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Discovery of Bioactive Compounds for Inflammatory Diseases

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (15 October 2022) | Viewed by 2840

Special Issue Editors

Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Taipa 999078, Macau, China
Interests: Chinese medicine; inflammatory diseases; pharmaceutics; drug delivery; quality control

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Guest Editor
Department of Anaesthesiology, LKS Faculty of Medicine, The University of Hong Kong, Hong Kong 999077, China
Interests: perioperative medicine; anaesthesia and neuroinflammation; perioperative cardioprotection; neurodegenerative diseases
Department of medicine, Shenzhen University, Shenzhen 518000, China
Interests: Chinese medicine; inflammatory diseases; pharmaceutics; drug delivery

Special Issue Information

Dear Colleagues,

Inflammation is a complex physiological response of the body in defense against various harmful stimuli. However, an excessive or prolonged inflammatory response might cause continuous damage to the body and induce different chronic diseases. In recent years, there has been an ongoing discovery of bioactive agents with anti-inflammatory effects originating from naturally occurring compounds as well as their derivates, and this has become one of the most exciting areas in drug development. In addition, different research models and methodologies also play important roles in demonstrating the effectiveness and elucidating the underlying biological mechanisms of such compounds for inflammatory diseases.

This Special Issue intends to capture the state of the art and contemporary progress in this field. Proposed topics include novel methods for the discovery and testing of anti-inflammatory compounds, natural products, synthesized compounds, novel mechanisms and targets of anti-inflammation, advanced models (both in vitro and in vivo), the development of research methodologies and technologies, etc.

We expect that combined, submitted articles will give a realistic assessment of the value of bioactive compounds to future pharmaceutical discovery.

Dr. Hua Yu
Dr. Tin-chun Gordon Wong
Dr. Wei Xiong
Guest Editors

Manuscript Submission Information

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Keywords

  • inflammatory diseases
  • natural products
  • structure-activity relationship
  • anti-Inflammation
  • antioxidant
  • experimental models
  • drug research and development

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Published Papers (1 paper)

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Research

29 pages, 6850 KiB  
Article
Pharmacokinetics, Prostate Distribution and Metabolic Characteristics of Four Representative Flavones after Oral Administration of the Aerial Part of Glycyrrhiza uralensis in Rats
by Haifan Liu, Guanhua Chang, Wenquan Wang, Zuen Ji, Jie Cui and Yifeng Peng
Molecules 2022, 27(10), 3245; https://doi.org/10.3390/molecules27103245 - 19 May 2022
Cited by 6 | Viewed by 2375
Abstract
(1) Background: The aerial part of G. uralensis had pharmacological effects against chronic non-bacterial prostatitis (CNP), and flavonoids are the main efficacy components. The purpose of this study was to obtain the pharmacokinetics, prostate distribution and metabolic characteristics of some flavonoids in rats. [...] Read more.
(1) Background: The aerial part of G. uralensis had pharmacological effects against chronic non-bacterial prostatitis (CNP), and flavonoids are the main efficacy components. The purpose of this study was to obtain the pharmacokinetics, prostate distribution and metabolic characteristics of some flavonoids in rats. (2) Methods: The prototype flavones and the metabolites of four representative flavonoids, namely puerarin, luteolin, kaempferol and pinocembrin in plasma, prostate, urine and feces of rats were analyzed by UPLC-Q-Exactive Orbitrap-MS. In addition, the pharmacokinetic parameters in plasma and distribution of prostate of four components were analyzed by HPLC-MS/MS. (3) Results: In total, 22, 17, 22 and 11 prototype flavones were detected in the prostate, plasma, urine and feces, respectively. The metabolites of puerarin in the prostate are hydrolysis and glucose-conjugated products, the metabolites of kaempferol and luteolin in the prostate are methylation and glucuronidation, and the metabolites of pinocembrin in the prostate are naringenin, oxidation, sulfation, methylation and glucuronidation products. The t1/2 of puerarin, luteolin, kaempferol and pinocembrin was 6.43 ± 0.20, 31.08 ± 1.17, 18.98 ± 1.46 and 13.18 ± 0.72 h, respectively. The concentrations of the four flavonoids in prostate were ranked as kaempferol > pinocembrin > luteolin > puerarin. (4) Conclusions: Methylation and glucuronidation metabolites were the main metabolites detected in the prostate. A sensitive and validated HPLC–MS/MS method for simultaneous determination of puerarin, luteolin, kaempferol and pinocembrin in rat plasma and prostate was described, and it was successfully applied to the pharmacokinetic and prostate distribution studies. Full article
(This article belongs to the Special Issue Discovery of Bioactive Compounds for Inflammatory Diseases)
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