{"title":"Six Phthalides as Potent Modulators of the Blood Tumor Barrier Increase the Transmembrane Transport of Compatible Compounds Via Transcellular and Paracellular Pathways","authors":"Xiao-jin Liu, Shu-yuan Shuai, Guo-song Zhang, Qin Zheng, Peng-yi Hu, Zi-qi Li, Ri-qun Liu, Shu-hua Xiao","doi":"10.1007/s11094-024-03103-3","DOIUrl":"https://doi.org/10.1007/s11094-024-03103-3","url":null,"abstract":"<p>The treatment of brain tumors is greatly limited due to the presence of the blood tumor barrier (BTB). Our previous research has shown that the essential oil of chuanxiong promoted temozolomide entry into glioma cells and enhanced temozolomide-induced anticancer efficiency <i>in vivo</i>. Phthalides account for the largest proportion of essential oil and, therefore, this study was conducted to investigate the effects of six phthalides on the transmembrane transport of compatible compounds across the BTB and the mechanism. The results showed that different concentrations of senkyunolide H (SH), senkyunolide A (SA), ligustilide (LIG), butylidenephthalide (BP), <i>n</i>-butylphthalide (NBP) and neocnidilide (NOL) significantly increase the permeability from A (apical side) to B (basolateral side) (Papp<sub>(AB)</sub>) of fluorescein isothiocyanate 4000 (FITC4000), while NBP, NOL and SA could also significantly increase Papp<sub>(B→A)</sub>. Western blot analysis indicated that these phthalides down-regulated expressions of claudin-5, occludin and ZO-1 to increase the permeability of BTB. LIG, SA, SH, NBP and NOL significantly increased Papp<sub>(AB)</sub> and the efflux ratio of the P-gp substrate rhodamine 123 attribute to down-regulate the expressions of P-gp. The expression of caveolin-1 was also down-regulated by the six phthalides. LIG, SA, SH, NBP and NOL acted as effective absorption enhancers in BTB via both the transcellular route and the paracellular route.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"184 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614767","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
V. B. Markeev, S. V. Tishkov, E. V. Blynskaya, K. V. Alekseev
{"title":"Study of the Pressing Process of N-Butyl-N-Methyl-1-Phenylpyrrolo-[1,2-a]Pyrazine-3-Carboxamide (GML-3) Tablets Using Mathematical Modeling Techniques","authors":"V. B. Markeev, S. V. Tishkov, E. V. Blynskaya, K. V. Alekseev","doi":"10.1007/s11094-024-03107-z","DOIUrl":"https://doi.org/10.1007/s11094-024-03107-z","url":null,"abstract":"<p><i>N</i>-Butyl-<i>N</i>-methyl-1-phenylpyrrolo[1,2-<i>a</i>]pyrazine-3-carboxamide (GML-3) is an original molecule developed at the Research Zakusov Institute of Pharmacology. GML-3 has both anxiolytic and antidepressant activity, which makes the development of tablets based on it a promising task. Optimization of the pressing process is currently an urgent task of the pharmaceutical industry because this technological stage has a significant impact on the disintegration of tablets and the release of the active pharmaceutical ingredient. The Heckel and Kuenz–Leuenberger models were used to study the pressing process of GML-3 tablets. These models were compared to select the most reliable description of pressing GML-3 tablets from granules. Granules with polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC) as a binder were used.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"12 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140615007","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Zhaobao Xiang, Xueli Ping, Pengfei Chen, Linfeng You, Bin Zhou
{"title":"Chemical Composition and Antioxidant Activity of Petroleum Ether Extract from Kaempferia galanga L.","authors":"Zhaobao Xiang, Xueli Ping, Pengfei Chen, Linfeng You, Bin Zhou","doi":"10.1007/s11094-024-03101-5","DOIUrl":"https://doi.org/10.1007/s11094-024-03101-5","url":null,"abstract":"<p><i>Kaempferia galanga</i> L. (KGL) from Hainan, China was extracted by ultrasonic-assisted extraction with 90% ethanol solution, and then extracted with petroleum ether after the ethanol extract was recovered to be alcohol free. The antioxidant activity of the petroleum ether fraction of KGL was first tested using the ABTS method. GC-MS was used to analyze the chemical constituents of the petroleum ether fraction. The scavenging effect on ABTS free radicals of the petroleum ether fraction was weak, indicating that the antioxidant activity of the petroleum ether fraction was moderate. A total of 25 chemical components were identified by GC-MS analysis. The main components with higher content were 2,6,11-trimethyl dodecane, ethyl <i>p</i>-methoxy cinnamate, and ethyl cinnamate, which accounted for 81.64%. Furthermore, 11 kinds of constituents of the petroleum ether extract were obtained from KGL for the first time. This experiment clarifies firstly the main chemical composition of petroleum ether fraction from KGL, which provides some scientific basis for the further exploration and use of petroleum ether fraction from KGL and the comparative analysis of the chemical composition of KGL in different regions.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"20 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614454","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Utilization of Phytochemicals as Nutraceutical in the Prophylaxis of Dengue","authors":"Jyoti Baranwal, Swastika Singh, Smriti Kushwaha, Archana Jyoti","doi":"10.1007/s11094-024-03105-1","DOIUrl":"https://doi.org/10.1007/s11094-024-03105-1","url":null,"abstract":"<p>Every year, during the monsoon season, dengue, an infectious disease transmitted by the <i>Aedes aegypti</i> mosquito and caused by the dengue virus, occurs. The frequency and prevalence of dengue fever, as well as deaths from its consequences, have increased dramatically in recent years. Despite the fact that the infection has affected a large number of people worldwide, no specific and efficient drug treatment is known. Researchers are working tirelessly to find a cure, focusing their efforts on developing therapeutic treatments that block or inhibit the activity of specific Dengue virus (DENV) proteins. This review focuses on the phytochemical constituents present in traditionally used natural remedies for the treatment of dengue such as papaya leaf extract, goat milk, kiwi fruit, dragon fruit, and coconut water. Undoubtedly, the contents of this review will motivate researchers to do more novel work in this area which will accelerate the journey towards the exploration of the pharmacological activity of natural compounds.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"61 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614772","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S. S. Antipov, D. V. Tarasova, M. M. Borodina, M. V. Likhodzievskaya, D. A. Cherenkov, T. N. Khmelevskaya, L. V. Antipova, V. G. Artyukhov
{"title":"Prospects of Creating Collagen Substances Based on a Study of the Physical and Chemical Characteristics of Proteins of Hydrobiont Dermal Emulsions","authors":"S. S. Antipov, D. V. Tarasova, M. M. Borodina, M. V. Likhodzievskaya, D. A. Cherenkov, T. N. Khmelevskaya, L. V. Antipova, V. G. Artyukhov","doi":"10.1007/s11094-024-03108-y","DOIUrl":"https://doi.org/10.1007/s11094-024-03108-y","url":null,"abstract":"<p>Proteins of the collagen family were identified in the dermal emulsion of a freshwater fish, the African clary catfish (<i>Clarias gariepinus</i>). Acumulative assessment of their physicochemical properties gave reason to consider the emulsion obtained using the developed method as a source of functional biopolymers, particularly collagen proteins. The fractional composition, charge state, molecular mass, and the ability for hydrolysis by <i>Clostridium histolytica</i> collagenase were experimentally determined. Evaluation of the amino-acid composition allowed the analogy and features of collagen proteins of animal and fish origin to be identified. The studied emulsions were shown to contain negatively charged proteins with molecular masses >100 kDa, the fractions of which contained predominantly collagen. The results supported the assumption that a significant part of the hydrobiont collagen was type I collagen, which made it possible to consider them in the future as a basis for various substances and served as a starting point for understanding the physicochemical functioning essentials and assessing the possibility of using them in pharmaceutical technologies.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"16 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614476","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"In-Vitro Effect of Ammodaucus Leucotrichus Flower and Fruit Essential Oils on Nitric Oxide Production and Arginase Activity in Human Peripheral Blood Mononuclear Cells (PBMC) from Patients with Behçet Disease","authors":"Djamel Messaoudene, Nourelhouda Ghozali, Hayet Neghliz, Tarek Benabdelkader, Houda Belguendouz, Malika Terahi, Fifi Otmani, Chafia Touil-Boukoffa","doi":"10.1007/s11094-024-03104-2","DOIUrl":"https://doi.org/10.1007/s11094-024-03104-2","url":null,"abstract":"<p><i>Ammodaucus leucotrichus</i> is an Algerian aromatic medicinal plant, widely known as “Oum-draiga or Kamoune-l’ibel”. In folk medicine, the flower and fruit of this plant are widely used for the treatment of cough, fever, diarrhea, colic, and cold. In this study, we describe for the first time the modulatory effects of flower and fruit essential oils (EOs) of <i>A. leucotrichus</i> subsp. <i>leucotrichus</i> on NOS and Arginase activities and their regulation during Behçet disease, an auto-inflammatory vasculitis of unknown etiology. The EOs were obtained by Clevenger-hydrodistillation and their chemical composition was analyzed by gas chromatography-mass spectrometry (GC-MS). The peripheral blood mononuclear cells of 20 patients and 15 control samples (PBMC) were cultured in RPMI-1640 and incubated with or without seeds and the flowers’ essential oil from <i>A. leucotrichus</i> was dissolved in DMSO (0.01%). Culture supernatants were harvested after 24 h of incubation. NO and urea measurements were, respectively, performed by modified Griess and Berthelot methods. Our results show that essential oils for both fruits and flowers significantly reduce the production of NO production in a concentration-dependent manner. In contrast, significantly increased urea was noted in treated PBMC of BD patients. Our study suggests that EOs extracted from the flower and fruit of <i>A. leucotrichus</i> could have potential immuno-modulatory effects characterized by a down-regulation and up-regulation of NO and urea, respectively, probably by NOS/Arginase balance regulation.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"153 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614478","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Synthesis, Characterization and Biological Evaluation of Novel Benzimidazole Derivatives against Candida albicans","authors":"Monika Chauhan, Shivani Gupta, Sarvesh Paliwal, Sumitra Nain","doi":"10.1007/s11094-024-03099-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03099-w","url":null,"abstract":"<p>In heterocyclic chemistry, benzimidazole is recognized as a “privileged structure” due to its association with a wide range of biological activities. In this present research work, we included the synthesis, characterization and biological evaluation of substituted derivatives. The designated derivatives were synthesized by the condensation method. <i>ortho</i>-Phenylenediamine was used as the starting material. The designated benzimidazole derivatives were synthesized using different acids and aldehydes. Further, the <i>in-vitro</i> antifungal-activity-synthesized compounds were evaluated against <i>Candida albicans</i> using the agar well diffusion method and the culture tube method. It was concluded that all the designated derivatives of benzimidazole exhibited prominent antifungal activity and can be considered as potent leads in future antifungal research.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"31 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Development of a Quantitative Determination Method for Polysorbate 80 in Biologicals by Size-Exclusion High-Performance Liquid Chromatography","authors":"O. B. Rounova, M. G. Korotkov, O. B. Ustinnikova","doi":"10.1007/s11094-024-03110-4","DOIUrl":"https://doi.org/10.1007/s11094-024-03110-4","url":null,"abstract":"<p>Aquantitative determination method for polysorbate 80 in biological medicinal preparations using size-exclusion chromatography with UV detection was developed. OASIS HLB solid-phase extraction cartridges were used to extract polysorbate 80 from formulations with high protein concentrations. The HPLC separation was performed using a TSKgel G2000SWX column in isocratic mode. The mobile phase was phosphate buffer (0.1 M) containing sodium sulfate (0.1 M) and sodium dodecyl sulfate (0.1%). The developed method could be used for quantitative determination of polysorbate 80 in biological medicinal products.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"184 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614817","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
G. S. Shakirzyanova, L. Yu. Izotova, O. Kh. Kholbekov, F. Yu. Zhaloliddinov, G. G. Rakhmonova, B. N. Babaev
{"title":"Synthesis of 5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-thiadiazole-2(3H)-thione] and Study of Its Anti-Inflammatory Activity","authors":"G. S. Shakirzyanova, L. Yu. Izotova, O. Kh. Kholbekov, F. Yu. Zhaloliddinov, G. G. Rakhmonova, B. N. Babaev","doi":"10.1007/s11094-024-03094-1","DOIUrl":"https://doi.org/10.1007/s11094-024-03094-1","url":null,"abstract":"<p>5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-thiadiazole-2(3<i>H</i>)-thione] was synthesized by oxidative condensation in the presence of chloride ions. The structure of the resulting compound was identified by an x-ray crystal structure analysis, for which the crystallographic data were obtained. The anti-inflammatory activity of the synthesized disulfide was studied for the first time in a carrageenan edema model. 5,5′-(Disulfanediyl)bis[3-phenyl-1,3,4-diazole-2(3<i>H</i>)-thione] was shown to have anti-inflammatory and antiexudative activity at doses of 10 and 20 mg/kg. Its effect was close to that of the drug Nimesil.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"41 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140560148","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Acetaminophen and Thiosalicylic Acid Sensor Based on Carbon Paste Electrode Modified with Multi-Walled Carbon Nanotubes and Natural Deep Eutectic Solvent","authors":"Ebrahim Zarei, Maryam Vafadar, Alireza Asghari","doi":"10.1007/s11094-024-03090-5","DOIUrl":"https://doi.org/10.1007/s11094-024-03090-5","url":null,"abstract":"<p>A carbon paste electrode (CPE) modified with multi-walled carbon nanotubes (MWCNTs) and natural deep eutectic solvent (NADES) was prepared and applied for the simultaneous voltammetric determination of acetaminophen (ACP) and thiosalicylic acid (TSA) in real samples. Electrochemical impedance spectroscopy (EIS) was applied for investigation of electron transfer rate of [Fe(CN)<sub>6</sub>]<sup>3-/4-</sup> as a redox couple probe on the MWCNTs/NADES/CPE surface. The modified electrode preserved and combined the properties of individual modifiers synergistically. Significant enhancement in the peak current responses of ACP and TSA were observed at the modified electrode compared to the bare electrode. Under the optimal conditions, a linear dynamic range of 5–2900 μM for ACP and 5–2250 μM for TSA was obtained. The limit of detection (LOD) for ACP and TSA were 4.71 μM and 4.35 μM, respectively. Finally, this method was successfully employed for the determination of ACP and TSA in real samples.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"38 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140560247","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}