Dataset Information

Naturally occurring phenylethanoids and phenylpropanoids: antimalarial potential.

ABSTRACT: Malaria as an infectious disease is one of the world's most dangerous parasitic diseases. There is an urgent need for the development of new antimalarial drugs. Natural products are a very rich source of new bioactive compounds. Our research aims to shed light on the recent studies which demonstrated the antimalarial potential of phenylpropanoids as a major natural-products class. This study involves an in silico analysis of naturally-occurring phenylpropanoids and phenylethanoids which showed 25 compounds with moderate to strong binding affinity to various amino acid residues lining the active site; P. falciparum kinase (PfPK5), P. falciparum cytochrome bc1 complex (cyt bc1), and P. falciparum lysyl-tRNA synthetase (PfKRS1); of Plasmodium falciparum parasite, a unicellular protozoan which causes the most severe and life-threatening malaria. Furthermore, the study was augmented by the assessment of antiplasmodial activity of glandularin, a naturally occurring dibenzylbutyrolactolic lignan, against chloroquine-sensitive 3D7 strain of P. falciparum using SYBR green I-based fluorescence assay, which showed high antimalarial activity with IC₅₀ value of 11.2 μM after 24 hours of incubation. Our results highlight phenylpropanoids and glandularin in particular as a promising chemical lead for development of antimalarial drugs.

SUBMITTER: Abdelmohsen UR

PROVIDER: S-EPMC10483269 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature

ACCESS DATA

Publications

Naturally occurring phenylethanoids and phenylpropanoids: antimalarial potential.

Abdelmohsen Usama Ramadan UR Bayoumi Soad A L SAL Mohamed Nesma M NM Mostafa Yaser A YA Ngwa Che J CJ Pradel Gabriele G Farag Salwa F SF

RSC advances 20230907 38

Malaria as an infectious disease is one of the world's most dangerous parasitic diseases. There is an urgent need for the development of new antimalarial drugs. Natural products are a very rich source of new bioactive compounds. Our research aims to shed light on the recent studies which demonstrated the antimalarial potential of phenylpropanoids as a major natural-products class. This study involves an <i>in silico</i> analysis of naturally-occurring phenylpropanoids and phenylethanoids which s ...[more]

PMID: 37692342

Similar Datasets

Project description:Peptides have revealed a large range of biological activities with high selectivity and efficiency for the development of new drugs, including neuroprotective agents. Therefore, this work investigates the neuroprotective properties of naturally occurring peptides, endomorphin-1 (EM-1), endomorphin-2 (EM-2), rubiscolin-5 (R-5), and rubiscolin-6 (R-6). We aimed at answering the question of whether well-known opioid peptides can counteract cell injury in a common in vitro model of Parkinson's disease (PD). Antioxidant activity of these four peptides was evaluated by the 2-diphenyl-1-picrylhydrazyl radical (DPPH) scavenging activity, oxygen radical absorbance capacity (ORAC), and ferric-reducing antioxidant power (FRAP) assays, while neuroprotective effects were assessed in a neurotoxic model induced by 6-hydroxydopamine (6-OHDA) in a human neuroblastoma cell line (SH-SY5Y). The mechanisms associated with neuroprotection were investigated by the determination of mitochondrial membrane potential (MMP), reactive oxygen species (ROS) production, and Caspase-3 activity. Among the tested peptides, endomorphins significantly prevented neuronal death induced by 6-OHDA treatment, decreasing MMP (EM-1) or Caspase-3 activity (EM-2). Meanwhile, R-6 showed antioxidant potential by FRAP assay and exhibited the highest capacity to recover the neurotoxicity induced by 6-OHDA via attenuation of ROS levels and mitochondrial dysfunction. Generally, we hypothesize that peptides' ability to suppress the toxic effect induced by 6-OHDA may be mediated by different cellular mechanisms. The protective effect caused by endomorphins results in an antiapoptotic effect (mitochondrial protection and decrease in Caspase-3 activity), while R-6 potency to increase a cell's viability seems to be mediated by reducing oxidative stress. Our results may provide new insight into neurodegeneration and support the short peptides as a potent drug candidate to treat PD. However, further studies should be conducted on the detailed mechanisms of how tested peptides could suppress neuronal injuries.

Dataset Information

Naturally occurring phenylethanoids and phenylpropanoids: antimalarial potential.

Publications

Naturally occurring phenylethanoids and phenylpropanoids: antimalarial potential.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets