The current proposal is designed as a first-in-human Phase 1 open-label, dose-escalation study to assess the safety, pharmacokinetics, and the maximum tolerated dose of DHM among healthy volunteers using a purified form of DHM from a local cGMP compliant source (Master Herbs, Inc).

开始日期2024-09-15

申办/合作机构

University of Southern California

JPRN-UMIN000042938

/ CompletedN/A

Investigation of ampelopsin absorption by different dosage forms: An open-label, randomized, three-drug, three-period, Latin square design, crossover study - Investigation of ampelopsin absorption by different dosage forms

开始日期2021-01-07

申办/合作机构

FANCL Corp.

NCT03606694

/ Active, not recruiting临床2期

Effect of Dihydromirycetin Administration on Glycemic Control, Insulin Sensitivity and Insulin Secretion in Patients With Type 2 Diabetes Mellitus

Dihydromyricetin has demonstrated promising effects in glycemic control, insulin sensitivity and insulin secretion, that above mentioned findings show that dihydromyricetin has an excellent potential effect in the treatment of type 2 diabetes mellitus patients.

开始日期2019-10-30

申办/合作机构

University of Guadalajara

100 项与二氢杨梅素相关的临床结果

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100 项与二氢杨梅素相关的转化医学

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100 项与二氢杨梅素相关的专利（医药）

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2,026

项与二氢杨梅素相关的文献（医药）

2025-12-31·Renal Failure

Dihydromyricetin protects against cisplatin-induced renal injury and mitochondria-mediated apoptosis via the EGFR/HSP27/STAT3 signaling pathway

Article

作者: Liu, Zhengye ; Ye, Weifeng ; Zhang, Gensheng ; Zhu, Runzhi ; Xu, Zheming ; Tao, Chang ; Chen, Zhenjie ; Lv, Zhisu ; Zhu, Bin ; Yan, Xiang ; Gong, Jianguang ; Han, Huirong ; Liu, Yang ; Zhang, Minjing ; Zhou, Suhan ; Zhang, Xue

BACKGROUNDCisplatin (CP) has been used as an effective chemotherapy drug for different types of cancers. Despite its therapeutic benefits, the clinical utility of CP is often hindered by adverse effects, notably acute kidney injury (AKI), which restricts its widespread application. Dihydromyricetin (DHM) is a flavonoid acquired from Ampelopsis grossedentata, exhibiting a range of pharmacological activities. The major objective of this research was to examine the possible molecular mechanism involved in CP-induced AKI and the protective function of DHM.METHODSIn this study, the protective function of DHM against CP-induced AKI was assessed in both mice and HK-2 cells. Kidney dysfunction parameters and renal morphology were evaluated to ascertain the extent of protection. Additionally, proteomics techniques were employed to investigate the protective effect of DHM and elucidate the underlying molecular mechanisms involved in mitigating CP-induced AKI. In addition, protein levels of epidermal growth factor receptor (EGFR), p-EGFR, heat shock protein 27 (HSP27), p-HSP27, STAT3, and p-STAT3 in renal tissues were investigated. Furthermore, an EGFR-blocking agent (gefitinib) or si-RNA of HSP27 was used to study the effects of inhibiting EGFR or HSP27 on CP-induced renal injury.RESULTSDHM decreased blood urea nitrogen (BUN) and creatinine in serum, alleviated renal morphological injury and downregulated the expression of CP-induced kidney injury molecule-1 and neutrophil gelatinase-related lipocalin. Proteomic data revealed HSP27 as a potential therapeutic target for AKI. DHM treatment resulted in the downregulation of EGFR, HSP27, and STAT3 phosphorylation, ultimately mitigating CP-induced AKI. In addition, the inhibition of EGFR or HSP27 reduced mitochondria-mediated apoptosis and CP-induced cell damage in HK-2 cells.CONCLUSIONSDHM effectively inhibited CP-induced oxidative stress, inflammation, and mitochondria-mediated apoptosis through the EGFR/HSP27/STAT3 pathway.

2025-07-01·European Journal of Pharmacology

Dihydromyricetin attenuates intervertebral disc degeneration by inhibiting NLRP3 inflammasome activation via the Keap1/Nrf2/HO-1 pathway

Article

作者: Zhang, Yuhang ; Guo, Di ; Hong, Hainan ; Xia, Tao

Intervertebral disc degeneration (IVDD) is a highly prevalent chronic degenerative condition that significantly compromises patients' quality of life. Currently employed clinical treatments include surgical intervention and symptom management strategies; however, effective pharmacological strategies are lacking. Dihydromyricetin (DHM) has remarkable anti-inflammatory and antioxidative properties. On the basis of these biological characteristics, we hypothesized that DHM might have therapeutic potential in IVDD through its anti-inflammatory effects. Network pharmacology analysis revealed 130 overlapping targets between DHM and IVDD, with the Kelch-like ECH-associated protein 1 (Keap1)/nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) signaling pathway emerging as a crucial regulatory axis. Experimental validation demonstrated that DHM treatment significantly ameliorated LSI-induced disc degeneration, as evidenced by reduced histopathological scores, upregulated expression of extracellular matrix (ECM) proteins. In vitro studies revealed that DHM effectively inhibited IL-1β-induced NOD-like receptor family pyrin domain containing 3 (NLRP3) inflammasome activation and pyroptosis by decreasing Keap1 expression and activating the Nrf2/HO-1 signaling pathway. Specific silencing of Nrf2 significantly attenuated the protective effects of DHM, further confirming the crucial role of the Keap1/Nrf2/HO-1 pathway in the therapeutic action of DHM. Through integrated network pharmacology analysis and experimental validation, this study demonstrated for the first time that DHM alleviates IVDD by inhibiting Keap1-mediated Nrf2 degradation and activating the Nrf2/HO-1 pathway to suppress NLRP3 inflammasome-mediated pyroptosis. Furthermore, these findings validate the therapeutic potential of natural bioactive compounds in IVDD, providing experimental evidence and a theoretical foundation for the development of novel therapeutic strategies against IVDD.

2025-07-01·Food Chemistry

Identifying key contributors to the sweet aftertaste of raw Pu-erh tea through analytical and sensory methods

Article

作者: Yi, Zhibiao ; Gu, Ying ; Yi, Lunzhao ; Yuan, Xiaoping ; Chen, Xian ; Chai, Chunrong ; Feng, Min ; Ruan, Linguang ; Hu, Yongdan

In this study, the key components contributing to raw Pu-erh tea (RAPT) sweet aftertaste were identified. Six RAPTs were investigated through sensory evaluation, mass spectrometry, and taste addition experiments, and 96 taste components of tea infusion were annotated and analyzed. Saliva analysis after drinking tea revealed that 27 components present in tea remained in the mouth. On the basis of the results of the multivariate statistical analyses, we hypothesized that alkaloids and flavonoids might influence the sweet aftertaste strength of RAPT. Finally, the results of the taste addition experiments revealed that theophylline and rutin are key components that significantly influence the sweet aftertaste intensity of the RAPT. This strategy can be used as a methodology for analyzing the taste of tea, and the results can provide an evaluation index for evaluating the quality of RAPT.

项与二氢杨梅素相关的新闻（医药）

2025-01-12

·CPHI制药在线

二氢杨梅素结构修饰研究进展

关注并星标CPHI制药在线二氢杨梅素是显齿蛇葡萄中最主要的黄酮类成分（结构式如下图所示，来源文献[3]），具有抗氧化、抗炎、抗病毒、抗癌、抗菌、抗疲劳、抗焦虑、降糖、保肝护肝、心脏保护、缓解阿尔茨海默病和缓解哮喘等作用，其安全性良好，大鼠与小鼠的急性口服毒性试验、长期毒性试验和基因毒性试验结果均为阴性。二氢杨梅素可制成片剂及胶囊用于解酒护肝；可作天然抗氧化剂以延缓衰老及保存食品；可作动物饲料的添加剂以增加肉质和缩短生长周期。二氢杨梅素的稳定性明显弱于其他黄酮类化合物，因为其具有6个羟基，特别是B环的羟基容易氧化，pH≥9、高温及光照均可加速其氧化，此外，肠黏膜通透性较低、体内半衰期短、药理活性不高及易变色等问题也限制了其开发利用。二氢杨梅素化学结构近年来，为了克服二氢杨梅素应用中存在的问题，研究者利用前药原理及拼合原理对二氢杨梅素进行改性，获得了一定的研究成果。二氢杨梅素自身具有大 π 键共轭体系及强配位氧原子等，其适宜的空间结构可与金属离子螯合，可将所得二氢杨梅素金属配合物添加到药品、食品及化妆品中，发挥其抗菌、抗氧化、抗衰老的作用。同时，二氢杨梅素含有6个羟基，具有一定的弱酸性，利用酯化反应改善其溶解性，进而提高在油脂中的抗氧化活性，可将二氢杨梅素酯化物应用到化妆品中提高抗氧化性、防皮肤衰老及减少添加抑菌防腐剂。目前，针对二氢杨梅素结构修饰的方法有化学法、微生物法、物理法、酶法等，因操作简便、易控制及成本低常使用化学法。利用化学法对二氢杨梅素结构修饰的着手点有：①通过酯化反应，可改善二氢杨梅素的脂溶性、抗氧化活性，进一步提高二氢杨梅素的生物活性。②通过酰化反应，可提高二氢杨梅素的脂溶性、抑菌性、抗氧化性等。③通过螯合反应，让金属离子与二氢杨梅素连接，使其抗氧化性提高。④通过糖苷化反应，可提高二氢杨梅素的稳定性和水溶性。 1、二氢杨梅素酯化物二氢杨梅素通过酯化可使其脂溶性增加，抗油脂氧化活性增加。有学者通过量子化学方法分析得出，二氢杨梅素结构中的6个羟基发生酯化反应的顺序为3-OH＞4'-OH＞5'-OH＞5-OH＞3'-OH＞7-OH，抗氧化能力的强弱为4'-OH≈5'-OH＞3'-OH＞7-OH＞5-OH＞3 -OH。表明二氢杨梅素在进行酯化反应设计时选择3-OH而保留4'-OH及5'-OH。研究表明，将醋酸酐和二氢杨梅素混合进行酯化反应，所得的二氢杨梅素酯化物的脂溶性提高。在溶于二氢杨梅素的吡啶溶液中加入月桂酰氯进行酯化，得到二氢杨梅素月桂酸酯，经证实，二氢杨梅素月桂酸酯能够持久稳定地在猪油中发挥抗氧化作用，且在猪油中的抗氧化能力比二氢杨梅素强。采用不同配比的乙酸酐与二氢杨梅素在磷酸为催化剂，丙酮和甲苯为溶剂的反应作用下合成不同酯化程度的二氢杨梅素酯，所得衍生物在猪油体系中具有较强的抗氧化作用，随酯化率升高，抗氧化性略有下降；但与二氢杨梅素相比，二氢杨梅素酯的抗氧化作用明显增强，表明酯化改变其脂溶性对其抗氧化作用有直接关系。 2、二氢杨梅素酰化物二氢杨梅素酰化后，其稳定性、抗氧化活性及抑菌活性明显改善。研究表明，二氢杨梅素乙酰化物比二氢杨梅素稳定性高，且在体内的作用时间延长。利用乙酸乙烯酯和二氢杨梅素发生酰化反应合成的二氢杨梅素酰化物，其脂溶性是二氢杨梅素的10倍，抗氧化活性也明显提高。对二氢杨梅素进行甲酰化结构修饰，合成的八种甲酯衍生物抗菌活性均优于二氢杨梅素，其中7，3'，4'三甲氧基二氢杨梅素的抗菌活性是二氢杨梅素的4倍。 3、二氢杨梅素金属配合物二氢杨梅素分子结构有较高的超离域度、完整的大π键共轭结构、强配位氧原子和合适的空间构型，可作为金属离子良好的螯合配体，并且螯合作用发生在3-羟基-4-羰基上或3'-，4'-酚羟基上从而消除金属离子对自由基氧化的催化作用。二氢杨梅素可与钴、镍、锌、铜等金属离子进行螯合反应，其清除自由基能力、抑菌杀菌能力及抗氧化能力提高。利用植物提取物中的二氢杨梅素合成相对纯的金纳米粒子可用于药物输送、组织/肿瘤成像、电化学免疫分析等。通过螯合反应得到二氢杨梅素-Co（Ⅱ）配合物，实验表明该配合物清除自由基的能力高于二氢杨梅素。有研究对合成的二氢杨梅素-Zn配合物、二氢杨梅素-Cr配合物和二氢杨梅素-VO配合物进行结构表征和生物活性试验，结果表明二氢杨梅素-VO配合物清除自由基能力最强，其他的作用效果差不多。利用二氢杨梅素和硝酸银等可合成二氢杨梅素-AgNPs，其抗真菌效果实验表明，二氢杨梅素-AgNPs对烟曲霉、黑曲霉、拟青霉、念珠菌均有抑制作用。此外，研究发现二氢杨梅素-Zn配合物稳定性、清除自由基能力、抑菌性方面均高二氢杨梅素。 4、二氢杨梅素糖苷化物糖苷化修饰具有以下优点，①可以改变药物分子的亲脂性、电性或空间立体位阻，从而改善药代动力学性质，增强生物活性；②糖苷化修饰后的化合物具有对某些类型细胞的特异性寻靶性质，提高了对作用受体亚型的选择性，从而可以大幅度降低毒副作用，改善疗效；③糖苷比其苷元更有利于药物的缓释吸收，且挥发性降低及稳定性增强；④糖苷化修饰的化合物大多水溶性增大，具有良好的内吸性，易于为人体接受、吸收，由此可大大提高生物利用度；⑤糖类亲水性强，透膜能力有限，通常在细胞表面及细胞间质发挥作用，因而可以降低常规药物的细胞内毒副作用；⑥在某些情况下糖基还可与前体药物发挥协同抗病毒作用。二氢杨梅素糖苷化物可提高亲水亲脂性、生物活性、选择特异性等，使得生物利用度提高。同时还能降低挥发性、毒副作用等，发挥协同作用抗病毒。但目前关于二氢杨梅素糖苷化物的研究比较少。研究报道，利用黑曲霉菌株产生的黄酮糖苷酶，在一定条件下与二氢杨梅素、蔗糖反应20h得到二氢杨梅素糖苷化物，其对糖尿病患者的血糖代谢作用明显。还有研究利用葡聚糖蔗糖酶合成了5 种二氢杨梅素糖苷化物（AMPLS-Gs），其中AMPLS-G1的水溶性、清除自由基能力及抗褐变能力明显提高，因此可将二氢杨梅素糖苷化物用于化妆品中起美白保湿的作用。参考资料 [1]毛敏,刘信平.二氢杨梅素衍生物的研究进展[J].云南化工,2020,47(06):19-20. [2]朱哲,杨悟新,强烈应,等.二氢杨梅素结构修饰研究进展[J].亚太传统医药,2012,8(04):172-174. [3]吴聪,王文茂,彭彩云,等.二氢杨梅素结构修饰及生物活性研究进展[J].天然产物研究与开发,2024,36(03):540-553. 作者简介小米虫，药品质量研究工作者，长期致力于药品质量研究及药品分析方法验证工作，现就职于国内某大型药物研发公司，从事药品检验分析及分析方法验证。 END 【智药研习社近期直播】来源：CPHI制药在线声明：本文仅代表作者观点，并不代表制药在线立场。本网站内容仅出于传递更多信息之目的。如需转载，请务必注明文章来源和作者。投稿邮箱：Kelly.Xiao@imsinoexpo.com ▼更多制药资讯，请关注CPHI制药在线▼ 点击阅读原文，进入智药研习社~

微生物疗法

2024-01-26

·PRNewswire

Three Journal of Pharmaceutical Analysis Studies Explore the Use of Traditional Chinese Medicine for Various Diseases

XI'AN, China, Jan. 26, 2024 /PRNewswire/ -- Despite demonstrating significant clinical efficacy against various diseases, the widespread use of Traditional Chinese Medicine (TCM) is still limited. This is mainly due to the complexity in their formulation and lack of sufficient pharmacological and safety-related data. To address this gap, a new issue of the Journal of Pharmaceutical Analysis presents three independent studies which assessed the potency of TCM-based compounds for various human diseases, along with their molecular mechanisms of action. Continue Reading Latest research unveils the potential of Traditional Chinese Medicine compounds for the treatment of human diseases The accumulation of excess fat in the liver leads to non-alcoholic fatty liver disease (NAFLD). Oridonin (ORI), a TCM derived from the Chinese herb Rabdosia rubescens, exhibits anti-inflammatory effects. An article available online on 21 August 2023 and published in Volume 13, Issue 11 of the journal in November 2023, now reveals that ORI regulates lipid homeostasis in the liver by maintaining the balance between triglyceride (TG) and phosphatidylethanolamine (PE), through modulation of adipose triglyceride lipase (ATGL) and ethanolamine phosphotransferase 1 (EPT1) expression via the liver X receptor alpha (LXRα) signaling pathway. "When the TG-PE lipid balance is disturbed, the seesaw tilts towards TG, increasing the risk of NAFLD. Restoring lipid homeostasis using compounds like oridonin can alleviate lipid accumulation and liver cytotoxicity," explains Professor Lan Tang. Tumor heterogeneity compromises the efficacy of radiotherapy for treating lung cancer. Radiosensitizers help prime tumor cells and improve their response to radiation. Now, in an article available online on 7 June 2023 and published in Volume 13, Issue 11 of the journal in November 2023, researchers found that ginsenoside Rg5 induced cell-cycle arrest and enhanced radiation-induced cell death. Ginsenoside Rg5 interacts with heat shock protein alpha (HSP90α) with high affinity and reduces the binding between HSP90 and cell division cycle 37 (CDC37), promoting HSP90-CDC37 client protein degradation. "Ginsenoside Rg5 can be potentially developed into a new drug for improving the sensitivity of lung cancer and other types of tumors to radiation therapy," the authors explain. Diabetic retinopathy (DR) is characterized by the activation of oxidative stress pathways in response to high glucose. In a study available online on 12 May 2023 and published in Volume 13, Issue 11 of the journal in November 2023, researchers synthesized a polymeric drug complex by combining a natural flavonoid antioxidant known as dihydromyricetin (DMY) with iron (Fe) ions in nano-coordinated polymer particles (NCPs). Fe-DMY NCPs can alleviate glucose-induced oxidative damage and reverse the pathological features of DR by decreasing the expression of key proteins involved in microvascular dysfunction. Fe-DMY NCPs could also inhibit the activation of Poldip2-Nox4-H2O2 signaling pathway and down-regulate important vascular function indicators such as VCAM-1, HIF-1α, and VEGF. Explaining its applications, the authors say, "We report for the first time the synthesis and validation of ultra-small Fe-DMY NCPs. Fe-DMY complexes bear the potential to alleviate the impact of DR on vision, thus improving the quality of life of affected individuals." These studies provide a scientific basis for the development of TCM-based compounds into effective targeted therapies for various diseases. Reference Titles of original papers: Oridonin restores hepatic lipid homeostasis in an LXRa-ATGL/EPT1 axis-dependent manner Ginsenoside Rg5 enhances the radiosensitivity of lung adenocarcinoma via reducing HSP90-CDC37 interaction and promoting client protein degradation Nanoscale coordination polymer Fe-DMY downregulating Poldip2-Nox4-H2O2 pathway and alleviating diabetic retinopathy Journal name: Journal of Pharmaceutical Analysis DOI: Media contact Mengjie Wang [email protected] Xi'an, China +86-(0)29-88960092 SOURCE Journal of Pharmaceutical Analysis

100 项与二氢杨梅素相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
2型糖尿病	临床2期	墨西哥	University of Guadalajara	2019-10-30
酒精相关疾病	临床1期	美国	University of Southern California	2024-09-15
酒精性肝疾病	临床1期	美国	University of Southern California	2024-09-15
流感病毒感染	临床前	中国	南方医科大学	2020-07-01