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Development and validation of an LC-MS/MS method for tyrphostin A9

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Journal of Pharmaceutical Analysis 2019年第3期9卷 163-169页

作者： Lyndsey F.Meyer Dhaval k.shah Department of Pharmaceutical Sciences School of Pharmacy and Pharmaceutical SciencesThe State University of New York at Buffalo

Here we have presented a sensitive and selective LC-MS/MS method for the quantification of tyrphostin A9, which is a selective inhibitor for platelet derived growth factor receptor tyrosine kinase and has been investigated in vitro as a potent oxidative phosphorylation uncoupler. The murine analytical method was developed for three biological matrices: cell culture media, 3T3-L1 cell lysate, and murine plasma. For each matrix the limit of detection and the limit of quantification were found to be 0.5 ng/mL and 1.0 ng/ mL, respectively. The range of standard curve for each matrix was 1.0-100 ng/mL, linearity was >0.99, and the precision and accuracy were within 20%. 3-(3,5-di-tert-butyl-4-hydroxyphenyl) propanoic acid was found to be the most suitable internal standard. The validated LC-MS/MS method was used to investigate stability and in vitro pharmacokinetics of tyrphostin A9. It was found that tyrphostin A9 is susceptible to hydrolysis, and the degradation product was identified as 3,5-di-tert-butyl-4- hydroxybenzaldehyde. Tyrphostin A9 was not stable in biological matrices, and the rate of its degradation in murine plasma was faster than that in cell culture media. In vitro pharmacokinetic studies revealed that tyrphostin A9 concentrations in the cell culture media declined in a bi-exponential manner and the concentrations inside the adipocytes remained constant, suggesting tyrphostin A9 has an intracellular binding site and is retained within the cell. The LC-MS/MS method presented here paves the way for further quantitative investigations involving tyrphostin A9.

关键词： Tyrphostin 9/ A9/AG-9/Malonoben/SF6847 LC-MS/MS Stability Pharmacokinetics Tyrosine kinase inhibitor

A comparison of centrifugation and tangential flow filtration for nanoparticle purification: A case study on acetalated dextran nanoparticles

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Particuology 2020年第3期18卷 189-196页

作者： Nishan k.shah Ryan Ivone Jie Shen Samantha A.Meenach University of Rhode Island College of PharmacyDepartment of Biomedical and Pharmaceutical SciencesKingstonRI 02881USA University of Rhode Island College of EngineeringDepartment of Chemical EngineeringKingstonRI 02881USA

Tangential fiow filtration (TFF) is a purification method commonly used in a multitude of fields,including particle ***,there is still a lack of comprehensive understanding of the effects of key TFF parameters on nanoparticle (NP) characteristics (purification outcomes).The present study aimed to investigate the influence of various factors on the characteristics of TFF-purified *** most commonly used NP purification method,centrifugation,was studied as a control.A design of experiment approach was implemented to investigate the influence of transmembrane pressure,flow rate,and initial drug loading on NP characteristics using paclitaxel as a model small *** the determination of optimized TFF parameters,the two purification methods were assessed using other model small molecules (*** and resveratrol).The results indicated that the TFF parameters and initial loading of the drug played important roles in the purified NP *** with the centrifugation method,TFF resulted in smaller NP with higher drug *** was able to circumvent issues associated with conventional centrifugation,while yielding similar results,and can potentially serve as a suitable large-scale purification method for polymeric NP.

关键词： Tangential flow filtration Nanoparticle purification Box-Behnken design Acetalated dextran Drug delivery

Possible implications of animal models for the assessment of visceral pain

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Animal Models and Experimental Medicine 2020年第3期3卷 215-228页

作者： Bharata Regmi Manoj k.shah Department of Surgery and Pharmacology Agriculture and Forestry University(AFU)RampurChitwanNepal

Acute pain,provoked generally after the activation of peripheral nociceptors,is an adaptive sensory function that alerts the individual to avoid noxious ***,uncontrolled acute pain has a maladaptive role in sensory activity leading to development of a chronic pain state which persists even after the damage is resolved,or in some cases,in the absence of an initial local acute *** numbers of people suffer from visceral pain at least once during their life span,leading to substantial health care *** studies reporting on the mechanism of visceral pain are accumulating,it is still not precisely ***,this review aims to elucidate the mechanism of visceral pain through an evaluation of different animal models and their application to develop novel therapeutic approaches for treating visceral *** assess the nociceptive responses in viscera,several visceral pain models such as inflammatory,traction,stress and genetic models utilizing different methods of measurement have been *** them,the inflammatory and traction models are widely used for studying the visceral pain mechanism of different disease conditions and post-operative surgery in humans and animals.A hapten,2,4,6-trinitrobenzene sulfonic acid(TNBS),has been extensively used as an inflammatory agent to induce visceral *** traction model seems to cause a strong pain stimulation and autonomic reaction and could thus be the most appropriate model for studying the underlying visceral pain mechanism and for probing the therapeutic efficacies of various anesthetic and analgesics for the treatment of visceral pain and hyperalgesia.

关键词： animal model inflammation noxious stimuli traction visceral pain

Synthesis,characterization and antimicrobial activity of some new biquinoline derivatives containing a thiazole moiety

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Chinese Chemical Letters 2012年第4期23卷 454-457页

作者： Nirav k.shah Nimesh M.shah Manish P.Patel Ranjan G.Patel Department of Chemistry Sardar Patel UniversityVallabh Vidyanagar 388120GujaratIndia

A series of new biquinoline derivatives containing a thiazole moiety were synthesized by a one-pot,base-catalyzed cyclocondensation reaction of 2-chloro-3-formyl quinoline,malononitrile and *** the synthesized compounds were characterized by elemental analysis,FT-IR,~1H NMR and ^（13）C NMR *** the synthesized compounds were screened against three bacterial pathogens,namely Bacillus cereus,*** and Escherichia coli and for antifungal activity against three fungal pathogens,Aspergillus niger,Fusarium oxisporum and Rhizopus using the disc diffusion method.

关键词： Quinoline Multicomponent reaction Thiazole Antimicrobial activity

Is myopia a protective factor against central serous chorioretinopathy?

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International Journal of Ophthalmology(English edition) 2016年第2期9卷 266-270页

作者： George J.Manayath Saurabh Arora Hardik Parikh Parag k.shah Sarvesh Tiwari Venkatapathy Narendran Department of Retina and Ocular Oncology Aravind Eye Hospital

AIM： To evaluate if any association exists between central serous chorioretinopathy （CSCR） and the refractive status of the eye. METHODS： This retrospective, institutional, case control study included 499 patients, wherein 262 patients diagnosed as acute CSCR, were compared with an age and gender matched control group of 237 patients. All patients were evaluated with a detailed systemic and ocular history, objective and subjective refractions for both eyes and complete ocular examination by a retina specialist, at all visits. Optical coherence tomography confirmed the diagnosis of CSCR. ~ RESULTS： The mean age was found to be 40.7y in the study group （Group 1） compared to 38 10y in the control group （Group 2）. Most common refractive status in the study group, was emmetropia seen in 191 patients （72.9%）, followed by hypermetropia seen in 47 patients （17.9%） and astigmatism seen in 21 patients （8.0%）. Only 3 subjects （1.1%） had myopia, which was less than or equal to 1.0 D, compared to 70 subjects （29.5%） in the control group, suggesting a statistically significant lower incidence of CSCR among the myopic patients （P〈 0.0001）. With respect to the systemic factors, 26 （9.9%） patients were using systemic steroids in the study group （Group 1） compared to none in the control group （Group 2） suggesting a statistically significant association of CSCR with systemic steroid use （P〈0.05）. No other significant systemic risk factors were noted. CONCLUSION： Though CSCR is a multifactorial disease, myopia serves as a protective factor for CSCR. Thus, myopic eyes are less likely to develop CSCR. Since both retinal pigment epithelium （RPE） and choriocapillaris are postulated in the pathogenesis of CSCR, chorio-retinal thinning and atrophy seen in myopic eyes are less likely to cause CSCR.

关键词： central serous chorioretinopathy refractivestatus myopia

Effect of Storage Temperature on Vitamin C, Total Phenolics,UPLC Phenolic Acid Profile and Antioxidant Capacity of Eleven Potato(Solanum tuberosum) Varieties

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Horticultural Plant Journal 2017年第2期3卷 73-89页

作者： Joseph Hubert Yamdeu Galani Pooja M.Mankad Avadh k.shah Nilesh J.Patel Rajeshkumar R.Acharya Jayant G.Talati Department of Agriculture and Veterinary Medicine Université des Montagnes Department of Biochemistry B.A. College of Agriculture Anand Agricultural University Main Vegetable Research Station Anand Agricultural University

Storage of potato tubers at low temperature affects their metabolism and may alter their phytochemical properties. There is a need to elucidate the changes in antioxidant compounds, activity and enzymes during storage of tubers. Eleven Indian potato varieties were evaluated for antioxidant parameters, after 0, 30, 60 and 90 days of storage at room temperature, 15 °C and 4 °C. Total phenolics(0.0786–0.1546 mg gallic acid equivalents·g^(-1)FW) and vitamin C content(0.0828–0.2416 mg·g^(-1)FW) varied among the varieties and were different with storage temperature; their levels fluctuated during storage but remained above the initial level until the last day of observation. Phenolic acid profiling by UPLC identified 12 compounds among which the most abundant was chlorogenic acid followed by gallic acid, sinapic acid and ellagic acid. Except para-coumaric acid which decreased at 4 °C, all the phenolic acids increased with storage. Caffeic acid, chlorogenic acid, protocatechuic acid and gallic acid mostly correlated with total phenolic content(r = 0.456, 0.482, 0.588 and 0.620, respectively). Antioxidant activity against both DPPH and ABTS radicals increased during the initial days of storage and then dropped to a level comparable or lower than the original value,irrespective of the storage temperature. Correlation study revealed that chlorogenic acid, gallic acid and ferulic acid mostly contributed to antioxidant activity. Activity of both antioxidant enzymes, superoxide dismutase and ascorbate peroxidase, increased initially but then decreased to values lower than the initial level and were not influenced by storage temperature. Correlation with antioxidant activity indicated that the enhancement of reactive oxygen scavenging species in cold stored tubers could result mainly from ascorbate peroxidase activity. Our results demonstrate that storage temperature adversely influences the metabolism and the content of antioxidant compounds in potato tubers, with subsequent inc

关键词： potato cold storage UPLC phenolics vitamin C antioxidant

Leveraging real-time data to drive quality improvement in a pediatric health system

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Pediatric Investigation 2018年第3期2卷 184-187页

作者： Sopnil Bhattarai Rahul k.shah Children's National Health System WashingtonDCUSA Division of Otolaryngology Children's National Health SystemWashingtonDCUSA

We are inundated by data;healthcare is no *** electronic medical record,the numerous patient care monitors,and the thousands of medications to be reconciled with specific dosing parameters are a few examples of the omnipresent and intimidating nature of data in *** the world,healthcare without data does not *** data represent many forms but are quickly moving towards electronic *** ubiquitous as data are the near universal finding that such data are *** is an urgent need for real-time data in improving processes and ultimately outcomes in *** data lag by four to eight weeks,if not longer,then true change cannot occur and harm continues in that *** review article discusses the urgent need for real-time data and demonstrates examples of how Children's National Medical Center in Washington,DC uses real-time data to drive outcomes.

关键词： Hospital acquired conditions (HAC) Joint Commission Preventable harm index Quality improvement Real-time data Tracer

Crystal Quality Improvement by Reductive Methylation of Surface Lysines

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Crystal Quality Improvement by Reductive Methylation of Surf...

In silico prediction of phytoconstituents from Ehretia laevis targeting TNF-αin arthritis

10～(th) International Conference on the Crystallization of Biological Macromlecules

作者： Ashit k.shah Jessie Chang Joseph D.Ng John P.Rose A2-1003 Gangan Vihar Bibewadi-Kondhwa RoadPune-4111 037INDIA Southeast Collaboratory for Structural Genomics Department of Biochemistry and Molecular BiologyUniversity of Georgia AthensGA 30602U.S.A Laboratory for Structural Biology University of Alabama in HuntsvilleHuntsvilleAL 35899U.S.A Southeast Collaboratory for Structural Genomics Department of Biochemistry and Molecular BiologyUniversity of Georgia AthensGA 30602U.S.A

＜正＞ Structural genomics project requires high throughput protein production, crystallization and structure determination. Obtaining high quality crystals, however, still remains a challenge and is a major bottleneck for rapid crystal production. Reductive methylation of surface lysines, as one of the crystal salvaging pathways in SECSG （Southeast Collaboratory for Structural Genomics）,

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Digital Chinese Medicine 2021年第3期4卷 180-190页

作者： Subhash R.Yende Sapan k.shah Sumit k.Arora keshav S.Moharir Govind k.Lohiya Department of Pharmacology Gurunanak College of PharmacyNagpurMaharashtra 440026India Department of Pharmaceutical Chemistry Priyadarshini J.L.College of PharmacyNagpurMaharashtra 440016India Department of Pharmacognosy and Phytochemistry Gurunanak College of PharmacyNagpurMaharashtra 440026India Department of Pharmaceutics Gurunanak College of PharmacyNagpurMaharashtra 440026India

Objective Rheumatoid arthritis(RA)is an autoimmune disease involving the synovial lining of the major *** therapies have noteworthy side *** study involved in silico evaluation of Ehretia laevis(***)phytoconstituents targeting tumor necrosis factor-α(TNF-α).Methods Molecular docking studies performed to investigate the binding pattern of the plant *** phytoconstituents along with the crystal structure of TNF-α(PDB ID:2 AZ5)using AutoDock Vina followed by a study of interacting amino acid residues and their influence on the inhibitory potentials of the active *** the pharmacokinetic profile and toxicity screening carried out using Swiss ADME and pk *** The docked results suggest that lupeol(-9.4 kcal/mol)andα-amyrin(-9.4 kcal/mol)has best affinity towards TNF-αcompared to standard drug thalidomide(-7.4 kcal/mol).The active chemical constituents represents better interaction with the conserved catalytic residues,leading to the inhibition/blockade of the TNF-α-associated signaling pathway in ***,pharmacokinetics and toxicity parameters of these phytochemicals were within acceptable limits according to ADMET *** The binding potential of phytoconstituents targeting TNF-αshowed promising ***,it encourages the traditional use of *** and provides vital information on drug development and clinical treatment.

关键词： Rheumatoid arthritis Ehretia laevis In silico Molecular docking Pharmacokinetics Tumor necrosis factor-α(TNF-α) Lupeol α-Amyrin