Delving into the Latest Updates on Arctigenin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

ARG

Target

ADIPOR1 x PDHK1 x PP2A

Action

agonists, inhibitors, stimulants

Mechanism

ADIPOR1 agonists(Adiponectin receptor protein 1 agonists), PDHK1 inhibitors(pyruvate dehydrogenase kinase 1 inhibitors), PP2A stimulants(Protein phosphatase 2A stimulants)

+ [1]

Therapeutic Areas

NeoplasmsImmune System DiseasesEndocrinology and Metabolic Disease+ [3]

Active Indication

OsteosarcomaDiabetic NephropathiesInflammation+ [1]

Inactive Indication

Pancreatic Cancer

Originator Organization

Kracie Ltd.

Active Organization

Luoyang Orthopedic Hospital of Henan Province

Icahn School of Medicine at Mount SinaiThe Second Affiliated Hospital of Xi'an Jiaotong University

+ [2]

Inactive Organization

University of ToyamaKracie Ltd.

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC21H24O6

InChIKeyNQWVSMVXKMHKTF-JKSUJKDBSA-N

CAS Registry7770-78-7

The purpose of this research study is to determine if consuming arctigenin, a natural compound from a Chinese herb called Arctium lappa (commonly called greater burdock), is safe, and to measure the intake level of arctigenin in blood. Arctigenin is being studied by researchers for potential health benefits such as helping to lower the risk of inflammation and cancer. A human study has been done measuring the uptake of arctigenin into blood after consumption of the herb extract containing arctigenin, and found no toxicity. Studies in mice demonstrated that consumption of arctigenin in pure form at a safe level is highly effective in inhibition of prostate cancer growth. Therefore, this study is designed to evaluate the safety and uptake rate of pure arctigenin in humans, which may be potentially used in the future for prostate cancer prevention.

Start Date15 Jan 2019

Sponsor / Collaborator

University of California, Los Angeles

[+1]

JPRN-UMIN000050011

/ CompletedPhase 2IIT

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-

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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2,162

Literatures (Medical) associated with Arctigenin

01 Dec 2025·Molecular Biology Reports

A review of six bioactive compounds from preclinical studies as potential breast cancer inhibitors

Review

Author: Rampogu, Shailima ; Oh, Tae Hwan ; Al-Antari, Mugahed A ; Shaik, Baji

Breast cancer is one of the predominant causes of mortality in women worldwide. Although therapeutics such as surgery, chemotherapy, hormonal therapy, and radiotherapy have been used, they are associated with adverse effects or multidrug resistance. The use of natural compounds is a promising strategy, owing to their abundance and medicinal value. This review focuses on six natural compounds, namely cinnamaldehyde, diosmin, taxifolin, phloretin, arctigenin, and eugenol, and details their mechanisms of breast cancer inhibition based on in vitro and in vivo studies. These compounds generally promote apoptosis and cell cycle arrest, hinder metastasis and invasion, and decrease tumor growth. This review reinforces the use of natural compounds as therapeutics for breast cancer from their preclinical studies. These compounds might be promising for drug development due to their abundance, high reliability, and safety.

01 Jul 2025·Food Chemistry

Effects of L-arginine supplementation on fat deposition and meat quality in growing lambs: Interactions with gut microbiota and metabolic signalling pathways

Article

Author: Zhao, Xin ; Li, Xuan ; Kang, Letian ; Duan, Yan ; Liu, Ting ; Jin, Ye

Arginine (ARG) improves meat quality and fat deposition; however, its effects on gut microbiota-mediated lipid metabolism in lambs remain unclear. Twenty-four lambs were divided into control (fed a basal diet) and ARG groups (with 1 % ARG added). In the ARG group, backfat thickness, shear force in the longissimus thoracis (LT) muscle, and C16:0 and SFA contents in the subcutaneous adipose tissue (SAT) were reduced, whereas the eye muscle area, a* value, and intramuscular fat, C18:2n-6c, C20:4n-6, C20:5n-3, and PUFA contents in the LT were elevated. Moreover, the ARG group exhibited higher levels of Prevotella, Akkermansia, Faecalibacterium, SCFAs, and GLP-1 in the colon, and lower serum triglyceride and glucose levels. Interestingly, ARG differentially regulated lipid metabolism in the SAT and LT via the GLP-1R/AMPK and triglyceride metabolism signalling pathways. Overall, ARG addition may optimise gut microbiota composition, fat deposition, and meat quality, providing application guidance for regulating fat deposition in lambs.

01 Jun 2025·Colloids and Surfaces B: Biointerfaces

Arginine tagged liposomal carrier for the delivery of celastrol for ferroptosis-induced hepatocellular carcinoma therapy

Article

Author: Zhu, Yuzhao ; Zhang, Denghai ; Zhang, Xue ; Wang, Chao ; Zhang, Kai ; Zhang, Jian ; Cai, Banglan ; Qi, Manman ; Zhao, Gang

Hepatocellular carcinoma (HCC) is a predominant malignant liver tumor that cannot be efficiently treated because of poor response, toxicity, and drug resistance. Ferroptosis is an iron-dependent way of cell death associated with abnormal intracellular lipid metabolism. Celastrol (Cel) has the ability to inhibit the progression of HCC by regulating multiple signaling pathways and induce ferroptosis. However, Cel exists the limitations of low water solubility, low oral bioavailability, and high organ toxicity. Cel was encapsulated in polyethylene glycol-based liposomes modified with L-arginine (Cel@Lip-Arg). Cel@Lip-Arg has a uniform size distribution (∼100 nm), high drug loading (80 %), and excellent ability to target liver cancer cells. In vitro experiments demonstrated that Cel@Lip-Arg considerably suppressed the activity of HuH7 (hepatoma) cells but had a negligible effect on L02 (normal) cells. Cel@Lip-Arg induced ferroptosis in hepatoma cells by promoting transferrin receptor expression, inhibiting system xc^- and glutathione peroxidase 4, and favoring intracellular peroxide accumulation. In vivo experiments revealed that Cel@Lip-Arg plays a therapeutic role by inducing ferroptosis. Compared to Cel, Cel@Lip-Arg had a higher anti-hepatoma activity and effectively reduced the toxicity of Cel in mice. Cel@Lip-Arg-induced ferroptosis was concluded to be an attractive strategy for the precise treatment of HCC.

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
Osteosarcoma	Preclinical	China	The Second Affiliated Hospital of Xi'an Jiaotong University	01 May 2025
Osteosarcoma	Preclinical	China	Luoyang Orthopedic Hospital of Henan Province	01 May 2025
Diabetic Nephropathies	Preclinical	China	Longhua Hospital Shanghai University of TCM	15 Nov 2016
Diabetic Nephropathies	Preclinical	-	Nephrology, Inc.	15 Nov 2016
Inflammation	Preclinical	United States	Icahn School of Medicine at Mount Sinai	01 Feb 2016
Peanut Hypersensitivity	Preclinical	United States	Icahn School of Medicine at Mount Sinai	01 Feb 2016
Pancreatic Cancer	Discovery	-	Kracie Ltd.	-
Pancreatic Cancer	Discovery	Japan	-	-
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	(znzlhvrvtq) = kksnlamvix zabmsgocmh (zcbirzxgqv ) View more	-	20 May 2013
				GBS-01 7.5g	(znzlhvrvtq) = epbbxzfskp zabmsgocmh (zcbirzxgqv ) View more