Journal of Developing Drugs最新文献

{"title":"In Vitro Anti-Acetylcholinesterase Activity of Crude Fruits Sap Extract of Solanum incanum in Green Peach Aphids","authors":"A. Umar, A. J. Mgutu, N. M. Piero, Njoroge W Ann, Gitahi S Maina, M. Maina, N. J. Muriithi, M. J. Kiambi, Ngure G Mutero, Mwonjoria K John","doi":"10.4172/2329-6631.1000142","DOIUrl":"https://doi.org/10.4172/2329-6631.1000142","url":null,"abstract":"Acetylcholinesterase is a key enzyme that terminates nerve impulses by catalyzing the hydrolysis of neurotransmitter, acetylcholine, in the nervous system in various organisms. Irreversible inhibitors have been developed as insecticides such as organophosphates and carbamates. Aqueous crude fruit sap extract of S. incanum was evaluated for acetylcholinesterase activity in green peach aphids using Ellman’s method and is found active in inhibiting the ACHe of green peach aphids. All tested concentrations of crude fruits sap extract of S. incanum possessed the ability to inhibit acetylcholinesterase of green peach aphids at dose dependent manner and IC50 of 49.9 was calculated. This study suggest that aqueous crude fruit sap extract of S. incanum inhibit the acetylcholinesterase of the green peach aphids and it is possible the extract has compounds that increase both the level and duration of the neurotransmitter action.","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"27 1","pages":"1-3"},"PeriodicalIF":0.0,"publicationDate":"2015-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89939439","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Routes of Opioid Abuse and its Novel Deterrent Formulations","authors":"A. Omidian, D. Mastropietro, H. Omidian","doi":"10.4172/2329-6631.1000141","DOIUrl":"https://doi.org/10.4172/2329-6631.1000141","url":null,"abstract":"This review aimed to investigate the abuse patterns of common prescription opioids currently on the market by collecting large-scale surveys of different abuser populations. Furthermore, we aimed to analyze the efficacy and properties of currently implemented abuse-deterrent formulations (ADF) for these compounds. Our investigation showed that while oxycodone and oxymorphone are primarily abused by oral ingestion and insufflations, respectively, their ADF products (reformulated OxyContin and Opana ER) show some encouraging results to deter their abuse. Tapentadol is not popular amongst abuser populations, its ADF are difficult to tamper with, and it does not produce significantly desirable effects in noncompliant patients when compared to other opioids. Hydromorphone is predominantly abused by injection, and any effective abuse-deterrent strategy must specifically prioritize and target this route. Current formulations have successfully conferred aversive properties onto the drug in the event of preparation for injection, yet overall rates of hydromorphone abuse remain high, suggesting that more innovative steps need to be taken. Despite novel deterrent technologies that collectively offer deterrence by insufflations, injection and co-ingestion with alcohol, more priority needs to be given to deterring the most common and accessible route of abuse, i.e., oral ingestion of multiple doses.","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"29 1","pages":"1-7"},"PeriodicalIF":0.0,"publicationDate":"2015-11-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76759015","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Antioxidant Activities of C3, 6-Dibenzoylated Phenyl-Thiosemicarbazone-Chitosans","authors":"Yunliang Dai, Zhimei Zhong","doi":"10.4172/2329-6631.1000140","DOIUrl":"https://doi.org/10.4172/2329-6631.1000140","url":null,"abstract":"Ten new C3, 6-dibenzoylated thiosemicarbazone-chitosan derivatives (with two different molecular weights) were prepared. The purpose of this study was to further investigate the antioxidant activities of this series of derivatives and the relationship between the structure and their antioxidant behavior. In order to know how the structure influenced the antioxidant activities of the derivatives, their structures were characterized by FT-IR spectroscopy and elemental analysis in this paper. In addition, the antioxidant activities of these new derivatives were also researched employing various established systems, such as hydroxyl radical (•OH)/superoxide anion (O2 −)/DPPH scavenging and reducing power. Besides that, the cell toxicity of those derivatives was determined with MTT method. The results indicated that 3,6-DBZPTSCZLCS, 3,6-DBZ(p-NP)TSCZLCS, 3,6-DBZ(o-CP)TSCZHCS, and 3,6-DBZ(p-NP)TSCZHCS had the potential to be used as natural antioxidants because of their excellent activities in all these assays. O O O O NH2 C S NNH C NH C NNH C S NH 3,6-DBZPTSCZCS 3,6-DBZPTSCZHCS , Mw= 200 KDa ; 3,6-DBZPTSCZLCS , Mw= 3 KDa . n Ten new 3, 6-diacetylated phenyl-thiosemicarbazone-chitosans were synthesized and characterized. The antioxidant activities of the derivatives were investigated.","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"15 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2015-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87171952","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Efficacy of Dobesilate in Allergic Rhinitis - Case Report","authors":"P. Cuevas, M. Hinojosa, J. Angulo, G. Giménez-Gallego","doi":"10.4172/2329-6631.1000139","DOIUrl":"https://doi.org/10.4172/2329-6631.1000139","url":null,"abstract":"Allergic rhinitis is a common condition that causes a negative effect on patient well-being. Antihistamines and glucocorticoids, the first line treatments usually administered for rhinitis, are normally associated to side effects. In addition, they may show limited efficiency in controlling nasal obstruction, edema and hyperemia occurring secondary to persistent inflammation. Dobesilate, an inhibitor of fibroblast growth factor and vascular endothelial growth factor, shows a markedly anti-inflammatory activity in several inflammation-dependent diseases and inflammation models. Our study shows that nostril spray application of dobesilate for one week is effective in reducing symptoms and signs in patients with seasonal allergic rhinitis.","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"26 1","pages":"1-3"},"PeriodicalIF":0.0,"publicationDate":"2015-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75709061","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"ABCG2 Inhibitors: Will They Find Clinical Relevance?","authors":"Jerec Ricci, Debbie Lovato, R. Larson","doi":"10.4172/2329-6631.1000138","DOIUrl":"https://doi.org/10.4172/2329-6631.1000138","url":null,"abstract":"Multiple drug resistance (MDR) is a prominent way by which cancer develops resistance to various chemotherapeutic agents and continues to be a hurdle in treating cancer patients. A few ATP binding cassette (ABC) transporters have been described as comprising the main mechanism behind MDR: ABCB1, ABCC1, and ABCG2. Of these three, ABCG2 is unique in that it seems to be mainly expressed in solid tumors. Despite the recent discovery of many compounds that inhibit its activity, it remains one of the least well-studied transporters in both animal models and in humans with regard to its contribution to MDR. Though the blockade of the ABCG2 efflux protein has great potential in reversing MDR in cancer, will it be enough to overcome chemoresistance in the clinic?","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"64 1","pages":"1-6"},"PeriodicalIF":0.0,"publicationDate":"2015-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76854212","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evidence that Food Proteins in Vaccines Cause the Development of FoodAllergies and Its Implications for Vaccine Policy","authors":"Vinu Arumugham","doi":"10.4172/2329-6631.1000137","DOIUrl":"https://doi.org/10.4172/2329-6631.1000137","url":null,"abstract":"Nobel Laureate Charles Richet demonstrated over a hundred years ago that injecting a protein into animals or humans causes immune system sensitization to that protein. Subsequent exposure to the protein can result in allergic reactions or anaphylaxis. This fact has since been demonstrated over and over again in humans and animal models. The Institute of Medicine (IOM) confirmed that food proteins in vaccines cause food allergy, in its 2011 report on vaccine adverse events. The IOM’s confirmation is the latest and most authoritative since Dr. Richet’s discovery. Many vaccines and injections contain food proteins. Many studies since 1940 have demonstrated that food proteins in vaccines cause sensitization in humans. Allergens in vaccines are not fully disclosed. No safe dosage level for injected allergens has been established. As a result, allergen quantities in vaccines and injections are not regulated. Allergen quantities in vaccine excipients are also not regulated. It has been demonstrated that a smaller quantity of allergen is needed to cause sensitization than elicitation. It is well recognized that many currently approved vaccines have enough allergen to cause anaphylaxis. Therefore, they contain more than enough allergen to cause sensitization. Children today have fewer childhood infectious diseases. They have less exposure to helminths. C-section birth rates have increased in the last few decades by 50%. C-section births are known to result in sub-optimal gut micro biome in the newborn. All the above result in an immune imbalance biased towards atopy. Vaccine schedules today include 30-40 shots. Up to five shots may be simultaneously administered in one sitting. Vaccines contain adjuvants such as pertussis toxins and aluminum compounds that also bias towards allergy. Adjuvants also increase the immunogenicity of injected food proteins. This combination of atopic children and food protein injection along with adjuvants, contributes to millions developing lifethreatening food allergies. Given the scale and severity of the food allergy epidemic, urgent action is needed to change vaccine policy concerning vaccine specifications, manufacture, vaccine package insert documentation requirements, the Vaccine Adverse Event Reporting System (VAERS) and the National Vaccine Injury compensation program. Many researchers have called for the removal of food proteins from vaccines and re-evaluation of adjuvants such as aluminum compounds. In the interim, food allergy warnings can be included in vaccine package inserts. Simultaneous administration of multiple vaccines can be stopped to avoid the combined negative effects of multiple food proteins and adjuvants.","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"83 1","pages":"1-3"},"PeriodicalIF":0.0,"publicationDate":"2015-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74319887","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Physical, Thermal and Spectral Properties of Biofield Treated 1,2,3-Trimethoxybenzene","authors":"M. Trivedi, R. M. Tallapragada, A. Branton, Dahryn Trivedi, G. Nayak, R. Mishra, S. Jana","doi":"10.4172/2329-6631.1000136","DOIUrl":"https://doi.org/10.4172/2329-6631.1000136","url":null,"abstract":"Study background: 1,2,3-Trimethoxybenzene is an important compound used for the synthesis of chemicals and pharmaceutical agents. The objective of this study was to investigate the influence of biofield energy treatment on the physical, thermal and spectral properties of 1,2,3-trimethoxybenzene. Methods: The study was performed by dividing the sample into two groups (control and treated). The control group remained as untreated, while the treated group received Mr Trivedi’s biofield energy treatment. The control and treated 1,2,3-trimethoxybenzene samples were then characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy, and ultra violetvisible spectroscopy (UV-Vis) analysis. Results: XRD studies revealed the significant increase in crystallite size of treated sample by 45.96% as compared to the control sample. DSC analysis showed a decrease in melting temperature of the treated sample (45.93oC) with respect to control (46.58oC). Additionally, the substantial change was evidenced in latent heat of fusion of treated sample by 64.18% as compared to the control. TGA analysis indicated a decrease in maximum thermal decomposition temperature (Tmax) of treated sample (151.92oC) as compared to the control sample (154.43oC). This indicated the decrease in thermal stability of the treated sample as compared to the control. FT-IR spectroscopic analysis showed an increase in the frequency of C-O bond in treated sample (1105→1174 cm-1) as compared to the control sample. However, UV analysis showed no changes in absorption peaks in treated sample as compared to the untreated sample. Conclusion: Overall, the result indicated that biofield energy treatment has altered the physical, thermal and spectral properties of the treated sample as compared to control. Hence, the treated sample could be used as an intermediate in the synthesis of organic compounds.","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"2015 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2015-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74264926","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"It is Good to Be an Orphan","authors":"Rebecca Smith, R. Lodder","doi":"10.4172/2329-6631.1000e146","DOIUrl":"https://doi.org/10.4172/2329-6631.1000e146","url":null,"abstract":"","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"37 1","pages":"1-2"},"PeriodicalIF":0.0,"publicationDate":"2015-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74527103","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Study on Blood Parameters of Tetrahydropyrimidine CarboxamideDerivatives on Breast Cancer","authors":"M. Jayanthi, P. Venkatesh, Sathiravada Veeraswamy Thirunavukkarasu","doi":"10.4172/2329-6631.1000135","DOIUrl":"https://doi.org/10.4172/2329-6631.1000135","url":null,"abstract":"Pyrimidine is one of the most important heterocycles exhibiting remarkable pharmacological activities. Pyrimidine is a heterocyclic aromatic organic compound containing 1,2,3,4-Tetrahydropyrimidine carboxamide derivatives ring which shows wide range of biological activities. Numerous methods for the synthesis of pyrimidine and also their diverse reactions offer enormous scope in the field of medicinal chemistry. The potential antitumor activities of 1,2,3,4-Tetrahydropyrimidine carboxamide derivatives were prepared and used for the anti Cancer treatment. Inhibitory action of the tumor of this compound was shown significantly improved blood parameter includes hemoglobin (HB), RBC, platelets and WBC. In-vivo studies results showed substantial improved blood parameters in compared to untreated control rats. The newly synthesized compound exhibited significant effects on the treated animals as compared to DMBA induced animals.","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"301 1","pages":"1-5"},"PeriodicalIF":0.0,"publicationDate":"2015-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75663853","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Why it is Important to Protect Intellectual Property and Data Confidentialityin Trade Agreements","authors":"R. Freeman","doi":"10.4172/2329-6631.1000E145","DOIUrl":"https://doi.org/10.4172/2329-6631.1000E145","url":null,"abstract":"","PeriodicalId":15589,"journal":{"name":"Journal of Developing Drugs","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2015-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89559846","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}