有机化学实验邻苯二甲酸二丁酯制备的绿色化研究

以对甲苯磺酸（PTS）为催化剂,邻苯二甲酸酐和正丁醇为原料,微量实验合成邻苯二甲酸二丁酯。最佳反应条件为：邻苯二甲酸酐为0．02mol,丁醇、苯酐物质的量比为3：1,催化刑用量为原料邻苯二甲酸酐物质的量的1．5％。反应时间0．45h,回流反应下酯化率可达95．8％。反应时间短．催化剂用量少易分离。能够重复使用,酯化率高,不污染环境,符舍绿色化学原则。     

Soapnut: A replacement of synthetic surfactant for cosmetic and biomedical applications

Surfactants are organic amphiphilic compounds used for various applications such as preparation of soap, detergent, shampoo and in pharmaceutical industries. However, many synthetic surfactants illustrate detrimental effect due to the presence of anti-foaming characteristics, toxic and corrosive nature. The literature does not reveal information about any surfactant which does not depict the above stated disadvantages. Therefore, in the current work, by preparing surfactant from a natural resource, the abovementioned issues have been tried to address. The present investigation focus on the preparation of a natural surfactant derived from the soapnut (Sapindus mukorossi) for its potential application against synthetic surfactants. The physicochemical properties of the soapnut ensures it as a strong wetting agent. The chemical composition, surface topography and functional group analysis of the prepared surfactant were carried out by EDX, confocal microscope and SEM analysis, respectively. The characterization result reveals that the prepared surfactant is free from the element or functional group contributing toxicity or environmental issues. This analysis is further confirmed from the corrosion analysis. In addition to the above, the anti-microbial property of the developed surfactant has also been identified. The variation of foaming stability as a function of time are also performed and are compared with the synthetic surfactants. The comparison ascertains excellent foam stability in case of soapnut and this can be recommended as wetting agent in dropwise evaporative cooling. The current investigation also includes the examination of the successful applicability of soapnut added water in cosmetic industries, adsorbent preparation sector and pharmaceutical industries.     

Perspectives for the use of biotechnology in green chemistry applied to biopolymers,fuels and organic synthesis: from concepts to a critical point of view

Since the eighteenth century, after the first industrial revolution, humans have been exploiting the planet's natural resources in an unsustainable manner. This has caused some irreversible impacts on the environment. Because of this, we are facing a change of philosophy within the scientific community about chemical and industrial processes. During the 1990s, the concepts of green chemistry began to solidify, while in parallel some major advances in biotechnology were achieved through developments of genomic sciences and genetic and metabolic engineering. This work will discuss some new insights into the use of biotechnology as an important tool in green chemistry, showing new applications to biopolymers, biofuels and as a new alternative to traditional organic synthesis, making chemical processes more sustainable and less damaging to the planet.     

The effectivity analysis of accumulation of liposomal, micellar, and water-soluble forms of diminazene in cells and in organs

The study was aimed at evaluating the effectiveness of liposomal, micellar, and water-soluble drug forms of diminazene for its localization in cells and selective accumulation at the sites of aggregation of pathogenic organisms. Pharmacological and dynamic properties of a new injection micellar diminazene preparation were experimentally determined. These properties were compared with the same parameters obtained for the water-soluble and liposomal diminazene aceturate drug forms. The drug forms studied may be arranged in the following order of decreasing effectiveness of accumulation of diminazene in red and white blood cells and in murine organs: liposome form, micellar form, and water-soluble form.     

Disease-directed design of biodegradable polymers: Reactive oxygen species and pH-responsive micellar nanoparticles for anticancer drug delivery

Herein, we report reactive oxygen species (ROS)- and pH-responsive biodegradable polyethylene glycol (PEG)-block-polycarbonate by installing thioether groups onto the polycarbonate and its self-assembled core/shell structured micelles for anticancer drug delivery. Oxidation of thioethers to sulfoxide and subsequently sulfone induces an increase in hydrophilicity, resulting in more hydrophilic micellar core. This phase-change caused the micelles to swell and enhance cargo release. Carboxylic acid groups have also been installed onto thioether-containing polycarbonate to promote loading of amine-containing anticancer doxorubicin through electrostatic interaction. Urea-functionalized thioether-containing PEG-block-polycarbonates were synthesized to mix with the acid-functionalized PEG-block-polycarbonate for stabilizing micelle structure through hydrogen-bonding interaction. The mixed micelles were 50?nm in diameter and had a 25?wt% loading capacity for doxorubicin. Enhanced drug release from the micelles was triggered by low pH and high content of ROS. Drug-encapsulated micelles accumulated in tumors through leaky tumor vasculature in PC-3 human prostate cancer xenograft mouse model.     

Role of organic cation transporters in the renal handling of therapeutic agents and xenobiotics

Organic cations (OCs) constitute a diverse array of compounds of physiological, pharmacological, and toxicological importance. Renal secretion of these compounds, which occurs principally along the proximal portion of the nephron, plays a critical role in regulating the concentration of OCs in the plasma and in clearing the body of potentially toxic xenobiotic OCs. Transepithelial OC transport in the kidney involves separate entry and exit steps at the basolateral and luminal aspects of renal tubular cells. It is increasingly apparent that basolateral and luminal OC transport reflects the concerted activity of a suite of separate transport processes arranged in parallel in each pole of proximal tubule cells. Most of the transporters that appear to dominate renal secretion of OCs belong to a single family of transport proteins: the OCT Family. The characterization of their activity, and their localization within distinct regions of the kidney, has permitted development of models describing the molecular and cellular basis of the renal secretion of OCs.     

The activity of organic anion transporter-3: Role of dexamethasone

Human organic anion transporter-3 (hOAT3) is richly expressed in the kidney, where it plays critical roles in the secretion, from the blood to urine, of clinically important drugs, such as anti-viral therapeutics, anti-cancer drugs, antibiotics, antihypertensives, and anti-inflammatories. In the current study, we examined the role of dexamethasone in hOAT3 transport activity in the kidney HEK293 cells. Cis-inhibition study showed that dexamethasone exhibited a concentration-dependent inhibition of hOAT3-mediated uptake of estrone sulfate, a prototypical substrate for the transporter, with IC₅₀ value of 49.91 μM. Dixon plot analysis revealed that inhibition by dexamethasone was competitive with a Ki = 47.08 μM. In contrast to the cis-inhibition effect of dexamethasone, prolonged incubation (6 h) of hOAT3-expressing cells with dexamethasone resulted in an upregulation of hOAT3 expression and transport activity, kinetically revealed as an increase in the maximum transport velocity V_max without meaningful alteration in substrate-binding affinity K_m. Such upregulation was abrogated by GSK650394, a specific inhibitor for serum- and glucocorticoid-inducible kinases (sgk). Dexamethasone also enhanced sgk1 phosphorylation. Our study demonstrated that dexamethasone exhibits dual effects on hOAT3: it is a competitive inhibitor for hOAT3-mediated transport, and interestingly, when entering the cells, it stimulates hOAT3 expression and transport activity through sgk1.     

毛细管胶束电动色谱-紫外间接检测环胞素制剂中的有机溶剂

用毛细管胶束电动色谱-紫外间接检测环胞素软胶囊及环胞素注射液中的有机溶剂含量.采用非涂层弹性石英毛细管;操作缓冲液为含0.26mol/L十二烷基硫酸钠的0.02mol/L苯巴比妥钠溶液(pH9.0);检测波长为235nm(间接检测);电泳过程中在进样端始终外加适当的压力使基线保持稳定.以甲醇为内标物,乙醇和1,2-丙二醇均在2.6～18mg/ml范围内呈良好的线性关系.连续进样分析所得峰面积和迁移时间的相对标准偏差均不大于1.3%.环胞素软胶囊中乙醇和1,2-丙二醇含量测定方法的回收率分别为99,2%和100.7%;环胞素注射液中乙醇含量测定方法的回收率为99.5%.     

Green synthesis of magnesium oxide nanoparticles and its applications: A review

Green synthesis approaches are gaining the attention of researchers and they follow a less hazardous process to obtain nanoparticles. Green synthetic methods are currently used in industry than other physicochemical methods. The magnesium oxide (MgO) nanoparticles have been effectively produced by green synthesis which is environmental friendly, non-toxic with greater stability and has broad range of opportunities for the production of this material in the nanoscale. But still some challenges have been raised for the production of same nanoparticles with huge amount by green synthesis approaches. This is because the biological extracts during the synthesis creates a barrier onto the elucidation of the reactions and their mechanisms. Therefore, this review deals the summing up of variety of biological substrates and different methodologies that can be utilized for the green synthesis of magnesium oxide nanoparticles with impact on their properties. This article also explains the mechanism routes reported in various literatures for better understanding. The energy and environmental applications of the MgO nanoparticles are also dealt with in this article.     

研究型学习在中医药独立院校有机化学教学的实践

培养高素质的中医药应用型人才是独立学院义不容辞的责任。有机化学课程是大学低年级开设的中医药重要基础课．通过在有机化学的教学中引入研究型学习,探索在基础课程中培养应用型中医药人才的模式与途径,达到培养应用型人才的目标。     

The effect of water-soluble polymers, PEG and PVP, on the solubilisation of griseofulvin in aqueous micellar solutions of Pluronic F127

The purpose of this study was to investigate the possibility of enhancing the solubilisation capacity of micellar solutions of Pluronic F127 for the poorly water-soluble drug griseofulvin by co-formulating with a water-soluble polymer. The effect of the addition of the polyethylene glycols PEG6000 and 35000, and the poly(vinylpyrrolidone)s PVP K30 and K90, on the solubilisation capacity of 1wt% solutions of Pluronic F127 was related to the effect of these additives on particle size as determined by dynamic light scattering measurements. The addition of PEG35000 to 1wt% F127 solutions significantly increased the solubility capacity expressed in terms of unit weight of F127; PVP K90 had a smaller effect but no enhancement was noted following the addition of PEG6000 or PVP K30. Solubilisation enhancement was thought to be a consequence of the association of the polymers with the E-blocks of the micelle corona so providing an expanded region of reduced polarity for drug solubilisation.     

Role of surfactant protein-A (SP-A) in lung injury in response to acute ozone exposure of SP-A deficient mice

Millions are exposed to ozone levels above recommended limits, impairing lung function, causing epithelial damage and inflammation, and predisposing some individuals to pneumonia, asthma, and other lung conditions. Surfactant protein-A (SP-A) plays a role in host defense, the regulation of inflammation, and repair of tissue damage. We tested the hypothesis that the lungs of SP-A(-/-) (KO) mice are more susceptible to ozone-induced damage. We compared the effects of ozone on KO and wild type (WT) mice on the C57BL/6 genetic background by exposing them to 2 parts/million of ozone for 3 or 6 h and sacrificing them 0, 4, and 24 h later. Lungs were subject to bronchoalveolar lavage (BAL) or used to measure endpoints of oxidative stress and inflammation. Despite more total protein in BAL of KO mice after a 3 h ozone exposure, WT mice had increased oxidation of protein and had oxidized SP-A dimers. In KO mice there was epithelial damage as assessed by increased LDH activity and there was increased phospholipid content. In WT mice there were more BAL PMNs and elevated macrophage inflammatory protein (MIP)-2 and monocyte chemoattractant protein (MCP)-1. Changes in MIP-2 and MCP-1 were observed in both KO and WT, however mRNA levels differed. In KO mice MIP-2 mRNA levels changed little with ozone, but in WT levels they were significantly increased. In summary, several aspects of the inflammatory response differ between WT and KO mice. These in vivo findings appear to implicate SP-A in regulating inflammation and limiting epithelial damage in response to ozone exposure.     

The transport of organic cations in the small intestine: Current knowledge and emerging concepts

A wide variety of drugs and endogenous bioactive amines are organic cations (OCs). Approximately 40% of all conventional drugs on the market are OCs. Thus, the transport of xenobiotics or endogenous OCs in the body has been a subject of considerable interest, since the discovery and cloning of a family of OC transporters, referred to as organic cation transporter (OCTs), and a new subfamily of OCTs, OCTNs, leading to the functional characterization of these transporters in various systems including oocytes and some cell lines. Organic cation transporters are critical in drug absorption, targeting, and disposition of a drug. In this review, the recent advances in the characterization of organic cation transporters and their distribution in the small intestine are discussed. The results of the in vitro transport studies of various OCs in the small intestine using techniques such as isolated brush-border membrane vesicles, Ussing chamber systems and Caco-2 cells are discussed, and in vivo knock-out animal studies are summarized. Such information is essential for predicting pharmacokinetics and pharmacodynamics and in the design and development of new cationic drugs. An understanding of the mechanisms that control the intestinal transport of OCs will clearly aid achieving desirable clinical outcomes.     

Green synthesis of zinc oxide nanoparticles: A review of the synthesis methodology and mechanism of formation

Zinc oxide is of significant importance for many industries due to its versatile properties, which have been enhanced with the production of this material in the nanoscale. Nonetheless, the increase in concerns related to environmental impact has led to the development of eco-friendly processes for its production. Recent interest in obtaining metal and metal oxide nanoparticles using biological approaches has been reported in the literature. This method was termed ‘green synthesis’ as it is a less hazardous process than chemical and physical synthesis methods currently used in the industry to obtain these nanomaterials. Zinc oxide nanoparticles have been successfully obtained by green synthesis using different biological substrates. However, large scale production using green synthesis approaches remains a challenge due to the complexity of the biological extracts that poses a barrier onto the elucidation of the reactions and mechanism of formation that occur during the synthesis. Hence, the current review includes a summary of the different sources of biological substrates and methodologies applied to the green synthesis of zinc oxide nanoparticles and the impact on their properties. This work also describes the advances on the understanding of the mechanism routes reported in the literature.     

The subacute and chronic toxicity of cetyltrimethylammonium bromide (CTAB), a cationic surfactant,in the rat

Cetyltrimethylammonium bromide (CTAB), a cationic surfactant, was given to male and female Sprague-Dawley rats in drinking water in dosages of approximately 10, 20, and 45 mg/kg/day for 1 year. The surfactant was well tolerated at the two lowest dose levels. At the highest dose level a reduction in body weight was observed. In males the body weight remained reduced throughout the study, but in females the body weight was reduced only during the first 2 months of the study. It was found that food conversion was less efficient in male rats during the first 7 weeks of the study. No compound-related gross pathologic changes were seen on autopsy and no microscopic alterations were found in the wall of stomach and small intestine of treated animals.     

Green synthesis of bismuth based nanoparticles and its applications - A review

Bismuth based nanoparticles (BBNs)exhibit immense potential due to unique physico chemical properties, therefore extensively applied in diverse technologies. On this account, a great deal of attention is being devoted to green synthesizing BBNs, which is an environmentally safe process, non-toxic, and stable, with a wide range of nanoscale production options. This review emphasizes the importance of green approaches for synthesizing BBNsusing bio extracts derived from plants and microorganisms. The selection of precursors, reducing agents, coating agents, solvents, quantity evaluation, and experimental conditions are all discussed in this review elaborately. Also,a consolidative account ona diverse range of applications of BBNsisbeing highlighted, along with recent breakthroughs of green synthetic technology based onthe knowledge of mechanism routes that have been available in the recent literature. Since review articles are often central points for beginners, this report leads readers to the articles that highlight the noteworthy advancement in the field of BBNs research. The goals of this study are to (i) outline advanced bismuth-based compounds that have been used to date, (ii) describe drawbacks in synthetic strategy and possible solutions, and (iii) make recommendations for future research.     

Pyrazolo[3,4-d]pyrimidine scaffold: A review on synthetic approaches and EGFR and VEGFR inhibitory activities

The pyrazolo[3,4-d]pyrimidine core has received a lot of interest from the medicinal chemistry community as a promising framework for drug design and discovery. It is an isostere of the adenine ring of adenosine triphosphate, which allows it to mimic kinase active site hinge region binding contacts. This scaffold has a wide pharmacological and biological value, one of which is as an anticancer agent. Many successful anticancer medicines have been designed and synthesized using pyrazolo[3,4-d]pyrimidine as a key pharmacophore. The main synthetic routes of pyrazolo[3,4-d]pyrimidines as well as their recent developments as promising anticancer agents acting as endothelial growth factor receptors and vascular endothelial growth factor receptor inhibitors, published in the time frame from 1999 to 2022, are summarized in this review to set the direction for the design and synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives for clinical deployment in cancer treatment.     

Experimental and chemometric strategies for the development of Green Analytical Chemistry (GAC) spectroscopic methods for the determination of organic pollutants in natural waters

The development of Green Analytical Chemistry (GAC) methods is one of the most active areas of Green Chemistry. Especially relevant are GAC methods devoted to the detection and quantification of environmental pollutants, because they should not pollute the environment more than the analyte to be determined. While considerable attention has been paid to develop environmentally friendly alternatives for the first stage of the global analytical process (e.g., sample preparation techniques), relatively fewer works are dedicated to implement green approaches for obtaining the analytical signal. Current strategies that are based on the principles of Green Chemistry for the determination of common organic pollutants in natural waters are detailed. The review collects and discusses selected publications from about the last 5 years relating to the topic, highlighting the role of multivariate calibration as a modern and very useful tool to achieve the pursued objectives.     

Synthetic methodologies in organic chemistry involving incorporation of [17O] and [18O] isotopes

This review is a critical survey of the literature that aims to highlight the most significant developments on synthetic strategies involving stable oxygen isotopes ([¹⁷O] and [¹⁸O]). The labeling methodologies are categorized in groups, according to the oxygen‐containing functional group.     

Neurotoxicity of organic solvent mixtures: Embryotoxicity and fetotoxicity

The toxicity of organic solvents at different concentrations was examined to determine their effect on pregnant rats and their offspring. A very serious effect which inhalational exposure to n-hexane, methyl-ethyl-ketone and a mixture of the two organic solvents produced in pregnant rats was a concentration-dependent increase of intrauterine mortality. In cases of only prenatal exposure, the persistence of reduced body growth was an important result obtained at all concentrations we investigated (first solvent experiment, 500 ppm; second solvent experiment, 800 ppm; and third solvent experiment, 1000 to 1500 ppm; 23 hr day). In these cases, a delay in the maturation of cerebellar cortex was also observed. In cases of pre- and postnatal solvent exposure, the effects of malnutrition were added to the solvent-induced retardation. This resulted in an extreme delay in tissue maturation accompanied by a retarded cell maturation. The solvents examined had no teratogenic effect in pregnant rodents and their offspring. Neurotoxicity was restricted to the known structures of the adult animals, whose axons were damaged. They did, however, show a concentration-dependent embryotoxic and fetotoxic effect.