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(CI) for each pair were calculated from determined EC50 values.ASEobtained yields were 1-5% for nonpolar and20-25% for polar solvents. Eighteen of theseextracts exhibited good antiplasmodial selectivity indices (SI >250). Exhibited fold increases in activity of aqueous and ethanol extracts of the polyherbals: PNF (5; 3), PFC (8; 0.8), PFH (6; 39), PFA (4; 0.3), PFT (1.3; 12.6), PFS (5.7; 0.2), indicating improved therapeutic selectivity, potential efficacy and safety for fold increases > 4. Out of 120 paired extracts, 21 aqueous and 16 ethanol extracts exhibited synergism with
CI < 0.8. Identified synergistic pairs informedconditions for improving therapeutic selectivity. The outcomes are likely to substantially advance phytotherapy and the future of medicine.
References:
1. Deshpande, Kuppast,. 2016. Med Chem., 6:1.
2. Izumiyama et al., 2009. Exp Parasitol. 121(2):144-150.
3. Nociari et al. 1998. JImmunol Meth, 213(2):157-167.
4. Ohrt et al. 2002. Antimicrob Agent Chemother., 46(8): 2518-2524.
INVESTIGATION OF THE INFLUENCE OF GLYCOSYLATED POLYPEPTIDE OF SEA URCHINS ON LPS-INDUCED PHOSPHORYLATION OF P38 MAP-KINASES IN U937 CELL CULTURE
© Baditch S.P., Malysheva I.A., Pozharitskaya O.N., Shikov A.N.
Saint Petersburg Institute of Pharmacy, Leningrad region, Vsevolozhsky district, 188663, Kuzmolovo P 245, Russia
The test object is a substance glycosylated polypeptide (GPP) 3.5 kDa. Peptide was isolated from the internal organs of the green sea urchins Strongylocentrotus droebachiensis (O.F. Müller, 1776) by original technology. It is proposed to use GPP for the treatment of postinflammatory conditions, in which the inflammatory process plays a key role. The parameters of the number of phosphorylated forms of MAP kinases and the total number of MAP kinases in U937 cell culture were evaluated by the immunoblot method [1, 2]. The aim of the study is to study the effect of the glycosylated polypeptide on LPS-induced phosphorylation of p38 MAP kinases
in U937 cell culture. To study the effect of GPP, the cell culture was incubated with lipopolysaccharide (LPS), then a specific inhibitor SB 203580 (Sigma) of human p38 MAP kinase and the test substance were added at various concentrations. An estimate of the number of phosphorylated forms of p38 MAP kinase in the model showed that the threshold concentration at which the inhibitory effect begins to appear is 25 ng/ml. Direct concentration dependence was observed in the range from 0.41 ng/ml to 2.50 ng/ml (Table 1). This action had the character of direct concentration dependence.
The IC50 of the GLP substance was 1.33 ng/ml.
Table 1. Effect of GPP on the level of phosphorylated forms of p38 MAP kinase in U937 cell culture stimulated by LPS (LPS stimulated cells without inhibitors were used as a negative control), M ± m
Samples, concentration, ng/ml Quantity of phospho-MAPKs p38 (% from control), M ± m
Intact group 39.4±2.6 (n = 12)
Negative control (stimulation of LPS) 100 (n = 12)
Positive control (specific inhibitor), 1880 26.3±1.6 (n = 12)
GPP, 2.50 26.4±1.4 (n = 9)
GPP, 1.25 48.6±2.1 (n = 9)
GPP, 0.63 64.9±1.8 (n = 12)
GPP, 0.41 72.5±1.7 (n = 6)
1 2 3 4 5 6 7 8 9 10 11 12 13 14
Figure 1. Effect of GPP on the level of phosphorylated forms of p38 MAP kinase: 1 - intact cells; 2 - cells + LPS; 3 - cells + LPS + + SB; 4 - cells + LPS + GPP 50 ng/ml; 5 - cells + LPS + GPP 50 ng/ml; 6 - cells + LPS + GPP 25 ng/ml; 7 - cells + LPS + GPP 25 ng/ml; 8 - cells + LPS + GPP 10 ng/ml; 9 - cells + LPS + GPP 2,5 ng/ml; 10 - cells + LPS + GPP 1,25 ng/ml; 11 - cells + LPS + + GPP 0,63 ng/ml; 12 - cells + LPS + GPP 0,41 ng/ml; 13 - cells + LPS + GPP 0,41 ng/ml; 14 - cells + LPS + GPP 0,16 ng/ml
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The results of the study, it can be concluded that the revealed inhibition of phosphorylation of p38 MAP kinases by the substance of GPP is one of the possible mechanisms of anti-inflammatory action of this substance.
This work was supported by Ministry of education and science of the Russian federation (Contract N 14.N08.12.0070).
References:
1. Kyriakis JM, Avruch J, 2001. Physiol Rev, 81:807-869.
2. Saklatvala J, 2004. Curr Opin Pharm., 4:372-377
ANTI-INFLAMMATORY ACTIVITY OF A FEED SUPPLEMENTED WITH DRY EXTRACTS OF BOSWELLIA SERRATA AND SALIXALBA IN LAYING HENS
© Martina Bertocchi1, Giulia Andreani1, Federica Medici1, Enea Ferlizza1,
Maurizio Scozzoli2, Augusta Zannoni1, Monica Forni1, Cinzia Benazzi1, Gloria Isani1
1 Department of Veterinary Medical Sciences, University of Bologna, Ozzano Emilia, Bologna, Italy;
2 Veterinarian SIROE, Italian Society Essential Oils
The resin of Boswellia serrata Roxb. and bark of Salix alba L. are commonly used for their anti-inflammatory activity. Hens are frequently affected by inflammatory intestinal disorders, during the critical period between the last vaccination and the early eggproduction, requiring pharmacological treatments. The aim of the present research was to investigate the effect of a feed supplemented with dry extracts of B. serrata and S. alba (150 mg/Kg feed of each extract) in laying hens during this critical phase. Metal concentration, biochemical and histopathological parameters were analysed using a multidisciplinary approach. Hens of two farms (10000 hens each) were fed supplemented feed and control feed for 3 weeks. Liver, ileum and plasma samples (n = 8) were obtained at fixed times (before, during and after the supplementation), from treated and control animals. At the end of the supplementation,in treated henshistopathological analyses of the ileum showeda significant reduction in crypt length, associated
with a lower inflammatoryinfiltrateand significantly lower Zn concentrations(14.6 ± 1.8 vs 16.9 ± 1.1 ^g/g wet weight, p < 0.05) presumably due to the beneficial effect of the applied phytoextracts. Moreover, it can be hypothesized that higher levels of intestinal Zn in control animals mightbe relatedto increased blood supply and increasednumber of Paneth cells, that are characterized by high concentrations of Zn. Serum chemistry analyses were indicative of a significant hypolipemic effect of the phytoextracts in treated hens (triglycerides 1257 ± 218 vs 1596 ± 139 mg/dL, p < 0.05; cholesterol 120 ± 25 vs 183 ± 5 mg/dL, p < 0.05). In conclusion, this research, though preliminary, demonstrated an anti-inflammatory effect ofa feed supplemented with dry extracts of B. serrata and S. alba in laying hens. These phytoextracts could reduce the risk of inflammatory conditions, while increasing the animal welfare and possibly the quality of animal productions.
NANOENCAPSULATION OF EXTRACTS: WHICH INNOVATION POTENTIAL DOES IT HAVE?
© Anna Rita Bilia, Benedetta Isacchi, Vieri Piazzini, Maria Camilla Bergonzi
Department of Chemistry, University of Florence, via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy
Extracts are complex mixtures of constituents having different polarities and absorption properties. In many cases, extracts have good activity in in vitro assays, which is not reproducible in in vivo experiments. Occasionally, constituents can be incompatible with other components in the formulation or have undesirable properties, consequently, nanotechnological strategies have attempted to enhance their efficacy. The nanosystems can increase selectivity and activity, protect against thermal- or photodegradation, reduce side effects, promote sustained release of active constituents, or
reduce the required dose, generally resulting in improved activity [1]. Nanostructures are usually assumed as a new phenomenon, but nature is all about nanoscale structures. A variety of functional nanostructures are present in nature and biology plays around with the molecular scale all the time, it is the level at which all biological reactions occur [2]. Nanomedicine is crucial in developing appropriate therapeutic treatments of emerging extracts with pleiotropic functions, including essential oils [3] and widely marketed ginseng, green tea, ginkgo, and milk thistle extracts [1, 4].
Obzory po kliniceskoj farmacologii i lekarstvennoj terapii [Reviews of clinical pharmacology and drug therapy]
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