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Niosomes of active Fumaria officinalis phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action.

ABSTRACT: 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 alkaloid-rich 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 neuropathic-pain.

SUBMITTER: Raafat KM

PROVIDER: S-EPMC7195756 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature

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Niosomes of active <i>Fumaria officinalis</i> phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action.

Raafat Karim M KM El-Zahaby Sally A SA

Chinese medicine 20200501

<h4>Background</h4><i>Fumaria officinalis</i> (<i>F. officinalis,</i> 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 <i>F. officinalis</i> 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.<h4>Methods< ...[more]

PMID: 32377229

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Project description:Background and aim Natural metabolites are rich in neuroactive and anti-inflammatory phytochemicals. Soapwort or Saponaria officinalis (Sap) has been utilized for its immunomodulatory and ant-rheumatic properties. Thus, the aim is to exploit Sap phytochemically and to investigate Sap isolated active phytochemicals effect to modulate diabetic neuropathy and inflammation, and their possible mechanisms of action. Experimental procedure Bio-guided chromatographic fractionation and phytochemical isolation of the most abundant Sap phytochemicals utilizing RP-HPLC, 13C, and 1H NMR, in-vivo models of diabetes, diabetic neuropathy, and inflammation were used. Glucometers, HbA1c micro-columns, in-vivo hind-paw edema, tail-flick, hot plate, and Von-Frey filaments methods were utilized to investigate the acute, subchronic, and long term diabetes, inflammation, hyperalgesia, and mechanical allodynia. In-vivo antioxidant, inhibitory alpha-amylase, and alpha-glucosidase, and serum insulin levels, IL-6, IL-10, and TNF-alpha cytokines levels were utilized to investigate Sap mechanisms of action. Results and conclusion The phytochemical post-hydrolysis RP-HPLC investigation results show six major peaks; Quillaic acid (12.5%), Quillaic acid 22 β-OH (11.25%), Gypsogenin (21.25%), Phytolaccinic acid (18.75%), Phytolaccinic acid (17.50%), and Echynocystic acid (15.10%). The bio-guided chromatographic fractionation investigation utilizing reversed phase HPLC, 13C and 1H NMR has shown that Quillaic acid (QA) is the most abundant and biologically active compound. Sap 20 mg/kg has shown the highest potency in normalization of blood glucose level (BGL) acutely (6-h), subchronically (eight-days), and longer-term (eight-weeks) correlated to Sap 10 and 7 mg/kg, and QA 0.7, 1.0, 2.0 mg/kg. The highest amelioration of diabetic neuropathy (thermal hyperalgesia and mechanical allodynia) was Sap 20 mg/kg. The anti-inflammatory potentials of Sap 20 mg/kg have shown dominance in decreasing carrageenan-induced in-vivo hind-paw edema. The anti-nociceptive mechanism of action might be due to Sap insulin secretagogue and the in-vivo antioxidant potentials. The reduction of IL-6 cytokines and TNF-alpha, along with the elevation of the IL-10 cytokine level might be the underlying Sap anti-inflammatory mechanism. Phytochemically, QA has shown to be the most abundant and biologically active compound in Sap extract. Sap has shown significant (p < 0.05) anti-diabetic, anti-diabetic neuropathy, and anti-inflammatory effects. Our results provide new insights into the potential effects of Saponaria and Quillaic acid as future alternative therapies against diabetic neuropathy and inflammation. Graphical abstract Image 1 Highlights • Sap and QA were the most potent antidiabetic neuropathy and anti-inflammatory compounds.• The mechanism: TNF-α and IL-6 reduction, IL-10 increase, and antioxidant effect.• Efficient natural extract and active compound improving inflammatory and diabetic neuropathy.

Project description:Prunus cerasus (P. cerasus) is an alternative-medicine used traditionally for amelioration of chronic-ailments marked by elevation in oxidative-stress like neuropathy. The oxidative-stress control was reported to ameliorate the inflammatory-process. This study aimed to phytochemically-investigate P. cerasus most-active phytochemicals utilizing in-vivo biological models to explore their gastroprotective, anti-inflammatory, and antinociceptive potentials and their possible mechanisms of action. Sonication with EtAc was used to extract P. cerasus fruit (Scf), and seed (Scs). The phytochemical-investigation of Scf was performed by RP-HPLC, while that of Scs was explored utilizing GC-FID. A bio-guided-fraction and isolation method was done utilizing column-chromatography, and have shown that cyanidin-3-glucoside (Cy3G) was the most-active constituent in Scf, while linoleic-acid (LA) was the most-active constituent in Scs. Scf, Scs, Cy3G, and LA significantly (p ? 0.05) protected the gastric-mucosa against HCl/EtOH-induced gastric-lesions. Scs (200?mg/kg) has shown the most gastroprotective-potentials, and had comparable-results to ranitidine (50?mg/kg). Scf, Scs, Cy3G, and LA have shown significant anti-inflammatory and antinociceptive potentials against carrageenan induced-edema and nociceptive-pain, respectively, where Scs (200?mg/kg) has shown the most anti-inflammatory and antinociceptive potentials, and had comparable results to ibuprofen (100?mg/kg). Scf, Scs, Cy3G, and LA have counter-acted carrageenan-induced oxidative-stress markers, with increased serum-catalase and reduced-glutathione levels, and decreased lipid-peroxidation. Histopathological-studies demonstrated gastroprotective potentials, regeneration and improvement of the spleen-structural architecture when treated with highest doses of Scs and Scf. The reduction of the pro-inflammatory TNF-alpha and IL-6, and elevation the anti-inflammatory factor IL-10 levels, spleen regenerative-capacity and oxidative-stress amelioration might be the main-mechanism responsible for P. cerasus anti-inflammatory potentials. P. cerasus appears to aid in ameliorating the inflammatory process, and reducing pain-thresholds while preserving the stomach.

Dataset Information

Niosomes of active Fumaria officinalis phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action.

Publications

Niosomes of active <i>Fumaria officinalis</i> phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action.

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