Akt stimulants(Proto-oncogene proteins c-akt stimulants), NF-κB inhibitors(Nuclear factor NF-kappa-B complex inhibitors), PI3K family stimulants(Phosphatidylinositol 3-kinase family stimulants)

+ [1]

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic Disease

Active Indication

Alzheimer DiseaseParkinson Disease

Inactive Indication-

Originator Organization-

Active Organization

GLA University

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC14H16O3

InChIKeyXYYAFLHHHZVPRN-GXTWGEPZSA-N

CAS Registry28808-62-0

100 Clinical Results associated with Fraxinellone

100 Translational Medicine associated with Fraxinellone

100 Patents (Medical) associated with Fraxinellone

185

Literatures (Medical) associated with Fraxinellone

01 Apr 2025·Phytomedicine

Cortex Dictamni-induced hepatotoxicity by enhanced oxidative phosphorylation: Insights from integrative transcriptomics, proteomics, and metabolomics analyses

Article

Author: Zhang, Mengmeng ; Zhang, Zhendong ; Liu, Shumin ; Deng, Geyu ; Yu, Donghua ; He, Wenjie ; Huang, Lin ; Wang, Yu ; Gao, Rui ; Chen, Pingping ; Sun, Huijuan ; Lu, Fang

BACKGROUNDCortex Dictamni (CD) is a traditional Chinese medicine that is commonly used to treat various skin diseases. Recently, clinical reports have highlighted its potential to induce severe hepatotoxicity. However, the underlying mechanisms of toxicity remain inadequately explored.PURPOSEThe aim of this study was to elucidate the intrinsic mechanisms of CD-induced hepatotoxicity.STUDY DESIGNHepatotoxicity was assessed in SD rats, and human primary hepatocytes (HPHs) and differentiated HepaRG (dHepaRG) cells were used for in vitro testing.METHODSThe major components of CD were determined using ultra-performance liquid chromatography (UPLC). Rats were randomly divided into control, CD-high (CD-H), CD-middle (CD-M), CD-low (CD-L), and isoniazid (INH) groups and administered oral gavage for four weeks. Serum biochemical indices, histopathological changes, apoptotic markers, and liver function were evaluated to assess hepatotoxicity. A comprehensive analysis of rat liver samples was performed using transcriptomic, proteomic, and metabolomic approaches to identify key pathways involved in CD-induced hepatotoxicity. In vitro toxicity validation of CD was performed using HPHs and dHepaRG cells. The key pathway was validated in vivo and in vitro.RESULTSCD primarily contained obacunone, fraxinellone, and dictamine. Administration of CD-H (9 times the maximum daily clinical dose in adults) and CD-M (3 times the maximum daily clinical dose in adults) for 4 weeks induced varying degrees of hepatotoxicity in rats. The CD-H group presented increased absolute and relative liver weights, reduced alanine aminotransferase (ALT) and bile acid transporter levels, and increased albumin (ALB) and cytochrome P450 (CYP) 3A4 levels, indicating significant hepatotoxicity in rats. Integrated multiomics analysis revealed that NADH dehydrogenase (ubiquinone) Fe-S protein 2 (Ndufs2) is a critical regulator of CD-induced hepatotoxicity involving oxidative phosphorylation (OXPHOS). CD inhibited the viability of HPHs and dHepaRG cells, demonstrating its significant cytotoxicity. Mechanistic validation revealed that CD upregulated Ndufs2, reactive oxygen species (ROS) and mitochondrial respiratory chain complex (MRCC) I, leading to nuclear factor erythroid 2-related factor 2 (Nrf2) pathway activation, apoptosis, mitochondrial dysfunction, and hepatotoxicity.CONCLUSIONIn summary, our study presents a comprehensive picture of the toxicity of CD in terms of dose and sex and reveals, for the first time, the central role of Ndufs2-regulated OXPHOS in CD-induced hepatotoxicity.

01 Jan 2025·Journal of Chromatography A

Nontarget analysis of natural flavor metabolites in tobacco extracts

Article

Author: Yang, Chun-Qiang ; Liu, Shan ; Xu, Xiu-Juan ; Wang, Jian-Wei ; Wang, Min ; Wang, Ren-Qi ; Ren, Meng

Large-scale production of tobacco generates significant amounts of waste, making the reuse and recycling of tobacco waste crucial for sustainability. However, the high diversity of tobacco metabolites requires a comprehensive analysis of tobacco waste extracts, so as to optimize extraction selectivity and recovery. In this study, we thoroughly analyzed the metabolic composition of 168 tobacco extracts using nontarget analysis. The extracts were derived from 56 tobacco wastes covering all four major tobacco types: flue-cured, dark air-cured, Burley, and Oriental tobaccos. From each sample, we obtained three types of extracts, such as concretes, absolutes, and supercritical fluid extraction (SFE) oils, through various extraction protocols. By matching deconvolved experimental MS/MS spectra with databases, 587 metabolites were putatively annotated, which were categorized into 24 groups, including alkaloids, indoles, and flavor compounds. The metabolic compositions of extracts from dark air-cured and Burley tobaccos were found to be similar, whereas flue-cured and Oriental tobaccos contained more diverse flavor components. Notably, concretes of various tobaccos prepared with 70 %-ethanol contained similar amounts of addictive alkaloids. However, the absolutes obtained by sequential extraction of these concretes with 95 %-ethanol effectively removed alkaloids while modestly maintaining the flavor compounds. Conversely, extraction protocols incorporating supercritical fluid extraction followed by 95 %-ethanol extraction resulted in the loss of most flavor compounds, likely due to the incompatibility between the solvents used in the two extraction steps. In conclusion, our study demonstrates that absolutes derived through secondary extraction with varying ethanol-water ratios holds significant potential for utilization.

01 Jan 2025·Chromatographia

Metabolites Identification of Two Novel Chemical Constituents From Melia. Toosendan Sieb.et Zucc. in Rats by UPLC/ESI/qTOF-MS Analysis

Author: Yang, Bingyou ; Liu, Yan ; Xu, Ranchen ; Gu, Siqi ; Liu, Yuan ; Naseem, Anam ; Fang, Ye ; Li, Shuning

Melia. toosendan Sieb.et Zucc., a potent herbal medicine, boasts diverse therapeutic properties.As the main components, the isotoosendanin blocks protective autophagy in chemotherapy-induced cultured cancer cells and xenograft tumor tissue to significantly enhancing anticancer activity, and the fraxinellone contributes to pesticidal activity, anti-inflammatory and immunomodulatory effects.Until now, the metabolic profiles remained unknown.In the present study, 13 metabolites of isotoosendanin and 13 metabolites of fraxinellone were characterized in the blood, urine, and feces of rats by UPLC/ESI/qTOF-MS anal.Five metabolites (F-M3, F-M5, I-M1, I-M5, I-M8) were fully characterized.The isotoosendanin and fraxinellone were mainly involved in hydrogenation, acetylation, and methylenation metabolic reactions.This is the first study illuminates the two components in vivo metabolism, laying the foundation for future pharmacodynamic and mechanistic investigations.It is necessary to deeply understand the process of drug activation, and deactivation, rationally design new drugs, and guide the research and development of new drugs.

100 Deals associated with Fraxinellone

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Preclinical	India	GLA University	06 Aug 2024
Parkinson Disease	Preclinical	India	GLA University	06 Aug 2024

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