Research progress of boron-containing drugs / 中国药科大学学报

@#In recent years, the research on boron-containing drugs, especially boric acid drugs, has been increasing gradually.Boron-containing drugs, which have been a new area of research for pharmaceutical chemists in the development of new drugs, play an increasingly important anti-inflammatory, antibacterial, and anti-tumor role.At present, five boron-containing drugs have been approved, many are under clinical trials, and more are under investigation around the world, which has greatly expanded the application of boron in the research of new drugs.This paper introduces the characteristics of boron, and reviews the indications of representative boron-containing drugs in various research stages, their binding mechanisms with targets, and their progress after entering clinical trials, aiming to provide reference for further research on boron-containing drugs.

Bioorthogonal click-to-release reaction for regulating iodo-BODIPY PDT probe / 药学学报

In this study, we synthesized six tetrazine-dipyrromethene boron difluoride (BODIPY) probes and achieved a remarkable up to 14-fold increase in singlet oxygen yield via tetrazine bioorthogonal click-to-release reactions. We systematically investigated the photodynamic activity of these probes, revealing crucial structure-activity relationships. Additionally, we evaluated the stability and release kinetics of these probes and identified P5 and P6 as ideal candidates for photodynamic therapy in live cells. This innovative strategy opens new avenues for fine-tuning the photodynamic properties of BODIPY dyes, thereby expanding their utility in cancer therapy.

Analysis of neutron beam quality control test items in boron neutron capture therapy (BNCT) equipment / 中华放射医学与防护杂志

Objective:To provide reference for establishing the testing method for quality control of neutron beam in boron neutron capture therapy (BNCT) equipment in China by testing the radiation characteristic parameters and dosimetry characteristic parameters of epithermal neutron beam in hospital neutron irradiator (IHNI).Methods:By comparing the uncertainties in the result of various test items with the deviation values recommended by the European Joint Research Center (EC-JRC), the feasibility of the relevant of testing method was analyzed and evaluated.Results:The uncertainty in epithermal neutron fluence rate was 2.7%. The uncertainty in ratio of thermal to epithermal neutron fluence rate was 3.1%. The uncertainty in ratio of fast neutron air kerma to epithermal neutron fluence rate was 9.3%. The uncertainty in ratio of gamma air kerma to epithermal neutron fluence rate was 8.7%. The uncertainty in spatial distribution of neutron fluence rate was 2.7%. The uncertainty in thermal neutron fluence rate in phantom was 1.8%. The uncertainty in neutron and gamma-ray dose rate in phantom was 17.1% and 4.0%, respectively.Conclusions:The uncertainty in neutron dose rate measurement result in phantom is higher, and further research is needed to improve the accuracy of the testing method. The uncertainty in the measurement result of other test items is lower, and the accuracy of the test result is expected to meet the allowable deviation value recommended by the European Joint Research Center, and the test method is feasible.

Development of dose verification methods for boron neutron capture therapy / 中华放射医学与防护杂志

To summarize the progress in BNCT dose verification method in the world and discusses their development prospects. Boron neutron capture therapy (BNCT) utilizes the specific capture reaction between the neutrons and boron drugs enriched in tumor cells to selectively kill tumor cells. In order to verify the accuracy of the radiotherapy plan and ensure the therapeutic effect on patients, it is necessary to measure the dose before treatment and compare the experimental radiation dose with the planned dose. The current BNCT dose measurement method mainly include point dose measurement method based on ionization chambers, thermoluminescence dosimeters and activation foils, two-dimensional dose measurement method based on films, and three-dimensional dose measurement method based on gel dosimeters.

The effect of lithium tetraborate as a novel cardioprotective agent after renal ischemia-reperfusion injury

Abstract Epidemiological studies suggest that acute kidney injury has certain effect on myocardial function. In this study, for the first time, we tested a boron compound namely lithium tetraborate an act as an anti-oxidant and anti-inflammatory agent in ischemia-reperfusion injury. For this, we employed an in vivo rat model with kidney ischemia reperfusion injury to evaluate cardiac injury to clarify the mechanisms of lithium tetraborate. The evaluation of cardiac injury through kidney artery occlusion and reperfusion rat model indicated that lithium tetraborate could (1) reduce oxidative stress-induced endothelial dysfunction; (2) attenuate the inflammatory response of cardiac cells; and (3) alleviate the apoptosis and necrosis of myocytes. In summary, lithium tetraborate demonstrates significant therapeutic properties that contribute to the amelioration of cardiac damage, and it could be a promising candidate for future applications in myocardial dysfunction.

Study of end-to-end magnetic anastomosis technique of infrahepatic inferior vena cava in rats / 器官移植

Objective To develop a magnetic anastomosis device for infrahepatic inferior vena cava and verify its feasibility and safety in rat models. Methods According to the anatomical characteristics of rat inferior vena cava, a magnetic device suitable for end-to-end anastomosis of infrahepatic inferior vena cava was designed and manufactured. The device consisted of the inner and outer rings. The inner ring was a coated neodymium-iron-boron magnetic ring, and the outer ring was made of polyetheretherketone by 3D printing. Ten fine holes are evenly distributed on the outer ring, of which 5 fine holes were used to load the fine needles, and the other 5 fine holes were mutually connected with the fine needles of the contralateral anastomosis ring during anastomosis. The outer ring was uniformly loaded with fine needles and then bonded with the inner ring to form a magnetic anastomosis complex. Bilateral ends of vessels passed through the anastomosis ring and were fixed to the fine needles, and then end-to-end vascular anastomosis was performed by mutual attraction of two magnetic anastomosis rings. Twenty SD rats were selected and received end-to-end anastomosis of infrahepatic inferior vena cava with magnetic anastomosis device. The time of vascular occlusion, postoperative survival, postoperative anastomotic patency, gross observation and histological examination of anastomotic stoma were analyzed. Results All rats successfully completed end-to-end magnetic anastomosis of the infrahepatic inferior vena cava, and the time of vascular occlusion was 4~6 min. One rat died at 10 d after operation, and the other rats survived within postoperative 2 months. The patency rates of anastomotic stoma in surviving rats at postoperative 1 d, 3 d, 1 month and 2 months were 100%, 100%, 95% and 95%, respectively. At 2 months after operation, no obvious displacement and angulation of the anastomosis device were seen. No signs of corrosion and cracking of the anastomosis rings were observed. No evident hyperplasia and edema of surrounding tissues were noted. Bilateral ends of vessels were completely healed, and no obvious stenosis or thrombosis was found at the anastomotic stoma. Histological examination showed high continuity of bilateral vascular walls of anastomotic stoma, the inner surface of anastomotic stoma was covered by endothelial cells, and no thrombus or fibrous tissue was attached. Conclusions It is safe and feasible to utilize the self-designed magnetic anastomosis device to perform end-to-end magnetic anastomosis of infrahepatic inferior vena cava in rat models.

Oxidative Damage to BV2 Cells by Trichloroacetic Acid: Protective Role of Boron via the p53 Pathway / 生物医学与环境科学（英文）

This study aimed to investigate the neurotoxicity induced by trichloroacetic acid (TCA) and the possible protective mechanisms of boron (B). Mouse BV2 cells were treated with TCA (0, 0.39, 0.78, 1.56, 3.12, 6.25, or 12.5 mmol/L) and B (0, 7.8, 15.6, 31.25, 62.5, 125, 500, or 1,000 mmol/L) for 3 h and 24 h, respectively. Then, reactive oxygen species, and supernatant proinflammatory cytokine and protein levels were analyzed after 24 h of combined exposure. Beyond the dose-dependent decrease in the cellular viability, it clearly increased after B supplementation ( P < 0.05). Moreover, B decreased oxidative damage, and significantly down-regulated IL-6 levels and up-regulated TNF-β production ( P < 0.05). B also decreased apoptosis via the p53 pathway. The present findings indicated that TCA may induce oxidative damage, whereas B mitigates these adverse effects by decreasing cell apoptosis.

Improving micropropagation of some grape cultivars via boron, calcium and phosphate

BACKGROUND: An efficient regeneration protocol is a priority for the successful application of plant biotechnology. Grape nodal explants were used to develop a micropropagation protocol for Thompson Seedless and Taify cvs. Explants were cultured on MS medium supplemented with Kinetin or benzylaminopurine (BA) and indolebutyric acid (IBA). RESULTS: For both cultivars, axillary buds were grown, only, on a medium enriched with kinetin, moreover, shoot tip necrosis and callus formation were observed on Thompson Seedless cv. cultures grown on a medium with BA. Supplementing the growth medium with 100 mM (boron) B and 2.5 mM (calcium) Ca successfully help overcome these phenomena. The highest regenerated shoot numbers (14 and 6.2 explant 1 ) for Taify and Thompson Seedless cvs., respectively, were on media supplemented with 13.2 mM BA + 4.9 mM IBA and BA 13.2 mM + 5.8 mM IBA, respectively. Moreover, these media supported the developing shoots to have the heaviest dry weights (1.46 and 0.72 mg explant 1 ) for Taify and Thompson Seedless cvs., respectively. Thompson Seedless cv. regenerated shoot numbers and their dry weights were significantly increased by increasing the MS medium PO4 concentration. However, these two parameters were significantly decreased for Taify cv. Developing shoots were elongated and rooted on MS medium enriched with 4.9 mM, IBA 100 mM B and 2.5 mM Ca. Plantlets were acclimatized and successfully transferred to the greenhouse conditions. CONCLUSIONS: A novel promising protocol for Thomson Seedless and Taify cvs. micropropagation using single nodes has been developed.

Synthesis of new boron containing compound (CCB-2) based on curcumin structure and its cytotoxic effect against cancer cells

Boron containing compound (BCC) offers the potential further development for therapy against malignant cancers.We successfully synthesized a new compound based on curcumin structure (curcumin analogue) containing boronatoms, namely, CCB-2 and revealed its cytotoxic activities on various cancer cell lines. The compound was simplysynthesized based on aldol condensation using acetone and 4-formylphenyl boronic acid resulted a symmetry CCB-2.The compound was then tested for cytotoxic activities in several cell lines. CCB-2 demonstrated cytotoxic effect onMCF-7/HER-2, MCF-7, RAW 264.7, and 4T1 with IC50 value of 12 µM, 54 µM, 26 µM, and < 10 µM, respectively,while less toxic in fibroblast cells. This compound performed superior cytotoxic against highly metastatic cancer cell,4T1. In addition, CCB-2 induced cells accumulation in G2/M phase, but decreased the accumulation of intracellularReactive oxygen species level in 4T1 cells. All the data suggest that this new compound is promising to be developedas anti-cancer agent rather than for Boron Neutron Capture Therapy-based cancer therapy

Nobiletin and its derivatives overcome multidrug resistance (MDR) in cancer: total synthesis and discovery of potent MDR reversal agents

Our recent studies demonstrated that the natural product nobiletin (NOB) served as a promising multidrug resistance (MDR) reversal agent and improved the effectiveness of cancer chemotherapy . However, low aqueous solubility and difficulty in total synthesis limited its application as a therapeutic agent. To tackle these challenges, NOB was synthesized in a high yield by a concise route of six steps and fourteen derivatives were synthesized with remarkable solubility and efficacy. All the compounds showed improved sensitivity to paclitaxel (PTX) in P-glycoprotein (P-gp) overexpressing MDR cancer cells. Among them, compound exhibited water solubility 280-fold higher than NOB. A drug-resistance A549/T xenograft model showed that at a dose of 50 mg/kg co-administered with PTX (15 mg/kg), inhibited tumor growth more effective than NOB and remarkably increased PTX concentration in the tumors P-gp inhibition. Moreover, Western blot experiments revealed that inhibited expression of NRF2, phosphorylated ERK and AKT in MDR cancer cells, thus implying of multiple mechanisms to reverse MDR in lung cancer.

Effect of Combined Application of Nitrogen and Boron on Yield Contributing Characters and Yield of Sesame (Sesamum indicum L.)

Sesame is an important oilseed crop due to its different types of commercial application. The produced oil from sesame uses for food and beauty care product preparation due to its high nutritive value. However, the yield of sesame is comparatively low than other oilseed crops. Nitrogen and Boron are essential nutrients for plant development and growth. So, the combined application of nitrogen and boron can increase the yield of sesame. From these perspectives, an experiment was carried out to study the effect of nitrogen and boron application on yield contributing characters and yield of sesame. The experiment consisted of four Nitrogen doses (N0: 0 kg N/ha (control), N1: 50 kg N/ha, N2: 60 kg N/ha, N3: 70 kg N/ha) and three Boron doses (B0: 0 kg B/ha (control), B1: 2 kg B/ha, B2: 3 kg B/ha). It was laid out in two factors Randomized Complete Block Design (RCBD) with three replications. Result demonstrated that combination of 60 kg N/ha and 3.0 kg B/ha were acceptable for getting better yield and maximum economic return from the studied parameters.

Evaluation of colemanite as a slow release source of boron fertilizer for potato

Aim: The present study was conducted with an objective to assess the suitability of colemanite (Ca2 B6.O11.5H2O) as a slow release source of boron to potato crop. Methodology: Soil was incubated with boron (1.25 and 2.50 mg kg-1 soil) using borax and colemanite for six weeks. Soil moisture was maintained at 80% field capacity. Soil samples were analyzed weekly for hot-water extractable boron content. Direct and residual effects of borax and colemanite on potato plant growth and boron uptake were studied in pot experiments. Leaf boron concentration was measured by an ICP-OES. Results: In laboratory incubation, although the rate of release of hot water extractable boron from colemanite was slower than borax, it was enough to meet the requirement of potato crop. Application of both the sources of boron increased its content significantly in soil as well as in potato leaves. This study revealed that boron uptake from colemanite was comparable to borax in meeting the boron requirement of potato. Interpretation: Soil incubation and pot experiment studies showed that colemanite is a suitable slow release source of boron fertilizer for potatoes

Addition of micronutrients to npk formulation and initial development of maize plants / Adição de micronutrientes a formulado npk e o desenvolvimento incial de plantas de milho

Micronutrients are essential nutrients for plant growth and development; however, the micronutrient content in soil is often insufficient to ensure maximum productivity, which creates the need for their application through fertilizers. This study compared the availability of zinc, boron, manganese and copper to the soil, their absorption, accumulation and effect in developing maize plants, supplied as granules mixed with NPK granules or as powder, coating NPK granules. The experiment was conducted in a greenhouse, in a randomized block design with four replications, using a soil classified as Oxisol and maize hybrid AG1051. The formulation for fertilizers used was 4-30-10 (N- P2O5 -K2O) with 0.3% zinc, 0.1% boron, 0.2% manganese and 0.2% copper applied at doses of 0, 150, 300, 600, 1200 and 2400 kg ha-1, furthermore, doses of 4-30-10 without micronutrients were applied to ensure variation only for micronutrient doses. Coating NPK granules with micronutrients was better than the mixture for soil Zn content, zinc concentration and accumulation in the shoot and dry mass production. Both fertilizers presented similar behavior for soil B content, B concentration and accumulation in shoots. However, for the greatest dose, B results were better for the mixture of granules. The addition of Mn and Cu to NPK formulation resulted in no response in the soil, although the mixture resulted in greater concentration of Mn in the shoot and coating granules showed greater accumulation of Cu.

Os micronutrientes são essenciais às plantas porém seus teores no solo podem não ser suficientes para altas produtividades, o que gera necessidade de aplicação via fertilizantes. Objetivou-se comparar a disponibilização de zinco, boro, manganês e cobre para o solo, sua absorção, acúmulo e efeito no desenvolvimento de plantas de milho, quando aplicados granulados e em mistura com grânulos NPK ou na forma de pó, revestindo grânulos de NPK. O experimento foi conduzido em casa de vegetação, com delineamento de blocos casualizados, com quatro repetições, com amostras de solo classificado como Latossolo Vermelho distrófico típico e híbrido de milho AG1051. Os fertilizantes utilizados foram de formulação 4-30-10 (N-P2O5-K2O) com 0,3 % de zinco, 0,1 % de boro, 0,2 % de manganês e 0,2 % de cobre aplicados nas doses de 0, 150, 300, 600, 1200 e 2400 kg ha-1. Doses complementares de 4-30-10 sem micronutrientes foram aplicadas para que todos os tratamentos recebessem as mesmas doses de nitrogênio, fósforo e potássio, variando somente as doses dos micronutrientes. O revestimento dos grânulos de NPK com micronutrientes é superior à mistura quando se compara o teor de zinco no solo, a concentração e o acúmulo de zinco na parte aérea e a produção de massa seca das plantas de milho. A mistura de micronutrientes granulados com grânulos de NPK apresenta comportamento semelhante para os teores de boro no solo, sua concentração e acúmulo na parte aérea. A adição de manganês e cobre ao formulado NPK não resultou em resposta no solo, embora a forma de mistura tenha resultado em maior concentração de manganês na parte aérea, e o revestimento de grânulos tenha mostrado maior acúmulo de cobre pelas plantas de milho.

Riesgo ambiental por arsénico y boro en las cuencas hidrográficas Sama y Locumba de Perú / Environmental risk due to arsenic and boron in the watersheds Sama y Locumba from Perú

Se efectuó un estudio para estimar el riesgo ambiental sostenible relativo ante concentraciones totales de arsénico y boro en aguas superficiales de las cuencas hidrográficas Sama y Locumba, en Tacna, Perú, a través de muestreos de tipo no probabilístico por conveniencia en puntos referenciales, durante los meses de agosto y noviembre del 2016, así como abril y junio del 2017. Se obtuvo que los valores de arsénico en los respectivos meses fueron 0,0731; 0,29835; 0,287 y 0,711 mg.L-1, lo que superó el límite máximo permisible (0,01 mg.L-1); este incumplimiento fue similar en cuanto al boro, pues se hallaron concentraciones de 8,681 y 4,148 mg.L-1, pero el valor máximo establecido es de 2,4 mg.L-1. Las concentraciones determinadas por meses revelaron diferencias estadísticamente significativas (pd≤0,05). Se concluyó que las aguas superficiales como recurso natural fueron no sostenibles y representaban un riesgo ambiental y para la salud humana

A study was carried out to estimate the relative sustainable environmental risk with total concentrations of arsenic and boron in superficial waters of the watersheds Sama and Locumba, in Tacna, Peru, through samplings of non probabilistic type by convenience in reference sites, during the months of August and November of 2016, as well as April and June, 2017. It was obtained that the arsenic values in the respective months were 0,0731; 0,29835; 0,287 and 0,711 mg.L-1, which overcame the permissible maximum limit (0,01 mg.L-1); this unfulfillment was similar as for the boron, because concentrations of 8,681 and 4,148 mg.L-1 were found, but the established maximum value is 2,4 mg.L-1. Concentrations determined per months revealed statistically significant differences (pd≤0,05). It was concluded that the superficial waters as natural resource were not sustainable and they represented an environmental risk and for the human health

Extraction and Separation of Boron in Anhydrite and Gypsum Minerals and Its Isotopic Measurement by Thermal Ionization Mass Spectrometry / 分析化学

The anhydrite and gypsum are the main sulfate minerals during evaporation of seawater or lake.They record the information about relative hydrogeology and the composition of mother liquor.Boron is diffluent element, and often occurs in all kinds of evaporites.Presently, the boron isotope has been applied widely in mineral deposits forming, geochemistry and palaeoenvironment.However, there is little research about characteristic of boron isotope in anhydrite and gypsum minerals, because of the low content of boron and micro-solubility in water and hydrochloric acid.This study developed a method of extracting and purifying boron in anhydrite and gypsum by phase transformation and ion-exchange.Firstly, the samples were mixed with ammonium hydrogen carbonate to transform the calcium sulfate to calcium carbonate.And diluted hydrochloric acid (1 mol/L) was added to resolve calcium carbonate.The percent conversion was about 85%in the first stage, and up to complete resolution by repeating this process.Secondly, boron specific ion-exchange resin ( Amberlite IRA 743 ) was used to gather the boron ions fully and further refined the samples with more than 1 μg of boron by anionic and cationic resin mixed by Ion Exchange Ⅱ and Dowex 50 W × 8.Finally, according to the modified method by He, the values of boron isotope were determined by TIMS.The boron content is analytically pure gypsum was 3.501 ± 0.128 μg/g ( n=12 , RSD=3.6%) and the average recovery was 100.47%.Besides, the δ11B value of analytically pure gypsum added with NIST SRM 951 was 17.98‰±0.21‰ (n=3, RSD=1.2%).This method has good repeatability and can meet the requirements of boron isotopic measurement of anhydrite and gypsum.

Determination of Trace ZnⅡ, CdⅡ and PbⅡ Metal Ions Using In-situ Bismuth-modified Boron Doped Diamond Electrode / 分析化学

Bismuth modified boron doped diamond (BDD) film electrode was employed for simultaneous determination of trace ZnⅡ,CdⅡand PbⅡby anodic stripping voltammetry.BiⅢwas simultaneously in-situ deposited on bismuth modified boron doped diamond electrode with ZnⅡ,CdⅡ and PbⅡ by pre-concentration.In the presence of BiⅢ,the sensitivity for determination of ZnⅡ,CdⅡ and PbⅡ was remarkably enhanced.Influence factors such as bismuth concentration,boron doped concentrations of BDD electrode,pH,preconcentration potential were investigated and optimized.Under the optimal conditions,the stripping peak currents increased linearly with the increasing concentration of ZnⅡ,CdⅡ and PbⅡ in the range of 10-300 μg/L.The limit of detection was 0.56 μg/L for ZnⅡ,0.32 μg/L for CdⅡand 0.75 μg/L for PbⅡ (S/N=3),respectively.The interference experiments showed that common ions had little influence on the determination except CuⅡ.In addition,the developed electrode displayed a good repeatability.The method was successfully applied to determination of ZnⅡ,CdⅡ and PbⅡ in real water samples with the standard addition recoveries of 92.0%-114.0%.

Soluble amino acid profile, mineral nutrient and carbohydrate content of maize kernels harvested from plants submitted to ascorbic acid seed priming

ABSTRACT Both the scientific community and society have shown interest in improving the content of amino acids, carbohydrates and mineral nutrients in maize because it represents an important staple food in many developing countries. Earlier studies demonstrated that the treatment of seeds using ascorbic acid (AsA-seed priming) enhanced soluble carbohydrates, proteins and soluble amino acids for other species. AsA seed priming in maize showed the potential for reducing abiotic stresses. The effects on grain quality have not been previously demonstrated. This study investigated the impacts of AsA seed priming on maize kernel quality of seeds produced by the plants generated from the primed seeds, based on the amino acid profile and carbohydrate and mineral nutrient contents. AsA seed priming improved the maize kernel quality with respect to the ascorbate content, boron allocation, total carbohydrate content and increased soluble amino acid levels, including serine, tyrosine, alanine, valine, glutamate, arginine, proline, aspartate, lysine and isoleucine, whereas soluble methionine was decreased. Therefore, AsA seed priming can represent a potential technique for improving maize grain quality.

High exposure to boron in drinking water and sperm parameters in Chilean young people / Exposición elevada a boro en el agua potable y parámetros de esperma en gente joven chilena

Our aim was to describe sperm parameters in residents from Northern Chile. We evaluated in 101 volunteers (18 and 30 years old) urinary and drinking water Boron levels using Inductively Coupled Plasma Mass Spectrometry; semen parameters were measured with standardized methods. Each individual was categorized in 3 levels of exposure: low (B levels in urine 2.94 mgL-1 or tap water 3.0 mgL-1), medium (urinary B between 2.95-7.4 mgL-1 and B in tap water with 3.0-7.0 mgL-1) and high (urinary B > 7.4 mgL-1 or tap water > 7.0 mgL-1). We found no significant differences among groups by pH, sperm concentration (45.1; 48.2 and 38 million/mL), motility 1th hour (38.1; 40.0 and 45.5 %) and vitality 1th hour (88.6; 88.0 and 76.9 %) respectively. Abnormal morphology was significant different (83.3; 90 and 83 %). Young men exposed to B in drinking water present sperm variations associated with the level of exposure. Most of these changes are positive at intermediate levels of B. For the highest exposures were observed negative changes in sperm morphology, concentration, motility and vitality, all relevant parameters of fertility. Beneficial effect is observed at medium exposure, like a "U curve".

El objetivo de este trabajo fue describir los parámetros espermáticos en residentes del norte de Chile. Se evaluaron en 101 voluntarios (18 y 30 años), los niveles urinarios y de agua potable de boro, usando "Inductively Coupled Plasma Mass Spectrometry". Los parámetros del semen se midieron con métodos estandarizados. Cada individuo se clasificó en 3 niveles de exposición: bajo (niveles B en la orina 2,94 mgL-1 o agua potable 3,0 mgL-1), medio (B urinario entre 2,95-7,4 mgL-1 y B en agua de beber con 3,0- 7,0 mgL-1) y alto (B urinario >7,4 mgL-1 o agua potable > 7,0 mgL-1). No se encontraron diferencias significativas entre los grupos por pH, concentración de espermatozoides (45,1; 48,2 y 38 millones/mL), motilidad a 1 hora (38,1; 40,0 y 45,5%) y vitalidad 1 hora (88,6; 88,0 y 76,9%) respectivamente. La morfología anormal fue significativamente diferente (83,3; 90 y 83%). Los hombres jóvenes expuestos a B en el agua potable presentan variaciones espermáticas asociadas con el nivel de exposición. La mayoría de estos cambios son positivos en niveles intermedios de B. Para las exposiciones más altas se observaron cambios negativos en la morfología, concentración, motilidad y vitalidad del esperma, parámetros relevantes de la fertilidad. Un efecto beneficioso se observa en la exposición media, como una "curva U".

Preparation of Silicon and Boron-doped Carbon Dots and Their Application in Hemoglobin Sensing / 分析化学

Heteroatom doping is an effective way to elevate the fluorescent performance of carbon dots. In this study, a microwave one-pot approach for the synthesis of SiBCDs was proposed by using citric acid ( C6 H8 O7 ) , boric acid ( H3 BO3 ) and (3-aminopropyl) triethoxy sliane ( APTES) as source materials. PAAS-SiBCDs were prepared with the assistance of microwave when sodium polyacrylate ( PAAS) was added in the precursor of SiBCDs. The products were characterized by X-ray diffraction ( XRD ) , X-ray photoelectron spectroscopy ( XPS ) and Fourier transform infrared ( FT-IR ) spectra, respectively, confirming that the product was amorphous CDs, with small amount of Si and B. The synthesized SiBCDs had good monodispersity with size of 4-8 nm, the average size of PAAS-SiBCDs was 5. 2 nm, and the excitation/emission maximum was 350 nm/445 nm. The quantum yield of SiBCDs was 20. 1%, and that of PAAS-SiBCDs was 34. 6%. Based on the quenching effect of hemoglobin ( Hb ) on the fluorescence PAAS-SiBCDs, a sensitive Hb detection method was developed. A linear range of 0. 21-5. 22 μmol/L was obtained together with a detection limit of 0. 06 μmol/L. The method was applied in the determination of Hb in human blood samples.

Design and development of fluorescent probe substrates for carboxylesterase 1 using BODIPY as the basic fluorophore / 药学学报

Carboxylesterase 1 (CE1) is an important serine hydrolase in mammals, which involved in the hydrolysis of a variety of compounds (endogenous substrates like cholesterol and xenobiotic compounds like ester-contain drugs and pesticides). This study aimed to design and develop the fluorescent probe substrates for human carboxylesterase 1 (hCE1), on the basis of the structural features of hCE1 preferred substrates. Four carboxylic esters deriving from BODIPY-8-carboxylic acid were designed and synthesized. After then, reaction phenotyping assays and chemical inhibition assays were used to evaluate the selectivity of these four ester derivatives towards hCE1. Our results clearly demonstrated that the substrate specificity of these ester substrates towards hCE1 would be improved with the decrease of the alcohol group on BODIPY-8-carboxylesters, while BODIPY-8-carboxylesters with small alcohol groups including methyl (BCM) and ethyl (BCE) esters could serve as the ideal probe substrates for hCE1. Given that BCM exhibit rapid hydrolytic rate in hCE1, we further investigate the enzymatic kinetics of this fluorescent probe substrate in both human liver microsomes (HLM) and recombinant hCE1, as well as to explore its potential application in high-throughput screening of hCE1 inhibitors by using HLM as enzyme source. The results showed that the kinetic behaviors and the affinity of BCM in HLM is much closed to those in recombinant hCE1, implying that hCE1 played the key roles in BCM hydrolysis in HLM. Furthermore, the inhibition study demonstrated that BCM could be used for rapid screening and characterization of hCE1 inhibitors, by using HLM to replace recombinant hCE1 as enzyme source.