Delving into the Latest Updates on Arctigenin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

ARG

Target

ADIPOR1 x PP2A

Mechanism

ADIPOR1 agonists(Adiponectin receptor protein 1 agonists), PP2A stimulants(Protein phosphatase 2A stimulants), Apoptosis stimulants

Therapeutic Areas

Immune System DiseasesEndocrinology and Metabolic DiseaseUrogenital Diseases+ [1]

Active Indication

Diabetic NephropathiesInflammationPeanut Hypersensitivity

Inactive Indication

Pancreatic Cancer

Originator Organization

Kracie Ltd.

Active Organization

Icahn School of Medicine at Mount SinaiLonghua Hospital Shanghai University of TCM

Nephrology, Inc.

Inactive Organization

University of ToyamaKracie Ltd.

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure

Molecular FormulaC21H24O6

InChIKeyNQWVSMVXKMHKTF-JKSUJKDBSA-N

CAS Registry7770-78-7

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

Start Date01 Mar 2018

Sponsor / Collaborator-

JPRN-UMIN000010111 / CompletedPhase 2IIT

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

Start Date11 Mar 2013

Sponsor / Collaborator

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

Start Date01 Jun 2011

Sponsor / Collaborator

National Cancer Center Hospital East

100 Clinical Results associated with Arctigenin

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100 Translational Medicine associated with Arctigenin

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100 Patents (Medical) associated with Arctigenin

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1,539

Literatures (Medical) associated with Arctigenin

01 Jan 2025·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

Author: 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.

01 Dec 2024·Phytomedicine

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

Article

Author: 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.

01 Dec 2024·Tissue and Cell

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

Article

Author: 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 Deals associated with Arctigenin

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Arctigenin	B05XB01	DB00125

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetic Nephropathies	Preclinical	-	Nephrology, Inc.	15 Nov 2016
Diabetic Nephropathies	Preclinical	CN	Longhua Hospital Shanghai University of TCM	15 Nov 2016
Inflammation	Preclinical	US	Icahn School of Medicine at Mount Sinai	01 Feb 2016
Peanut Hypersensitivity	Preclinical	US	Icahn School of Medicine at Mount Sinai	01 Feb 2016
Pancreatic Cancer	Discovery	-	Kracie Ltd.	-
Pancreatic Cancer	Discovery	JP	-	-
Pancreatic Cancer	Discovery	-	University of Toyama	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


JPRN-UMIN000005787 (ASCO2013)	Phase 1	Pancreatic Cancer	15	GBS-01 3g	(jgjxokpxdc) = tgoungnizu zegvvtobrb (atbpomjeru ) View more	-	20 May 2013
				GBS-01 7.5g	(jgjxokpxdc) = bygefyzrgv zegvvtobrb (atbpomjeru ) View more