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Optimizing physicochemical properties of naturalantioxidants and geroprotectors: L-carnosine and melatonin
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Resumo(s)
The issue of “Healthy Ageing” has become a significant challenge due to the continuous grow
of World Population Ageing. Advancing health and well-being into old age and ensuring
supportive environments is a main objective of NATO’s Department of Economic and Social
Affairs Population Division [1].
Natural antioxidants such as L-carnosine and melatonin have been successfully used as
geroprotectors. They reduce the risk of developing ageing-related diseases which is one the
main aspects of healthy ageing. New formulation of the existing APIs is a widely used
approach to optimize their physicochemical properties. Carnosine underwent reactions with a
number of organic acids resulting in the discovery of seven new salts. The obtained salts were
characterized by X-ray powder diffraction and thermal analyses. The structures were
determined using X-ray Powder Diffraction (XRPD). The carnosine salts with glycolic and
succinic acids might be of higher interest since both components possess antioxidant activity
and carnosine, when used as a nutraceutical is usually combined with other antioxidants.
Thus, the new formulation of carnosine as a salt with an acid possessing antioxidant activity
can enhance its biological activity. Melatonin was co-crystallized with a number of coformers
from various chemical groups. Two new co-crystals of melatonin with DABCO and
piperazine were obtained by using mechanochemical technique (kneading). The structure of
melatonin-DABCO co-crystal was established from a single crystal obtained by
recrystallization from dichloromethane. The structure of melatonin-piperazine was solved
using XRPD. Though only one of the obtained co-crystals can find a direct application in
Pharmaceutical industry (DABCO does not belong to the GRAS list), our results confirm the
reactivity of melatonin in co-crystallization processes, and emphasizes the need to continue
the search for an improved formulation.
Descrição
Dissertação de mestrado, Inovação Quimica e Regulamentação, Faculdade de Ciências e Tecnologia, Universidade do Algarve, 2015
Palavras-chave
Antioxidantes Engenharia dos cristais L-carnosina Melatonina