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Pharmacological and analytical aspects of artemisinin for malaria: Advances and challenges

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Asian Pacific Journal of Tropical Medicine 2019年第8期12卷 339-346页

作者： Sravani Karri Sanjay Sharma Ginpreet Kaur NMIMS School of Pharmacy and Technology ManagementShirpurMaharashtraIndia425405 NMIMS Shobhaben Pratapbhai Patel School of Pharmacy and Technology ManagementMumbaiMaharashtraIndia400056

Malaria remains a major tropical health burden owing to the development of resistance and decreased sensitivity to the frequently used conventional antimalarial drugs. The drug like artemisinin possesses potent antimalarial activities, but has some limitations. Therefore, new strategies are to be implemented for optimal utilization of artemisinin to improve its therapeutic effectiveness and to overcome its limitations. The present review focuses on present scenario of malaria and pharmacological as well as analytical aspects of artemisinin. Data from 2000 to 2018 were collected from NCBI for understanding the various analytical techniques used for estimation of artemisinin. This review will reveal the facts about artemisinin which can be utilized to develop novel drug delivery system either in a combination or as alone for the wellbeing of the patients suffering from malaria.

关键词： Malaria Artemisinin Pharmacokinetics Mechanism Analytical techniques

QSAR,docking studies and pharmacophore identification of phenylmethyl phenoxy propyl amino propanoic acid derivatives as leukotriene A_4 hydrolase inhibitors

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药学学报 2010年第5期45卷 615-623页

作者： SONAWANE Lalit V BARI Sanjaykumar B Drug Design and Development R. C. Patel Institute of Pharmaceutical Education and Research Karwand Naka Shirpur Dist. - Dhule Maharashtra State 425405 India

The enzyme leukotriene A4 (LTA4) plays an important role as precursor of slow reactive substances as LTC4, LTD4, and LTE4. It is an attractive target for molecular modeling and QSAR study. Our effort is mainly focused on exploring the SAR for inhibitors of the LTA4 hydrolase through docking study, pharmacophore modeling and molecular descriptor study. The binding of these small molecules on LTA4 hydrolase enzyme was described by the models developed on 2D molecular descriptors, with good predictive power (39 compounds, 6 descriptors, r2 0.98, SEE 0.167, F-value 268.53, q2 0.90, r2adj 0.97, P-value < 0.0001, SD of residuals 0.15). Docking studies were employed to presume the probable binding conformation of these analogues and exploring the SAR for the compounds. The novel pharmacophore represents the ligand features that are involved in interactions with the target protein, as well as the space around the ligand occupied by the protein. The efforts are aimed to discover the SAR for the inhibitors of LTA4 hydrolase through techniques of QSAR, docking and pharmacophore.

关键词： LTA4 hydrolase QSAR molecular descriptor docking pharmacophore

Aloin attenuates chronic constriction injury-induced neuropathic pain in rats by inhibiting inflammatory cytokines and oxidative stress

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Asian Pacific Journal of Tropical Biomedicine 2021年第5期11卷 205-213页

作者： Aarti S.Kale Avinash R.Wadkar Umesh B.Mahajan Lalit A.Birari Sateesh Belemkar Sameer N.Goyal Shreesh Ojha Sanjay J.Surana Chandragouda R.Patil Kalpesh R.Patil Department of Pharmacology R.C.Patel Institute of Pharmaceutical Education and ResearchShirpur-425405Dist.DhuleMaharashtraIndia School of Pharmacy&Technology Management SVKM's NMIMSMPTPShirpur-425405Dist-DhuleMaharashtraIndia Shri Vile Parle Kelavani Mandal's Institute of Pharmacy Dhule-424001MaharashtraIndia Department of Pharmacology and Therapeutics College of Medicine and Health SciencesUnited Arab Emirates UniversityP.O.Box 17666Al AinAbu DhabiUAE Department of Pharmacognosy R.C.Patel Institute of Pharmaceutical Education and ResearchShirpur-425405Dist.DhuleMaharashtraIndia

Objective:To investigate the effect of aloin against chronic constriction injury(CCI)-induced neuropathic pain in ***:Rats were randomly divided into 7 groups:GroupⅠ(normal control),GroupⅡ(sham-operated),GroupⅢ(CCI control)and GroupⅣ,Ⅴ,Ⅵ,andⅦ,which underwent CCI surgery and then were administered with aloin(5 mg/kg,p.o.;25 mg/kg,p.o.;125 mg/kg,p.o.)and gabapentin(50 mg/kg,p.o.),respectively for 14 *** neuropathy was induced by silk ligatures(4-0)loosely placed around the sciatic *** thresholds against mechanical stimuli(Von-Frey filaments)and thermal stimuli(12℃and 40℃)were measured at midplantar paw region ipsilateral to the compressed nerve on day-3,7,11,and *** concentration of cytokines including tumor necrosis factor-α(TNF-α),interleukin-6,and interleukin-1βwas estimated at *** day 14,motor nerve conduction velocity was determined under urethane anesthesia(1.25 g/kg).Oxidative stress parameters(malondiadehyde,glutathione,catalase,and superoxide dismutase)were estimated in sciatic nerve homogenates at day *** nerve samples were processed for histological ***:Aloin significantly reduced CCI-induced mechanical and thermal *** also improved motor nerve conduction velocity and decreased oxidative stress in nerve *** addition,it decreased pro-inflammatory cytokine levels and restored the histoarchitecture of compressed sciatic ***:Aloin mitigates CCI-induced neuropathic pain in rats by inhibiting oxidative stress and pro-inflammatory cytokines in the afflicted sciatic nerve.

关键词： Aloin Chronic constriction injury Antioxidant Neuropathic pain

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江永县柚实雷瘿蚊的发生与防治

植物保护 2002年第4期28卷 34-35页

作者：卢胜进湖南省江永县香柚研究所江永425405

经室内饲养和柚园系统调查明确 ,柚实雷瘿蚊在湖南江永 1年发生 4代 ,以老熟幼虫在柚园土中或以幼虫在虫果内越冬 ,4月下旬始见成虫。以幼虫蛀食果实 ,1年有 4～ 5个危害高峰期 ,其中第 2个高峰期危害最严重。不同栽培条件柚园各代发生... 详细信息

经室内饲养和柚园系统调查明确 ,柚实雷瘿蚊在湖南江永 1年发生 4代 ,以老熟幼虫在柚园土中或以幼虫在虫果内越冬 ,4月下旬始见成虫。以幼虫蛀食果实 ,1年有 4～ 5个危害高峰期 ,其中第 2个高峰期危害最严重。不同栽培条件柚园各代发生期有差异 ,世代重叠明显。对该虫应采用综合防治措施 ,加强植物检疫 ,科学栽培 ,及时处理虫果 ;在成虫羽化始见期。

关键词：柚实雷瘿蚊危害防治措施形态特征生活史柑桔类果实害虫发生规律

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波尔多液配制改进技术研究

中国南方果树 2002年第2期31卷 22-23页

作者：卢胜进湖南省江永县香柚研究所 425405

波尔多液是由硫酸铜、石灰和水配制而成的无机杀菌剂.在植物及病菌的分泌物、有机酸及空气中的二氧化碳等的作用下,波尔多液中铜盐溶解释放出铜离子,铜离子进入病菌体内致细胞原生质蛋白质凝固变性而杀菌,具有很强的保护性杀菌能力,并... 详细信息

波尔多液是由硫酸铜、石灰和水配制而成的无机杀菌剂.在植物及病菌的分泌物、有机酸及空气中的二氧化碳等的作用下,波尔多液中铜盐溶解释放出铜离子,铜离子进入病菌体内致细胞原生质蛋白质凝固变性而杀菌,具有很强的保护性杀菌能力,并且还有药效范围广,作用持久,成本低等优点,故果农普遍用来防治果树病害.然而,常规的两液同倒法和硫酸铜倒入石灰液法,操作起来较费事,特别是大果园和成年果园,每次施药量较多,配制工作量大,迫切要求改进配制技术,达到省力化.为此,我们历时3年的探索,对常规配制波尔多液技术进行了改进,现报告如下.

关键词：波尔多液配制技术改进技术无机杀菌剂

LC,MS^n and LC-MS/MS studies for the characterization of degradation products of amlodipine

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Journal of Pharmaceutical Analysis 2015年第1期5卷 33-42页

作者： Ravi N.Tiwari Nishit Shah Vikas Bhalani Anand Mahajan Department of Pharmaceutical Chemistry SVKM's NMIMSSchool of Pharmacy and Technology ManagementNear Bank of Tapi RiverAgra-Mumbai RoadBabuldeShirpurDist.Dhule 425405MaharashtraIndia Department of Pharmaceutical Chemistry Sinhgad Institute of PharmacyPuneMaharashtraIndia

In the present study,comprehensive stress testing of amlodipine（AM） was carried out according to International Conference on Harmonization（ICH） Q1A（R2） *** was subjected to acidic,neutral and alkaline hydrolysis,oxidation,photolysis and thermal stress *** drug showed instability in acidic and alkaline conditions,while it remained stable to neutral,oxidative,light and thermal stress.A total of nine degradation products（DPs） were formed from *** could be separated by the developed gradient LC method on a C18 *** products formed under various stress conditions were investigated by LC-MS/MS *** previously developed LC method was suitably modified for LC-MS/MS studies by replacing phosphate buffer with ammonium acetate buffer of the same concentration（pH 5.0）.A complete fragmentation pathway of the drug was first established to characterize all the degradation products using LC-MS/MS and multi-stage mass（MS^n） fragmentation *** obtained mass values were used to study elemental compositions,and the total information helped with the identification of *** with its degradation pathway.

关键词： Amlodipine LC-MS/MS Characterization Degradation pathway

Hybrid Metamodel—NSGA-III—EDAS Based Optimal Design of Thin Film Coatings

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Computers, Materials & Continua 2021年第2期66卷 1771-1784页

作者： Kamlendra Vikram Uvaraja Ragavendran Kanak Kalita Ranjan Kumar Ghadai Xiao-Zhi Gao Department of Mechanical Engineering Vel Tech Rangarajan Dr.Sagunthala R&D Institute of Science and TechnologyAvadi600062India Department of Electronics and Telecommunication Engineering MPSTME SVKM’S Narsee Monjee Institute of Management StudiesShirpur425405India Department of Mechanical Engineering Sikkim Manipal Institute of TechnologySikkim Manipal UniversityMajhitar737136India School of Computing University of Eastern FinlandKuopio70211Finland

In this work,diamond-like carbon(DLC)thin film coatings are deposited on silicon substrates by using plasma-enhanced chemical vapour deposition(PECVD)*** varying the hydrogen(H2)flow rate,CH4−Argon(Ar)flow rate and deposition temperature(Td)as per a Box-Behnken experimental design(BBD),15 DLC deposition experiments are carried *** Young’s modulus(E)and the coefficient of friction(COF)for the DLCs are *** using a second-order polynomial regression approach,two metamodels are built for E and COF,that establish them as functions of H2 flow rate,CH4-Ar flow rate and Td.A non-dominated sorting genetic algorithm(NSGA-III)is used to obtain a set of Pareto solutions for the multi-objective optimization of E maximization and COF *** to various practical scenarios,evaluation based on distance from average solution(EDAS)approach is used to identify the most feasible solutions out of the Pareto solution *** experiments are conducted which shows the efficacy of the polynomial regression—NSGA-III—EDAS hybrid *** surface morphology of the DLCs deposited as per the optimal predictions is also studied by using atomic force microscopy.

关键词： Multi-objective optimization regression analysis thin-film coating

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防治柑桔红蜘蛛不当施药的原因及对策

中国果业信息 2000年第4期 43-44页

作者：卢胜进湖南省江永县香柚研究所!425405

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江永香柚“瘤突”果发生情况调查

中国南方果树 2003年第2期32卷 17-18页

作者：卢胜进何源委湖南省江永县香柚研究所 425405 湖南省江永县农业局

江永香柚(即沙田柚)近年发生'瘤突'果面积呈上升趋势,1998年前仅个别柚园发生,至2002年发生'瘤突'果面积约近200hm2,占全县香柚面积的2.17%,平均'瘤突'果率17.9%,高的达98%以上.为明确其发生原因及矫治措施,笔者于1998-2002年开展了专... 详细信息

江永香柚(即沙田柚)近年发生'瘤突'果面积呈上升趋势,1998年前仅个别柚园发生,至2002年发生'瘤突'果面积约近200hm2,占全县香柚面积的2.17%,平均'瘤突'果率17.9%,高的达98%以上.为明确其发生原因及矫治措施,笔者于1998-2002年开展了专项研究.

关键词：江永香柚 “瘤突”果发生情况调查鉴定试验系统调查分类调查防治