A novel strategy by combining foam fractionation with high-speed countercurrent chromatography for the rapid and efficient isolation of antioxidants and cytostatics from Camellia oleifera cake.

Camellia oleifera cake is a by-product, which is rich in functional chemical components. However, it is typically used as animal feed with no commercial value. The purpose of this study was to isolate and identify compounds from Camellia oleifera cake using a combination of foam fractionation and high-speed countercurrent chromatography (HSCCC) and to investigate their biological activities. Foam fractionation with enhanced drainage through a hollow regular decahedron (HRD) was first established for simultaneously enriching flavonoid glycosides and saponins for further separation of target compounds. Under suitable operating conditions, the introduction of HRD resulted in a threefold increase in enrichment ratio with no negative effect on recovery. A novel elution-extrusion countercurrent chromatography (EECCC) coupled with the consecutive injection mode was established for the successful simultaneous isolation of flavonoid glycosides and saponins. As a result, 38.7 mg of kaemferol-3-O-[2-O-D-glucopyranosyl-6-O-α-L-rhamnopyranosyl]-ß-D-glucopyranoside (purity of 98.17%, FI), 70.8 mg of kaemferol-3-O-[2-O-ß-D-xylopyranosyl-6-O-α-L-rhamnopyranosyl]-ß-D-glucopyranoside (purity of 97.52%, FII), and 560 mg of an oleanane-type saponin (purity of 92.32%, FIII) were separated from the sample (900 mg). The present study clearly showed that FI and II were natural antioxidants (IC50 < 35 µg/mL) without hemolytic effect. FIII displayed the effect of inhibiting Hela cell proliferation (IC50 < 30 µg/mL). Further erythrocyte experiments showed that this correlated with the extremely strong hemolytic effect of FIII. Overall, this study offers a potential strategy for efficient and green isolation of natural products, and is beneficial to further expanding the application of by-products (Camellia oleifera cake) in food, cosmetics, and pharmacy.

Exploring the in vitro anti-inflammatory activity of gross saponins of Tribulus terrestris L. fruit by using liquid chromatography-mass spectrometry-based cell metabolomics approach.

Our previous studies confirmed the efficacy of gross saponins of Tribulus terrestris L. fruit in treating cerebral ischemia. This study aimed to investigate the related mechanisms in vitro. The lipopolysaccharide-induced BV2 cells model was constructed and treated with gross saponins at different concentrations to explore its anti-inflammatory activity. The cell metabolite changes were tracked by liquid chromatography-mass spectrometry (LC-MS)-based metabolomics, and the metabolic biomarkers and related metabolic pathways were analyzed. Molecular biochemistry analysis was further used to verify the relevant inflammatory pathways. The results showed that the saponins reduced nitric oxide release and the secretion of tumor necrosis factor-alpha, interleukin-1ß, and interleukin-6 from lipopolysaccharide-induced BV2 cells. Metabolic perturbations occurred in lipopolysaccharide-treated BV2 cells, which could be reversed by drug treatment via mainly regulating glycerophospholipid metabolism, tryptophan metabolism, purine metabolism pathways, etc. The western blot analysis demonstrated that saponin could suppress the activation of the inflammatory-related signaling pathway. The present study explored the in vitro anti-inflammatory mechanism of gross saponins of Tribulus terrestris L. fruit using an LC-MS-based cell metabolomics approach, which confirms the great potential of LC-MS for drug efficacy evaluation and can be applied in other herbal medicine-related analyses.

Effects of topping on rhizome, and analysis of chemical composition, antioxidant activity and α-amylase and α-glucosidase inhibition of the aerial parts in Polygonatum cyrtonema.

Polygonatum cyrtonema is a perennial plant, and it has long been used in traditional Chinese medicine for food and medicine. The medicinal part of P.cyrtonema is the rhizome; however, the aerial part has not been studied. To understand the effect of the topping of aerial parts on the yield and chemical components of rhizomes, as well as the chemical constituents, antioxidant, and in vitro hypoglycemic activities of the aerial stem, leave, and flower parts of P.cyrtonema, the present study was conducted. The results showed that compared to the control (CK) treatment, the topping of the aerial part increased rhizome weight gain coefficient (3.43) and the total saponin content (37.60 mg/g) significantly (P<0.01) than the CK treatment. The contents of total phenols and total flavonoids in PCL and PCF were significantly (P<0.01) higher than those in rhizomes; however, the polysaccharide content (10.47%) in PCR (whole rhizome) was higher than that in PCS (3.65%), PCL (5.99%), and PCF (4.76%) content. The protein and amino acid contents in PCS, PCL, and PCF were higher than those in rhizomes. The protein and amino acid contents in PCS, PCL, and PCF were higher than those in rhizomes. PCS, PCL, and PCF showed strong antioxidant activity (DPPH, ·OH, ABTS, and FRAP), which were better than traditional medicinal parts (the rhizome).In vitro hypoglycemic results showed that PCS, PCL, and PCF had certain inhibitory activities on α-amylase and α-glucosidase (66.25% and 52.81%), which were close to the hypoglycemic activity of rhizomes (67.96% and 52.22%). The leaf extracts also showed better inhibitory activity. To sum up, the topping measures can improve yield and total saponin content of the rhizomes from P.cyrtonema, which can be applied to improve production. The stems, leaves, and flowers had a much stronger antioxidant and hypoglycemic activities and higher the total polyphenols, flavonoids, proteins, and amino acid content. Therefore, stems, leaves, and flowers of Polygonatum can be fully developed according to different needs. they are typically used in animal feed, food storage and cosmetics.

[New steroidal saponins from aerial parts of Paris polyphylla var. chinensis].

The shortage of Paridis Rhizoma promotes comprehensive utilization and development research of waste aerial parts of the original plant. The chemical compositions of the aerial parts of Paris polyphylla var. chinensis were clarified based on the ultrahigh performance liquid chromatography tandem quadrupoles time of flight mass spectrometry(UPLC-QTOF-MS/MS) in the previous investigation, and a series of flavonoids and steroidal saponins were isolated. The present study continued the isolation and structure identification of the new potential compounds discovered based on UPLC-QTOF-MS/MS. By using silica gel, ODS, flash rapid preparation, and other column chromatography techniques, combined with prepared high performance liquid chromatography, five compounds were isolated from the 75% ethanol extract of the aerial parts of P. polyphylla var. chinensis, and their structures were identified by spectral data combined with chemical transformations, respectively, as(23S,25R)-23,27-dihydroxy-diosgenin-3-O-α-L-rhamnopyranosyl-(1→2)-[ß-D-glucopyranosyl-(1→3)]-ß-D-glucopyranoside(1),(25R)-26-O-ß-D-glucopyranosyl-furost-5-en-3ß,22α,26-triol-3-O-α-L-rhamnopyranosyl-(1→2)-[ß-D-glucopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→4)]-ß-D-glucopyranoside(2),(25R)-27-O-ß-D-glucopyranosyl-5-en-3ß,27-dihydroxyspirost-3-O-α-L-rhamnopyranosyl-(1→2)-[ß-D-glucopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→4)]-ß-D-glucopyranoside(3),(25R)-27-O-ß-D-glucopyranosyl-5-en-3ß,27-dihydroxyspirost-3-O-α-L-rhamnopyranosyl-(1→2)-[ß-D-glucopyranosyl-(1→3)]-ß-D-glucopyranoside(4), and aculeatiside A(5). Among them, compounds 1-4 were new ones, and compound 5 was isolated from P. polyphylla var. chinensis for the first time.

Oriental traditional herbal Medicine--Puerariae Flos: A systematic review.

ETHNOPHARMACOLOGICAL RELEVANCE: Pueraria Flos (PF), a traditional herbal medicine, is botanically from the dried flowers of Pueraria lobate (Willd.) Ohwi. (Chinese: ) or Pueraria thomsonii Benth. (Chinese: ). It has a long history of thousands of years in China for awakening the spleen, clearing the lungs, relieving alcohol. AIM OF THE REVIEW: This review aims to report the up-to-date research progress in ethnopharmacology, phytochemistry, pharmacology and toxicology, metabolism and therapeutic application of PF, so as to provide a strong basis for future clinical treatment and scientific research. MATERIALS AND METHODS: Relevant information on PF was collected from scientific literature databases including PubMed, CNKI and other literature sources (Ph.D. and M.Sc. dissertations and Chinese herbal classic books) by using the keyword "Puerariae". RESULTS: Briefly, phytochemical research report has isolated 39 flavonoids, 19 saponins and 25 volatile oils from PF. Flavonoids and saponins are the most important bioactive compounds, and most of the quality control studies focus on these two types of compounds. Modern pharmacological studies have revealed their significant biological activities in relieving alcoholism, hepatoprotective, anti-tumor, anti-inflammatory, and anti-oxidation, which provides theoretical support for the traditional use. CONCLUSIONS: Comprehensive analysis showed that pharmacological activity of most purified compounds from PF had not been reported. Kakkalide, tectoridin and their deglycosylated metabolites (irisolidone and tectorigenin) has been focused on excessively due to their higher content and better activities. This leads to low development and resources waste. Interestingly, PF made a breakthrough in the field of food. Many kinds of fat-lowering foods such as PILLBOX Onaka have been popular in Japan market, which received extensive attention. Therefore, we suggest that future research can be paid attention on the development of the plant's function in the field of food and medicine, as well as the transformation from experimental to clinical.

[Comparison of chemical compositions of different parts of Xanthoceras sorbifolium seeds based on UHPLC-Q-Orbitrap HRMS].

Xanthoceras sorbifolium seeds have a wide range of applications in the food and pharmaceutical industries. To compare and analyze the chemical compositions of different parts of X. sorbifolium seeds and explore the potential value and research prospects of non-medicinal parts, this study used ultra-high-performance liquid chromatography quadrupole Orbitrap high-resolution mass spectrometry(UHPLC-Q-Orbitrap HRMS) to detect the chemical composition of various parts of the seeds. A total of 82 components were preliminary identified from X. sorbifolium seeds, including 5 amino acids, 4 polyphenols, 3 phenylpropionic acids, 7 organic acids, 15 flavonoids, 6 glycosides, and 23 saponins. Mass spectrometry molecular networking(MN) analysis was conducted on the results from different parts of the seeds, revealing significant differences in the components of the seed kernel, seed coat, and seed shell. The saponins and flavonoids in the seed kernel were superior in terms of variety and content to those in the seed coat and shell. Based on the chromatographic peaks of different parts from multiple batches of samples, multivariate statistical analysis was carried out. Four differential components were determined using HPLC, and the average content of these components in the seed kernel, seed coat, and seed shell were as follows: 0.183 6, 0.887 4, and 1.440 1 mg·g~(-1) for fraxin; 0.035 8, 0.124 1, and 0.044 5 mg·g~(-1) for catechin; 0.032 9, 0.072 0, and 0.221 5 mg·g~(-1) for fraxetin; 0.435 9, 2.114 7, and 0.259 7 mg·g~(-1) for epicatechin. The results showed that catechin and fraxetin had relatively low content in all parts, while fraxin had higher content in the seed coat and seed shell, and epicatechin had higher content in the seed kernel and seed coat. Therefore, the seed coat and seed shell possess certain development value. This study provides rapid analysis and comparison of the chemical compositions of different parts of X. sorbifolium seeds, which offers an experimental basis for the research and clinical application of medicinal substances in X. sorbifolium seeds.

Advances in the Bioactivities of Phytochemical Saponins in the Prevention and Treatment of Atherosclerosis.

Atherosclerosis (AS) is a chronic inflammatory disease characterized by hardening and narrowing of arteries. AS leads to a number of arteriosclerotic vascular diseases including cardiovascular diseases, cerebrovascular disease and peripheral artery disease, which pose a big threat to human health. Phytochemicals are a variety of intermediate or terminal low molecular weight secondary metabolites produced during plant energy metabolism. Phytochemicals from plant foods (vegetables, fruits, whole grains) and traditional herb plants have been shown to exhibit multiple bioactivities which are beneficial for prevention and treatment against AS. Many types of phytochemicals including polyphenols, saponins, carotenoids, terpenoids, organic sulfur compounds, phytoestrogens, phytic acids and plant sterols have already been identified, among which saponins are a family of glycosidic compounds consisting of a hydrophobic aglycone (sapogenin) linked to hydrophilic sugar moieties. In recent years, studies have shown that saponins exhibit a number of biological activities such as anti-inflammation, anti-oxidation, cholesterol-lowering, immunomodulation, anti-platelet aggregation, etc., which are helpful in the prevention and treatment of AS. This review aims to summarize the recent advances in the anti-atherosclerotic bioactivities of saponins such as ginsenoside, soyasaponin, astra-galoside, glycyrrhizin, gypenoside, dioscin, saikosaponin, etc.

Comparative transcriptome analysis reveals key genes for polyphyllin difference in five Paris species.

Paris species accumulate a large amount of steroidal saponins, which have numerous pharmacological activities and have become an essential component in many patented drugs. However, only two among all Paris species. Paris are identified as official sources due to high level of bioactive compounds. To clarify the composition of steroidal saponins and the molecular basis behind the differences between species, we investigated transcriptome and metabolic profiles of leaves and rhizomes in Paris polyphylla var. chinensis (PPC), Paris polyphylla var. yunnanensis (PPY), Paris polyphylla var. stenophylla (PPS), Paris fargesii (PF), and Paris mairei (PM). Phytochemical results displayed that the accumulation of steroidal saponins was tissue- and species-specific. PF and PPS contained more steroidal saponins in leaves than rhizomes, while PPY accumulated more steroidal saponins in rhizomes than leaves. PPC and PM contained similar amounts of steroidal saponins in leaves and rhizomes. Transcriptome analysis illustrated that most differentially expressed genes related to the biosynthesis of steroidal saponins were abundantly expressed in rhizomes than leaves. Meanwhile, more biosynthetic genes had significant correlations with steroidal saponins in rhizomes than in leaves. The result of CCA indicated that ACAT, DXS, DWF1, and CYP90 constrained 97.35% of the variance in bioactive compounds in leaves, whereas CYP72, UGT73, ACAT, and GPPS constrained 98.61% of the variance in phytochemicals in rhizomes. This study provided critical information for enhancing the production of steroidal saponins by biotechnological approaches and methodologies.

Anticancer effect of buddlejasaponin IV and buddlejasaponin IVa from Clinopodium umbrosum on oral cancer cells (HN-5).

PURPOSE: Due to the existence of bioactive compounds with different biological activity in the genus Clinopodium; C. umbrosum was selected to evaluate its cell toxicity. METHODS: C. umbrosum aerial parts were solvent extracted and extracts were fractionated via various chromatographic techniques, so as to obtain two pure saponins, buddlejasaponin IVa and buddlejasaponin IV. The cytotoxicity activity of the extracts and the two pure compounds on oral cancer cells (HN-5) and human umbilical vein endothelial cells (HUVECs) were investigated by 3-(4,5-Dimethylthiazol-2-Yl)-2,5-Diphenyltetrazolium Bromide (MTT) method. To evaluate the effect on apoptosis induction, HN-5 cells were treated for 24 h and studied by FITC Annexin V/PI staining using flow cytometry. Subsequently, the apoptosis pathway was studied through real-time RT PCR. Besides, the scratch test was performed to study the cell migration. RESULTS: The cytotoxic activity of petroleum ether, chloroform and methanol extracts on HN-5 oral cancer cells after 24 h of treatment was calculated with IC50 values of >250, >167 and 239.5 µg/mL, respectively. The cytotoxic findings for buddlejasaponin IVa and buddlejasaponin IV showed that buddlejasaponin IV possessed superior cytotoxicity whilst both compounds showed their cytotoxicity through the apoptotic pathway with increasing Bax/Bcl2 ratio and the level of caspase 9. Also, HN-5 cells migration was reduced with two saponin compounds. CONCLUSION: C. umbrosum possessed significant cytotoxicity on HN-5 cells and the mechanism of cytotoxicity for its two major compounds, buddlejasaponin IVa and buddlejasaponin IV, was identified as the mitochondrial pathway of apoptosis reducing the invasive potential of HN-5 cells.

[Research progress of steroidal saponins in Paris polyphylla var. yunnanensis and their microbial transformation].

Steroidal saponins, important natural organic compounds in Paris polyphylla var. yunnanensis, have good biological activity. Structural modification of steroidal saponins by microbial transformation could produce a large number of products with novel structures and excellent bioactivity, which can provide functional compounds for the research and development of steroidal drugs. This study summarized the research progress in steroidal saponins and their microbial transformation in P. polyphylla var. yunnanensis. P. polyphylla var. yunnanensis contains 112 steroidal saponins, 8 of which are used as substrates in 35 transformation reactions by 25 microbial species, with the highest transformation rate of 95%. Diosgenin is the most frequently used substrate. Furthermore, the strains, culture medium, reaction conditions, transformation rate, transformation reaction characteristics, and biological activities of the transformed products were summarized. This review may provide reference for the further research on microbial transformation of steroidal saponins in P. polyphylla var. yunnanensis.

[Two new steroidal alkaloids from ripe berries of Solanum nigrum].

Two previously undescribed steroidal alkaloids, compounds 1-2, along with two known ones(3-4), were isolated from the 80% ethanol extract of ripe berries of Solanum nigrum by chromatographic methods, including silica gel, ODS, and HPLC. Based on spectroscopic and chemical evidence, including IR, NMR, and HR-ESI-MS data, the structures of the isolated compounds were identified as 12ß,27-dihydroxy solasodine-3-O-ß-D-glucopyranoside(1), 27-hydroxy solasodine-3-O-ß-D-glucopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)]-ß-D-glucopyranoside(2), solalyraine A(3), and 12ß,27-dihydroxy solasodine(4). Compounds 1-2 were tested for their potential effects against the proliferation of A549 cells, which revealed that compounds 1-2 had weak cytotoxic activity.

Metabolic profiling of soyasaponin Bb in rat plasma, urine, bile, and feces after intragastric administration.

Soyasaponin Bb is one of the bioactive oleanolic acid-type triterpenoid saponins mainly isolated from soybean. It possesses significant antithrombosis, hypolipidemic, anticancer, and antioxidant activities. However, the metabolic profiles of soyasaponin Bb are still unknown. The present study investigated the metabolites of soyasaponin Bb in plasma, bile, urine, and feces samples after intragastric administration using ultra-performance liquid chromatography coupled with quadrupole-time-of-flight-mass spectrometry, and its possible metabolic pathways were subsequently proposed. Using the metabolite profiling strategy, 11 metabolites were first identified from urine, plasma, bile, and feces of rats after intragastric administration of soyasaponin Bb. Hydroxylation and hydrolysis were the major metabolic pathways of soyasaponin Bb in rat. The results expand our knowledge of the metabolism of soyasaponin Bb, which could provide valuable information for better comprehension of future pharmacological research.

Differentiation of three Asparagus species by UHPLC-MS/MS based molecular networking identification and chemical profile analysis.

Asparagi Radix (AR), a traditional Chinese medicine, is the dried roots of Asparagus cochinchinensis (Lour.) Merr. Modern pharmacological studies have shown that AR has various excellent bioactivities, such as antioxidative, antitumor, antibacterial, anti-inflammatory, and hypoglycemic effects. However, the quality control method of AR is incomplete and there are various AR adulterants in markets due to their similar morphological characters. Here, holistic and practical quality evaluation methods were developed to chemically distinguish three common Asparagus species in markets, including Asparagus cochinchinensis (Lour.) Merr., Asparagus officinalis L., and Asparagus lycopodineus (Baker) F.T.Wang & Tang. The chemical constituents of three species were rapidly tentatively annotated using a combination of ultra-high pressure liquid chromatography-linear ion trap-orbitrap high resolution mass spectrometry (UHPLC-LTQ-Orbitrap-MS) and molecular networking (MN). Fifty-six steroidal saponins were annotated, including common and characteristic chemical constituents of the three Asparagus species. Besides, to establish holistic and practical methods to differentiate three Asparagus species, an HPLC-ELSD (evaporative light scattering detector) was applied for fingerprint analysis and content determination of the sum of protoneodioscin and protodioscin of twenty samples. Each Asparagus species showed characteristic chemical profile and AR showed much higher level of the sum of protoneodioscin and protodioscin than that in the others. The above analyses showed that the three Asparagus species mainly contain steroidal saponins and the developed HPLC-ELSD profile of saponin can be used to differentiate them. In conclusion, this study reveals the different chemical constituents of three Asparagus species and provides relatively feasible quality evaluation methods for them which are essential for the rational utilization of these Asparagus species.

Effect of biotic stress on the presence of secondary metabolites in field pea grains.

BACKGROUND: The presence of secondary metabolites responsible for off-flavours in peas may influence consumers' acceptance. These undesirable compounds may increase due to biotic stress or cultivar. Therefore, grains from two pea (Pisum sativum L.) cultivars (Crécerelle and Firenza) exposed to biotic stress were studied in terms of protein content, electrophoretic polypeptide profile, lipoxygenase activity, saponin content and volatile compounds. RESULTS: No differences were observed in the electrophoretic polypeptide profile of pea samples across cultivar or biotic stress. The cultivar noticeably affected the volatile compounds and lipoxygenase activity. The biotic stress significantly increased the saponin content. CONCLUSION: The cultivar showed more noticeable impact on the presence of off-flavour compounds than the biotic stress. The development of pea protein ingredients needs the thorough choice of raw materials in terms of cultivar and control of biotic stress in order to ensure acceptance by consumers. © 2022 Society of Chemical Industry.

[Spatial distribution characteristics of metabolities in rhizome of Paris polyphylla var. yunnanensis: based on MALDI-MSI].

In this study, a method was established for in-situ visualization of metabolite distribution in the rhizome of Paris polyphylla var. yunnanensis. To be specific, through matrix-assisted laser desorption/ionization-mass spectrometry imaging(MALDI-MSI), the spatial locations of steroidal saponins, amino acids, organic acids, phytosterols, phytoecdysones, nucleosides, and esters in rhizome of the medicinal plant were directly analyzed, and six unknown compounds with differential distribution in rhizome tissues were identified. The specific procedure is as follows: preparation of rhizome tissue section, matrix screening and optimization, and MALDI-MSI analysis. The results showed that the steroidal saponins were mainly distributed in the central, amino acids in epidermis and cortex, low-molecular-weight organic acids in central epidermis, phytosterols in the epidermis and lateral cortex, the phytoecdysones in epidermis and cortex, nucleosides(uneven distribution) in epidermis and cortex, growth hormones around the epidermis and cortex, particularly outside the cortex, and esters in cortex with unobvious difference among different tissues. In this study, the spatial distribution of meta-bolites in the rhizome of P. polyphylla var. yunnanensis was characterized for the first time. The result can serve as a reference for identifying and extracting endogenous metabolites of P. polyphylla var. yunnanensis, exploring the synthesis and metabolism mechanisms of the metabolites, and evaluating the quality of medicinal materials.

Bacopa monnieri: historical aspects to promising pharmacological actions for the treatment on central nervous system diseases / Bacopa monnieri: aspectos históricos de las acciones farmacológicas prometedoras para el tratamiento de enfermedades del sistema nervioso central

Bacopa monnieri(L.) Wettst. (Plantaginaceae), also known as Brahmi, has been used to improve cognitive processes and intellectual functions that are related to the preservation of memory. The objective of this research is to review the ethnobotanical applications, phytochemical composition, toxicity and activity of B. monnieri in the central nervous system. It reviewed articles on B. monnieri using Google Scholar, SciELO, Science Direct, Lilacs, Medline, and PubMed. Saponins are the main compounds in extracts of B. monnieri. Pharmacological studies showed that B. monnieri improves learning and memory and presents biological effects against Alzheimer's disease, Parkinson's disease, epilepsy, and schizophrenia. No preclinical acute toxicity was reported. However, gastrointestinal side effects were reported in some healthy elderly individuals. Most studies with B. monnieri have been preclinical evaluations of cellular mechanisms in the central nervous system and further translational clinical research needs to be performed to evaluate the safety and efficacy of the plant.

Bacopa monnieri (L.) Wettst. (Plantaginaceae), también conocida como Brahmi, se ha utilizado para mejorar los procesos cognitivos y las funciones intelectuales que están relacionadas con la preservación de la memoria. El objetivo de esta investigación es revisar las aplicaciones etnobotánicas, composición fitoquímica, toxicidad y actividad de B. monnieri en el sistema nervioso central. Se revisaron artículos sobre B. monnieri utilizando Google Scholar, SciELO, Science Direct, Lilacs, Medline y PubMed. Las saponinas son los principales compuestos de los extractos de B. monnieri. Los estudios farmacológicos mostraron que B. monnieri mejora el aprendizaje y la memoria y presenta efectos biológicos contra la enfermedad de Alzheimer, la enfermedad de Parkinson, la epilepsia y la esquizofrenia. No se informó toxicidad aguda preclínica. Sin embargo, se informaron efectos secundarios gastrointestinales en algunos ancianos sanos. La mayoría de los estudios con B. monnieri han sido evaluaciones preclínicas de los mecanismos celulares en el sistema nervioso central y es necesario realizar más investigaciones clínicas traslacionales para evaluar la seguridad y eficacia de la planta.

Antiglycation and antioxidant activities of the crude extract and saponin fraction of Tribulus terrestris before and after microcapsule release.

OBJECTIVE: The present study investigated antiglycation and antioxidant activities of crude dry extract and saponin fraction of Tribulus terrestris. It also developed a method of microencapsulation and evaluated antiglycation and antioxidant activities of crude dry extract and saponin fraction before and after microcapsule release. METHODS: Antiglycation activity was determined by relative electrophoretic mobility (REM), free amino groups and inhibition of advanced glycation end-product (AGE) formation. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric ion-reducing antioxidant power (FRAP), nitric oxide (NO) and thiobarbituric acid reactive species (TBARS) tests. Microcapsules were prepared using maltodextrin as wall material and freeze-drying as encapsulation technique. Morphological characterization of microcapsules was evaluated by scanning electron microscopy, and encapsulation efficiency and microcapsule release were determined by total saponins released. Antiglycation and antioxidant assays were performed using crude dry extract and saponin fraction of T. terrestris before and after release. RESULTS: Saponin fraction showed an increase of 32.8% total saponins. High-performance liquid chromatography-mass spectrometry analysis showed the presence of saponins in the obtained fraction. Antiglycation evaluation by REM demonstrated that samples before and after release presented antiglycation activity similar to bovine serum albumin treated with aminoguanidine. Additionally, samples inhibited AGE formation, highlighting treatment with saponin fraction after release (89.89%). Antioxidant tests demonstrated antioxidant activity of the samples. Crude dry extract before encapsulation presented the highest activities in DPPH (92.00%) and TBARS (32.49%) assays. Saponin fraction before encapsulation in FRAP test (499 µmol Trolox equivalent per gram of dry sample) and NO test (15.13 µmol nitrite formed per gram of extract) presented the highest activities. CONCLUSION: This study presented antiglycation activity of crude dry extract and saponin fraction of T. terrestris, besides it demonstrated promising antioxidant properties. It also showed that the encapsulation method was efficient and maintained biological activity of bioactive compounds after microcapsule release. These results provide information for further studies on antidiabetic and antiaging potential, and data for new herbal medicine and food supplement formulations containing microcapsules with crude extract and/or saponin fraction of T. terrestris.

Evaluation of nutritional and medicinal potential of defatted Sapindus mukorossi seed kernel.

This work deals with the evaluation of nutritional and medicinal potential of a defatted kernel of Sapindus mukorossis seed. Defatted sapindus seed kernel is a rich source of proteins (33.4 ± 2.12%), which show balanced amino acid composition for the requirement of adults as per the World Health Organization. Protein isolate possesses 29 kDa molecular weight peptide, which shows trypsin inhibitor activity. It also showed around 31.2% reduction in amylase activity while aqueous Ethanol and ethanol extracts showed 55% and 72.83%, respectively. Aqueous ethanol and ethanol extracts were found to contain polyphenols and saponins. Polyphenol content in aqueous ethanol and ethanol extract was 4.50 ± 0.15 mg/g and 5.7 ± 0.34 mg/g ferulic acid equivalent, respectively, while 0.72 ± 0.68% and 1.2 ± 0.23% Oleonolic acid equivalent saponins, respectively. Both these extracts showed potent antioxidant activity, and the rate of DPPH scavenging activity was higher than the ferulic acid standard. The deffated seed also contains dietary fibers in which 3.8 ± 0.01% are soluble, and 2.2 ± 0.03% are insoluble fibers.

Microencapsulation of steroidal saponins from agave sap concentrate using different carriers in spray drying.

Concentrated agave sap is a product with in vivo proven hypocholesterolemic and hypoglycemic activities, as well as in vitro anticancer potential. In the present work, a factorial design was used to determine the suitable drying conditions of concentrated agave by studying the effect of inlet temperature (150 °C, 180 °C and 210 °C) and the type of carrier agent (maltodextrin, hydroxypropyl methylcellulose, guar gum and xanthan gum). The response variables for each treatment were the product recovery and microencapsulated saponins. Further characterization of concentrated agave powders was performed: solubility in water, hygroscopicity, moisture content, tap density, bulk density, Carr's index followability and morphology by scanning electron microscopy analysis. The hydroxypropyl methylcellulose proved to improve physicochemical properties and enhance product yield, using 210 °C inlet temperature and a mix of carrier agents of maltodextrin/hydroxypropyl methylcellulose/xanthan gum at 50/48.5/1.5 (w/w/w) proportion exhibited the highest saponin recovery of 53.81%. Moreover, different carrier agents in powders revealed two shapes, regular spherical shape with smooth surface and collapsed shapes. The use of polymers excipients helped to decrease the stickiness of the desired product and enhanced the powder stability and microencapsulation of the steroidal saponins.

Encapsulating Calendula arvensis (Vaill.) L. Florets: UHPLC-HRMS Insights into Bioactive Compounds Preservation and Oral Bioaccessibility.

Wild edible plants, once consumed in times of famine or for health purposes, today represent an interesting dietary supplement, aimed at enriching local dishes and/or formulating healthy nutraceutical products. In fact, the broad content of different, and diversely bioactive, specialized metabolites therein suggests new scenarios of use which, in order to be as functional as possible, must maximize the bioactivity of these compounds while preserving their chemistry. In this context, based on a recent investigation on the metabolic profile of the organs of Calendula arvensis that highlighted that florets are abundant in flavonol glycosides and triterpene saponins, the freeze-drying encapsulation of their alcoholic extract (FE) into maltodextrin (MD) was investigated. FE-MD chemical composition was evaluated using Fourier Transform InfraRed spectroscopy (FTIR), while ultra-high performance liquid chromatography coupled with high-resolution tandem mass spectrometry (UHPLC-HRMS/MS) techniques were employed to unravel FE compound preservation also during in vitro simulated digestion. The establishment of H-bonds between FE compounds and MD hydroxyl groups was in line with FE-MD biocompatibility in Caco-2 cells, while in vitro digestion mostly affected structural integrity and/or diversity. Flavonol compounds underwent deglycosylation and demethylation, while deacylation, beyond oxidation, involved triterpene saponins, which massively preserve their aglycone core.