An overview of inflammation: mechanism and consequences

Inflammation is an essential response provided by the immune systems that ensures the survival during infection and tissue injury. Inflammatory responses are essential for the maintenance of normal tissue homeostasis. The molecular mechanism of inflammation is quite a complicated process which is initiated by the recognition of specific molecular patterns associated with either infection or tissue injury. The entire process of the inflammatory response is mediated by several key regulators involved in the selective expression of proinflammatory molecules. Prolonged inflammations are often associated with severe detrimental side effects on health. Alterations in inflammatory responses due to persistent inducers or genetic variations are on the rise over the last couple of decades, causing a variety of inflammatory diseases and pathophysiological conditions.     

An overview of inflammation: mechanism and consequences

Inflammation is an essential response provided by the immune systems that ensures the survival during infection and tissue injury.Inflammatory responses are essential for the maintenance of normal tissue homeostasis.The molecular mechanism of inflammation is quite a complicated process which is initiated by the recognition of specific molecular patterns associated with either infection or tissue injury.The entire process of the inflammatory response is mediated by several key regulators involved in the selective expression of proinflammatory molecules.Prolonged inflammations are often associated with severe detrimental side effects on health.Alterations in inflammatory responses due to persistent inducers or genetic variations are on the rise over the last couple of decades,causing a variety of inflammatory diseases and pathophysiological conditions.     

微生物产色素机制及其生物活性

近年来,随着人工合成色素的大量使用引起一系列环境和健康问题,增加了人们对安全、无毒天然色素的需求.天然色素主要来源于植物和微生物,由于植物生长周期较长使植物源色素在大规模应用中受限.与植物源天然色素相比,微生物源色素易于大规模快速培养,具有更广阔的应用前景.本文系统总结了不同微生物源色素产生机制,及其在抗菌、抗氧化及抗...     

An overview of animal cell substrates for biological products

The issue of which cells to use as substrates for the production of biological products, and especially vaccines, has been with us in one form or another ever since the development of cell cultures in the 1950s.The major cell substrate events that occurred over the past 50 years are reviewed briefly. Although numerous conferences were held during that period, incomplete resolution of some cell substrate issues has remained. Specifically, the potential oncogenicity of cellular DNA derived from continuous cell lines, and the tests that are used to rule out the presence of adventitious agents have been recognized as areas that could benefit greatly from studies using state-of-the-art techniques.A collaborative effort involving WHO, NIAID, and IABS resulted from consensus recommendations of a 2004 conference, and the prospects for revised guidance in the near future on the characterization and use of animal cell substrates are bright.     

Liver glucokinase: An overview on the regulatory mechanisms of its activity

Blood glucose is the primary cellular substrate and in vivo must be tightly maintained. The liver plays a key role in glucose homeostasis increasing or decreasing glucose output and uptake during fasting and feeding. Glucokinase (GCK) is central to this process. Its activity is modulated in a coordinated manner via a complex set of mechanisms: in the postprandial period, the simultaneous rise in glucose and insulin increases GCK activity by enhanced gene expression, changes in cellular location, and interaction with regulatory proteins. Conversely, in the fasting state, the combined decrease in glucose and insulin concentrations and increase in glucagon concentrations, halt GCK activity. Herein we summarize the current knowledge regarding the regulation of hepatic GCK activity.     

Identification, biological activity, and mechanism of the anti-ischemic quinolone analog

The quinolone analog SQ-4004 has been identified as a potentially excellent anti-ischemic agent, which exhibited highly potent efficacy in reducing infarct volume size in vivo rat MCAO model (32.1% at 0.01mg/kg) and potent cardioprotective effect at myocardial infarction in vivo model (26.6% at 0.01mg/kg) while it exhibited highly reduced anti-bacterial activity. The mechanistic study revealed that the anti-ischemic activity might exert via an anti-apoptotic pathway, which implies its therapeutic uses against the ischemic cell injuries including ischemic stroke and ischemic heart disease.     

Study on the potential anti-cancer activity of phosphonium and ammonium-based ionic liquids

The anti-cancer activity and cytotoxicity of phosphonium and ammonium-based ionic liquids (ILs) have been determined for the first time via NCI’s in vitro 60 human tumor cell lines. The preliminary SAR showed that the chain length of alkyl substitution on the cations plays crucial role towards anti-tumor activity and cytotoxicity of these ionic liquids. In general, phosphonium-based ILs were found to be more active and less cytotoxic as compared to ammonium ILs. Cell line data and hollow fiber study has demonstrated the potential of ILs to be developed as therapeutic agent.     

Phosphatase activity of benthic marine algae. An overview

This review provides an account of the phosphatase activities of benthicmarine algae and is based on reports for more than a hundred species, includingcyanobacteria, red, brown and green algae. Particular emphasis is given to theuse of phosphomonoesterase activity as a rapid means of assessing thephosphorusstatus of the alga and thus indirectly that of the environment. Anunderstandingof the influence of environmental factors and the growth pattern of theparticular alga is important in carrying out assays. For instance, the responseto light differs markedly between species, especially in short-term assays,whenthe effect can be obvious or none. Considerations about the methodology formeasuring "alkaline phosphatase activity" are discussed, particularly whethertosimulate field conditions or to use optimum conditions. Recommendations aresuggested concerning the best methodology for routine use, followed by adiscussion of the future prospects for the method.     

Synthesis of cholesteryl doxorubicin and its anti-cancer activity

Doxorubicin (dox) has been used as anti-cancer agent, but there are disadvantages such as rapid excretion, short retention time and cardiotoxicity. For giving lipophilic properties to dox, it was modified with cholesterol derivatives that were validated as a component of liposomal gene delivery. This article describes the synthesis of dox derivatives (lipo-dox A-D), their cytotoxicity and cellular uptake. In A549, HeLa, MCF7 and MDA MB 231 cell lines, lipo-dox A and lipo-dox B substituted at alcohol group showed similar anti-cancer effect as dox, but lipo-dox C and lipo-dox D substituted at amino group did not. As a result, the amino group of dox seems an important site for its cancer cell inhibition. Lipophilic property of lipo-dox A and lipo-dox B induced more accumulation in cells compared to parent drug. Therefore, the newly synthesized lipo-dox A and lipo-dox B would be a good candidate for anti-cancer agent.     

An efficient synthesis and biological activity of substituted p-benzoquinones

An efficient synthesis of 2,5-diarylamino-3,6-dichloro-1,4-benzoquinone derivatives has been achieved by condensing mono substituted anilines with tetrachloro-p-benzoquinone in presence of fused sodium acetate as condensing agent under microwave irradiation without any solvent. All the synthesized compounds were tested for their antibacterial and antitumour activity using standard drugs.     

An overview of gene activity in the fat body of Drosophila gibberosa

In the larval fat body of Drosophila gibberosa, polytene chromosome structure and activity exhibit cytological differences from chromosomes of midgut and salivary glands. These differences include long-persisting puffs, transient puffs and long-persisting band modulations. Some early ecdysteroid-induced puffs are present in all three organs but few late puffs are present in the fat body. Comparative studies reveal, therefore, that late larval-early pupal puffing is enhanced in salivary glands relative to gut, fat body and Malpighian tubules. After the fat body breaks up in the prepupa, the rate of programmed cell death and the corresponding slow decline of chromosomal activity also differ from cell to cell and from other organs.by M.L. Pardue     

Synthesis and anti-cancer activity of chalcone linked imidazolones

A series of novel chalcone linked imidazolones were prepared and evaluated for their anti-cancer activity against a panel of 53 human tumour cell lines derived from nine different cancer types: leukemia, lung, colon, CNS, melanoma, ovarian, renal, prostate and breast. Some of these hybrids (6, 7 and 8) showed good anti-cancer activity with GI₅₀ values ranging from 1.26 to 13.9 μM. When breast carcinoma cells (MCF-7) were treated with 10 μM concentration of compounds TMAC, CA-4, 6 and 8 cell cycle arrest was observed in G2/M phase. Surprisingly, the increased concentration of the same compound to 30 μM caused accumulation of cells in G0/G1 phase of the cell cycle.     

Molecular mechanism of the anti-cancer activity of cerivastatin,an inhibitor of HMG-CoA reductase,on aggressive human breast cancer cells

Statins are currently used for the treatment of hypercholesterolemia. Recently, we demonstrated that cerivastatin also reduces the proliferation and invasion of aggressive breast cancer cells, MDA-MB-231. In this report, a molecular mechanism to explain its anti-cancer action is proposed by combining the study of cerivastatin effect on both gene expression (microarray) and signal transduction pathways. Firstly, the expression of 13 genes was modified by cerivastatin and confirmed at protein level. They could contribute to the inhibition of both cell proliferation (down-regulation of cyclin D1, PCNA, c-myc and up-regulation p21(Waf1), p19(INK4d), integrin beta8) and cell invasion, either directly (decrease in u-PA, MMP-9, u-PAR, PAI-1 and increase in anti-oncogenes Wnt-5a and H-cadherin) or indirectly by stimulating an anti-angiogenic gene (thrombospondin-2). The anti-angiogenic activity was confirmed by in vivo experiments. Secondly, we demonstrated that the biochemical mechanism of its anti-cancer action could be mainly explained by the inhibition of RhoA-dependent cell signalling. This hypothesis was supported by the fact that a RhoA inhibitor (C3 exoenzyme) or a dominant negative mutant RhoA (N19RhoA) induced similar effects to those of cerivastatin. In conclusion, cerivastatin, by preventing RhoA prenylation, inhibits (i) the RhoA/ROCK pathway, leading to defective actin stress fibres formation responsible for the loss of traction forces required for cell motility and (ii) the RhoA/FAK/AKT signalling pathway that could explain the majority of cancer-related gene modifications described above. Thus, the inhibition of RhoA cell signalling could be a good strategy in therapy of aggressive forms of breast cancer.     

Genetics of anorexia nervosa: An overview of genome-wide association studies and emerging biological links

Anorexia nervosa (AN) is a complex disorder with a strong genetic component. Comorbidities are frequent and there is substantial overlap with other disorders. The lack of understanding of the molecular and neuroanatomical causes has made it difficult to develop effective treatments and it is often difficult to treat in clinical practice. Recent advances in genetics have changed our understanding of polygenic diseases, increasing the possibility of understanding better how molecular pathways are intertwined. This review synthetizes the current state of genetic research providing an overview of genome-wide association studies (GWAS) findings in AN as well as overlap with other disorders, traits, pathways, and imaging results. This paper also discusses the different putative global pathways that are contributing to the disease including the evidence for metabolic and psychiatric origin of the disease.     

Mode of action and determination of antioxidant activity in the dietary sources: An overview

Determination of antioxidant/capacity in the dietary, food, drugs, and biological samples is an interesting approach for testing the safety of these compounds and for drug development. Investigating the google searching engines for the words (measurement + antioxidant + capacity) yielded more than 20 million results, which makes it very difficult to follow. Therefore, collecting the common methods to measure the antioxidant activity/capacity in the food products and biological samples will reduce the burden for both the students and researchers. Nowadays, it is widely accepted that a plant-based diet with a high intake of dietary sources such as vegetables, fruits, and other nutrient-rich plant foods may decrease the effect of oxidative stress-related diseases. In this review article, we have provided the most recent advances in the most common in vitro methods used for evaluating the antioxidant potential of numerous food products, plant extracts, and biological fluids. We have also provided detailed procedures on how to perform them and analyze the results. This review article shall be a comprehensive reference for all techniques used in this area.     

Dihydroxylated E,E,Z-docosatrienes. An overview of their synthesis and biological significance

Dihydroxylated E,E,Z-docosatrienes are acyclic lipoxygenase metabolites of 22-carbon atom polyunsaturated fatty acids (PUFAs) containing a conjugated E,E,Z-triene flanked by two secondary allylic alcohols. The two main metabolites, protectin D1 (PD1) and its regioisomer maresin 1 (MaR1), were shown to be actively involved in the resolution and more specifically the termination of the inflammation process.Studies directed at the synthesis of E,E,Z-docosatrienes have been undertaken to resolve stereochemical ambiguities, and provide standards for biological evaluation and reference samples for in-vivo detection and lipidomic analyses.In this review we provide a brief update of the literature on the biological significance of E,E,Z-docosatrienes and the role that synthetic organic chemists has played in the development of these lipids, providing an overview and comparison of the different strategies employed to access synthetic E,E,Z-docosatriene standards.     

Synthesis and anti-cancer activity evaluation of new aurone derivatives

Abstract

In this study, we have synthesized 2-[3- or 4-(2-aryl-2-oxoethoxy)arylidene]benzofuran-3-one derivatives (D1–D38) and evaluated their anti-cancer activities. The final compounds were obtained in multistep synthesis reactions using benzofuranon-3-one derivatives (A1–A4, B) as starting materials which were gained in various synthetic ways. Aurone derivatives (C1–C10) were acquired with the condensation reaction of these starting materials and 3-/4-hydroxybenzaldehyde which were then reacted with α-bromoacetophenones to get final compounds. The anti-cancer activity of the selected compounds was performed by National Cancer Institute (NCI), USA against 60 human tumor cell lines derived from nine neoplastic diseases. Compounds exhibited anti-cancer activity in varying ratios.