Growth Inhibition Effect of DL-Lysine Acetylalicylate on sw480 Colon Carcinoma Cells

Objective： To investigate the effect of DL-lysine acetylsalicylate on proliferation of colon carcinoma cells line sw480. Methods： After treatment of DL-lysine acetylsalicylate, the study was performed by observing sw480 colorectal cancer cells with phase contrast microscope, making growth curve, and examining the inhibition rate of sw480 cells with MTT assay. Results： The morphology of sw480 cells showed characteristics of apoptosis, the cell growth curve showed inhibited proliferation of sw480 cells when treated with DL-lysine acetylsalicylate （P〈0.05）. The rate of inhibition was upward when the drug concentration increased. Conclusion： DL-lysine acetylsalicylate for injection can inhibit the growth of sw480 colorectal cancer cells obviously in a dose dependent manner.

Psychotropic effects of aspirin, acetylsalicylate cobalt and acetylsalicylate zinc at various doses

For the first time it is shown that psychotropic action of acetylsalicylates at various doses is manifested as a nonmonotonic dependence having its peaks at therapeutic and ultra-low dose zones. It is discovered that development of effects of aspirin resembles that of acetylsalicylate zinc. Acetylsalicylate cobalt at extremely low doses zone showed the highest antidepressant activity, demonstrating toxicity at high doses. Generally, it is revealed that the use of aspirin and its salts at high doses range causes maximum psychotropic effects development, usually accompanied by side-effects. Therefore, aspirin, acetylsalicylate cobalt and zinc at extremely low doses are recommended for further study as psychotropic medications.

Stability Studies of Lysine Acetylsalicylate(Aspirin Derivative):Mechanisms of Hydrolysis

To control the stability of the lysine acetylsalicylate compound (LAS) in aqueous solution, some studies of the hydronium ion-catalyzed, hydroxide ion-catalyzed, and spontaneous reactions of this active ingredient in water solutions have been carried out. The pH-rate profile (log kobs = f(pH)), shows that the hydrolysis reaction of the LAS, is conducted by a catalysis acid-base mechanism, with multiple reaction pathways. The rate constants, kH, kOH and k0 to the reaction pathways catalyzed by H3O+, HO– ions and to the spontaneous reaction, for the hydrolysis reaction of the reagent LAS, were determined. The results show that the studied compound LAS is unstable in basic medium and the hydrolysis reaction catalyzed by HO– ions is predominant.For a known acidity (pH ≈ 10), studies conducted for different temperatures of the medium, clearly indicate, that the experimental rate constant kobs,depends on the temperature according to the Arrhenius equation. The activation parameters: activation energy (Ea), enthalpy (ΔH≠) and entropy (ΔS≠), for the transition state were determined, The very negative value obtained for the activation parameter ΔS*, first indicates that in the transition state there is gain in order, then this late state, resembles the products and that probably for the mechanism of the LAS hydrolysis reaction catalyzed by HO– ions, the rate-determining step is a bimolecular reaction. Finally from all these results, the mechanism for the reaction pathway catalyzed by HO– ions has been elucidated.

Analgesic Effects of Tetrodotoxin Combined with Acetylsalicylic Acid on Acetic Acid-induced Abdominal Constriction and Formalin Test in Mice

Aim To study the effects of tetrodotoxin （TTX） combined with acetylsalicylic acid （ASA） on nociceptive stimulus in mice. Methods To assess the antinociceptive effects of TTX, ASA or TTX plus ASA, the acetic acid-induced abdominal constriction test and formalin pain test were used. Results TTX （0.5 - 4.0 μg· kg^-1 ） or ASA （25 - 200 mg· kg^-1 ） im produced a significant inhibition of acetic acid-induced abdominal constriction. The median inhibitory doses （ID508） were 2.1 μg· kg^-1 for TTX（ and 64 mg· kg^-1 for ASA. TTX and ASA also showed a dose-dependent inhibition of the second phase response in the formalin pain model, the ID508, being 2.3μg·kg^-1 and 74.2 mg· kg^-1, respectively. The ihteraction between TTX and ASA was synergistic, as evidenced by the fact that （1） when ASA alone compared with the combination of TTX （0.79 μg · kg^-1 or 0.39μg· kg^-1 ） and ASA, the ID508, of ASA reduced from 64.0 mg· kg^-1 to 5.8 mg· kg^-1 or 12.6 mg· kg^-1, and from 74.2 mg· kg^-1 to 7.4 mg· kg^-1 or 13.0 mg· kg^-1 on tile two models of nociceptive tests, respectively; and that （2） synergism in the analgesic effects was shown by isobiolographic analysis. Conclusion TTX, ASA and the combination of the two drags produce analgesic effects in acetic acid-induced abdominal constriction test and formalin-induced pain test. The interactions between TTX and ASA may be useful in developing novel analgesic agents.

Effects of Acetylsalicylic Acid and Calcium Chloride on Photosynthetic Apparatus and Reactive Oxygen-Scavenging Enzymes in Chrysanthemum Under Low Temperature Stress with Low Light

The effects of acetylsalicylic acid （ASA）, CaCl2, and ASA ＋ CaCl2 on the photosynthetic apparatus and antioxidant enzyme activities were investigated in chrysanthemum Jinba （a cut flower cultivar） under low temperature stress with low light （TL stress） （16/12℃, day/night, PFD 100 μmol m^-2 s-1）. The results showed that under TL stress, the net photosynthesis rate （Pn）, carboxylation efficiency （CE）, apparent quantum yield （AQY）, maximal photochemical efficiency （Fv/Fm） of PSII, quantum yield of PSII electron transport （ФPSII）, and photochemical quenching （qP） of the chrysanthemum leaves in all treatments were significantly decreased, but the decreases were alleviated by ASA, CaCl2, and ASA ＋ CaCl2 treatments compared with the controls. The alleviating effect of ASA ＋ CaCI2 was better than either ASA or CaCl2 single treatment. Moreover, the ASA ＋ CaCl2 treatment highly improved the chlorophyll content, relatively improved the number and size of chloroplast and starch grain in the leaves of chrysanthemum plants compared with ASA and CaCl2 treatments. It was indicated that ASA and/or CaCI2 could regulate the photosynthetic functions in the leaves of chrysanthemum plants to enhance the resistance against TL stress. On the other hand, reduction in relative conductance rate implied that ASA and/ or CaCl2 could protect from membrane injury in leaves of chrysanthemum plants. The activities of SOD, POD, and CAT in the treated leaves of chrysanthemum were increased as compared with the controls. It was suggested that ASA and/or CaCl2 had positive regulation effects on the defence enzyme activities in chrysanthemum leaves which could protect the photosynthetic apparatus to a certain degree under the TL stress. In brief, the treatment of ASA together with CaCl2 was better for chrysanthemum plants to adapt TL stress than single ASA or CaCl2 treatments.

Acetylsalicylic acid supplementation improves protein utilization efficiency while vitamin E supplementation reduces markers of the inflammatory response in weaned pigs challenged with enterotoxigenic E.coli

Background： This experiment was conducted to test the hypothesis that vitamin E（Vit E） and acetylsalicylic acid（ASA）, a cyclooxygenase-2（COX-2） inhibitor, will additively reduce the production of the immunosuppressive molecule prostaglandin E_2（PGE_2） and hence reduce inflammatory responses in weaner pigs experimentally infected with an enterotoxigenic strain of E. coli.Methods： The experiment was conducted in a research facility with 192 individually-housed male weaner pigs（Landrace × Large White） weighing 6.6 ± 0.04 kg（mean ± SEM）. The pigs were experimentally infected with an enterotoxigenic strain of E. coli and were allocated to a 2 × 3 factorial design with the respective factors being without and with 125 ppm ASA and three levels of Vit E supplementation（50, 100 or 200 IU/kg diet, dl-α-tocopheryl acetate）.Results： Acetylsalicylic acid supplementation improved average daily gain（P 〈 0.05） and tended to improve feed：gain ratio（P 〈 0.10） during the first 14 d after weaning. Acetylsalicylic acid supplementation also improved（P 〈 0.001） amino acid utilization efficiency（as assessed by plasma urea level） and tended to decrease（P 〈 0.10） PGE2 production in the liver without affecting smal intestinal histology and tight junction protein mR NA expression in the jejunal epithelium. Vitamin E supplementation greater than 100 IU/kg diet sustained both the plasma Vit E concentration（P 〈 0.001） and plasma haptoglobin content（P 〈 0.001） after weaning. However, there was no additive effects of the combined supplementation of ASA and Vit E on performance, intestinal barrier function and inflammatory responses of weaned pigs.Conclusions： Although ASA and vitamin E improved amino acid utilization efficiency and reduced acute inflammatory responses, ASA and vitamin E did not additively reduce production of PGE2 and inflammatory responses in weaner pigs experimental y infected with an enterotoxigenic strain of E. coli.

Effect of graded doses of acetylsalicylic acid on sperm chromatin integrity and maturity of germinal epithelium in adult male mouse

Objective:To evaluate the effect of graded doses of acetylsalicylic acid (ASA) on sperm chromatin integrity and sex hormones in the adult male mouse.Methods:Forty-nine male adult mice were divided into seven groups. Control group received no drug, sham group received ASA solvent (dimethylsulfoxide 0.1%), groups 3 to 7 received different doses of 0.05, 0.10, 0.50, 1.00 and 5.00 mg ASA, daily for 14 d, respectively. On day 15, evaluations were made by sperm chromatin dispersion test for the study of DNA sperm integrity, radioimmunoassay for the study of testosterone and luteinizing hormone (LH) level and histopathology of testis for Jhonson's scoring.Results: ASA in groups 0.50, 1.00 and 5.00 mg reduced big halo sperms. DNA fragmentation significantly increased just in 5 mg group. Serum level of testosterone in doses of 0.50, 1.00 and 5.00 mg groups reduced significantly (P<0.01) while LH level was not affected. Johnson's score reduced in all ASA treated groups.Conclusions: Administration of ASA over the 14 days in dose of 5.00 mg increases sperm DNA fragmentation index and therefore reduces DNA integrity and in doses of 0.50, 1.00, 5.00 mg reduces serum testosterone level with no effect on LH. Generally, ASA has deleterious effects on the male reproductive indices even in low doses.

Acetylsalicylic Acid Administered in Patients with Type 2 Diabetes Mellitus and Its Effect on the Antioxidant Enzyme System

Type 2 diabetes mellitus and its complications are associated with oxidative stress and the depletion of antioxidant defenses. The influence of acetylsalicylic acid on reversing the decrease in antioxidants, insulin resistance, glucose homeostasis, and inflammatory cascade can help prevent diabetes complications. Purpose: The aim of the study was to evaluate the effect of acetylsalicylic acid on the antioxidant enzymatic system in patients with diabetes. Methods: A randomized, double-blind, placebo-controlled clinical trial was carried out in 21 patients of both sexes with Type 2 diabetes for less than five years at the time of diagnosis, without pharmacological treatment, and randomly selected. Acetylsalicylic acid (300 mg) was administered orally for three months to the study group (n = 11) compared to the placebo control group (n = 10). Before and after the intervention, anthropometric and metabolic measurements were taken, fasting plasma glucose, glycated hemoglobin A1c, lipid profile panel, glutathione peroxidase, superoxide dismutase, catalase, and antioxidant capacity/activity were determined;values are presented as mean ± standard deviation. Intra- and intergroup differences were tested by Wilcoxon signed rank and Mann-Whitney U test, respectively;p-value ≤ 0.05 was considered statistically significant. Results: The acetylsalicylic acid group showed a decrease in weight (85.6 ± 19.3 vs. 84.1 ± 19.0 kg p = 0.01), cholesterol (205.9 ± 16.6 vs. 186.0 ± 23.2 mg/dL p = 0.02), and glycated hemoglobin A1c (7.8% ± 0.9% vs. 7.0% ± 0.7% p = 0.02). The placebo group exhibited reduction in weight (76.1 ± 14.9 vs. 74.9 ± 15.0 kg p = 0.04), glycated hemoglobin A1c (6.9% ± 0.6% vs. 6.2% ± 0.4% p = 0.004), and total antioxidant capacity (4.1 ± 0.5 vs. 4.8 ± 0.3 mmol/L p = 0.002). Conclusion: The administration of acetylsalicylic acid did not modify the antioxidant enzyme system.

Acetylsalicylic acid for metal stent in malignant distal common bile duct obstruction:A randomized controlled trial

Background:Endoscopic biliary drainage is the treatment of choice for patients with malignant distal common bile duct obstruction.Self-expandable metal stents have clinical advantages including an increased duration of patency that may be prolonged by acetylsalicylic acid(ASA)use.The aim of this study was to investigate whether ASA had a positive effect on the patency of self-expandable metal stents compared with placebo.Methods:This prospective,multicenter,double-blinded,and randomized placebo-controlled trial was conducted from October 2017 to May 2020 in Korea.Patients who underwent palliative endoscopic biliary drainage with self-expandable metal stents for malignant distal bile duct obstruction were enrolled,and allocated to ASA treatment or placebo.The study outcomes were the rate of stent dysfunction at 6 months,duration of stent patency,risk factors for stent dysfunction,and any adverse events.Results:Interim analysis included 24 and 28 patients in the ASA and placebo groups,respectively.There was no significant difference between the ASA and placebo groups in stent dysfunction(25.0%vs.20.7%,P=0.761)or the duration of stent patency(150.97±10.55 vs.158.07±8.70 days,P=0.497).Six patients experienced suspected ASA-related adverse events,and there was one lethal case.Conclusions:ASA did not prolong stent patency.This study was terminated early because of the possibility of serious adverse events related to ASA treatment of these patients receiving palliative care.

Banana Peel for Acetylsalicylic Acid Retention

A method for adsorption involving banana peel (BP) was studied to remove the pollutant acetylsalicylic acid (ASA) in aqueous medium. The results show that bioadsorbent has satisfactory maximum adsorption capacity (2.29 mg/g) for removing this analgesic and anti-inflammatory drug in aqueous solution (pH 7.0) using the Langmuir mathematical model. The tested concentrations of this pollutant were higher than the levels commonly found in the aquatic environment. This and other results suggest the BP as an alternative to ASA removal in water contaminated with pharmaceuticals pollutants.

Using o-Acetylsalicylic Acid Grafted by 3-Aminopropyl Triethoxysilane to Assemble Strong Covalently Bonded Luminescent Terbium Hybrids

The modification of o-acetylsalicylic acid by 3-aminopropyl triethoxysilane (APS) was achieved and the assembly of their corresponding organic-inorganic molecular-based hybrid material with the two moieties bridged by covalent bonds was obtained. It is utilized to coordinate to terbium ions and further happened hydrolysis and polycondensation processes by chemical active triethoxysilyl groups. The photophysical properties show that the triplet energy of modified o-acetylsalicylic acid is efficiently responsible for the antenna effect and matches with the emissive energy level of metal ions. Consequently, the intramolecular energy transfer process completed within these molecular-based hybrids and strong green emission of Tb 3+ was achieved.

Acetylsalicylic acid interferes with embryonic kidney growth and development by a prostaglandin-independent mechanism

AIM To evaluate the effects of the non-selective, non-steroidal anti-infammatory drug （NSAID） acetylsalicylic acid （ASA）, on ex vivo embryonic kidney growth and development.METHODS Pairs of fetal mouse kidneys at embryonic day 12.5 were cultured ex vivo in increasing concentrations of ASA （0.04-0.4 mg/mL） for up to 7 d. One organ from each pair was grown in control media and was used as the internal control for the experimental contralateral organ. In some experiments, organs were treated with ASA for 48 h and then transferred either to control media alone or control media containing 10 μmol/L prostaglandin E2 （PGE2） for a further 5 d. Fetal kidneys were additionally obtained from prostaglandin synthase 2 homozygous null or heterozygous （PTGS2-/- and PTGS2-/＋） embryos and grown in culture. Kidney cross-sectional area was used to determine treatment effects on kidney growth. Whole-mount labelling to fluorescently detect laminin enabled crude determination of epithelial branching using confocal microscopy.RESULTSIncreasing ASA concentration （0.1, 0.2 and 0.4 mg/mL） significantly inhibited metanephric growth （P 〈 0.05）. After 7 d of culture, exposure to 0.2 mg/mL and 0.4 mg/mL reduced organ size to 53% and 23% of control organ size respectively （ P 〈 0.01）. Addition of 10 μmol/L PGE2 to culture media after exposure to 0.2 mg/mL ASA for 48 h resulted in a return of growth area to control levels. Application of control media alone after cessation of ASA exposure showed no benefit on kidney growth. Despite the apparent recovery of growth area with 10 μmol/L PGE2, no obvious renal tubular structures were formed. The number of epithelial tips generated after 48 h exposure to ASA was reduced by 40% （0.2 mg/mL; P 〈 0.05） and 47% （0.4 mg/mL; P 〈 0.01）. Finally, growth of PTGS2-/- and PTGS2＋/- kidneys in organ culture showed no differences, indicating that PTGS2 derived PGE2 may at best have a minor role.CONCLUSIONASA reduces early renal growth and development but the role of prostaglandins in this may be minor.

Trend Analysis of Combined Drugs Creation （for Example Acetylsalicylic Acid）

The pharmaceutical market of Ukraine in January 2015 was registered 71 drug based acetylsalicylic acid （ASA）, for which 52% combined. The most common combinations of ASA with acetaminophen and caffeine （45.9%）, magnesium hydroxide （18.9%）, bisoprolol （10.8%）, ascorbic acid （8.1%）, clopidogrel （5.4%）. Comparing markets combined drugs ASA of Ukraine, the Russian Federation, 28 EU countries, Norway, Switzerland, India, Syria, Australia and the USA identified the active pharmaceutical ingredients, combined with ASA in a single dosage form. The analysis of questionnaires 40 pharmacists pharmacies Temopil, Khmelnytsky and Kyiv regions of Ukraine noted that the biggest demand is mono-drugs ASA, Citramon, Askofen and Cardiomagnyl Methods of pharmacoeconomic studies proved efficient use Upsaryn UPSA with vitamin C tabl. spike, tuba in box number 20 BMS （France）, Citramon tablets number 6 PJSC ＂Monfarm＂ （Ukraine） and Cardiomagnyl tabl. film-coated shell 75 mg in bottle number 100 Nycomed Austria （Austria）. On the basis of six State Forms of drugs in Ukraine （2009-2014） was found that the combination of drugs based on ASA is recommended to use of ascorbic acid （Aspiryn C, Asprovit C, Upsarin UPSA with vitamin C）, dipyridamole （Agrenox）, magnesium hydroxide （Cardiomagnyl, Cardiomagnyl Forte）. Some of the standard combination of ASA （combination of paracetamol and caffeine） are not in form. For optimize State Form of drugs by improving health system in Ukraine can be useful pharmacoeconomic analysis of combination therapies with the current official system to note the combination of ASA with statins, esomeprazole, isosorbide.

比较教学法在仪器分析实验教学中的应用

仪器分析实验是医学预防及医学检验等专业的重要实验课程之一。为提升本科生的创新实践能力,设计了分别利用高效液相色谱仪(HPLC)和超高效合相色谱仪(UPC2)测定复方阿司匹林片中乙酰水杨酸和咖啡因含量的实验,并将思政元素有机地融入其中。教学实践表明,通过对不同仪器原理、功能特点的比较学习,可以激发学生的实验兴趣和探索精神,增强学生解决问题的能力,进而提升学生的科学素养。

阿司匹林肠溶片在健康成年受试者中的生物等效性

目的评价阿司匹林肠溶片在中国健康成年受试者中的生物等效性及安全性。方法采用单中心、随机、开放、两制剂、两顺序、四周期、完全重复试验设计。受试者每周期空腹或餐后单次口服1片受试制剂(test preparation,T)或参比制剂(reference preparation,R)。采用LC-MS/MS法测定不同时间点血浆中乙酰水杨酸(acetylsalicylic acid,ASA)的血药浓度,并进行两制剂的生物等效性及安全性评价。结果餐后试验组口服T和R后ASA的主要药代动力学参数为:C max分别为(690.97±196.91)ng·ml^(-1)和(669.28±337.40)ng·ml^(-1),AUC 0-t分别为(867.37±228.64)ng·h·ml^(-1)和(821.16±349.85)ng·h·ml^(-1),AUC 0-∞分别为(883.48±233.72)ng·h·ml^(-1)和(923.59±287.95)ng·h·ml^(-1);T max分别为(8.98±2.47)h和(10.69±3.75)h。经对数转换后C max、AUC 0-t和AUC 0-∞的几何均值比均在80.00%~125.00%范围之内,两制剂生物等效。空腹试验组口服T和R后ASA的主要药代动力学参数:C max分别为(466.83±222.89)ng·ml^(-1)和(441.42±211.99)ng·ml^(-1),AUC 0-t分别为(753.24±269.49)ng·h·ml^(-1)和(678.50±278.85)ng·h·ml^(-1),AUC 0-∞分别为(809.11±309.27)ng·h·ml^(-1)和(726.51±267.00)ng·h·ml^(-1);T max分别为(5.81±2.53)h和(6.41±2.47)h。经对数转换后C max、AUC 0-t和AUC 0-∞的几何均值比不在80.00%~125.00%范围之内,两制剂生物不等效。试验过程中,空腹组无不良事件发生,餐后组共报告2例次不良事件,均无严重不良事件。结论两种阿司匹林肠溶片在餐后条件下人体内生物等效,空腹条件下人体内生物不等效,制剂安全。

基于科研素养和创新能力培养的有机化学实验教学改革与探索

为培养学生的科研素养和创新能力,我们在乙酰水杨酸的合成实验教学中,将常规实验教学和开放实验教学相融合,构建了以常规实验基本技能训练为基础,以开放性实验综合素质培养为目的实验教学模式,并对教学效果进行评价。教学实践表明,该模式的实施在强化学生的实验技能,激发学生对科研的兴趣,加强对学生科研素养和创新能力的培养等方面收到较好的效果。

赖氨匹林对血小板聚集粘附和血栓形成的影响

赖氨匹林（ＬＡＳ）体内给药９０．４ｍｇ·ｋｇ－１（相当于乙酸水杨酸５０ｍｇ·ｋｇ－１）可明显抑制凝血酶和胶原诱导的大鼠血小板聚集，并呈剂量依赖性地抑制ＡＤＰ诱导的血小板聚集。ＬＡＳ９０．４ｍｇ·ｋｇ－１可降低大鼠血小板粘附率，呈剂量依赖性地减轻实验性血栓的重量，同时ＬＡＳ７０ｍｇ·ｋｇ－１可明显延长小鼠尾动脉出血时间。上述结果提示：抑制血小板聚集和降低血小板的粘附性是ＬＡＳ抗血栓和延长小鼠尾动脉出血时间的机制之一。

膨润土负载型固体酸的制备、表征及催化乙酰水杨酸合成反应

用无水浸渍法制备了膨润土负载型固体酸催化剂,以乙酰水杨酸合成反应为探针考察了制备及反应条件对催化性能的影响,通过XRD、DTA及离子酸度等分析测试技术对催化剂进行表征分析。结果表明,当用体积分数10%HCl浸泡12 h以上,负载5.0 mmol/g ZnCl2或4.0 mmol/g CuCl2,550℃下焙烧活化3 h,制备固体酸及固体酸用量为水杨酸的5%,水杨酸和乙酸酐投料摩尔比为1∶2,反应温度为80～90℃,反应时间为1 h,产率可达96.6%。制备的固体酸催化剂可替代浓硫酸并能重复使用。

乙酰水杨酸－聚天冬酰胺棒状药物体外释放的研究

以乙酰水杨酸为模型药物，将药物以共价键键合于聚天冬酰胺高分子母体，制成棒伏。体外释放在Ｔｒｉｓ－ＨＣｌ（ＰＨ７．４）缓冲溶液介质中，温度为３７±０．１℃时，其释放初期的释药量为其膜剂的近１／３０，能较好地控制释药初期的“爆释”现象。

水杨酸、乙酰水杨酸对番茄幼苗叶片中PPO和POD的诱导作用

以番茄品种改良美国908和合作906为试验材料,研究了水杨酸(SA)和乙酰水杨酸(ASA)喷雾处理6-7叶期幼苗后,叶片内多酚氧化酶(PPO)和过氧化物酶(POD)活性在120 h内的变化.结果显示:SA和ASA对2个番茄品种的适宜诱导浓度分别为1 mmol/L和1.39 mmol/L;SA和ASA对PPO活性的诱导效果无显著差异,但对POD活性的诱导效果SA极显著强于ASA;合作906的PPO活性增幅显著大于改良美国908,而POD活性增幅却显著小于改良美国908,且合作906对诱导处理反应更敏感.研究表明,SA和ASA能显著提高番茄幼苗叶片的PPO、POD活性,而酶活性变化在品种和诱导剂间有显著差异.