Niosomes of active Fumaria officinalis phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action
Background: Fumaria officinalis (F. officinalis, FO) has been used in many inflammatory and painful-ailments. The
main aim of this work is to perform an in-depth bio-guided phytochemical investigation of F. officinalis by identifying
its main-active ingredients. Optimizing pharmacokinetics via niosomal-preparation will also be done to enhance their
in vivo antineuropathic and anti-inflammatory potentials, and to explore their possible-mechanism of actions.
Methods: Bio-guided phytochemical-investigations including fractionation, isolation, chromatographic-standardization,
and identification of the most active compound(s) were done. Optimized niosomal formulations of F. officinalis
most active compound(s) were prepared and characterized. An in vivo biological-evaluation was done exploring
acute, subchronic, and chronic alloxan-induced diabetes and diabetic-neuropathy, and carrageenan-induced acute
inflammatory-pain and chronic-inflammatory edema.
Results: In-vivo bio-guided fractionation and chromatographic phytochemical-analysis showed that the alkaloidrich
fraction (ARF) is the most-active fraction. ARF contained two major alkaloids; Stylopine 48.3%, and Sanguinarine
51.6%. In-vitro optimization, analytical, and in vivo biological-investigations showed that the optimized-niosome, Nio-
2, was the most optimized niosomal formulation. Nio-2 had particle size 96.56 ± 1.87 nm and worked by improving
the pharmacokinetic-properties of ARF developing adequate entrapment-efficiency, rapid-degradation, and acceptable
stability in simulated GI conditions. FO, ARF, and Nio 2 were the most potent antidiabetic and anti-inflammatory
compounds. The reduction of the pro-inflammatory tumor necrosis factor-alpha (TNF-alpha) and Interleukin 6 (IL-6),
and elevation the anti-inflammatory factor IL-10 levels and amelioration of the in vivo oxidative-stress might be the
main-mechanism responsible for their antinociceptive and anti-inflammatory activities.
Conclusions: Fumaria officinalis most-active fraction was identified as ARF. This study offers an efficient and novel
practical oral formulation ameliorating various inflammatory conditions and diabetic complications especially
Chinese Medicine,DOI: https://doi.org/10.1186/s13020-020-00321-1, ISSN: 1749-8546, Volume: 15, Issue: 40, Pages Range: 1-22,