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Interaction mechanism between luteoloside and corn silk glycans and the synergistic role in hypoglycemic activity 木犀草苷与玉米丝糖的相互作用机制及其在降血糖活性中的协同作用
IF 4.8 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-16 DOI: 10.1007/s13659-024-00428-0
Shihui Qin, Yanlang Li, Huiyan Shao, Yang Yu, Yina Yang, Yi Zeng, Jia Huang, Jiang-miao Hu, Liu Yang
{"title":"Interaction mechanism between luteoloside and corn silk glycans and the synergistic role in hypoglycemic activity","authors":"Shihui Qin,&nbsp;Yanlang Li,&nbsp;Huiyan Shao,&nbsp;Yang Yu,&nbsp;Yina Yang,&nbsp;Yi Zeng,&nbsp;Jia Huang,&nbsp;Jiang-miao Hu,&nbsp;Liu Yang","doi":"10.1007/s13659-024-00428-0","DOIUrl":"10.1007/s13659-024-00428-0","url":null,"abstract":"<div><p>As the two most principal active substances in the corn silk, polysaccharides and flavonoids, the mechanism of interaction between them has been a topic of intense research. This study provides an in-depth investigation of the interaction mechanism between corn silk glycans and luteoloside (LUT) and the synergistic role that result from this interaction. The interaction mechanism was evaluated by isothermal titration calorimetry (ITC) and circular dichroism (CD), and the synergistic role was evaluated by the expression of glucose transporters (GLUT-1), insulin secretion and surface plasmon resonance (SPR). CD and ITC results indicated that the interaction between CSGs and LUT mainly driven by the Cotton effects, enthalpy and entropy-driven. This interaction precipitated the formation of complexes (CSGs/LUT complexes) between corn silk glycans (CSGs) with four different molecular weights and luteoloside (LUT). Furthermore, the CSGs and LUT play a synergistic role in glucose regulation through GLUT-1 expression and insulin secretion experiments, compared to single luteoloside group.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2024-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10789705/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139471429","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Neuroprotective properties of exosomes and chitosan nanoparticles of Tomafran, a bioengineered tomato enriched in crocins 富含鳄鱼毒素的生物工程番茄 Tomafran 的外泌体和壳聚糖纳米颗粒的神经保护特性。
IF 4.8 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-12 DOI: 10.1007/s13659-023-00425-9
Mikel Etxebeste-Mitxeltorena, Enrique Niza, Cristián Martinez Fajardo, Carmen Gil, Lourdes Gómez-Gómez, Ana Martinez, Oussama Ahrazem
{"title":"Neuroprotective properties of exosomes and chitosan nanoparticles of Tomafran, a bioengineered tomato enriched in crocins","authors":"Mikel Etxebeste-Mitxeltorena,&nbsp;Enrique Niza,&nbsp;Cristián Martinez Fajardo,&nbsp;Carmen Gil,&nbsp;Lourdes Gómez-Gómez,&nbsp;Ana Martinez,&nbsp;Oussama Ahrazem","doi":"10.1007/s13659-023-00425-9","DOIUrl":"10.1007/s13659-023-00425-9","url":null,"abstract":"<div><p>Saffron has many pharmacological properties in addition to being a frequently used food seasoning. Crocin and picrocrocin which accumulate in saffron stigma, are responsible for these pharmacological properties. These natural products have health‐promoting effects for the prevention and treatment of numerous diseases, including age‐related cognitive and memory disfunction. Currently, crocin and picrocrocin are obtained from saffron, considered as the spice with the highest price in the market. To develop an efficient and low‐cost approach to producing these compounds with high bioactivity, biosynthetic genes isolated from saffron can be exploited in the metabolic engineering of heterologous hosts and the production of crocins in productive crop plants. Recently, we engineered tomato fruit producing crocins (Tomafran). In this study, we demonstrated that crocin-rich extract, encapsulated in chitosan or in exosomes may function as a neuroprotective strategy. Crocins contained in the Tomafran extracts and much lower doses in chitosan nanoparticles or exosomes were enough to rescue the neuroblastoma cell line SH-SY5Y after damage caused by okadaic acid. Our results confirm the neuroprotective effect of Tomafran and its exosomes that may be useful for the delay or prevention of neurodegenerative disorders such as Alzheimer’s disease.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2024-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10784249/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139428840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Koningipyridines A and B, two nitrogen-containing polyketides from the fungus Trichoderma koningiopsis SC-5 Koningipyridines A 和 B,来自真菌 Trichoderma koningiopsis SC-5 的两种含氮多酮。
IF 4.8 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-11 DOI: 10.1007/s13659-024-00429-z
Weiwei Peng, Qi Huang, Xin Ke, Wenxuan Wang, Yan Chen, Zihuan Sang, Chen Chen, Siyu Qin, Yuting Zheng, Haibo Tan, Zhenxing Zou
{"title":"Koningipyridines A and B, two nitrogen-containing polyketides from the fungus Trichoderma koningiopsis SC-5","authors":"Weiwei Peng,&nbsp;Qi Huang,&nbsp;Xin Ke,&nbsp;Wenxuan Wang,&nbsp;Yan Chen,&nbsp;Zihuan Sang,&nbsp;Chen Chen,&nbsp;Siyu Qin,&nbsp;Yuting Zheng,&nbsp;Haibo Tan,&nbsp;Zhenxing Zou","doi":"10.1007/s13659-024-00429-z","DOIUrl":"10.1007/s13659-024-00429-z","url":null,"abstract":"<div><p>Two novel koninginin derivatives, koningipyridines A and B (<b>1</b> and <b>2</b>), along with four known compounds (<b>3˗6</b>) were isolated from the EtOAc extract of the endophytic fungus <i>Trichoderma koningiopsis</i> SC-5. Among them, koningipyridine A featured an unprecedented pentacyclic ketal skeleton with the formation of a fascinating 6/6/5/6/5 fused ring system and shared a characteristic pyridine core, which represents the first example of nitrogen-containing koninginin-type natural product. Moreover, koningipyridine B was the first member in the koninginin family sharing a unique 6/6/5 dihydropyridine skeleton, and it was suggested to be the critical biosynthetic precursor of koningipyridine A. The structures of <b>1</b> and <b>2</b> were elucidated by the interpretation of 1D and 2D NMR spectroscopy, HRESIMS data, as well as theoretical calculations of <sup>13</sup>C NMR and electronic circular dichroism (ECD). Moreover, all isolates were screened for antimicrobial activities against <i>Staphylococcus aureus</i>, MRSA, and <i>Escherichia coli</i> as well as the cytotoxic effects against three cancer cell lines (A549, Hela, and HepG2).</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2024-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10784257/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139416057","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Precision enzyme discovery through targeted mining of metagenomic data 通过有针对性地挖掘元基因组数据精准发现酶。
IF 4.8 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-11 DOI: 10.1007/s13659-023-00426-8
Shohreh Ariaeenejad, Javad Gharechahi, Mehdi Foroozandeh Shahraki, Fereshteh Fallah Atanaki, Jian-Lin Han, Xue-Zhi Ding, Falk Hildebrand, Mohammad Bahram, Kaveh Kavousi, Ghasem Hosseini Salekdeh
{"title":"Precision enzyme discovery through targeted mining of metagenomic data","authors":"Shohreh Ariaeenejad,&nbsp;Javad Gharechahi,&nbsp;Mehdi Foroozandeh Shahraki,&nbsp;Fereshteh Fallah Atanaki,&nbsp;Jian-Lin Han,&nbsp;Xue-Zhi Ding,&nbsp;Falk Hildebrand,&nbsp;Mohammad Bahram,&nbsp;Kaveh Kavousi,&nbsp;Ghasem Hosseini Salekdeh","doi":"10.1007/s13659-023-00426-8","DOIUrl":"10.1007/s13659-023-00426-8","url":null,"abstract":"<div><p>Metagenomics has opened new avenues for exploring the genetic potential of uncultured microorganisms, which may serve as promising sources of enzymes and natural products for industrial applications. Identifying enzymes with improved catalytic properties from the vast amount of available metagenomic data poses a significant challenge that demands the development of novel computational and functional screening tools. The catalytic properties of all enzymes are primarily dictated by their structures, which are predominantly determined by their amino acid sequences. However, this aspect has not been fully considered in the enzyme bioprospecting processes. With the accumulating number of available enzyme sequences and the increasing demand for discovering novel biocatalysts, structural and functional modeling can be employed to identify potential enzymes with novel catalytic properties. Recent efforts to discover new polysaccharide-degrading enzymes from rumen metagenome data using homology-based searches and machine learning-based models have shown significant promise. Here, we will explore various computational approaches that can be employed to screen and shortlist metagenome-derived enzymes as potential biocatalyst candidates, in conjunction with the wet lab analytical methods traditionally used for enzyme characterization.</p></div>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":""},"PeriodicalIF":4.8,"publicationDate":"2024-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10781932/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139416058","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Eco-friendly approaches to phytochemical production: elicitation and beyond. 植物化学物质生产的生态友好型方法:诱导及其他。
IF 4.7 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-10 DOI: 10.1007/s13659-023-00419-7
Kritika Jalota, Vikas Sharma, Chiti Agarwal, Suruchi Jindal
{"title":"Eco-friendly approaches to phytochemical production: elicitation and beyond.","authors":"Kritika Jalota, Vikas Sharma, Chiti Agarwal, Suruchi Jindal","doi":"10.1007/s13659-023-00419-7","DOIUrl":"10.1007/s13659-023-00419-7","url":null,"abstract":"<p><p>Highly ameliorated phytochemicals from plants are recognized to have numerous beneficial effects on human health. However, obtaining secondary metabolites directly from wild plants is posing a great threat to endangered plant species due to their over exploitation. Moreover, due to complicated structure and stereospecificity chemical synthesis of these compounds is a troublesome procedure. As a result, sustainable and ecofriendly in vitro strategy has been adopted for phytochemicals production. But, lack of fully differentiated cells lowers down cultured cells productivity. Consequently, for enhancing yield of metabolites produced by cultured plant cells a variety of methodologies has been followed one such approach includes elicitation of culture medium that provoke stress responses in plants enhancing synthesis and storage of bioactive compounds. Nevertheless, for conclusive breakthrough in synthesizing bioactive compounds at commercial level in-depth knowledge regarding metabolic responses to elicitation in plant cell cultures is needed. However, technological advancement has led to development of molecular based approaches like metabolic engineering and synthetic biology which can serve as promising path for phytochemicals synthesis. This review article deals with classification, stimulating effect of elicitors on cultured cells, parameters of elicitors and action mechanism in plants, modern approaches like metabolic engineering for future advances.</p>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":"5"},"PeriodicalIF":4.7,"publicationDate":"2024-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10776560/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139401356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Flavonoids as dual-target inhibitors against α-glucosidase and α-amylase: a systematic review of in vitro studies. 类黄酮作为α-葡萄糖苷酶和α-淀粉酶的双靶抑制剂:体外研究的系统回顾。
IF 4.7 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-08 DOI: 10.1007/s13659-023-00424-w
Thua-Phong Lam, Ngoc-Vi Nguyen Tran, Long-Hung Dinh Pham, Nghia Vo-Trong Lai, Bao-Tran Ngoc Dang, Ngoc-Lam Nguyen Truong, Song-Ky Nguyen-Vo, Thuy-Linh Hoang, Tan Thanh Mai, Thanh-Dao Tran
{"title":"Flavonoids as dual-target inhibitors against α-glucosidase and α-amylase: a systematic review of in vitro studies.","authors":"Thua-Phong Lam, Ngoc-Vi Nguyen Tran, Long-Hung Dinh Pham, Nghia Vo-Trong Lai, Bao-Tran Ngoc Dang, Ngoc-Lam Nguyen Truong, Song-Ky Nguyen-Vo, Thuy-Linh Hoang, Tan Thanh Mai, Thanh-Dao Tran","doi":"10.1007/s13659-023-00424-w","DOIUrl":"10.1007/s13659-023-00424-w","url":null,"abstract":"<p><p>Diabetes mellitus remains a major global health issue, and great attention is directed at natural therapeutics. This systematic review aimed to assess the potential of flavonoids as antidiabetic agents by investigating their inhibitory effects on α-glucosidase and α-amylase, two key enzymes involved in starch digestion. Six scientific databases (PubMed, Virtual Health Library, EMBASE, SCOPUS, Web of Science, and WHO Global Index Medicus) were searched until August 21, 2022, for in vitro studies reporting IC<sub>50</sub> values of purified flavonoids on α-amylase and α-glucosidase, along with corresponding data for acarbose as a positive control. A total of 339 eligible articles were analyzed, resulting in the retrieval of 1643 flavonoid structures. These structures were rigorously standardized and curated, yielding 974 unique compounds, among which 177 flavonoids exhibited inhibition of both α-glucosidase and α-amylase are presented. Quality assessment utilizing a modified CONSORT checklist and structure-activity relationship (SAR) analysis were performed, revealing crucial features for the simultaneous inhibition of flavonoids against both enzymes. Moreover, the review also addressed several limitations in the current research landscape and proposed potential solutions. The curated datasets are available online at https://github.com/MedChemUMP/FDIGA .</p>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":"4"},"PeriodicalIF":4.7,"publicationDate":"2024-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10772047/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139376993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antiproliferative polyketides from fungus Xylaria cf. Longipes SWUF08-81 in different culture media. 在不同培养基中从真菌 Xylaria cf. Longipes SWUF08-81 中提取的抗增殖多酮。
IF 4.7 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-06 DOI: 10.1007/s13659-023-00427-7
Kittiwan Sresuksai, Sasiphimol Sawadsitang, Phongphan Jantaharn, Pakin Noppawan, Audomsak Churat, Nuttika Suwannasai, Wiyada Mongkolthanaruk, Thanaset Senawong, Sarawut Tontapha, Pairot Moontragoon, Vittaya Amornkitbamrung, Sirirath McCloskey
{"title":"Antiproliferative polyketides from fungus Xylaria cf. Longipes SWUF08-81 in different culture media.","authors":"Kittiwan Sresuksai, Sasiphimol Sawadsitang, Phongphan Jantaharn, Pakin Noppawan, Audomsak Churat, Nuttika Suwannasai, Wiyada Mongkolthanaruk, Thanaset Senawong, Sarawut Tontapha, Pairot Moontragoon, Vittaya Amornkitbamrung, Sirirath McCloskey","doi":"10.1007/s13659-023-00427-7","DOIUrl":"10.1007/s13659-023-00427-7","url":null,"abstract":"<p><p>Bioactive compounds from the wood-decay fungus Xylaria cf. longipes SWUF08-81, cultivated in three different culture media (GM, YM and PDB), were isolated. Their structures and stereochemistry were deduced from spectroscopic and MS data analysis, together with quantum chemical calculations of <sup>13</sup>C NMR chemical shifts and electronic circular dichroism (ECD) spectra. Five undescribed polyketides including dibenzofuran (1), mellein (2), dihydroisocoumarin (15), and two pyrans (16, 17), together with twenty-three compounds were determined. Compounds 18 and 20 were significantly toxic against cancer cell lines (HCT116, HT29, MCF-7 and HeLa) based on the MTT assay. Quantification by HPLC showed that 18 was produced three-fold higher in the broth of PDB than YM. These studies showed that the production of different compounds were primarily dependent on nutrition sources and it has given a starting point for the growth optimization conditions for the scaling up of bioactive compounds production.</p>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":"6"},"PeriodicalIF":4.7,"publicationDate":"2024-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10770013/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139105740","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Modulation of mitochondrial activity by sugarcane (Saccharum officinarum L.) top extract and its bioactive polyphenols: a comprehensive transcriptomics analysis in C2C12 myotubes and HepG2 hepatocytes. 甘蔗(Saccharum officinarum L.)顶部提取物及其生物活性多酚对线粒体活性的调节:C2C12 肌管和 HepG2 肝细胞中的综合转录组学分析。
IF 4.7 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-05 DOI: 10.1007/s13659-023-00423-x
Kengo Iwata, Farhana Ferdousi, Yoshinobu Arai, Hiroko Isoda
{"title":"Modulation of mitochondrial activity by sugarcane (Saccharum officinarum L.) top extract and its bioactive polyphenols: a comprehensive transcriptomics analysis in C2C12 myotubes and HepG2 hepatocytes.","authors":"Kengo Iwata, Farhana Ferdousi, Yoshinobu Arai, Hiroko Isoda","doi":"10.1007/s13659-023-00423-x","DOIUrl":"10.1007/s13659-023-00423-x","url":null,"abstract":"<p><p>Age-related mitochondrial dysfunction leads to defects in cellular energy metabolism and oxidative stress defense systems, which can contribute to tissue damage and disease development. Among the key regulators responsible for mitochondrial quality control, peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α) is an important target for mitochondrial dysfunction. We have previously reported that bioactive polyphenols extracted from sugarcane top (ST) ethanol extract (STEE) could activate neuronal energy metabolism and increase astrocyte PGC-1α transcript levels. However, their potential impact on the mitochondria activity in muscle and liver cells has not yet been investigated. To address this gap, our current study examined the effects of STEE and its polyphenols on cultured myotubes and hepatocytes in vitro. Rhodamine 123 assay revealed that the treatment with STEE and its polyphenols resulted in an increase in mitochondrial membrane potential in C2C12 myotubes. Furthermore, a comprehensive examination of gene expression patterns through transcriptome-wide microarray analysis indicated that STEE altered gene expressions related to mitochondrial functions, fatty acid metabolism, inflammatory cytokines, mitogen-activated protein kinase (MAPK) signaling, and cAMP signaling in both C2C12 myotubes and HepG2 hepatocytes. Additionally, protein-protein interaction analysis identified the PGC-1α interactive-transcription factors-targeted regulatory network of the genes regulated by STEE, and the quantitative polymerase chain reaction results confirmed that STEE and its polyphenols upregulated the transcript levels of PGC-1α in both C2C12 and HepG2 cells. These findings collectively suggest the potential beneficial effects of STEE on muscle and liver tissues and offer novel insights into the potential nutraceutical applications of this material.</p>","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"14 1","pages":"2"},"PeriodicalIF":4.7,"publicationDate":"2024-01-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10766937/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139097102","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
β-carboline derivative Z86 attenuates colorectal cancer cell proliferation and migration by directly targeting PI3K β-咔啉衍生物 Z86 通过直接靶向 PI3K 抑制结直肠癌细胞的增殖和迁移
IF 4.7 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-03 DOI: 10.1007/s13659-023-00422-y
Shiyun Nie, Lizhong Chang, Ying Huang, Heyang Zhou, Qianqing Yang, Lingmei Kong, Yan Li
{"title":"β-carboline derivative Z86 attenuates colorectal cancer cell proliferation and migration by directly targeting PI3K","authors":"Shiyun Nie, Lizhong Chang, Ying Huang, Heyang Zhou, Qianqing Yang, Lingmei Kong, Yan Li","doi":"10.1007/s13659-023-00422-y","DOIUrl":"https://doi.org/10.1007/s13659-023-00422-y","url":null,"abstract":"<p>Phosphoinositide 3-kinase (PI3Ks) are lipid kinases widely involved in cell proliferation, metastasis and differentiation. Constitutive activation of the PI3K/Akt/mTOR signaling are well confirmed in colorectal cancers (CRCs). In this study, we identified isopropyl 9-ethyl-1-(naphthalen-1-yl)-9 H-pyrido[3,4-b] indole-3-carboxylate (Z86), as a novel PI3Kα inhibitor with the IC<sub>50</sub> value of 4.28 µM. The binding of Z86 to PI3Kα was further confirmed with DARTS and CETSA assay. Immunofluorescence analysis and western blotting data demonstrated that Z86 effectively attenuated PI3K/AKT pathway. Z86 caused dramatic proliferation inhibition of CRCs through G0/G1 cycle arrest rather than apoptosis induction. Besides, the migration of CRCs was also relieved by Z86. The present study not only identified Z86 as a novel PI3Kα inhibitor with potent inhibitory efficiency on PI3K-mediated CRCs growth and migration, but also elucidated a reasonable molecular mechanism of Z86 in the Wnt signaling pathway inhibition.</p><h3 data-test=\"abstract-sub-heading\">Graphical Abstract</h3>\u0000","PeriodicalId":718,"journal":{"name":"Natural Products and Bioprospecting","volume":"189 1","pages":""},"PeriodicalIF":4.7,"publicationDate":"2024-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139082280","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Disclosing the potential of Cupressus leylandii A.B. Jacks & Dallim, Eucalyptus globulus Labill., Aloysia citrodora Paláu, and Melissa officinalis L. hydrosols as eco-friendly antimicrobial agents. 揭示 Cupressus leylandii A.B. Jacks & Dallim、Eucalyptus globulus Labill.、Aloysia citrodora Paláu 和 Melissa officinalis L. 水溶液作为环保型抗菌剂的潜力。
IF 4.7 3区 化学
Natural Products and Bioprospecting Pub Date : 2024-01-02 DOI: 10.1007/s13659-023-00417-9
Heloísa H S Almeida, Pedro J L Crugeira, Joana S Amaral, Alírio E Rodrigues, Maria-Filomena Barreiro
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