International Journal of Peptide Research and Therapeutics最新文献

Synthetic studies of the mutant proinsulin syndrome demonstrate correlation between folding efficiency and age of diabetes onset.

IF 2 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2025-01-01 Epub Date: 2024-11-20 DOI: 10.1007/s10989-024-10665-z

Balamurugan Dhayalan, Yen-Shan Chen, Chun-Lun Ni, Michael A Weiss

{"title":"Synthetic studies of the mutant proinsulin syndrome demonstrate correlation between folding efficiency and age of diabetes onset.","authors":"Balamurugan Dhayalan, Yen-Shan Chen, Chun-Lun Ni, Michael A Weiss","doi":"10.1007/s10989-024-10665-z","DOIUrl":"10.1007/s10989-024-10665-z","url":null,"abstract":"<p><strong>Purpose: </strong>Heterozygous mutations in the insulin gene can give rise to a monogenic diabetes syndrome due to toxic misfolding of the variant proinsulin in the endoplasmic reticulum (ER) of pancreatic β-cells. Clinical mutations are widely distributed in the sequence (86 amino acids). Misfolding induces chronic ER stress and interferes in <i>trans</i> with wildtype biosynthesis and secretion. In the present work we sought to study relative folding efficiencies of proinsulin variants in relation to age of disease onset.</p><p><strong>Methods: </strong>To enable efficient preparation of non-foldable variants, we developed a four-segment native chemical-ligation scheme that exploits two native cysteines (Cys<sup>B19</sup> and Cys<sup>A6</sup>; residues 19 and 71 in proinsulin) and an alanine in the connecting domain (Ala<sup>C20</sup>; residue 50). From N- to C terminus, the four segments have respective lengths 18, 31, 22 and 15 residues-convenient to \"mix and match\" native and variant synthetic segments as a platform technology.</p><p><strong>Results: </strong>Folding of the reduced and unfolded polypeptides was investigated under three conditions: pH 10.6 (which promotes disulfide pairing as in the pharmaceutical manufacture of insulin) and pH 7.4 in the absence or presence of \"foldase\" protein disulfide isomerase. Whereas wild-type proinsulin efficiently folds to form a single dominant product (in accordance with classical studies), the clinical variants exhibited marked impairment, especially at neutral pH.</p><p><strong>Conclusion: </strong>Among representative clinical variants, relative folding yields correlated with both degree of ER stress in cell culture and ages of clinical diabetes onset (neonatal, adolescence or adulthood). Implications for the native mechanism of nascent protein folding are discussed.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"31 1","pages":""},"PeriodicalIF":2.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11759498/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143046642","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Molecular Chimera in Cancer Drug Discovery: Beyond Antibody Therapy, Designing Grafted Stable Peptides Targeting Cancer.

IF 2 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2025-01-01 Epub Date: 2025-02-17 DOI: 10.1007/s10989-025-10690-6

Arpan Chowdhury, Prajesh Shrestha, Seetharama D Jois

{"title":"Molecular Chimera in Cancer Drug Discovery: Beyond Antibody Therapy, Designing Grafted Stable Peptides Targeting Cancer.","authors":"Arpan Chowdhury, Prajesh Shrestha, Seetharama D Jois","doi":"10.1007/s10989-025-10690-6","DOIUrl":"10.1007/s10989-025-10690-6","url":null,"abstract":"<p><strong>Background: </strong>Several cancer therapies are being developed, and given the variability of different cancer types, the goal of these therapies is to remove the invasive tumor from the body, kill the cancer cells, or else retard the growth. These include chemotherapeutic agents and targeted therapy using small molecules and antibodies. However, antibodies can generate an immune response upon repeated administration, and producing antibodies could be expensive.</p><p><strong>Purpose: </strong>The purpose of this review is to describe different therapeutic approaches utilized for cancer therapy, the current therapeutic approaches, and their limitations. As a novel strategy to combat cancer, designing new stable peptide scaffolds such as cyclotides and sunflower trypsin inhibitors (SFTI) is described.</p><p><strong>Results: </strong>Stable peptides that can target proteins can be used as therapeutic agents. Here, we review the utilization and amalgamation of plant-based peptides with biological epitopes in designing molecules called \"Molecular Chimeras\" using a grafted peptide strategy. These cyclic peptides can bind to target receptors or modulate protein-protein interactions as they bind with high affinity and selectivity. Grafted peptides also possess better serum stability owing to the head-to-tail cyclization and other structural modifications.</p><p><strong>Conclusion: </strong>Stable cyclic peptides outweigh the other biologicals in terms of stability and manufacturing process. Peptides and peptidomimetics can be used as therapeutic agents, and these molecules provide alternatives for biologicals and small molecule inhibitors as drugs.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"31 3","pages":"38"},"PeriodicalIF":2.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11832722/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143457999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Isolation of Peptide Ligands for the HIV Capsid Protein p24 by Phage-Display.

IF 2 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2025-01-01 Epub Date: 2025-02-07 DOI: 10.1007/s10989-025-10696-0

Jerry Woo, Emily Orozco, Srinivas S Thota, Maede Chabi, Katerina Kourentzi, Richard Willson, Brian K Kay

{"title":"Isolation of Peptide Ligands for the HIV Capsid Protein p24 by Phage-Display.","authors":"Jerry Woo, Emily Orozco, Srinivas S Thota, Maede Chabi, Katerina Kourentzi, Richard Willson, Brian K Kay","doi":"10.1007/s10989-025-10696-0","DOIUrl":"10.1007/s10989-025-10696-0","url":null,"abstract":"<p><strong>Purpose: </strong>Isolate renewable and cost-efficient affinity reagents that will facilitate the detection of p24, the capsid protein of Human Immunodeficiency Virus (HIV), by screening phage-displayed combinatorial peptide libraries and identifying peptide ligands.</p><p><strong>Method: </strong>Four in-house combinatorial peptide libraries were screened for binders in three progressive rounds against monomeric p24 protein. Peptide binders were characterized by ELISA and Surface Plasmon Resonance (SPR) and one peptide sequence was evaluated in a lateral flow assay (LFA).</p><p><strong>Result: </strong>We identified 26 unique peptide sequences that exhibit varying phage ELISA signals above background for p24. We subsequently validated the binding of one linear and two cyclized peptide sequences with synthetic peptides. Alanine-scanning identified several residues critical to binding in the linear peptide. The linear peptide could be used for p24 detection in ELISA and LFAs.</p><p><strong>Conclusion: </strong>Phage-displayed combinatorial peptide libraries are suitable for isolation of binders against p24 and potentially other targets. Upon identification of a minimal binding sequence, the subsequent characterization and future optimization of it can lead to a variety of diagnostic assays.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"31 2","pages":"32"},"PeriodicalIF":2.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11805844/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143382409","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthetic Short Cryptic Antimicrobial Peptides as Templates for the Development of Novel Biotherapeutics Against WHO Priority Pathogen 以合成短隐性抗菌肽为模板，开发针对世界卫生组织重点病原体的新型生物治疗药物

IF 2.5 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2024-09-12 DOI: 10.1007/s10989-024-10632-8

Manjul Lata, Vrushti Telang, Pooja Gupta, Garima Pant, Mitra Kalyan, Jesu Arockiaraj, Mukesh Pasupuleti

{"title":"Synthetic Short Cryptic Antimicrobial Peptides as Templates for the Development of Novel Biotherapeutics Against WHO Priority Pathogen","authors":"Manjul Lata, Vrushti Telang, Pooja Gupta, Garima Pant, Mitra Kalyan, Jesu Arockiaraj, Mukesh Pasupuleti","doi":"10.1007/s10989-024-10632-8","DOIUrl":"https://doi.org/10.1007/s10989-024-10632-8","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>The emergence of multidrug-resistant pathogens through excessive and indiscriminate use of antibiotics, together with the lack of highly efficient treatment options for bacterial infections, has raised the development of novel antimicrobial agents to top priority. In this context, cryptic host defense peptides (cHDPs) are being explored as a novel class of antimicrobial agents. In this study, short peptides were designed from the long nonantibacterial protein ToAP2 and analysed for their positive net charge, hydrophobicity, hydrophobic moment, hydrophobic and hydrophilic planes.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>From the designed fragments, five 15 amino acid fragments were synthesised by solid-phase peptide synthesis (SPPS) and analysed for antimicrobial activity against ESKAPE pathogens. All the peptides were subject to cytotoxicity, mode of action, structure and function studies to find the best template for further optimisation.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>Among them, two peptides, FKL15 and SKL15, showed better efficiency in killing P. aeruginosa under physiological salt and plasma conditions with no cytotoxicity issues. Further, the peptides destroyed the bacterial membranes and adopted a random coil structure in the presence of the bacteria.</p><h3 data-test=\"abstract-sub-heading\">Conclusions</h3><p>The data indicates that FKL15 and SKL15 are promising antimicrobial peptides against antibiotic-resistant bacteria with great potential to develop as drugs with high economic value.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"107 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142176854","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Molecular Mechanism of NL13 Peptide of Adenosyl Homocysteinase Against ER Stress through Nrf2 Signaling Cascade 腺苷同型半胱氨酸酶 NL13 肽通过 Nrf2 信号级联对抗 ER 压力的分子机制

IF 2.5 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2024-09-12 DOI: 10.1007/s10989-024-10637-3

Purabi Sarkar, Karan Naresh Amin, Ranjith Balakrishnan, Kunka Mohanram Ramkumar, Jesu Arockiaraj

{"title":"Molecular Mechanism of NL13 Peptide of Adenosyl Homocysteinase Against ER Stress through Nrf2 Signaling Cascade","authors":"Purabi Sarkar, Karan Naresh Amin, Ranjith Balakrishnan, Kunka Mohanram Ramkumar, Jesu Arockiaraj","doi":"10.1007/s10989-024-10637-3","DOIUrl":"https://doi.org/10.1007/s10989-024-10637-3","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Purpose</h3><p>This study investigates the regulatory role of NL13, a compound derived from adenosyl homocysteinase of cyanobacteria, on ER stress-induced apoptosis in endothelial cells by modulating the Keap1-Nrf2 signaling pathway.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>Human endothelial cells (EA.hy926) were exposed to thapsigargin (TPG) to induce ER stress and then pretreated with varying concentrations of NL13. The study employed qPCR to assess changes in gene expression related to ER stress markers (GRP78, CHOP, ATF6, and PERK) and Nrf2. Additionally, reactive oxygen species (ROS) levels and the expression of apoptotic proteins (Bcl2 and Bax) were evaluated. In-silico molecular docking was used to explore potential interactions between NL13 and Keap1-Nrf2.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>NL13 significantly reduced oxidative and ER stress in endothelial cells. It downregulated ER stress markers (GRP78, CHOP, ATF6, PERK) while upregulating Nrf2 expression. NL13 also decreased ROS formation and modulated the expression of apoptotic proteins, increasing Bcl2 and decreasing Bax. Molecular docking revealed interactions of NL13 with critical amino acids in Keap1-Nrf2, suggesting a functional binding that enhances Nrf2 signaling.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>NL13 exerts cytoprotective effects against ER stress in endothelial cells by modulating the Keap1-Nrf2 signaling pathway and reducing apoptosis. These findings highlight the potential of NL13 as a therapeutic agent for conditions involving ER stress and oxidative damage. </p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"385 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142176855","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Unlocking the Potential of Retro-Inverso (RI) Peptides as Future Drug Candidates 挖掘逆转录病毒 (RI) 多肽作为未来候选药物的潜力

IF 2.5 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2024-09-10 DOI: 10.1007/s10989-024-10639-1

Othman Al Musaimi

{"title":"Unlocking the Potential of Retro-Inverso (RI) Peptides as Future Drug Candidates","authors":"Othman Al Musaimi","doi":"10.1007/s10989-024-10639-1","DOIUrl":"https://doi.org/10.1007/s10989-024-10639-1","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>With the rising demand for peptide-based drugs, enhancing their stability against proteolytic degradation has become a critical challenge. Strategies to improve peptide stability include cyclization, substitution of L-amino acids with D-amino acids, incorporation of β-amino acids, and various formulation techniques. An innovative approach involves modifying the peptide backbone by reversing the amide bond direction and inverting the stereochemistry of amino acids in the same segment. This approach results in the formation of retro-inverso peptides, which offer increased stability, permeability, and cellular uptake.</p><h3 data-test=\"abstract-sub-heading\">Purpose</h3><p>The aim of this review is to provide a comprehensive analysis of retro-inverso peptides, focusing on their concept, synthesis, and applications as potential therapeutic agents, drug delivery systems, and in aesthetic applications.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>The review explores the theoretical underpinnings of retro-inverso peptide design and its application to both linear and cyclic peptides. The synthesis strategies of retro-inverso peptides are discussed in detail, along with their formulation and practical utility in various biomedical fields.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>Retro-inverso peptides show promise in enhancing peptide stability and improving biological properties such as permeability and cellular uptake. Their unique structure offers advantages in drug development and potential as therapeutic agents or drug carriers.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>Retro-inverso peptides represent a valuable strategy for overcoming the limitations of conventional peptides, especially regarding stability and bioavailability. This review highlights their potential in therapeutic development and other applications, reinforcing the importance of continued research and innovation in peptide chemistry.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"9 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2024-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142176856","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Chitosan-Coated Scorpion Venom Ameliorates Acute Lung Injury Caused by Klebsiella Pneumoniae 壳聚糖包裹的蝎毒可改善肺炎克雷伯氏菌引起的急性肺损伤

IF 2.5 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2024-09-03 DOI: 10.1007/s10989-024-10635-5

Burak Oskay, Kazim Sahin, Figen Caliskan, Tolga Mercantepe, Sena Sahin Aktura, Levent Tumkaya, Atilla Topcu, Adnan Yilmaz, Sibel Mataraci Karakas, Zihni Acar Yazici

{"title":"Chitosan-Coated Scorpion Venom Ameliorates Acute Lung Injury Caused by Klebsiella Pneumoniae","authors":"Burak Oskay, Kazim Sahin, Figen Caliskan, Tolga Mercantepe, Sena Sahin Aktura, Levent Tumkaya, Atilla Topcu, Adnan Yilmaz, Sibel Mataraci Karakas, Zihni Acar Yazici","doi":"10.1007/s10989-024-10635-5","DOIUrl":"https://doi.org/10.1007/s10989-024-10635-5","url":null,"abstract":"<p>Nosocomial infections caused by antibiotic-resistant bacteria result in significant economic costs and human health issues, including acute lung injury. The purpose of this study was to investigate the scorpion venom in countering lung injury induced by bacterial sepsis. <i>Androctonus crassicauda</i> (Acra) scorpion venom was fractionated using HPLC and tested against bacteria. The anti-bacterial fraction obtained at 36th min (AcraX) was used to generate chitosan-coated particles. Following induction of sepsis in rats, they were administered venom on the sixth hour and sacrificed at 24 h. Lung tissues were used for histopathological analyses and after homogenization, for cytokine (TNF-α, IL-1β, IL-6, and IL-10) measurements by ELISA. Immunohistochemical examinations were performed in terms of extracellular matrix and fibrosis using anti-MMP-2 and MMP-9 antibodies. Among the bacterial strains used in our research for the antibacterial effect of AcraX (<i>S.aureus</i>,<i> K.pneumoniae</i>,<i> A.baumannii</i>,<i> and P.aeruginosa</i>), positive results were obtained only against <i>Klebsiella pneumoniae</i>. The regenerative effect of the venom against lesions developed in tissue and HeLa cell line was also observed. 100% vitality was achieved in the HeLa cell line exposed to the venom. This was also observed histologically via changes in the alveolar septa in lung tissue sections and a decrease in areas of inflammation and the hyaline membrane structure in the sepsis group. In conclusion, Acra venom acts as an efficient anti-inflammatory agent against <i>K. pneumoniae</i> induced pneumoniae.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"53 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2024-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142176858","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Potential and Limitation of Peptides from Native Plants of Uttarakhand 北阿坎德邦本土植物肽的潜力和局限性

IF 2.5 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2024-09-03 DOI: 10.1007/s10989-024-10634-6

Neha Kamboj, Rahul Kumar, Navin Kumar, Pankaj Gautam

{"title":"Potential and Limitation of Peptides from Native Plants of Uttarakhand","authors":"Neha Kamboj, Rahul Kumar, Navin Kumar, Pankaj Gautam","doi":"10.1007/s10989-024-10634-6","DOIUrl":"https://doi.org/10.1007/s10989-024-10634-6","url":null,"abstract":"<p>Knowledge of plant-based medicines in the Uttarakhand region is extensive, and these remedies are utilized for preventive and curative purposes. Traditional medical knowledge and herbal remedies form the backbone of primary health care system. The native plants in Uttarakhand are essential to the local tribes because they can produce food and medicine. Examples include Buransh (<i>Rhododendron</i>) flowers, Sal (<i>Shorea robusta</i>), Chora (<i>Angelica glauca</i>), Timuru (<i>Zanthoxylum armatum</i>), Jatamansi (<i>Nardostachys</i>), Kutki (<i>Picrorhiza kurroa</i>), Brahma Kamal (<i>Saussurea obvallata</i>). The diverse range of plants in this area may be explored for antimicrobial peptides (AMPs) or proteins that can serve as alternative treatments to combat resistant Gram-positive and Gram-negative bacteria effectively. Given the ever-increasing drug resistance among clinical pathogens, the value of novel AMPs is particularly relevant. In plants, the distinguishing feature of antimicrobial peptides (AMPs) lies in the plentiful occurrence of cysteine residues, which contribute to the formation of numerous disulfide bonds. Several plant AMP families exist as defensins, hairpin-like peptides, thionins, knottin-type peptides (cyclic and linear), snakins, α-hairpins, and lipid transfer proteins. Some plants AMPs possess high levels of amino acids other than cysteine. Plant AMPs have the unique capability to cluster into distinct families and share conserved structural folds. Over time, computational approaches have gained prominence in understanding the crucial facets of antimicrobial peptides (AMPs). These approaches offer the advantage of reducing the time and expense associated with traditional wet lab experiments. Several databases and tools have been created to aid researchers in providing up-to-date details on AMPs. However, despite the growing possibility of AMP resources in biological repositories, locating plant-derived AMPs remains challenging.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"8 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2024-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142176859","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The Cytotoxic Effects of Turkish Bee Venom (Apis mellifera) on Selected Cancer Cell Lines 土耳其蜂毒（Apis mellifera）对部分癌细胞株的细胞毒性作用

IF 2.5 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2024-09-02 DOI: 10.1007/s10989-024-10631-9

Anara Babayeva, Esra Dibek, İbrahim Kıvrak, Bekir Çöl

{"title":"The Cytotoxic Effects of Turkish Bee Venom (Apis mellifera) on Selected Cancer Cell Lines","authors":"Anara Babayeva, Esra Dibek, İbrahim Kıvrak, Bekir Çöl","doi":"10.1007/s10989-024-10631-9","DOIUrl":"https://doi.org/10.1007/s10989-024-10631-9","url":null,"abstract":"<p>The prevalence of cancer is so high globally that it is imperative to identify effective treatments. The use of bee products in the field of cancer therapeutics has gained significant attention as a promising alternative. Female worker bees (<i>Apis mellifera</i>) produce bee venom, which contains a complex array of biologically active compounds, including enzymes and peptides. Bee venom exhibits a range of biological activities with potential human health benefits, which vary across bee species and geographic locations. The objective of this study was to investigate the cytotoxicity of Turkish bee venom for the first time on some of the selected cancer cell lines. Bee venom was collected and resuspended in water and ethanol. The study analyzed both forms of Turkish bee venom for major peptides and proteins using HPLC-VWD and SDS-PAGE. The major components identified were apamin, melittin, phospholipase A2, and hyaluronidase. Cytotoxic activities were evaluated on eight distinct cell lines (seven cancerous cells and one control) using MTT assays. The Turkish bee venom demonstrated cytotoxicity with 48-hour IC50 values of 14.8 ± 0.6, 5.7 ± 0.2, 8.1 ± 0.1, 7.1 ± 0.1, 8.5 ± 0.2, 7.2 ± 0.1, 7.9 ± 0.1, and 8.0 ± 0.1 µg/mL for Phoenix-AMPHO (CRL-3213), PC-3, Huh-7, Caco-2, HT-29, SW-48, CARM-L12 TG3, and A-673, respectively. The 72-hour IC50 values were 8.2 ± 0.2, 4.5 ± 0.3, 7.1 ± 0.1, 6.4 ± 0.1, 6.0 ± 0.3, 7.2 ± 0.1, 2.1 ± 0.1, and 6.0 ± 0.2 µg/mL, respectively. In conclusion, the study demonstrated that both forms of Turkish bee venom exhibited significant cytotoxic effects on the analyzed cancer cells. The cell lines CARM-L12 TG3, PC-3, and A-673 exhibited the most pronounced responses to the bee venom.</p>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"59 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2024-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142176857","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Kinetic and Thermodynamic Study of Margatoxin Peptide Interaction with Human Serum Albumin: Studied by Biophysical and Docking Methods Margatoxin 肽与人血清白蛋白相互作用的动力学和热力学研究：生物物理和对接方法研究

IF 2.5 4区生物学

International Journal of Peptide Research and Therapeutics Pub Date : 2024-08-29 DOI: 10.1007/s10989-024-10633-7

Faride Ranjbari, Ali Nosrat, Mohammad Zaefizadeh, Farzaneh Fathi

{"title":"Kinetic and Thermodynamic Study of Margatoxin Peptide Interaction with Human Serum Albumin: Studied by Biophysical and Docking Methods","authors":"Faride Ranjbari, Ali Nosrat, Mohammad Zaefizadeh, Farzaneh Fathi","doi":"10.1007/s10989-024-10633-7","DOIUrl":"https://doi.org/10.1007/s10989-024-10633-7","url":null,"abstract":"<p>The scorpion-derived peptide margatoxin (MgTx) can make it possible to create novel and targeted medications for treatment of cancer. In this study, for the first time, we report an investigation of the human serum albumin (HSA) protein interaction with MgTx in aqueous solution. For this, biophysical methods including spectral, surface plasmon resonance (SPR), zeta potential and also in silico molecular docking technique at physiological conditions were used for examining kinetic binding and thermodynamic data. This interaction was done for a series of MgTx concentrations at three temperatures. The comparison of the K<sub>D</sub> kinetic value at 308 ° K and 298 ° K in SPR and UV spectroscopy shows that the complex between the MgTx and HSA has high strength at lower temperatures. The resulted positive data for ΔH and ΔS show that the major interaction force involved in the formation of the MgTx/HSA complex is hydrophobic forces. Also, the decreasing of zeta-potential values by adding of MgTx concentrations confims that the MgTx molecules could bind to HSA more by hydrophobic forces. In addition, according to the docking results, there are a very small number of strong interactions such as hydrogen bonds and salt bridges compared to the hydrophobic forces in the HSA and MgTx interaction.</p><h3 data-test=\"abstract-sub-heading\">Graphical Abstract</h3>","PeriodicalId":14217,"journal":{"name":"International Journal of Peptide Research and Therapeutics","volume":"77 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2024-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142176860","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0