Volkova, A. A.Povarnina, P. YuNikiforov, D. M.Gudasheva, T. A....
4页
查看更多>>摘要：It is well known that the neurotrophins nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) are involved in learning and memory. Specialists of Zakusov Research Institute of Pharmacology designed and synthesized dimeric dipeptide mimetics of the 1(st) (GK-6) and 4(th) (GK-2) NGF loops and the 1(st) (GSB-214), 2(nd) (GTS-201), and 4(th) (GSB-106) BDNF loops that in vitro activated TrkA or TrkB receptors, respectively. Differences in the activation of PI3K/AKT, MAPK/ERK, and PLC-gamma 1 were recorded during incubation in HT-22 cell culture for 5 - 180 min. This work was aimed to study the mnemotropic activity of the original NGF and BDNF mimetics in the new-object recognition test in rats. The dipeptides were administered once intraperitoneally. It was found that GK-2 (0.5 and 1.0 mg/kg) and GSB-214 (0.1 and 1.0 mg/kg), activating PI3K/AKT and PLC-gamma 1 signaling pathways without affecting MAPK/ERK, statistically significantly improved long-term memory. Dipeptides GK-2 and GSB-214 seem promising for further development as drugs for correcting memory impairments.
查看更多>>摘要：Chitosan microspheres with lappaconitine hydrobromide were obtained by ionotropic gelation with sodium tripolyphosphate as a crosslinking agent. The efficiency of microencapsulation, i.e., the proportion of substance encapsulated inside the capsules of the initial amount was determined by a direct method. The release of the antiarrhythmic drug from the microspheres under conditions simulating the gastrointestinal tract was studied. Lappaconitine hydrobromide was microencapsulated by biopolymers from solutions during the study. The prepared microspheres were found to be free flowing and have a high capture rate and high percentage yield. It has been proven that polyelectrolyte microencapsulation makes it possible to obtain new sustained-release dosage forms of the antiarrhythmic drug lappaconitine hydrobromide for oral administration. The developed microsphere form of the antiarrhythmic drug can maintain a therapeutic concentration in the body for a longer time, which allows the frequency of drug administration and its toxic action to be reduced.
Kim, Su BinKim, Kwang JoonShrestha, JitendraOh, Yoon Sin...
7页
查看更多>>摘要：A series of 30 new analogs maintaining the backbone structure of FTY720 were synthesized by a very simple method. Regardless of newly introduced aromatic and non-aromatic head groups, the obtained structures showed cytotoxic effects. Specifically, in the case of aromatic head structures, only the head group containing nitrogen showed cytotoxic effects. In the case of non-aromatic head group, compound 23 with a relatively long chain head group showed this effect even at low concentrations. All the cytotoxic compounds showed protein phosphatase 2A activity and apoptotic effects regardless of the sphingosine kinase 1/2 inhibitory effect. Therefore, it was confirmed that the FTY720 backbone structure was an important factor that activated PP2A, resulting in anticancer effects.
查看更多>>摘要：This study was conducted to investigate the repair effect and mechanism of new platelet lysate film-forming spray (NPLFS) on rat skin burn wound model with a commonly used clinical dressing as the control. Forty-five SD rats were randomly divided into groups, including NPLFS treated (group A, n = 15), platelet-rich plasma (PRP) plaster group (group B, n = 15), and saline gauze cover group (group C, n = 15), fixed with 3M Tegaderm transparent film dressing. The healing rates on the 5th, 10th, 15th and 20th day, the histological hematoxylin and eosin (HE) staining changes on the 10th and 20th day, and the expression of CD31 on the 7th and 21th day after injury were observed. On the day 15 of treatment, the wounds in groups A and B were significantly reduced, while the degree of reduction in group C was not significant. On the day 20 of treatment, the wounds in groups A and B were completely healed and appeared flat, while the wounds in group C were only partly healed. On day 10, the HE staining showed significant increase in neovascularization in groups A and B as compared to group C (n = 3). The CD31 expression on day 20 after treatment showed that the integrated option densities (IODs) for rats in group A (20.13 +/- 1.50) and group B (21.15 +/- 0.79) were significantly higher than in group C (15.39 +/- 1.41, P < 0.01). Therefore, NPLFS can promote the healing of burn wounds, and the effect is similar to that of PRP.
查看更多>>摘要：In addition to methods such as radiotherapy and surgery, another effective way that is preferred for the treatment of cancer is based on the use of chemotherapeutic agents. Although there are more than hundred drugs for cancer treatment, there is still a need to develop new anticancer drugs because of reasons such as drug resistance, side effects, low selectivity and severe toxicity. Benzimidazole and benzothiazole ring systems are the basis of chemical structures of many important drugs because of their different pharmacological properties. In this work, due to potential anticancer effects of benzothiazole and benzimidazole ring systems, eight new compounds that contain both these ring systems in the same chemical structure were synthesized. The structures of obtained compounds were characterized by the IR, NMR, and mass spectroscopy and by elemental analysis data. Cytotoxic effects of the synthesized compounds were tested on Caco-2 (ATCC HTB-37), A549 (ATCC CCL-185) and NIH3T3 (ATCC CRL-1658) cell lines. Two compounds (3c and 3e) were determined as the most effective agents that showed activity comparable with that of the reference drug Cisplatin.
查看更多>>摘要：Some pyrazinamide derivatives (2a-2e, 2a '-2e ', and 2a ''-2e '') were synthesized and evaluated as antimycobacterial agents against Mycobacterium tuberculosis H37Rv strain. These derivatives were designed by structural modification of pyrazinamide with alkyl chains and six-membered hetereocylic rings, respectively. The title compounds were synthesized using pyrazinamide as the starting material for haloakylation (1a-1c), and then halo-alkylpyrazinamides were reacted with appropriate heterocyclic rings. The structures of compounds were confirmed by H-1 NMR, C-13 NMR, mass spectroscopy, and elemental analysis. The activity of pyrazinamide derivatives was assayed using microplate alamar blue assay (MABA) and characterized by minimum inhibitory concentrations (MICs). Results showed that the obtained pyrazinamide derivatives exhibited high inhibitory effect on M. tuberculosis. The antimycobacterial activity of compounds 2b ', 2d ', and 2e ' was the best among all compounds tested, and their MIC values were about 6.25 m mu/mL. These compounds have ethylene chain between pyrazinamide moiety and six-membered hetereocylic rings.
查看更多>>摘要：Xanthine is the most ubiquitous heterocyclic aromatic compound and have attracted much synthetic interest due to their numerous pharmacological activities. It is one of the principal moiety for leads in the field of drug discovery and development and plays a fundamental role in the area of medicinal chemistry. In this review paper, we tried to compile recent developments in xanthine and its derivatives, recently developed as anti-alzheimer's and anti-parkinsonism, anti-cancer, anti-asthmatic, anti-diabetic, anti-depressant and anxiolytic, analgesic and anti-inflammatory, diuretic, anti-epileptic, anti-tuberculosis, anti-microbial, sirtuin inhibitors and ligands of adenosine receptor subtypes.
Yakupova, L. R.Yunusova, S. G.Safiullin, R. L.Yunusov, M. S....
5页
查看更多>>摘要：The stability to oxidation during long-term storage of neutral lipids of common borage (Borago officinalis L.) seeds was studied. The organoleptic indices and contents of pigments and fatty acids remained almost unchanged for two years. The antioxidant activity of neutral lipids (NL) and polar lipids (PL) of B. officinalis seeds was determined using a model of radical chain oxidation of methyl oleate. Both NL and PL were found to contain antioxidants suppressing the oxidation of methyl oleate. The antioxidant activity and antioxidant content in NL were greater than those in PL of B. officinalis seeds. Long-term storage of B. officinalis seed oil was possible because of the presence of the antioxidant a-tocopherol.
查看更多>>摘要：Three new compounds "Viburnoate A-C" and two known compounds, namely, 4, 4-dimethyl-hexan-3-ol (1) and 4-tert-butyl-benzoic acid isobutyl ester (2), were isolated from ethyl acetate (EtOAc) fraction of medicinally important plant Viburnum grandiflorum. These compounds were isolated from the plant material by chromatographic techniques and then characterized using mass spectrometry, FTIR, H-1 NMR and C-13 NMR spectroscopic techniques. The study indicated Viburnoate A-C as new compounds. Viburnoate A, Viburnoate C, and isobutyl 4-(tert-butyl) benzoate are aromatic esters, while Viburnoate B and 4, 4-dimethylhexanol are aromatic aldehyde and alcohol, respectively. The isolated compounds were tested against bacteria (E. coli and S. aureus). The inhibition zones of Viburnoate A-C compounds against E. coli were 9 (+/- 0.2), 11 (+/- 0.4), 9 (+/- 0.4) mm and those against S. aureus were 13 (+/- 0.3), 16 (+/- 0.2), 15 (+/- 0.3) mm, respectively. The results indicated that Viburnoate B exhibited highest inhibition activity against both bacteria, which might be due to less crowded oxygen species.
Trang Huyen Xuan HoangTien Huu NguyenPhung Thanh HuongRaal, Ain...
6页
查看更多>>摘要：2-Methoxypancracine is a montanine-type alkaloid exhibiting anti-inflammatory, antioxidant, and antibacterial effects. The bulbs of Hippeastrum reticulatum (L'Her.) Herb. contain large amounts of 2-methoxypancracine. The aim of this study was to develop a HPLC-DAD method to quantify 2-methoxypancracine content in H. reticulatum. The HPLC analysis was carried out using a Poroshell 120 EC-C18 column eluted with acetonitrile and 0.01% methylamine (35:65, v/v) mixture in water at a flow rate of 0.5 mL/min with detection at 205 nm. Method validation was performed to assure its linearity, precision, accuracy, as well as the limit of detection (LOD) and limit of quantitation (LOQ). 2-Methoxypancracine displayed a linear relationship within a range of 2.5 - 103 mu g/mL. The developed method was shown to be precise with relative standard deviation less than 2.5%. The average recovery of 2-methoxypancracine was 101.2. The LOD and LOQ values were calculated as 0.08 mu g/mL and 0.25 mu g/mL, respectively. The concentrations of 2-methoxypancracine in the alkaloid fraction and in the dried powder of H. reticulatum were 28.95%, and 0.0740%, respectively. The validated method provides a useful tool for the quantification of 2-methoxypancracine in H. reticulatum. This is the first report of significant 2-methoxypancracine content in H. reticulatum.
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