The study of wound healing activity of Thespesia populnea L. bark, an approach for accelerating healing through nanoparticles and isolation of main active constituents.

The present study provides an evaluation for the wound healing activity of the ethanolic extract of Thespesia populnea L. bark (EBE) and its successive fractions in two doses level (1&2%), designed for determining the most bioactive fraction and the suitable dose. Furthermore, development of the most convenient formulation for these bioactive fractions through either their direct incorporation into hydrogel formulations or incorporation of chitosan-loaded nanoparticles with these bioactive fractions into hydrogel formulations. The highest excision wound healing activity was observed in petroleum ether (Pet-B) followed by ethyl acetate (Etac-B) fractions at the high dose (2%). The most suitable formulation designed for the Etac-B fraction was found to be the chitosan-loaded nanoparticles incorporated in the hydrogel formulation, while the conventional hydrogel formulation was observed to be the highly acceptable formulation for Pet-B fraction. Further phytochemical studies of the bioactive fractions led to the isolation of many compounds of different chemical classes viz; beta-sitosterol and lupeol acetate isolated from the Pet-B, in addition to cyanidin and delphinidin from the Etac-B. Our results revealed that EBE and its bioactive fractions (Pet-B & Etac-B) could be considered as strong wound healers through their anti-oxidant and anti-inflammatory activities, in addition to stimulating collagen synthesis.

In Vivo Antihypertensive Activity and UHPLC-Orbitrap-HRMS Profiling of Cuphea ignea A. DC.

Cuphea ignea A. DC. is an ornamental tropical plant belonging to the family Lythraceae. The aim of this study is to verify the in vivo antihypertensive potential of C. ignea A. DC. and to explore its metabolic profile using a UHPLC-Orbitrap-HRMS technique. The results revealed that the ethanolic extract of the leaves in two doses (250 and 500 mg/kg b.wt.) significantly normalized the elevated systolic blood pressure in N(G)-nitro-l-arginine-methyl ester-induced hypertension in rats. An angiotensin-converting enzyme (ACE) concentration was significantly decreased by the high dose extract compared to lisinopril. Nitric oxide (NO) level was significantly restored by both doses. Concerning the oxidative stress parameters, both doses displayed significant reduction in malondialdehyde (MDA) level while the high dose restored elevated glutathione level. These biochemical results were clearly supported by the histopathological examination of the isolated heart and aorta. A UHPLC-Orbitrap-HRMS study was represented by a detailed metabolic profile of leaves and flowers of C. ignea A. DC., where 53 compounds were identified among which flavonoids, fatty acids, and hydrolysable tannins were the major identified classes. This study established scientific evidence for the use of C. ignea A. DC., a member of genus Cuphea as a complementary treatment in the management of hypertension.

Delineating a potent antiviral activity of Cuphea ignea extract loaded nano-formulation against SARS-CoV-2: In silico and in vitro studies.

The outbreak of coronavirus disease-2019, caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is a worldwide emerging crisis. Polyphenols are a class of herbal metabolites with a broad-spectrum antiviral activity. However, most polyphenols encounter limited efficacy due to their poor solubility and degradation in neutral and basic environments. Thus, the effectiveness of their pharmaceutical application is critically dependent on the delivery systems to overcome the aforementioned drawbacks. Herein, Polyphenols-rich Cuphea ignea extract was prepared and its constituents were identified and quantified. Molecular docking was conducted for 15 compounds in the extract against SARS-CoV-2 main protease, among which rutin, myricetin-3-O-rhamnoside and rosmarinic acid depicted the most promising antiviral activity. Further, a self-nanoemulsifying formulation, composed of 10% oleic acid, 40% tween 20 and propylene glycol 50%, was prepared to improve the solubility of the extract components and enable its concurrent delivery permitting combined potency. Upon dilution with aqueous phases, the formulation rapidly Formsnanoemulsion of good stability and excellent dissolution profile in acidic pH when compared to the crude extract. It inhibited SARS-CoV-2 completely in vitro at a concentration as low as 5.87 µg/mL presenting a promising antiviral remedy for SARS-CoV-2, which may be attributed to the possible synergism between the extract components.

Bioassay-guided fractionation and identification of antidiabetic compounds from the rind of Punica Granatum Var. nana.

This study aimed to evaluate the antidiabetic potential of the rind of Punica granatum var. nana. Acute oral toxicity test revealed the safety profile of its ethanolic extract. The extract was administered at 200 mg/kg b.wt to streptozotocin-induced diabetic rats. Serum diagnostic markers of diabetes (insulin, glucose and glycated hemoglobin), inflammatory mediators (tumor necrosis factor-α, interleukin-6, and nitric oxide), and oxidative stress (total antioxidant capacity and reduced glutathione and malondialdehyde) were assayed. The ethanolic extract was further fractionated and assessed for the aforementioned bioactivities at two different doses (100 and 200 mg/kg b.wt). The results revealed that the ethyl acetate fraction of rind exhibited the highest activities. Using different chromatographic techniques, four compounds were isolated and identified as rutin, gallic acid, nictoflorin, and tulipanin. In conclusion: The ethyl acetate fraction of the rind of Punica granatum var. nana may provide a potential therapeutic approach for hyperglycemia.

Efficient wound healing composite hydrogel using Egyptian Avena sativa L. polysaccharide containing ß-glucan.

The purpose of this study was to develop an efficient wound healing PVA-biopolymer composite hydrogel using the polysaccharide derived from Egyptian Avena sativa L. The prepared polysaccharide showed high ß-glucan content which accelerates wound healing. The ß-glucan content was 13.28% and GC analysis revealed that glucose was the major sugar component (71.19%). Different PVA-polysaccharide hydrogels combined with different polymers and loaded with 0.3% bacitracin zinc were developed using the freezing-thawing method. The used polymers were; polyvinylpyrrolidone (PVP), Carbopol 940 (CP), hydroxyethylcellulose (HEC), hydroxypropyl methylcellulose (HPMC), and sodium carboxymethylcellulose (Na CMC). The prepared hydrogels were characterized by determination of gel fraction, swelling ratio, mechanical and bioadhesive properties. The results revealed that hydrogels prepared using anionic (NaCMC and CP) and more hydrophilic (HEC) polymers showed better swelling ratio, bioadhesive and mechanical characters compared with hydrogels prepared using cationic (PVP) or less hydrophilic (HPMC) polymers. For two selected formulations containing HEC (F7) and NaCMC (F9), disk diffusion method and In vitro microbial penetration were performed for microbiological assessment. In addition, In vivo evaluation of the anti-inflammatory and wound healing activity compared with conventional products were performed on rats. The results showed higher anti-inflammatory activity of F7 (21.4% edema reduction) compared with F9 (19.8% edema reduction). Similarly, F7 showed better healing (99% relative wound size reduction) than F9 (75%). The current study revealed the potential of using the prepared Egyptian Avena sativa L. polysaccharide and HEC for development of an efficient wound healing dressing with antimicrobial and anti-inflammatory activities.

Metabolic profile and hepatoprotective effect of Aeschynomene elaphroxylon (Guill. & Perr.).

Liver diseases are life-threatening and need urgent medical treatments. Conventional treatment is expensive and toxic, so the urge for nutraceutical hepatoprotective agents is crucial. This study is considered the first metabolic profile of Aeschynomene elaphroxylon (Guill. & Perr.) extracts of; flowers, leaves & bark adopting UPLC-Orbitrap HRMS analysis to determine their bioactive metabolites, and it was designed to investigate the potential hepatoprotective activity of A. elaphroxylon flowers and bark extracts against CCl4-induced hepatic fibrosis in rats. Forty-nine compounds of various classes were detected in the three extracts, with triterpenoid saponins as the major detected metabolite. Flowers and bark extracts presented similar chemical profile while leaves extract was quite different. The antioxidant activities of the flowers, leaves & bark extracts were measured by in vitro assays as Fe+3 reducing antioxidant power and Oxygen radical absorbance capacity. It revealed that flowers and bark extracts had relatively high antioxidant activity as compared to leaves extract. Based on the metabolic profile and in vitro antioxidant activity, flowers and bark ethanolic extracts were chosen for alleviation of hepatotoxicity induced by CCl4 in rats. The hepatoprotective activity was studied through measuring hepatotoxicity biomarkers in serum (ALT, AST, and Albumin). Liver tissues were examined histopathologically and their homogenates were used in determining the intracellular levels of oxidative stress biomarkers (MDA, GSH), inflammatory markers (TNF-α). Flowers and bark ethanolic extracts exerted a significant hepatoprotective effect through reduction in the activities of ALT, AST and Albumin, the tested extracts reduced oxidative stress by increasing GSH content and reducing the MDA level. Furthermore, the extracts decreased levels of pro-inflammatory TNF-α. Moreover, the present study revealed the potentiality of A. elaphroxylon in ameliorating the CCl4-induced hepatic fibrosis in rats. In this aspect, A. elaphroxylon can be used with other agents as a complementary drug.

Chemical Composition, Antimicrobial and Antitumor Potentiality of Essential Oil of Ferula tingitana L. Apiaceae Grow in Libya.

BACKGROUND: Ferula tingitana L. (Apiaceae) has been considered to have abortive and menstruation-inducing properties. It used to treat sore throat, fever, indigestion, and pains. OBJECTIVES: The objective of this study is to establish the chemical composition of the essential oil of flower, leaves of F. tingitana, and to throw light on antimicrobial, cytotoxic activities of Libyan plant. MATERIALS AND METHODS: The chemical composition of the essential oil of flower (0.06% w/v) and leaves (0.1% w/v) of F. tingitana was comparatively analyzed by gas chromatography/mass spectrometry using nonpolar column DB-5. RESULTS: A total of 28-32 components were identified, 15 being common in both samples. The main constituents of both flower- and leave-derived oil samples were α-thujene (13.5%-2.3%), elemol (8.9%-8.3%), eudesmol (0.6%-9.7%) and cadinol (2.2%-13.8%), respectively. The principle difference was a considerably more pronounced sesquiterpenes presence in the leaves-oil, amounting to 74.0%, than in the flower counterpart (39.9%). Caryophyllene (5.6%) and elemol (8.9%) were the major sesquiterpenes detected in flower-oil while leaves-oil showed less amounts of sesquiterpenoid hydrocarbons (27.7%) and represented by eudesmadiene (9.0%). On the contrary, while remaining the dominant group in both oil samples, monoterpenoids are relatively more abundant in flower-derived oil constituting 57.7% versus 24.5% detected in leaves. CONCLUSION: Leaves-oil sample being mostly efficient as antibacterial against Bacillus subtilis and Neisseria gonorrhoeae with potency 48.3, 41.9% compared to tetracycline standard antibacterial drug. The essential oil samples revealed marked in vitro cytotoxicity against breast (MCF7), cervical (HELA) and liver(HEPG2) carcinoma cell lines with IC50% (6.9, 4.8), (8.6, 10.9), and (4.4, 4.2) for the flower-, leaves-derived oil sample, respectively. SUMMARY: Comparative analysis of the investigated oil samples indicates more pronounced monoterpene contents in Ferula tingitana flower. The principle monoterpenoid constituents of both oils are α-thujene. Sesquiterpenes presence is considerably more pronounced in the leaves-derived oil sampleElemol, cadinol, α-thujene and a-terpinoline, the major components of the flower- and leaves-derived oil in the present work and were not detected in the Turkish sample. The differences may be due to climatic and other extrinsic conditions such as where and when the samples were collectedWhen screened for antimicrobial activity, the flower- and leaves-derived oil of F. tingitana exhibited a mild effect against all tested Gram-negative and Gram-positive microorganisms. However, not displayed growth inhibitory effect against the fungus Aspergillus flavus and Candida albicansOn assessing the cytotoxic activity, the flower- and leaves-derived oil exhibited specific and significant effects on the viability of the selected human cell lines, viz., hormone-responsive breast carcinoma cell line (MCF7), cervical carcinoma cell line (HELA), and liver carcinoma cell line (HEPG2). Abbreviations used: F: Flower-derived oil of F. tingitana; L: Leaves-derived oil of F. tingitana; IPP: Isopentenyl pyrophosphate or also isopentenyl diphosphate; DMAPP: Dimethylally pyrophosphate or also dimethylallyl diphosphate; GPP: Geranyl pyrophosphate; GGPP: Geranylgeranyl pyrophosphate; MEP: Methylerythritol phosphate pathway; FPP: Farnesyl pyrophosphate; GC/MS: Analysis gas chromatography/mass spectroscopy; SRB: Sulforhodamine B.

In vitro evaluation of cytotoxic activity of the ethanol extract and isolated compounds from the corms of Liatris spicata (L.) willd on HepG2.

Investigation of the ethanol extract of the corms of Liatris spicata (L.) willd led to the isolation of two sterols: stigmasterol and its 3-O-glucoside, a triterpene: obtusifoliyl acetate, two benzofurans: euparin and 6-hydroxy-3-methoxytremetone, three phenolic acids: protocatechuic, vanillic and ferulic acid and a sesquiterpene lactone igalan. The structures of the isolated compounds were established on the basis of physicochemical properties and spectral analysis (IR, EI/MS, 1H NMR and 13C NMR). The ethanol extract and its isolated compounds evidenced cytotoxic activities against human liver cancer cell line (HepG2), where igalan showed the highest potency (3.83 ± 0.043) µg/mL, its effect was comparable to that of the standard drug doxorubicin® (3.73 ± 0.036) µg/mL.

A new acylated flavonol from the aerial parts of Asteriscus maritimus (L.) Less (Asteraceae).

Phytochemical investigation of the flowering aerial parts of Asteriscus maritimus (L.) Less (Asteraceae) led to the isolation of a new compound: patuletin 7-O-ß-D-[(2″'S) 6″(3″'-hydroxy-2″'-methyl-propanoyl)] glucopyranoside, together with five known metabolites; ß-sitosterol 2, chlorogenic acid 3, P-hydroxy -methylbenzoate 4, luteolin 5 and protocatechuic acid 6. The structures of the isolated compounds were determined by comprehensive analyses of its 1D and 2D NMR, HRMS and compared with previously known analogues. The ethanolic extract of the flowering aerial parts of A. maritimus was found to be safe (LD50 = 4.6 mg/kg) and possess significant antioxidant and anti-inflammatory activities and this was in accordance with its high phenolic content (107.36 ± 0.051 mg GAE/g extract).