Chaowei Liang, Yongzhi Ma, Minni Ding, Fang Gao, Kewang Yu, Siyu Wang, Ying Qu, Huiming Hua, Dahong Li
{"title":"积雪草酸及其衍生物:药理学见解与应用","authors":"Chaowei Liang, Yongzhi Ma, Minni Ding, Fang Gao, Kewang Yu, Siyu Wang, Ying Qu, Huiming Hua, Dahong Li","doi":"10.1016/j.ejmech.2025.117429","DOIUrl":null,"url":null,"abstract":"<div><div><em>Centella asiatica</em> (L.) Urban has been utilized in wound healing remedies for nearly 3000 years. Asiatic acid (<strong>AA</strong>), a pentacyclic triterpenoid characterized by ursane-type skeleton, serves as principal bioactive constituent of <em>Centella asiatica</em>, exhibits remarkable therapeutic potential across a spectrum of health conditions. Pharmacological investigations have revealed that <strong>AA</strong> exerts direct regulatory effects on a multitude of enzymes, receptors, inflammatory mediators, and transcription factors. This article systematically examines the therapeutic applications of <strong>AA</strong> and its derivatives in the management of neurodegenerative diseases, cancer, cardiovascular disorders, and infections. Additionally, recent advancements in the structural modification of <strong>AA</strong> are summarized, offering new insights for the development of low-toxicity, effective <strong>AA</strong>-based therapeutics and diagnostic agents. However, several challenges remain, including the paucity of clinical trials, uncertainties in dosage and treatment regimens, limited data on long-term safety and side effects, and poor bioavailability. Addressing these limitations is crucial for advancing <strong>AA</strong>-based therapies and ensuring their clinical applicability.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"289 ","pages":"Article 117429"},"PeriodicalIF":6.0000,"publicationDate":"2025-02-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Asiatic acid and its derivatives: Pharmacological insights and applications\",\"authors\":\"Chaowei Liang, Yongzhi Ma, Minni Ding, Fang Gao, Kewang Yu, Siyu Wang, Ying Qu, Huiming Hua, Dahong Li\",\"doi\":\"10.1016/j.ejmech.2025.117429\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div><em>Centella asiatica</em> (L.) Urban has been utilized in wound healing remedies for nearly 3000 years. Asiatic acid (<strong>AA</strong>), a pentacyclic triterpenoid characterized by ursane-type skeleton, serves as principal bioactive constituent of <em>Centella asiatica</em>, exhibits remarkable therapeutic potential across a spectrum of health conditions. Pharmacological investigations have revealed that <strong>AA</strong> exerts direct regulatory effects on a multitude of enzymes, receptors, inflammatory mediators, and transcription factors. This article systematically examines the therapeutic applications of <strong>AA</strong> and its derivatives in the management of neurodegenerative diseases, cancer, cardiovascular disorders, and infections. Additionally, recent advancements in the structural modification of <strong>AA</strong> are summarized, offering new insights for the development of low-toxicity, effective <strong>AA</strong>-based therapeutics and diagnostic agents. However, several challenges remain, including the paucity of clinical trials, uncertainties in dosage and treatment regimens, limited data on long-term safety and side effects, and poor bioavailability. Addressing these limitations is crucial for advancing <strong>AA</strong>-based therapies and ensuring their clinical applicability.</div></div>\",\"PeriodicalId\":314,\"journal\":{\"name\":\"European Journal of Medicinal Chemistry\",\"volume\":\"289 \",\"pages\":\"Article 117429\"},\"PeriodicalIF\":6.0000,\"publicationDate\":\"2025-02-23\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0223523425001941\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0223523425001941","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Asiatic acid and its derivatives: Pharmacological insights and applications
Centella asiatica (L.) Urban has been utilized in wound healing remedies for nearly 3000 years. Asiatic acid (AA), a pentacyclic triterpenoid characterized by ursane-type skeleton, serves as principal bioactive constituent of Centella asiatica, exhibits remarkable therapeutic potential across a spectrum of health conditions. Pharmacological investigations have revealed that AA exerts direct regulatory effects on a multitude of enzymes, receptors, inflammatory mediators, and transcription factors. This article systematically examines the therapeutic applications of AA and its derivatives in the management of neurodegenerative diseases, cancer, cardiovascular disorders, and infections. Additionally, recent advancements in the structural modification of AA are summarized, offering new insights for the development of low-toxicity, effective AA-based therapeutics and diagnostic agents. However, several challenges remain, including the paucity of clinical trials, uncertainties in dosage and treatment regimens, limited data on long-term safety and side effects, and poor bioavailability. Addressing these limitations is crucial for advancing AA-based therapies and ensuring their clinical applicability.
期刊介绍:
The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers.
A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.