HMGB1 inhibitors(High Mobility Group Protein B1 inhibitors), NLRP3 inhibitors(NACHT, LRR and PYD domains-containing protein 3 inhibitors), TLR4 antagonists(Toll like receptor 4 antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesEndocrinology and Metabolic Disease+ [1]

Active Indication

Diabetic NephropathiesParkinson DiseaseIschemic stroke

Inactive Indication-

Originator Organization-

Active Organization

Beijing University of Traditional Chinese MedicineDongzhimen Hospital Affiliated to Beijing University of Chinese MedicineChinese PLA Academy of Military Medical Sciences

+ [3]

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with Acteoside

100 Translational Medicine associated with Acteoside

100 Patents (Medical) associated with Acteoside

Literatures (Medical) associated with Acteoside

01 Dec 2024·Biochemical and Biophysical Research Communications

CRISPR/Cas9 targeted editing of UDP-rhamnose: Rhamnosyltransferase gene decreases its functions in acteoside biosynthesis and pest resistance in Rehmarmia glutinosa

Article

Author: Zhou, Yanqing ; Shao, Luying

UDP-rhamnose: rhamnosyltransferases (URTs)in Rehmarmia glutinosa (RgURT1-RgURT4)may catalyze two key downstream steps of acteoside biosynthesis. Moreover, they were identified from Rehmarmia glutinosa and preliminarily characterized, but their bioinformatics analysis and functions remain to be further explored. The present study mainly focused on investigating their bioinformatics function prediction, genotype-dependent expression, and roles for acteoside biosynthesis and pest resistance with CRISPR/Cas9 technology.Some key findings were as follows:they had a low identity but a typical PSPG box of rhamnosyltransferases, belonging to Glycosyltansferase-GTB type superfamily; They could be expressed depending on genotype,but RgURT4 expression is the highest; Based on RgURT4, two sgRNAs were designed and cloned into pBWA(V)HS-zmpl vector to construct a pBWA(V)HS-Cas9-RgURT vector. It was transferred to Rehmarmia glutinosa using Agrobacterium-mediated transformation so that hygromycin-resistant R. glutinosa plants were obtained. Sequencing indicated that CRISPR/Cas9 targeted editing resulted in base replacements in RgURT4,while its expression was decreased among these edited plants; A few of them had yellower leaves with white dots, lower acteoside and a little higher decaffeoylacteoside than WTs; Tetranychus cinnbarinus among them was observed by stereomicroscope. The results demonstrated that CRISPR/Cas9-mediated RgURT4 editing reduced the acteoside content and pest resistance but decaffeoylacteoside content of Rehmarmia glutinosa. This study will contribute to the function analyses of rhamnosyltransferases gene and downstream steps of acteoside biosynthesis as well as its CRISPR-Cas9-based molecular breeding.

01 Feb 2024·Biochemical Pharmacology

Acteoside alleviates blood–brain barrier damage induced by ischemic stroke through inhibiting microglia HMGB1/TLR4/NLRP3 signaling

Article

Author: Wang, Jingwen ; Liao, Yucheng ; Weng, Yan ; Yang, Jianhua ; Ding, Yi ; Guo, Chao ; Hou, Qiang ; Wen, Limei ; Wen, Aidong ; Hu, Junping

Ischemic stroke (IS) can cause severe harm, inducing oxidative stress, inflammation, and pyroptotic death. IS treatment efficacy remains limited, and microglia are important regulators of IS-related blood-brain barrier (BBB) damage. It is thus vital that new therapeutic agents capable of targeting microglia be identified to treat IS-related damage to the BBB. Acteoside (ACT), which is a compound derived from Cistanche tubulosa (Schenk) Wight., offers promising bioactivity, but its ability to protect against central nervous system injury remains to be documented. To clarify the protective benefits and mechanisms through which ACT can protect against damage to the BBB, a rat middle cerebral artery occlusion (MCAO) model system was herein employed. These in vivo analyses demonstrated that ACT was able to significantly reduce cerebral infarct size while improving their neurological scores and altering neurotrophic and inflammatory factor release. RNA sequencing and molecular docking studies highlighted the ability of ACT to exert its protective benefits via the HMGB1/TLR4/NLRP3 axis. Western immunoblotting and immunofluorescent staining for tight junction proteins additionally confirmed the ability of ACT to preserve BBB integrity. The underlying mechanisms were then explored with an oxygen-glucose deprivation (OGD) model in vitro with BV2 cells. This strategy thus confirmed that the ability of ACT to suppress microglial inflammatory and pyroptotic activity was HMGB1/TLR4/NLRP3 pathway-dependent. These data thus offer novel evidence that ACT can protect against IS-related damage to the BBB through the abrogation of inflammatory and pyroptotic activity, underscoring its promise as a novel lead compound for the therapeutic treatment of IS.

01 Feb 2019·Iranian journal of basic medical sciencesQ4 · MEDICINE

Methanolic leaf extract of Punica granatum attenuates ischemia-reperfusion brain injury in Wistar rats: Potential antioxidant and anti-inflammatory mechanisms.

Q4 · MEDICINE

ArticleOA

Author: Venkatanarasappa Venkataranganna, Marikunte ; Lakshminarayanashastry Viswanatha, Gollapalle ; Lingeswara Prasad, Nunna Bheema

OBJECTIVESThis study was conducted to evaluate the cerebroprotective effect of methanolic leaf extract of Punica granatum (MePG) in Wistar rats.MATERIALS AND METHODSThe MePG was initially assessed for in vitro antioxidant activity, and later evaluated on LPS-induced RAW 264.7 cell line assay. Finally, the MePG was evaluated against ischemia-reperfusion (I/R) induced brain injury in Wistar rats.RESULTSIn DPPH, FRAP and ORAC assays, the MePG has exhibited potent antioxidant activity. Further, the MePG has significantly inhibited the generation of nitrite, ROS and TNF-α in LPS-induced RAW 264.7 cell lines. Besides, global ischemia followed by reperfusion caused significant changes in the neurological and behavioral functions in I/R control animals compared to sham control. Additionally, in the I/R control group there was a substantial decrease in the catalase and superoxide dismutase activities; Likewise, reduced glutathione levels reduced and lipid peroxidation levels enhanced significantly. Also, pro-inflammatory cytokines such as TNF-α, IL-6, and ICAM-I were increased and the levels of IL-10 was decreased significantly. Furthermore, the I/R insult caused increase in brain volume and cerebral infarct formation. Similarly, histopathology of the brain tissue revealed hallmarks like necrosis, leukocyte infiltration, cerebral edema and vascular congestion in I/R control. Notably, MePG (200 and 400 mg/kg) pretreatment for 7 days, has attenuated all the I/R-persuaded pathological changes compared to I/R control. In addition, the LC-MS/MS analysis showed presence of acteoside, apigenin, gallic acid, gossypin, pentagalloyl glucose, quercetin, and rutin as major ingredients in the MePG.CONCLUSIONThese findings suggest that the MePG possesses significant cerebroprotective activity.

100 Deals associated with Acteoside

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Diabetic Nephropathies	Preclinical	CN	Beijing University of Traditional Chinese Medicine	01 Sep 2024
Diabetic Nephropathies	Preclinical	CN	Dongzhimen Hospital Affiliated to Beijing University of Chinese Medicine	01 Sep 2024
Parkinson Disease	Preclinical	CN	Chinese PLA Academy of Military Medical Sciences	01 Jul 2024
Parkinson Disease	Preclinical	CN	People's Liberation Army Air Force Military Medical University	01 Jul 2024
Ischemic stroke	Preclinical	CN	Xijing Hospital	01 Feb 2024
Ischemic stroke	Preclinical	CN	Xinjiang Medical University	01 Feb 2024

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

Acteoside

Overview

Basic Info

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation