Journal of Pharmaceutical and Biopharmaceutical Research最新文献_第3页

Effect of experimental hyperglycemia on intestinal elimination and biliary excretion of ibuprofen enantiomers in hyperglycemic rats 实验性高血糖对高血糖大鼠肠道消除和胆汁排泄布洛芬对映体的影响

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2022-01-01 DOI: 10.25082/jpbr.2022.02.001

Hawsar Othman Mohamed, A. Almási, P. Perjési

{"title":"Effect of experimental hyperglycemia on intestinal elimination and biliary excretion of ibuprofen enantiomers in hyperglycemic rats","authors":"Hawsar Othman Mohamed, A. Almási, P. Perjési","doi":"10.25082/jpbr.2022.02.001","DOIUrl":"https://doi.org/10.25082/jpbr.2022.02.001","url":null,"abstract":"Diabetic complications are mostly due to hyperglycemia. Hyperglycemia is reported to be associated with oxidative stress. It can result in changes in the activities of drug-metabolizing enzymes and membrane-integrated transporters, which can modify the fate of drugs and other xenobiotics. An in vivo intestinal perfusion model was used to investigate how experimental hyperglycemia affects intestinal elimination and biliary excretion of ibuprofen enantiomers in the rat. Experimental diabetes was induced by intravenous (i.v.) administration of streptozotocin. The intestinal perfusion medium contained 250 µM racemic ibuprofen. A validated isocratic chiral HPLC method with UV detection was developed to determine the amount of the two enantiomers in the intestinal perfusate and the bile. The results indicated that experimental diabetes doesn’t cause a statistically significant difference in the disappearance of ibuprofen enantiomers from the small intestine. Analysis of the bile samples detected only the (S)-IBP enantiomer. Excretion of the ibuprofen enantiomer to the bile decreased in experimental diabetes. The observed changes can affect the pharmacokinetics of drugs administered in hyperglycemic individuals.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"123 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76801130","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}

引用次数: 0

Efficacy and mechanism of KRAS G12C PROTAC in inhibiting the proliferation of pancreatic cancer cells KRAS G12C PROTAC抑制胰腺癌细胞增殖的作用及机制

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2022-01-01 DOI: 10.25082/jpbr.2021.01.002

Shuai Gao, Fangxia Zou, Li-xia Zheng, Yun-jie Wang, Xinyu Feng, Deshuai Liu, Yu Mao, L. Ye, Jingwei Tian

{"title":"Efficacy and mechanism of KRAS G12C PROTAC in inhibiting the proliferation of pancreatic cancer cells","authors":"Shuai Gao, Fangxia Zou, Li-xia Zheng, Yun-jie Wang, Xinyu Feng, Deshuai Liu, Yu Mao, L. Ye, Jingwei Tian","doi":"10.25082/jpbr.2021.01.002","DOIUrl":"https://doi.org/10.25082/jpbr.2021.01.002","url":null,"abstract":"Pancreatic cancer is a rare but highly malignant cancer with few effective treatments available. Targeting cancers bearing specific genetic mutations offers a new approach for cancer therapy. PROTAC (proteolysis-targeting chimeras) is an emerging technique to design targeted therapy and increasing evidence supports its utility. This study examined the in vitro pharmacodynamics and mechanism of PROTAC K-Ras Degrader-1 (PKD-1), a PROTAC molecule, in inhibiting the proliferation of pancreatic cancer cells. We used a pancreatic cancer cell line, MIA PaCa-2 cells, to examined the binding and degradation-promoting capabilities of PKD-1 on KRAS G12C protein and further evaluated the effects of PKD-1 on cell viability, cell cycle and apoptosis. PKD-1 was able to bind to KRAS G12C protein, promoted its degradation for up to 72 h, reduced cell viability, increased cell cycle arrest and promoted cell apoptosis. Mechanistic study found that the efficacy of PKD-1 was at least partially mediated by promoting 26S proteasome degradation process. Combined, these results extended previous findings and support the potential utility of PROTAC molecules such as PKD-1 as a new treatment strategy against pancreatic cancer.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90702165","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}

引用次数: 0

Differentiation between drug-type, fibre-type and intermediate-type in cannabis samples: HPLC-UV versus GC-FID 大麻样品中药物型、纤维型和中间型的鉴别:HPLC-UV vs GC-FID

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2021-01-01 DOI: 10.25082/JPBR.2020.02.003

Kian Kadkhodaei, Nina Biei, E. Vidiella, Pamela Osmenaj, G. Cannazza, M. Schmid

{"title":"Differentiation between drug-type, fibre-type and intermediate-type in cannabis samples: HPLC-UV versus GC-FID","authors":"Kian Kadkhodaei, Nina Biei, E. Vidiella, Pamela Osmenaj, G. Cannazza, M. Schmid","doi":"10.25082/JPBR.2020.02.003","DOIUrl":"https://doi.org/10.25082/JPBR.2020.02.003","url":null,"abstract":"Cannabis sativa is known to be the most abused illegal drug worldwide. To date it is not only used as a medicine but has been established as a lifestyle product. The most relevant phytocannabinoids represent the ingredients delta-9-tetrahydrocannabinol (9-THC) and cannabidiol (CBD), whereby only 9-THC shows a psychoactive effect. Since 2017, the so-called CBD-hemp containing CBD as main ingredient is distributed in many countries as a legal alternative. In these products, 9-THC must not exceed a certain percentage. It is hardly possible to differentiate between THC-hemp and CBD-hemp presenting a major challenge for authorities. Therefore, there is the need to develop fast and efficient analysis methods to distinguish between fibre-type, drug-type and intermediate-type cannabis products. The aim of this study was to compare two simple and inexpensive HPLC-UV and GC-FID methods for their ability to quantify phytocannabinoids in dried cannabis plant material. For this purpose, a set of 37 fresh and dried cannabis samples randomly chosen from seizures of Austrian police was subject to complementary quantification of 9-THC and CBD. After having taken into account decomposition of certain phytocannabinoids, the result of this quantitative study showed good correlation between HPLC-UV and GC-FID regardless of quantifying cannabis leaves or buds.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"338 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80708772","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}

引用次数: 0

Pharmacokinetics study of potential anti-CML drug Cyclobentinib (CB1107) by HPLC–MS/MS 高效液相色谱-质谱联用技术研究潜在抗cml药物环本替尼(CB1107)的药代动力学

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2021-01-01 DOI: 10.25082/jpbr.2021.01.001

Xinghua Zhao, Jiaojiao Zhang, Yutong Liang, Jie Li, Shi Ding, Wang Yang, Ye Chen, Ju Liu

{"title":"Pharmacokinetics study of potential anti-CML drug Cyclobentinib (CB1107) by HPLC–MS/MS","authors":"Xinghua Zhao, Jiaojiao Zhang, Yutong Liang, Jie Li, Shi Ding, Wang Yang, Ye Chen, Ju Liu","doi":"10.25082/jpbr.2021.01.001","DOIUrl":"https://doi.org/10.25082/jpbr.2021.01.001","url":null,"abstract":"Purpose: A simple, sensitive and specific HPLC–MS/MS method was established to analysis the pharmacokinetics of CB1107 in mouses. Methods: A simple, selective, and sensitive high-throughput liquid chromatography-tandem mass spectrometry (LC-MS-MS) method has been developed and validated for quantitative determination of CB1107 in rat serum.Chromatographic separation was achieved on a Zorbax Extend C18 Rapid Resolution HD column (4.6 mm × 50 mm, 1.8 μm). The column temperature was maintained at 35℃ and at flow rate of 0.6 mL/min. Injection volume was 20 μL. The mobile phases consisted of 0.1% formic acid in water (mobile phase A)and 0.1% formic acid in acetonitrile (mobile phase B), and total run time was 30min. MS-MS detection was performed in the selected monitoring mode of electrospray positive ionization reaction. Results: The pharmacokinetic characteristics of CB1107 in mice belong to the two-compartment model.When the doses were 400 mg/kg, 600 mg/kg and 800 mg/kg, corresponding area under the plasma concentration-time curve (AUC) respectively were 20.011±1.24 mg/h/L, 26.778±2.19 mg/h/L, 38.82±1.44 mg/h/L, suggesting that CB1107 have a good absorption in the body.And the AUC of three doses are proportional, indicating that CB1107 conforms to linear pharmacokinetics in vivo. Conclusion: This method was successfully applied to study the pharmacokinetics at three different doses of CB1107 after oral administration in mouses. In this study, the bioactivity mechanism of CB1107, by the pharmacokinetic investigation of CB1107 in vivo.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"42 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91011690","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}

引用次数: 0

Cholinergic receptor blockers affect the protective effect of Angong Niuhuang pill on neurologic deficits and intestinal injury in intracerebral hemorrhage mice 胆碱能受体阻滞剂影响安宫牛黄丸对脑出血小鼠神经功能缺损及肠道损伤的保护作用

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2021-01-01 DOI: 10.25082/JPBR.2020.02.002

Yunqi Yang, Tian Wang, Shumin Yue, Mingan Li, Lin Zhou, F. Fu

{"title":"Cholinergic receptor blockers affect the protective effect of Angong Niuhuang pill on neurologic deficits and intestinal injury in intracerebral hemorrhage mice","authors":"Yunqi Yang, Tian Wang, Shumin Yue, Mingan Li, Lin Zhou, F. Fu","doi":"10.25082/JPBR.2020.02.002","DOIUrl":"https://doi.org/10.25082/JPBR.2020.02.002","url":null,"abstract":"Stroke is a devastating disease, intracerebral hemorrhage (ICH) is a devastating subtype. This study aimed to investigate whether cholinergic receptors participate in the process of Angong Niuhuang Pill (ANP) improving neurological function and relieving intestinal injury in ICH mice. The mice were treated with ANP, cholinergic receptor blockers, atropine (ATR), penehyclidine hydrochloride (PHC) or methyllycaconitine (MLA). Male CD-1 mice were randomly divided into 9 groups, Sham, ICH, ANP (0.2 g/kg), ANP plus ATR, ANP plus PHC, ANP plus MLA, ATR, PHC, MLA. ICH model is made by collagenase VII injection (0.075 U). ANP (0.2 g/kg) was administered by gavage after 30 min of ICH. MLA, ATR, PHC was given at 15 min after ICH. Neurological function was evaluated by Garcia test. Intestinal injury was observed by histological analysis. Endotoxin (ET) was measured by enzyme-linked immunosorbent assay. Compared to the Sham group, the score of Garcia test in the ICH significantly decreased. ANP increased significantly the score of ICH mice. ANP also ameliorated the intestinal injury caused by ICH. Cholinergic receptor blockers reversed partially the improvement of neurological function and intestinal injury by ANP. ANP attenuates the neurological deficits and intestinal injury in ICH mice and the protective effect of ANP may be involved in the regulation of the cholinergic system.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86391069","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}

引用次数: 1

Phylogenetic analyses and genomic variation of the 2019-nCoV 新型冠状病毒的系统发育分析及基因组变异

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2020-08-24 DOI: 10.25082/JPBR.2020.01.004

F. Haq, S. Saleem, M. Imran, A. Ghazal, Kashif Ahmad, Muhammad Roman, S. Rahman, Samin Ullah, Iftekhar Ahmad, Habibah Mehmood, Wajahat Ullah

{"title":"Phylogenetic analyses and genomic variation of the 2019-nCoV","authors":"F. Haq, S. Saleem, M. Imran, A. Ghazal, Kashif Ahmad, Muhammad Roman, S. Rahman, Samin Ullah, Iftekhar Ahmad, Habibah Mehmood, Wajahat Ullah","doi":"10.25082/JPBR.2020.01.004","DOIUrl":"https://doi.org/10.25082/JPBR.2020.01.004","url":null,"abstract":"There is a rising global concern about the SARS CoV-2 as a public health threat. Complete genome sequence have been released by the worldwide scientific community for understanding the molecular characteristics and evolutionary origin of this virus. Aim of the current context is to present phylogenetic relationship and genomic variation of 2019-nCoV. Based on availability of genomic information, we constructed a phylogenetic tree including also representatives of other coronaviridae, such as Middle East respiratory syndrome, severe acute respiratory syndrome and Bat coronavirus. The phylogenetic tree analysis suggested that SARS CoV-2 significantly clustered with bat SARS like coronavirus genome, however structural analysis revealed mutation in Spike Glycoprotein and nucleocapsid protein. However our phylogenetic and genomic analysis suggests that bats can be the reservoir for this virus. Lack of forest might be the fact in association of bats with human environment. It is also difficult to study on bats due to absence of proper reagent and availability of few species for research. We confirm high sequence similarity (>99%) among sequenced SARS CoV-2 genomes, and 96% genome identity with the bat coronavirus, confirming the notion of a zoonotic origin of SARS CoV-2.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-08-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84117803","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}

引用次数: 1

Study on the interaction of some (E)-2-benzylidenebenzosuberone derivatives with serum albumin by UV-Vis method, inhibitory effect on topoisomerase 紫外-可见法研究(E)-2-苄基苯并亚酮衍生物与血清白蛋白的相互作用及其对拓扑异构酶的抑制作用

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2020-08-14 DOI: 10.25082/jpbr.2020.01.003

Z. Rozmer, P. Perjési

引用次数: 2

Developments in encapsulation of insulin: Is oral delivery now possible? 胰岛素包封的进展:口服给药现在可行吗?

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2019-08-13 DOI: 10.25082/JPBR.2019.02.005

A. Singh, Yizhen Guo, Anika Singh, Wenrui Xie, Patrick Jiang

{"title":"Developments in encapsulation of insulin: Is oral delivery now possible?","authors":"A. Singh, Yizhen Guo, Anika Singh, Wenrui Xie, Patrick Jiang","doi":"10.25082/JPBR.2019.02.005","DOIUrl":"https://doi.org/10.25082/JPBR.2019.02.005","url":null,"abstract":"This review presents the possibilities of oral delivery of insulin. Insulin, being readily destroyed/ transformed by the proteolytic enzymes and first-pass effects in the digestive system, has mainly been administered through injection, such as intravenous injection and transdermal injection. With developments in the material sciences, appropriate encapsulation methodologies have been developed that could be employed to protect insulin from the digestive effects of the human GI system, and thereby have opened a gateway of research exploring the oral route of insulin delivery. One approach is to incorporate insulin into an emulsion with an appropriate oil-phase, which protects the insulin from degradation. Coating with natural or synthetic polymeric materials, or with lipids, followed by size-reduction to 100-1000 nm is applied as another common approaches of insulin encapsulation. Other approaches like liposomes, nanogels, etc. are also being explored. This review gives a summary of methods of preparation as well as in vitro and in vivo bioavailability of insulin through these methods. It is observed that the oral bioavailability of insulin intake has increased from about 0.1% to about 20% for encapsulated insulin.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-08-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79788422","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}

引用次数: 12

Isolation and identification of Shenghua microorganisms in fermented chili pepper from Southwest China 西南发酵辣椒中盛华菌的分离与鉴定

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2019-08-05 DOI: 10.25082/JPBR.2019.02.004

Qing-feng Meng, Lunwei Zhu, Yao Zhang, Longjie Zhang, Shaobin Fu

引用次数: 1

Spectroscopic and molecular docking studies on the binding mechanism of Mobic and lipase Mobic与脂肪酶结合机理的光谱与分子对接研究

Journal of Pharmaceutical and Biopharmaceutical Research Pub Date : 2019-05-13 DOI: 10.25082/JPBR.2019.02.002

Bao-Sheng Liu, Xu Cheng, Hongcai Zhang

{"title":"Spectroscopic and molecular docking studies on the binding mechanism of Mobic and lipase","authors":"Bao-Sheng Liu, Xu Cheng, Hongcai Zhang","doi":"10.25082/JPBR.2019.02.002","DOIUrl":"https://doi.org/10.25082/JPBR.2019.02.002","url":null,"abstract":"Under simulated physiological conditions (pH=7.40), the interaction between non-steroidal anti-inflammatory drug mopicol and lipase was studied by fluorescence spectrum, ultraviolet absorption spectrum, circular dichroism spectrum and computer simulation technique. The experimental results showed that Mobic could quench the fluorescence of lipase by static quenching, and the binding site number is about 1. According to Forster's theory of non-radiation energy transfer, the binding distance between Mobic and lipase was obtained, r 0, indicating that hydrophobic force played a major role in the formation of Mobic and lipase complex. The results of synchronous fluorescence spectra, UV spectra and circular dichroism spectra showed that Mobic changed the conformation of lipase. The molecular docking results showed that the binding position of Mobic was close to the active center, indicating that Mobic could change the microenvironment of amino acid residues at the active center of lipase catalysis. The results of docking showed that there was hydrogen bond between Mobic and lipase, so the interaction between Mobic and lipase was driven by hydrophobic interaction and hydrogen bond.","PeriodicalId":16703,"journal":{"name":"Journal of Pharmaceutical and Biopharmaceutical Research","volume":"93 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88550257","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}

引用次数: 3