. It was found that in the majority of patients with aseptic meningitis, the levels of IL-1β, TNF-α, IL-10 in CSF were increased and exceeded the serum cytokines levels. The severe course of meningitis was characterized by significantly higher concentrations of IL-1β and TNF-α in CSF, which was confirmed by positive correlation between AMSS score and IL-1β concentration (r=0.46, p<0.01), IL-10 (r=0.32, p<0.01), TNF-α (r=0.62, p<0.05). The IL-10/TNF-α ratio was – 17.8. PCT level in CSF was within normal limits in the majority of patients with meningitis. Increasing of anti-inflammatory cytokine levels in aseptic meningitis contributes to preventing of excessive inflammatory/immune responses in the brain. This can cause a longer diseases course and a longer recovery period. This can an indicate active production of cytokines in the central nervous system due to intrathecal inflammation and activation of immune responses caused by viral infection, but not due to penetration across the blood-brain barrier.
The study was conducted on seventy individuals of both genders who have been exposed to human cytomegalovirus, a common illness in Iraq. Total cases of human cytomegvirus associated with malignant brain tumors were detected by a real time PCR technique. This resulted in only thirty-six cases of true infection. Of these 24 cases were female, while 12 cases of male infected. The titer to assay the presence of anti- and pro-inflammatories was assessed in sera of all patients by using ELISA kits to evaluate cytokines. This indicated that the pro-inflammatory IL12, after seven days increased (1.67±0.23 pg/ml), while IL4, an anti-inflammatory, decreased to reach (0.39±0.16 pg/ml) (at p<0.05) in the plasm of the experimental patients compared with the control group.
Our interest has focused on the investigation of the anti-obese potential of kidney beans (P. vulgaris) pods extract. In the course of the study, obesity development in rats was induced with high-calorie diet. Control and obese rats then have consumed with aqueous kidney beans (P. vulgaris) pods extract during 6 weeks (200 mg/kg). Results show that the long-term consumption of P. vulgaris pods extract can lead to the reduction of hyperglycemia and insulin resistance development. Furthermore, we saw a normalization of lipid peroxidation parameters and oxidative modification of protein due to the consumption of the kidney beans (P. vulgaris) pods extract. Our experimental data demonstrate the ability of the kidney beans (P. vulgaris) pod extracts to mitigate obesity development but the details of this mechanism remains to be not fully understood.
To research and deepen the understanding of the links between morphological tubular kidney lesion parameters and serum markers – neutrophil gelatinase-associated lipocalin (NGAL) and interleukin-18 (IL-18), in patients with chronic glomerulonephritis (CGN) with saved renal function, as well as to estimate therapeutic correction of identified changes using ACE inhibitor ramipril. The diagnosis of “chronic glomerulonephritis” was verified based on clinical, laboratory and morphological data. Patients were divided into 2 clinical groups: patients with CGN and arterial hypertension (AH) and without AH. We used the data of renal biopsies to analyze the indicators of tubular kidney lesion in patients with CGN. Levels of serum NGAL and IL-18 were measured by means of ELISA kits. Treatment of patients was carried out over 24 weeks using the ACE inhibitor ramipril. The average daily dose of ramipril for the entire treatment period for patients with AH was 12.8±5.6 mg, patients of the second group – without AH, were treated with ramipril at a dose of 2.5 mg. On the basis of rank correlation analysis, we demonstrated that the level of serum NGAL is directly correlated with interstitial fibrosis (r=0.65; p<0.05), serum IL-18 – with dystrophic changes in the epithelium of renal tubules (r=0.81; p<0.05).
Conclusion. Serum levels of NGAL and IL-18 are one of the most sensitive markers of tubular kidney lesion and have diagnostic efficiency up to 97%. A 24-week treatment with ACE inhibitor ramipril in patients with CGN with and without AH leads to a decrease in the levels of tubular kidney lesion markers.
Doxorubicin cardiotoxicity is caused by various mechanisms, most importantly by oxidative stress originating in the mitochondria. Tirapazamine is a hypoxia-activated anticancer experimental drug. Both drugs in normoxia conditions undergo univalent reduction, thus tirapazamine may compete with doxorubicin in univalent reduction enzyme uptake. Herein, tirapazamine derivatives consisted of drug molecules and alkyl chain-connected triphenylphosphine cations that bring about an accumulation in mitochondria. The aim of this study was to evaluate the interaction of newly synthesized tirapazamine derivatives with doxorubicin in rat cardiomyocytes via an vitro model. In the work, H9C2 cells were incubated with combinations of doxorubicin, tirapazamine and seven variants of tirapazamine derivatives. After 24 hours, cell viability was assessed using MTT assay and the results were confirmed by microscopic observation. Tirapazamine in all tested concentrations did not revealed significant protective activity to cardiomyocytes treated with doxorubicine. However, tirapazamine derivatives diminished the cytotoxic effect of doxorubicin regardless of concentration and alkyl chain length. Tirapazamine derivatives have shown protective effects in relation to cardiomyocytes treated with doxorubicin and the mechanism of this phenomenon must be confirmed.
Nicotiana glauca (Solanaceae), or tree tobacco, is found in dry arid climates of North America, Africa and Europe. It has been reported to have both toxic and medicinal properties. The main aim of this study was to analyze the phytochemical screening and quantitative estimation of polyphenols, flavonoids and flavonols of crude extracts from the leaves of Nicotiana glauca and to evaluate its in vitro antioxidant properties. Three different solvents were used to extract bioactive compounds from powdered leaves of Nicotiana glauca: dichloromethane (DCM), ethyl acetate (AE) and n-buthanol (n-BuOH). The three extracts were then subjected to qualitative phytochemical screening using standard procedures. Total phenolics, total flavonoids and total flavonols contents of the extracts were measured by Folin Ciocalteu and Aluminium chloride methods respectively. Furthermore, the antioxidant capacity evaluation was performed using the DPPH, ABTS, DMSO alcalin, Phenantroline, FRAP and CUPRAC methods. The three extracts were then subjected to qualitative phytochemical screening using standard procedures. These methods showed the presence of polyphenols and comarines in all extracts. Moreover, flavonoids, tannins, steroids and quinones were reported in the AE and n-BuOH extracts. In addition, alkaloids were seen to be present in DCM extract, while saponines and phlobatannins were absent in all extracts. The antioxidant capacity evaluation was performed using the DPPH, ABTS, DMSO alcalin, Phenantroline, FRAP and CUPRAC methods.
Results using the DPPH method showed strong free radical scavinging activity for three extracts. This activity decreased with increasing concentration in the following order: n-BuOH>AE>DCM. In other assays, all extracts showed good antioxidant activity which decreased with increasing concentration in the following order: AE > n-BuOH > DCM. Extracts were compared with standards: BHT, BHA, Tanic acid and α-Tocopherol. The antioxidant of these extracts is probably related to polyphenols content (351.55±0.07, 284.98±0.08 and 133.8±0.06 mg/g), flavonoids (105.97±0.04, 164.44±0.07 and 1.18±0.005 mg/g) and flavonols (22.41±0.24, 18.75±0.46 mg/g) in AE and n-BuOH, respectively.
As a conclusion, the results of the present study indicate that Nicotiana glauca leaves could be considered as a potential source of natural antioxidants.
Despite a fairly large amount of literature data about the involvement of hydrogen sulfide in physiological and pathophysiological processes, its role in gastrointestinal tract functioning has not been studied sufficiently. This review systematizes and generalizes the mechanisms of H2S-associated regulation of gastrointestinal secretion and motility on the basis of literature sources processing and own research results. We analysed world professional literature and sources in Google Scholar, PubMed, MedLine, Embase, Cochrane, and data from more than 50 articles and books on the problem were processed in the article. This review gives a synopsis of the H2S function in the regulation of the secretory and motor-evacuation function, and in stimulating the reparative properties of the digestive tract, and indicates the main mechanisms.