Evaluating the inhibitory potential of Withania somnifera on platelet aggregation and inflammation enzymes: An in vitro and in silico study

Context Withania somnifera (L.) Dunal is traditionally used for treating various ailments, but lacks scientific evaluation.

Objective This study evaluates Withania somnifera (WS) for its effect on platelet activity and inflammatory enzymes.

Materials and methods Aqueous and ethanolic (1:1) leaf extracts were subjected to in vitro indirect haemolytic activity using Naja naja venom, human platelet aggregation was quantified for lipid peroxidation using arachidonic acid (AA) as agonist and 5-lipoxygenase (5-LOX) levels were determined using standard spectrometric assays. Further, molecular docking was performed by the ligand fit method using molegro software package (Molegro ApS, Aarhus, Denmark).

Results The study found that aqueous and ethanol extracts have very negligible effect (15%) with an IC₅₀ value of 13.8?mg/mL on PLA₂ from Naja naja venom. Further, extracts of WS also had very little effect (18%) with an IC₅₀ value of 16.6?mg/mL on malondialdehyde (MDA) formation. However, a 65% inhibition of 5-LOX with an IC₅₀ value of 0.92?mg/mL was observed in 1:1 ethanol extracts. The same was evident from SAR model with the active ingredient withaferin A binding predominantly on Phe 77, Tyr 98, Arg 99, Asp 164, Leu 168, Ser 382, Arg 395, Tyr 396 and Tyr 614 with an atomic contact energy value of??128.96 compared to standard phenidone (?103.61). Thus, the current study validates the application of WS for inflammatory diseases.

Conclusion This study reveals the inhibitory potential of W. somnifera on inflammatory enzymes and platelet aggregation. Thus, WS can serve as a newer, safer and affordable medicine for inflammatory diseases.     

Dietary and herbal supplements use among patients hospitalized in internal medicine departments

ObjectivesTo assess consumption of dietary and herbal supplements (DHS) among patients in internal medicine departments and determine whether such use is documented in their medical files.Methods267 patients from three internal medicine departments of an academic medical center in Haifa, Israel were assessed prospectively with questionnaires about their DHS use in the month preceding hospitalization. DHS were categorized into vitamins & minerals, herbal supplements and others. Further data was then collected from patients' medical records on socio-demographic and medical characteristics, as well as documentation of DHS use.Results123 patients (50.6 %) used DHS on a daily basis. Most of them (53.7 %) were using more than one DHS. DHS use was more prevalent in older (OR = 1.02 [1.001–1.036], p = 0.034) and educated (OR = 0.482 [0.252-0.923], p = 0.028) patients. Vitamins & minerals were used mainly to enhance vitality and address laboratory abnormalities, whereas herbal supplements were used mainly for gastrointestinal problems (p < 0.001). DHS use was reported to the physicians by 42 % of the patients, mostly at the patients’ initiative [92 (82.1 %), p < 0.001)]. Vitamins and minerals were the most reported category of DHS (94 (57.3 %), p < 0.001). The use of DHS was reported to physicians for 112 DHS (41.8 %) but only 32 DHS (11.9 %) were documented in their medical files. The documentation of vitamins and minerals was significantly higher compared to herbal supplements documentation (29 (17.7 %) & 3 (2.9 %) respectively, P < 0.001).ConclusionsDHS are commonly used by patients hospitalized in the internal medicine departments. Many patients do not report such use to the physicians, and more strikingly, physicians do not document DHS use in patient medical files. This communication gap may have serious medico-legal ramifications due to DHS side effects and DHS interactions with other DHS and with conventional drugs.     

经食管实时三维超声心动图评价房性心律失常对二尖瓣结构和功能的影响

目的:应用经食管实时三维超声心动图(RT-3D-TEE)技术,探讨房性心律失常对二尖瓣结构和功能的影响.方法:选取2018年6月~2019年6月本院收治的房性心律失常拟行射频消融的患者49例纳入观察组,另外选取21例正常窦性心律者作为对照组,所有患者均行经胸超声心电图(TTE)和经食管实时三维超声心动图(RT-3D-TEE)检查,将两组患者的瓣环投影面积(A2D)、瓣环周长(C3D)、瓣环高度(H)、瓣环前后径(DAP)、瓣环前外侧至后内侧直径(DAIPm)、左室射血分数(LVEF)、左心房前后径(Lad)等参数进行比较,并分别计算对合面积和对合指数,之后采取二项Logistic回归分析或逐步线性回归对各参数及临床因素与对合指数的相关性进行分析.结果:两组患者在LVEF和对合面积方面的比较无明显差异(P>0.05),在A2D、C3D、H、DA、PDAIPm、Lad方面的比较,房性心律失常组患者明显高于正常窦性心律组患者(P<0.05),且观察组患者的对合指数明显降低(P<0.05).将49例观察组患者以不同心律失常类型分为持续性房颤、阵发性房颤、房扑、混合型房性心律失常4个亚组,采用单因素方差分析,发现在LVEF、C3D、Lad、对合指数方面的比较,各亚组间无明显差异(P>0.05).采用二项Logistic回归分析发现,女性是导致对合指数低的危险因素,另外对合指数较低、房性心律失常是导致二尖瓣返流的重要因素.结论:房性心律失常对患者二尖瓣的A2D、C3D、H、DA、PDAIPm、Lad等都会造成较大影响,从而降低对合指数,影响二尖瓣的正常功能,导致二尖瓣返流的发生.     

行为-结构化-关系干预模式对短期住院孤独症谱系障碍儿童的疗效分析

目的 探讨以行为-结构化-关系(BSR)干预模式对短期住院孤独症谱系障碍(ASD)儿童的干预疗效,为改善ASD儿童的预后提供参考依据。方法 选取2015年12月－2016年12月确诊为ASD的2~6岁儿童141例,随机分为治疗组和对照组。治疗组ASD儿童均接受BSR模式的短期课程训练,训练课程包括个别辅导、游戏课、运动课、音乐课等,每天训练时间6 h,持续1个月;对照组ASD儿童处于干预等待,接受随访观察和评估。所有ASD儿童干预前、后均接受儿童心理教育评估(第三版)(PEP-3)来进行各方面能力变化的评估。结果 治疗组、对照组干预前各副测验的原积分差异无统计学意义(P>0.05)。两组ASD儿童干预后认知、语言理解、模仿、情感表达、社会互动、行为特征-非语言、适应行为的原积分比较,差异均有统计学意义(t=2.41、2.02、4.14、3.69、4.42、2.69、2.96,P<0.05);但小肌肉、大肌肉、自理的原积分比较,差异无统计学意义(t=-1.13、-1.05、-0.84,P>0.05)。结论 BSR干预模式能够有效改善短期住院ASD儿童的预后,可推广用于儿童ASD的治疗。     

Chalcone hybrids and their antimalarial activity

Malaria, one of the most striking, re-emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug-resistant malaria, creating an urgent need to develop novel antimalarial agents. Chalcone derivatives are ubiquitous in nature and have become indispensable units in medicinal chemistry applications due to their diverse biological profiles. Many chalcone derivatives demonstrate potential in vitro and in vivo antimalarial activity, so chalcone could be a useful template for the development of novel antimalarial agents. This review covers the recent development of chalcone hybrids as antimalarial agents. The critical aspects of the design and structure–activity relationship of these compounds are also discussed.     

Children's diets,pesticide uptake,and implications for risk assessment: An Israeli case study

The presence of pesticides in the Israeli food supply is well documented but little is known about the risks posed by children's diets for potential exposures. We investigated potential exposures to food-borne pesticides in a sample of 301 urban Israeli children (2008–10). Data from a food frequency questionnaire, 24 hour food recall, and Israel's national pesticide monitoring program were used to estimate uptake factors for 26 compounds in 27 fruits and vegetables. A pilot risk assessment was performed and the findings were compared with the Israel Ministry of Health's 2012 pesticide risk assessment for the general population. The surveyed children had higher potential exposures than the general population for over one third of the compounds, and uptake factors exceeded the Acceptable Daily Intake in ten compounds. Methamidophos, exceeded the ADI at the 25th percentile and fenamiphos, iprodione, and oxydemethon methyl, exceeded the ADI at the 50 percentile. ADIs for several compounds were exceeded even though the residues detected were below the statutory limit. Improved monitoring, enforcement, and revision of the Maximum Residue Limit for certain food/pesticide pairs are indicated as is the need to incorporate data on children's actual food consumption in national risk assessments.     

Glutathione S-transferase in the midgut tissue of gypsy moth (Lymantria dispar) caterpillars exposed to dietary cadmium

Activity of glutathione S-transferase (GST) in midgut of gypsy moth caterpillars exposed to 10 and 30 μg Cd/g dry food was examined. Based on the enzyme reaction through conjugation with glutathione, overall activity remained unaltered after acute and chronic treatment. No-observed-effect-concentration (10 μg Cd/g dry food) significantly increased activity only after 3-day recovery following cadmium administration. Almost all comparisons of the indices of phenotypic plasticity revealed statistically significant differences. Despite the facts that GST has important role in xenobiotic biotransformation, our results indicate that this enzyme in insect midgut does not represent the key factor in cadmium detoxification.