Mangostanin Derivatives as Novel and Orally Active Phosphodiesterase 4 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.

Author: DengJinhui, HeXixin, HuangYi-You, HuangYue, LiangJinhao, LuoHai-Bin, TianYi-Jing, XieXi, ZhouQian, ZhuJiaqi, ZhuZiran

Paper Details 
Original Abstract of the Article :
Idiopathic pulmonary fibrosis (IPF) is a progressive lung disease, and its incidence rate is rapidly rising. However, effective therapies for the treatment of IPF are still lacking. Phosphodiesterase 4 (PDE4) inhibitors were reported to be potential anti-fibrotic agents, but their clinical use was h...See full text at original site
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引用元:
https://doi.org/10.1021/acs.jmedchem.1c01085

データ提供:米国国立医学図書館(NLM)

Mangostanin Derivatives: A New Hope for Idiopathic Pulmonary Fibrosis

The lung, a vital organ that allows us to breathe, can be afflicted by idiopathic pulmonary fibrosis (IPF), a progressive disease with no known cure. This research, published in Journal of Medicinal Chemistry, explores the potential of mangostanin derivatives as novel and orally active PDE4 inhibitors for treating IPF. The research investigated the efficacy and safety of these derivatives in preclinical studies, offering hope for a new therapeutic approach to this debilitating disease.

The Potential of Mangostanin Derivatives

The study demonstrated that a novel mangostanin derivative, designated as 18a, exhibited potent inhibitory activity against PDE4, a key enzyme involved in the development of IPF. Importantly, 18a showed a favorable safety profile, lacking the emetic side effects associated with other PDE4 inhibitors. Furthermore, oral administration of 18a in a bleomycin-induced IPF rat model demonstrated comparable anti-fibrotic effects to pirfenidone, a currently used anti-fibrotic drug.

A New Era for IPF Treatment

This research offers a promising avenue for developing new treatments for IPF, a disease that currently lacks effective therapies. The development of safe and effective PDE4 inhibitors, like 18a, could revolutionize IPF treatment, offering hope for patients struggling with this devastating condition. Remember, research and innovation are essential for finding solutions to the challenges of human health.

Dr.Camel's Conclusion

The discovery of mangostanin derivatives as potential anti-fibrotic agents is like finding a hidden oasis in the desert of IPF research. This research offers a new path toward treating this debilitating disease, promising a future where patients can breathe easier. Just as a camel adapts to the harsh desert environment, researchers are constantly adapting and innovating to find solutions for complex health challenges. This research is a testament to the dedication and perseverance of scientists in their quest to improve human health.

Date :
  1. Date Completed 2021-12-06
  2. Date Revised 2021-12-14
Further Info :

Pubmed ID

34520193

DOI: Digital Object Identifier

10.1021/acs.jmedchem.1c01085

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SNS
PICO Info
in preparation
Languages

English

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