Diverse Molecular Targets for Chalcones with Varied Bioactivities

Zhou, Bo; Xing, Chengguo

doi:10.4172/2161-0444.1000291

Cited by 107 publications

(128 citation statements)

References 183 publications

(184 reference statements)

Supporting

Mentioning

124

Contrasting

Unclassified

Order By: Relevance

“…Chalcones possess a wide range of biological activities, mainly against parasites [7 -9] and, several antiparasitic mechanisms have been reported and proposed. [12,21] Considering that chalcones 1 and 3 causing extensive morphological alteration on the tegument of adult schistosomes, ATPDase inhibition may not be the only suggested target of schistosomicidal action and other mechanisms may be involved. In this regard, it is reported that the therapeutic potential of chalcones is related to their structure as α,β-unsaturated ketones and, therefore, to their action as Michael acceptors, which could capture nucleophiles, such as cysteine, and bind covalently to proteins and enzymes.…”

Section: Resultsmentioning

confidence: 99%

In Vitro and in Vivo Antischistosomal Activities of Chalcones

Pereira

Alves

Silveira

et al. 2018

Chemistry & Biodiversity

View full text Add to dashboard Cite

In this study, we evaluated the in vitro and in vivo schistosomicidal activities of chalcones against Schistosoma mansoni worms. In vitro assays revealed that chalcones 1 and 3 were the most active compounds, without affecting significantly mammalian cells. Confocal laser scanning microscopy and scanning electron microscopy studies revealed reduction on the numbers of tubercles and morphological alterations in the tegument of S. mansoni worms after in vitro incubation with chalcones 1 and 3. In a mouse model of schistosomiasis, the oral treatment (400 mg/kg) with chalcone 1 or 3 significantly caused a total worm burden reduction in mice. Chalcone 1 showed significant inhibition of the S. mansoni ATP diphosphohydrolase activity, which was corroborated by molecular docking studies. The results suggested that chalcones could be explored as lead compounds with antischistosomal properties.

show abstract

Section: Resultsmentioning

confidence: 99%

In Vitro and in Vivo Antischistosomal Activities of Chalcones

Pereira

Alves

Silveira

et al. 2018

Chemistry & Biodiversity

View full text Add to dashboard Cite

show abstract

“…1,290–292 Numerous synthetic (Figure 8) and natural chalcones (Table 1) have been reported to exhibit antimicrotubule activities.…”

Section: Medicinal Aspects Of Chalconesmentioning

confidence: 99%

“…Chalcones have been extensively studied, with many minireviews published 1,3,4,7–22 . However, the accurate mechanisms of action for the wide-ranging biological activities of chalcones are still not well understood.…”

Section: Introductionmentioning

confidence: 99%

Chalcone: A Privileged Structure in Medicinal Chemistry

et al. 2017

View full text Add to dashboard Cite

Privileged structures have been widely used as an effective template in medicinal chemistry for drug discovery. Chalcone is a common simple scaffold found in many naturally occurring compounds. Many chalcone derivatives have also been prepared due to their convenient synthesis. These natural products and synthetic compounds have shown numerous interesting biological activities with clinical potentials against various diseases. This review aims to highlight the recent evidence of chalcone as a privileged scaffold in medicinal chemistry. Multiple aspects of chalcone will be summarized herein, including the isolation of novel chalcone derivatives, the development of new synthetic methodologies, the evaluation of their biological properties, and the exploration of the mechanisms of action as well as target identification. This review is expected to be a comprehensive, authoritative, and critical review of the chalcone template to the chemistry community.

show abstract

“…In many instances, a single chalcone may demonstrate multiple bioactive properties. These diverse bioactivities may be attributed to the flexible structural conformation of the chalcone backbone, leading to promiscuous substrate behavior [11]. Two chalcones, 4-hydroxyderricin (1) and xanthoangelol (2), are the most abundant in this plant and possess cytotoxic, anti-inflammatory, and antidiabetic properties [12].…”

Section: Introductionmentioning

confidence: 99%

A Review of the Medicinal Uses and Pharmacology of Ashitaba

Caesar

Cech

2016

Planta Med

View full text Add to dashboard Cite

Medicinal plants are commonly employed for therapeutic purposes throughout the world. A recent National Health Interview Survey estimated that nearly 18 % of adults in the United States regularly took non-vitamin, non-mineral dietary supplements in 2012 [1]. Because of the popularity of herbal medicines, it is important to understand the chemical basis behind the purported activities of botanicals. Angelica, a member of the Apiaceae (Umbelliferae) family, is a large genus comprised of over 60 species. Members of the genus have been utilized as medicines across the world, most notably in Asia, to treat numerous ailments, including influenza, hepatitis, arthritis, indigestion, fever, and microbial infections [2]. An increasing number of studies are being conducted on a medicinally promising member of the genus, Angelica keiskei Koidzumi (Apiaceae), or ashitaba. This large leafy perennial plant native to the Pacific coast of Japan is used throughout Asia for its diuretic, laxative, stimulant, and galactagogue properties [3]. In the past decade, several active constituents representing chalcones, flavanones, and coumarins have been isolated and characterized from ashitaba, and several bioactiv-ities have been described. This review presents the current progress on ashitaba pharmacological studies, with a focus on isolated secondary metabolites, biological activity, toxicological data, and clinical relevance. Bioactive Metabolites Isolated from Ashitaba ! Chalcones Most of the literature on the bioactive metabolites from ashitaba concerns the diverse activity of various chalcones (l " Table 1 and Fig. 1), which are most abundant in the root bark of the plant [4]. Chalcones are formed from phenylpropanoid starter units, extended with three malonyl-CoA molecules. The resulting polyketide is folded by the enzyme chalcone synthase to promote Claisen condensations and subsequent enolizations [5]. Interestingly, the bioactive chalcones found in ashitaba are prenylated at the 5′-position (l " Fig. 1), indicating that these molecules have undergone multiple biosynthetic steps, travelling through the acetate, shikimate, and isoprenoid pathways.

show abstract

Diverse Molecular Targets for Chalcones with Varied Bioactivities

Cited by 107 publications

References 183 publications

In Vitro and in Vivo Antischistosomal Activities of Chalcones

In Vitro and in Vivo Antischistosomal Activities of Chalcones

Chalcone: A Privileged Structure in Medicinal Chemistry

A Review of the Medicinal Uses and Pharmacology of Ashitaba

Contact Info

Product

Resources

About