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A facile synthesis of 6-amino-2H, 4H-pyrano[2,3-F]pyrazole-5-carbonitriles in deep eutectic solvent

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Chinese Chemical Letters 2016年第3期27卷 370-374页

作者： Manisha R.Bhosle Lalit D.Khillare Sambhaji T.dhumal Ramrao A.Mane Department of Chemistry Dr. Babasaheb Ambedkar Marathwada University Aurangabad 431004 Maharashtra India

A convenient synthesis of 6-amino-2H,4H-pyrano[2,3-F]pyrazole-5-carbonitriles has been accomplished by one pot four-component cyclocondensation of aromatic aldehydes（1a-o） malanonitrile（2）, ethyl acetoacetate（3）, and hydrazine hydrate（4） in freshly prepared deep eutectic solvent, DES（choline chloride：urea）. This protocol has afforded corresponding pyrano[2,3-F]pyrazoles in shorter reaction time with high yields, and it avoids the use of typical toxic catalysts and solvents.

关键词： Choline chloride Cyclocondensation DES One pot Urea Pyranopyrazoles

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Determination of soil physicochemical attributes in farming sites through visible,near-infrared diffuse reflectance spectroscopy and PLSR modeling

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Ecological Processes 2018年第1期7卷 285-296页

作者： Amol D.Vibhute Karbhari V.Kale Suresh C.Mehrotra Rajesh K.dhumal Ajay D.Nagne Geospatial Technology Research Laboratory Department of Computer Science and ITDr.Babasaheb Ambedkar Marathwada UniversityAurangabadMaharashtra 431004India Department of Computer Science and IT Dr.Babasaheb Ambedkar Marathwada UniversityAurangabadMaharashtra 431004India

Introduction:An accurate and reliable detection of soil physicochemical attributes(SPAs)is a difficult and complicated issue in soil *** SPA may be varied spatially and temporally with the complexity of *** the past,SPA detection has been obtained through routine soil chemical and physical laboratory ***,these laboratory methods do not fulfill the rapid ***,diffuse reflectance spectroscopy(DRS)can be used to nondestructively detect and characterize soil attributes with superior *** the present article,we report a study done through spectral curves in the visible(350–700 nm)and near-infrared(700–2500 nm)(VNIR)region of 74 soil specimens which were agglomerated by farming sectors of Phulambri Tehsil of the Aurangabad region of Maharashtra,*** quantitative analysis of VNIR spectrum was ***:The spectra of agglomerated farming soils were acquired by the Analytical Spectral Device(ASD)Field spec 4 *** soil spectra of the VNIR region were preprocessed to get pure spectra which were the input for regression *** partial least squares regression(PLSR)model was computed to construct the calibration models,which were individually validated for the prediction of SPA from the soil *** computed model was based on a correlation study between reflected spectra and detected *** detected SPAs were soil organic carbon(SOC),nitrogen(N),soil organic matter(SOM),pH values,electrical conductivity(EC),phosphorus(P),potassium(K),iron(Fe),sand,silt,and *** accuracy of the PLSR model-validated determinant(R^(2))values were SOC 0.89,N 0.68,SOM 0.93,pH values 0.82,EC 0.89,P 0.98,K 0.82,Fe 0.94,sand 0.98,silt 0.90,and clay 0.69 with root mean square error of prediction(RMSEP)3.51,4.34,2.66,2.12,4.11,1.41,4.22,1.56,1.89,1.97,and 9.91,*** to the experimental results,the VNIR-DRS was better for detection of SPA and produced more accurate predictions for ***

关键词： VNIR reflectance spectroscopy First-derivative transformation Soil physicochemical attributes Partial least squares regression(PLSR) Spectral pre-treatment Nondestructive technique Soil spectral features

Dendrimer-based magnetic resonance imaging agents for brain cancer

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Science China Materials 2018年第11期61卷 1420-1443页

作者： Ling Ding Zhenbin Lyu Dinesh dhumal Chai-Lin Kao Monique Bernard Ling Peng Aix-Marseille Universite CNRSCentre Interdisciplinaire de Nanoscience de Marseille《Equipe Labellise Ligue Contre le Cancer》Marseille France Aix-Marseillle UniversitY CNRSCentre de Resonance Magn＆ique Biologique et MedicaleMarseilleFrance Department of Medicinal and Applied Chemistry Kaohsiung Medical UniversityKaohsiungTaiwanChina Department of Medical Research Kaohsiung Medical University HospitalKaohsiungTaiwanChina

Brain cancer is one of the most lethal and difficult-to-treat cancers because of its physical location and biological barriers. The mainstay of brain cancer treatment is surgical resection, which demands precise imaging for tumor localization and delineation. Thanks to advances in bioimaging, brain cancer can be detected earlier and resected more reliably. Magnetic resonance imaging（MRI） is the most common and preferred method to delineate brain cancer, and a contrast agent is often required to enhance imaging ***, a special family of synthetic macromolecules,constitute a particularly appealing platform for constructing MRI contrast agents by virtue of their well-defined three-dimensional structure, tunable nanosize and abundant surface terminals, which allow the accommodation of high payloads and numerous functionalities. Tuning the dendrimer size,branching and surface composition in conjunction with conjugation of MRI functionalities and targeting moieties can alter the relaxivity for MRI, overcome the blood-brain barrier and enhance tumor-specific targeting, hence improving the imaging quality and safety profile for precise and accurate imaging of brain tumors. This short review highlights the recent progress, opportunities and challenges in developing dendrimer-based MRI contrast agents for brain tumor imaging.

关键词： dendrimer contrast agent blood-brain barrier tumor targeting magnetic resonance imaging

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An ionizable supramolecular dendrimer nanosystem for effective siRNA delivery with a favorable safety profile

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Nano Research 2021年第7期14卷 2247-2254页

作者： Dinesh dhumal Wenjun Lan Ling Ding Yifan Jiang Zhenbin Lyu Erik Laurini Domenico Marson Aura Tintaru Nelson Dusetti Suzanne Giorgio Juan Lucio Iovanna Sabrina Pricl Ling Peng Aix-Marseille Université CNRSCentre Interdisciplinaire de Nanoscience de Marseille(CINaM)UMR 7325Equipe Labellisée Ligue Contre le CancerMarseille 13288France Aix-Marseille Université INSERMCNRSInstitut Paoli-CalmettesCentre de Recherche en Cancérologie de Marseille(CRCM)Marseille 13288France Aix-Marseille Université CNRSCentre de Résonance Magnétique Biologique et Médicale(CRMBM)UMR 7339Marseille 13385France Aix-Marseille Université CNRSInstitut de Chimie Radicalaire(ICR)UMR 7273Marseille 13013France Molecular Biology and Nanotechnology Laboratory Department of Engineering and ArchitecturesUniversity of TriesteTrieste 34127Italy Department of General Biophysics Faculty of Biology and Environmental ProtectionUniversity of LodzLodz 90-136Poland

Gene therapy using small interfering RNA(siRNA)is emerging as a novel therapeutic approach to treat various ***,safe and efficient siRNA delivery still constitutes the major obstacle for clinical implementation of siRNA *** we report an ionizable supramolecular dendrimer vector,formed via self-assembly of a small amphiphilic dendrimer,as an effective siRNA delivery system with a favorable safety *** virtue of the ionizable tertiary amine terminals,the supramolecular dendrimer has a low positively charged surface potential and no notable cytotoxicity at physiological ***,this ionizable feature imparted sufficient surface charge to the supramolecular dendrimer to enable formation of a stable complex with siRNA via electrostatic *** resulting siRNA/dendrimer delivery system had a surface charge that was neither neutral,thus avoiding aggregation,nor too high,thus avoiding cytotoxicity,but was sufficient for favorable cellular uptake and endosomal release of the *** tested in different cancer cell lines and patient-derived cancer organoids,this dendrimer-mediated siRNA delivery system effectively silenced the oncogenes Myc and Akt2 with a potent antiproliferative effect,outperforming the gold standard vector,Lipofectamine ***,this ionizable supramolecular dendrimer represents a promising vector for siRNA *** concept of supramolecular dendrimer nanovectors via self-assembly is new,yet easy to implement in practice,offering a new perspective for supramolecular chemistry in biomedical applications.

关键词： dendrimer self-assembly ionizable vector siRNA delivery gene silencing non-viral vector

A self-assembling prodrug nanosystem to enhance metabolic stability and anticancer activity of gemcitabine

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Chinese Chemical Letters 2022年第5期33卷 2481-2485页

作者： Mei Cong Guangling Xu Shaoyou Yang Jing Zhang Wenzheng Zhang Dinesh dhumal Erik Laurini Kaiyue Zhang Yi Xia Sabrina Pricl Ling Peng Weidong Zhao School of Pharmacy Xinxiang Medical UniversityXinxiang 453003China Henan Key Laboratory of Immunology and Targeted Drugs School of Laboratory MedicineXinxiang Medical UniversityXinxiang 453003China Henan Collaborative Innovation Center of Molecular Diagnosis and Laboratory Medicine School of Laboratory MedicineXinxiang Medical UniversityXinxiang 453003China Aix-Marseille Université CNRSCenter Interdisciplinaire de Nanoscience de MarseilleUMR 7325Equipe Labellisépar La LigueMarseille 13288France Chongqing Key Laboratory of Natural Product Synthesis and Drug Research School of Pharmaceutical SciencesChongqing UniversityChongqing 401331China Molecular Biology and Nanotechnology Laboratory Department of Engineering and ArchitectureUniversity of TriesteTrieste 34127Italy Department of General Biophysics Faculty of Biology and Environmental ProtectionUniversity of LodzLodz 90-236Poland

Self-assembly is a powerful approach in molecular engineering for biomedical applications,in particu-lar for creating self-assembling ***,we report a self-assembling prodrug of the anticancer drug gemcitabine(Gem)based on amphiphilic dendrimer *** prodrug reported in this study demonstrates high drug loading(40%)and robust ability to self-assemble into small nanomicelles,which increase the metabolic stability of Gem and enable entry into cells via endocytosis,hence bypassing transport-mediated *** addition,this prodrug nanosystem exhibited an effective pH-and enzyme-responsive release of Gem,resulting in enhanced anticancer activity and reduced *** ad-vantageous features of both prodrug-and nanotechnology-based drug delivery,this self-assembling Gem prodrug nanosystem constitutes a promising anticancer *** study also offers new perspectives of the amphiphilic dendrimer nanoplatforms for the development of self-assembling prodrugs.

关键词： Self-assembling prodrug Gemcitabine Amphiphilic dendrimer Anticancer candidate Nanomicelles

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Systematic review on the risk-benefit ratio of morphine for acute heart failure

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Journal of Acute Disease 2023年第3期12卷 89-95页

作者： Rushikesh S.Haridas Sheetal Shelke Girish Patrike Deepak Patil Sainath dhumal Department of General Medicine Vilasrao Deshmukh Government Medical CollegeLaturIndia Department of Otorhinolaryngology MIMSR Medical CollegeLaturIndia Department of General Medicine Dr.Balasaheb Vikhe Patil Rural Medical CollegeLoniIndia Department of General Medicine MIMSR Medical CollegeLaturIndia

Objective:To evaluate morphine's risk-benefit profile in the treatment of acute heart ***:Different electronic databases,including PubMed,MEDLINE,Cochrane Library,and Google Scholar,as well as ***,were searched for articles published between 2012 and *** risk of bias in the present study was evaluated by employing randomized controlled trials(RCTs)checklist that assesses the effectiveness of new interventions through random assignment of participants to different treatment *** two-part tool was used to address the five specific domains such as selection bias,performance bias,detection bias,attrition bias,and selective reporting *** of the quality of diagnostic accuracy studies was conducted using the RevMan software(version 5.4),a quality assessment ***:A total of 13 studies were included in the present review,in which there were 5 retrospective studies,3 randomized-control studies,2 prospective studies,1 multicenter pharmacodynamics study,1 multicenter cardiac magnetic resonance imaging study,and 1 open-label,cross-over *** mortality of acute heart failure patients treated with morphine was higher compared to those without ***:Acute heart failure patients who do not receive morphine have a lower mortality rate compared to those who receive *** the adverse effects,including mortality associated with morphine,there is a pressing need for further research to explore alternative and effective treatment options in acute heart failure.

关键词： Acute heart failure Hospital mortality Morphine Side-effects Invasive ventilation

Economical effect of lumen apposing metal stents for treating benign foregut strictures

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World Journal of Gastrointestinal Endoscopy 2018年第10期10卷 294-300页

作者： Alexander Hallac Wichit Srikureja Eashen Liu Parag dhumal Ashish Thatte Nishant Puri Providence Gastroenterology SpokaneWa 99204United States College of Business Economics and ComputingUniversity of Wisconsin-ParksideKenoshaWI 53144United States School of Business Administration Gonzaga UniversitySpokaneWa 99258United States

AIM To evaluate the clinical and economical efficacy of lumen apposing metal stent(LAMS) in the treatment of benign foregut *** A single center retrospective database of patients who underwent endoscopic treatment of benign foregut strictures between January 2014 and May 2017 was analyzed. A control group of non-stented patients who underwent three endoscopic dilations was compared to patients who underwent LAMS placement. Statistical tests performed included independent t-tests and fiveparameter regression analysis RESULTS Nine hundred and ninety-eight foregut endoscopic dilations were performed between January 2014 and May 2017. 15 patients underwent endoscopic LAMS placement for treatment of benign foregut stricture. Thirty-six patients with recurrent benign foregut strictures underwent three or more endoscopic dilations without stent placement. The cost ratio of endoscopic dilation to LAMS(stent, placement and retrieval) is 5.77. Cost effective analysis demonstrated LAMS to be economical after three endoscopic dilation *** was cost effective after two dilations in the Postsurgical stricture subgroup. CONCLUSION Endoscopists should consider LAMS for the treatment of benign foregut strictures if symptoms persist past three endoscopic dilations. Post-surgical strictures may benefit from LAMS if symptoms persist after two dilations in a post-surgical. Early intervention with LAMS appears to be a clinically and economically viable option for durable symptomatic relief in patients with these strictures.

关键词： Benign esophageal stricture Endoscopy economics Stent economics Self expandable metallic stents Esophageal diseases

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γ—氨基丁酸对麻醉狗的中枢性降压作用

医学资料选编 1982年第3期 57-58页

作者： dhumal V R 石米扬

γ—氨基丁酸(GABA)广泛分布于中枢神经系统(Berl 和 Waelsh 1958年),已知静脉内注射或脑室内给药可引起血压下降(Elliot 和 Hobbiger 1959年;Stanton 1963年;Takah-ashi 等1958年).dhumal 等1976年报导 GABA 通过释放递质来调节体温,... 详细信息

γ—氨基丁酸(GABA)广泛分布于中枢神经系统(Berl 和 Waelsh 1958年),已知静脉内注射或脑室内给药可引起血压下降(Elliot 和 Hobbiger 1959年;Stanton 1963年;Takah-ashi 等1958年).dhumal 等1976年报导 GABA 通过释放递质来调节体温,同时也可能是血

关键词：降压作用 GABA 肾上腺素可卡因肾上腺能α-受体兴奋药局部麻醉药中枢性脑室内升压反应降压效应

Jamun(Syzygium cumini(L.)Skeels)seed bioactives and its biological activities:A review

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Food Bioscience 2022年第6期50卷 2035-2050页

作者： Manoj Kumar Muzaffar Hasan Jose M.Lorenzo Sangram dhumal Jyoti Nishad Nadeem Rais Aman Verma Sushil Changan Mrunal Deepak Barbhai Radha Deepak Chandran Ravi Pandiselvam Marisennayya Senapathy Abhijit Dey Prakash Chandra Pradhan Pran Mohankumar Vishal P.Deshmukh Ryszard Amarowicz Mohamed Mekhemar Baohong Zhang Chemical and Biochemical Processing Division ICAR – Central Institute for Research on Cotton TechnologyMumbai400019India Department of Biology East Carolina UniversityGreenvilleNC27858USA Agro Produce Processing Division ICAR – Central Institute of Agricultural EngineeringBhopal462038India Centro Tecnológico de la Carne de Galicia rúa Galicia n◦4Parque Tecnológico de GaliciaSan Cibrao das Viñas32900OurenseSpain Área de Tecnología de los Alimentos Facultad de Ciencias de OurenseUniversidad de Vigo32004OurenseSpain Division of Horticulture RCSM College of AgricultureKolhapur416004MaharashtraIndia Department of Food Technology Shaheed Rajguru College of Applied Sciences for WomenUniversity of Delhi110096India Department of Pharmacy Bhagwant UniversityAjmer305004India Division of Plant Improvement and Pest Management ICAR – Central Arid Zone Research Institute (CAZRI)JodhpurIndia Division of Crop Physiology Biochemistry and Post-Harvest TechnologyICAR – Central Potato Research InstituteShimla171001India School of Biological and Environmental Sciences Shoolini University of Biotechnology and Management SciencesSolan173229India Department of Veterinary Sciences and Animal Husbandry Amrita School of Agricultural SciencesAmrita Vishwa Vidyapeetham UniversityCoimbatore642109Tamil NaduIndia Division of Physiology Biochemistry and Post-Harvest TechnologyICAR – Central Plantation Crops Research Institute (CPCRI)Kasaragod671 124KeralaIndia Department of Rural Development and Agricultural Extension College of AgricultureWolaita Sodo UniversityWolaita SodoEthiopia Department of Life Sciences Presidency University86/1 College StreetKolkata700073West BengalIndia Sardarkrushinagar Dantiwada Agricultural University BanaskanthaGujarat385506India School of Agricultural Sciences Karunya Institute of Technology and SciencesCoimbatore641114Tamil NaduIndia Bharati Vidyapeeth (Deemed to be University) Yashwantrao Mohite Institute of ManagementKaradIndia Institute of Animal

Jamun(Syzygium cumini Skeels)is a nutritious fruit and has historically been used as both as an edible and a traditional *** jamun seed is an inedible by-product of the ***,their high concentration of phytochemicals makes them valuable components of *** studies on diverse biological activities of jamun seeds have warranted their application in human health and biomedical *** review paper discusses critically the phytochemical composition of jamun seeds and the bioactivities,including their antioxidant,anti-inflammatory,anti-cancer,antidiabetic,anti-microbial,anti-obesity,hepato-protective,cardio and gastro-protective *** bioactivity of jamun seed is related to the presence of phenols,flavonoids,steroids,alkaloids,triterpenoids,tannins,and *** research in vivo,and in vitro experiments with human and animal cell models support the idea that jamun seed extract can be valuable additions in food and biomedical fields due to the diverse bio-functional ***,in-depth and systematic in vivo clinical trials using human subjects must be conducted to confirm the safe consumption limit and establish other therapeutic roles of jamun seeds for their abundant utilization as a nutraceutical or pharmacological ***,research is required to understand the exact mechanisms of the bioactivities exhibited by jamun seeds.

关键词： Bioactivity Jamun seeds Phytochemicals Health promoting activity