A hundred million tons of young apples are thinned and discarded in the orchard per year, aiming to increase the yield and quality of apples. We fermented thinned young apples using a potential probiotic fungus, Eurotium cristatum, which notably disrupted the microstructure of raw samples, as characterized by the scanning electron microscope. Fermentation substantially altered the metabolite profiles of samples, which are predicted to alleviate colitis via regulating inflammatory response and response to lipopolysaccharide by using network pharmacology analysis. In vivo, oral gavage of water extracts of E. cristatum fermented young apples (E.YAP) effectively alleviated DSS-induced colitis, restored the histopathology damage, reduced the levels of inflammatory cytokines, and promoted colonic expressions of tight junction proteins. Moreover, E.YAP ameliorated gut dysbacteriosis by increasing abundances of Lactobacillus,Blautia, Muribaculaceae, and Prevotellaceae_UCG-001 while inhibiting Turicibacter, Alistipes, and Desulfovibrio. Importantly, E.YAP increased colonic bile acids, such as CA, TCA, DCA, TUDCA, and LCA, thereby alleviating colitis via PXR/NF-κB signaling. Furthermore, a synbiotic combination with Limosilactobacillus reuteri WX-94, a probiotic strain isolated from feces of healthy individuals with anti-inflammatory properties, augmented anticolitis capacities of E.YAP. Our findings demonstrate that E.YAP could be a novel, potent, food-based anti-inflammatory prebiotic for relieving inflammatory injuries.

02 Jan 2024·Expert opinion on emerging drugs

Emerging drugs for the treatment of irritability associated with autism spectrum disorder

Review

Author: Arabzadeh Bahri, Razman ; Akhondzadeh, Shahin ; Motavaselian, Mohsen ; Shamabadi, Ahmad ; Karimi, Hanie

INTRODUCTION:

Autism spectrum disorder (ASD) is an early-onset disorder with a prevalence of 1% among children and reported disability-adjusted life years of 4.31 million. Irritability is a challenging behavior associated with ASD, for which medication development has lagged. More specifically, pharmacotherapy effectiveness may be limited against high adverse effects (considering side effect profiles and patient medication sensitivity); thus, the possible benefits of pharmacological interventions must be balanced against potential adverse events in each patient.

AREAS COVERED:

After reviewing the neuropathophysiology of ASD-associated irritability, the benefits and tolerability of emerging medications in its treatment based on randomized controlled trials were detailed in light of mechanisms and targets of action.

EXPERT OPINION:

Succeeding risperidone and aripiprazole, monotherapy with memantine may be beneficial. In addition, N-acetylcysteine, galantamine, sulforaphane, celecoxib, palmitoylethanolamide, pentoxifylline, simvastatin, minocycline, amantadine, pregnenolone, prednisolone, riluzole, propentofylline, pioglitazone, and topiramate, all adjunct to risperidone, and clonidine and methylphenidate outperformed placebo. These effects were through glutamatergic, γ-aminobutyric acidergic, inflammatory, oxidative, cholinergic, dopaminergic, and serotonergic systems. All medications were reported to be safe and tolerable. Considering sample size, follow-up, and effect size, further studies are necessary. Along with drug development, repositioning and combining existing drugs supported by the mechanism of action is recommended.

20 Mar 2023·JOURNAL OF BIOLOGICAL REGULATORS AND HOMEOSTATIC AGENTS

Propentofylline's Anti-Nociception Effect in a Rat Model of Vincristine-Induced Neuropathic Pain

Author: Wang, Fang ; Ha, Siyuan ; Fu, Jun

A large proportion of cancer patients suffer from devastating neuropathic pain.Vincristine (Vin), a first-line anticancer therapy, usually induces this pain, which neg. affects the life quality of patients.To explore propentofylline's effect on Vin-induced neuropathic pain and its potential mechanism of action.A Vin-induced rat model was used in this study.Vin (125μg/kg) was administered i.p. every other day for 8 days (days 1~8), to establish neuropathic pain model in rats.Then, the rats were randomized into the model group and three treatment groups (low-, mid- and high-dosage groups).On days 8~14, the three treatment groups received daily i.p. injections of propentofylline (PPF) at 6.25, 12.5, and 25 mg/kg/day, while all groups received equal volumes of physiol. saline.Behavioral tests were conducted, to check pain hypersensitivity on days 0, 8, 10, 14 and 21.Glial activation was assessed using immunohistochem. method on day 14.Spinal cord pro-inflammatory cytokines and chemokine levels were estimated using ELISA (ELISA) on days 8, 14 and 21.Vin-induced pain hypersensitivity was significantly suppressed by mid-dosage and high-dosage PPF treatment, starting from day 10 (p < 0.05 or 0.01).On day 14, activated glial numbers decreased significantly on mid- and high-dosage PPF treatments (p < 0.05 or 0.01).High-dosage PPF treatment significantly reduced MCP-1 (monocyte chemoattractant protein-1) up-regulation (p < 0.01).The up-regulation of pro-inflammatory cytokines were significantly reduced by mid-dosage and high-dosage PPF (p < 0.01 or 0.05).Neuroinflammation plays a crucial role in the progression of Vin-induced neuropathic pain.PPF could attenuate this pain, through weakening the recruitment of neuroinflammation, thereby relieving pain hypersensitivity in rat.

News (Medical) associated with Propentofylline

08 Sep 2022

·www.prnewswire.com

Entrepreneurial Accelerator Program (EAP) Portfolio Company receives $400,000 Research Grant from The National Cancer Institute to study a repurposed drug in treatment of Glioblastoma

SHREVEPORT, La., Sept. 8, 2022 /PRNewswire/ -- Entrepreneurial Accelerator Program (EAP) portfolio company Oleolive, Inc. has been awarded a Small Business Technology Transfer (STTR) Phase 1 $400,000 research grant from the National Cancer Institute for "Chemosensitization of Glioblastoma by Propentofylline." Drs. Nhan Tran and Joseph Loftus, investigators at Mayo Clinic and experts in Glioblastoma Multiforme (GBM), collaborated with Oleolive on the proposal. Propentofylline (PPF) was originally tested in multiple clinical trials for Alzheimer's disease but, although shown to be safe and effective, was not brought to the commercial market. PPF is considered a repurposed drug, defined as a drug developed for one indication and repositioned to treat another, in this case GBM. Repurposed drugs require less money and time for development and overall costs much less compared to research and development of new drugs. GBM is a brain cancer with no effective therapeutics that claims the lives of over 15,000 Americans each year. GBM has poor clinical outcomes due to therapy-resistant tumor cells leading to recurrence; therefore, therapeutic strategies that enhance tumor cell chemosensitivity are essential for improved patient outcomes. This project will evaluate if PPF increases sensitization of GBM tumor cells to chemotherapy. This research could lead to a therapeutic strategy to extend survival for GBM patients beyond the current average of 1.25 years. About Oleolive, Inc . Oleolive, Inc. is a preclinical private biotechnology company founded in 2017, located in Shreveport, Louisiana. The company is developing therapeutics to treat a variety of human indications, including brain cancer, Alzheimer's disease, fibrosis, and traumatic blood loss in austere environments. The company has received more than $5M in STTRs and small business innovation research (SBIR) grant awards from multiple funding sources including the National Institute on Aging, the National Cancer Institute, the National Heart, Lung, and Blood Institute and the Department of Defense. Oleolive also manufactures the dietary ingredient Oligen which contains compounds from Extra Virgin Olive Oil that promote healthy aging. To learn more about Oleolive, Inc. please visit our website , or contact [email protected] with inquiries. Research reported in this publication was supported by the National Cancer Institute of the National Institutes of Health under Award Number R41CA268286. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. SOURCE Entrepreneurial Accelerator Program

Small molecular drugCollaborate

100 Deals associated with Propentofylline

External Link

KEGG	Wiki	ATC	Drug Bank
D01630	Propentofylline	N06BC02	DB06479

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cerebrovascular Disorders	South Korea	Sanofi	30 Oct 1997

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	NDA/BLA	European Union	Hoechst Pakistan Ltd.	-
Alzheimer Disease	NDA/BLA	Canada	Hoechst Pakistan Ltd.	-
Dementia, Vascular	NDA/BLA	European Union	Hoechst Pakistan Ltd.	-
Dementia, Vascular	NDA/BLA	Canada	Hoechst Pakistan Ltd.	-
Glioblastoma	Preclinical	United States	Oleolive, Inc.	17 Nov 2022

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