{"title":"荆芥芦丁的抗菌和抗癌活性的综合分析","authors":"Sudhakar Chekuri , Sanjeeva Reddy Sirigiripeta , Sreenu Thupakula , Satyanarayana Swamy Vyshnava , Sultana Ayesha , Sai Bindu Karamthote Cheniya , Raghu Kuruva , Roja Rani Anupalli","doi":"10.1016/j.bbrc.2025.151833","DOIUrl":null,"url":null,"abstract":"<div><h3>Background</h3><div>Antibiotic resistance and cancer demand alternative therapeutic strategies. Rutin, a polyphenol from <em>Acalypha indica</em> L., exhibits notable antioxidant, antibacterial, and anticancer properties. This study isolates and evaluates rutin for its bioactivity.</div></div><div><h3>Methods</h3><div>Rutin was extracted using Soxhlet extraction, purified via column chromatography and HPLC, and characterized by HR-MS and NMR. Antibacterial activity was assessed by disc diffusion against <em>Staphylococcus aureus</em>, <em>Escherichia coli</em>, <em>Klebsiella pneumoniae</em>, and <em>Pseudomonas aeruginosa</em>. Cytotoxicity was tested on MCF-7 and MDA-MB-231 breast cancer cells. Molecular docking evaluated binding to human protein disulfide isomerase (PDI).</div></div><div><h3>Results</h3><div>Rutin showed antibacterial activity with inhibition zones of 5.0–9.2 mm, strongest against <em>S. aureus</em>. It exhibited dose- and time-dependent cytotoxicity with IC<sub>50</sub> values of 22.31 ± 1.28 μg/mL (MCF-7) and 20.43 ± 0.81 μg/mL (MDA-MB-231) at 24 h. Docking analysis revealed strong affinity to human PDI (−5.84 kcal/mol, Ki = 52.19 μM).</div></div><div><h3>Conclusions</h3><div>Rutin from <em>Acalypha indica</em> L. demonstrates significant antibacterial and anticancer activity, with strong PDI interaction, supporting its potential as a natural therapeutic agent.</div></div>","PeriodicalId":8779,"journal":{"name":"Biochemical and biophysical research communications","volume":"765 ","pages":"Article 151833"},"PeriodicalIF":2.5000,"publicationDate":"2025-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Rutin isolated from Acalypha indica L.: A comprehensive analysis of its antibacterial and anticancer activities\",\"authors\":\"Sudhakar Chekuri , Sanjeeva Reddy Sirigiripeta , Sreenu Thupakula , Satyanarayana Swamy Vyshnava , Sultana Ayesha , Sai Bindu Karamthote Cheniya , Raghu Kuruva , Roja Rani Anupalli\",\"doi\":\"10.1016/j.bbrc.2025.151833\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Background</h3><div>Antibiotic resistance and cancer demand alternative therapeutic strategies. Rutin, a polyphenol from <em>Acalypha indica</em> L., exhibits notable antioxidant, antibacterial, and anticancer properties. This study isolates and evaluates rutin for its bioactivity.</div></div><div><h3>Methods</h3><div>Rutin was extracted using Soxhlet extraction, purified via column chromatography and HPLC, and characterized by HR-MS and NMR. Antibacterial activity was assessed by disc diffusion against <em>Staphylococcus aureus</em>, <em>Escherichia coli</em>, <em>Klebsiella pneumoniae</em>, and <em>Pseudomonas aeruginosa</em>. Cytotoxicity was tested on MCF-7 and MDA-MB-231 breast cancer cells. Molecular docking evaluated binding to human protein disulfide isomerase (PDI).</div></div><div><h3>Results</h3><div>Rutin showed antibacterial activity with inhibition zones of 5.0–9.2 mm, strongest against <em>S. aureus</em>. It exhibited dose- and time-dependent cytotoxicity with IC<sub>50</sub> values of 22.31 ± 1.28 μg/mL (MCF-7) and 20.43 ± 0.81 μg/mL (MDA-MB-231) at 24 h. Docking analysis revealed strong affinity to human PDI (−5.84 kcal/mol, Ki = 52.19 μM).</div></div><div><h3>Conclusions</h3><div>Rutin from <em>Acalypha indica</em> L. demonstrates significant antibacterial and anticancer activity, with strong PDI interaction, supporting its potential as a natural therapeutic agent.</div></div>\",\"PeriodicalId\":8779,\"journal\":{\"name\":\"Biochemical and biophysical research communications\",\"volume\":\"765 \",\"pages\":\"Article 151833\"},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2025-04-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Biochemical and biophysical research communications\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0006291X25005479\",\"RegionNum\":3,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biochemical and biophysical research communications","FirstCategoryId":"99","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0006291X25005479","RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
摘要
抗生素耐药性和癌症需要替代治疗策略。芦丁是一种来自猕猴桃的多酚,具有显著的抗氧化、抗菌和抗癌特性。本研究分离并评价了芦丁的生物活性。方法采用索氏提取法提取芦丁,柱层析和高效液相色谱法纯化芦丁,并用HR-MS和NMR对芦丁进行表征。采用圆盘扩散法测定对金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌和铜绿假单胞菌的抑菌活性。对MCF-7和MDA-MB-231乳腺癌细胞进行细胞毒性试验。分子对接评价了与人蛋白二硫异构酶(PDI)的结合。结果芦丁对金黄色葡萄球菌的抑制范围为5.0 ~ 9.2 mm,抑菌活性最强。其细胞毒性表现出剂量依赖性和时间依赖性,24 h IC50值分别为22.31±1.28 μg/mL (MCF-7)和20.43±0.81 μg/mL (MDA-MB-231)。对接分析显示其对人PDI有较强的亲和力(−5.84 kcal/mol, Ki = 52.19 μM)。结论荆芥芦丁具有较强的抗菌和抗癌活性,与PDI有较强的相互作用,具有作为天然治疗药物的潜力。
Rutin isolated from Acalypha indica L.: A comprehensive analysis of its antibacterial and anticancer activities
Background
Antibiotic resistance and cancer demand alternative therapeutic strategies. Rutin, a polyphenol from Acalypha indica L., exhibits notable antioxidant, antibacterial, and anticancer properties. This study isolates and evaluates rutin for its bioactivity.
Methods
Rutin was extracted using Soxhlet extraction, purified via column chromatography and HPLC, and characterized by HR-MS and NMR. Antibacterial activity was assessed by disc diffusion against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. Cytotoxicity was tested on MCF-7 and MDA-MB-231 breast cancer cells. Molecular docking evaluated binding to human protein disulfide isomerase (PDI).
Results
Rutin showed antibacterial activity with inhibition zones of 5.0–9.2 mm, strongest against S. aureus. It exhibited dose- and time-dependent cytotoxicity with IC50 values of 22.31 ± 1.28 μg/mL (MCF-7) and 20.43 ± 0.81 μg/mL (MDA-MB-231) at 24 h. Docking analysis revealed strong affinity to human PDI (−5.84 kcal/mol, Ki = 52.19 μM).
Conclusions
Rutin from Acalypha indica L. demonstrates significant antibacterial and anticancer activity, with strong PDI interaction, supporting its potential as a natural therapeutic agent.
期刊介绍:
Biochemical and Biophysical Research Communications is the premier international journal devoted to the very rapid dissemination of timely and significant experimental results in diverse fields of biological research. The development of the "Breakthroughs and Views" section brings the minireview format to the journal, and issues often contain collections of special interest manuscripts. BBRC is published weekly (52 issues/year).Research Areas now include: Biochemistry; biophysics; cell biology; developmental biology; immunology
; molecular biology; neurobiology; plant biology and proteomics