Bioactive Research Articles

The Immunologic Downsides Associated with the Powerful Translation of Current COVID-19 Vaccine mRNA Can Be Overcome by Mucosal Vaccines

The action of mRNA-based vaccines requires the expression of the antigen in cells targeted by lipid nanoparticle–mRNA complexes. When the vaccine antigen is not fully retained by the producer cells, its local and systemic diffusion can have consequences depending on both the levels of antigen expression and its biological activity. A peculiarity of mRNA-based COVID-19 vaccines is the extraordinarily high amounts of the Spike antigen expressed by the target cells. In addition, vaccine Spike can be shed and bind to ACE-2 cell receptors, thereby inducing responses of pathogenetic significance including the release of soluble factors which, in turn, can dysregulate key immunologic processes. Moreover, the circulatory immune responses triggered by the vaccine Spike is quite powerful, and can lead to effective anti-Spike antibody cross-binding, as well as to the emergence of both auto- and anti-idiotype antibodies. In this paper, the immunologic downsides of the strong efficiency of the translation of the mRNA associated with COVID-19 vaccines are discussed together with the arguments supporting the idea that most of them can be avoided with the advent of next-generation, mucosal COVID-19 vaccines.

Cobalt‐Catalyzed Hydroarylation of 2,3‐Dihydrofuran to Access α‐Arylated Tetrahydrofurans

AbstractThe α‐arylated tetrahydrofurans, commonly found in biologically active molecules, exhibit diverse biological activities and pharmacological effects. The functionalization of 2,3‐dihydrofuran offers a potential route for the synthesis of substituted tetrahydrofurans. Nevertheless, the development of earth‐abundant metal‐catalyzed regioselective hydrofunctionalization of 2,3‐dihydrofuran for the synthesis of substituted tetrahydrofurans remains to be pursued. Herein, we report a cobalt‐catalyzed hydroarylation of 2,3‐dihydrofuran, which serves as the first example of cobalt hydride‐catalyzed alkene hydroarylation. This reaction provides an efficient method for the synthesis of α‐arylated tetrahydrofurans with high reaction efficiency, exclusive α‐arylation selectivity, and remarkable functional group compatibility.

Phytosomes as Novel Drug Delivery Methods

As newly identified phytochemicals increase, studies on their potential medicinal applications in biological contexts will be updated. Nevertheless, these chemicals' limited solubility and susceptibility to degradation limit their use in medicinal and food applications. Currently, learning more about vesicular drug delivery methods may aid in enhancing these features. Because of their exceptional trapping capability, safety, and biocompatibility, vesicles have been demonstrated to be extremely promising delivery methods for a variety of beneficial phytochemicals at a cellular level. Phytosomes, a kind of vesicular drug carrier, combine phytochemicals with phospholipids to produce a complex that enhances compound stability overall and improves the absorption and bioavailability of bioactive compounds. One of the newest, smaller-sized lipid-based vesicles to increase the transport of plant- based nutraceuticals is the nano-phytosome. To guarantee a good safety profile and fulfill repeatability requirements, physical measurements that provide details on the dynamics of release and formulation stability must be thoroughly analyzed. Although there is presently not enough data from clinical trials to make judgments about the biological activities of specific preparations, the overall strength of the evidence supporting these formulations is positive and encourages more study in this area. Clinical trials on standardized products that demonstrate greater effectiveness than unformulated components or extracts will be essential in the future to raise awareness of these technologies.

Unveiling the Biological Activities, Pharmacological Potential, and Health Benefits of Sorbifolin: A Comprehensive Review.

Bioactive phytochemicals act as important factors with preventive and therapeutic potential in the pathogenesis of several disorders, often related to oxidative stress. Many dietary plant secondary metabolites could lower these conditions. Sorbifolin is one of these metabolites. This work is the first review of sorbifolin, a flavone detected in various plant matrices as a major compound. The present study discussed the natural sources, extraction, purification, quantification, and assessment of the biological activities of sorbifolin. Several databases including Google Scholar, Web of Sciences, and Science-Direct were consulted for relevant English articles related to sorbifolin, the phytochemical profiles of several medicinal plants containing this compound, and its biological activities, such as antioxidant, anticancer, antimicrobial, anti-inflammatory, and antidiabetic. The positive in vitro and in silico outcomes reported in the literature should be followed by additional in vivo and clinical investigations to further research the mechanisms of action, pharmacokinetic/pharmacodynamic activities, toxicological effects, pharmacological properties, and therapeutic potential of sorbifolin.

Pimarane diterpenoids: sources, structures and biological activities

Pimarane diterpenoids: sources, structures and biological activities

Glucocorticoids influence on rat hematological parameters and catalase activity

In this study, the impact of glucocorticoid, betamethasone dipropionate on enzyme activity in vitro and its effects on hematological parameters in vivo was investigated. The immobilized catalase, crucial for cell oxidative stress response via hydrogen peroxide reduction, exhibited a robust electrocatalytic response, maintaining its biological activity. The in vitro inhibition kinetics of catalase, as determined by electrocatalytic methods and expressed using Lineweaver-Burke diagrams, revealed an uncompetitive type of inhibition with altered Imax and Km in the presence of a range of betamethasone dipropionate concentrations. The in vivo experiments conducted on Rattus norvegicus demonstrated significant alterations in hematological parameters following betamethasone dipropionate administration. These changes included a decrease in erythrocyte count, an increase in hemoglobin, a reduction in mean corpuscular volume (MCV), and an elevation in mean corpuscular hemoglobin (MCH) and mean corpuscular hemoglobin concentration (MCHC). Notably, the leukocyte counts substantially increased. The observed hematological shifts suggest an impact of betamethasone dipropionate on the hematopoietic system, reinforcing the need for cautious corticosteroid administration. The findings underline the necessity for judicious corticosteroid treatment, acknowledging both enzymatic and systemic repercussions.

Odontites linkii subsp. cyprius Ethanolic Extract Indicated In Vitro Anti-Acanthamoeba Effect

This study aims to investigate three endemic ethanolic leaf extracts from Cyprus for anti-Acanthamoeba activities: Odontites linkii subsp. cyprius (Boiss.) Bolliger, Ptilostemon chamaepeuce subsp. cyprius (Greuter) Chrtek & B. Slavík, and Quercus alnifolia Poech. Screening for radical scavenging activity, total phenolic content (TPC), and total flavonoid content (TFC) were performed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABST) methods, Folin–Ciocalteu method, and aluminum chloride method, respectively. An antibacterial-susceptibility test (AST) was performed using a broth microdilution assay to estimate the minimum inhibitory concentration (MIC) using iodonitrotetrazolium chloride (INT). Trypan blue (0.5%) was used to assess in vitro anti-Acanthamoeba cell viability of the ethanolic leaf extracts after 24-, 48-, and 72-h exposure—screening of ethanolic leaf extracts with liquid chromatography–mass spectrometry (LC-MS) for known compounds with biological activity. The ethanolic leaf extract of Odontites linkii subsp. cyprius demonstrated the highest anti-Acanthamoeba activity, with an inhibitory concentration (IC50) of 7.02 mg/mL after 72 h. This extract also showed an in vitro minimum inhibitory concentration (MIC) of 0.625 mg/mL against Enterococcus faecalis, a common nosocomial pathogen. The LC-MS analysis revealed the presence of bioactive iridoid compounds in O. linkii subsp. cyprius, further highlighting its potential as a source for new drug compounds. The ethanolic extract of O. linkii subsp. cyprius demonstrated a dose-dependent and time-dependent anti-Acanthamoeba effect in vitro. This study is the first to report the presence of iridoid compounds and anti-Acanthamoeba activities in the ethanolic extract of O. linkii subsp. cyprius. These promising findings highlight the potential of plant extracts, particularly O. linkii subsp. cyprius, as a source for new drug compounds for Acanthamoeba infections.

Association of Oral Manifestations with Iron Deficiency Anemia: A Case-Control Study

Insufficient iron levels cause oral signs of iron insufficiency. Iron is necessary for several biological activities, including oral tissue health. Low iron levels might alter oral tissues, causing particular symptoms. The aim of this study to detect the oral manifestations of iron deficiency anemia as well as to investigate the link between the severity of these manifestations and the degree of the iron deficiency. The study includes 100 patients with iron deficiency anemia at an Azadi Teaching Hospital, in Duhok City, North of Iraq, and 98 healthy persons. A full history was obtained, and complete blood count and serum ferritin were recorded. In terms of gender distribution, a clear dominance of females was observed, as they represented 94% of the total cases compared to only 6% for males. Regarding the severity of anemia, most patients had moderate to mild degrees, while severe anemia cases represented a smaller percentage (12%). The comparison between patients and healthy people showed highly significant statistical differences in all pathological changes of the oral mucosa. Complete absence of pathological changes was more common in healthy controls (85%) than in patients (34%). Some pathological changes were closely associated with iron deficiency anemia, such as atrophic glossitis and angular cheilitis. This study concludes by highlighting the strong correlation between iron deficiency anemia (IDA) and oral mucosal lesions, and the most common oral manifestations are present in patients with severe iron deficiency anemia.

DNA barcoding, micromorphology and metabolic traits of selected Ficus L. (Moraceae) species from Egypt

AbstractThe genus Ficus of the family Moraceae, is one of the largest genera of angiosperms, with diverse pharmaceutical applications and biological activities. The traditional approaches based on the morphological traits have been frequently implemented for taxonomical identification of the different taxa of Ficus, however, encompassing these features are quite laborious, due to the dependence of these phenotypic traits on the environmental conditions. So, authenticating the taxonomical identity of the Ficus taxa with molecular barcoding and metabolic profiling, as relatively stable traits, could be a relevant approach for confirming the traditional phenotypic traits of this genus. Nine species of the genus Ficus namely F. amplissima Sm., F. benjamina L. F. binnendijkii, F. drupacea var. pubescens, F. elastica Roxb., F. microcarpa L., F. religiosa L., F. tinctoria subsp. gibbosa and F. virens var. sublancelata in Egypt, were selected for this study. From the anatomical features, three species of subsection Urostigma, F. religiosa, F. virens var. sublanceolata have cystoliths on the abaxial layer, whereas in F. amplissima it was on the adaxial layer. The UPGMA dendrogram of the studied Ficus taxa has been generated from the 21 anatomical characters, categorized the studied taxa into two clusters (I and II) of average distance ~ 3.5, each cluster has been further divided into subclusters I and II. The sub-cluster I includes F. religiosa, F. virens var. sublanceolata and F. tinctoria subsp. gibbosa were grouped together to subsection Urostigma, while the sub-cluster II of the cluster I includes F. benjamina and F. amplissima. From the DNA barcoding analysis, three clusters I, II and III were emerged, the cluster I includes F. benjamina, F. binnendjikee, and F. amplissima. The cluster II, F. virens var. sublanceolata and F. religiosa that belong to subsection Urostigma, while, the cluster III includes F. elastica and F. drupacea var. pubescens, F. microcarpa that belongs to subsection Conosycea. From the metabolic profiling of Ficus species, the major compounds; H-cycloprop-azulen-7-ol, 3,7,11,15-Tetramethyl-2-hexadecen-1-ol, 2-(9-octadecenyloxy), pentadecanoic acid, phytol, sitosterol and 9,12-octadecadienoic acid were the common among the taxa, with an obvious fluctuation, that could be a chemotaxonomic markers for these species of Ficus. Based on the metabolic profiling, two distinct clusters I and II were evolved, the cluster I involve F. elastica, F. benjamina, F. drupacea var. pubescens, F. amplissima, while, the cluster II had F. tinctoria subsp. gibbosa and F. religiosa. The fluctuation on the metabolites of the tested Ficus species could be a metabolic fingerprint for each species. So, the delamination of the tested plants based on their anatomical traits was typically matched to the separation based on the ITS sequence analysis.

Isolation of new isoflavonoids derivatives from Genista carinalis Griseb. and biological activity

Isolation of new isoflavonoids derivatives from <i>Genista carinalis</i> Griseb. and biological activity

Turkish Astragalus Species: Botanical Aspects, Secondary Metabolites, and Biotransformation

Abstract Astragalus is a widespread genus comprising approximately 3500 species, both annual and perennial, found across Asia, Europe, Africa, and the Americas. In Turkey, it is represented by 63 sections and 485 taxa with a high endemism ratio (51%). In traditional medicine, the roots of various Astragalus species represent very old and well-known drugs used for antiperspirant, diuretic, and tonic purposes, as well as for the treatment of nephritis, diabetes, leukemia, and uterine cancer. The genus Astragalus is the richest source of cycloartane-type compounds, which display a diverse range of bioactivities, such as wound healing, immunomodulatory, antitumor, hepatoprotective, antimutagenic, antiviral, and antiprotozoal activities. Moreover, cycloastragenol, the main sapogenol of many cycloartane-type glycosides found in the Astragalus genus, has gained attention as a potent telomerase activator over the past decade. The preparation of cycloastragenol derivatives could be significant in the near future due to their unique bioactivity. This review covers the botanical aspects of Astragalus L., as well as the phytochemical and biological activity studies conducted on Turkish Astragalus species, with a special focus on cycloartenols. It contains 36 articles reporting the phytochemistry of 29 Astragalus species and 111 new compounds, including 104 triterpene saponins. In addition to the phytochemical studies, this review summarizes the biotransformation studies on Astragalus cycloartanes via endophytic fungi isolated from the tissues of Astragalus species.

Study of anti-inflammatory activity and acute toxicity indicators of new silver salt of pyrazole-3-carboxamide

Objective. To study the anti-inflammatory activity and some toxicological indicators of the new derivative of pyrazole-3-carboxamide SSP. Materials and methods. To assess the biological activity of the compound, its anti-inflammatory effect was studied in the model of acute inflammatory edema caused by sub-plantar injection of carrageenan solution into a rat`s hind leg. The duration effect was assessed by the intensity of suppression of the inflammatory response in relation to the control level. In order to study the safety of the substance, the local irritant effect was determined when applied cutaneously in the experiments on rats. The severity of the irritant effect was assessed by the erythema degree, the amount of edema and the increase in local skin temperature. In addition, acute toxicity of the substance under study was determined. The test compound and reference drugs were applied to the skin. Results. The study of acute toxicity of the compound SSP and the reference drug nystatin when applied cutaneously to rats showed that LD50 of both substances was more than 2500,0 mg/kg. Indicators of the degree of local irritating effect of the drugs demonstrate its absence. At the same time, the studied SSP compound has no anti-inflammatory effect administered either orally or cutaneously. Conclusions. The data obtained allow us to classify the new silver salt of pyrazol-3-carboxamide SSP as a class 5 non-toxic substance. The studied SSP compound has no local irritant effect and does not demonstrate anti-inflammatory activity in the carrageenan inflammation model.

Innovative organic nutrient management and land arrangements improve soil health and productivity of wheat (Triticum aestivum L.) in an organic farming system

IntroductionSoil health is vital for ecosystems, but excessive use of fertilizers, chemicals, and irrigation harms soil fertility, leading to reduced yields and degradation. Thus, exploring innovative land arrangements and nutrient management for staple crops such as wheat is essential. Organic farming offers a promising solution. This study hypothesized that an appropriate land arrangement, combined with split applications of farmyard manure (FYM) and liquid organic fertilizer, can enhance wheat productivity while also improving soil health. The objective of this study was to investigate the effects of different sowing methods and organic nutrient management practices on the productivity of wheat and soil health.MethodsThis study aimed to examine the impact of sowing methods and nutrient management practices on soil health and organic wheat productivity during the winter seasons of 2021–22 and 2022–23 at the Organic Farming Unit (Agronomy), Rajasthan College of Agriculture, MPUAT, Udaipur. The experiment was arranged in a split-plot design, with three land arrangements/sowing methods in the main plot and eight nutrient management approaches in the subplots.ResultsConcerning different land arrangements, the furrow irrigated raised bed sowing (FIRB) method resulted in the maximum wheat yield (4.34 t ha−1) compared with flat row sowing and zero tillage sowing. With respect to nutrient management practices, 75% of the recommended dose of N (RDN) through the FYM was basal + 25% RDN with the 1st irrigation + Jeevamrut application at 500 L ha−1 during sowing, and the 1st irrigation + Panchagavya spraying at 5% during the booting stage resulted in the highest grain yield (4.47 t ha−1). Both the zero tillage and FIRB land arrangements resulted in better soil biological activities and microbial counts than did flat sowing. The results indicate that sowing wheat via the FIRB method, with the recommended nitrogen dose applied through split applications of FYM along with liquid organic manures such as Jeevamrut and Panchagavya, can be an excellent option for organic wheat cultivation. This approach can enhance both yield and soil health.ConclusionSeventy-five percent RDN through FYM as a basal + 25% RDN during the 1st irrigation + Jeevamrut at 500 L ha−1 during sowing and the 1st irrigation + spraying of Panchagavya at 5% during the booting stage effectively increased the growth and yield of organic wheat. With respect to land arrangements, both FIRB and zero tillage resulted in better growth, yield, and soil biological properties. The practical utility of this study is the optimization of split applications of FYM and land arrangements for organic wheat cultivation.

A multidirectional study on chemical fingerprints and biological activities of three Cistus extracts (C. creticus, C. laurifolius, and C. salviifolius) with ethnomedicinal uses

A multidirectional study on chemical fingerprints and biological activities of three Cistus extracts (C. creticus, C. laurifolius, and C. salviifolius) with ethnomedicinal uses

Genus Stachys—Phytochemistry, Traditional Medicinal Uses, and Future Perspectives

The genus Stachys represents one of the most extensive genera within the subfamily Lamioideae and ranks as one of the largest genera in the Lamiaceae family. Many Stachys species are associated with a rich history in traditional medicine across various cultures, and their extracts and essential oils are rich in non-volatile and volatile compounds. Because of their complex profile of bioactive substances, Stachys members are considered to possess an extensive spectrum of therapeutic properties, including antioxidant, anti-inflammatory, analgesic, antibacterial, cytotoxic, and wound-healing effects, as well as benefits for memory enhancement, lipid profile regulation, blood glucose control, and weight management. Despite the wide distribution and chemical diversity of the genus, studies on its biological activities remain limited. The aim of this review is to summarize the most relevant data from studies on the bioactive compounds, traditional uses, and pharmacological properties of Stachys species found in databases such as Science Direct, PubMed, and Scopus. Specific keywords were used in the search strategy, including “bioactive compounds”, “Stachys”, “Lamiaceae”, “Stachys extract”, “Stachys essential oil”, “traditional uses”, “chemical composition”, “therapeutic potential”, “clinical trials”, “in vivo studies”, “in vitro studies”. The search strategy was performed according to the guidelines for Preferred Reporting Items for Systematic Reviews and Meta-Analyses. Data from 171 studies were included. The manuscript highlights the drug-discovery potential of Stachys species, emphasizing their potential applications in medicine, cosmetics, dietary supplements, and the food industry. Moreover, it provides important data that could assist Stachys research programs.

AcsS inhibits the hemolytic activity and thermostable direct hemolysin (TDH) gene expression in Vibrio parahaemolyticus

Vibrio parahaemolyticus produces a key virulent factor known as thermostable direct hemolysin (TDH). TDH exhibits diverse biological activities, including hemolytic activity. The β-type hemolysis observed on Wagatsuma agar due to TDH is recognized as the Kanagawa phenomenon (KP). The tdh2 gene is primarily responsible for TDH production and the associated KP. AcsS was originally identified as an activator of swimming and swarming motility in V. parahaemolyticus. However, the extent of its potential to regulate other cellular pathways remains unclear. In this study, we explored the regulatory effects of AcsS on the hemolytic activity and tdh2 expression in V. parahaemolyticus. The data showed that V. parahaemolyticus hemolytic activity and tdh2 transcription were under the negative control of AcsS. Additionally, in vitro binding assays revealed that His-AcsS could not bind to the regulatory DNA region of tdh2. However, overexpression of AcsS in an Escherichia coli strain suppressed the expression of tdh2. Collectively, these results suggested that AcsS suppresses the hemolytic activity of V. parahaemolyticus through the downregulation of tdh2 transcription. The data enhanced our understanding of the regulatory networks governing tdh2 expression and the roles of AcsS in this bacterium.

Extraction, purification, structural characterization, bioactivities, modifications and structure–activity relationship of polysaccharides from Ophiopogon japonicus: a review

Ophiopogon japonicus (Thunb.) Ker Gawl., is a traditional Chinese medicine (TCM) with a history of thousands of years. O. japonicus polysaccharides (OJPs), as one of the main active ingredient, are a kind of representative pharmacological bioactive macromolecules and mainly composed of Glc and Fru with molecular weight between 2.48 and 325 kDa. OJPs have a variety of biological activities, such as hypoglycemic, cardioprotective, immunomodulatory, improvement of obesity, and renal protective activity. In this review, the extraction, purification and structural characterization of OJPs were systematically reviewed, and its biological function, molecular mechanism and structure–activity relationship were analyzed. Additionally, this review summarized and found that structural modifications such as liposome modification, sulfation modification, and polyethylene glycol modification have improved the pharmacological activity and bioavailability of OJPs. Overall, this work will help to better understand OJPs and provide a theoretical review of their further development and utilization in the field of medicine and health food.

“Antimicrobial and antioxidant capacity of Dunaliella salina, Tetraselmis chuii and Isochrysis galbana and their potential use in food.” a systematic review

AbstractThe main compounds extracted from the biomass of marine microalgae have antioxidant, antimicrobial, antifungal, anti-inflammatory and antitumor effects, making the possibility of using these properties in the development of foods feasible. Despite the proven biological activity of microalgae, there are still challenges regarding the production and use of microalgal biomass or its derivatives in food industries that are related to high production costs, and there is little research regarding the evaluation of their safety and the search for their application in food development. Therefore, this research aimed to collect information regarding the biological activities of marine microalgae, which allows their use as a natural antimicrobial additive in food matrices and as an ingredient in the development of functional foods with antioxidant capacity. The search interval for the PRISMA (preferred reporting items for systematic reviews and meta-analyses) guidelines was five years. Different methods for the extraction of antioxidant and antimicrobial compounds from the marine microalgae Dunaliella salina, Tetraselmis chuii and Isochrysis galbana were compared and discussed, and the viability of their use and application in food matrices and in the food industry in general were analyzed. It was concluded that there are research gaps in the use of microalgae biomass as an extract, the identification of bioactive molecules for use in the food industry as antimicrobial agents and for the development of functional foods with antioxidant capacity.

Phytochemical Compounds, and Antioxidant, Anti-Hyperglycemic, and Anti-Inflammatory Activity of Microencapsulated Garambullo (Myrtillocactus geometrizans) Extract During In Vitro Digestion and Storage

Garambullo fruit (Myrtillocactus geometrizans) is a rich source of phytochemical compounds that exhibit antioxidant, anti-hyperglycemic, and anti-inflammatory activities, helping to prevent diseases associated with oxidative stress. The objective of this study was to evaluate phenolic compound (PC), betalain (BL), betaxanthin (BX), and betacyanin (BC) contents, and in vitro biological activities (antioxidant, anti-hyperglycemic, and anti-inflammatory) in microencapsulated garambullo extract during in vitro gastrointestinal digestion and storage. Microencapsulation was performed using spray drying. Arabic Gum (GA, 10% in feed solution) and soy protein isolate (SPI, 7% in feed solution) were used as wall materials. After in vitro digestion, the microcapsules (GA, SPI) exhibited higher bioaccessibility (p ≤ 0.05) of PC, BL, BX, and BC, and higher antioxidant activity (AA), compared to the non-encapsulated extract. Both microcapsules showed bioaccessibility in anti-hyperglycemic activity: α-amylase (GA: 90.58%, SPI: 84.73%), α-glucosidase (GA: 76.93%, SPI: 68.17%), and Dipeptidyl peptidase-4 (DPP-4) (GA: 52.81%, SPI: 53.03%); and in anti-inflammatory activity: cyclooxygenase-1 (COX-1) (GA: 78.14%, SPI: 77.90%) and cyclooxygenase-2 (COX-2) (GA: 82.77%, SPI: 84.99%). During storage, both microcapsules showed a similar trend with a significant decrease (p ≤ 0.05) in PC (GA: 39.29%, SPI: 39.34%), BL (GA: 21.17%, SPI: 21.62%), BX (GA: 23.89%, SPI: 23.45%), BC (GA: 19.55%, SPI: 19.84%), and AA (GA: 41.59%, SPI: 42.51%) after 60 days at 30 °C. Both microcapsules retained anti-hyperglycemic activity evaluated by the inhibitory activity of α-amylase (GA: 68.84%, SPI: 70.18%), α-glucosidase (GA: 59.93%, SPI: 58.69%), and DPP-4 (GA: 52.81%, SPI: 53.01%), and anti-inflammatory activity evaluated by the inhibitory activity of COX-1 (GA: 82.18%, SPI: 82.81%) and COX-2 (GA: 81.11%, SPI: 81.08%). Microencapsulation protected the phytochemical compounds and in vitro biological activities by allowing controlled release during in vitro digestion compared to the non-encapsulated extract. However, after 60 days storage at 30 °C, 60% of PC and AA, 80% of BL, BX, and BC, and 20–45% of the anti-hyperglycemic and anti-inflammatory activity were lost.

Production of Value-Added Arabinofuranosyl Nucleotide Analogues from Nucleoside by an In Vitro Enzymatic Synthetic Biosystem

Arabinofuranosyl nucleotide analogue (arabinoside) and the derived compounds, a family of nucleoside analogues, exhibit diverse, typically biological activities and are widely used as antibacterial, antiviral, anti-inflammatory, and antitumor drugs in both clinical and preclinical trials. Despite their long and rich history in medicinal chemistry, the biosynthesis of arabinoside has only been sporadically designed and studied and has remained a challenging task. In this study, an in vitro synthetic enzymatic biosystem was designed and constructed for the production of arabinoside from low-cost nucleoside, based on a phosphorolysis -isomerization-dephosphorylation enzymatic cascade conversion routes. The enzymatic system achieves the biosynthesis of arabinoside by isomerizing the ribose part of nucleoside to arabinose. The reaction conditions affecting the yield of arabinoside were investigated and optimized, including meticulous enzyme selection, key enzyme dosage, the concentration of orthophosphate, and reaction time. Under the optimized conditions, we achieved the production of 0.12 mM of arabinofuranosylguanine from 0.5 mM of guanosine, representing 24% of the theoretical yield. Furthermore, this biosystem also demonstrated the capability to produce other arabinosides, such as vidarabine, spongouridine, and hypoxanthine arabinofuranoside from corresponding nucleosides. Overall, our biosynthesis approach provides a pathway for the biosynthesis of arabinoside.