bims-antpol 2024-06-09 papers

Issue of 2024–06–09
three papers selected by
Rick Sheridan, EMSKE Phytochem

Food Res Int. 2024 Jul;pii: S0963-9969(24)00574-X. [Epub ahead of print]188 114504

Structure-function relationships in (poly)phenol-enzyme binding: Direct inhibition of human salivary and pancreatic α-amylases.

Rizliya Visvanathan, Michael J Houghton, Elizabeth Barber, Gary Williamson.

(Poly)phenols inhibit α-amylase by directly binding to the enzyme and/or by forming starch-polyphenol complexes. Conventional methods using starch as the substrate measure inhibition from both mechanisms, whereas the use of shorter oligosaccharides as substrates exclusively measures the direct interaction of (poly)phenols with the enzyme. In this study, using a chromatography-based method and a short oligosaccharide as the substrate, we investigated the detailed structural prerequisites for the direct inhibition of human salivary and pancreatic α-amylases by over 50 (poly)phenols from the (poly)phenol groups: flavonols, flavones, flavanones, flavan-3-ols, polymethoxyflavones, isoflavones, anthocyanidins and phenolic acids. Despite being structurally very similar (97% sequence homology), human salivary and pancreatic α-amylases were inhibited to different extents by the tested (poly)phenols. The most potent human salivary α-amylase inhibitors were luteolin and pelargonidin, while the methoxylated anthocyanidins, peonidin and petunidin, significantly blocked pancreatic enzyme activity. B-ring methoxylation of anthocyanidins increased inhibition against both human α-amylases while hydroxyl groups at C3 and B3' acted antagonistically in human salivary inhibition. C4 carbonyl reduction, or the positive charge on the flavonoid structure, was the key structural feature for human pancreatic inhibition. B-ring glycosylation did not affect salivary enzyme inhibition, but increased pancreatic enzyme inhibition when compared to its corresponding aglycone. Overall, our findings indicate that the efficacy of interaction with human α-amylase is mainly influenced by the type and placement of functional groups rather than the number of hydroxyl groups and molecular weight.

Keywords: Carbohydrate digestion; Enzyme inhibition; Flavonoid; Polyphenol; Quercetin; Starch

DOI: https://doi.org/10.1016/j.foodres.2024.114504

Drug Discov Today. 2024 Jun 01. pii: S1359-6446(24)00175-2. [Epub ahead of print] 104050

Unlocking the potential of flavonoid-based cocrystal and co-amorphous systems.

Khushi Rode, Indrani Maji, Srushti Mahajan, Pankaj Kumar Singh.

Flavonoids are polyphenolic compounds that have multiple benefits in treating various life-threatening diseases. Despite their diverse pharmacological activities, the market potential of flavonoids is hampered due to their poor solubility and low bioavailability after oral administration. The current review highlights the role of cocrystals and co-amorphous systems (CAMs) in enhancing the solubility, permeability, bioavailability, and therapeutic efficacy of flavonoids. It also explains the significance of flavonoid-based coformers in the formation of cocrystals and CAMs with other APIs to improve their efficacy. Future perspectives, patented formulations, commercial medications (including their phases of clinical trials), and challenges associated with the use of flavonoid-based cocrystals and CAMs are also mentioned in the review.

Keywords: bioavailability; co-amorphous systems (CAM); cocrystals; coformer; flavonoids

DOI: https://doi.org/10.1016/j.drudis.2024.104050

Curr Drug Deliv. 2024 Jun 06.

Nanovesicles as Potential Carriers for Delivery of Antiviral Drugs: A Comprehensive Review.

Sabitri Bindhani, Amit Kumar Nayak.

Different nanocarriers-based strategies are now extensively being used as an important strategy for improving drug efficacy and responsiveness, reducing toxicity issues related to drugs and harmful side effects, and overcoming the numerous significant difficulties related to absorption and bioavailability. Amongst different nanocarriers, nanovesicles are excellent and versatile systems for effectively delivering biomolecules, drugs, and targeted ligand distribution and location. Nanovesicles are nanosized self-assembling spherical capsules with an aqueous core and one/more lipid(s) layers. Several synthetic nanovesicles have been developed and investigated for their prospective uses in delivering drugs, proteins, peptides, nutrients, etc. Important procedures for nanovesicle manufacturing are thin-film hydration, unshaken method, ethanol injection, ether injection, proliposomes, freeze-drying, hot method, cold method, reverse-phase evaporation, and ultrasonication. Liposomes, liposomes, ethosomes, exosomes, and transferosomes (elastic vesicles) are the nonvesicular candidates extensively investigated to deliver antiviral drugs. This review article comprehensively reviews different nanovesicles, their compositions, manufacturing, and applications as potential carriers for effectively delivering different antiviral drugs to treat viral diseases.

Keywords: Nanocarriers; antiviral drugs; drug delivery.; liposomes; nanovescicles

DOI: https://doi.org/10.2174/0115672018313783240603114509