Triterpene Compounds Research Articles

Synthesis and antitumor evaluation of glycyrrhetinic acid‐dithiocarbamate hybrids

AbstractGlycyrrhetinic acid (GA) is a naturally occurring triterpene compound. The aim of this study was to employ the pharmacophore hybrid strategy to merge GA with various dithiocarbamates and obtain novel compounds with better antitumor activities. We present a two‐step synthetic protocol wherein the GA derivative underwent reaction with carbon disulfide and various secondary amines in a one‐pot manner under mild conditions, facilitating the preparation of a series of structurally novel GA‐dithiocarbamate derivatives. Bioassay screening revealed that the representative compound 3c demonstrated the capacity to reduce the mitochondrial membrane potential in Hep3B and Huh‐7 cells, induce nuclear apoptosis, inhibit invasion and migration, and prompt both early and late apoptosis. Furthermore, our research findings indicated that this apoptotic phenomenon may be associated with the expression of Bcl‐2, Bax, Bak, PARP, and cleaved‐PARP proteins. Utilizing network pharmacology for predicting core targets and signaling pathways of compound 3c for hepatocellular carcinoma (HCC) treatment involved employing molecular docking models to demonstrate high affinity between compound and target protein. In conjunction with Western blot analysis, compound 3c may impact HCC through the PI3K‐AKT‐mTOR pathway.

Oleanolic acid induces hepatic injury by disrupting hepatocyte tight junction and dysregulation of farnesoid X receptor-mediated bile acid efflux transporters.

Oleanolic acid (OA) is a naturally occurring pentacyclic triterpene compound that has been reported to cause cholestatic liver injury. However, the regulation and pathogenic role of bile acids in OA-induced development of cholestatic liver injury remains largely unclear. Farnesoid X receptor (FXR) is a metabolic nuclear receptor that plays an important role in bile acid homeostasis in the liver by regulating efflux transporters bile salt export pump (BSEP) and multidrug resistance-associated protein 2 (MRP2). The aim of this study was to investigate the effect of OA on hepatocyte tight junction function and determine the role of FXR, BSEP, and MRP2 in the mechanism of impairment of transport of bile acids induced by OA. Both in vivo and in vitro models were used to characterize the OA-induced liver injury. The liquid chromatography-tandem mass spectrometry (LC-MS) was employed to characterize the efflux function of the transporters, and the results showed that OA caused a blockage of bile acids efflux. OA treatment resulted in decreased expression levels of the tight junction proteins zonula occludens-1 and occludin. Immunofluorescence results showed that OA treatment significantly reduced the number of bile ducts and the immunofluorescence intensity. Pretreatment with agonists of FXR and MRP2, respectively, in animal experiments attenuated OA-induced liver injury, while pretreatment with inhibitors of BSEP and MRP2 further aggravated OA-induced liver injury. These results suggest that OA inhibits FXR-mediated BSEP and MRP2, leading to impaired bile acid efflux and disruption of tight junctions between liver cells, resulting in liver damage.

Enhancing the medicinal properties and phytochemical content of bitter melon (Momordica charantia L.) through elicitation with brassinosteroid, ethrel, and carrageenan

Bitter melon (Momordica charantia L.) is well-known for its high protein, steroid, alkaloid, mineral, lipid, triterpene, and phenolic compound content, as well as its medicinal properties, particularly its anti-diabetic effects. To investigate the impact of elicitors on the morphology and phytochemical characteristics of bitter melon (Jounpouri cultivar) over two consecutive years (2018 and 2019), we conducted a field experiment. The study aimed to determine the effects of Ethrel, brassinosteroids (BRs), and k-carrageenan on yield and the production of anti-diabetic agents in M. charantia farm crops. The elicitors included ten levels, ranging from a control group to Ethrel (100, 300, and 600 mg l− 1), brassinosteroids (BRs) (0.1, 0.5, and 1 mg l− 1), and k-carrageenan (200, 400, and 600 mg l− 1). These characteristics included leaf area, leaf length, leaf width, fruit parameters, carbohydrate content, total phenols and flavonoid accumulation, antioxidant activity, total acid, ascorbic acid, momordicine, and charantin. Across both years, we observed the highest flavonoid accumulation and antioxidant activity in the Ethrel treatment group. Specifically, applying 0.5 mg l− 1 BRs and 300 mg l− 1 Ethrel led to an 18.8% and 14.8% increase in momordicine content, respectively. All elicitor treatments, particularly at 0.1 mg l− 1 BRs, significantly increased leaf area, leaf length, and leaf width compared to the control group in both cropping years. Additionally, the application of all elicitors resulted in increased fruit weight, dimensions, and yield over the two consecutive years. Notably, in 2018, 600 mg l− 1 Ethrel contributed to enhanced fruit weight and yield, while in 2019, 0.5 mg l− 1 BRs exhibited the same effect. Metabolic and physiological changes in bitter squash induced by employed elicitors over two different years (2018–2019) are strongly dependent on a variety of environmental factors such as temperature and rainfall. In conclusion, using BRs as an elicitor has the potential to optimize the health benefits of bitter melon by increasing the content of two bioactive molecules, momordicine and charantin.

Exploring the Bioactive Potential of Taraxacum officinale F.H. Wigg Aerial Parts on MDA Breast Cancer Cells: Insights into Phytochemical Composition, Antioxidant Efficacy, and Gelatinase Inhibition within 3D Cellular Models

In this work, aerial parts of Taraxacum officinale F.H. Wigg. produced in Umbria, Italy, were chemically investigated by solid-phase microextraction/gas chromatography–mass spectrometry (SPME/GC-MS) to describe their volatile profile. The results obtained showed the preponderant presence of monoterpenes, with limonene and 1,8-cineole as the main components. Further analyses by GC/MS after derivatization reaction were performed to characterize the non-volatile fraction highlighting the presence of fatty acids and di- and triterpenic compounds. T. officinale methanol and dichloromethane extracts, first analyzed by HRGC/MS, were investigated to evaluate the antioxidant activity, cytotoxicity, and antiproliferative properties of MDA cells on the breast cancer cell line and MCF 10A normal epithelial cells as well as the antioxidant activity by colorimetric assays. The impact on matrix metalloproteinases MMP-9 and MMP-2 was also explored in 3D cell systems to investigate the extracts’ efficacy in reducing cell invasiveness. The extracts tested showed no cytotoxic activity with EC50 > 250 µg/mL on both cell lines. The DPPH assay revealed higher antioxidant activity in the MeOH extract compared with the DCM extract, while the FRAP assay showed a contrasting result, with the DCM extract exhibiting slightly greater antioxidant capacity. After treatment for 24 h with a non-cytotoxic concentration of 500 µg/mL of the tested extracts, gelatin zymography and Western blot analyses demonstrated that both MeOH and DCM extracts influenced the expression of MMP-9 and MMP-2 in MDA cells within the 3D cell model, leading to a significant decrease in the levels of these gelatinases, which are crucial markers of tumor invasiveness.

Recent trends in the elucidation of complex triterpene biosynthetic pathways in horticultural trees

Abstract Triterpene (C30 isoprene compounds) represents the most structurally diverse class of natural products and has been extensively exploited in the food, medicine and industrial sectors. Decades of research on medicinal triterpene biosynthetic pathways have revealed their roles in stress tolerance and shaping microbiota. However, the biological function and mechanism of triterpenes are not fully identified. Even this scientific window narrows down for horticultural trees. The lack of knowledge and a scalable production system limits the discovery of triterpene pathways. Recent synthetic biology research revealed several important biosynthetic pathways that define their roles and address many societal sustainability challenges. Here, I review the chemical diversity and biosynthetic enzymes involved in triterpene biosynthesis of horticultural trees. This review also outlines the integrated Design-Build-Test-Learn (DBTL) pipelines for the discovery, characterization and optimization of triterpene biosynthetic pathways. Further, these DBTL components share many fundamental and technical difficulties, highlighting opportunities for interdisciplinary collaboration between researchers worldwide. This advancement opens up unprecedented opportunities for the bioengineering of triterpene compounds towards development and scaleup processes.

Peritoneal dialysis promotes microbial-driven biosynthesis pathways of sesquiterpenes and triterpenes compounds in end-stage renal disease patients

The concept of the gut-kidney axis is gaining significant attention due to the close relationship between gut microbiota and kidney disease. Peritoneal dialysis is recognized as a crucial renal replacement therapy for end-stage renal disease (ESRD). The alterations in gut microbiota and related mechanisms after receiving this dialysis method are not fully understood. This study conducted shotgun metagenomic sequencing on fecal samples from 11 end-stage renal disease patients who did not receive dialysis (ESRD_N) and 7 patients who received peritoneal dialysis (ESRD_P). After quality control and correlation analysis of the data, our study is aimed at exploring the impact of peritoneal dialysis on the gut microbiota and health of ESRD patients. Our research findings indicate that the complexity and aggregation characteristics of gut microbiota interactions increase in ESRD_P. In addition, the gut microbiota drives the biosynthesis pathways of sesquiterpenes and triterpenes in ESRD_P patients, which may contribute to blood purification and improve circulation. Therefore, our research will lay the foundation for the prevention and treatment of ESRD.

Improving Water Solubility and Skin Penetration of Ursolic Acid through a Nanofiber Process to Achieve Better In Vitro Anti-Breast Cancer Activity.

Woman's breast cancer has always been among the top ten causes of cancer death, and nearly 2% to 5% of locally advanced breast cancers develop a fungating breast wound. Fungal breast cancer leads to skin ulcers, wound ruptures, and other bacterial infections in patients. Ursolic acid (UA), a natural pentacyclic triterpene compound, is widely distributed in many fruits. Previous studies demonstrated that UA has anti-breast cancer, antifungal, and improved wound-healing effects. UA, however, had poor water solubility and low bioavailability, restricting its clinical application. Nanofibers have the advantages of rapid dissolution, improved stability, and bioavailability of active ingredients. We had successfully prepared ursolic acid nanofibers (UANFs) and effectively improved their water solubility and skin penetration. UANFs can increase water solubility by improving the physicochemical properties, including increased surface area, intermolecular bonding with excipients, and amorphous transformation. Furthermore, UANFs had better anti-breast cancer activity than raw UA. UANFs inhibited the expression of phospho-signal transducer and activator of transcription 3 (STAT3) and phospho-extracellular regulated protein kinases (ERK)1/2, and induced cleaved caspase-3 protein expression, but had no effect on the raw UA treatment. In summary, UANFs enhanced the skin absorption of UA and improved its anti-breast cancer efficacy. We expect that UANFs can be used as an anti-breast cancer treatment and reduce the discomfort of breast cancer patients during dressing changes, but more detailed efficacy and safety trials still need to be conducted in further studies.

Determination of Biologically Active Compounds and Antioxidant Capacity In Vitro in Fruit of Small Cranberries (Vaccinium oxycoccos L.) Growing in Natural Habitats in Lithuania.

The composition of flavonols, proanthocyanidins, anthocyanins, triterpene compounds, and chlorogenic acid in small cranberry fruit samples collected in natural habitats in Lithuania and variation in the antioxidant capacity of cranberry fruit extracts was determined. This study showed that in the flavonol group, hyperoside and myricetin-3-O-galactoside predominated in cranberry fruit samples; in the anthocyanin group, the predominant compounds were cyanidin-3-O-galactoside, cyanidin-3-O-arabinoside, peonidin-3-O-galactoside, and peonidin-3-O-arabinoside, and in the group of triterpene compounds, ursolic acid was predominant. The highest total amounts of flavonols and anthocyanins were found in the samples collected in Čepkeliai State Strict Nature Reserve (2079.44 ± 102.99 μg/g and 6993.79 ± 350.22 μg/g, respectively). Cluster analysis of the chemical composition of small cranberry fruit samples revealed trends in the accumulation of bioactive compounds in cranberry fruit. Cranberry fruit samples collected in central Lithuania had higher levels of triterpene compounds. Statistical correlation analysis showed the strongest correlation between the quantitative composition of cyanidin-3-O-arabinoside and peonidin-3-O-arabinoside and the reducing capacity of the ethanolic extracts of the cranberry fruit samples assessed in vitro by the FRAP assay (r = 0.882, p < 0.01 and r = 0.805, p < 0.01, respectively). Summarizing the results, the geographical factor affects the variation of the quantitative composition of biologically active compounds in cranberry fruit samples.

Evaluation of potential Synergistic effect of Cranberry extract and Amoxicillin-Clavulanic acid using Checkerboard method

This study investigates the potential synergistic effect of Cranberry (Vaccinium oxycoccos) extract and Amoxicillin-Clavulanic acid in enhancing antibacterial effectiveness and combating resistance. The main objectives of this study are do determine the MIC and FIC values for Amoxicillin-Clavulanic Acid and Vaccinium oxycoccos extract on different bacterial strains, and therefore to evaluate the synergistic effect of compounds combined. Vaccinium oxycoccos extract is rich in proanthocyanidins, phenolic acids, anthocyanins, vitamin C, and triterpene compounds, and has demonstrated antibacterial, antifungal, and anti-inflammatory properties. This study specifically evaluates its potential to inhibit biofilm formation by gram-negative bacteria. Amoxicillin, a semi-synthetic penicillin, is combined with Clavulanic acid, a β-lactamase inhibitor, to treat various bacterial infections. However, the rising antimicrobial resistance challenges the efficacy of this antibiotic combination. The effectiveness of combining antibiotics and natural substances in inhibiting bacterial growth can vary among different bacteria. This research emphasizes the importance of personalized treatment for each bacterial strain to effectively combat antibiotic-resistant infections.

Anti-Inflammatory, Antioxidant, and Genoprotective Effects of Callus Cultures Obtained from the Pulp of Malus pumila cv Miller (Annurca Campana Apple).

Apples are rich in phytochemicals useful for human health. However, environmental factors can greatly affect the accumulation of these compounds. To face this problem, the callus culture technique was used to obtain large quantities of phytochemicals. Specifically, two callus cultures were obtained from ripe Annurca apple pulp (Malus pumila cv Miller) and cultivated under different light conditions: darkness and an 18-h photoperiod. The hydro-alcoholic extracts from the calli underwent analysis using GC-MS, GC-FID, and HPLC-DAD-ESI-MSn to determine the qualitative and quantitative content of phenolic and triterpenic acids. The study revealed the predominant presence of triterpenic compounds in both calli. Furthermore, we investigated their radical scavenging and antioxidant activities through DPPH, ABTS, ORAC assays, and lipoxygenase inhibition activity. Genoprotection was evaluated via nicking assay, and the anti-inflammatory effect was investigated via Griess assay on LPS-injured murine macrophages. All the analyses performed were compared with peel and pulp hydroalcoholic extracts. The results showed that both calli primarily show anti-inflammatory activity and moderate antioxidant effect and can protect DNA against oxidative stimuli. This data encouraged further research aimed at utilizing callus as a bioreactor to produce secondary metabolites for use in preventive and therapeutic applications to combat acute or chronic age-associated diseases.

Botanical Extracts and Compounds of Castanea Plants and Methods of Use: US20190125818A1 - The United States Patent Evaluation.

Bacterial infections are increasingly difficult to combat, which makes them a threat to public health on a global level. Staphylococcus aureus is considered one of the main causes of infections in hospitals, as it has a variety of virulence factors, as well as is able to produce bacterial biofilms, which, consequently, bring numerous damages to public health as a result of increased resistance to conventional antibiotics and a longer hospital stay. Therefore, the use of compounds extracted from medicinal plants is a potential pharmaceutically acceptable target, as they do not have toxicity and the potential to disrupt biofilms produced by Staphylococcus aureus already evidenced, thus revealing their relevance to our study. The objective of this work was to perform a critical analysis of a patent with natural extracts against bacterial biofilms found in the United States Patent and Trademark Office (USPTO) database, to map the possible bioactive compounds that may serve as potential future antimicrobial drugs. A technological survey was carried out to verify existing patents using natural extracts with anti-biofilm potential. For this, it was searched with the keywords: Botanical extracts AND biofilms; which were performed in the United States Patent and Trademark Office (USPTO) database. Thus, the selected patent used a non-aqueous extract partitioned and vacuum-contracted, subsequently lyophilized for assays with antimicrobial potential. Because of this, a patent was analyzed regarding its chemistry, and biological activity, followed by a critical analysis of the technology proposed in the invention. When using the keywords Botanical extracts AND biofilms in the USPTO, it was possible to find twenty-two inventions; however, only four patents in the USPTO were in agreement with the proposal of the natural extract having antimicrobial activity and an anti-biofilm potential, of which two belonged to the same applicant with similar proposals. The key point of this invention was to enable the compounds of the Castanea sativa plant and its methods of obtaining the extract to present a significant antimicrobial action associated or not with antibiotics, promoting the development of new therapies against bacterial infections capable of disrupting biofilms. The invention developed a methodology for extracting Castanea sativa, in which pentacyclic triterpene compounds were found mostly in its leaves. Whereas for the extraction, the crude methanol extracts called extracts 224 from the ground leaves were made by maceration, filtered, combined, concentrated under pressure in rotary evaporators, and lyophilized. After that, they were resuspended in water and partitioned in succession with hexane, ethyl acetate, and butanol. The most active refined partition was the 224C extract with the solvent ethyl acetate, which was subjected to further fractionation using silica column chromatography. Resulting in the most refined extract, which was 224C-F2, capable of acting directly on the quorum sensing of bacteria, mainly Staphylococcus aureus, blocking the translation of RNAIII, including a series of exotoxins. Regarding the antimicrobial capacity against Staphylococcus aureus, it presented Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of 1.56 μg/mL-1 and > 100 μg/mL -1, respectively. Given the analyzed patent, it was possible to verify the importance of alternatives to reduce the impact of bacterial biofilms, which causes damage to industries in general and to health. From this, the invention analyzed has a promising proposal with antimicrobial potential focusing on the great impact of bacterial biofilms. Therefore, natural extracts with antibiofilmic potential can help to minimize the economic losses caused to health due to these multidrug-resistant microorganisms with different virulence mechanisms.

Celastrol inhibits mouse B16-F10 melanoma cell survival by regulating the PI3K/AKT/mTOR signaling pathway and repressing HIF-1α expression.

Melanoma, with its high degree of malignancy, stands as one of the most dangerous skin cancers and remains the primary cause of death from skin cancer. With studies demonstrating the potential of traditional Chinese medicine to intervene and treat melanoma, we turned our attention to celastrol. Celastrol is a triterpene compound extracted from the traditional Chinese medicine derived from Tripterygium wilfordii. Previous studies have shown that celastrol exerts inhibitory effects on various malignant tumors, including melanoma. Hence, our goal was to clarify the impact of celastrol on cell viability, apoptosis, and cell cycle progression by elucidating its effects on the PI3K/AKT/mTOR pathway. CCK-8 and wound healing assays were used to determine the effect of celastrol on the viability and migration of B16-F10 cells. Changes in cell apoptosis, cell cycle, reactive oxygen species (ROS), and mitochondrial membrane potential were detected by flow cytometry. PI3K/AKT/mTOR pathway proteins and HIF-α mRNA expression in B16-F10 cells were detected by western blotting and qPCR. Moreover, the addition of a PI3K activator demonstrated that celastrol could inhibit the function of B16-F10 cells via the PI3K/AKT/mTOR pathway. Celastrol inhibited the viability and migration of B16-F10 cells. Through the inhibition of the PI3K/AKT/mTOR pathway down-regulates the expression of HIF-α mRNA, thereby causing an increase of ROS in cells and a decrease in the mitochondrial membrane potential to promote cell apoptosis and cell cycle arrest. The inhibitory effect of celastrol on B16-F10 cells was further demonstrated by co-culturing with a PI3K activator. Celastrol inhibits the function of B16-F10 cells by inhibiting the PI3K/AKT/mTOR cellular pathway and regulating the expression of downstream HIF-α mRNA.

Asiatic acid alleviates vascular remodeling in BAPN-induced aortic dissection through inhibiting NF-κB p65/CX3CL1 signaling.

Inflammation assumes a pivotal role in the aortic remodeling of aortic dissection (AD). Asiatic acid (AA), a triterpene compound, is recognized for its strong anti-inflammatory properties. Yet, its effects on β-aminopropionitrile (BAPN)-triggered AD have not been clearly established. The objective is to determine whether AA attenuates adverse aortic remodeling in BAPN-induced AD and clarify potential molecular mechanisms. Invitro studies, RAW264.7 cells pretreated with AA were challenged with lipopolysaccharide (LPS), and then the vascular smooth muscle cells (VSMCs)-macrophage coculture system was established to explore intercellular interactions. To induce AD, male C57BL/6J mice at three weeks of age were administered BAPN at a dosage of 1 g/kg/d for four weeks. To decipher the mechanism underlying the effects of AA, RNA sequencing analysis was conducted, with subsequent validation of these pathways through cellular experiments. AA exhibited significant suppression of M1 macrophage polarization. In the cell coculture system, AA facilitated the transformation of VSMCs into a contractile phenotype. In the mouse model of AD, AA strikingly prevented the BAPN-induced increases in inflammation cell infiltration and extracellular matrix degradation. Mechanistically, RNA sequencing analysis revealed a substantial upregulation of CX3CL1 expression in BAPN group but downregulation in AA-treated group. Additionally, it was observed that the upregulation of CX3CL1 negated the beneficial impact of AA on the polarization of macrophages and the phenotypic transformation of VSMCs. Crucially, our findings revealed that AA is capable of downregulating CX3CL1 expression, accomplishing this by obstructing the nuclear translocation of NF-κB p65. The findings indicate that AA holds promise as a prospective treatment for adverse aortic remodeling by suppressing the activity of NF-κB p65/CX3CL1 signaling pathway.

Poria acid inhibit the growth and metastasis of renal cell carcinoma by inhibiting the PI3K/akt/NF-κb signaling pathway

BackgroundPoria acid (PAC) is a triterpene compound found in Poria cocos, a traditional Chinese medicine (TCM). The current study aims to explore the therapeutic effects and potential mechanisms of PAC on the migration and proliferation of human renal cell carcinoma (RCC) cells as well as tumor growth in animal model. MethodsCell viability and proliferative capacity of normal renal cells and RCC cells were investigated by MTT assay. In addition, 786-O cells were divided into four groups and treated with different concentrations of PAC (0, 20, 40, and 60 μM) for 48 h. Cell scratch test and cell invasion assay were performed to evaluate the effects of PAC on the invasion and migration of RCC cells, respectively. The effects of PAC on apoptosis of RCC cells and expression levels of PI3K/Akt/NF-kB signaling pathway-related biomarkers were investigated using TUNEL staining and Western blotting methods, respectively. Effects of PAC on the inhibitory activity of RCC tumor in mice were evaluated in a 786-O CDX model. ResultsThe study found that PAC inhibited the viability of RCC cells in a dose-dependent manner, as demonstrated by in vitro cell assays (p < 0.05). However, PAC showed no significant inhibitory effect on normal renal cells (p > 0.05). PAC also significantly inhibited the migration and invasion of RCC via EMT/MMP signaling pathways (p < 0.05). Immunofluorescence and immunoblotting results showed that PAC induced the apoptosis of RCC, which was accompanied by changes in the expression levels of apoptosis-related proteins (p < 0.05). Moreover, PAC significantly downregulated the PI3K/Akt/NF-kB signaling pathway in a concentration-dependent manner (p < 0.05). The effect of PAC on RCC apoptosis was dramatically reversed by 740Y–P (PI3K agonist) (p < 0.05) but significantly enhanced in the presence of LY294002 (PI3K inhibitor) (p < 0.05). The results of in vivo experiment also demonstrated that the antitumor activity of PAC was achieved by affecting the PI3K/Akt/NF-kB signaling pathway. ConclusionsPAC can effectively suppress the proliferation, invasion and migration of RCC cells, and exhibit anti-tumor effects in RCC model by inhibiting the PI3K/Akt/NF-kB signaling pathway.

Comparative Phytoprofiling of Achillea millefolium Morphotypes: Assessing Antioxidant Activity, Phenolic and Triterpenic Compounds Variation across Different Plant Parts.

Achillea millefolium L., commonly known as yarrow, is a versatile and widely distributed plant species with a rich history of ethnopharmacological significance. This study aimed to evaluate the comparative differences of A. millefolium inflorescence morphotypes. The phytochemical profile of white and pink inflorescence morphotypes was characterised by a complex of thirty-four phenolic and triterpene compounds. The species has distinct morphotypes of white and pink inflorescence. Phenolic and triterpenic profiles were determined, and individual compounds were quantified in inflorescence, leaf, and stem samples of two morphotypes tested. The antioxidant activity of plant extracts was evaluated by free radical scavenging (ABTS) and ferric-reducing antioxidant power (FRAP) assays. Caffeoylquinic acids predominated in all parts of the plant tested. Chlorogenic acid and 3,5-dicaffeoylquinic acid were the principal compounds in the phenolic profile. Betulin, betulinic acid, and α-amyrin were the prevailing triterpenic components in the triterpenic profiles of Achillea millefolium morphotypes. The predominant flavonoids in inflorescences were flavones, while in leaves, flavonols were the organ-specific compounds. The quantitative differences were observed between plant parts of morphotypes. Leaves consistently displayed the highest amounts of identified compounds and have been testified as the main source of antioxidant activity. Overall, white inflorescences accumulated a higher total amount of compounds compared to pink ones. The observed differences between morphotypes derived from the same population reflect the differences in specialised metabolites and their chemotypes. This study addresses gaps in knowledge, particularly in phenolic and triterpenic profiling of coloured inflorescence morphotypes, enhancing our understanding of chemotypes and morphotypes within the species.

Ursolic acid alleviates meiotic abnormalities induced by 3-nitropropionic acid in mouse oocytes

3-nitropropionic acid (3-NPA), a toxic metabolite produced by mold, is mainly found in moldy sugarcane. 3-NPA inhibits the activity of succinate dehydrogenase that can induce oxidative stress injury in cells, reduce ATP production and induce oxidative stress in mouse ovaries to cause reproductive disorders. Ursolic acid (UA) has a variety of biological activities and is a pentacyclic triterpene compound found in many plants. This experiment aimed to investigate the cytotoxicity of 3-NPA during mouse oocyte in vitro maturation and the protective effects of UA on oocytes challenged with 3-NPA. The results showed that UA could alleviate 3-NPA-induced oocyte meiotic maturation failure. Specifically, 3-NPA induced a decrease in the first polar body extrusion rate of oocytes, abnormal distribution of cortical granules, and an increase in the proportion of spindle abnormalities. In addition, 3-NPA caused mitochondrial dysfunction and induced oxidative stress, including decreases in the GSH, mitochondrial membrane potential and ATP levels, and increases in the ROS levels, and these effects led to apoptosis and autophagy. The addition of UA could significantly improve the adverse effects caused by 3-NPA. In general, our data show that 3-NPA affects the normal development of oocytes during the in vitro culture, and the addition of UA can effectively repair the damage caused by 3-NPA to oocytes.

Antihyperglycemic and antihyperlipidemic effects of fruit extract of Hodgsonia heteroclita (Roxb.) Hook. f. & Thomson in diabetic mice

Ethnopharmacological relevanceHodgsonia heteroclita has been known as an important traditionally consumed medicinal plant of North-East India known to have antidiabetic properties. This study aims to investigate the effects of the ethanolic fruit extract of Hodgsonia heteroclita against hyperglycemia and hyperlipidemia by using streptozotocin (STZ) treated diabetic mice. Materials and methodsThe fruits of H. heteroclita were collected from the various parts of Kokrajhar district, Assam India (Geographic coordinates: 26°24′3.85″ N 90°16′22.30″ E). Basic morphological evaluations were carried out by the Botanical Survey of India, Eastern circle, Shillong, who also certified and identified the plant. Hexane, chloroform, and ethanolic extracts of the fruit of H. heteroclita were investigated for α-amylase inhibition assay as a rapid screening tool for examining anti-diabetic activity. The efficacy of ethanolic extract at a dose of 100, 200, and 300 mg/kg body weight was tested for 21 days in STZ-induced diabetic mice. The body weight, fasting plasma glucose and serum lipids, and hepatic glycogen levels were measured in experimental animals to examine the antihyperglycemic and antihyperlipidemic efficacy of the extract. Both HPTLC and LC-MS analysis was performed to examine the phyotochemicals present in the ethanolic extract of H. heteroclita. ResultsIt has been observed that treatment with the ethanolic extract dose-dependently reduced the plasma glucose levels, total cholesterol, low density lipoprotein-cholesterol, very low-density lipoprotein-cholesterol, triglyceride, and increased the body weight, liver glycogens and high-density lipoprotein-cholesterol in STZ treated diabetic mice. HPTLC demonstrated the presence of triterpene compounds and LC-MS analysis revealed the presence Cucurbitacin I, Cucurbitacin E, and Kuguacin G as the triterpene phytoconstituents. ConclusionThe present study demonstrated that ethanolic fruit extract of H. heteroclita improved both glycemic and lipid parameters in mice model of diabetes.

A Review of Recent Progresses on Olive Oil Chemical Profiling, Extraction Technology, Shelf-life, and Quality Control.

Olive oil (OO) is widely recognized as a main component in the Mediterranean diet owing to its unique chemical composition and associated health-promoting properties. This review aimed at providing readers with recent results on OO physicochemical profiling, extraction technology, and quality parameters specified by regulations to ensure authentic products for consumers. Recent research progress on OO adulteration were outlined through a bibliometric analysis mapping using Vosviewer software. As revealed by bibliometric analysis, richness in terms of fatty acids, pigments, polar phenolic compounds, tocopherols, squalene, sterols, and triterpenic compounds justify OO health-promoting properties and increasing demand on its global consumption. OO storage is a critical post-processing operation that must be optimized to avoid oxidation. Owing to its great commercial value on markets, OO is a target to adulteration with other vegetable oils. In this context, different chemometric tools were developed to deal with this problem. To conclude, increasing demand and consumption of OO on the global market is justified by its unique composition. Challenges such as oxidation and adulteration stand out as the main issues affecting the OO market.

СОВРЕМЕННЫЕ МИКРОБИОЛОГИЧЕСКИЕ ПОДХОДЫ К ПОЛУЧЕНИЮ ШТАММА ХЛЕБОПЕКАРНЫХ ДРОЖЖЕЙ, ПЕРСПЕКТИВНОГО ДЛЯ СОЗДАНИЯ ОБОГАЩЕННЫХ ПИЩЕВЫХ ИНГРЕДИЕНТОВ

The aim of the study is to use modern microbiological approaches to obtain a new strain of baker's yeast. The objects of the study were strains of baker's yeast from the Laboratory of Baker's Yeast Biotechnology of the Institute of Food Biotechnology. Selection and screening of the yeast strain were carried out by clonal plating of the original strain cells on agar media with glucose-asparagine medium (8 % DM) and with malt wort (12 and 18 % DM). The content of crude protein in the yeast biomass was determined by the Kjeldahl method on an automatic BEGER unit (Slovenia). Biomass accumulation was determined by the gravimetric method after cultivation, separating the solid and liquid fractions by centrifugation. Maltase, zymase and proteolytic activities were determined according to known methods. Ergosterol content – spectrophotometric method based on extraction with ethanol and sulfuric acid with triterpene compounds, at a wavelength of λ = 328 nm. The biomass (solid fraction) was separated from the filtrate by centrifugation in a laboratory centrifuge OPM-16 for 15 min at a rotor speed of 6000 rpm. Comparative studies were conducted to select the most productive strain of baker's yeast in terms of biochemical parameters. Comparative characteristics of yeast strains allowed us to select the most promising one – Saccharomyces cerevisiae Y-581, characterized by the ability to a higher level of protein synthesis, maltase, zymase activities, as well as ergosterol and osmosensitivity indicators. A two-stage selection and screening for the above indicators were carried out with the selected strain. As a result of microbiological approaches relative to the original strain S. cerevisiae Y-581, a population of Saccharomyces cerevisiae 581-GA-21c was isolated, characterized by a higher biosynthetic capacity not only in relation to ergosterol and protein, but also to the synthesis of enzymes, especially proteolytic ones. The isolated strain had a higher permeability of the cell membrane, as evidenced by its osmosensitivity indicators. The new strain also had distinctive features in morphological characteristics. This strain will be used in the field of obtaining enriched ingre¬dients for the development of new types of food products.

РАЗРАБОТКА СОСТАВА И ОЦЕНКА КАЧЕСТВА КОМБИНИРОВАННОГО СРЕДСТВА ДЛЯ ПОЛОСТИ РТА

Inflammatory diseases of the oral cavity belong to the category of widespread pathologies and are characterized by a diverse etiology. For their treatment and prevention, herbal remedies that have the properties of a complex effect on the causes and nature of the development of the inflammatory process are quite often and quite reasonably used. Jujube leaves seem to be a promising source of biologically active substances (BAS) for inclusion in anti-inflammatory drugs for the oral cavity due to their significant content of flavonoids, phenolcarboxylic acids, triterpene compounds and other groups of BAS, which individually and in combination determine the target activity. In addition, according to the literature, compounds that cause an anesthetic effect in the oral cavity were found in the leaves of jujube. Free radical oxidation and subsequent disruption of the integrity of cell membranes play a significant role in the pathogenesis of oral diseases. In this regard, a promising direction in the comprehensive prevention and treatment of oral diseases is the use of antioxidant drugs, among which ethyl methylhydroxypyridine succinate (EMHPS) is quite popular in this regard. EMGPS inhibits the oxidation of biological membranes, increases the activity of antioxidant enzymes, and also participates in the regulation of metabolic activity of cells. It seemed appropriate to develop a composition and evaluate the quality of an oral product based on a complex of biologically active substances from jujube leaves and EMGPS with a predicted complex anti-inflammatory and antioxidant effect. Determination of commodity indicators of jujube leaves, dry residue, alcohol content in the alcohol extract and pH of the oral product was carried out using pharmacopoeial methods. pH was measured using a Mettler Toledo pH meter. An alcoholic extract from jujube leaves in the form of a tincture was obtained by fractional maceration using 40% ethyl alcohol, which selectively extracts flavonoids from this raw material. The quantitative content of flavonoids was determined by differential spectrophotometry using a Shimadzu UV-1800 spectrophotometer. Quantitative analysis of EMGPS was carried out titrimetrically using the non-aqueous titration method. It has been established that the developed oral product containing tincture of jujube leaves and EMGPS is characterized by satisfactory quality indicators. The proposed methods for the quantitative determination of active substances make it possible to statistically reliably control their content in the composition.