{"title":"Accumulation of Natural and Artificial Radionuclides by Medicinal Plant Raw Materials Using Nettle Leaves as an Example","authors":"N. A. D’yakova","doi":"10.1007/s11094-024-03166-2","DOIUrl":"https://doi.org/10.1007/s11094-024-03166-2","url":null,"abstract":"<p>The purpose of the present research was to study peculiarities in the accumulation of natural and artificial radioisotopes in medicinal plant raw material using nettle (<i>Urtica dioica</i> L.) leaves as an example. The specific activities of the main long-lived artificial radioisotopes (cesium-137 and strontium-90) and naturally occurring radionuclides (thorium-232, potassium-40, and radium-226) in experimental samples of upper soil layers and nettle leaves were determined on a RADEK MKGB-01 spectrometer-radiometer. All studied samples of nettle leaves collected in natural and artificial phytocenoses of Voronezh Region met existing radiation safety requirements (first group). A correlation analysis of the specific activities of artificial and natural radionuclides in the soil and nettle leaves showed a close relationship between these numerical indicators that confirmed their contamination primarily through soil. The specific activities of strontium-90, cesium-137, thorium-232, potassium-40, and radium-226 in the medicinal plant raw material increased as their specific activities in the soil increased. High accumulations of cesium-137 and potassium-40 from the upper soil layers were noted for nettle leaves growing in Voronezh Region. A detailed analysis of the dependence of the calculated accumulation coefficients of natural and artificial radioisotopes in nettle leaves revealed trends toward their decrease with increases in the specific activities of the radionuclides in the soil, which indicated physical mechanisms for regulating their uptake into the plant were present.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"49 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141772314","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}
Chandrakant G. Bonde, Ritesh P. Bhole, Ashish Asrodkar, Rupesh V Chikhale, Shailendra S. Gurav
{"title":"Design, Synthesis and Biological Evaluation of (Z)-1-(Benzo[D]Thiazol-2-yl)-2-(3-Substituted Thiazolidine-4-One) Hydrazine Dpre1 Inhibitors as Antimycobacterial Agents","authors":"Chandrakant G. Bonde, Ritesh P. Bhole, Ashish Asrodkar, Rupesh V Chikhale, Shailendra S. Gurav","doi":"10.1007/s11094-024-03164-4","DOIUrl":"https://doi.org/10.1007/s11094-024-03164-4","url":null,"abstract":"<p>A simple and promising methodology was employed for the synthesis of <i>(Z</i>)-1-(benzo[<i>d</i>]thiazol-2-yl)-2-(3-substituted thiazolidine-4-one) hydrazine as antitubercular agents<i>.</i> In vitro activity was tested against <i>Mycobacterium tuberculosis</i>. Two derivatives among all the synthesized compounds were found to be highly effective. Furthermore, to rationalize the observed biological activity data, a molecular docking study has also been carried out against a potential target DprE1 enzyme. The interaction was shown between the oxygen of thiazolidinediones and Ser228. The bond distance (O—H) is 2.35 Å. The π-π-stacking was seen between His137 and thiazole ring electrons. The binding score of compound 15 is –7 kcal/mol, which suggests an excellent binding affinity toward the Dpre1 receptor.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"32 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141718417","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":"Biopharmaceutical Evaluation of a Photoprotective Preparation Based on Melanin Isolated from Seed Episperm of Horse Chestnut (Aesculus hippocastanum L.)","authors":"L. B. Azimova, A. V. Filatova, A. S. Turaev","doi":"10.1007/s11094-024-03160-8","DOIUrl":"https://doi.org/10.1007/s11094-024-03160-8","url":null,"abstract":"<p>The article focused on a study of the release of melanin from its gel dosage form and the toxicological properties of the gel. The recorded release of melanin from the gel was fastest during the first 3 h (50.8%). The remaining amount of melanin was subsequently released gradually as the system equilibrium shifted. The photoprotective action of the drug was prolonged because of the slowed melanin release. Symptoms of acute toxicosis and lethal outcomes were not recorded in all experimental animals during studies of the acute toxicity parameters of the developed gel based on melanin isolated from horse chestnut seed episperm with subcutaneous administration and cutaneous application at doses of 1500, 2000, 2500, and 3000 mg/kg. The developed photoprotective gel belonged to class Vof practically harmless substances. The LD<sub>50</sub> value for cutaneous application to rats was >2500 mg/kg.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"12 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608762","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}
Cemre Aydeğer, Yasemen Adalı, Mustafa Makav, Hüseyin Avni Eroğlu
{"title":"Investigation of the Effects of Dimethyl Sulfoxide in Experimental Gout with Comparison of Dexamethasone and Indomethacin","authors":"Cemre Aydeğer, Yasemen Adalı, Mustafa Makav, Hüseyin Avni Eroğlu","doi":"10.1007/s11094-024-03154-6","DOIUrl":"https://doi.org/10.1007/s11094-024-03154-6","url":null,"abstract":"<p>Gout arthritis is an inflammatory arthritis characterized by increased serum uric acid and accumulation of monosodium urate (MSU) crystals in soft tissues. The treatment for gout arthritis is centered on reducing uric acid agents with long-term and anti-inflammatory agents during attack times. In recent studies, it is noteworthy that Indomethacin and Dexamethasone have positive effects in the treatment of gout. Dimethyl sulfoxide (DMSO) is a lipophilic solvent and has an anti-inflammatory effect at appropriate doses. Based on this information, for this study, the effects of these three agents were investigated in rats using a gut model to compare their efficacy. In the study, a total of 48 female 3–4-month rats were divided equally into 8 groups: Control, Indomethacin, DMSO, Dexamethasone, Gout, Gout+Indomethacin, Gout+DMSO, Gout +Dexamethasone. During the eight-week study, a gout arthritis model was used that included 10 mg MSU given intra-articularly in the right foot. Indomethacin 12.5 mg/kg intragastric, DMSO 0.1 ml intraperitoneally and dexamethasone 0.2 mg/kg were administered subcutaneously to the related groups once a day for seven days. At the end of the study, collected articular tissues were stained with haematoxylin and eosin after the fixation and decalcification processes were done. The findings obtained showed that inflammation was reduced in treatment groups compared to the Control groups (all p values 0.002). Also, synovial proliferation was remarkably decreased in the Gout+Dexamethasone group compared to the Gout group (<i>p</i> = 0.019). As a result of these findings, although the three agents all reduced inflammation in gout arthritis, DMSO was shown to be more advantageous due to its having fewer side-effects.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"78 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608758","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}
M. V. Petropavlovskaya, M. E. Palkeeva, A. S. Molokoedov, M. V. Ovchinnikov, M. V. Sidorova
{"title":"Comparative Evaluation of Alternative Deblocking Agents to Piperidine for Solid-Phase Synthesis of Peptides","authors":"M. V. Petropavlovskaya, M. E. Palkeeva, A. S. Molokoedov, M. V. Ovchinnikov, M. V. Sidorova","doi":"10.1007/s11094-024-03169-z","DOIUrl":"https://doi.org/10.1007/s11094-024-03169-z","url":null,"abstract":"<p>The availability of piperidine, which is widely used for deblocking α-amine groups in solid-phase peptide synthesis using Fmoc methodology, is now significantly limited because this reagent is classified as a controlled substance. Therefore, a search for other available reagents capable of removing Fmoc-protection seems relevant. The suitability of three deblocking reagents based on secondary amines (4-methylpiperidine, pyrrolidine, and piperazine) for the solid-phase synthesis of peptides of various structures, i.e., atosiban (an analog of the neurohypophysial hormone oxytocin), metilin [an agonist of the apelin receptor (APJ)], and a fragment of the 11-19 amino-acid segment of the regulatory myosin light chain was comparatively assessed. These reagents were shown to be suitable alternatives to piperidine for the preparation of the physiologically active peptides being studied.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"154 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608761","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":"Microextraction Recovery of Tilmicosin Phosphate for HPLC-UV Determination in Washings from Surfaces of Pharmaceutical Equipment","authors":"Z. R. Gizatulina, S. Yu. Garmonov, A. V. Bulatov","doi":"10.1007/s11094-024-03173-3","DOIUrl":"https://doi.org/10.1007/s11094-024-03173-3","url":null,"abstract":"<p>A method for microextraction recovery and concentration of tilmicosin phosphate in washings from surfaces of pharmaceutical equipment for its determination by high-performance liquid chromatography with spectrophotometric detection was proposed. The developed method involved dispersion of the extractant (1-dodecanol) in an aqueous solution of a sample while rotating a cotton disk equipped with an inserted magnetic stirrer followed by crystallization of the extract upon cooling the extraction system. The extractant was applied beforehand to the cotton disk. Effective dispersion of the extractant in the aqueous phase during rotation of the cotton disk ensured a high degree of analyte recovery (94%). The detection limit of tilmicosin phosphate (3σ) reached 0.7 mg/L. The determined concentrations ranged from 2 to 250 mg/L. The analytical capabilities of the developed method were demonstrated using quantitative determination of tilmicosin phosphate in washings from surfaces of pharmaceutical equipment after completion of its cleaning as examples.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"2010 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608755","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 Peroral Dosage Form of a Nitrosyl Iron Complex with Thiosulfate Ligands, an Exogenous Nitric Oxide (NO) Donor","authors":"V. O. Novikova, O. V. Pokidova, N. A. Sanina","doi":"10.1007/s11094-024-03170-6","DOIUrl":"https://doi.org/10.1007/s11094-024-03170-6","url":null,"abstract":"<p>The composition and technology for obtaining a solid dosed stable dosage form of a promising representative of the class of nitrogen monoxide (NO) donors, an anionic tetranitrosyl iron complex with thiosulfate ligands Na<sub>2</sub>[Fe<sub>2</sub>(S<sub>2</sub>O<sub>3</sub>)<sub>2</sub>(NO)<sub>4</sub>]·4H<sub>2</sub>O, were developed. The rate of NO generation by the complex could be modulated by using different types of excipients or by varying their concentrations. Albumin was found to be the optimal prolonging agent in the manufacture of this dosage form. The developed dosage form expanded the arsenal of long-acting NO-donor medicines used to treat socially significant diseases.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"14 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608880","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}
A. Elgeziry, R. Ghazala, A. Abdelbary, M. Barakat, O. Nayel, C. A. Ismail
{"title":"Targeting Endothelial Progenitor Cells Reparative Potential Via Canonical Wnt/NOX-4 Signaling Pathway in Rats Dyslipidemia: Role of Resveratrol","authors":"A. Elgeziry, R. Ghazala, A. Abdelbary, M. Barakat, O. Nayel, C. A. Ismail","doi":"10.1007/s11094-024-03155-5","DOIUrl":"https://doi.org/10.1007/s11094-024-03155-5","url":null,"abstract":"<p>Signaling pathways guiding the reparative function of endothelial progenitor cells (EPCs) are complex. Conflicts involve the double-face role of NADPH oxidase-4 (NOX-4) and canonical Wnt/ β-catenin pathways in endothelial dysfunction. Resveratrol confers vasoprotection, yet its molecular mechanism is not clearly delineated. The study investigated whether targeting Wnt/β-catenin/NOX-4 signaling pathway could improve EPC repair in dyslipidemia, and whether it is a therapeutic target for resveratrol vasoprotection. Thirty-six Wistar rats were assigned as normal or dyslipidemic and fed on standard-chow or high-fat diet (HFD), respectively. Dyslipidemic rats received an 8-week oral vehicle or resveratrol (10 mg/kg/day). Eight weeks later, body and visceral-fat weights, and lipid profiles were assessed. Aortae were dissected for histopathological examination and immunohistochemical assessment of the EPC marker (CD133/VEGF receptor-2), and b-catenin expression. Aortic NOX-4 mRNAexpression and vascular function were performed. EPC regenerative capacity evidenced by their count and vascular reactivity was reduced by dyslipidemia. Dysregulation of endothelial Wnt/ β-catenin signaling, and NOX-4 expression were noted in conjunction with endothelial atherogenesis and oxidative stress. Resveratrol conferred endothelial protection, anti-atherogenic, and antioxidant action in HFD-fed rats. Improvement of EPC reparative potential played a pivotal role in resveratrol vasoprotection and was mediated by an endothelial Wnt/ β-catenin/NOX-4 signaling crosstalk, constituting a novel therapeutic target for improving EPC repair profile in dyslipidemia.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"25 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608757","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}
Boyuan Pan, Linna Fu, Heng Du, Guangbin Liu, Bingchao Duan, Kui Lu
{"title":"Design and Spectral Validation of RAD51 Inhibitors Based on BRC4 (1523-1546)","authors":"Boyuan Pan, Linna Fu, Heng Du, Guangbin Liu, Bingchao Duan, Kui Lu","doi":"10.1007/s11094-024-03163-5","DOIUrl":"https://doi.org/10.1007/s11094-024-03163-5","url":null,"abstract":"<p>RAD51 is a core factor for homologous recombination to repair DNA double-strand breaks and overexpressed in breast cancer cells. Truncated peptide BRC4 (1523-1537) was obtained by computer simulation which had the highest binding free energy targeting RAD51. To enhance the binding affinity to the target protein, six nicotinic acid derivatives were modified at the <i>N</i>-terminal of BRC4 (1523-1537) by Fmoc solid-state synthesis to obtain nicotinamide-modified peptides. The interaction of RAD51 (181-200) with BRC4 (1523-1537) and nicotinamide-modified peptides was verified by circular dichroism (CD) spectroscopy and fluorescence spectroscopy. In conclusion, modifying small molecule pharmacophores can improve binding ability. According to spectral results, 2-chloro-5-fluoronicotinic acid modified BRC4 (1523-1537) has the most significant influence on the secondary structure of RAD51 (181-200); binding constant is 1.1×10<sup>4</sup> L·mol<sup>-1</sup>. Cell experiments showed that BRC4 (1523-1537) modified with nicotinic acid N-oxide had the best inhibitory effect on the proliferation of MDA-MB-231 cells.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"49 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608759","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}
P. Yu. Mylnikov, A. V. Shchulkin, S. V. Seleznev, S. K. Pravkin, Yu. V. Abalenikhina, E. N. Yakusheva
{"title":"Development and Validation of a Method for Quantification of Lisinopril, Indapamide, Metoprolol, Valsartan, and Amoldipine in Human Blood Serum by HPLC-MS/MS","authors":"P. Yu. Mylnikov, A. V. Shchulkin, S. V. Seleznev, S. K. Pravkin, Yu. V. Abalenikhina, E. N. Yakusheva","doi":"10.1007/s11094-024-03171-5","DOIUrl":"https://doi.org/10.1007/s11094-024-03171-5","url":null,"abstract":"<p>A method for quantification of antihypertensive drugs (lisinopril, indapamide, metoprolol, valsartan, and amlodipine) in human blood serum was developed using high-performance liquid chromatography with tandem mass spectrometric detection (HPLC-MS/MS). MeOH with added fexofenadine hydrochloride as an internal standard was used for sample preparation. The developed method was validated for the following parameters: selectivity, limit of quantitation, linearity, intra- and inter-run accuracy and precision, sample transfer, matrix effect, extraction effect, and sample stability. The analytical range of the method for all analytes was 1 – 1000 ng/mL, which made it possible to assess the patient adherence to treatment and conduct therapeutic drug monitoring.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"39 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141608760","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}