Synthesis and evaluation for anti-HCoV-OC43 activity of novel aloperine derivatives with different core structures / 药学学报

In this study, we designed and synthesized 12 novel aloperine derivatives with different core structures. Among them, compound 3 with a ten-membered ring core was obtained through a special ring expansion reaction after γ-H Huffman elimination of quaternary ammonium salt, and the structure was verified by X-single crystal diffraction. Furthermore, their antiviral activity against human β-coronavirus HCoV-OC43 was evaluated by CCK-8 assay. Quaternary ammonium salt 2a and 3 had a good inhibitory effect against HCoV-OC43, and 2a had the highest anti-HCoV-OC43 activity with an EC50 values of 3.77 μmol·L-1 and a SI value of over 53.1. Schrӧdinger molecular docking results showed that both 2a and 3 might display their anti-HCoV-OC43 activity by directly acting on host TMPRSS2 and SR-B1. The results expanded the structural types of endocyclic aloperine and the function against coronavirus, and provided useful scientific data for the development of pharmaceutical applications of these compounds.

Glyphosate-resistant soybeans yield in function of glyphosate salts, doses and stadium phenological / Produtuvidade de cultivares de soja em função dos sais de glyphosate, doses e épocas de aplicação

Given the importance of soybean to the global economy and as a food source, improving crop management techniques is integral to obtaining higher yields. As such, this study aimed to assess the yield of soybean cultivars as a function of different glyphosate salt formulations, doses and application times. Two field experiments were conducted simultaneously using a randomized block design and 3x4x2 factorial scheme, with three repetitions. Factor A consisted of three glyphosate formulations: isopropylamine salt (Roundup Original®), ammonium salt (Roundup WG®), and potassium salt (Zapp Qi®), factor B four application times: 0, 14, 28, 42 days after planting (DAP), and factor C two doses: the recommended dose of 720 grams of acid equivalent per hectare and twice that (1440 grams of acid equivalent per hectare). There was no difference between the glyphosate salts for the BMX Ativa RR® cultivar, but yields of BMX Apolo RR® submitted to ammonium salt were 28% higher than those recorded for the other salts studied. Glyphosate potassium salt resulted in lower soybean yields. Potassium salt application between 14 and 28 DAP caused greater toxicity in both the soybean cultivars analyzed.

Diante da importância da cultura da soja tanto na economia mundial quanto para a alimentação, a melhoria das técnicas de cultivo torna-se um ponto fundamental na obtenção de maiores produtividades. Desta forma o objetivo do trabalho foi avaliar a produtividade de cultivares de soja sob a influência da aplicação de diferentes sais de glyphosate, doses e épocas de aplicação. Dois experimentos de campo foram realizados simultaneamente em delineamento de blocos casualizados com arranjo trifatorial (3x4x2) com três repetições. O fator A consistiu de três formulações de glyphosate: sal de isopropilamina (Roundup Original®), sal de amônio (Roundup WG®), sal de potássio (Zapp Qi®). O fator B consistiu de quatro épocas de aplicação: 0, 14, 28, 42 dias após a semeadura (DAS). O fator C consistiu em duas doses: a dose recomendada de 720 gramas de equivalente ácido por hectare e duas vezes a dose recomendada com 1440 gramas de equivalente ácido por hectare. Para a cultivar BMX Ativa RR® não se observou diferença quanto aos sais, porém a cultivar BMX Apolo RR® submetida a aplicação de sal de amônio demostrou uma produtividade 28% superior em relação aos demais sais. O glyphosate na formulação sal de potássio apresentou redução da produtividade da cultura da soja. Aplicações de glyphosate na formulação sal de potássio realizadas entre os 14 e 28 dias após a semeadura causam maior toxidez em ambas cultivares de soja utilizadas.

Antibacterial dental adhesive containing nanoantibacterial inorganic fillers / 华西口腔医学杂志

OBJECTIVE@#This investigation aimed to develop a novel antibacterial dental adhesive containing nanoantibacterial inorganic fillers and measure the dentin bonding strength, mechanical properties, and antibacterial property of the novel adhesive in vitro.@*METHODS@#Novel nanoantibacterial inorganic fillers containing quaternary ammonium salt with long chain alkyl were synthesized on the basis of previous research. These novel nanoantibacterial inorganic fillers were added into the dental adhesive to prepare novel nanoantibacterial dental resin composite at mass fractions of 0%, 2.5%, 5.0%, 7.5%, and 10%; 0% was used as control. Dentin shear bonding test was used to evaluate the bonding strength. Flexural test was utilized to measure the novel resin composite flexural strength and elastic modulus. A dental plaque microcosm biofilm model with human saliva as inoculum was formed. Colony forming unit, lactic acid production, and live/dead assay of the biofilm on novel dental adhesive were calculated to assess the effect of novel dental adhesive on human dental plaque microcosm biofilm.@*RESULTS@#The dentin shear bond strength, flexural strength, and elastic modulus were 28.9 MPa, 86.6 MPa, and 4.2 GPa, respectively, when the nanoantibacterial inorganic filler mass fraction in the dental adhesive reached approximately 5.0%. Consequently, the dentin shear bond strength and mechanical properties significantly increased. Addition of 2.5% nanoantibacterial inorganic fillers into the dental adhesive exerted no adverse effect on the mechanical properties significantly (P>0.05). Dental adhesive containing 5% or more nanoantibacterial inorganic fillers inhibited the metabolic activity of the dental plaque microcosm biofilm significantly, thereby displaying a strong antibacterial potency (P<0.05).@*CONCLUSIONS@#This novel antibacterial dental adhesive, which contained 5.0% nanoantibacterial inorganic filler, exhibited promising bonding strength, mechanical property, and antibacterial ability. Hence, this adhesive can be potentially used in caries inhibition in dental application.

Disinfection for Prosthetic Sockets in 19 Wearers / 中国康复理论与实践

Objective To explore the possibities of routine disinfection for prosthetic sockets. Methods From June to August, 2016, 19 lower limbs prosthesis wearers wiped their prosthetic socket surfaces and sprayed the stump socks with a compound of quaternary ammoni-um salt every night for three weeks. Meanwhile, field investigation and sampling were carried out weekly. Staphylococcus aureus, Pseudo-monas aeruginosa, Escherichia Coli and Candida albicans were isolated and identified, and colony counting was carried out. Results After disinfection, the number of bacteria on the prosthetic socket reduced 1.8-3.0 log, and the number of fungi reduced 1.6-1.9 log. One strain of Staphylococcus aureus and one strain of Escherichia Coli were isolated before disinfection and one strain of Pseudomonas aeruginosa was isolated after disinfection. Eczema and itching symptoms relieved or disappeared and deodorant effect was distinguished after continuous disinfection. Conclusion Disinfection on prosthetic sockets with compound of quaternary ammonium salt may control the microbial contam-ination and odor, reduce the incidence of eczema and other skin diseases.

Novel Pharmaceutical Gels Containing Glyccerihizic Acid Ammonium Salt for Chronic Wounds.

Aims: This study aimed at preparing pharmaceutical gels containing Glyccerihizic Acid Ammonium Salt (GAM) for healing of chronic wounds followed by in-vitro and in-vivo characterization of the prepared gels to ensure their suitability, efficacy and safety. Place and Duration of Study: Department of Pharmaceutics, faculty of Pharmacy (El- Minia University) and Department of Histology, Faculty of medicine, El-Minia University, from September 2011 to June 2012. Methodology: Preformulation studies including infra-red and differential scanning calorimetry were performed on the drug and the polymers to confirm their physicochemical compatibility. Pluronic F-127, Carbomer 940, sodium alginate and hydroxypropyl methyl cellulose were used as gelling agents. The gel formulations were evaluated for in-vitro release and characterized for their physicochemical properties. The base that exhibited the highest release rate was subjected to further histological studies in wounded rats to demonstrate the effect of drug concentration on the histopathological changes post applications. Results: Physicochemical compatibility studies demonstrated the absence of interaction between the drug and the polymers. The physical appearance of the prepared gel was accepted. Microscopic examinations confirmed the absence of any particles or grittiness. Sodium alginate-based gels exhibited the highest drug release rate. Statistical analysis showed high significant differences as compared to other formulations (P<0.001). Kinetic studies showed that all formulations exhibited first-order release rate. Histopathological studies demonstrated that wound closure was faster in animals treated with 3% (w/w) drug as compared to those treated with 1% (w/w) drug. No signs of irritation were noticed among all treated animals Conclusion: GAM prepared in sodium alginate base gave the highest in-vitro release pattern, which followed first-order release rate. A concentration of 3% w/w GAM of this base would give better healing effect in a shorter time.

Effect Evaluation of 3M~(TM) Surface Disinfectant on ICU Environment / 中华医院感染学杂志

OBJECTIVE To compare the disinfection effect of 3MTM object surface disinfectant(3M disinfectant) with that of chlorine-containing disinfectants in ICU environment. METHODS The floor, instrument panel board, ward bed tables,computer key boards and telephone keyings were sampled respectively before disinfection, 15 minutes and 4 hours after disinfetion in six ICUs. The bactericide rate of 3M disinfectant and chlorine-containing was compared. RESULTS In the 96 specimens collected, 26 from ward bed tables(48.15%)and 22 from instrument panel board, computer key boards and telephone keyings (26.83%)excede the standard of Ministry of Health(

Protective effects of quateranary ammonium salt derivative (F2) of haloperidol on ischemia and reperfusion injury in rat hearts / 中国药理学通报

AIM: To study the effects of quateranary ammonium salt derivative (F2) of haloperidol on ischemia and reperfusion injury in rat hearts. METHODS: Ischemia and reperfusion injury in rat hearts was induced by occluding the left anterior descending coronary artery for 30 min and restoring blood reperfusion for 30 min. F2(1, 2, 4 mg·kg-1, respectively) was intravenously injected before heart ischemia. Plasma creatine kinase (CK), creatine kinase isoenzyme MB(CK-MB), lactate dehydrogenase(LDH), α-Hydroxybutyrate dehydrogenase (HBDH), grutamicoxalacetic transaminase(GOT), superoxide dismutase (SOD) activity and malondiadehyde (MDA) contents were measured. The pathologic changes of ischemia and reperfusion myocardium were observed on the transmission electron microscopy. RESULTS: F2 reduced the release of CK, CK-MB LDH, HBDH, GOT from I/R rat hearts, increased the activity of SOD and decreased the MDA contents. In F2(1mg·kg-1) group, the serum CK-MB LDH HBDH concentration was lowered significantly (vs I/R group P<0.01 or P<0.05). In F2(2 and 4 mg·kg-1) groups serum CK CK-MB LDH HBDH GOT concentration and MDA contents were decreased significantly (vs I/R group P<0.01), and SOD increased significantly (vs I/R group P<0.01). The decrease of CK, CK-MB, LDH, HBDH, MDA in F2(4 mg·kg-1) group was more remarkable than that in F2(2 mg·kg-1) group (P<0.01). CK-MB in F2(4 mg·kg-1) group was lowered than that in Verapamil (2 mg·kg-1) group (P<0.05). For morphology, myocytes of I/R heart showed intracellular edema, disarrangement and rapture of myocardial fiber, damaged mitochondria, marginated and concentrated nucleus. F2 modified these changes. CONCLUSION: F2 may play an apparent role against rat heart ischemia/reperfusion injury in dose-dependent manner.

Protective effects of quateranary ammonium salt derivative (F_2) of haloperidol on ischemia and reperfusion injury in rat hearts / 中国药理学通报

AIM To study the effects of quateranary ammonium salt derivative (F 2) of haloperidol on ischemia and reperfusion injury in rat hearts. METHODS Ischemia and reperfusion injury in rat hearts was induced by occluding the left anterior descending coronary artery for 30 min and restoring blood reperfusion for 30 min. F 2 (1, 2, 4 mg?kg -1 , respectively) was intravenously injected before heart ischemia. Plasma creatine kinase (CK), creatine kinase isoenzyme MB(CK MB), lactate dehydrogenase(LDH),? Hydroxybutyrate dehydrogenase (HBDH), grutamic oxalacetic transaminase(GOT), superoxide dismutase (SOD) activity and malondiadehyde (MDA) contents were measured. The pathologic changes of ischemia and reperfusion myocardium were observed on the transmission electron microscopy. RESULTS F 2 reduced the release of CK,CK MB LDH,HBDH,GOT from I/R rat hearts, increased the activity of SOD and decreased the MDA contents. In F 2 (1mg?kg -1 ) group, the serum CK MB LDH HBDH concentration was lowered significantly (vs I/R group P

Effect of quateranary ammonium salt derivative (F_2) of haloperidol on calcium in vascular smooth muscle cells / 中国药理学通报

AIM To observe the effect of quateranary ammonium salt derivative (F 2) of haloperidol on calcium level in vascular smooth muscle cells (VSMCs) isolated from thoracic aortas of rat. METHODS VSMCs were loaded with Fluo 3 AM, a calcium sensitive fluorescent dye, and [Ca 2+ ] i was determined by the use of laser scanning confocal microscope (LCSM). RESULTS In Ca 2+ (1 26 mmol?L -1 ) bath solution, intracellular calcium fluorescent intensity (FI) in VSMCs was increased when application with 30 mmol?L -1 KCl, and then was inhibited after addition with F 2. The FI of the ASMCs with different concentrations of F 2 (0 1,1,10,100 ?mmol?L -1 )within three minutes were 64%?9%( n =16, P