Antimicrobial Activity of Curcumin and Deuterated Curcumin

Abstract

Deuterium (D) and hydrogen (H) are bioisosteres because they are similar in size and shape with alike physiochemical properties and hence expect similar biological activity. The purpose of replacing H with D is to extend the time the active drug species spends in plasma, resulting in increased effectiveness and/or the avoidance of unwanted side effects. Deutetrabenazine was the first deuterated medicinal molecule, recently authorized by the FDA for the treatment of chorea “an involuntary movement disorder” associated with tardive dyskinesia and Huntington’s disease. Curcumin is found to have a long history of use in human disorders such as inflammation, metabolic syndrome, arthritis, anxiety, antimicrobial, hyperlipidemia, etc., Curcumin’s oral bioavailability and water solubility are low, resulting in poor absorption, rapid metabolism, and systemic elimination. To overcome curcumin’s drawbacks, H/D exchange was performed in curcumin, which was then characterized and tested for antibacterial, antifungal, and anti-tubercular activities. The deuterated compound showed equipotent antibacterial activity when compared with the non-deuterated compound and had better anti-fungal, anti-tubercular activity compared to its parent compound.

Enhancing the Properties of Natural Products and Other Drugs: Deuterium: A Novel Approach

“…This difference in the value of partition coefficient and solubility could be mainly due to the exchange of isotope deuterium instead of hydrogen. The slight change in pharmacokinetic profile is related to the difference in bond character between C-H and C-D. As a result, exchanging hydrogen for deuterium at the right place in the chemical structure can considerably slow down metabolism, potentially increasing plasma drug concentration 21 .…”

Phytochemical Screening of <i>Diospyros paniculata</i> Bark and <i>In Vitro</i> Cytotoxic Study on Human Breast Cancer Cell Line

“…The parts of the tree have different uses. The leaves are used in fish poison, fruits to heal burns, a decoction of fruits for gonorrhoea and blood poisoning, and stem bark in rheumatism and ulcers, seeds of the plant have been traditionally used as a remedy for respiratory ailments, such as coughs and asthma, In some regions, the twigs and roots of D. paniculata are employed in folk medicine to manage conditions like diabetes and hypertension 11 . The present work focused on the phytochemical profile of methanol extract and its fractionation with different solvents by separating funnel method, in vitro cytotoxicity of all the above fractions tested against MCF-7 cell line by MTT assay, isolation of bioactive from the CF by column chromatography and their characterisation by FTIR, 1 H NMR, and 13 C NMR.…”