Arctigenin(Arctigenin) - 药物靶点：ADIPOR1 x PP2A_在研适应症：糖尿病肾病，炎症，花生过敏_专利_临床

概要

基本信息

药物类型

小分子化药

别名

ARG

靶点

ADIPOR1 x PP2A

作用机制

ADIPOR1激动剂(脂联素受体蛋白-1激动剂)、PP2A刺激剂(蛋白质磷酸酶2A刺激剂)、细胞凋亡刺激剂

治疗领域

免疫系统疾病内分泌与代谢疾病泌尿生殖系统疾病+ [1]

在研适应症

糖尿病肾病炎症花生过敏

非在研适应症

胰腺癌

原研机构

Kracie Ltd.

在研机构

Icahn School of Medicine at Mount Sinai上海中医药大学附属龙华医院

Nephrology, Inc.

非在研机构

University of ToyamaKracie Ltd.

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)临床前

特殊审评-

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结构

分子式C21H24O6

InChIKeyNQWVSMVXKMHKTF-JKSUJKDBSA-N

CAS号7770-78-7

关联

3

项与 Arctigenin 相关的临床试验

JPRN-UMIN000050011 / Completed临床2期IIT

Efficacy and safety of HMB/Gln/Arg for the prophylaxis of chemoradiation -induced mucositis in head and neck squamous cell carcinoma: Randomized Phase II Clinical Study - Efficacy and safety of HMB/Gln/Arg for the prophylaxis of chemoradiation -induced mucositis in head and neck squamous cell carcinoma: Randomized Phase II Clinical Study

开始日期2018-03-01

申办/合作机构-

JPRN-UMIN000010111 / Completed临床2期IIT

Phase 2a trial of GBS-01 for advanced pancreatic cancer refractory to gemcitabine and fluoropyrimidine chemotherapy. - GBS-01 Phase IIa

开始日期2013-03-11

申办/合作机构

National Cancer Center Hospital East

[+1]

JPRN-UMIN000005787 / CompletedIIT

Phase 1/2 study of GBS-01 in patients with gemcitabine-refractory advanced pancreatic cancer. - GBS-01 Phase I/II

开始日期2011-06-01

申办/合作机构

National Cancer Center Hospital East

100 项与 Arctigenin 相关的临床结果

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100 项与 Arctigenin 相关的转化医学

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100 项与 Arctigenin 相关的专利（医药）

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1,539

项与 Arctigenin 相关的文献（医药）

2025-01-01·Food Chemistry

Protective effects and molecular mechanisms of Litopenaeus vannamei treated with l-arginine/l-lysine against myofibrillar proteins oxidation and quality degradation during freeze-thaw cycles

Article

作者: Luo, Wenwen ; He, Mengxue ; Sun, Jianan ; Zhang, Yejun ; Mao, Xiangzhao

The storage and processing of Litopenaeus vannamei are often challenged by the freeze-thaw (F-T) cycle phenomenon. This study delved into the influence of pretreatment with l-arginine (Arg) and l-lysine (Lys) on the myofibrillar proteins oxidation and quality of shrimp subjected to F-T cycles. Arg and Lys pretreatment notably improved water-holding capacity (WHC), textural integrity as well as the myofibrillar structure of the shrimps. A lesser reduction in the amounts of immobile and bound water was found in the amino acid-treated groups, and the oxidation of lipids and proteins were both decelerated. Molecular simulation results indicated that Arg and Lys could form hydrogen and salt-bridge bonds with myosin, enhancing the stability of Litopenaeus vannamei. The study concludes that Arg and Lys are effective in alleviating the adverse effects of F-T cycles on the quality of Litopenaeus vannamei, and provides a new solution for the quality maintenance during storage and processing.

2024-12-01·Phytomedicine

Arctigenin ameliorates high-fat diet-induced metabolic disorders by reshaping gut microbiota and modulating GPR/HDAC3 and TLR4/NF-κB pathways

Article

作者: Zhang, Zengli ; Li, Changhao ; Wang, Nana

BACKGROUNDArctigenin (AG), a phenylpropanoid lignan from the medicinal and food homologous plant Arctium lappa l., is known for its anti-cancer, anti-inflammatory and antioxidant properties. However, the pharmacological effects of AG on metabolic disorders remain limited, and specific mechanisms based on gut microbiota have not been reported.PURPOSEThis study aimed to evaluate the regulation of glycolipid metabolism by AG in obese mice and investigate the potential mechanisms associated with gut microbes.METHODSThe anti-obesity efficacy of AG was evaluated in high-fat diet (HFD)-fed mice. 16S rRNA gene sequencing and GC-MS were used to detect changes in gut microbes and metabolite levels. Immunohistochemistry, immunofluorescence, and polymerase chain reaction were used to validate the molecular mechanisms of gut microbe-derived metabolites involved in the improvement of intestinal homeostasis and hepatic metabolism by AG.RESULTSWe found that AG significantly ameliorated HFD-induced glucolipid metabolism disorders, liver degeneration and the imbalance of macrophage M1/M2 polarization. In addition, AG attenuated intestinal barrier damage, inflammation and imbalance of Th17/Treg immune in HFD mice. Importantly, AG promoted short-chain fatty acid (SCFA)-producing bacteria and SCFA levels, which regulated the G protein-coupled receptor (GPR)41/43 and HDAC3 pathways to induce FOXP3 protein expression and consequently maintained intestinal Th17/Treg immunity. AG also inhibited lipopolysaccharide (LPS) production leading to attenuation of TLR4/NF-κB-mediated intestinal inflammation. Furthermore, AG upregulated intestinal MCT1 protein levels to promote absorption of SCFA and activated the hepatic GPR41/43/109a-AMPK pathway to regulate lipid metabolism, and thus reduced lipid accumulation.CONCLUSIONThis study first demonstrated that AG could modulate the gut microbiota and derived metabolites to repair intestinal damage and regulate hepatic metabolic pathways, thereby ameliorating metabolic disorders induced by HFD. These findings support the great potential of AG as a novel prebiotic to fight obesity and chronic metabolic diseases by targeting the gut microbiota.

2024-12-01·Tissue and Cell

L‐arginine mitigates choroid plexus changes in Alzheimer’s disease rat model via oxidative/inflammatory burden and behavioral modulation

Article

作者: Fattah, Islam Omar Abdel ; El-Din, Wael Amin Nasr ; Nasr El-Din, Wael Amin ; Abdel Fattah, Islam Omar

Aging is a risk factor for Alzheimer's disease (AD), leading to choroid plexus (CP) alterations. This study aimed to explore the possible therapeutic mechanisms of ARG on AD-induced CP changes. Sprague-Dawley rats were divided into 6 groups (n = 7 per group): adult, adult+ARG, aged, aged+ARG, aged+AD, and aged+AD+ARG groups. Evaluations were for Y-maze test, serum levels of oxidative/inflammatory markers, and serum and cerebrospinal fluid (CSF) markers of AD, histopathology, immunohistochemistry, and histomorphometry. The aged+AD group demonstrated a significant decline in maze test parameters, total antioxidant capacity (TAC), brain-derived neurotrophic factor (BDNF) levels, and vascular endothelial growth factor (VEGF) immunoexpression, while tumour necrosis factor-α (TNF-α), interleukin-1 beta (IL-1β), beta-amyloid (Aβ) levels and amyloid protein precursor (APP), and heat shock protein90 (HSP90) immunoexpressions were significantly increased. Sections of this group showed flat epitheliocytes, congested capillaries, connective tissue expansion, and degenerated endothelium. These parameters were modulated by ARG administration, via increased levels of TAC (1.37 vs 2.17 mmol/L), (p = 0.018) BDNF (serum: 48.50 vs 78.41; CSF: 4.07 vs 7.11 pg/ml) (p< 0.001), and VEGF (0.07 vs 0.26 OD) (p< 0.001), in addition to decreased levels of TNF-α (86.63 vs 41.39 pg/ml) (p< 0.001), IL-1β (96.04 vs 39.57 pg/ml) (p< 0.001), Aβ (serum: 67.40 vs 47.30; CSF: 189.26 vs 169.84 pg/ml) (p< 0.001), and HSP90 (0.54 vs 0.13 OD) (p< 0.001). In conclusion, ARG ameliorates the AD-associated CP changes, including histopathological, oxidative/inflammatory, and AD markers, and VEGF and HSP90 immunohistochemical alterations. Dietary ARG consumption is recommended to avoid AD progression in the elderly.

100 项与 Arctigenin 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Arctigenin	B05XB01	DB00125

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
糖尿病肾病	临床前	-	Nephrology, Inc.	2016-11-15
糖尿病肾病	临床前	中国	上海中医药大学附属龙华医院	2016-11-15
炎症	临床前	美国	Icahn School of Medicine at Mount Sinai	2016-02-01
花生过敏	临床前	美国	Icahn School of Medicine at Mount Sinai	2016-02-01
胰腺癌	药物发现	-	Kracie Ltd.	-
胰腺癌	药物发现	日本	-	-
胰腺癌	药物发现	-	University of Toyama	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


JPRN-UMIN000005787 (ASCO2013)	临床1期	胰腺癌	15	GBS-01 3g	(膚淵築積齋製憲齋衊餘) = 簾鬱齋餘廠構膚積襯鹽構鬱衊遞觸構獵積糧鑰 (艱鑰壓壓齋艱鹹蓋範製 ) 更多	-	2013-05-20
				GBS-01 7.5g	(膚淵築積齋製憲齋衊餘) = 餘餘觸鬱憲築膚齋鏇壓構鬱衊遞觸構獵積糧鑰 (艱鑰壓壓齋艱鹹蓋範製 ) 更多