[Translation] A randomized, double-blind, placebo-controlled phase Ib clinical trial/extension study to evaluate the PK-PD characteristics, efficacy and safety of Leonurine Sulfate Tablets in patients with dyslipidemia

探索试验药（硫酸益母草碱片）用于治疗血脂异常患者的PK-PD特征；初步探索试验药（硫酸益母草碱片）用于治疗血脂异常患者的疗效和安全性。

[Translation]

Explore the PK-PD characteristics of the experimental drug (leonurine sulfate tablets) for the treatment of patients with dyslipidemia; Preliminary exploration of the efficacy and safety of the experimental drug (leonurine sulfate tablets) for the treatment of patients with dyslipidemia.

Start Date06 May 2022

Sponsor / Collaborator

Zhuhai Hengqin New Area Zhongzhu Zhengtai Med Mgmt Co., Ltd.

[+1]

CTR20191574 / CompletedPhase 1

评估硫酸益母草碱片在健康志愿者中安全性、耐受性、药代动力学和药效学动力学特性试验

[Translation] A study to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic properties of leonurine sulfate tablets in healthy volunteers

评估健康志愿者连续口服不同剂量硫酸益母草碱片的安全性、耐受性、药代动力学特性，为II期临床试验设计提供依据。评估健康志愿者连续口服不同剂量硫酸益母草碱片的药效动力学特性，探索硫酸益母草碱片对健康志愿者肠道菌群的影响，为II期临床试验及后期临床试验设计提供依据。

[Translation]

To evaluate the safety, tolerability and pharmacokinetic characteristics of different doses of Leonurine Sulfate Tablets in healthy volunteers, and provide a basis for the design of Phase II clinical trials. To evaluate the pharmacodynamic characteristics of different doses of Leonurine Sulfate Tablets in healthy volunteers, and explore the effect of Leonurine Sulfate Tablets on the intestinal flora of healthy volunteers, and provide a basis for the design of Phase II clinical trials and later clinical trials.

Start Date08 Aug 2019

Sponsor / Collaborator

Zhuhai Hengqin New Area Zhongzhu Zhengtai Med Mgmt Co., Ltd.

[+1]

CTR20190238 / CompletedPhase 1

随机、两周期、两序列、交叉、单剂量、单一中心，评估食物对硫酸益母草碱片剂药代动力学特性影响试验

[Translation] A randomized, two-period, two-sequence, crossover, single-dose, single-center trial to evaluate the effect of food on the pharmacokinetic properties of leonurine sulfate tablets

评估食物对硫酸益母草碱片剂药代动力学特性的影响，为后续临床试验给药方案设计提供依据。

[Translation]

To evaluate the effect of food on the pharmacokinetic properties of leonurine sulfate tablets and provide a basis for the design of dosing regimens in subsequent clinical trials.

Start Date21 Feb 2019

Sponsor / Collaborator

Zhuhai Hengqin New Area Zhongzhu Zhengtai Med Mgmt Co., Ltd.

[+1]

100 Clinical Results associated with Leonurine Sulfate

100 Translational Medicine associated with Leonurine Sulfate

100 Patents (Medical) associated with Leonurine Sulfate

182

Literatures (Medical) associated with Leonurine Sulfate

01 Dec 2024·Biomaterials

Injectable bioadhesive hydrogel as a local nanomedicine depot for targeted regulation of inflammation and ferroptosis in rheumatoid arthritis

Article

Author: Zhang, Kaibo ; Xie, Chaoming ; Yang, Runze ; Fu, Weili ; Yan, Liwei ; Lu, Xiong ; Xu, Tianhao

Medicine intervention is the major clinical treatment used to relieve the symptoms and delay the progression of rheumatoid arthritis (RA), but is limited by its poor targeted delivery and short therapeutic duration. Herein, we developed an injectable and bioadhesive gelatin-based (Gel) hydrogel as a local depot of leonurine (Leon)-loaded and folate-functionalized polydopamine (FA-PDA@Leon) nanoparticles for anti-inflammation and chondroprotection in RA. The nanoparticles could protect Leon and facilitate its entry into the M1 phenotype macrophage for intracellular delivery of Leon, while the hydrogel tightly adhered to the tissues in the joint cavity and prolonged the retention of FA-PDA@Leon nanoparticles, thus achieving higher availability and therapeutic efficiency of Leon. In vitro and in vivo experiments demonstrated that the Gel/FA-PDA@Leon hydrogel could strongly suppress the inflammatory response by down-regulating the JAK2/STAT3 signaling pathway in macrophages and protect the chondrocytes from ferritinophagy/ferroptosis. This contributed to maintaining the structural integrity of articular cartilage and accelerating the joint functional recovery. This work provides an effective and convenient strategy to achieve higher bioavailability and long-lasting therapeutic duration of medicine intervention in arthritis diseases.

25 Jul 2024·Frontiers in Bioscience-Landmark

Leonurine Ameliorates Diabetic Nephropathy through GPX4-Mediated Ferroptosis of Endothelial Cells

Article

Author: Chen, Xu ; Yin, Kai ; Yu, Xinyuan ; Zhu, Xiao ; Zhang, Yaoyuan ; Li, Yuan

BACKGROUNDDiabetic nephropathy (DN) is a common microvascular complication of diabetes mellitus (DM). Ferroptosis is an atypical form of iron-dependent, modulated cell death that has been shown to occur in human umbilical vein endothelial cells (HUVECs). Leonurine (LEO) is a single active ingredient extracted from Leonurus japonicus Houtt. It has various biological activities, including anti-inflammatory and anti-cancer effects. However, whether LEO affects ferroptosis in DN has yet to be investigated.METHODSAn animal model of DN was established by subjecting C57/BL6 mice to a high-fat diet (HFD) while being induced with Streptozotocin (STZ). A cellular model of DN was established by exposing HUVECs to a high glucose (HG) concentration of 30 mM.RESULTSLEO was found to improve DN and to attenuate the degree of glomerulosclerosis and tubular atrophy in the mouse model. Additionally, it markedly decreased the levels of ferroptosis markers. Molecular analyses revealed that LEO inhibited HG-induced oxidative stress in HUVECs, thereby decreasing endothelial cell (EC) dysfunction. Furthermore, LEO was found to reduce ferroptosis and reverse EC dysfunction by increasing the expression of glutathione peroxidase 4 (GPX4) and nuclear factor erythroid 2-related factor 2 (Nrf2). The suppression of Nrf2 in HG-induced HUVECs inhibited LEO-GPX4 axis-mediated ferroptosis and increased EC dysfunction.CONCLUSIONSLEO exerts anti-DN effects both in vivo and in vitro by suppressing GPX4-mediated EC ferroptosis. Mechanistically, LEO appears to induce Nrf2-mediated GPX4 expression to inhibit ferroptosis, thereby reducing EC dysfunction. This study provides a new perspective on the treatment of diseases using natural medicines. It involves a novel form of cell death that could potentially lead to better treatment of DN.

01 Jul 2024·Phytomedicine

A facile fluorescence-coupling approach to visualizing leonurine uptake and distribution in living cells and Caenorhabditis elegans

Article

Author: Zhou, Ziyuan ; Lin, Jiajie ; Li, Junjie ; Gao, Lei ; Hong, Xiaobing ; Shi, Hao ; Yan, Jinwu ; Yang, Jinrong ; Zhao, Jiamin ; Wong, Nai-Kei ; Li, Yiwen ; Wu, Chaofeng

BACKGROUNDCaenorhabditis elegans (C. elegans) has been recognized for being a useful model organism in small-molecule drug screens and drug efficacy investigation. However, there remain bottlenecks in evaluating such processes as drug uptake and distribution due to a lack of appropriate chemical tools.PURPOSEThis study aims to prepare fluorescence-labeled leonurine as an example to monitor drug uptake and distribution of small molecule in C. elegans and living cells.METHODSFITC-conjugated leonurine (leonurine-P) was synthesized and characterized by LC/MS, NMR, UV absorption and fluorescence intensity. Leonurine-P was used to stain C. elegans and various mammalian cell lines. Different concentrations of leonurine were tested in conjunction with a competing parent molecule to determine whether leonurine-P and leonurine shared the same biological targets. Drug distribution was analyzed by imaging. Fluorometry in microplates and flow cytometry were performed for quantitative measurements of drug uptake.RESULTSThe UV absorption peak of leonurine-P was 490∼495 nm and emission peak was 520 nm. Leonurine-P specifically bound to endogenous protein targets in C. elegans and mammalian cells, which was competitively blocked by leonurine. The highest enrichment levels of leonurine-P were observed around 72 h following exposure in C. elegans. Leonurine-P can be used in a variety of cells to observe drug distribution dynamics. Flow cytometry of stained cells can be facilely carried out to quantitatively detect probe signals.CONCLUSIONSThe strategy of fluorescein-labeled drugs reported herein allows quantification of drug enrichment and visualization of drug distribution, thus illustrates a convenient approach to study phytodrugs in pharmacological contexts.

100 Deals associated with Leonurine Sulfate

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hyperlipidemias	Phase 2	CN	Fudan University	-
Hyperlipidemias	Phase 2	CN	Zhuhai Hengqin New Area Zhongzhu Zhengtai Med Mgmt Co., Ltd.	-
Primary Hyperlipidemia	Phase 1	CN	Zhuhai Hengqin New Area Zhongzhu Zhengtai Med Mgmt Co., Ltd.	06 May 2022
Primary Hyperlipidemia	Phase 1	CN	Fudan University	06 May 2022

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