Sustained drug release behavior of captopril-incorporated chitosan/carboxymethyl cellulose biomaterials for antihypertensive therapy.

Captopril (CTP) is an oral drug widely used to treat high blood pressure and congestive heart failure. In this study, CTP-incorporated biomaterials for antihypertensive therapy were synthesized from chitosan, carboxymethyl cellulose, and plasticizers. The physicochemical properties of the prepared biomaterials were characterized using FE-SEM, FT-IR analysis, and physical properties. CTP release experiments were carried out in buffer solutions at various pH values and temperatures. Results indicated that above 99.0 % of CTP was released within 180 min. Optimization of the experimental conditions for CTP release was analyzed by using response surface methodology (RSM). Results of CTP release through artificial skin indicated that CTP was continuously released above 95.0 % from the prepared biomaterials for 36.0 h. The CTP release mechanisms into a buffer and through artificial skin followed pseudo-Fickian diffusion mechanism and non-Fickian diffusion mechanisms, respectively. Moreover, angiotensin-converting enzyme (ACE) inhibition (related to cardiovascular disease) via the released CTP clearly reveals that the prepared biomaterials have a high potential as a transdermal drug delivery agent in antihypertensive therapy.

Multidirectional insights into the phytochemical, biological, and multivariate analysis of extracts from the aerial part of Swertia perennis Linnaeus.

Swertia perennis Linnaeus (SP) has been utilised to treat gastritis. We report the qualitative and quantitative phytochemical analysis, antioxidant and enzyme inhibitory activities of SP. The correlation between the biological activities and total bioactive contents of the extracts was also studied via multivariate analysis. Methanol extract contained many active compounds and exhibited good antioxidant activity. Therefore, this was selected for further phytochemical profiling and stability studies. Fourteen compounds were identified by ultra-performance liquid chromatography-electrospray ionisation-orbitrap-mass spectrometry for the first time from this plant. Iridoids, xanthones, and flavonoids were the main components. Methanol extract exhibited good stability and antioxidant capacity in stability studies, with low toxicity, and showed a protective effect on the oxidation of olive and sunflower oils. SP has the potential to be developed and used as an antioxidant, or as urease and XO inhibitors, and its methanol extract could be used as a natural oil stabiliser.

Exploring the Pharmacological Potential of Onosma riedliana: Phenolic Compounds and Their Biological Activities.

Onosma riedliana Binzet & Orcan, a traditionally used plant species, has been explored for its therapeutic potential in this study. The work presented here is the first report on the phenolic profile and biological activity of this species. Three extracts of varying polarity were prepared, with the methanolic extract containing the highest phenolic content (97.62 ± 0.20 mgGAE/g). Key phenolic compounds identified included pinoresinol, hesperidin, 4-hydroxybenzoic acid, and p-coumaric acid. The methanolic extract exhibited exceptional antioxidant properties, rivaling Trolox as a positive control, primarily attributed to hesperidin and luteolin. Moreover, the ethyl acetate extract demonstrated remarkable inhibition of cholinesterase and tyrosinase enzymes, while the methanolic extract displayed potent activity against carbohydrate hydrolytic enzymes, α-amylase and α-glucosidase. Again, phenolic compounds were shown to be responsible for the inhibition of cholinesterases and tyrosinase, but not for α-amylase and α-glucosidase. These findings underscore Onosma riedliana's potential for incorporation into diverse pharmaceutical formulations, given its multifaceted bioactivity.

Phenolic compounds, antioxidant capacity, and α-amylase and α-glucosidase inhibitory activity of ethanol extracts of perilla seed meal.

Perilla frutescens is a medicinal herb that is commonly cultivated in Asian countries. Perilla seed is extensively pressed for cooking oil extraction. However, phenolic chemicals are still abundant in pressed perilla seed meal (PSM), which was previously thought to be useless after oil extraction. In our study, PSM was extracted using five solvents (water and 25%, 50%, 75%, and 100% ethanol) based on different ethanol concentrations, and its antioxidant activity, phenolic compounds, and inhibitory effects against key enzymes related to diabetes mellitus were evaluated. The 75% ethanol extract had higher phenolic (105.58 mg GAE/g DW) and flavonoid (66.52 mg QE/g DW) contents and showed better antioxidant and inhibitory effects against α-glucosidase and α-amylase. Analysis of the phenolic compounds of the five extracts by HPLC indicated the presence of apigenin, rosmarinic acid, benzoic acid, caffeic acid, and vanillic acid. Therefore, because of its high antioxidant activity and inhibitory capacity against enzymes relevant to diabetes, the 75% ethanol extract of perilla seed meal has the most potential to be used as a functional or nutraceutical food in the prevention and treatment of oxidation and diabetes.

Angiotensin I-Converting Enzyme-Inhibitory Activity and Phytochemical Profile of Constituents of the Leaves of Rehmannia glutinosa f. hueichingensis.

The root of Rehmannia glutinosa Liboschitz forma hueichingensis HSIAO has been used as a tonic and treatment for urinary and skin disorders in Japanese Kampo medicine. Phytochemical investigation of the root has been well reported, but that of the leaves is limited. To explore the potential value of R. glutinosa leaves, we focused on the angiotensin I-converting enzyme (ACE)-inhibitory activity. The leaf extract exhibited ACE-inhibitory activity, and the inhibitory potency of leaves was stronger than that of roots. Using this activity as an indicator, we isolated linaride (1), 6-O-hydroxybenzoyl ajugol (2), acteoside (3), leucosceptoside A (4), martynoside (5), luteolin (6), apigenin (7), and chrysoeriol (8) by separating and purifying the extract. We then examined the ACE-inhibitory activities of 1-8, catalpol (9), aucubin (10), ajugol (11), and echinacoside (12). Among them, 3, 6, and 12 displayed the most potent inhibitory activity. A simultaneous analytical method was also developed using compounds contained in R. glutinosa leaves and roots, and their contents were compared. The method consisted of extraction with 50% aqueous methanol under sonication for 60 min and LC/MS measurement. R. glutinosa leaves tended to have higher levels of majority of the analytes than the roots, including 3 and 6, which had higher ACE-inhibitory activity. These results suggest that 3 and 6 contribute to the ACE-inhibitory activity of R. glutinosa leaves, which may represent a useful medicinal resource for hypertension.

Production of marine bacterial metalloprotease A69 and evaluation of its potential in preparing soybean peptides with angiotensin-converting enzyme-inhibitory activity.

BACKGROUND: Marine bacteria secrete a variety of proteases, which are a good source to explore proteases with application value. However, only a few marine bacterial proteases with a potential in bioactive peptides preparation have been reported. RESULTS: The metalloprotease A69 from the marine bacterium Anoxybacillus caldiproteolyticus 1A02591 was successfully expressed in the food safe bacterium Bacillus subtilis as a secreted enzyme. A technique to efficiently produce protease A69 in a 15-L bioreactor was established, with a production of 8988 U mL-1 . Based on optimizing the hydrolysis parameters of A69 on soybean protein, a process for soybean protein peptides (SPs) preparation was set up, in which soybean protein was hydrolyzed by A69 at 4000 U g-1 and 60 °C for 3 h. The prepared SPs had a high content (> 90%) of peptides with a molecular mass less than 3000 Da and contained 18 amino acids. The prepared SPs showed high angiotensin-converting enzyme (ACE)-inhibitory activity, with an IC50 value of 0.135 mg mL-1 . Moreover, three ACE-inhibitory peptides, RPSYT, VLIVP and LAIPVNKP, were identified from the SPs using liquid chromatography-mass spectrometry analysis. CONCLUSION: The marine bacterial metalloprotease A69 has a promising potential for preparing SPs with good nutritional and potential antihypertensive effects, laying a good foundation for its industrial production and application. © 2023 Society of Chemical Industry.

Chemical Composition of the Cinnamomum malabatrum Leaf Essential Oil and Analysis of Its Antioxidant, Enzyme Inhibitory and Antibacterial Activities.

Cinnamomum species are a group of plants belonging to the Lauraceae family. These plants are predominantly used as spices in various food preparations and other culinary purposes. Furthermore, these plants are attributed to having cosmetic and pharmacological potential. Cinnamomum malabatrum (Burm. f.) J. Presl is an underexplored plant in the Cinnamomum genus. The present study evaluated the chemical composition by a GC-MS analysis and antioxidant properties of the essential oil from C. malabatrum (CMEO). Further, the pharmacological effects were determined as radical quenching, enzyme inhibition and antibacterial activity. The results of the GC-MS analysis indicated the presence of 38.26 % of linalool and 12.43% of caryophyllene in the essential oil. Furthermore, the benzyl benzoate (9.60%), eugenol (8.75%), cinnamaldehyde (7.01%) and humulene (5.32%) were also present in the essential oil. The antioxidant activity was indicated by radical quenching properties, ferric-reducing potential and lipid peroxidation inhibition ex vivo. Further, the enzyme-inhibitory potential was confirmed against the enzymes involved in diabetes and diabetic complications. The results also indicated the antibacterial activity of these essential oils against different Gram-positive and Gram-negative bacteria. The disc diffusion method and minimum inhibitory concentration analysis revealed a higher antibacterial potential for C. malabatrum essential oil. Overall, the results identified the predominant chemical compounds of C. malabatrum essential oil and its biological and pharmacological effects.

Design, synthesis, and biological evaluation of novel HIV-1 protease inhibitors containing pyrrolidine-derived P2 ligands to combat drug-resistant variant.

The design, synthesis, and biological evaluation of a novel series of HIV-1 protease inhibitors containing pyrrolidines with diverse linkers as the P2 ligands and various aromatic derivatives as the P2' ligands were described. A number of inhibitors demonstrated potent efficacy in both enzyme and cellular assays, as well as relatively low cytotoxicity. In particular, inhibitor 34b with a (R)-pyrrolidine-3-carboxamide P2 ligand and a 4-hydroxyphenyl P2' ligand displayed exceptional enzyme inhibitory activity with an IC50 value of 0.32 nM. Furthermore, 34b also exhibited robust antiviral activity against both wild-type HIV-1 and drug-resistant variant with low micromolar EC50 values. In addition, the molecular modelling studies revealed the extensive interactions between inhibitor 34b and the backbone residues of both wild-type and drug-resistant HIV-1 protease. These results suggested the feasibility of utilizing pyrrolidine derivatives as the P2 ligands and provided valuable information for further design and optimization of highly potent HIV-1 protease inhibitors.

Green synthesis and characterization of silver nanoparticles through the Piper cubeba ethanolic extract and their enzyme inhibitory activities.

Introduction: The area of "Green Synthesis of Nano-medicine," as compared to its synthetic counterparts, is a relatively safer research technology for various biomedical applications, including identification, therapeutic application, and prevention of pathological conditions, pain control, safety, and development of human wellness. The present study explored the synthesis and characterization of AgNPs using the ethanolic extract of Piper cubeba fruit as a reducing and stabilizing agent and its potential as an enzyme inhibitory agent. Urease inhibitors are helpful against many severe diseases, including gastric ulcers induced by Helicobacter pylori. Method: The fruits of the Piper cubeba plant were taken and ground to a fine powder. Plant material was added to 500 ml ethanol, and the mixture was filtered. The solvent of the filtrate was evaporated, and a thick, gummy extract was obtained and stored at 4°C in the refrigerator. AgNPs were green synthesized from solutions of AgNO3 using the P. cubeba extract, which was indicated by a change in the color from light brown to deep brown. The synthesized AgNPs were characterized via Ultraviolet-visible (UV-Vis) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), and scanning electron microscopy (SEM). Results and Discussion: Analysis showed the reduction of Ag+ to Ag0 at room temperature (25°C), and the average particle size of AgNPs was in the range of 40-80 nm. Consequently, the synthesized AgNPs were evaluated for their anti-urease activity. The maximum urease inhibition of the Piper cubeba ethanolic extract was 88.5% at 5 mg conc., and of derived nanoparticles was 78.6% at 0.05 mg conc. The results were nearly similar to the control drug, i.e., thiourea (0.5 and 0.6 mM conc., respectively). Conclusion: The study concluded that the P. cubeba extract, as well as its green-derived AgNPs, might prove to be a better and safer substitute for their enzyme inhibitory potential in emerging medicine and novel drug delivery techniques to improve and maintain human health.

Metabolite profiling and bioactivity of Cicerbita alpina (L.) Wallr. (Asteraceae, Cichorieae).

Cicerbita alpina (L.) Wallr. is a perennial herbaceous plant in the tribe Cichorieae (Lactuceae), Asteraceae family, distributed in the mountainous regions in Europe. In this study, we focused on the metabolite profiling and the bioactivity of C. alpina leaves and flowering heads methanol-aqueous extracts. The antioxidant activity of extracts, as well as inhibitory potential towards selected enzymes, involving in several human diseases, including metabolic syndrome (α-glucosidase, α-amylase, and lipase), Alzheimer's disease, (cholinesterases: AChE, BchE), hyperpigmentation (tyrosinase), and cytotoxicity were assessed. The workflow comprised ultra-high-performance liquid chromatography-high-resolution mass spectrometry (UHPLC-HRMS). UHPLC-HRMS analysis revealed more than 100 secondary metabolites, including acylquinic, acyltartaric acids, flavonoids, bitter sesquiterpene lactones (STLs), such as lactucin, dihydrolactucin, their derivatives, and coumarins. Leaves showed a stronger antioxidant activity compared to flowering heads, as well as lipase (4.75 ± 0.21 mg OE/g), AchE (1.98 ± 0.02 mg GALAE/g), BchE (0.74 ± 0.06 mg GALAE/g), and tyrosinase (49.87 ± 3.19 mg KAE/g) inhibitory potential. Flowering heads showed the highest activity against α-glucosidase (1.05 ± 0.17 mmol ACAE/g) and α-amylase (0.47 ± 0.03). The obtained results highlighted C. alpina as a rich source of acylquinic, acyltartaric acids, flavonoids, and STLs with significant bioactivity, and therefore the taxon could be considered as a potential candidate for the development of health-promoting applications.

Peptidomic analysis of the angiotensin-converting-enzyme inhibitory peptides in milk fermented with Lactobacillus delbrueckii QS306 after ultrahigh pressure treatment.

In this study, we assessed the effect of ultrahigh pressure (UHP) treatment on the concentration of peptides and angiotensin-converting enzyme (ACE) inhibitory activity in milk fermented with Lactobacillus delbrueckii QS306. The peptides were identified using peptidomic analysis, and 313 unique peptides were identified. These peptides were derived from 53 precursor proteins. Before and after UHP treatment, 361 (22.2%) peptide sequences exhibited difference, and 53 peptide segments were significantly different. Among them, small peptides (amino acid residues ≤6) isoelectric were point at pH 5-6, and the net charge was mainly positive or neutral. With hydrophobicity and ACE inhibitory activity as screening indicators, 214 small peptides with potential ACE inhibitory activity were identified, and 130 new peptides had potential ACE inhibitory activity. A novel ACE inhibitory peptide VAPFP was synthesized, whose in vitro inhibition rate was 10.56 µmol\/L. Therefore, using peptidomics, the changes in peptide sequences and enhancement in ACE inhibitory activity before and after UHP treatment could be effectively identified in milk fermented with Lactobacillus delbrueckii QS306. This study provided a convenient method for the discovery and identification of new ACE inhibitory peptides.

Heliotropium procubens Mill: Taxonomic Significance and Characterization of Phenolic Compounds via UHPLC-HRMS- In Vitro Antioxidant and Enzyme Inhibitory Activities.

The aim of the present study was the phytochemical analysis of the aerial parts of Heliotropium procumbens Mill., a herb from Boraginaceae plant family not previously studied. The methanol (ME) and aqueous extracts (WE) of the aerial parts were assayed for their total phenolic and flavonoid content and antioxidant properties, using free radical scavenging (DPPH, ABTS), reducing power (FRAP, CUPRAC), phosphomolybdenum and metal chelating assays. The extracts displayed considerable free radical scavenging activity against DPPH and ABTS radicals, with potential values of 46.88 and 68.31 mg TE/g extract for ME, and 93.43 and 131.48 mg TE/g extract for WE, respectively. Key clinical enzymes involved in neurodegenerative diseases AChE and BChE, diabetes (α-amylase and α-glucosidase) and skin whitening (tyrosinase) were also assayed. The phytochemical profile of the studied species was determined through UHPLC-HRMS, whereby 26 secondary metabolites were identified, three of which (luteolin-7-glucoside, lithospermic and rosmarinic acids) were isolated and structurally determined by NMR spectral means. H. procubens was found to harbor bioactive metabolites and could, hence, serve as a source of biological activities which could be further explored and exploited for potential applications.

Valorization of Chicken Slaughterhouse Byproducts to Obtain Antihypertensive Peptides.

Hypertension (HTN) is the leading cause of premature deaths worldwide and the main preventable risk factor for cardiovascular diseases. Therefore, there is a current need for new therapeutics to manage this condition. In this regard, protein hydrolysates containing antihypertensive bioactive peptides are of increasing interest. Thus, agri-food industry byproducts have emerged as a valuable source to obtain these hydrolysates as they are rich in proteins and inexpensive. Among these, byproducts from animal origin stand out as they are abundantly generated worldwide. Hence, this review is focused on evaluating the potential role of chicken slaughterhouse byproducts as a source of peptides for managing HTN. Several of these byproducts such as blood, bones, skins, and especially, chicken feet have been used to obtain protein hydrolysates with angiotensin-converting enzyme (ACE)-inhibitory activity and blood pressure-lowering effects. An increase in levels of endogenous antioxidant compounds, a reduction in ACE activity, and an improvement of HTN-associated endothelial dysfunction were the mechanisms underlying their effects. However, most of these studies were carried out in animal models, and further clinical studies are needed in order to confirm these antihypertensive properties. This would increase the value of these byproducts, contributing to the circular economy model of slaughterhouses.

Biochemical and Genomic Characterization of Two New Strains of Lacticaseibacillus paracasei Isolated from the Traditional Corn-Based Beverage of South Africa, Mahewu, and Their Comparison with Strains Isolated from Kefir Grains.

Lacticaseibacillus paracasei (formerly Lactobacillus paracasei) is a nomadic lactic acid bacterium (LAB) that inhabits a wide variety of ecological niches, from fermented foodstuffs to host-associated microenvironments. Many of the isolated L. paracasei strains have been used as single-strain probiotics or as part of a symbiotic consortium within formulations. The present study contributes to the exploration of different strains of L. paracasei derived from non-conventional isolation sources-the South African traditional fermented drink mahewu (strains MA2 and MA3) and kefir grains (strains KF1 and ABK). The performed microbiological, biochemical and genomic comparative analyses of the studied strains demonstrated correlation between properties of the strains and their isolation source, which suggests the presence of at least partial strain adaptation to the isolation environments. Additionally, for the studied strains, antagonistic activities against common pathogens and against each other were observed, and the ability to release bioactive peptides with antioxidant and angiotensin I-converting enzyme inhibitory (ACE-I) properties during milk fermentation was investigated. The obtained results may be useful for a deeper understanding of the nomadic lifestyle of L. paracasei and for the development of new starter cultures and probiotic preparations based on this LAB in the future.

Physicochemical properties and in vitro hypoglycemic activities of hsian-tsao polysaccharide fractions by gradient ethanol precipitation method.

Hsian-tsao polysaccharides fractions (HPs), including HP20, HP40, HP60, and HP80, were fractioned by gradient precipitation of 20 %, 40 %, 60 %, and 80 % (v/v) ethanol, respectively. Their physicochemical properties and in vitro hypoglycemic activities (inhibitory activities on α-amylase and α-glucosidase, glucose adsorption capacity, and glucose diffusion retardation) were determined. The results showed that, with ethanol upward, the average particle size, molecular weight, and apparent viscosity of HPs were decreased while carbohydrate and uronic acid contents, absolute zeta potential, and thermal stability were increased. Each of the HPs contained Rha, Ara, Gal, Xyl, Man, and GalA with different molar ratios, indicative of anionic heteropolysaccharides with uronic acid. HPs, with diverse structures and surface morphologies as proved by FTIR and SEM, whose solutions were pseudoplastic fluids, exhibited elastic behavior of weak gel networks at concentrations of >1 %. Moreover, HPs showed inhibitory activities on α-amylase and α-glucosidase, of which HP80 was the strongest. For α-amylase, HP20 and HP60 behaved as mixed inhibitors, while HP40 and HP80 were non-competitive. For α-glucosidase, HPs acted as mixed inhibitors. Additionally, HPs possessed glucose adsorption capacity and glucose diffusion retardation, with the best for HP20. These results suggested that HPs possessed hypoglycemic activities, which could be developed as functional food or hypoglycemic drugs.

Phytochemical profiling and antioxidant, enzyme-inhibitory, and toxic activities of extracts from Adonis ramosa Franch.

This study investigated the content and biological activity of three solvent extracts of Adonis ramosa Franch (AR), which contains 12 types of phytochemicals. The overall yield and total protein content of the aqueous extract were the highest, and it exhibited the highest hydroxyl and superoxide radical-scavenging abilities, copper chelating abilities, and cupric reducing antioxidant capacity. Ethanol extract had the highest total phenolic, flavonoid, and carbohydrate contents, and it showed the highest iron chelating activity, and HClO- and nitrite-scavenging abilities. Methanol AR extract contained the highest total steroid and tannin contents; it also demonstrated high radical- and reactive oxygen species-scavenging abilities and had the best ferric reducing antioxidant power, which allowed it to effectively prevent ß-carotene bleaching. Methanol extract also showed good stability and low toxicity. All tested solvent extracts of AR exhibited weak enzyme-inhibitory activities for four enzymes (α-glucosidase, α-amylase, acetylcholinesterase and butyrylcholinesterase). Overall, AR can serve as a natural antioxidant.

Ultrasound-alkaline combined extraction improves the release of bound polyphenols from pitahaya (Hylocereus undatus 'Foo-Lon') peel: Composition, antioxidant activities and enzyme inhibitory activity.

In this study, ultrasound-assisted alkaline hydrolysis was used to extract polyphenols from pitahaya peel. The effects of sonication time, ultrasonic density, NaOH concentration and the liquid-material ratio on the total phenolic content (TPC), total flavonoid content (TFC) and antioxidant activity of the extracts were studied. The composition and content difference of the extracts were analyzed and the inhibitory effect of α-amylase and α-glucosidase was measured. The results of single-factor analysis showed that when the sonication time was 45 min, the ultrasonic density was 32 W/L, the NaOH solution concentration was 6 M and the liquid-material ratio was 30 mL/g, the release of phenolic compounds was the largest and the antioxidant activity was the strongest. An UPLC-QTOF-MS/MS method was used to analyze the components and contents of the extracts. We found that there was a great difference in the component content of the free polyphenol extract and the bound polyphenol extract. From the results, we concluded that there was a strong correlation between the type and content of phenolic compounds and antioxidant activities, indicating that phenolic compounds were the main compounds of these biological activities. Moreover, the bound polyphenol extracts showed a significant inhibitory effect on α-amylase and α-glucosidase was stronger than that of the free polyphenol extracts. In addition, scanning electron microscopy showed that ultrasound-assisted extraction is crucial to the destruction of the cell wall and the release of bound polyphenols. Therefore, the pitahaya peel has the potential for therapeutic, nutritional, and functional food applications, and ultrasound-assisted alkaline hydrolysis is an effective means to release phenolic compounds.

Bioactive Saponins of Primula vulgaris Huds. Promote Wound Healing through Inhibition of Collagenase and Elastase Enzymes: in Vivo, in Vitro and in Silico Evaluations.

Primula vulgaris Huds. leaves and roots were used to treat skin damage and inflammation in Anatolian Folk Medicine. This study aimed to assess the ethnopharmacological use of the plant using in vivo, in vitro, and in silico test models. Linear incision and circular excision wound models were used to determine the in vivo wound-healing potential of the plant extracts and fractions. In vitro assays including hyaluronidase, collagenase, and elastase inhibitory activities were carried out for the active compounds to discover their activity pathways. Structure-based molecular modeling was performed to understand inhibitory mechanisms regarding collagenase and elastase at the molecular level. The butanol fraction of the roots of P. vulgaris showed the highest wound-healing activity. Through activity-guided fractionation and isolation techniques, primulasaponin I (1) and primulasaponin I methyl ester (2) were stated as the major active compounds. These compounds exerted their activities through the inhibition of collagenase and elastase enzymes. Primulasaponin I methyl ester isolated from butanol fraction was found to be the strongest agent, especially with the values of 29.65 % on collagenase and 38.92 % on elastase inhibitory activity assays, as well as molecular docking studies. The present study supports scientific data for the traditional use of P. vulgaris and the wound healing properties of the plant can be referred to secondary metabolites as especially saponins found in the roots.

Phytochemical Profiling and Bio-Potentiality of Genus Scutellaria: Biomedical Approach.

Scutellaria (Lamiaceae) comprises over 360 species. Based on its morphological structure of calyx, also known as Skullcap, it is herbaceous by habit and cosmopolitan by habitat. The species of Scutellaria are widely used in local communities as a natural remedy. The genus contributed over three hundred bioactive compounds mainly represented by flavonoids and phenols, chemical ingredients which serve as potential candidates for the therapy of various biological activities. Thus, the current review is an attempt to highlight the biological significance and its correlation to various isolated bioactive ingredients including flavonoids, terpenoids, phenols, alkaloids, and steroids. However, flavonoids were the dominant group observed. The findings of the Scutellaria reveal that due to its affluent basis of numerous chemical ingredients it has a diverse range of pharmacological potentials, such as antimicrobial, antioxidant, antifeedant, enzyme inhibition, anti-inflammatory, and analgesic significance. Currently, various bioactive ingredients have been investigated for various biological activities from the genus Scutellaria in vitro and in vivo. Furthermore, these data help us to highlight its biomedical application and to isolate the responsible compounds to produce innovative medications as an alternative to synthetic drugs.

Evaluation of antioxidant, enzyme inhibition, nitric oxide production inhibitory activities and chemical profiles of the active extracts from the medicinal and edible plant: Althaea officinalis.

To develop the medicinal and edible plant resources of Althaea officinalis Linn in Europe and other places, this study concentrated on the bioactive ingredients of its different extracts. The phytochemical compositions of MeOH extracts were evaluated by UPLC-DAD-ESI-Q-TOF-MSn analysis. The in vitro antioxidant properties, enzymes inhibitory effects and nitric oxide (NO) production inhibitory activities of fractions obtained from the aerial parts of Althaea officinalis (APAO) were evaluated. The results identified 76 compounds, including 8 phenolic acids, 17 flavonoids, 6 coumarins, 9 triterpenes and 11 alkaloids. Fr. C-2 of APAO was found to have the highest TPC (175.8 ± 1.5 mg GAE/g) and TFC (466.9 ± 5.0 mg RE/g) with the highest antioxidant capacity in DPPH, ABTS, CUPRAC, FRAP and ß-carotene bleaching assays. Fr. A showed noticeable inhibition of α-glucosidase with an IC50 value of 3.8 ± 0.1 µg/mL. However, Fr. B displayed stronger inhibitory activity on 5-lipoxygenase than quercetin, with the IC50 value of 8.4 ± 1.6 µg/mL. In addition, Fr. B also possessed potent inhibitory activities on NO production toward LPS-activated RAW 264.7 Cells with an IC50 value of 15.7 ± 1.6 µg/mL. Our findings suggest that different Althaea officinalis extracts may be considered sources of phenolic and flavonoid compounds with high potential as natural antioxidants, anti-inflammatory agents and blood sugar regulators. In addition, they can also be used in food and nutraceutical products with enhanced bioactivities.