Antiarthritic activity of Physalis peruviana fruit extract via inhibition of inflammatory mediators: Integrated in vitro, in vivo and in silico study.

ETHNOPHARMACOLOGICAL RELEVANCE: P. peruviana fruit, native to Andean region, is cultivated worldwide for its adaptability to various soil natures and climatic conditions. It is increasingly consumed for its high nutritional profile and history of ethnomedical uses including treatment of arthritis. Little pharmacological evidences support this folk use except for previous in vitro study that reported significant inhibition of protein denaturation. AIM OF THE STUDY: The study aims at providing new in vivo evidence on antiarthritic activity of P. peruviana fruits in vivo that justifies its traditional use through mechanism-based experiment. MATERIAL AND METHODS: Inhibition of inflammatory mediators is considered one of the key treatments to alleviate painful symptoms of rheumatoid arthritis (RA). Anti-inflammatory activity was assessed against COX-1 and COX-2 activity in vitro. Serum TNFα, IL-1ß and IL-6 were traced using in vivo model of adjuvant-induced arthritis. Gross/inflammatory changes in rat paw, relative mass indices of spleen and liver were further investigated together with joint tissue histoarchitecture. Seven metabolites from different phytochemical classes, that were previously reported in P. peruviana fruit, were evaluated in silico against TNF-α target protein (PDB ID: 2AZ5) to assess their inhibitory effect. This was followed by assessment of their drug-likeness based on Lipinski's rule according to their physicochemical and pharmacokinetic properties. RESULTS: High dose of extract (E-1000 mg) improved adjuvant-induced cachexia and attenuated immune-inflammatory responses in paw and serum parameters, with equipotent effect to MTX, in addition to minimal side effect profile on spleen and liver. Histopathological study of knee joint tissues confirmed dose-dependent improvement in arthritic groups treated with P. peruviana fruit extracts. The insilico study recommended steroidal lactones withaperuvin E/C and hydroxywithanolide E as promising lead compounds for inhibiting TNF enzyme as evidenced by docking scores of 6.301, 5.488 and 5.763 kcal/mol, respectively, fitting as well the Lipinski's rule of drug likeness. CONCLUSION: The study provided novel approach that rationalize folk use of P. peruviana fruit in treatment of arthritis.

Innovative Processing Technologies to Develop a New Segment of Functional Citrus-Based Beverages: Current and Future Trends.

The food industries are interested in developing functional products due to their popularity within nutritional and healthy circles. Functional fruit-based beverages represent one of the fast-growing markets due to the high concentrations of bioactive compounds (BCs), which can be health promoters. Hence, functional beverages based on citrus fruits are a potential way to take advantage of their nutritional and bioactive properties that could attract the interest of consumers. In order to ensure microbial and quality stability, the beverages are subjected to preservation treatment; however, the application of high temperatures leads to the loss of thermolabile BCs. Nowadays, innovative processing technologies (IPT) such as pulsed electric field (PEF), high-pressure processing (HPP), ultrasound processing (US), ohmic heating (OH), and microwave (MW) are a promising alternative due to their efficiency and low impact on juice BCs. The available literature concerning the effects of these technologies in functional fruit-based beverages is scarce; thus, this review gathers the most relevant information about the main positive and negative aspects of the IPT in functional properties, safety, and consumer acceptance of functional citrus-based beverages, as well as the use of citrus by-products to promote the circular economy in citrus processing.

Development of Lepidium sativum Extracts/PVA Electrospun Nanofibers as Wound Healing Dressing.

Lepidium sativum L. (Garden cress/Hab El Rashad) (Ls), family Brassicaceae, has considerable importance in traditional medicine worldwide because of its antioxidant and anti-inflammatory activities. Ls fruits were used in Ayurvedic medicines as a useful drug for injuries, skin, and eye diseases. The aim of this study was to examine the effectiveness of the total ethanol extract (TEE) and polysaccharide (Poly) of Ls seeds loaded on poly(vinyl alcohol) (PVA) nanofibers (NFs) as a wound healing dressing and to correlate the activity with the constituents of each. TEE and Poly were phytochemically analyzed qualitatively and quantitatively. Qualitative analysis proved the presence of phenolic acids, flavonoids, tannins, sterols, triterpenes, and mucilage. Meanwhile, quantitative determinations were carried out spectrophotometrically for total phenolic and total flavonoid contents. High-performance liquid chromatography (HPLC) for TEE identified 15 phenolic acids and flavonoid compounds, with gallic acid and catechin as the majors. Separation, purification, and identification of the major compounds were achieved through a Puriflash system, column Sephadex LH20, and spectroscopic data (1H, 13C NMR, and UV). Eight compounds (gallic acid, catechin, rutin, kaempferol-3-O-rutinoside, quercetin-3-O-rhamnoside, kaempferol-3-O-rhamnoside, quercetin, and kaempferol) were obtained. Gas-liquid chromatography (GLC) analysis for Poly identified 11 compounds, with galactose being the main. The antioxidant activity for both extracts was measured by three different methods based on different mechanisms: 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing ability of plasma (FRAP), and 3-ethylbenzothiazoline-6-sulfonic acid (ABTS). TEE has the highest effectiveness as an antioxidant agent with IC50 82.6 ± 8.35 µg/mL for DPPH and 772.47 and 758.92 µM Trolox equivalent/mg extract for FRAP and ABTS, respectively. The PVA nanofibers (NFs) for each sample were fabricated by electrospinning. The fabricated NFs were characterized by SEM and Fourier transform infrared spectroscopy (FTIR); the results revealed successful encapsulation of TEE and Poly in the prepared NFs. Moreover, the swelling index of TEE in the prepared NFs shows that it is the most appropriate for use as a wound dressing. Cytotoxicity studies indicated a high cell viability with IC50 216 µg/mL and 1750 µg/mL for TEE and Poly, respectively. Moreover, the results revealed that nanofibers possess higher cell viability compared to solutions with the same sample quantities: 9-folds for TEE and 4-folds for Poly of amount 400 µg. The in vitro wound healing test showed that the TEE nanofibers performed better than Poly nanofibers in accelerating wound healing, with 90% for TEE, more than that for the Poly extract (82%), after 48 h. These findings implied that the incorporation of TEE in PVA nanofibers was more efficient than incorporation of Poly in improving the biological activity in wound healing. In conclusion, the TEE and polysaccharides of L. sativum L seed are ideal candidates for nanofibrous wound dressings. Furthermore, the contents of phenolic acids and flavonoids in TEE, which have potential antioxidant activity, make the TEE of L. sativum more favorable for wound healing dressing.

Chemosystematic significance of flavonoids isolated from Diplotaxis acris (Brassicaceae) and related taxa.

The chemosystematic relationship of four Diplotaxis species; Diplotaxis acris, Diplotaxis erucoides, Diplotaxis harra and Diplotaxis muralis were surveyed from the flavonoids point of view. These species were found to produce 33 flavonoids (7 flavones and 26 flavonols), including 11 compounds were isolated in the present study from D. acris. Among them, seven flavonoids were identified for the first time; luteolin (4), kaempferol (8), kaempferol 3-O-ß-glucopyranoside-7-O-α-rhamnopyranoside (13), quercetin 3-O-ß-glucopyranoside (16), quercetin 7-O-ß-glucopyranoside (20), isorhamnetin (22) and isorhamnetin 3-O-ß-glucopyranoside-7-O-α-rhamnopyranoside (32). Their structures were recognized on the basis of chemical and spectroscopic techniques (1D & 2D NMR, UV, EI & ESI/MS). The isolated flavonoids may provide useful taxonomic characters at the infraspecific levels of classification where the flavonoid profile of D. acris and D. harra is similar and different from the other species.

Digalacturonide flavones from Egyptian Lantana camara flowers with in vitro antioxidant and in vivo hepatoprotective activities.

A new digalacturonide flavone, luteolin 7-O-beta-galacturonyl-(2 --> 1)-O-beta-galacturonide (1), was isolated along with nine known flavone glycosides from the aqueous methanolic extract of Lantana camara (L.) flowers. Their structures were determined on the basis of the spectral data. The extract of L. camara was evaluated for antioxidant and hepatoprotective properties in the acetaminophen-induced mouse liver damage model. 1 exhibited significant antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay with an IC50 value of 27.2 microM. Pre-treatment with L. camara extract (25 and 75 mg/ kg body weight) decreased the activities of alkaline phosphatase (ALP), serum glutamate oxaloacetate transaminase (SGOT), and serum glutamate pyruvate transaminase (SGPT) enzyme levels that were elevated by acetaminophen. Both doses of the L. camara extract ameliorated the histopathological and histochemical alterations induced by acetaminophen. The results indicate that the L. camara extract possesses hepatoprotective activity against acetaminophen-induced liver damage.