Current Aspects in Pharmaceutical Research and Development Vol. 2最新文献

{"title":"Investigation on Phytochemical Constituents and Antimicrobial Properties of Crude Flower Extract of Tecoma stans (L.) Juss. ex Kunth","authors":"Sowjanya Pulipati, P. Babu","doi":"10.9734/bpi/caprd/v2/13232d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/13232d","url":null,"abstract":"Since plants are used as therapeutic agents, the present study is designed to evaluate the phytochemical profile and antimicrobial activities of flower of Tecoma stans (L.) ethanolic extract (TSEE) against selective Gram-positive, Gram-negative bacteria in-vitro. Tecoma stans is a flowering perennial shrub belongs to the family Bignoniaceae. The entire plant possesses medicinal value and used for the treatment of various ailments.  The dried flowers were extracted by cold maceration process using ethanol. Presence of phytoconstituents such as alkaloids, glycosides, saponins, carbohydrates, tannins, phenolics compounds, steroids and flavonoids were observed. The antimicrobial activity was carried against bacteria like Staphylococcus aureus, Enterococcus faecalis, Bacillus subtilis, Bacillus megaterium, Streptococcus mutans, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Proteus vulgaris by means of agar well diffusion method. \u0000The TSEE extract exhibited moderate to high level of broad-spectrum antimicrobial activities against these microorganisms. The diameters of zone of inhibition range from 20.33±0.57 to 09.33±1.52 mm; the activity was compared with standard tetracycline. MIC was performed by two-fold broth dilution method and the inhibition range was found to be 31.2 mg/ml to 125 mg/ml. The MBC values lies between 62.5 to 150 mg/ml. The results reported in the present work shows evidence that Tecoma stans flowers possess phytochemicals that exhibit broad spectrum antimicrobial activity against tested pathogenic bacteria.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74680571","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":"Antioxidant and Anti-Osteosarcoma Effect of Edible Fungi Pleurotus ostreatus","authors":"J. Bindhu, E. Vihashinee, A. Rubiga","doi":"10.9734/bpi/caprd/v2/13436d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/13436d","url":null,"abstract":"Osteosarcoma is a rare primary malignancy of bone and is extremely rare type, which accounts for about 0.2% of all cancer. It is treated with the advanced drugs which have effluent side effects when compared to the medicinal plants and phytoconstituents. The fundamental intention of this study is to study the antibacterial movement, phytochemical screening and anticancer action of ethanolic concentrate of Pleurotus ostreatus. The antimicrobial movement of Pleurotus ostreatus was recognized against two G -ve and two G +ve bacteria by agar well dissemination strategy. Based on the zone of inhibition formed the antimicrobial activity intensity were analyzed. The qualitative investigation of phytochemical screening was done which helps in analyzing the bioactive compounds present in the extract ethanolic and has demonstrated the nearness of flavonoids, terpenoids, alkaloids, saponins, starches, tannins, amino acids and steroids. The antioxidant test was done through DPPH and FRAP method. The invitro anticancer and cell toxicity of Pleurotus ostreatus against (osteosarcoma) human bone cancer cell lines compared to normal cell lines were premeditated. The anticancer test was experience against HL60 cancer cells of osteosarcoma. Subsequently, this investigation closes the ethanolic concentrate of Pleurotus ostreatus can be connected as a solid antimicrobial and anticancer properties.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87066621","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":"Role of PKC in CD47-Mediated Phosphatidylserine Expression Pathway in Jurkat T Cells: A Preliminary Study","authors":"I. Uchendu, Ogbonna Kosisochukwu Doris, Oguji Cyprian Emeka, Omeh Johnson Obiechina, Ochi John Chidubem, Udeh Abel Chukwuebuka, Obigeorge Chibueze Joseph, C. Nnam, Olatunji Omokungbe","doi":"10.9734/bpi/caprd/v2/13381d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/13381d","url":null,"abstract":"Treatment failure in T-cell acute lymphoblastic leukaemia (T-ALL) occurs when leukemic blasts acquire resistance to chemotherapeutic agents. Current research efforts are focused on the search for targets for the development of more effective and less toxic anti-leukemic drugs. CD47 has been suggested to be involved in chemo-resistance and cell metastasis. Although several potential mechanisms were suggested to explain the therapeutic effect of CD47-targeting; the downstream effectors which lead to different effects by CD47 are still not well understood. In this preliminary study we assessed the role of Protein kinase C (PKC) in CD47-mediated phosphatidylserine expression pathway in jurkat T cells. Jurkat T cells were incubated with anti-CD47 mAb (BRIC 126), anti-CD44 mAb (BRIC 235) or control in the presence or absence of Bisindolylmaleimide I, hydrochloride (PKC inhibitor). Cells were stained with annexin-V FITC. Flow cytometry analysis was used for measurement of fluorescence intensity. Cell viability was detected using trypan blue exclusion test. PKC inhibition enhanced phosphatidylserine expression in CD47 receptor mediated leukaemia cells apoptotic pathway. This indicates that PKC may be involved in CD47- mediated PS exposure pathway in jurkat T cells. The observations from this study identify CD47 and PKC as novel functional proteins in jurkat T cells with promising therapeutic potential. This study would provide insight for targeted therapy against T- ALL disease.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84657464","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":"Determining the Enhancement of Oral Bioavailability VIA Solid Lipid Nanoparticles of Anticancer Drug Dasatinib - An In-vitro Cytotoxicity and Pharmacokinetic Study","authors":"A. Arafath, B. Jaykar","doi":"10.9734/bpi/caprd/v2/4309f","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/4309f","url":null,"abstract":"Objective: Dasatinib (DST) is a Biopharmaceutics Classification System Class II drug having very low solubility and high permeability. Low aqueous solubility and poor dissolution of DST lead to poor bioavailability, Thus, limited aqueous solubility is the bottleneck for the therapeutic outcome of DST. Animal data suggest that the absolute bioavailability of DST is about 14–34% due to an extensive first-pass effect. To overcome hepatic first-pass metabolism and to enhance oral bioavailability, lipid-based drug delivery systems such as solid lipid nanoparticles (SLNs) can be used. \u0000Methods: SLNs are submicron colloidal carriers having a size range of 50–1000 nm. These are prepared with physiological lipid and dispersed in water or aqueous surfactant solution. DST can be conveniently loaded into SLNs to improve the oral bioavailability by exploiting the intestinal lymphatic transport. An optimal system was evaluated for bioavailability study in rats compared with that of DST suspension (SUS). \u0000Results: An in vitro cytotoxicity study was done by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay method through ATCC cell lines; the percent inhibition was more in SLN when compared with SUS. The pharmacokinetics of DST-SLNs after oral administration in male Wistar rats was studied. The bioavailability of DST was increased by 2.28 fold when compared with that of a DST SUS. \u0000Conclusion: The results are indicative of SLNs as suitable lipid-based carrier system for improving the oral bioavailability of DST.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86975930","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":"Determination of Antifungal and Anti-Aflatoxigenic Activity of the Essential Oil of Lippia lasiocalycina Cham (Verbenacea)","authors":"Wanessa Sales de Almeida, S. G. Lima, Marcelo Costa dos Santos, C. A. Sobrinho, R. Bacelar, M. Muratori","doi":"10.9734/bpi/caprd/v2/12860d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/12860d","url":null,"abstract":"Contamination of food by aflatoxin-producing fungal species generates huge economic losses and directly affects the health of consumers. The search for more natural preservation methods has raised interest in the potential of essential oils like antifungals in food. In this study, we aimed to evaluate the potential inhibition of Lippia lasiocalycina essential oil on fungal growth and aflatoxin B1 production by Aspergillus flavus strains. The minimum inhibitory concentration of the essential oil of L. lasiocalycina was determined against a strain of Aspergillus flavus. The potential for inhibition of fungal growth and aflatoxin B1 production was tested by direct contact and by the action of volatile compounds. Aflatoxin production was determined by HPLC. L. lasiocalycina essential oil inhibited 94% growth of Aspergillus flavus by direct contact and the volatile compounds potentiate the production of aflatoxin B1. The essential oil of Lippia lasiocalycina proved to be applicable in the production chain of aflatoxin B1 marketed as standard for use in scientific research.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"39 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87591715","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":"Molecular Docking and Pharmacokinetic Prediction Studies of Novel Coumarin Derivatives as Arylamine N- acetyltransferase 2 Inhibitors","authors":"S. George, P. K. Sujith, M. Chandran, Kumaran Santhalingam","doi":"10.9734/bpi/caprd/v2/12583d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/12583d","url":null,"abstract":"Arylamine N-acetyltransferases are xenobiotic-metabolizing enzymes responsible for detoxification of many drugs and carcinogens. It catalyzes the N- or O-acetylation of various arylamine and heterocyclic amine substrates and is able to bioactivate several known carcinogens. The levels of NATs in the body have important consequences with regard to an individual's susceptibility to certain drug-induced toxicities and cancers. Objective of present study is to analyse the affinity of computationally designed coumarin derivatives on NAT2 with AutoDock 4.0.1 software and to investigate the interactions between the target compounds and the amino acid residues of the enzyme. Molecular properties of designed compounds were studied by using Molinspiration. All compounds obeyed lipinski rule of five which suggest that these compound have excellent drug likeness properties and are preferable as an orally acting drug.  In present study, pharmacokinetic prediction on coumarin derivatives were done using pkCSM software. ADMET properties prediction results shown that all designed compounds possess well metabolic characteristics without obvious toxicities. Among the designed compounds 3, 6- dibutyl-7-hydroxy-4-oxo-2-chlrobenzyl -4H chromene -8- carbaldehyde (compound 5) shows more binding energy value (-9.08). These values suggested that the designed coumarin derivatives are excellent inhibitors of NAT2.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74109163","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":"Phytochemical Investigation of Crotalaria Species-Isolation of a New Dihydro Chalcone from Crotalaria ramosissima","authors":"V. Namratha","doi":"10.9734/bpi/caprd/v2/13153d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/13153d","url":null,"abstract":"Natural products once served as the only source of medicines to mankind. Plants often synthesize unexpected novel structures which are biologically active, by various biosynthetic pathways. Phytochemical analysis of medicinal plants revealed the presence of various chemical constituents like alkaloids, flavonoids, Saponins, Glycosides, Triterpenoids, which possess a wide range  of Pharmacological activity. The Genus Crotalaria, family fabaceae includes 500 species distributed in tropical and subtropical regions and can be used as medical folklore remedies for treating different health disorders. Several flavones, chalcones and Chromeno chalcones have been isolated from these genus. A detailed re-investigation of Crotalaria ramisissima resulted in the isolation of a new dimethyl, dihydro chalcone Crotaramin, whose structure elucidation was determined by 2D spectral methods.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"37 4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80191858","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 Emphasizing the Efficiency of a Cellulosolytic Preparation on the Hydrolyzed Wood Wastes","authors":"A. Ionescu, A. Casarica, R. Stoica, Nicoleta Ene","doi":"10.9734/bpi/caprd/v2/13079d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/13079d","url":null,"abstract":"According to the literature data, the cellulose, the most abundant organic molecule on Earth, is found mainly as a structural component of plants and algal cell walls, it is also produced by some animals such as tunicates, and it can be produced also by several bacteria, by a natural pathway or by biotechnology. Due to this situation, there are many studies focused on the use of this kind of renewable source and having as their issues the preparation of different valuable products, such as sugars, ethanol. Different chemicals, the whole yeasts biomass valorization with agricultural applications or for biofuels development. Our issue of this present study was to verify if we can avoid the microbial additional activity during the process, mostly while the conversion starts from some materials already pretreated, such as the paper and cellulose industry’s wastes, by using them as substrate in an optimized culture media formula, for the further yeasts strains development.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85098270","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":"An Overview of Fast Dissolving Oral Thin Film","authors":"S. Muthukumar, R. Gayathri, A. Abarnadevika, C. Sanakr, Vinesha Ravi","doi":"10.9734/bpi/caprd/v2/4600f","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/4600f","url":null,"abstract":"Many pharmaceutical companies are switching their products from tablets to fast dissolving oral thin films (OTFs). Films have all the advantages of tablets (precise dosage, easy administration) and those of liquid dosage forms (easy swallowing, rapid bioavailability). Statistics have shown that four out of five patients prefer orally disintegrating dosage forms over conventional solid oral dosages forms. Pediatric, geriatric, bedridden, emetic patients and those with Central Nervous System disorders, have difficulty in swallowing or chewing solid dosage forms. Many of these patients are non-compliant in administering solid dosage forms due to fear of choking. OTFs when placed on the tip or the floor of the tongue are instantly wet by saliva. As a result, OTFs rapidly hydrate and then disintegrate and/or dissolve to release the medication for local and/or systemic absorption. This technology provides a good platform for patent non- infringing product development and for increasing the patent life-cycle of the existing products. The application of fast dissolving oral thin films is not only limited to buccal fast dissolving system, but also expands to other applications like gastroretentive, sublingual delivery systems.","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"65 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85618140","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":"Destabilization of Abnormal Methylation Enzymes as an Effective Therapeutic Strategy via Induction of Terminal Differentiation to Take Out Both Cancer Stem Cells and Cancer Cells","authors":"M. Liau, Paul A. Fruehauf, Zhongqiu Zheng, J. Fruehauf","doi":"10.9734/bpi/caprd/v2/13544d","DOIUrl":"https://doi.org/10.9734/bpi/caprd/v2/13544d","url":null,"abstract":"The objective of this study was to develop cancer drugs effective to take out both cancer stem cells (CSCs) and cancer cells, particularly CSCs since these cells stood in the way to deny the success of conventional therapies to put cancer away. \u0000The association of methylation enzymes with telomerase constitutes a unique abnormality of cancer cells. This abnormality locks methylation enzymes in an exceptionally stable and active state so that hypomethylation of nucleic acids necessary for the cells to undergo Terminal Differentiation (TD) cannot take place. Human body produces metabolites that are able to eliminate telomerase from abnormal methylation enzymes of cancer cells to allow TD to proceed. Cell Differentiation Agent-2 (CDA-2) is a preparation of human metabolites from freshly collected urine, which has been approved for cancer therapy by the Chinese FDA. The effective components of CDA-2 are Differentiation Inducers (DIs) to target on the telomerase of abnormal methylation enzymes and Differentiation Helper Inducers (DHIs) which are the inhibitors of individual enzymes of ternary methylation enzymes. CDA-2 was very effective for the therapy of Myelodysplastic Syndrome (MDS), which is a disease attributable to Cancer Stem Cells (CSCs). We have previously carried out extensive studies on the DHIs of CDA-2.We are now focusing on the DIs of CDA-2 in order to formulate synthetic CDA for the prevention and therapy of cancer via targeting of CSCs. \u0000DIs were purified from CDA-2 solution by procedures including differential solvent extraction, gel filtration, ion exchange chromatography, TLC, and HPLC. The mass of purified active preparation was determined by mass spectroscopy. DI activity was based on the Nitro Blue Tetrazolium (NBT) assay of HL-60 cells. \u0000DIs of CDA-2 were found predominantly as acidic liposomal complexes extractable by dichloromethane. A good proportion of which became covalently linked to inactive carriers which were not soluble in dichloromethane, but soluble in alcohols. We have identified pregnenolone as a DHI of active liposomal complexes. After dissociation from pregnenolone, the active DIs of CDA-2 were not associated with UV absorption peaks of HPLC. We suspected that the active DIs might be acidic peptides derived from endogenous proteins, because we have previously found that acidic peptides of CDA-2 were active DIs. We, thus, randomly picked pentapeptides containing at least two acidic amino acid residues from the sequences of (alpha)- and (beta)-hemoglobin for synthesis to test their DI activities. Indeed, acidic pentapeptides of hemoglobin were active as DIs, although the activities were not impressive. Retinoic Acid (RA) and 12-O-TetradecanoylPhorbol-13-Acetate (TPA) are well known DIs with much better activities. \u0000In this study, we found Pyrvinium Pamoate (PP) as the best DHI, and triinosinate + tetrainosinate (I3 + I4) as an acceptable DHI. \u0000With effective DIs and DHIs on hand, our deliberated CDA formulations w","PeriodicalId":10848,"journal":{"name":"Current Aspects in Pharmaceutical Research and Development Vol. 2","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76507191","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}