Pharmacological effects of bioactive agents in earthworm extract:A comprehensive review

This review compiles information from the literature on the chemical composition,pharmacological effects,and molecular mechanisms of earthworm extract(EE)and suggests possibilities for clinical translation of EE.We also consider future trends and concerns in this domain.We summarize the bioactive components of EE,including G-90,lysenin,lumbrokinase,antimicrobial peptides,earthworm serine protease(ESP),and polyphenols,and detail the antitumor,antithrombotic,antiviral,antibacterial,anti-i nflammatory,analgesic,antioxidant,wound-healing,antifibrotic,and hypoglycemic activities and mechanisms of action of EE based on existing in vitro and in vivo studies.We further propose the potential of EE for clinical translation in anticancer and lipid-modifying therapies,and its promise as source of a novel agent for wound healing and resistance to antibiotic tolerance.The earthworm enzyme lumbrokinase embodies highly effective anticoagulant and thrombolytic properties and has the advantage of not causing bleeding phenomena due to hyperfibrinolysis.Its antifibrotic properties can reduce the excessive accumulation of extracellular matrix.The glycolipoprotein extract G-90 can effectively scavenge reactive oxygen groups and protect cellular tissues from oxidative damage.Earthworms have evolved a well-developed defense mechanism to fight against microbial infections,and the bioactive agents in EE have shown good antibacterial,fungal,and viral properties in in vitro and in vivo experiments and can alleviate inflammatory responses caused by infections,effectively reducing pain.Recent studies have also highlighted the role of EE in lowering blood glucose.EE shows high medicinal value and is expected to be a source of many bioactive compounds.

Gut lumen-targeted oral delivery system for bioactive agents to regulate gut microbiome

Gut microbiome(GM)is closely related to the overall health status for the human being.The dysfunction of microbiome can lead to many diseases such as inflammation,cancer and neurodegenerative disease.Therefore,it's of great importance to develop effective strategy to regulate GM.Gut lumen-targeted oral delivery system(GLT-ODS)has been extensively investigated and widely used in food science and engineering in these years,due to the targeted delivery property,controlled release profile,high biocompatibility and enhanced bioavailability of cargos.Herein,we comprehensively summarized the current advances in GLT-ODS for bioactive agent.Specifically,we systematically summarize the GLT-ODS for pre-agents(prebiotics and probiotics)and anti-agents(antibiotics and bacteriophages)according to the type of cargos.Through in-depth discussion of representative researches,we refined the limitations of existing research in carrier material and target selection,and drew a blueprint for the future technological research and development.We believe that GLT-ODS will become a safe,efficient,simple and precise GM management strategy for improvement of health and shine in the development of precision food and pharmaceutical engineering in future.

Potential bioactive coating system for high-performance absorbable magnesium bone implants

Magnesium alloys are considered the most suitable absorbable metals for bone fracture fixation implants.The main challenge in absorbable magnesium alloys is their high corrosion/degradation rate that needs to be controlled.Various coatings have been applied to magnesium alloys to slow down their corrosion rates to match their corrosion rate to the regeneration rate of the bone fracture.In this review,a bioactive coating is proposed to slow down the corrosion rate of magnesium alloys and accelerate the bone fracture healing process.The main aim of the bioactive coatings is to enhance the direct attachment of living tissues and thereby facilitate osteoconduction.Hydroxyapatite,collagen type I,recombinant human bone morphogenetic proteins 2,simvastatin,zoledronate,and strontium are six bioactive agents that show high potential for developing a bioactive coating system for high-performance absorbable magnesium bone implants.In addition to coating,the substrate itself can be made bioactive by alloying magnesium with calcium,zinc,copper,and manganese that were found to promote bone regeneration.

Gathering scientific evidence for a new bioactive natural ingredient:The combination between chemical profiles and biological activities of Flueggea virosa extracts

Flueggea virosa (Roxb. ex Willd.) Royle is a plant with several traditional uses in tropical countries. To study the potential usefulness, extracts from stem barks and leaves of F. virosa were obtained with different solvents. The phytochemical composition was assessed using LC-MS and NMR. Triterpenes, as oleanolic (0.05-88.09 mg/g extract), and ursolic (0.03-94.36 mg/g extract) acids were determined. In addition, ellagic and gallic acid derivatives were present in large concentrations in some of the extracts. Antioxidant (radical scavenging, reduction ability, and metal chelating) and enzyme inhibitory (cholinesterase, tyrosinase, amylase, and glucosidase) effects were assessed by in vitro chemical assays. The methanol extracts and infusions from both parts show higher antioxidant ability when compared with ethyl acetate extracts, and the antioxidant capacity was correlated with the total phenolic contents of the tested extracts. The extracts demonstrate enzyme inhibitory abilities on AChE and BChE, and multivariate approaches allowed for correlating the activities with the presence of triterpenoids (R > 0.8). Furthermore, molecular docking was used to get insights into the interactions between the triterpenoids and the tested enzymes. Together, these results indicate that F. virosa represents a significant source of naturally-occurring bioactive compounds that can be exploited as a new ingredient for the development of novel functional products with promising biological properties.

Integration of in vitro and in silico approaches to assess three Astragalus species from Turkey flora:A novel spotlight from lab bench to functional applications

Members of the genus Astragalus have a great interest as a source of natural bioactive compounds on a scientific platform.To provide multidirectional insights into three Astragalus species(A.setulosus,A.anthylloides,and A.ovalis),the current work focused on the chemical characterization and biological properties of their extracts(aerial parts and roots).The chemical characterization of the extracts was detected by HPLC-MS/MS analysis.The biological properties were evaluated by antioxidant,enzyme inhibitory,and cytotoxic parameters.Assays for radical quenching,reducing capacity,and metal chelation were also used to evaluate antioxidant properties.To test the enzyme inhibitory effects of the extracts,cholinesterases,tyrosinase,α-amylase,andα-glucosidase were utilized as target enzymes.Two cancer cell lines,(MCF-7(human breast cancer cell line)and HeLa(Human cervix cancer cell line),were selected to evaluate cytotoxic effects.Generally,5-caffeoylquinic acid(2.43-283.92μg/g extract),hyperoside(4.33-216.22μg/g extract)and rutin(1.09-184.98μg/g extract)were the main constituents.The extracts from aerial parts and roots of A.anthylloides showed stronger radical scavenging and reducing power abilities compared to A.setulosus and A.ovalis.The best AChE and BChE inhibitory effects were determined in the aerial parts of A.setulosus(2.18 mg GALAE/g)and roots of A.ovalis(4.76 mg GALAE/g),respectively.The extracts of A.ovalis had the highest tyrosinase inhibitory abilities.The extract from aerial parts of A.setulosus showed stronger cytotoxic effects compared to other extracts.Pearson’s correlation analysis revealed that the presence of some compounds(resveratrol,p-coumaric,5-caffeoylquinic,and ferulic acids,etc)was linked to the observed biological activities.Molecular docking was also provided for the possible interaction of enzymes as well as protein targets of the tested cell lines.Our findings provide a scientific basis for the Astragalus species,which may serve as a source of naturally occurring bioactive compounds for health-promoting applications.

Chemical characterization,comprehensive antioxidant capacity,and enzyme inhibitory potential of leaves from Pistacia terebinthus L.(Anacardiaceae)

Pistacia terebinthus,Anacardiaceae,is used in traditional medicine and its fruits are consumed as coffee in Turkey.However,the research on the chemical and biological activity of P.terebinthus leaves is almost lack.In the present study,we aimed to evaluate the comprehensive antioxidant capacity(DPPH,ABTS,reducing power and metal chelating activity)and enzyme inhibitory effects(against AChE,BChE,α-amylase,α-glucosidase,and tyrosinase)as well as phytochemical content of the leaves extracts from P.terebinthus.The phytochemical composition in extracts were analysed using UHPLC-MS.Total phenolics and flavonoids contents of the extracts were 65.51-210.54 mg GAE/g and 54.94-169.89 mg RE/g,respectively.The highest level of total phenolic content was found in the methanol extract while the maximum total flavonoid content observed in ethyl acetate extract.The antioxidant results showed that methanol extract(ABTS:3.29 mmol TE/g,DPPH:2.06 mmol TE/g,CUPRAC:2.67 mmol TE/g,FRAP:1.62 mmol TE/g,Metal chelating activity:65.65 mg EDTA/g)exhibited promising antioxidant capacity.The methanol extract also demonstrated important enzyme inhibitory effects.The results suggest that the extracts of P.terebinthus leaves has the potential to be used as good candidate of natural antioxidants and enzyme inhibitors.