Synthesis and evaluation of asiatic acid derivatives as anti-fibrotic agents: structure/activity studies.

Steroids

School of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu 610064, Sichuan Province, China. Electronic address:

Published: April 2015

Fibrotic diseases are characterized by the over-accumulation of fibrous components in the extracellular matrix and the liver, which can lead to liver cirrhosis. Current treatment options cannot reverse or halt liver fibrosis, motivating a search for newer treatment options. Previously, we showed that asiaticoside, a bioactive triterpene glycoside from Centella asiatica, has anti-fibrotic properties. Here, the aglycone asiatic acid was chemically modified, and these derivatives were evaluated for their potential as anti-fibrotic agents. The data obtained from in vivo testing of these compounds in a rodent CCl4-induced liver injury model are discussed. The information obtained from these studies may be useful in the design of novel anti-fibrotic agents.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.steroids.2014.11.001DOI Listing

Publication Analysis

Top Keywords

anti-fibrotic agents
12
asiatic acid
8
treatment options
8
synthesis evaluation
4
evaluation asiatic
4
acid derivatives
4
anti-fibrotic
4
derivatives anti-fibrotic
4
agents structure/activity
4
structure/activity studies
4

Similar Publications

High-density lipoprotein nanoparticles spontaneously target to damaged renal tubules and alleviate renal fibrosis by remodeling the fibrotic niches.

Nat Commun

January 2025

College of Polymer Science and Engineering, West China School of Public Health, Med-X center of materials, Sichuan University, Chengdu, Sichuan, 610065, China.

Chronic kidney disease (CKD) ultimately causes renal fibrosis and end-stage renal disease, thus seriously threatens human health. However, current medications for CKD and fibrosis are inefficient, which is often due to poor targeting capability to renal tubule. In this study, we discover that biomimetic high-density lipoprotein (bHDL) lipid nanoparticles possess excellent targeting ability to injured tubular epithelial cells by kidney injury molecule-1(KIM-1) mediated internalization.

View Article and Find Full Text PDF

Purpose Of Review: Proliferative vitreoretinopathy (PVR) is a severe complication of retinal detachment and trauma, posing significant challenges to surgical success and visual prognosis. Despite advancements in vitreoretinal surgery, PVR incidence remains unchanged, this review presents a synthesis of the principal clinical and preclinical research findings from recent years.

Recent Findings: Recent research has focused on anti-inflammatory, antiproliferative, and antifibrotic agents.

View Article and Find Full Text PDF

Navelina oranges () are rich in phytonutrients and bioactive compounds, especially flavonoids like hesperidin. This study investigates the anti-inflammatory and anti-fibrotic properties of hesperidin (HE) and a polyphenol mixture from Navelina oranges (OE) in human hepatocytes (Hepa-RG) and hepatic stellate cells (LX-2), in order to elucidate the underlying molecular mechanisms. In Hepa-RG cells, HE treatment increased expression of cannabinoid receptor 2 (CB2R), which was associated with down-regulation of p38 mitogen-activated protein kinases (p38 MAPK) but had minimal impact on cyclooxygenase-2 (COX-2) and transforming growth factor-β (TGF-β) levels.

View Article and Find Full Text PDF

Advances in Selenium and Related Compounds Inhibiting Multi-Organ Fibrosis.

Drug Des Devel Ther

January 2025

Hubei Selenium and Human Health Institute, The Central Hospital of Enshi Tujia and Miao Autonomous Prefecture, Enshi, 445000, People's Republic of China.

Selenium (Se), a critically essential trace element, plays a crucial role in diverse physiological processes within the human body, such as oxidative stress response, inflammation regulation, apoptosis, and lipid metabolism. Organ fibrosis, a pathological condition caused by various factors, has become a significant global health issue. Numerous studies have demonstrated the substantial impact of Se on fibrotic diseases.

View Article and Find Full Text PDF

Antifibrotic potential of reserpine (alkaloid) targeting Keap1/Nrf2; oxidative stress pathway in CCl-induced liver fibrosis.

Chem Biol Interact

February 2025

Centre of Excellence in Molecular Biology, University of the Punjab, Thokar Niaz Baig, Lahore, 53700, Pakistan; Applied and Functional Genomics Lab, Centre of Excellence in Molecular Biology, University of the Punjab, Lahore, Pakistan. Electronic address:

The death rate due to liver cancer approaches 2 million annually, the majority is attributed to fibrosis. Currently, there is no efficient, safe, non-toxic, and anti-fibrotic drug available, suggesting room for better drug discovery. The current study aims to evaluate the anti-fibrotic role of reserpine, an alkaloid plant compound against CCl-induced liver fibrosis.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!