Biological Activity of Selected Natural and Synthetic Terpenoid Lactones

Surowiak, Alicja Karolina; Balcerzak, Lucyna; Lochyński, Stanisław; Strub, Daniel

doi:10.3390/ijms22095036

Cited by 25 publications

(18 citation statements)

References 102 publications

(121 reference statements)

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“…Currently, this issue is mitigated by the development of modern and sophisticated therapies such as gene therapy, immunotherapy, or targeted therapy which show promising clinical outcomes but at high costs. A more approachable path consists of the replacement of synthetic drugs with natural compounds which exhibit similar pharmacological activities and can be chemically modified in order to obtain a suitable bioavailability [1]. Amongst all-natural bioactive compounds, triterpenes represent one of the most promising categories, not only for their large plethora of compounds but also for their wide range of pharmacological activities, such as anti-tumor, antioxidant, anti-viral, anti-microbial, cardioprotective, antidiabetic, neuroprotective, etc., [2].…”

Section: Introductionmentioning

confidence: 99%

The Optimized Delivery of Triterpenes by Liposomal Nanoformulations: Overcoming the Challenges

Milan

Mioc

Prodea

et al. 2022

IJMS

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The last decade has witnessed a sustained increase in the research development of modern-day chemo-therapeutics, especially for those used for high mortality rate pathologies. However, the therapeutic landscape is continuously changing as a result of the currently existing toxic side effects induced by a substantial range of drug classes. One growing research direction driven to mitigate such inconveniences has converged towards the study of natural molecules for their promising therapeutic potential. Triterpenes are one such class of compounds, intensively investigated for their therapeutic versatility. Although the pharmacological effects reported for several representatives of this class has come as a well-deserved encouragement, the pharmacokinetic profile of these molecules has turned out to be an unwelcomed disappointment. Nevertheless, the light at the end of the tunnel arrived with the development of nanotechnology, more specifically, the use of liposomes as drug delivery systems. Liposomes are easily synthesizable phospholipid-based vesicles, with highly tunable surfaces, that have the ability to transport both hydrophilic and lipophilic structures ensuring superior drug bioavailability at the action site as well as an increased selectivity. This study aims to report the results related to the development of different types of liposomes, used as targeted vectors for the delivery of various triterpenes of high pharmacological interest.

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Section: Introductionmentioning

confidence: 99%

The Optimized Delivery of Triterpenes by Liposomal Nanoformulations: Overcoming the Challenges

Milan

Mioc

Prodea

et al. 2022

IJMS

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“…Lactones are a group of compounds widely distributed in nature [ 1 , 2 , 3 , 4 ]. Chemically, they can be classified as intramolecular esters of hydroxycarboxylic acids with different ring sizes.…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial Activity of Lactones

Mazur

Masłowiec

2022

Antibiotics

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The development of bacterial resistance to antibiotics and the consequent lack of effective therapy is one of the biggest problems in modern medicine. A consequence of these processes is an urgent need to continuously design and develop novel antimicrobial agents. Among the compounds showing antimicrobial potential, lactones are a group to explore. For centuries, their antimicrobial activities have been used in folk medicine. Currently, novel lactone compounds are continuously described in the literature. Some of those structures exhibit high antimicrobial potential and some are an inspiration for design and synthesis of future drugs. This paper describes recent developments on antimicrobial lactones with smaller ring sizes, up to seven membered ε-lactones. Their isolation from natural sources, chemical synthesis, synergistic activity with antibiotics, and effects on quorum sensing are presented herein.

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“…Artemisinin (Art), as a sesquiterpene lactone with peroxyl group extracted from Artemisia annua L., has been widely used in the treatment of malaria due to the characteristics of high efficiency and low toxicity, and has saved millions of lives in the past 40 years (Correa et al, 2019). In recent years, it has been reported to treat inflammation, immune regulation, anti-fibrosis, and other pathological processes (Pacios-Michelena et al, 2021;Surowiak et al, 2021;Zhang et al, 2021b). Dihydroartemisinin (DHA) is a derivative of artemisinin and harbors nearly 10 times bioavailability as much as that of artemisinin.…”

Section: Introductionmentioning

confidence: 99%

Dihydroartemisinin ameliorates palmitate-induced apoptosis in cardiomyocytes via regulation on miR-133b/Sirt1 axis

Qi¹,

Xu²,

Li³

et al. 2022

Biocell

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Excessive fat ectopically deposited in the non-adipose tissues is considered as one of the leading causes of myopathy. The aim of this study was to investigate the role of Dihydroartemisinin (DHA) in palmitate (PAL)incubated H9c2 cells (lipotoxicity-induced cell injury model). Cell viability of PAL-treated cells was determined by MTT assay, and apoptotic regulators were examined by qRT-PCR and western blot analysis, in the absence or in the presence of DHA, respectively. Expression levels of miR-133b and Sirt1 were also evaluated by qRT-PCR and western blotting examination. PAL decreased the viability of H9c2 cells and enhanced the expression of apoptotic genes. DHA reversed the effect of PAL on cell viability and lowed the level of Caspase3 and Bax. It also lowered the expression of miR-133b, while enhanced the expression of Bcl-2. Sirt1 was revealed as target of miR-133b through transcriptional regulation and the process was affected by DHA. DHA partially protected against the PAL-induced lipotoxicity by influencing the expression of miR-133b that hindered the activity of Sirt1. DHA may be used as a potential treatment in clinical management for lipotoxicity induced heart complications.

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Biological Activity of Selected Natural and Synthetic Terpenoid Lactones

Cited by 25 publications

References 102 publications

The Optimized Delivery of Triterpenes by Liposomal Nanoformulations: Overcoming the Challenges

The Optimized Delivery of Triterpenes by Liposomal Nanoformulations: Overcoming the Challenges

Antimicrobial Activity of Lactones

Dihydroartemisinin ameliorates palmitate-induced apoptosis in cardiomyocytes via regulation on miR-133b/Sirt1 axis

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