{"title":"微rna对糖尿病相关勃起功能障碍中内皮素受体表达的调控。","authors":"Haibo Li, Jinwei You, Jiao Cang, Yanchufei Zhang, Yuanfang Xiang, Chenchen Yu, Lianjun Pan, Qipeng Zhang, Feng Pan","doi":"10.1016/j.bcp.2025.117397","DOIUrl":null,"url":null,"abstract":"<p><p>Erectile dysfunction (ED) is one of the common complications of type 2 diabetes mellitus (T2DM), feathered by a complex vascular and endothelial pathogenesis and limited therapeutic options. Endothelin receptor type A (ETA), a key receptor for endothelin, mediates chronic and persistent contractile effects in the penile corpus cavernosum (CC), and is a potential target for ED treatment. Dysregulated microRNAs (miRNAs) have been implicated in the pathophysiology of ED, playing critical regulatory roles and suitable for drug development. This study investigates the role of dysregulated miRNAs in regulating the endothelin receptor type A gene (EDNRA) in T2DMED. We found that ETA levels were significantly higher in the CCs of T2DMED rats. Using artificial intelligence (AI)-assisted prediction algorithms, potential miRNAs targeting EDNRA were identified, and miRNA expression profiles in the CCs of control and T2DMED rats were analyzed using RNA-chip technology and testified by quantitative Polymerase Chain Reaction (qPCR). As a result, miR-30-5p and its families, miR-96-5p, and miR-27a-3p were significantly downregulated in the T2DMED group. Luciferase assays confirmed the inhibitory role of these miRNAs on the 3'-untranslated region (3'-UTR) of EDNRA. Hypoxia, a fundamental pathogenic factor in T2DMED, was shown to suppress miRNA expression and increase ETA expression in vitro in penile smooth muscle cells. Additionally, local lentiviral delivery of miR-30-5p in vivo significantly reduced ETA levels in the CCs of T2DMED rats and restored erectile function. In conclusion, downregulated miRNAs contribute to T2DMED pathogenesis by upregulating ETA expression. Targeting EDNRA-regulating miRNAs could offer a novel therapeutic approach for T2DMED.</p>","PeriodicalId":8806,"journal":{"name":"Biochemical pharmacology","volume":" ","pages":"117397"},"PeriodicalIF":5.6000,"publicationDate":"2025-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Regulation of endothelin receptor expression by microRNAs in diabetes related erectile dysfunction.\",\"authors\":\"Haibo Li, Jinwei You, Jiao Cang, Yanchufei Zhang, Yuanfang Xiang, Chenchen Yu, Lianjun Pan, Qipeng Zhang, Feng Pan\",\"doi\":\"10.1016/j.bcp.2025.117397\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Erectile dysfunction (ED) is one of the common complications of type 2 diabetes mellitus (T2DM), feathered by a complex vascular and endothelial pathogenesis and limited therapeutic options. Endothelin receptor type A (ETA), a key receptor for endothelin, mediates chronic and persistent contractile effects in the penile corpus cavernosum (CC), and is a potential target for ED treatment. Dysregulated microRNAs (miRNAs) have been implicated in the pathophysiology of ED, playing critical regulatory roles and suitable for drug development. This study investigates the role of dysregulated miRNAs in regulating the endothelin receptor type A gene (EDNRA) in T2DMED. We found that ETA levels were significantly higher in the CCs of T2DMED rats. Using artificial intelligence (AI)-assisted prediction algorithms, potential miRNAs targeting EDNRA were identified, and miRNA expression profiles in the CCs of control and T2DMED rats were analyzed using RNA-chip technology and testified by quantitative Polymerase Chain Reaction (qPCR). As a result, miR-30-5p and its families, miR-96-5p, and miR-27a-3p were significantly downregulated in the T2DMED group. Luciferase assays confirmed the inhibitory role of these miRNAs on the 3'-untranslated region (3'-UTR) of EDNRA. Hypoxia, a fundamental pathogenic factor in T2DMED, was shown to suppress miRNA expression and increase ETA expression in vitro in penile smooth muscle cells. Additionally, local lentiviral delivery of miR-30-5p in vivo significantly reduced ETA levels in the CCs of T2DMED rats and restored erectile function. In conclusion, downregulated miRNAs contribute to T2DMED pathogenesis by upregulating ETA expression. Targeting EDNRA-regulating miRNAs could offer a novel therapeutic approach for T2DMED.</p>\",\"PeriodicalId\":8806,\"journal\":{\"name\":\"Biochemical pharmacology\",\"volume\":\" \",\"pages\":\"117397\"},\"PeriodicalIF\":5.6000,\"publicationDate\":\"2025-10-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Biochemical pharmacology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1016/j.bcp.2025.117397\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biochemical pharmacology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.bcp.2025.117397","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Regulation of endothelin receptor expression by microRNAs in diabetes related erectile dysfunction.
Erectile dysfunction (ED) is one of the common complications of type 2 diabetes mellitus (T2DM), feathered by a complex vascular and endothelial pathogenesis and limited therapeutic options. Endothelin receptor type A (ETA), a key receptor for endothelin, mediates chronic and persistent contractile effects in the penile corpus cavernosum (CC), and is a potential target for ED treatment. Dysregulated microRNAs (miRNAs) have been implicated in the pathophysiology of ED, playing critical regulatory roles and suitable for drug development. This study investigates the role of dysregulated miRNAs in regulating the endothelin receptor type A gene (EDNRA) in T2DMED. We found that ETA levels were significantly higher in the CCs of T2DMED rats. Using artificial intelligence (AI)-assisted prediction algorithms, potential miRNAs targeting EDNRA were identified, and miRNA expression profiles in the CCs of control and T2DMED rats were analyzed using RNA-chip technology and testified by quantitative Polymerase Chain Reaction (qPCR). As a result, miR-30-5p and its families, miR-96-5p, and miR-27a-3p were significantly downregulated in the T2DMED group. Luciferase assays confirmed the inhibitory role of these miRNAs on the 3'-untranslated region (3'-UTR) of EDNRA. Hypoxia, a fundamental pathogenic factor in T2DMED, was shown to suppress miRNA expression and increase ETA expression in vitro in penile smooth muscle cells. Additionally, local lentiviral delivery of miR-30-5p in vivo significantly reduced ETA levels in the CCs of T2DMED rats and restored erectile function. In conclusion, downregulated miRNAs contribute to T2DMED pathogenesis by upregulating ETA expression. Targeting EDNRA-regulating miRNAs could offer a novel therapeutic approach for T2DMED.
期刊介绍:
Biochemical Pharmacology publishes original research findings, Commentaries and review articles related to the elucidation of cellular and tissue function(s) at the biochemical and molecular levels, the modification of cellular phenotype(s) by genetic, transcriptional/translational or drug/compound-induced modifications, as well as the pharmacodynamics and pharmacokinetics of xenobiotics and drugs, the latter including both small molecules and biologics.
The journal''s target audience includes scientists engaged in the identification and study of the mechanisms of action of xenobiotics, biologics and drugs and in the drug discovery and development process.
All areas of cellular biology and cellular, tissue/organ and whole animal pharmacology fall within the scope of the journal. Drug classes covered include anti-infectives, anti-inflammatory agents, chemotherapeutics, cardiovascular, endocrinological, immunological, metabolic, neurological and psychiatric drugs, as well as research on drug metabolism and kinetics. While medicinal chemistry is a topic of complimentary interest, manuscripts in this area must contain sufficient biological data to characterize pharmacologically the compounds reported. Submissions describing work focused predominately on chemical synthesis and molecular modeling will not be considered for review.
While particular emphasis is placed on reporting the results of molecular and biochemical studies, research involving the use of tissue and animal models of human pathophysiology and toxicology is of interest to the extent that it helps define drug mechanisms of action, safety and efficacy.