Around 50 % of the worldwide population is affected by dandruff, which is triggered by a variety of factors. The yeast Malassezia globosa has been labeled as the most probable causative agent for the onset of dandruff. The β-carbonic anhydrase (CA) of MgCA was recently validated as an anti-dandruff target, with its inhibition being responsible for in vivo growth defects in the fungus. As classical CA inhibitors of the sulfonamide type give rise to permeability problems through biological membranes, finding non-sulfonamide alternatives for MgCA inhibition is of considerable interest in the cosmetic field. We recently screened a large library of human (h) CA inhibitors for MgCA inhibition, including different chemotypes, such as monothiocarbamates, dithiocarbamates, phenols, and benzoxaboroles. Herein, we expanded the research toward new MgCA inhibitors by considering a set of natural polyphenols (including flavones, flavonols, flavanones, flavanols, isoflavones, and depsides) that exhibited MgCA inhibitory activity in the micromolar range, as well as selectivity for the fungal isozyme over off-target human isoforms. The binding mode of representative derivatives within the MgCA catalytic cleft was investigated by docking studies using a homology-built model.
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http://dx.doi.org/10.1002/cmdc.201800015 | DOI Listing |
Nat Commun
January 2025
Modern Research Center for Traditional Chinese Medicine, Beijing Institute of Traditional Chinese Medicine, Beijing University of Chinese Medicine, 102488, Beijing, PR China.
Echinacoside (ECH), one of the most representative phenylethanoid glycosides (PhGs), has considerable neuroprotective effects and is an effective ingredient in numerous commercial drugs. Here, we elucidate the complete ECH biosynthetic pathway in the medicinal plant Cistanche tubulosa. In total, 14 related genes are cloned and functionally characterized.
View Article and Find Full Text PDFFood Chem
January 2025
Department of Industrial Engineering, University of Padova, Via Marzolo 9, 35131 Padova, Italy. Electronic address:
The study evaluated the application of a novel high-pressure microbial inactivation method combining dense carbon dioxide with modified atmosphere packaging on organic fresh-cut squash (Cucurbita moschata). Approximately 4 g or 32 g of squash was packed in plastic pouches filled with CO to test two different gas-to-product ratios and treated with the high-pressure method at previously optimized process conditions (45 °C, 6.0 MPa and 40 min).
View Article and Find Full Text PDFDiscov Oncol
January 2025
Department of Biotechnology, School of Bio Sciences and Technology (SBST), Vellore Institute of Technology (VIT), Vellore, 632014, India.
Cancer, one of the deadliest diseases, has remained the epicenter of biological research for more than seven decades. Yet all the efforts for a perfect therapeutic cure come with certain limitations. The use of medicinal plants and their phytochemicals as therapeutics has received much attention in recent years.
View Article and Find Full Text PDFCurr Med Chem
January 2025
Healthy Ageing Research Centre, Neyshabur University of Medical Sciences, Neyshabur, Iran.
Neuroblastoma (NB) is a rare embryonal neuroendocrine tumor that primarily affects children aged 5 years old or younger. In advanced stages, NB requires a multifaceted treatment approach, including a combination of surgery, chemo, and radiation therapy. However, high-risk NB is still associated with poor prognosis, long-term side effects, and a high chance of relapse.
View Article and Find Full Text PDFIndian J Clin Biochem
January 2025
Department of Biochemistry, College of Medicine and J.N.M Hospital, WBUHS, Kalyani, West Bengal 741235 India.
Radiation therapy uses ionizing radiation (IR) to kill cancer cells. However, during radiotherapy normal cells are also damaged and killed by the generation of reactive oxygen species. Polyphenolic compounds are known to mitigate the damaging effects of radiation.
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